Identification
- Summary
Cobicistat is a CYP3A inhibitor used to increase the systemic exposure of atazanavir or darunavir in combination with other antiretroviral agents in the treatment of HIV-1 infection.
- Brand Names
- Evotaz, Genvoya, Prezcobix, Rezolsta, Stribild, Tybost
- Generic Name
- Cobicistat
- DrugBank Accession Number
- DB09065
- Background
Cobicistat, marketed under the name Tybost (formerly GS-9350), indicated for treating infection with human immunodeficiency virus (HIV). Although it does not have any anti-HIV activity, cobicistat acts as a pharmacokinetic enhancer by inhibiting cytochrome P450 3A isoforms (CYP3A) and therefore increases the systemic exposure of coadministered agents that are metabolized by CYP3A enzymes. More specifically, cobicistat is indicated to increase systemic exposure of atazanavir or darunavir (once daily dosing regimen) in combination with other antiretroviral agents in the treatment of HIV-1 infection. Increasing systemic exposure of anti-retrovirals (ARVs) without increasing dosage allows for better treatment outcomes and a decreased side effect profile.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Cobicistat (DB09065)
- Weight
- Average: 776.03
Monoisotopic: 775.354960183 - Chemical Formula
- C40H53N7O5S2
- Synonyms
- 1,3-thiazol-5-ylmethyl [(2R,5R)-5-{[(2S)-2-({[(2-isopropyl-1,3-thiazol-4-yl)methyl](methyl)carbamoyl}amino)-4-(morpholin-4-yl)butanoyl]amino}-1,6-diphenylhexan-2-yl]carbamate
- Cobicistat
- External IDs
- GS 9350
- GS-9350
- GS9350
Pharmacology
- Indication
Cobicistat is a CYP3A inhibitor indicated to increase systemic exposure of atazanavir or darunavir (once daily dosing regimen) in combination with other antiretroviral agents in the treatment of HIV-1 infection. It is not interchangeable with ritonavir to increase systemic exposure of darunavir 600 mg twice daily, fosamprenavir, saquinavir, or tipranavir due to lack of exposure data. The use of cobicistat is not recommended with darunavir 600 mg twice daily, fosamprenavir, saquinavir or tipranavir. Complex or unknown mechanisms of drug interactions preclude extrapolation of ritonavir drug interactions to certain cobicistat interactions. Cobicistat and ritonavir when administered with either atazanavir or darunavir may result in different drug interactions when used with concomitant medications.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used as adjunct in combination to manage Hiv-1 infection Combination Product in combination with: Atazanavir (DB01072) •••••••••••• Adjunct therapy in treatment of Hiv-1 infection •••••••••••• Used in combination to manage Hiv-1 infection Combination Product in combination with: Tenofovir alafenamide (DB09299), Emtricitabine (DB00879), Elvitegravir (DB09101) •••••••••••• Used as adjunct in combination to manage Hiv-1 infection Combination Product in combination with: Darunavir (DB01264) •••••••••••• Used in combination to manage Hiv-infection Combination Product in combination with: Tenofovir disoproxil (DB00300), Emtricitabine (DB00879), Elvitegravir (DB09101) •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Not Available
- Mechanism of action
Cobicistat is a mechanism-based inhibitor of cytochrome P450 3A (CYP3A) isoforms. Inhibition of CYP3A-mediated metabolism by cobicistat increases the systemic exposure of CYP3A substrates atazanavir and darunavir and therefore enables increased anti-viral activity at a lower dosage. Cobicistat does not have any anti-HIV activity on its own.
Target Actions Organism ACytochrome P450 3A4 inhibitorHumans ACytochrome P450 3A5 inhibitorHumans ACytochrome P450 3A7 inhibitorHumans - Absorption
Median peak plasma concentrations were observed at 3.5 hours post-dose.
- Volume of distribution
Not Available
- Protein binding
97-98% bound to human plasma proteins.
- Metabolism
Cobicistat is metabolized by CYP3A and to a minor extent by CYP2D6 enzymes and does not undergo glucuronidation.
- Route of elimination
With single dose administration of [14C] cobicistat after multiple dosing of cobicistat for six days, the mean percent of the administered dose excreted in feces and urine was 86.2% and 8.2%, respectively.
- Half-life
The terminal plasma half-life of cobicistat is approximately 3 to 4 hours.
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
The most common adverse reactions reported during clinical trials were jaundice (13%), ocular icterus (15%), and nausea (12%).
- 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 software1,2-Benzodiazepine The metabolism of 1,2-Benzodiazepine can be decreased when combined with Cobicistat. Abametapir The serum concentration of Cobicistat can be increased when it is combined with Abametapir. Abatacept The metabolism of Cobicistat can be increased when combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be decreased when combined with Cobicistat. Abiraterone The metabolism of Abiraterone can be decreased when combined with Cobicistat. - Food Interactions
- Avoid St. John's Wort. St. John's Wort is contraindicated as it induces the CYP3A metabolism of cobicistat and may reduce its serum concentration.
- Take at the same time every day.
- Take with 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 Tybost Tablet, film coated 150 mg/1 Oral Gilead Sciences, Inc. 2014-09-24 Not applicable US 
Tybost Tablet, film coated 150 mg Oral Gilead Sciences Ireland Uc 2016-09-08 Not applicable EU 
Tybost Tablet, film coated 150 mg Oral Gilead Sciences Ireland Uc 2016-09-08 Not applicable EU Tybost Tablet 150 mg Oral Gilead Sciences 2015-04-10 Not applicable Canada 
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Evotaz Cobicistat (150 mg/1) + Atazanavir sulfate (300 mg/1) Tablet Oral A-S Medication Solutions 2015-01-29 Not applicable US EVOTAZ Cobicistat (150 MG) + Atazanavir (300 MG) Tablet, film coated Oral Bristol Myers Squibb Pharma Eeig 2015-10-14 Not applicable Italy 
Evotaz Cobicistat (150 mg) + Atazanavir sulfate (300 mg) Tablet, film coated Oral Bristol Myers Squibb Pharma Eeig 2020-12-22 Not applicable EU Evotaz Cobicistat (150 mg/1) + Atazanavir sulfate (300 mg/1) Tablet Oral E.R. Squibb & Sons, L.L.C. 2015-01-29 Not applicable US Evotaz Cobicistat (150 mg) + Atazanavir sulfate (300 mg) Tablet Oral Bristol Myers Squibb 2016-02-11 2017-09-22 Canada
Categories
- ATC Codes
- J05AR09 — Emtricitabine, tenofovir disoproxil, elvitegravir and cobicistat
- J05AR — Antivirals for treatment of HIV infections, combinations
- J05A — DIRECT ACTING ANTIVIRALS
- J05 — ANTIVIRALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE
- J05AR — Antivirals for treatment of HIV infections, combinations
- J05A — DIRECT ACTING ANTIVIRALS
- J05 — ANTIVIRALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE
- J05AR — Antivirals for treatment of HIV infections, combinations
- J05A — DIRECT ACTING ANTIVIRALS
- J05 — ANTIVIRALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE
- J05AR — Antivirals for treatment of HIV infections, combinations
- J05A — DIRECT ACTING ANTIVIRALS
- J05 — ANTIVIRALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE
- J05AR — Antivirals for treatment of HIV infections, combinations
- J05A — DIRECT ACTING ANTIVIRALS
- J05 — ANTIVIRALS FOR SYSTEMIC USE
- J — ANTIINFECTIVES FOR SYSTEMIC USE
- Drug Categories
- Acids, Acyclic
- Anti-HIV Agents
- Anti-Infective Agents
- Antiinfectives for Systemic Use
- Antivirals used in combination for the treatment of HIV infections
- BCRP/ABCG2 Inhibitors
- Carbamates
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (weak)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A4 Inhibitors (strong)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Inhibitors
- Cytochrome P-450 CYP3A5 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A5 Inhibitors (strong)
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A7 Inhibitors
- Cytochrome P-450 CYP3A7 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A7 Inhibitors (strong)
- Cytochrome P-450 CYP3A7 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Enzyme Inhibitors
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B3 inhibitors
- Organic Anion Transporting Polypeptide 1B1 Inhibitors
- Organic Anion Transporting Polypeptide 1B3 Inhibitors
- Other Miscellaneous Therapeutic Agents
- P-glycoprotein inhibitors
- Sulfur Compounds
- Thiazoles
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as n-carbamoyl-alpha amino acids and derivatives. These are compounds containing an alpha amino acid (or a derivative thereof) which bears an carbamoyl group at its terminal nitrogen atom.
- Kingdom
- Organic compounds
- Super Class
- Organic acids and derivatives
- Class
- Carboxylic acids and derivatives
- Sub Class
- Amino acids, peptides, and analogues
- Direct Parent
- N-carbamoyl-alpha amino acids and derivatives
- Alternative Parents
- Alpha amino acid amides / Amphetamines and derivatives / 2,4-disubstituted thiazoles / N-acyl amines / Morpholines / Heteroaromatic compounds / Carbamate esters / Ureas / Trialkylamines / Secondary carboxylic acid amides show 7 more
- Substituents
- 2,4-disubstituted 1,3-thiazole / Alpha-amino acid amide / Amine / Amphetamine or derivatives / Aromatic heteromonocyclic compound / Azacycle / Azole / Benzenoid / Carbamic acid ester / Carbonic acid derivative show 26 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- carbamate ester, ureas, monocarboxylic acid amide, 1,3-thiazole, morpholines (CHEBI:72291)
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- LW2E03M5PG
- CAS number
- 1004316-88-4
- InChI Key
- ZCIGNRJZKPOIKD-CQXVEOKZSA-N
- InChI
- InChI=1S/C40H53N7O5S2/c1-29(2)38-43-34(27-53-38)25-46(3)39(49)45-36(16-17-47-18-20-51-21-19-47)37(48)42-32(22-30-10-6-4-7-11-30)14-15-33(23-31-12-8-5-9-13-31)44-40(50)52-26-35-24-41-28-54-35/h4-13,24,27-29,32-33,36H,14-23,25-26H2,1-3H3,(H,42,48)(H,44,50)(H,45,49)/t32-,33-,36+/m1/s1
- IUPAC Name
- (1,3-thiazol-5-yl)methyl N-[(2R,5R)-5-[(2S)-2-{[methyl({[2-(propan-2-yl)-1,3-thiazol-4-yl]methyl})carbamoyl]amino}-4-(morpholin-4-yl)butanamido]-1,6-diphenylhexan-2-yl]carbamate
- SMILES
- CC(C)C1=NC(CN(C)C(=O)N[C@@H](CCN2CCOCC2)C(=O)N[C@H](CC[C@H](CC2=CC=CC=C2)NC(=O)OCC2=CN=CS2)CC2=CC=CC=C2)=CS1
References
- General References
- German P, Warren D, West S, Hui J, Kearney BP: Pharmacokinetics and bioavailability of an integrase and novel pharmacoenhancer-containing single-tablet fixed-dose combination regimen for the treatment of HIV. J Acquir Immune Defic Syndr. 2010 Nov;55(3):323-9. doi: 10.1097/QAI.0b013e3181eb376b. [Article]
- Mathias AA, German P, Murray BP, Wei L, Jain A, West S, Warren D, Hui J, Kearney BP: Pharmacokinetics and pharmacodynamics of GS-9350: a novel pharmacokinetic enhancer without anti-HIV activity. Clin Pharmacol Ther. 2010 Mar;87(3):322-9. doi: 10.1038/clpt.2009.228. Epub 2009 Dec 30. [Article]
- Larson KB, Wang K, Delille C, Otofokun I, Acosta EP: Pharmacokinetic enhancers in HIV therapeutics. Clin Pharmacokinet. 2014 Oct;53(10):865-72. doi: 10.1007/s40262-014-0167-9. [Article]
- Lepist EI, Phan TK, Roy A, Tong L, Maclennan K, Murray B, Ray AS: Cobicistat boosts the intestinal absorption of transport substrates, including HIV protease inhibitors and GS-7340, in vitro. Antimicrob Agents Chemother. 2012 Oct;56(10):5409-13. doi: 10.1128/AAC.01089-12. Epub 2012 Jul 30. [Article]
- External Links
- KEGG Drug
- D09881
- PubChem Compound
- 25151504
- PubChem Substance
- 310264999
- ChemSpider
- 25084912
- BindingDB
- 50447471
- 1306284
- ChEBI
- 72291
- ChEMBL
- CHEMBL2095208
- ZINC
- ZINC000085537014
- PharmGKB
- PA166165092
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Cobicistat
- FDA label
- Download (467 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 Active Not Recruiting Treatment Human Immunodeficiency Virus Type 1 (HIV-1) Infection 1 4 Completed Basic Science Abnormality of Adipose Tissue / Antiviral Drug Adverse Reaction / Body Fat Disorder / Cardiovascular Abnormalities / HIV Lipodystrophy Syndrome / Human Immunodeficiency Virus Type 1 (HIV-1) Infection / Vascular Diseases / Weight Changes 1 4 Completed Health Services Research Human Immunodeficiency Virus (HIV) Infections 1 4 Completed Other Healthy Subjects (HS) 2 4 Completed Other Human Immunodeficiency Virus (HIV) Infections 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral Tablet, coated Oral Tablet, film coated Oral Tablet, film coated Oral 150 mg Tablet Oral 800.000 mg Tablet Oral 150 mg Tablet, film coated Oral 150 MG Tablet, film coated Oral 150 mg/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US7800788 No 2010-09-21 2022-02-02 US US5914331 Yes 1999-06-22 2018-01-02 US US6043230 Yes 2000-03-28 2018-01-25 US US5814639 Yes 1998-09-29 2017-03-29 US US6642245 Yes 2003-11-04 2021-05-04 US US6703396 Yes 2004-03-09 2021-09-09 US US5922695 Yes 1999-07-13 2018-01-25 US US5935946 Yes 1999-08-10 2018-01-25 US US5977089 Yes 1999-11-02 2018-01-25 US US8592397 No 2013-11-26 2024-01-13 US US8716264 No 2014-05-06 2024-01-13 US US5843946 Yes 1998-12-01 2016-06-01 US US7470506 Yes 2008-12-30 2019-12-23 US USRE43802 Yes 2012-11-13 2017-04-19 US US8597876 Yes 2013-12-03 2019-12-23 US US7700645 Yes 2010-04-20 2027-06-26 US USRE42889 Yes 2011-11-01 2017-04-19 US US8518987 Yes 2013-08-27 2024-08-16 US USRE43596 Yes 2012-08-21 2017-11-09 US US5849911 Yes 1998-12-15 2017-12-20 US US6087383 Yes 2000-07-11 2019-06-21 US US8148374 Yes 2012-04-03 2030-03-03 US US7635704 Yes 2009-12-22 2027-04-26 US US7176220 Yes 2007-02-13 2027-02-27 US US8981103 Yes 2015-03-17 2027-04-26 US US8633219 Yes 2014-01-21 2030-10-24 US US9296769 Yes 2016-03-29 2033-02-15 US US7803788 No 2010-09-28 2022-02-02 US US8754065 Yes 2014-06-17 2033-02-15 US US7390791 Yes 2008-06-24 2025-10-17 US US9457036 No 2016-10-04 2024-01-13 US US9744181 No 2017-08-29 2024-01-13 US US9891239 Yes 2018-02-13 2030-03-03 US US9889115 Yes 2018-02-13 2019-12-23 US US10039718 Yes 2018-08-07 2033-04-06 US US10786515 No 2020-09-29 2038-07-19 US US10786518 No 2020-09-29 2038-07-19 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility 0.1 mg/mL FDA Label - Predicted Properties
Property Value Source Water Solubility 0.00125 mg/mL ALOGPS logP 4.36 ALOGPS logP 4.99 Chemaxon logS -5.8 ALOGPS pKa (Strongest Acidic) 14.18 Chemaxon pKa (Strongest Basic) 6.69 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 7 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 138.02 Å2 Chemaxon Rotatable Bond Count 20 Chemaxon Refractivity 211.49 m3·mol-1 Chemaxon Polarizability 83.42 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]- 296.9942714 predictedDarkChem Lite v0.1.0 [M-H]- 258.8442 predictedDeepCCS 1.0 (2019) [M+H]+ 299.4908714 predictedDarkChem Lite v0.1.0 [M+H]+ 260.77182 predictedDeepCCS 1.0 (2019) [M+Na]+ 298.0614714 predictedDarkChem Lite v0.1.0 [M+Na]+ 266.5122 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- 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
- Mathias AA, German P, Murray BP, Wei L, Jain A, West S, Warren D, Hui J, Kearney BP: Pharmacokinetics and pharmacodynamics of GS-9350: a novel pharmacokinetic enhancer without anti-HIV activity. Clin Pharmacol Ther. 2010 Mar;87(3):322-9. doi: 10.1038/clpt.2009.228. Epub 2009 Dec 30. [Article]
- Nanda K, Stuart GS, Robinson J, Gray AL, Tepper NK, Gaffield ME: Drug interactions between hormonal contraceptives and antiretrovirals. AIDS. 2017 Apr 24;31(7):917-952. doi: 10.1097/QAD.0000000000001392. [Article]
- Wang P, Shehu AI, Liu K, Lu J, Ma X: Biotransformation of Cobicistat: Metabolic Pathways and Enzymes. Drug Metab Lett. 2016;10(2):111-23. [Article]
- FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
- Cobicistat FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- 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
- Mathias AA, German P, Murray BP, Wei L, Jain A, West S, Warren D, Hui J, Kearney BP: Pharmacokinetics and pharmacodynamics of GS-9350: a novel pharmacokinetic enhancer without anti-HIV activity. Clin Pharmacol Ther. 2010 Mar;87(3):322-9. doi: 10.1038/clpt.2009.228. Epub 2009 Dec 30. [Article]
- Tseng A, Hughes CA, Wu J, Seet J, Phillips EJ: Cobicistat Versus Ritonavir: Similar Pharmacokinetic Enhancers But Some Important Differences. Ann Pharmacother. 2017 Nov;51(11):1008-1022. doi: 10.1177/1060028017717018. Epub 2017 Jun 19. [Article]
- Cobicistat FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- 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
- CYP3A7
- Uniprot ID
- P24462
- Uniprot Name
- Cytochrome P450 3A7
- Molecular Weight
- 57525.03 Da
References
- Tseng A, Hughes CA, Wu J, Seet J, Phillips EJ: Cobicistat Versus Ritonavir: Similar Pharmacokinetic Enhancers But Some Important Differences. Ann Pharmacother. 2017 Nov;51(11):1008-1022. doi: 10.1177/1060028017717018. Epub 2017 Jun 19. [Article]
- Mathias AA, German P, Murray BP, Wei L, Jain A, West S, Warren D, Hui J, Kearney BP: Pharmacokinetics and pharmacodynamics of GS-9350: a novel pharmacokinetic enhancer without anti-HIV activity. Clin Pharmacol Ther. 2010 Mar;87(3):322-9. doi: 10.1038/clpt.2009.228. Epub 2009 Dec 30. [Article]
- Cobicistat FDA Label [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- 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
- Mathias AA, German P, Murray BP, Wei L, Jain A, West S, Warren D, Hui J, Kearney BP: Pharmacokinetics and pharmacodynamics of GS-9350: a novel pharmacokinetic enhancer without anti-HIV activity. Clin Pharmacol Ther. 2010 Mar;87(3):322-9. doi: 10.1038/clpt.2009.228. Epub 2009 Dec 30. [Article]
- Cobicistat FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- 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
- CYP3A7
- Uniprot ID
- P24462
- Uniprot Name
- Cytochrome P450 3A7
- Molecular Weight
- 57525.03 Da
References
- Mathias AA, German P, Murray BP, Wei L, Jain A, West S, Warren D, Hui J, Kearney BP: Pharmacokinetics and pharmacodynamics of GS-9350: a novel pharmacokinetic enhancer without anti-HIV activity. Clin Pharmacol Ther. 2010 Mar;87(3):322-9. doi: 10.1038/clpt.2009.228. Epub 2009 Dec 30. [Article]
- Cobicistat FDA Label [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
- Mathias AA, German P, Murray BP, Wei L, Jain A, West S, Warren D, Hui J, Kearney BP: Pharmacokinetics and pharmacodynamics of GS-9350: a novel pharmacokinetic enhancer without anti-HIV activity. Clin Pharmacol Ther. 2010 Mar;87(3):322-9. doi: 10.1038/clpt.2009.228. Epub 2009 Dec 30. [Article]
- Cobicistat versus ritonavir boosting and differences in the drug–drug interaction profiles with co-medications [Link]
- Cobicistat FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- 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
- Tseng A, Hughes CA, Wu J, Seet J, Phillips EJ: Cobicistat Versus Ritonavir: Similar Pharmacokinetic Enhancers But Some Important Differences. Ann Pharmacother. 2017 Nov;51(11):1008-1022. doi: 10.1177/1060028017717018. Epub 2017 Jun 19. [Article]
- Mathias AA, German P, Murray BP, Wei L, Jain A, West S, Warren D, Hui J, Kearney BP: Pharmacokinetics and pharmacodynamics of GS-9350: a novel pharmacokinetic enhancer without anti-HIV activity. Clin Pharmacol Ther. 2010 Mar;87(3):322-9. doi: 10.1038/clpt.2009.228. Epub 2009 Dec 30. [Article]
- Cobicistat FDA Label [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- 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
- Lepist EI, Phan TK, Roy A, Tong L, Maclennan K, Murray B, Ray AS: Cobicistat boosts the intestinal absorption of transport substrates, including HIV protease inhibitors and GS-7340, in vitro. Antimicrob Agents Chemother. 2012 Oct;56(10):5409-13. doi: 10.1128/AAC.01089-12. Epub 2012 Jul 30. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
- Gene Name
- ABCG2
- Uniprot ID
- Q9UNQ0
- Uniprot Name
- ATP-binding cassette sub-family G member 2
- Molecular Weight
- 72313.47 Da
References
- Lepist EI, Phan TK, Roy A, Tong L, Maclennan K, Murray B, Ray AS: Cobicistat boosts the intestinal absorption of transport substrates, including HIV protease inhibitors and GS-7340, in vitro. Antimicrob Agents Chemother. 2012 Oct;56(10):5409-13. doi: 10.1128/AAC.01089-12. Epub 2012 Jul 30. [Article]
- 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 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
- 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
Drug created at May 11, 2015 22:33 / Updated at February 20, 2024 23:55