Identification
- Summary
Asunaprevir is an NS3 protease inhibitor used to treat hepatitis C genotype 1b.
- Generic Name
- Asunaprevir
- DrugBank Accession Number
- DB11586
- Background
Asunaprevir, also named BMS-650032, is a potent hepatitis C virus (HCV) NS3 protease inhibitor. It has been shown to have a very high efficacy in dual-combination regimens with daclatasvir in patients chronically infected with HCV genotype 1b.2 It was developed by Bristol-Myers Squibb Canada and approved by Health Canada on April 22, 2016. The commercialization of asunaprevir was cancelled one year later on October 16, 2017.4
- Type
- Small Molecule
- Groups
- Approved, Investigational, Withdrawn
- Structure
Structure for Asunaprevir (DB11586)
- Weight
- Average: 748.286
Monoisotopic: 747.270476492 - Chemical Formula
- C35H46ClN5O9S
- Synonyms
- Asunaprevir
- External IDs
- BMS 650032
- BMS-650032
Pharmacology
- Indication
Asunaprevir is indicated in combination with other agents for the treatment of chronic hepatitis C in adult patients with hepatitis C virus genotypes 1 or 4 and compensated liver cirrhosis.5
Hepatitis C is a liver disease caused by the hepatitis C virus. The chronic state of this condition accounts for 60-80% of the cases from which the risk of cirrhosis of the liver within 20 years is of around 15-30%.6 The genotype 1 is the most common type of hepatitis C in the United States and the most difficult to treat.7
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat Chronic hepatitis c genotype 1 •••••••••••• ••••• Used in combination to treat Chronic hepatitis c genotype 4 •••••••••••• ••••• - Contraindications & Blackbox Warnings
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Studies in vitro demonstrated a significant antiviral activity in HCV replicon cell systems with an EC50 of 4nm and 1nm against the HCV genotype 1a and 1b respectively.2 These studies showed a limited activity against the genotypes 2 and 3. This property makes asunaprevir a highly selective anti-HCV agent that is not effective against HCV closely related virus.3 Asunaprevir produce robust declines in HCV RNA levels in patients with HCV genotype 1 infection.1In clinical studies, it has been shown that asunaprevir is well-tolerated and the mean maximum HCV RNA level reduction from baseline was of approximately 2.87 log10 IU/ml.2
Monotherapy clinical studies with asunaprevir showed a mean maximum decline of HCV RNA in the range of 0.28-2.87 log10 IU/ml when administered in increasing doses from 10-600 mg. When asunaprevir was used as a combination product, it was possible to obtain a sustained virological response (aviremia 24 weeks after completion of therapy) in 83-92% of the patients.3
- Mechanism of action
Asunaprevir is a highly active HCV NS3 protease inhibitor.1 The genome of HCV has a positive polarity which allows it to be translated into a protein in the host cell without further transformation steps. However, the resultant protein needs to be divided by the enzyme NS3 protease into single proteins in order to be able to exert its enzymatic activity or structural role. Therefore, due to NS3 vital importance for viral replication, the inhibiting action of asunaprevir causes a robust antiviral activity.3
Target Actions Organism AGenome polyprotein inhibitorHepatitis C virus genotype 1b (isolate BK) - Absorption
In preclinical studies, asunaprevir showed a high liver-to-plasma AUC ratio. It is rapidly absorbed within 30 minutes of administration.5 Clinical pharmacokinetic studies showed a Tmax of 2-4 hours.3 The pharmacokinetic profile act in a dose-proportional manner and in a dose of 100 mg the steady-state Cmax and AUC was 572 ng/ml and 1887 ng x h/mL. The absolute bioavailability is reported to be 9.3%. The absorption of asunaprevir is increased with food.8
- Volume of distribution
The registered volume of distribution at steady state is 194 L.8
- Protein binding
Protein binding of asunaprevir is very high and it can reach more than 99% of the administered dose independently of the dose. In vitro studies with human Caco-2 cells indicated that asunaprevir is a substrate of P-gp, OATP1B1 and OATP2B1.8
- Metabolism
Asunaprevir is metabolized by the liver.3 The metabolism is mainly marked by oxidative reactions mediated by the activity of CYP3A.8 Asunaprevir seems to weakly induce its own metabolism and from the circulating dose, just about 5% of the administered dose is formed by metabolites.5 The metabolites of asunaprevir are formed after mono- and bis-oxidation, N-dealkylation, loss of isoquinoline ring and O-demethylation. All the metabolic reactions form about 15 metabolites and studies have reported that the main metabolic activity is performed by CYP3A4 and CYP3A5 with some minor activity from CYP2A6, CYP2B6, CYP2C9, CYP2C19 and CYP2D6.8
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- Route of elimination
Asunaprevir is primarily eliminated via the feces.3 From the administered dose, 84% is excreted by feces mainly as metabolites and less than 1% of the dose is recovered as metabolites in the urine. The proportion of unchanged asunaprevir recovered in feces represents only 7.5% of the dose.8
- Half-life
Clinical pharmacokinetic studies showed a mean terminal half-life of 15-20 hours.3
- Clearance
Clinical pharmacokinetic studies showed a mean oral clearance of 302-491 L/h.3
- Adverse Effects
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Toxicity studies showed no carcinogenic nor genotoxic potential related to asunaprevir. In the case of overdose, clinical studies reported no unexpected adverse events.8 Asunaprevir had no effects on fertility in preclinical studies. It has been shown that asunaprevir gets localized in the GI tract and liver and thus, increased hepatic transaminases were observed as well as changes in iron metabolism and decreased serum proteins. These effects are not progressive and asunaprevir was generally well tolerated.5
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Asunaprevir can be increased when it is combined with Abametapir. Abatacept The metabolism of Asunaprevir can be increased when combined with Abatacept. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Asunaprevir. Abiraterone The metabolism of Asunaprevir can be decreased when combined with Abiraterone. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Asunaprevir. - Food Interactions
- Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of asunaprevir. Co-administration of asunaprevir with St. John's Wort is contraindicated.
- Exercise caution with grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of asunaprevir.
- Take with or without food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Sunvepra Capsule 100 mg Oral Bristol Myers Squibb 2016-04-22 2017-10-16 Canada 
Categories
- ATC Codes
- J05AP06 — Asunaprevir
- J05AP — Antivirals for treatment of HCV infections
- J05A — DIRECT ACTING ANTIVIRALS
- J05 — ANTIVIRALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE
- Drug Categories
- Amides
- Antiinfectives for Systemic Use
- Antiviral Agents
- Antivirals for Systemic Use
- Antivirals for treatment of HCV infections
- Cytochrome P-450 CYP2A6 Substrates
- Cytochrome P-450 CYP2B6 Substrates
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C9 Substrates
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (moderate)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (weak)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Inducers
- Cytochrome P-450 CYP3A5 Inducers (weak)
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Direct Acting Antivirals
- Enzyme Inhibitors
- HCV Protease Inhibitors
- Heterocyclic Compounds, Fused-Ring
- HIV Protease Inhibitors
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B1/SLCO1B1 Substrates
- OATP1B3 inhibitors
- OATP2B1/SLCO2B1 substrates
- Organic Anion Transporting Polypeptide 2B1 Inhibitors
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Protease Inhibitors
- Sulfones
- Sulfur Compounds
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as oligopeptides. These are organic compounds containing a sequence of between three and ten alpha-amino acids joined by peptide bonds.
- Kingdom
- Organic compounds
- Super Class
- Organic acids and derivatives
- Class
- Carboxylic acids and derivatives
- Sub Class
- Amino acids, peptides, and analogues
- Direct Parent
- Oligopeptides
- Alternative Parents
- Valine and derivatives / Proline and derivatives / N-acyl-alpha amino acids and derivatives / Alpha amino acid amides / Isoquinolines and derivatives / Pyrrolidinecarboxamides / N-acylpyrrolidines / Alkyl aryl ethers / Pyridines and derivatives / Aryl chlorides show 16 more
- Substituents
- Alkyl aryl ether / Alpha-amino acid amide / Alpha-amino acid or derivatives / Alpha-oligopeptide / Aminosulfonyl compound / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid show 32 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Hepatitis C Virus
Chemical Identifiers
- UNII
- S9X0KRJ00S
- CAS number
- 630420-16-5
- InChI Key
- XRWSZZJLZRKHHD-WVWIJVSJSA-N
- InChI
- InChI=1S/C35H46ClN5O9S/c1-9-19-16-35(19,31(44)40-51(46,47)22-11-12-22)39-28(42)25-15-21(49-29-24-14-20(36)10-13-23(24)26(48-8)17-37-29)18-41(25)30(43)27(33(2,3)4)38-32(45)50-34(5,6)7/h9-10,13-14,17,19,21-22,25,27H,1,11-12,15-16,18H2,2-8H3,(H,38,45)(H,39,42)(H,40,44)/t19-,21-,25+,27-,35-/m1/s1
- IUPAC Name
- tert-butyl N-[(2S)-1-[(2S,4R)-4-[(7-chloro-4-methoxyisoquinolin-1-yl)oxy]-2-{[(1R,2S)-1-[(cyclopropanesulfonyl)carbamoyl]-2-ethenylcyclopropyl]carbamoyl}pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]carbamate
- SMILES
- COC1=CN=C(O[C@@H]2C[C@H](N(C2)C(=O)[C@@H](NC(=O)OC(C)(C)C)C(C)(C)C)C(=O)N[C@@]2(C[C@H]2C=C)C(=O)NS(=O)(=O)C2CC2)C2=C1C=CC(Cl)=C2
References
- General References
- Lok AS, Gardiner DF, Lawitz E, Martorell C, Everson GT, Ghalib R, Reindollar R, Rustgi V, McPhee F, Wind-Rotolo M, Persson A, Zhu K, Dimitrova DI, Eley T, Guo T, Grasela DM, Pasquinelli C: Preliminary study of two antiviral agents for hepatitis C genotype 1. N Engl J Med. 2012 Jan 19;366(3):216-24. doi: 10.1056/NEJMoa1104430. [Article]
- McPhee F, Friborg J, Levine S, Chen C, Falk P, Yu F, Hernandez D, Lee MS, Chaniewski S, Sheaffer AK, Pasquinelli C: Resistance analysis of the hepatitis C virus NS3 protease inhibitor asunaprevir. Antimicrob Agents Chemother. 2012 Jul;56(7):3670-81. doi: 10.1128/AAC.00308-12. Epub 2012 Apr 16. [Article]
- Gentile I, Buonomo AR, Zappulo E, Minei G, Morisco F, Borrelli F, Coppola N, Borgia G: Asunaprevir, a protease inhibitor for the treatment of hepatitis C infection. Ther Clin Risk Manag. 2014 Jun 26;10:493-504. doi: 10.2147/TCRM.S66731. eCollection 2014. [Article]
- Health Canada [Link]
- Health Canada Approved Drug Products: Sunvepra (asunaprevir) capsule [Link]
- WHO [Link]
- HepatitisCentral [Link]
- Australian Therapeutic Goods Administration: Australian Public Assessment Report for asunaprevir [Link]
- External Links
- PubChem Compound
- 16076883
- PubChem Substance
- 347827994
- ChemSpider
- 17235944
- BindingDB
- 50287594
- 1652103
- ChEBI
- 134723
- ChEMBL
- CHEMBL2105735
- ZINC
- ZINC000085540202
- PharmGKB
- PA166128168
- PDBe Ligand
- 2R9
- Wikipedia
- Asunaprevir
- PDB Entries
- 4nwl / 4wf8 / 4wh6 / 5eqs
- MSDS
- Download (23.7 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Treatment Hepatitis C Virus (HCV) Infection 1 4 Unknown Status Treatment Chronic Hepatitis C Virus (HCV) Infection 1 4 Withdrawn Treatment Chronic Hepatitis C Virus (HCV) Infection 1 3 Completed Basic Science Chronic Hepatitis C Virus (HCV) Infection 1 3 Completed Treatment Hepatitis C Virus (HCV) Infection 7
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule Not applicable 100 mg/1 Capsule Oral 100 mg Capsule, liquid filled Oral 100 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 145-155 ºC 'MSDS water solubility <50 mg/L Australian Public Assessment - Predicted Properties
Property Value Source Water Solubility 0.00299 mg/mL ALOGPS logP 3.12 ALOGPS logP 3.37 Chemaxon logS -5.4 ALOGPS pKa (Strongest Acidic) 3.77 Chemaxon pKa (Strongest Basic) 1.85 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 9 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 182.33 Å2 Chemaxon Rotatable Bond Count 13 Chemaxon Refractivity 186.82 m3·mol-1 Chemaxon Polarizability 76.14 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 240.46361 predictedDeepCCS 1.0 (2019) [M+H]+ 242.18736 predictedDeepCCS 1.0 (2019) [M+Na]+ 248.51631 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Hepatitis C virus genotype 1b (isolate BK)
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Zinc ion binding
- Specific Function
- Core protein packages viral RNA to form a viral nucleocapsid, and promotes virion budding. Modulates viral translation initiation by interacting with HCV IRES and 40S ribosomal subunit. Also regula...
- Gene Name
- Not Available
- Uniprot ID
- P26663
- Uniprot Name
- Genome polyprotein
- Molecular Weight
- 327190.435 Da
References
- Gentile I, Buonomo AR, Zappulo E, Minei G, Morisco F, Borrelli F, Coppola N, Borgia G: Asunaprevir, a protease inhibitor for the treatment of hepatitis C infection. Ther Clin Risk Manag. 2014 Jun 26;10:493-504. doi: 10.2147/TCRM.S66731. eCollection 2014. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInducer
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Australian Therapeutic Goods Administration: Australian Public Assessment Report for asunaprevir [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInducer
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Australian Therapeutic Goods Administration: Australian Public Assessment Report for asunaprevir [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
- Gene Name
- CYP2A6
- Uniprot ID
- P11509
- Uniprot Name
- Cytochrome P450 2A6
- Molecular Weight
- 56501.005 Da
References
- Australian Therapeutic Goods Administration: Australian Public Assessment Report for asunaprevir [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- Australian Therapeutic Goods Administration: Australian Public Assessment Report for asunaprevir [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Australian Therapeutic Goods Administration: Australian Public Assessment Report for asunaprevir [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- Australian Therapeutic Goods Administration: Australian Public Assessment Report for asunaprevir [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Eley T, Garimella T, Li W, Bertz RJ: Asunaprevir: A Review of Preclinical and Clinical Pharmacokinetics and Drug-Drug Interactions. Clin Pharmacokinet. 2015 Dec;54(12):1205-22. doi: 10.1007/s40262-015-0299-6. [Article]
- Australian Therapeutic Goods Administration: Australian Public Assessment Report for asunaprevir [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
- Gene Name
- SLCO1B1
- Uniprot ID
- Q9Y6L6
- Uniprot Name
- Solute carrier organic anion transporter family member 1B1
- Molecular Weight
- 76447.99 Da
References
- Eley T, Han YH, Huang SP, He B, Li W, Bedford W, Stonier M, Gardiner D, Sims K, Rodrigues AD, Bertz RJ: Organic anion transporting polypeptide-mediated transport of, and inhibition by, asunaprevir, an inhibitor of hepatitis C virus NS3 protease. Clin Pharmacol Ther. 2015 Feb;97(2):159-66. doi: 10.1002/cpt.4. Epub 2014 Dec 20. [Article]
- FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
- Medicines.org: SUNVEPRA® asunaprevir PRODUCT INFORMATION [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
- Gene Name
- SLCO1B3
- Uniprot ID
- Q9NPD5
- Uniprot Name
- Solute carrier organic anion transporter family member 1B3
- Molecular Weight
- 77402.175 Da
References
- Eley T, Han YH, Huang SP, He B, Li W, Bedford W, Stonier M, Gardiner D, Sims K, Rodrigues AD, Bertz RJ: Organic anion transporting polypeptide-mediated transport of, and inhibition by, asunaprevir, an inhibitor of hepatitis C virus NS3 protease. Clin Pharmacol Ther. 2015 Feb;97(2):159-66. doi: 10.1002/cpt.4. Epub 2014 Dec 20. [Article]
- FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
- Medicines.org: SUNVEPRA® asunaprevir PRODUCT INFORMATION [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
- Gene Name
- SLCO2B1
- Uniprot ID
- O94956
- Uniprot Name
- Solute carrier organic anion transporter family member 2B1
- Molecular Weight
- 76709.98 Da
References
- Eley T, Han YH, Huang SP, He B, Li W, Bedford W, Stonier M, Gardiner D, Sims K, Rodrigues AD, Bertz RJ: Organic anion transporting polypeptide-mediated transport of, and inhibition by, asunaprevir, an inhibitor of hepatitis C virus NS3 protease. Clin Pharmacol Ther. 2015 Feb;97(2):159-66. doi: 10.1002/cpt.4. Epub 2014 Dec 20. [Article]
- Australian Therapeutic Goods Administration: Australian Public Assessment Report for asunaprevir [Link]
- Medicines.org: SUNVEPRA® asunaprevir PRODUCT INFORMATION [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Australian Therapeutic Goods Administration: Australian Public Assessment Report for asunaprevir [Link]
Drug created at April 27, 2016 23:10 / Updated at February 20, 2024 23:54