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values | class_subclass stringclasses 511
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|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
DB00001 | Lepirudin | Lepirudin is a recombinant hirudin formed by 65 amino acids that acts as a highly specific and direct thrombin inhibitor.[L41539,L41569] Natural hirudin is an endogenous anticoagulant found in _Hirudo medicinalis_ leeches.[L41539] Lepirudin is produced in yeast cells and is identical to natural hirudin except for the a... | solid | Lepirudin is indicated for anticoagulation in adult patients with acute coronary syndromes (ACS) such as unstable angina and acute myocardial infarction without ST elevation. In patients with ACS, lepirudin is intended for use with [aspirin].[L41539] Lepirudin is also indicated for anticoagulation in patients with hepa... | Lepirudin is a recombinant hirudin that acts as a highly specific thrombin inhibitor. Its activity is measured by anti-thrombin units (ATUs) that correspond to the amount of lepirudin required to neutralize a unit of the World Health Organization α-thrombin (89/588) standard. The activity of lepirudin is 16,000 ATU/mg.... | Lepirudin is a direct thrombin inhibitor used as an anticoagulant in patients for whom heparin is contraindicated.[L41539,A3] Thrombin is a serine protease that participates in the blood-clotting cascade, and it is formed by the cleavage of pro-thrombin. Active thrombin cleaves fibrinogen and generates fibrin monomers ... | Lepirudin administered as a single intravenous bolus injection of 0.4 mg/kg in 9 healthy volunteers (male and female) resulted in a C<sub>max</sub> of 2924 ng/mL, a t<sub>max</sub> of 0.17 h and an AUC<sub>0-∞</sub> of 2500 ng•h/mL.[L41539] When 0.1, 0.15 and 0.2 mg/kg of lepirudin was administered as a single intraven... | As a polypeptide, lepirudin is expected to be metabolized by the sequential cleavage of amino acids by kidney exoproteases, which have carboxypeptidase and dipeptidase-like activity.[L41539,L41544] The C-terminal cleavage of lepirudin aminoacids (aminoacids 1 to 65) produces four metabolites with anti-thrombotic activi... | The acute toxicity of intravenous lepirudin was evaluated in mice (0.1-1000 mg/kg), rats (1-1000 mg/kg), and monkeys (1-100 mg/kg), and toxicity was not detected at the doses investigated.[L41539] The acute toxicity of lepirudin administered subcutaneously was also evaluated in mice (1-1250 mg/kg) and rats (1-500 mg/kg... | Lepirudin has an initial half-life of approximately 10 minutes, and in young healthy volunteers, it has a terminal half-time of 1.3 hours.[L41539] Lepirudin has a first-order elimination kinetic; plasma concentration increases proportionally as the lepirudin intravenous dose is increased. Elimination half-life values o... | In human plasma, the protein binding of lepirudin was approximately 3%.[L41539] | Lepirudin is mostly excreted through urine (48.3%). About 35% of lepirudin is excreted unchanged, while metabolites are found in a smaller proportion (2.5% of M1, 5.4% of M2, 3.9% of M3 and 1.6% of M4).[L41544] | The volume of distribution of lepirudin at steady state was 12.2 L in healthy young subjects (n=18, 18-60 years), 18.7 L in healthy elderly subjects (n=10, 65-80 years), 18.0 L in renally impaired subjects (n=16, creatinine clearance < 80 mL/min, and 32.1 L in heparin-induced thrombocytopenia patients (n=73).[L41539] T... | The clearance of lepirudin is proportional to the glomerular filtration rate. On average, lepirudin clearance was 164 mL/min in healthy young subjects (n=18, 18-60 years) and 25% lower in women than in men. In healthy elderly subjects (n=10, 65-80 years), clearance was 139 mL/min, about 20% lower than in younger patien... | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"withdrawn"
] | [
"B01AE",
"B01A",
"B01",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "273.19",
"description": "Refludan 50 mg vial",
"unit": "vial"
}
] | [
{
"approved": "1993-01-19",
"country": "United States",
"expires": "2010-01-19",
"number": "5180668"
}
] | [Leu1, Thr2]-63-desulfohirudin | Desulfatohirudin | Hirudin variant-1 | Lepirudin | Lepirudin recombinant | R-hirudin | 3.4.21.5 | Coagulation factor II | [
"Refludan",
"Refludan",
"Refludan",
"Refludan",
"Refludan",
"Refludan"
] | [] | [] | [
"P00734"
] | [] | [] | [] |
DB01022 | Phylloquinone | Vitamin K1, also called phylloquinone or phytonadione, is a fat soluble vitamin.[L33319,L33345] Phylloquinone is a cofactor of the enzyme γ-carboxylase, which modifies and activates precursors to coagulation factors II, VII, IX, and X.[A234264,A234195,A234259] It is indicated in the treatment of coagulation disorders d... | liquid | Oral phylloquinone is indicated to treat prothrombin deficiency caused by coumarin or indanedione derivatives; and hypoprothrombinemia secondary to antibacterial therapy, salicylates, or obstructive jaundice or biliary fistulas with concomitant bile salt administration.[L33345]
Parenteral (intravenous, intramuscular... | Phylloquinone is a vitamin K indicated in the treatment of coagulation disorders due to faulty formation of coagulation factors II, VII, IX, and X caused by deficiency or interference in the activity of vitamin K.[L33319] It has a long duration of action as vitamin K is cycled in the body,[A234259] and a wide therapeut... | Vitamin K is a cofactor of gamma-carboxylase.[A234264,A234195] Gamma carboxylase attaches carboxylic acid functional groups to glutamate, allowing precursors of factors II, VII, IX, and X to bind calcium ions.[A234259] Binding of calcium ions converts these clotting factors to their active form, which are then secreted... | A 4 µg oral dose of phylloquinone is 13% ± 9% bioavailable, with a T<sub>max</sub> of 4.7 ± 0.8 hours.[A234264] 1.5 ± 0.8 nmol is found in the plasma compartment, and 3.6 ± 3.4 nmol is found in the second compartment.[A234264]
A 10 mg intramuscular phylloquinone dose is 89.2% ± 25.4% bioavailable.[A234344] The same ... | Phylloquinone's phytyl side chain is omega hydroxylated by CYP4F2.[A137578] The side chain is then cleaved to 5 or 7 carbons long, and then glucuronidated prior to elimination.[A234104,A234109,A234114,A234119]
Vitamin Ks in general undergo a cycle of reduction to vitamin K hydroquinone by vitamin K epoxide reductase... | High doses of vitamin K1 are not associated with toxicity.[A234259] Intravenous administration has been associated with an increased risk of toxicity.[A234284] These patients should be treated with symptomatic and supportive measures.
The intravenous LD<sub>50</sub> in mice is 1170 mg/kg and the oral LD<sub>50</sub>... | Intravenous phylloquinone has an initial half life of 22 minutes, followed by a half life of 125 minutes.[A234104] | null | Intravenous phylloquinone is 36% eliminated in the feces in 5 days and 22% recovered in urine in 3 days.[A234104,A234329] | The steady state volume of distribution of phylloquinone is 20 ± 6 L in subjects who are also taking phenprocoumon therapy.[A234374] | Intravenous phylloquinone is 90% cleared in 2 hours, and 99% cleared in 8 hours.[A234104,A234329] A 10 mg intravenous dose of phylloquinone has a mean clearance of 91 ± 24 mL/min.[A234344] | Organic compounds | Lipids and lipid-like molecules | Prenol lipids | Quinone and hydroquinone lipids | [
"approved",
"investigational"
] | [
"B02BA",
"B02B",
"B02",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "2.76",
"description": "Vitamin K1 10 mg/ml",
"unit": "ml"
},
{
"cost": "4.79",
"description": "Vitamin K1 Pediatric 2 mg/ml",
"unit": "ml"
},
{
"cost": "5.95",
"description": "Mephyton 5 mg tablet",
"unit": "tablet"
},
{
"cost": "35.0",
"description... | [] | 2-Methyl-3-(3,7,11,15-tetramethyl-2-hexadecenyl)-1,4-naphthalenedione | 2-Methyl-3-[(2E)-3,7,11,15-tetramethyl-2-hexadecenyl]naphthoquinone | 2-Methyl-3-phytyl-1,4-naphthochinon | 2-Methyl-3-phytyl-1,4-naphthoquinone | 3-Phytylmenadione | alpha-Phylloquinone | Fitomenadiona | Phyllochinon | Phyllochinonum | Phylloquino... | [
"Adeks - Dps",
"Adeks Tablets",
"Adult Infuvite Multiple Vitamins",
"Adult Infuvite Multiple Vitamins",
"Adult Infuvite Multiple Vitamins",
"Adult Infuvite Multiple Vitamins",
"AquaMEPHYTON",
"AquaMEPHYTON",
"Decara K Vegicaps",
"Infuvite Adult",
"Infuvite Adult",
"Infuvite Pediatric",
"Infu... | [
"Aqua-Mephyton",
"Konakion"
] | [
"Omega-3 Rx Complete",
"M.V.I. Pediatric",
"Pro Pcos Citrus",
"Pro Hers Vanilla",
"M.V.I. Adult",
"M.V.I. Adult",
"Pediatric Infuvite Multiple Vitamins",
"Pediatric Infuvite Multiple Vitamins",
"Adult Infuvite Multiple Vitamins",
"Adult Infuvite Multiple Vitamins",
"Pediatric Infuvite Multiple V... | [
"P38435",
"P02818"
] | [
"P78329",
"Q9Y5Z9",
"Q9BQB6"
] | [] | [] |
DB01373 | Calcium | Calcium plays a vital role in the anatomy, physiology and biochemistry of organisms and of the cell, particularly in signal transduction pathways. The skeleton acts as a major mineral storage site for the element and releases Ca2+ ions into the bloodstream under controlled conditions. Circulating calcium is either in t... | solid | Calcium plays a vital role in the anatomy, physiology and biochemistry of organisms and of the cell, particularly in signal transduction pathways. It is vital in cell signaling, muscular contractions, bone health, and signalling cascades. | Calcium (Ca2+) plays a pivotal role in the physiology and biochemistry of organisms and the cell. It plays an important role in signal transduction pathways, where it acts as a second messenger, in neurotransmitter release from neurons, contraction of all muscle cell types, and fertilization. Many enzymes require calci... | Calcium plays a vital role in the anatomy, physiology and biochemistry of organisms and of the cell, particularly in signal transduction pathways. More than 500 human proteins are known to bind or transport calcium. The skeleton acts as a major mineral storage site for the element and releases Ca2+ ions into the bloo... | null | null | null | null | null | The kidney excretes 250 mmol a day in urine, and resorbs 245 mmol, leading to a net loss in the urine of 5 mmol/d. | null | null | null | null | null | null | [
"nutraceutical"
] | [
"M05BB",
"M05B",
"M05",
"M",
"A11AA",
"A11A",
"A11",
"A",
"M05BB",
"M05B",
"M05",
"M",
"A11GB",
"A11G",
"A11",
"A",
"M05BB",
"M05B",
"M05",
"M",
"M05BB",
"M05B",
"M05",
"M",
"M05BB",
"M05B",
"M05",
"M"
] | [
"Humans and other mammals"
] | [] | [] | Calcio | Calcium, elemental | Elemental calcium | Kalzium | CACH2 | CACN2 | CACNL1A1 | Calcium channel, L type, alpha-1 polypeptide, isoform 1, cardiac muscle | CCHL1A1 | Voltage-gated calcium channel subunit alpha Cav1.2 | 7.2.2.10 | ATP-dependent Ca(2+) pump PMR1 | ATPase 2C1 | Ca(2+)/Mn(2+)-ATPase 2C1 | KIAA1347 | P... | [
"24 Multivitamins + Minerals",
"50 Plus Multiple Vitamins & Minerals",
"7030 Calcium Gold",
"7030 Calcium Gold",
"7030 Calcium Premium",
"7030 Calcium Premium",
"7030 Calcium Premium",
"A D Calcium Tab",
"A-D Calcium Cap",
"A.R.T.H. Away Formula",
"A/o-26 - Caplet",
"Acti-cal/mag 2:1 + Zinc an... | [] | [
"Pure Calcium calcium",
"Oyster Shell Calcium with Vitamin D",
"O-Cal Prenatal Vitamin",
"Cavan One",
"Zingiber",
"PreNatal Vitamins Plus",
"Prenatal Vitamin No 53 Iron Fum Folic Acid Docusate CA DHA",
"Vitafol Caplet",
"Ferrous Sulfate",
"PreFol-DHA",
"Focalgin B",
"Nata Komplete",
"PreNata... | [
"Q13936",
"P98194",
"P02585",
"P63316",
"Q01082",
"P04271",
"P20810",
"P49747",
"P19801",
"Q99584",
"P05187",
"P05109",
"P06702",
"P29034",
"P00450",
"P12644",
"P08493",
"Q8TAB3",
"O75340",
"P0DP23",
"P0DP24",
"P0DP25"
] | [] | [] | [] |
DB00002 | Cetuximab | Cetuximab is a recombinant chimeric human/mouse IgG1 monoclonal antibody that competitively binds to epidermal growth factor receptor (EGFR) and competitively inhibits the binding of epidermal growth factor (EGF).[A227973] EGFR is a member of the ErbB family of receptor tyrosine kinases found in both normal and tumour ... | liquid | Cetuximab indicated for the treatment of locally or regionally advanced squamous cell carcinoma of the head and neck in combination with radiation therapy. It is indicated for treating a recurrent locoregional disease or metastatic squamous cell carcinoma of the head and neck in combination with platinum-based therapy ... | Cetuximab is an anticancer agent that works by inhibiting the growth and survival of epidermal growth factor receptor (EGFR)-expressing tumour cells with high specificity and higher affinity than epidermal growth factor (EGF) and transforming growth factor-alpha (TGF-α), which are natural ligands of EGFR.[L31418] Cetux... | The epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein and a type I receptor tyrosine kinase expressed on both normal and malignant cells. It has been investigated as a therapeutic target for anticancer treatment, as it is often upregulated in cancer types, including head and neck, colon, and recta... | After administration of a 400 mg/m<sup>2</sup> initial dose followed by a 250 mg/m<sup>2</sup> weekly dose, the steady-state levels of cetuximab was reached by the third weekly infusion with mean peak and trough concentrations across studies ranging from 168 µg/mL to 235 µg/mL and 41 µg/mL to 85 µg/mL, respectively.[L3... | Like other monoclonal antibodies, cetuximab is expected to undergo lysosomal degradation by the reticuloendothelial system and protein catabolism by a target‐mediated disposition pathway.[A40006] | The intravenous LD<sub>50</sub> is > 300 mg/kg in mice and > 200 mg/kg in rats.[L31408] There is limited information on the overdose from cetuximab.
In clinical trials, cetuximab was associated with serious and fatal infusion reactions, cardiopulmonary arrest or sudden death, and serious dermatologic toxicities. Pul... | After administration of a 400 mg/m<sup>2</sup> initial dose followed by a 250 mg/m<sup>2</sup> weekly dose, the mean half-life for cetuximab was approximately 112 hours, with a range of 63 to 230 hours.[L30448] | There is no information available. | There is limited information available. | The volume of the distribution is about 2-3 L/m<sup>2</sup> and is independent of dose.[L30448] | In patients with recurrent and/or metastatic squamous cell carcinoma of the head and neck, the estimated clearance rate was 0.103 L/h.[A228003] At doses ranging from 200 to 400 mg/m<sup>2</sup>, complete saturation of systemic clearance was observed. In a population pharmacokinetic study, female patients had a 25% low... | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"L01FE",
"L01F",
"L01",
"L"
] | [
"Humans and other mammals"
] | [] | [
{
"approved": "1999-03-02",
"country": "Canada",
"expires": "2016-03-02",
"number": "1340417"
}
] | Cetuximab | Cétuximab | Cetuximabum | 2.7.10.1 | ERBB | ERBB1 | HER1 | Proto-oncogene c-ErbB-1 | Receptor tyrosine-protein kinase erbB-1 | CD16-I | CD16B | Fc-gamma RIII | Fc-gamma RIII-beta | Fc-gamma RIIIb | FCG3 | FCGR3 | FcR-10 | FcRIII | FcRIIIb | IGFR3 | IgG Fc receptor III-1 | C1QG | CD16-II | CD16A | CD16a anti... | [
"Erbitux",
"Erbitux",
"Erbitux",
"Erbitux",
"Erbitux"
] | [] | [] | [
"P00533",
"O75015",
"P02745",
"P02746",
"P02747",
"P08637",
"P12314",
"P12318"
] | [] | [] | [] |
DB00003 | Dornase alfa | Dornase alfa is a biosynthetic form of human deoxyribunuclease I (DNase I) enzyme. It is produced in genetically modified Chinese hamster ovary (CHO) cells using recombinant DNA technology. The 260-amino acid sequence of dornase alfa is identical to the endogenous human enzyme. Dornase alfa cleaves extracellular DNA to... | liquid | Used as adjunct therapy in the treatment of cystic fibrosis. | Cystic fibrosis (CF) is a disease characterized by the retention of viscous purulent secretions in the airways. These thick secretions contribute both to reduced pulmonary function and to frequent pulmonary infection. Purulent pulmonary secretions of individuals with cystic fibrosis contain very high concentrations of ... | Dornase alfa is a biosynthetic form of human DNase I. The enzyme is involved in endonucleolytic cleavage of extracellular DNA to 5´-phosphodinucleotide and 5´-phosphooligonucleotide end products. It has no effect on intracellular DNA. Optimal activity is dependent on the presence of divalent cations such as calcium and... | Studies in rats and monkeys after inhalation of dornase alfa shows very little systemic absorption (less than 15% for rats and less than 2% for monkeys). The results were also witnessed in patients. Dornase alfa is also associated with very low accumulation with no serum concentration greater than 10ng/mL observed no m... | While no conclusive studies have yet been published, dornase alfa is expected to be metabolized by proteases in biofluids. | Adverse reactions occur at a frequency of < 1/1000 and are usually mild and transient in nature. Reported adverse effects include chest pain (pleuritic/non-cardiac), fever, dyspepsia, voice alteration (hoarseness), pharyngitis, dyspnea, laryngitis, rhinitis, decreased lung function, rash, urticaria, and conjunctivitis.... | null | null | null | In studies in rats and monkeys, the initial volume of distribution is similar to the serum volume. Concentrations in sputum decline rapidly after inhalation. | Studies in rats indicate that, following aerosol administration, the disappearance half-life of dornase alfa from the lungs is 11 hours. In humans, sputum DNase levels declined below half of those detected immediately post-administration within 2 hours but effects on sputum rheology persisted beyond 12 hours. | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"R05CB",
"R05C",
"R05",
"R"
] | [
"Humans and other mammals"
] | [
{
"cost": "3.21",
"description": "Lufyllin 200 mg tablet",
"unit": "tablet"
},
{
"cost": "3.84",
"description": "Lufyllin-gg tablet",
"unit": "tablet"
},
{
"cost": "3.99",
"description": "Lufyllin-GG 200-200 mg tablet",
"unit": "tablet"
},
{
"cost": "4.62",
"d... | [
{
"approved": "2005-02-22",
"country": "Canada",
"expires": "2015-02-28",
"number": "2184581"
},
{
"approved": "2004-10-26",
"country": "Canada",
"expires": "2013-05-28",
"number": "2137237"
}
] | Deoxyribonuclease (human clone 18-1 protein moiety) | Dornasa alfa | Dornase alfa | Dornase alfa, recombinant | Dornase alpha | Recombinant deoxyribonuclease (DNAse) | 3.1.21.1 | Deoxyribonuclease I | DNase I | DNL1 | DRNI | [
"Pulmozyme",
"Pulmozyme"
] | [
"Viscozyme"
] | [] | [
"P24855"
] | [] | [] | [] |
DB00004 | Denileukin diftitox | Denileukin diftitox is an IL2-receptor-directed cytotoxin, is a recombinant DNA-derived fusion protein composed of the amino acid sequences for diphtheria toxin fragments A and B (Met<sub>1</sub>-Thr<sub>387</sub>)-His and the sequence for human interleukin-2 (IL-2; Ala<sub>1</sub>-Thr<sub>133</sub>).[L51254] It is des... | liquid | Denileukin diftitox was previously indicated for the treatment of adult patients with persistent or recurrent cutaneous T-cell lymphoma (CTCL) whose malignant cells express the CD25 component of the IL-2 receptor.[L26381] It is also indicated for the treatment of adult patients with relapsed or refractory Stage I-III C... | Denileukin diftitox is an anticancer drug with cytocidal actions on cancer cells.[L51254] Denileukin diftitox demonstrated the ability to deplete immunosuppressive regulatory T lymphocytes (T<sub>regs</sub>) and antitumor activity through direct cytocidal action on IL-2R-expressing tumours.[L51254] | Denileukin diftitox is a fusion protein composed of truncated diphtheria toxin (DT), which is a cytocidal moiety, and the full-length sequence of interleukin-2 (IL-2), which acts as a ligand for the IL-2 receptor.[A264344] Denileukin diftitox is reported to bind to a high- or intermediate-affinity receptor.[A264344] On... | Following a single dose of denileukin diftitox 9 mcg/kg via one-hour infusion in patients with CTCL, the geometric mean (coefficient of variation [CV]%) maximum serum concentration (C<sub>max</sub>) was 94.4 ng/mL (77%) and area under the concentration over time curve (AUC<sub>0-inf</sub>) was 20700 ng x min/L (60%) on... | Denileukin diftitox is expected to be metabolized into small peptides by catabolic pathways.[L51254] | There is limited information regarding the acute toxicity (LD<sub>50</sub>) and overdose of denileukin diftitox. | The arithmetic mean (CV%) denileukin diftitox terminal half-life is 112 minutes (31%) on the first day of the first cycle.[L51254] | null | null | The geometric mean (CV%) volume of distribution of denileukin diftitox is 5.0 L (43%) on the first day of the first administration cycle.[L51254] | The geometric mean (CV%) clearance is 36.5 mL/min (73%) after the first dose of denileukin diftitox at the recommended dose level.[L51254] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L01XX",
"L01X",
"L01",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "878.4",
"description": "Ontak 150 mcg/ml vial",
"unit": "ml"
}
] | [] | DAB(SUB 389)IL2 | Denileukin | Denileukin diftitox | Interleukin-2/diptheria toxin fusion protein | N-L-METHIONYL-387-L-HISTIDINE-388-L-ALANINE-1-388-TOXIN (CORYNEBACTERIUM DIPHTHERIAE STRAIN C7) (388->2') PROTEIN WITH 2-133-INTERLEUKIN 2 (HUMAN CLONE PTIL2-21A) | N-MET-187-HIS-388-ALA-1-388-TOXIN (CORYNEBACTERIUM DIPH... | [
"Ontak"
] | [] | [] | [
"P01589",
"P14784"
] | [] | [] | [] |
DB00005 | Etanercept | Dimeric fusion protein consisting of the extracellular ligand-binding portion of the human 75 kilodalton (p75) tumor necrosis factor receptor (TNFR) linked to the Fc portion of human IgG1.[L14862,A216522] The Fc component of etanercept contains the CH2 domain, the CH3 domain and hinge region, but not the CH1 domain of ... | liquid | Etanercept is indicated for the treatment of moderately to severely active rheumatoid arthritis in adults and in chronic moderate to severe plaque psoriasis in patients 4 years of age and older.[L14862,L45523] It is also used to manage signs and symptoms of polyarticular idiopathic arthritis and Juvenile Psoriatic Arth... | Etanercept binds specifically to tumor necrosis factor (TNF) and thereby modulates biological processes that are induced or regulated by TNF.[L14862,A216522] Such processes or molecules affected include the level of adhesion molecules expressed, as well as serum levels of cytokines and matrix metalloproteinases. | There are two distinct receptors for TNF (TNFRs), a 55 kilodalton protein (p55) and a 75 kilodalton protein (p75). The biological activity of TNF is dependent upon binding to either cell surface receptor (p75 or p55).[A216522] Etanercept is a dimeric soluble form of the p75 TNF receptor that can bind to two TNF molecul... | Population pharmacokinetic modeling in adults with RA, AS, or who were healthy showed a subcutaneous bioavailability of 56.9% with a Ka of 0.0223/h.[A215352] Another model in pediatric JIA patients showed an increased Ka of 0.05/h with a high mean interindividual variability of 215%.[A215357] Cmax after a single 25 mg ... | As etanercept is a fusion protein antibody, it is assumed to be metabolized via proteinases similarly to endogenous proteins. | null | Etanercept has a mean half-life of elimination of 102 hours in RA patients.[L14862] Population models have shown a mean half-life of 68 hours in healthy adults and 70.7-94.8 hours in pediatric JIA patients.[A215657,A215357] | No significant protein binding has been identified. | null | Population pharmacokinetic modeling predicts a total Vd of 5.49 L with a peripheral compartment of 1.24 L in adults with RA and an apparent Vd with subcutaneous administration in pediatric JIA patients of 7.88 L.[A215352,A215357] | Etanercept has a mean apparent clearance of 160 mL/h in RA patients.[L14862] Population models predict a mean apparent clearance of 132 mL/h in healthy adults and 0.0576 L/h in pediatric JIA patients.[A215657,A215357] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L04AB",
"L04A",
"L04",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "250.37",
"description": "Enbrel 25 mg kit",
"unit": "each"
},
{
"cost": "488.74",
"description": "Enbrel 50 mg/ml sureclick syr",
"unit": "syringe"
},
{
"cost": "1016.57",
"description": "Enbrel 4 25 mg Kit (1 Box = 1 Kit = Four 25 mg Vials)",
"unit": "box"
}... | [
{
"approved": "2009-06-16",
"country": "Canada",
"expires": "2023-02-27",
"number": "2476934"
},
{
"approved": "2000-03-14",
"country": "Canada",
"expires": "2013-09-14",
"number": "2123593"
},
{
"approved": "2007-10-02",
"country": "United States",
"expires": "20... | Etanercept | etanercept-szzs | etanercept-ykro | Recombinant human TNF | rhu TNFR:Fc | rhu-TNFR:Fc | TNFR-Immunoadhesin | Cachectin | TNF-a | TNF-alpha | TNFA | TNFSF2 | Tumor necrosis factor ligand superfamily member 2 | LT-alpha | TNF-beta | TNFB | TNFSF1 | Tumor necrosis factor ligand superfamily member 1 | Fc-gamma... | [
"Benepali",
"Benepali",
"Benepali",
"Benepali",
"Benepali",
"Benepali",
"Benepali",
"Brenzys",
"Brenzys",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
... | [
"Davictrel",
"Tunex"
] | [
"Enbrel",
"Enbrel"
] | [
"P01375",
"P01374",
"P12314",
"P12318",
"P31994",
"P31995",
"P08637",
"O75015",
"P02745",
"P02746",
"P02747"
] | [] | [] | [] |
DB00006 | Bivalirudin | Bivalirudin is a synthetic 20 residue peptide (thrombin inhibitor) which reversibly inhibits thrombin. Once bound to the active site, thrombin cannot activate fibrinogen into fibrin, the crucial step in the formation of thrombus. It is administered intravenously. Because it can cause blood stagnation, it is important t... | solid | For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is plan... | Bivalirudin mediates an inhibitory action on thrombin by directly and specifically binding to both the catalytic site and anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible because thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site... | Inhibits the action of thrombin by binding both to its catalytic site and to its anion-binding exosite. Thrombin is a serine proteinase that plays a central role in the thrombotic process, acting to cleave fibrinogen into fibrin monomers and to activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalent... | Following intravenous administration, bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 +/- 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr intravenous infusion given over 4 hours. | 80% proteolytic cleavage | Based on a study by Gleason et al., the no-observed-adverse-effect level (NOAEL) for bivalirudin, administered to rats via intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h. | * Normal renal function: 25 min (in normal conditions)
* Creatinine clearance 10-29mL/min: 57min
* Dialysis-dependant patients: 3.5h | Other than thrombin and red blood cells, bivalirudin does not bind to plasma proteins. | Bivalirudin is cleared from plasma by a combination of renal mechanisms (20%) and proteolytic cleavage. | 0.2L/kg | * 3.4 mL/min/kg [Normal renal function]
* 3.4 mL/min/kg [mild renal function]
* 2.7 mL/min/kg [moderate renal function]
* 2.8 mL/min/kg [severe renal function]
* 1 mL/min/kg [Dialysis-dependent patients] | Organic compounds | Organic Polymers | Polypeptides | null | [
"approved",
"investigational"
] | [
"B01AE",
"B01A",
"B01",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "780.0",
"description": "Angiomax 250 mg vial",
"unit": "vial"
}
] | [
{
"approved": "1993-03-23",
"country": "United States",
"expires": "2010-05-23",
"number": "5196404"
},
{
"approved": "1999-12-14",
"country": "Canada",
"expires": "2010-08-17",
"number": "2065150"
},
{
"approved": "2009-10-06",
"country": "United States",
"expire... | Bivalirudin | Bivalirudina | Bivalirudinum | 3.4.21.5 | Coagulation factor II | 1.11.2.2 | MPO | [
"Angiomax",
"Angiomax",
"Angiomax",
"Angiomax",
"Angiomax RTU",
"Angiox",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivaliru... | [
"Angiox",
"Hirulog"
] | [] | [
"P00734"
] | [
"P05164"
] | [] | [] |
DB00007 | Leuprolide | Leuprolide is a synthetic 9-residue peptide analogue of gonadotropin-releasing hormone (GnRH). Unlike the endogenous decapeptide GnRH, leuprolide contains a single D-amino acid (D-leucyl) residue, which helps to increase its circulating half-life from three to four minutes to approximately three hours.[A203222] As a Gn... | solid | Leuprolide is indicated for the treatment of advanced prostate cancer [L13781, L34415] and as palliative treatment of advanced prostate cancer.[L13790]
It is also used for the treatment of pediatric patients with central precocious puberty (CPP).[L13784, L13787]
In combination with oral [norethisterone] (also k... | Leuprolide is a gonadotropin-releasing hormone (GnRH) analogue that functions as a GnRH receptor superagonist.[A203132, A203222] After an initial spike in GnRH-mediated steroidal production, including testosterone and estradiol, prolonged use results in a significant drop in circulating steroid levels, in line with tho... | Gonadotropin-releasing hormone (GnRH) is a naturally occurring decapeptide that modulates the hypothalamic-pituitary-gonadal (HPG) axis. GnRH binds to corresponding receptors (GnRHRs) on the anterior pituitary gonadotropes, which in turn release luteinizing hormone (LH) and follicle-stimulating hormone (FSH); these, in... | Leuprolide is typically administered as a single-dose long-acting formulation employing either microsphere or biodegradable solid depot technologies.[A203126] Regardless of the exact formulation and initial dose strength, the C<sub>max</sub> is typically achieved by 4-5 hours post-injection and displays large variabili... | Radiolabeling studies suggest that leuprolide is primarily metabolized to inactive penta-, tri-, and dipeptide entities, which are likely further metabolized. It is expected that various peptidases encountered throughout systemic circulation are responsible for leuprolide metabolism.[L10310, L13781, L13784, L13787, L13... | Leuprolide is considered extremely safe, with low dose-related toxicity and comparatively mild adverse effects.[A203126] Prostate cancer patients treated with leuprolide at doses as high as 20 mg/day for two years showed no additional adverse effects compared to those receiving 1 mg/day.[L13814] | Leuprolide has a terminal elimination half-life of approximately three hours.[L10310, L13781, L13784, L13787, L13790, L13814, L34415] | Leuprolide displays _in vitro_ binding to human plasma proteins between 43% and 49%.[L10310, L13781, L13784, L13787, L13790, L13814, L34415] | Following administration of 3.75 mg leuprolide depot suspension to three patients, less than 5% of the initial dose was recovered as unchanged or pentapeptide metabolite in the urine.[L10310, L13781, L13784, L13814] | Leuprolide has an apparent steady-state volume of distribution of 27 L following intravenous bolus administration to healthy males. The volume of distribution for indicated routes of subcutaneous or intramuscular injection has not been reported.[L10310, L13781, L13784, L13787, L13790, L13814, L34415] | Leuprolide administered as a 1 mg intravenous bolus in healthy males has a mean systemic clearance between 7.6 and 8.3 L/h.[L10310, L13781, L13784, L13787, L13790, L13814, L34415] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L02AE",
"L02A",
"L02",
"L",
"L02AE",
"L02A",
"L02",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "385.33",
"description": "Leuprolide 2wk 1 mg/0.2 ml kit",
"unit": "kit"
},
{
"cost": "400.74",
"description": "Leuprolide Acetate 1 mg/0.2ml Kit 2.8ml 2-Week Kit",
"unit": "box"
},
{
"cost": "493.2",
"description": "Eligard 7.5 mg syringe",
"unit": "syringe"
... | [
{
"approved": "2000-03-14",
"country": "United States",
"expires": "2016-12-13",
"number": "6036976"
},
{
"approved": "2014-12-30",
"country": "United States",
"expires": "2031-02-05",
"number": "8921326"
},
{
"approved": "2008-09-30",
"country": "United States",
... | Leuprorelin | Leuprorelina | Leuproreline | Leuprorelinum | GnRH receptor | GnRH-R | GRHR | GNRH | GRH | LHRH | Progonadoliberin I | [
"Camcevi",
"Camcevi",
"Camcevi",
"Camcevi",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Fen... | [
"Camcevi",
"Leuplin",
"LeuProMaxx",
"Memryte",
"Prostap 3",
"Prostap SR"
] | [
"Viadur",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Lupron Depot",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Lupaneta Pack",
"Lupaneta Pack",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprol... | [
"P30968",
"P01148"
] | [] | [] | [] |
DB00008 | Peginterferon alfa-2a | Peginterferon alfa-2a is a form of recombinant interferon used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most co... | liquid | Peginterferon alfa-2a is indicated for the treatment of HCV in combination with other antiviral drugs in patients over 5 years of age with compensated liver disease [FDA Label]. May be used as a monotherapy in patients with contraindications to or significant intolerance to other anti-viral therapies.
Peginterferon ... | Peginterferon alfa-2a induces the body's innate antiviral response [FDA Label]. | Peginterferon alfa-2a is derived from recombinant human interferon's alfa-2a moeity [FDA Label]. It binds to and activates human type 1 interferon receptors causing them to dimerize. This activates the JAK/STAT pathway. Activation of the JAK/STAT pathway increases expression of multiple genes in multiple tissues involv... | Peginterferon alfa-2a reaches peak plasma concentration 72-96 hours after subcutaneous administration [FDA Label]. Trough concentrations at week 48 are approximately 2 fold higher than week 1. The peak to trough ratio at week 48 is 2. | null | Peginterferon alfa-2a may manifest neuropsychiatric complications include suicide, suicidal ideation, homicidal ideation, depression, relapse of drug addiction, and drug overdose [FDA Label]. Hypertension, supraventricular arrhythmias, chest pain, and myocardial infarction have been observed in patients using Peginterf... | The mean terminal half-life of peginterferon alfa-2a is 164 in a range of 84-353 hours [FDA Label]. | null | null | null | The mean systemic clearance of peginterferon alfa-2a is 94 milliliters per hour [FDA Label]. | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L03AB",
"L03A",
"L03",
"L",
"L03AB",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "642.64",
"description": "Pegasys 180 mcg/ml vial",
"unit": "ml"
},
{
"cost": "2533.2",
"description": "Pegasys 180 mcg/0.5 ml conv.pk",
"unit": "each"
},
{
"cost": "2634.53",
"description": "Pegasys (1 Kit = Four 180 mcg/ml Vials Prefilled Syringes) Box",
"unit... | [
{
"approved": "2009-06-30",
"country": "Canada",
"expires": "2017-04-23",
"number": "2203480"
},
{
"approved": "2000-10-03",
"country": "Canada",
"expires": "2016-03-26",
"number": "2172664"
}
] | PEG-IFN alfa-2A | PEG-Interferon alfa-2A | Peginterferon alfa-2a | Pegylated Interfeaon alfa-2A | Pegylated interferon alfa-2a | Pegylated interferon alpha-2a | Pegylated-interferon alfa 2a | IFN-alpha binding protein | IFN-alpha/beta receptor 2 | IFN-R-2 | IFNABR | IFNARB | Interferon alpha binding protein | Type I in... | [
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Peg... | [] | [
"Pegasys Rbv",
"Pegasys Rbv"
] | [
"P48551",
"P17181"
] | [
"P05177"
] | [] | [] |
DB00009 | Alteplase | Alteplase is a recombinant tissue plasminogen activator (rt-PA) used as a thrombolytic agent.[L43125] It cleaves plasminogen to form plasmin, an enzyme involved in the degradation of fibrin clots. In the absence of fibrin, the alteplase-mediated conversion of plasminogen is limited, thanks to the high affinity between ... | liquid | Alteplase is indicated for the treatment of acute ischemic stroke (AIS) and for use in acute myocardial infarction (AMI) for the reduction of mortality and incidence of heart failure. Alteplase is also indicated for the lysis of acute massive pulmonary embolism, defined as acute pulmonary emboli obstructing blood flow ... | Alteplase binds to fibrin and plasminogen. Alteplase specificity for fibrin is achieved thanks to its high affinity for lysine residues. Also, it can bind plasminogen via loop structures called kringles, stabilized by three disulphide linkages similar to the ones in plasminogen. The specificity of alteplase for plasmin... | Alteplase is a recombinant tissue plasminogen activator (rt-PA) that converts plasminogen to plasmin in a fibrin-dependent process. In the absence of fibrin, alteplase converts a limited amount of plasminogen. However, in the presence of fibrin clots, alteplase binds to fibrin and cleaves the arginine-valine bond at po... | Healthy volunteers with a baseline endogenous tissue plasminogen activator (t-PA) of 3.3 ng/ml had a 290-fold increase in baseline concentrations after receiving alteplase at an infusion rate of 0.25 mg/kg for 30 min; with an infusion rate of 0.5 mg/kg, a 550-fold increase was observed.[A252270] Acute myocardial infarc... | Alteplase is mainly metabolized by the liver. The carbohydrate and polypeptide domains of alteplase interact with hepatic glycoprotein receptors, leading to receptor-mediated endocytosis.[A252270] _In vivo_ studies suggest that alteplase follows zero-order kinetics, meaning that its metabolism is saturable at higher pl... | Toxicity information regarding alteplase is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as risk of bleeding and thromboembolic events.[L43125] Symptomatic and supportive measures are recommended. The carcinogenic potential of alteplase or its effect o... | Alteplase has an initial half-life of less than 5 minutes in patients with acute myocardial infarction (AMI). The dominant initial plasma half-life of the 3-hour and the accelerated regimens for AMI are similar.[L43125] | Not available. | In healthy volunteers, more than 80% of alteplase is eliminated through urine 18 hours after administration.[A252270] | The initial volume of distribution approximates plasma volume.[L43125] The average volume of distribution of the central compartment goes from 3.9 to 4.3 L, and the volume of distribution at steady state goes from 7.2 to 12 L.[A252270] | Alteplase has a plasma clearance between 380 and 570 mL/min.[L43125] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"B01AD",
"B01A",
"B01",
"B",
"S01XA",
"S01X",
"S01",
"S"
] | [
"Humans and other mammals"
] | [
{
"cost": "106.33",
"description": "Cathflo activase 2 mg vial",
"unit": "vial"
},
{
"cost": "2389.85",
"description": "Activase 50 mg vial",
"unit": "vial"
},
{
"cost": "4779.71",
"description": "Activase 100 mg vial",
"unit": "vial"
}
] | [] | Alteplasa | Alteplase | Alteplase (genetical recombination) | Alteplase, recombinant | Alteplase,recombinant | Plasminogen activator (human tissue-type protein moiety) | rt-PA | t-PA | t-plasminogen activator | Tissue plasminogen activator | Tissue plasminogen activator alteplase | Tissue plasminogen activator, recombi... | [
"Activase",
"Activase",
"Activase RT-PA",
"Activase RT-PA",
"Activase RT-PA Inj",
"Activase RT-PA Inj",
"Activase RT-PA Inj",
"Cathflo",
"Cathflo Activase",
"Lysatec RT - Pa"
] | [] | [
"Lysatec RT - Pa",
"Activase RT-PA",
"Activase RT-PA"
] | [
"P00747",
"P02671",
"P02679",
"P05121"
] | [] | [] | [] |
DB00010 | Sermorelin | Sermorelin acetate is the acetate salt of an amidated synthetic 29-amino acid peptide (GRF 1-29 NH 2 ) that corresponds to the amino-terminal segment of the naturally occurring human growth hormone-releasing hormone (GHRH or GRF) consisting of 44 amino acid residues | liquid | For the treatment of dwarfism, prevention of HIV-induced weight loss | Sermorelin is used in the treatment of children with growth hormone deficiency or growth failure. Geref increases plasma growth hormone (GH) concentration by stimulating the pituitary gland to release GH. Geref is similar to the full-length native hormone (44 residues) in its ability to stimulate GH secretion in humans... | Sermorelin binds to the growth hormone releasing hormone receptor and mimics native GRF in its ability to stimulate growth hormone secretion. | null | null | null | 11-12 min | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"withdrawn"
] | [
"V04CD",
"V04C",
"V04",
"V",
"H01AC",
"H01A",
"H01",
"H"
] | [
"Humans and other mammals"
] | [] | [] | Sermorelin | GHRH receptor | GRF receptor | GRFR | Growth hormone-releasing factor receptor | [] | [
"Geref"
] | [] | [
"Q02643"
] | [] | [] | [] |
DB00011 | Interferon alfa-n1 | Interferon alfa-n1 consists of purified, natural (n is for natural) alpha interferon subtypes, at least two of which are glycosylated. This differs from recombinant alpha interferons, which are individual non-glycosylated proteins produced from individual alpha interferon genes. | liquid | For the treatment of venereal or genital warts caused by the Human Papiloma Virus. | Upregulates the expression of MHC I proteins, allowing for increased presentation of peptides derived from viral antigens. This enhances the activation of CD8+ T cells that are the precursors for cytotoxic T lymphocytes (CTLs) and makes the macrophage a better target for CTL-mediated killing. Interferon alpha also indu... | Interferon alpha binds to type I interferon receptors (IFNAR1 and IFNAR2c) which, upon dimerization, activate two Jak (Janus kinase) tyrosine kinases (Jak1 and Tyk2). These transphosphorylate themselves and phosphorylate the receptors. The phosphorylated INFAR receptors then bind to Stat1 and Stat2 (signal transducers ... | null | null | null | 1.2 hours (mammalian reticulocytes, in vitro); >20 hours (yeast, in vivo); >10 hours (Escherichia coli, in vivo). | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L03AB",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [] | [] | Interferon alfa-n1 | Interferon alpha-n1 (INS) | WELL-FERON | WELLFERON | CRF2-1 | Cytokine receptor class-II member 1 | Cytokine receptor family 2 member 1 | IFN-alpha/beta receptor 1 | IFN-R-1 | IFNAR | Type I interferon receptor 1 | IFN-alpha binding protein | IFN-alpha/beta receptor 2 | IFN-R-2 | IFNABR | IFNARB | ... | [
"Wellferon Inj 10 000 000unit/ml",
"Wellferon Inj 3000000unit/ml"
] | [
"Wellferon"
] | [] | [
"P17181",
"P48551"
] | [
"P05177"
] | [] | [] |
DB00012 | Darbepoetin alfa | Human erythropoietin with 2 aa substitutions to enhance glycosylation (5 N-linked chains), 165 residues (MW=37 kD). Produced in Chinese hamster ovary (CHO) cells by recombinant DNA technology. | liquid | For the treatment of anemia (from renal transplants or certain HIV treatment) | Darbepoetin alfa is used in the treatment of anemia. It is involved in the regulation of erythrocyte differentiation and the maintenance of a physiological level of circulating erythrocyte mass. | Darbepoetin alfa stimulates erythropoiesis by the same mechanism as endogenous erythropoietin. Erythropoietin interacts with
progenitor stem cells to increase red cell production. Binding of erythropoietin to the erythropoietin receptor leads to receptor dimerization, which facilitates activation of JAK-STAT signaling... | null | null | null | null | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"B03XA",
"B03X",
"B03",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "156.36",
"description": "Aranesp 25 mcg/ml vial",
"unit": "ml"
},
{
"cost": "162.61",
"description": "Aranesp (Albumin Free) 25 mcg/ml vial",
"unit": "vial"
},
{
"cost": "250.2",
"description": "Aranesp 40 mcg/ml vial",
"unit": "ml"
},
{
"cost": "375.3"... | [
{
"approved": "2003-03-18",
"country": "Canada",
"expires": "2010-10-15",
"number": "2165694"
},
{
"approved": "2002-11-05",
"country": "Canada",
"expires": "2014-08-16",
"number": "2147124"
}
] | Darbepoetin | Darbepoetin alfa | Darbepoetin alfa,recombinant | Darbepoetina alfa | EPO-R | [
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Ara... | [] | [] | [
"P19235"
] | [] | [] | [] |
DB00013 | Urokinase | Urokinase is an endogenous peptide that is cleaved in the presence of plasmin between lysine 158 and isoleucine 159 to yield active urokinase.[A191943] Urokinase remains connected between these 2 chains by a sulfhydryl bond.[A191943]
Urokinase was granted FDA approval on 16 January 1978.[L12138] | liquid | In Canada, urokinase is indicated for lysis of acute massive pulmonary emboli, acute thrombi obstructing coronary arteries, occlusive thromboemboli in peripheral arteries and grafts, and restoration of patency to intravenous catheters.[L12141] | Urokinase is a serine protease that activates plasminogen to an active fibrinolytic protease.[A191928] The duration of action is short due to the short half life.[L12138] Patients should be counselled regarding the risk of bleeding, anaphylaxis, infusion reactions, and cholesterol embolization.[L12138 | Urokinase is a serine protease.[A191928] It cleaves plasminogen to form the active fibrinolytic protease, plasmin.[A191928] | Urokinase is delivered intravenously, so the bioavailability is high. | Because urokinase is a protein, it is expected to be metabolized by proteases to smaller proteins and amino acids. | Patients experiencing an overdose may present with bleeding.[L12141] Treat patients with symptomatic and supportive measures which may include application of local pressure, administration of whole blood or plasma, and administration of aminocaproic acid.[L12141] | Urokinase has a half life of 12.6±6.2 minutes.[L12138] | Data regarding the protein binding of urokinase in plasma is not readily available. | Urokinase is eliminated in the bile and urine.[L12138] | The volume of distribution of urokinase is 11.5L.[L12138] | Data regarding the clearance of urokinase is not readily available. | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational",
"withdrawn"
] | [
"B01AD",
"B01A",
"B01",
"B"
] | [
"Humans and other mammals"
] | [] | [] | Kinase (enzyme-activating), uro-urokinase | TCUK | Tissue culture urokinase | Two-chain urokinase | Urochinasi | Urokinase | Urokinasum | Uroquinasa | 3.4.21.7 | MO3 | Monocyte activation antigen Mo3 | U-PAR | UPAR | Endothelial plasminogen activator inhibitor | PAI | PAI-1 | PAI1 | PLANH1 | Serpin E1 | Monocyte Arg-se... | [
"Kinlytic",
"Kinlytic (urokinase for Injection)",
"Kinlytic Open-cath"
] | [
"Abbokinase"
] | [] | [
"P00747",
"Q03405",
"P05121",
"P05120",
"P05154",
"P98164",
"Q9Y5Y6",
"P14543"
] | [
"P39900"
] | [] | [] |
DB00014 | Goserelin | Goserelin is a synthetic hormone. In men, it stops the production of the hormone testosterone, which may stimulate the growth of cancer cells. In women, goserelin decreases the production of the hormone estradiol (which may stimulate the growth of cancer cells) to levels similar to a postmenopausal state. When the medi... | solid | Goserelin is indicated for:
- Use in combination with flutamide for the management of locally confined carcinoma of the prostate
- Palliative treatment of advanced carcinoma of the prostate
- The management of endometriosis
- Use as an endometrial-thinning agent prior to endometrial ablation for dysfunctional ute... | The pharmacokinetics of goserelin have been determined in both male and female healthy volunteers and patients. In these studies, goserelin was administered as a single 250µg (aqueous solution) dose and as a single or multiple 3.6 mg depot dose by subcutaneous route. | Goserelin is a synthetic decapeptide analogue of LHRH. Goserelin acts as a potent inhibitor of pituitary gonadotropin secretion when administered in the biodegradable formulation. The result is sustained suppression of LH and serum testosterone levels. | Inactive orally, rapidly absorbed following subcutaneous administration. | Hepatic | No experience of overdosage from clinical trials. | 4-5 hours | 27.3% | Clearance of goserelin following subcutaneous administration of a radiolabeled solution of goserelin was very rapid and occurred via a combination of hepatic and urinary excretion. More than 90% of a subcutaneous radiolabeled solution formulation dose of goserelin was excreted in urine. | * 44.1 ± 13.6 L [subcutaneous administration of 250 mcg] | * 121 +/- 42.4 mL/min [prostate cancer with 10.8 mg depot] | Organic compounds | Organic acids and derivatives | Carboxylic acids and derivatives | Amino acids, peptides, and analogues | [
"approved"
] | [
"L02AE",
"L02A",
"L02",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "451.19",
"description": "Zoladex 3.6 mg implant syringe",
"unit": "syringe"
},
{
"cost": "1380.65",
"description": "Zoladex 10.8 mg implant syringe",
"unit": "syringe"
}
] | [
{
"approved": "2006-10-10",
"country": "United States",
"expires": "2022-04-13",
"number": "7118552"
},
{
"approved": "2007-05-22",
"country": "United States",
"expires": "2022-04-09",
"number": "7220247"
},
{
"approved": "2009-03-10",
"country": "United States",
... | Goserelin | Goserelina | LCGR | LGR2 | LH/CG-R | LHR | LHRHR | LSH-R | Luteinizing hormone receptor | GNRH | GRH | LHRH | Progonadoliberin I | GnRH receptor | GnRH-R | GRHR | [
"Zoladex",
"Zoladex",
"Zoladex",
"Zoladex",
"Zoladex",
"Zoladex",
"Zoladex",
"Zoladex LA"
] | [] | [] | [
"P22888",
"P01148",
"P30968"
] | [] | [] | [] |
DB00015 | Reteplase | Human tissue plasminogen activator, purified, glycosylated, 355 residues purified from CHO cells. Retavase is considered a "third-generation" thrombolytic agent, genetically engineered to retain and delete certain portions of human tPA. Retavase is a deletion mutein of human tPA formed by deleting various amino acids p... | liquid | For lysis of acute pulmonary emboli, intracoronary emboli, and management of myocardial infarction. | Reteplase cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cause myocardial infarction. | Reteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. | null | null | null | null | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"B01AD",
"B01A",
"B01",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "2605.93",
"description": "Retavase vial half-kit",
"unit": "vial"
}
] | [
{
"approved": "2007-12-18",
"country": "Canada",
"expires": "2012-04-15",
"number": "2107476"
}
] | Human t-PA (residues 1-3 and 176-527) | Reteplasa | Reteplase | Reteplase, recombinant | Reteplase,recombinant | 3.4.21.7 | Endothelial plasminogen activator inhibitor | PAI | PAI-1 | PAI1 | PLANH1 | Serpin E1 | [
"Rapilysin",
"Retavase",
"Retavase",
"Retavase",
"Retavase",
"Retavase"
] | [] | [] | [
"P00747",
"P02671",
"P05121"
] | [] | [] | [] |
DB00016 | Erythropoietin | Erythropoietin (EPO) is a growth factor produced in the kidneys that stimulates the production of red blood cells. It works by promoting the division and differentiation of committed erythroid progenitors in the bone marrow [FDA Label]. Epoetin alfa (Epoge) was developed by Amgen Inc. in 1983 as the first rhEPO commerc... | liquid | Indicated in adult and paediatric patients for the:
- treatment of anemia due to Chronic Kidney Disease (CKD) in patients on dialysis and not on dialysis.
- treatment of anemia due to zidovudine in patients with HIV-infection.
- treatment of anemia due to the effects of concomitant myelosuppressive chemotherapy,... | Erythropoietin and epoetin alfa are involved in the regulation of erythrocyte differentiation and the maintenance of a physiological level of circulating erythrocyte mass. It is reported to increase the reticulocyte count within 10 days of initiation, followed by increases in the RBC count, hemoglobin, and hematocrit, ... | Erythropoietin or exogenous epoetin alfa binds to the erythropoietin receptor (EPO-R) and activates intracellular signal transduction pathways [A33079]. The affinity (Kd) of EPO for its receptor on human cells is ∼100 to 200 pM [A33080]. Upon binding to EPO-R on the surface of erythroid progenitor cells, a conformation... | The time to reach peak concentration is slower via the subcutaneous route than the intravenous route which ranges from 20 to 25 hours, and the peak is always well below the peak achieved using the intravenous route (5–10% of those seen with IV administration).[A33080] The bioavailability of subcutaneous injectable eryt... | Binding of erythropoietin and epoetin alfa to EPO-R leads to cellular internalization, which involves the degradation of the ligand. Erythropoietin and epoetin alfa may also be degraded by the reticuloendothelial scavenging pathway or lymphatic system [A33080]. | Overdose from epoetin alfa include signs and symptoms associated with an excessive and/or rapid increase in hemoglobin concentration, including cardiovascular events. Patients with suspected or known overdose should be monitored closely for cardiovascular events and hematologic abnormalities. Polycythemia should be man... | **Healthy volunteers:** The half life is approximately 4 hours in healthy volunteers receiving an intravenous injection [F85]. A half-life of approximately 6 hours has been reported in children [F85].
**Adult and paediatric patients with CRF:** The elimination half life following intravenous administration ranges fr... | No information of serum protein binding available. | Erythropoietin and epoetin alfa are cleared via uptake and degradation via the EPO-R-expressing cells, and may also involve other cellular pathways in the interstitium, probably via cells in the reticuloendothelial scavenging pathway or lymphatic system [A33080]. Only a small amount of unchanged epoetin alfa is found i... | In healthy volunteers, the volume of distribution of intravenous epoetin alfa was generally similar to the plasma volume (range of 40–63.80 mL/kg), indicating limited extravascular distribution [A33080, A33076]. | **Healthy volunteers: ** In male volunteers receiving intravenous epoetin alfa, the total body clearance was approximately 8.12 ± 1.00 mL/h/kg [A33076].
**Cancer patients receiving cyclic chemotherapy:** The average clearance was approximately 20.2 ± 15.9 mL/h/kg after 150 Units/kg three times per week (TIW) subcut... | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"B03XA",
"B03X",
"B03",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "34.14",
"description": "Epogen 2000 unit/ml vial",
"unit": "vial"
},
{
"cost": "37.09",
"description": "Procrit 2000 unit/ml vial",
"unit": "vial"
},
{
"cost": "47.53",
"description": "Epogen 3000 unit/ml vial",
"unit": "vial"
},
{
"cost": "55.63",
... | [
{
"approved": "1997-05-27",
"country": "Canada",
"expires": "2014-05-27",
"number": "1339047"
}
] | 1-165-Erythropoietin (human clone λHEPOFL13 protein moiety), glycoform α | E.P.O. | EPOETIN | Epoetin alfa | Epoetin alfa rDNA | Epoetin alfa-epbx | Epoetin alfa, recombinant | Epoetin epsilon | Epoetin gamma | Epoetin gamma rDNA | Epoetin kappa | Epoetin omega | Epoetin theta | Epoetin zeta | Epoetina alfa | Epoetina ... | [
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseame... | [
"Epobel",
"Epocept",
"Epofit",
"Epogin",
"Eqralys",
"Nanokine"
] | [] | [
"P19235"
] | [] | [] | [] |
DB00017 | Salmon calcitonin | Synthetic peptide, 32 residues long formulated as a nasal spray. | liquid | Used in the treatment of symptomatic Paget's disease for patients unresponsive to alternate treatments or intolerant to such treatments. In addition, it is used in emergency situations when serum calcium levels must be decreased quickly until the underlying condition is identified. It can also be added to existing ther... | Calcitonin inhibits bone resorption by osteoclasts (bone remodeling cells) and promotes bone formation by osteoblasts. This leads to a net increase in bone mass and a reduction in plasma calcium levels. It also promotes the renal excretion of ions such as calcium, phosphate, sodium, magnesium, and potassium by decreasi... | Calcitonin binds to the calcitonin receptor (found primarily in osteoclasts) which then enhances the production of vitamin D producing enzymes (25-hydroxyvitamine D-24-hydroxylase), leading to greater calcium retention and enhanced bone density. Binding of calcitonin to its receptor also activates adenylyl cyclase and ... | Salmon calcitonin is rapidly absorbed with bioavailability of 71% following subcutaneous injection and 66% following intramuscular injection in humans. Via the nasal route, the bioavailability varies between 3 to 5% relative to IM. | Salmon calcitonin primarily undergoes degradation in the kidneys to form pharmacologically inactive metabolites. It is also metabolized in the blood and the peripheral tissue. | Salmon calcitonin was shown to inhibit lactation in animals and is not recommend in nursing mothers. While research in animals have shown a decrease in fetal weight, no studies have yet shown similar results in humans. It is recommended however to proceed carefully when administering salmon calcitonin to pregnant women... | Half-life elimination (terminal): I.M. 58 minutes; SubQ 59 to 64 minutes; Nasal: ~18 to 23 minutes | Protein binding is about 30 to 40%. | Urine. Studies with injectable calcitonin show increases in the excretion of filtered phosphate, calcium, and sodium by decreasing their tubular reabsorption in the kidney. | 0.15 to 0.3 L/kg | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"H05BA",
"H05B",
"H05",
"H"
] | [
"Humans and other mammals"
] | [
{
"cost": "8.81",
"description": "Caltine 100 (100 Iu/Ml) 100 iu/ml",
"unit": "ml"
},
{
"cost": "29.94",
"description": "Calcimar 200 iu/ml",
"unit": "ml"
},
{
"cost": "30.73",
"description": "Miacalcin 200 unit/ml vial",
"unit": "ml"
},
{
"cost": "34.3",
"des... | [
{
"approved": "1998-03-31",
"country": "United States",
"expires": "2015-03-31",
"number": "5733569"
},
{
"approved": "2002-08-27",
"country": "United States",
"expires": "2021-02-02",
"number": "6440392"
},
{
"approved": "2012-08-14",
"country": "United States",
... | Calcitonin (Salmon Synthetic) | Calcitonin salmon | Calcitonin salmon recombinant | Calcitonin-salmon | Calcitonin, salmon | Calcitonina salmón sintética | Recombinant salmon calcitonin | Salmon calcitonin | CT-R | [
"Apo-calcitonin Injectable",
"Apo-calcitonin Nasal Spray",
"Calcimar",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calciton... | [
"Calcimar"
] | [] | [
"P30988"
] | [] | [] | [] |
DB00018 | Interferon alfa-n3 | Purified, natural (n is for natural) human interferon alpha proteins (consists of 3 forms or polymorphisms including 2a, 2b and 2c). 166 residues, some are glycosylated (MW range from 16 kD to 27 kD). | liquid | For the intralesional treatment of refractory or recurring external condylomata acuminata. | Interferon alfa-n3 upregulates the expression of MHC I proteins, allowing for increased presentation of peptides derived from viral antigens. This enhances the activation of CD8+ T cells that are the precursors for cytotoxic T lymphocytes (CTLs) and makes the macrophage a better target for CTL-mediated killing. Interfe... | Interferon alpha binds to type I interferon receptors (IFNAR1 and IFNAR2c) which, upon dimerization, activate two Jak (Janus kinase) tyrosine kinases (Jak1 and Tyk2). These transphosphorylate themselves and phosphorylate the receptors. The phosphorylated INFAR receptors then bind to Stat1 and Stat2 (signal transducers ... | null | null | null | null | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [] | [
"Humans and other mammals"
] | [
{
"cost": "412.87",
"description": "Alferon n 5 million unit vial",
"unit": "ml"
}
] | [] | Interferon alfa-n3 | CRF2-1 | Cytokine receptor class-II member 1 | Cytokine receptor family 2 member 1 | IFN-alpha/beta receptor 1 | IFN-R-1 | IFNAR | Type I interferon receptor 1 | IFN-alpha binding protein | IFN-alpha/beta receptor 2 | IFN-R-2 | IFNABR | IFNARB | Interferon alpha binding protein | Type I interferon ... | [
"Alferon"
] | [
"Alferon",
"Alferon N"
] | [] | [
"P17181",
"P48551"
] | [
"P05177"
] | [] | [] |
DB00019 | Pegfilgrastim | Pegfilgrastim is a PEGylated form of the recombinant human granulocyte colony-stimulating factor (G-CSF) analogue, [filgrastim].[A187601] The drug is approved for use to decrease the incidence of infection, as manifested by febrile neutropenia, in susceptible patients with with non-myeloid cancer receiving myelosuppres... | liquid | Pegfilgrastim is indicated to decrease the incidence of infection, as manifested by febrile neutropenia, in patients with non myeloid malignancies receiving myelosuppressive anti-cancer drugs associated with a clinically significant incidence of febrile neutropenia.[L44221]
It is also indicated to increase survival... | Pegfilgrastim is a recombinant human granulocyte colony-stimulating factor (G-CSF) that promotes the production, proliferation, and maturation of neutrophils, which are white blood cells involved in both innate and adaptive immune responses.[A187631,A248855] The safety and efficacy of pegfilgrastim in reducing the risk... | Neutrophils are short-lived immune cells that are highly susceptible to cell death following myelosuppressive chemotherapy. This marked reduction in neutrophil numbers during chemotherapy increases the risk of hospitalization, infection, and infection-related mortality. It also directly impacts the clinical outcome of ... | Pegfilgrastim has a lower absolute bioavailability than filgrastim following subcutaneous administration. The absorption of pegfilgrastim is largely dependent on the lymphatic system due to the attached PEG group contributing to the large size of the drug. It is slowly absorbed following subcutaneous administration wit... | It is not know whether pegfilgrastim is metabolized into major metabolites.[L10022] Once it binds to the therapeutic target, pegfilgrastim is internalized by the neutrophil and undergoes nonspecific degradation.[A29] | The maximum safe dose of pegfilgrastim has not been established; however, the highest dose used in clinical trials was 300 mcg/kg.[A248855] Overdosage of pegfilgrastim may result in leukocytosis and bone pain. Events of edema, dyspnea, and pleural effusion have been reported in a single patient who self-administered pe... | The serum half-life of Pegfilgrastim is highly variable depending on the absolute neutrophil count, with the range of 15 to 80 hours following subcutaneous administration. The median serum half-life of 42 hours.[A187607,L9746] | The plasma protein binding of pegfilgrastim is unlikely.[L10022] | The polyethylene glycol moiety limits the renal clearance by glomerular filtration of pegfilgrastim, making neutrophil-mediated clearance as the predominant route of elimination.[A187607] This elimination pathway is initiated by the binding of pegfilgrastim to the G-CSF receptor on the neutrophil cell surface, leading ... | Pegfilgrastim appears to have a volume of distribution of approximately 170 L.[A33290] | Pegfilgrastim has a self-regulating clearance that involves neutrophil-induced clearance.[A29,A187631] The clearance is dependent on the number of neutrophils and body weight of the patient: the clearance increases with increasing number of granulocytes and lower body weights.[L9746] Pegfilgrastim is not eliminated fro... | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"L03AA",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "4026.05",
"description": "Neulasta 6 mg/0.6ml Solution 0.6ml Syringe",
"unit": "syringe"
},
{
"cost": "4102.37",
"description": "Neulasta 6 mg/0.6 ml syringe",
"unit": "syringe"
}
] | [
{
"approved": "2007-07-31",
"country": "Canada",
"expires": "2024-07-31",
"number": "1341537"
},
{
"approved": "1997-07-29",
"country": "Canada",
"expires": "2014-07-29",
"number": "1339071"
}
] | Granulocyte colony-stimulating factor pegfilgrastim | peg-filgrastim | Pegfilgrastim | pegfilgrastim-apgf | pegfilgrastim-bmez | pegfilgrastim-cbqv | pegfilgrastim-jmdb | G-CSF receptor | G-CSF-R | GCSFR | 3.4.21.37 | Bone marrow serine protease | ELA2 | Elastase-2 | HLE | Human leukocyte elastase | Medullasin | PMN el... | [
"Armlupeg",
"Cegfila",
"Fulphila",
"Fulphila",
"Fulphila",
"Fulphila",
"Fulphila",
"Fylnetra",
"Grasustek",
"Lapelga",
"Lapelga",
"Neulasta",
"Neulasta",
"Neulasta",
"Neulasta",
"Neulasta",
"Neulasta",
"Neulasta",
"Neulasta",
"Neupopeg",
"Neupopeg",
"Neupopeg",
"Niopeg",
... | [] | [] | [
"Q99062"
] | [
"P08246"
] | [] | [] |
DB00020 | Sargramostim | Sargramostim is a human recombinant granulocyte macrophage colony-stimulating factor (GM-CSF) expressed in yeast. It is a glycoprotein that is 127 residues. Substitution of Leu23 leads to a difference from native protein. | liquid | For the treatment of cancer and bone marrow transplant | Sargramostim is used in the treatment of bone marrow transplant recipients or those exposed to chemotherapy an recovering from acut myelogenous leukemia, Leukine or GM-CSF is a hematopoietic growth factor which stimulates the survival, clonal expansion (proliferation) and differentiation of hematopoietic progenitor cel... | Sargramostim binds to the Granulocyte-macrophage colony stimulating factor receptor (GM-CSF-R-alpha or CSF2R) which stimulates a JAK2 STAT1/STAT3 signal transduction pathway. This leads to the production of hemopoietic cells and neutrophils | null | null | null | null | null | null | null | * 420 mL/min/m2 [Normal people with liquid LEUKINE (IV)]
* 431 mL/min/m2 [Normal people with lyophilized LEUKINE (IV)]
* 549 mL/min/m2 [Normal people with liquid LEUKINE (SC)]
* 529 mL/min/m2 [Normal people with lyophilized LEUKINE (SC)] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L03AA",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "204.79",
"description": "Leukine 250 mcg vial",
"unit": "vial"
},
{
"cost": "0.42",
"description": "Bio-immunex capsule",
"unit": "capsule"
}
] | [
{
"approved": "2000-12-05",
"country": "Canada",
"expires": "2017-12-05",
"number": "1341150"
}
] | Recombinant human granulocyte-macrophage colony stimulating factor | rGM-CSF | rHu GM-CSF | Sargramostim | CDw116 | CSF2R | CSF2RY | GM-CSF-R-alpha | GMCSFR-alpha | GMR-alpha | IL-3 receptor subunit alpha | IL-3R subunit alpha | IL-3R-alpha | IL-3RA | IL3R | CDw131 | GM-CSF/IL-3/IL-5 receptor common beta subunit | IL3R... | [
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine"
] | [
"Leucomax"
] | [] | [
"P15509",
"P26951",
"P32927",
"P34741",
"P13727"
] | [] | [] | [] |
DB00022 | Peginterferon alfa-2b | Peginterferon alfa-2b is a form of recombinant interferon used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most co... | liquid | Peginterferon alfa-2b is indicated for the treatment of HCV in combination with [DB00811] and a NS3/4A protease inhibitor for genotype 1 or without a NS3/4A protease inhibitor for genotypes 2-6 [FDA Label]. May be used as a monotherapy in patients with contraindications to or significant intolerance to other anti-viral... | Peginterferon alfa-2b inhibits viral replication in infected cells, suppresses cell proliferation, induces apoptosis, and exerts an anti-angiogenic effect [FDA Label]. Exerts immunomodulatory effects such as enhancement of the phagocytic activity of macrophages, activation of NK cells, stimulation of cytotoxic T-lympho... | Peginterferon alfa-2b is derived from recombinant human interferon's alfa-2b moeity [FDA Label]. It binds to and activates human type 1 interferon receptors causing them to dimerize. This activates the JAK/STAT pathway. Activation of the JAK/STAT pathway increases expression of multiple genes in multiple tissues involv... | Peginterferon alfa-2b reaches peak plasma concentration 15-44 hours after subcutaneous administration [FDA Label]. The mean absorption half-life is 4.6 hours. After multiple doses the bioavailability of Peginterferon alfa-2b increases with trough concentrations at week 48 3-fold higher than those at week 4. | null | Peginterferon alfa-2b may manifest neuropsychiatric complications include suicide, suicidal ideation, homicidal ideation, depression, relapse of drug addiction, and drug overdose [FDA Label]. Hypertension, supraventricular arrhythmias, chest pain, and myocardial infarction have been observed in patients using Peginterf... | The mean half-life of elimination of Peginterferon alfa-2b is 40 hours in a range of 22-60 hours [FDA Label]. | null | Renal elimination accounts for 30% of Peginterferon alfa-2b elimination [FDA Label]. | null | The estimated apparent clearance of Peginterferon alfa-2b is 22 milliters per hour per kilogram [FDA Label]. | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"L03AB",
"L03A",
"L03",
"L",
"L03AB",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "553.4",
"description": "Peg-Intron 50 mcg kit",
"unit": "kit"
},
{
"cost": "553.4",
"description": "Peg-Intron redipen 50 mcg",
"unit": "redipen"
},
{
"cost": "581.02",
"description": "Peg-Intron redipen 80 mcg",
"unit": "redipen"
},
{
"cost": "607.19",... | [
{
"approved": "2008-02-19",
"country": "Canada",
"expires": "2025-02-19",
"number": "1341567"
},
{
"approved": "2002-02-26",
"country": "Canada",
"expires": "2016-10-31",
"number": "2329474"
}
] | Peginterferon alfa-2b | CRF2-1 | Cytokine receptor class-II member 1 | Cytokine receptor family 2 member 1 | IFN-alpha/beta receptor 1 | IFN-R-1 | IFNAR | Type I interferon receptor 1 | IFN-alpha binding protein | IFN-alpha/beta receptor 2 | IFN-R-2 | IFNABR | IFNARB | Interferon alpha binding protein | Type I interfer... | [
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"PegIntron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"PegIntron",
"PegIntron",
"PegIntron",
"PegIntron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron... | [
"PEG-Intron"
] | [
"Pegetron",
"Pegetron",
"Pegetron",
"Victrelis Triple",
"Victrelis Triple",
"Victrelis Triple",
"Victrelis Triple",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron"
] | [
"P17181",
"P48551"
] | [
"P05177",
"P10635",
"P11712"
] | [] | [] |
DB00023 | Asparaginase Escherichia coli | Asparaginase derived from _Escherichia coli_ (L-asparagine amidohydrolase, EC 3.5.1.1) is an enzyme responsible for the metabolism of L-asparagine, by catalyzing L-asparagine into L-aspartic acid and ammonia. It also facilitates the production of oxaloacetate which is needed for general cellular metabolism. Asparaginas... | liquid | Indicated as a component of a multi-agent chemotherapeutic regimen for the treatment of patients with acute lymphoblastic leukemia (ALL).[L39809] | In clinical trials of patients with previously untreated, standard-risk ALL, administration of asparaginase resulted in a decrease of plasma asparagine levels from average of 41 μM to less than 3 μM [FDA Label]. The native asparaginase in whom plasma enzyme activity before treatment was greater than 0.1 International U... | Asparagine is a non-essential amino acid that maintains DNA, RNA and protein synthesis and promotes cell growth. While healthy and normal cells are capable of obtaining asparagine via dietary intake or synthesizing the asparagine from aspartate via asparagine synthetase activity, lymphoblastic leukemic cells lack the a... | In a study in patients with metastatic cancer and leukemia, daily intravenous administration of L-asparaginase derived from _E. coli_ resulted in a cumulative increase in plasma levels. Following intramuscular injection in patients with metastatic cancer and leukemia, peak plasma levels of asparaginase was achieved 14 ... | null | No studies assessing the mutagenic or carcinogenic potential of _E. coli_ L-asparagine have been conducted. In the Ames assay, no mutagenic effect was demonstrated when tested against Salmonella typhimurium strains [FDA Label]. No studies have been performed on impairment of fertility [FDA Label]. Following a single, i... | Plasma half life of L-asparagine derived from _E. coli_ following intravenous injection was 8-30 hrs [FDA Label]. Plasma half-life was 34 to 49 hours after intramuscular injection [FDA Label]. Half-life (mean ± SD) of native _E. coli_ asparaginase is approximately 1.28 ± 0.35 days [A31999]. | null | null | Apparent volume of distribution was slightly greater than the plasma volume. Asparaginase levels in cerebrospinal fluid were less than 1% of concurrent plasma levels [A31999]. | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L01XX",
"L01X",
"L01",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "74.6",
"description": "Elspar 10000 unit vial",
"unit": "vial"
}
] | [] | Asparaginase | Asparaginase (E. coli) | Colaspase | Escherichia coli L-asparaginase | L-asparaginase | L-asparagine amidohydrolase | Serpin A7 | T4-binding globulin | TBG | [
"Elspar",
"Kidrolase",
"Rylaze",
"Spectrila",
"Spectrila"
] | [] | [] | [] | [] | [
"P05543"
] | [] |
DB00024 | Thyrotropin alfa | Thyrotropin alfa is a recombinant form of thyroid stimulating hormone used in performing certain tests in patients who have or have had thyroid cancer. It is also used along with a radioactive agent to destroy remaining thyroid tissue in certain patients who have had their thyroid gland removed because of thyroid cance... | liquid | For detection of residueal or recurrent thyroid cancer | Binding of thyrotropin alfa to TSH receptors on normal thyroid epithelial cells or on well-differentiated thyroid cancer tissue stimulates iodine uptake and organification. Thyrogen is an exogenous source of human TSH that offers an additional diagnostic tool in the follow-up of patients with a history of well-differen... | Thyrotropin Alfa binds to the thyrotropin receptors found on any residual thyroid cells or tissues. This stimulates radioactive iodine uptake for better radiodiagnostic imaging. | Time to peak: Median: 10 hours (range: 3-24 hours)
After a single intramuscular injection of 0.9 mg of thyrotropin alfa: Cmax= 116+38mU/L, Tmax=22+8.5 hours. AUC=5088+1728 mU·hr/L. | null | No difference in efficacy and toxicity between adult and geriatric patients. No studies in lactating women, pregnant women and pediatrics. Cautionary administration is advised. | 25 ± 10 hours | null | kidney and liver | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"vet_approved"
] | [
"H01AB",
"H01A",
"H01",
"H"
] | [
"Humans and other mammals"
] | [
{
"cost": "1196.4",
"description": "Thyrogen 1.1 mg vial",
"unit": "vial"
}
] | [
{
"approved": "1998-11-24",
"country": "United States",
"expires": "2015-11-24",
"number": "5840566"
}
] | Recombinant Human Thyroid Stimulating Hormone | Recombinant thyrotropin alfa | rhTSH | rTSH | Thyrotropin alfa | Thyrotropin alpha | LGR3 | Thyroid-stimulating hormone receptor | TSH-R | [
"Thyrogen",
"Thyrogen",
"Thyrogen",
"Thyrogen",
"Thyrogen"
] | [] | [] | [
"P16473"
] | [] | [] | [] |
DB00025 | Antihemophilic factor, human recombinant | Human recombinant antihemophilic factor (AHF) or Factor VIII, 2332 residues, glycosylated, produced by CHO cells | solid | The human recombinant antihemophilic factor is indicated for use in adults and children with hemophilia A for the control and prevention of bleeding episodes, perioperative management, and routine prophylaxis to prevent or reduce the frequency of bleeding episodes.[L41025, L36130] | Antihemophilic Factor binds factor IXa along with calcium and phospholipid, This complex converts factor X to factor Xa to facilitate clotting cascade. | Antihemophilic factor (AHF) is a protein found in normal plasma which is necessary for clot formation. The administration of AHF provides an increase in plasma levels of AHF and can temporarily correct the coagulation defect of patients with hemophilia A (classical hemophilia). | null | null | null | 8.4-19.3 hrs | null | null | null | * 4.1 mL/h•kg [Previously treated pediatric patients] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"B02BD",
"B02B",
"B02",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "1.01",
"description": "Monoclate-p 1000 unit kit",
"unit": "kit"
},
{
"cost": "1.01",
"description": "Monoclate-p 1500 unit kit",
"unit": "kit"
},
{
"cost": "1.01",
"description": "Monoclate-p 250 unit kit",
"unit": "kit"
},
{
"cost": "1.01",
"descr... | [
{
"approved": "2007-09-11",
"country": "Canada",
"expires": "2013-10-01",
"number": "2124690"
},
{
"approved": "1997-09-23",
"country": "Canada",
"expires": "2014-09-23",
"number": "1339477"
}
] | Antihemophilic factor (recombinant) | Antihemophilic factor recombinant | Antihemophilic factor, human recombinant | Antihemophilic factor, recombinant | Coagulation factor VIII, recombinant | Factor VIII (rDNA) | Factor VIII (Recombinant) | Factor VIII recombin | Factor VIII, recombinant | Human Factor VIII (Recombina... | [
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Adv... | [
"Bioclate",
"Helixate",
"Hyate:C",
"Koate-HP",
"Kogenate",
"Monarc-M",
"ReFacto"
] | [] | [
"P00742",
"P00740",
"P04275",
"O14832",
"P07307",
"P11021",
"P27797",
"P27824",
"P49257",
"Q07954",
"Q8NI22"
] | [
"P00734",
"P04070"
] | [] | [] |
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