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Cobicistat

Generic Name
Cobicistat
Brand Names
Evotaz, Genvoya, Prezcobix, Rezolsta, Stribild, Tybost
Drug Type
Small Molecule
Chemical Formula
C40H53N7O5S2
CAS Number
1004316-88-4
Unique Ingredient Identifier
LW2E03M5PG
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.

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.

Associated Conditions
Human Immunodeficiency Virus (HIV) Infections, Human Immunodeficiency Virus Type 1 (HIV-1) Infection
Associated Therapies
-

Effect of Cobicistat Versus Ritonavir Boosting on the Brain Permeation of Darunavir in HIV-infected Individuals

Phase 4
Terminated
Conditions
AIDS-related Dementia Complex
Interventions
First Posted Date
2015-07-21
Last Posted Date
2017-02-02
Lead Sponsor
University Hospital, Basel, Switzerland
Target Recruit Count
7
Registration Number
NCT02503462
Locations
🇨🇭

Division of Infectious Diseases, University Hospital Basel, Basel, BS, Switzerland

Relative Bioavailability and Food Effect for Darunavir/Cobicistat/Emtricitabine/Tenofovir Alafenamide Fixed Dose Combination

Phase 1
Completed
Conditions
Healthy
Interventions
Drug: Darunavir/Cobicistat/Emtricitabine/Tenofovir alafenamide FDC
Drug: Elvitegravir /Cobicistat/Emtricitabine/Tenofovir alafenamide FDC
Other: High-fat Breakfast
Drug: Darunavir
Drug: Emtricitabine/Tenofovir alafenamide (FTC/TAF)
Drug: Cobicistat
Other: Standardized Regular Breakfast
First Posted Date
2015-06-18
Last Posted Date
2017-10-17
Lead Sponsor
Janssen Sciences Ireland UC
Target Recruit Count
72
Registration Number
NCT02475135

Taste Properties of Atazanavir and Cobicistat

Phase 1
Completed
Conditions
HIV in Adults
Interventions
Drug: Atazanavir
Drug: Cobicistat
Drug: Active Pharmaceutical Ingredient
First Posted Date
2014-12-04
Last Posted Date
2022-01-05
Lead Sponsor
Bristol-Myers Squibb
Target Recruit Count
6
Registration Number
NCT02307656
Locations
🇺🇸

Senopsys Llc, Woburn, Massachusetts, United States

A Phase 1 Antiretroviral Drug-Drug Interaction Study in Healthy Volunteers (DDI)

Phase 1
Completed
Conditions
Infection, Human Immunodeficiency Virus
Interventions
First Posted Date
2014-10-29
Last Posted Date
2018-01-24
Lead Sponsor
ViiV Healthcare
Target Recruit Count
32
Registration Number
NCT02277600
Locations
🇺🇸

GSK Investigational Site, San Antonio, Texas, United States

Study of Cobicistat-Boosted Atazanavir (ATV/co), Cobicistat-Boosted Darunavir (DRV/co) and Emtricitabine/Tenofovir Alafenamide (F/TAF) in Children With HIV

Phase 2
Recruiting
Conditions
Acquired Immune Deficiency Syndrome (AIDS)
HIV Infections
Interventions
Drug: ATV
Drug: Third Unboosted Drug
Drug: DRV
Drug: LPV/r
Drug: Cobicistat TOS
Drug: Cobicistat
Drug: F/TAF
Drug: BR
Drug: F/TAF TOS
First Posted Date
2013-12-20
Last Posted Date
2024-11-20
Lead Sponsor
Gilead Sciences
Target Recruit Count
130
Registration Number
NCT02016924
Locations
🇹🇭

Siriraj Hospital, Bangkok, Thailand

🇹🇭

Srinagarind Hospital, Khon Kaen, Thailand

🇹🇭

Queen Savang Vadhana Memorial Hospital, Sriracha, Thailand

and more 31 locations

The Interaction of Two HIV Medications With Blood Clot Medications in Healthy Volunteers

Phase 1
Completed
Conditions
HIV
Interventions
First Posted Date
2013-07-11
Last Posted Date
2017-07-02
Lead Sponsor
National Institutes of Health Clinical Center (CC)
Target Recruit Count
40
Registration Number
NCT01896622
Locations
🇺🇸

National Institutes of Health Clinical Center, 9000 Rockville Pike, Bethesda, Maryland, United States

Bioequivalence Study of Individual Atazanavir and Cobicistat Compared With Atazanavir in Fixed-dose Combination With Cobicistat

Phase 1
Completed
Conditions
Human Immunodeficiency Virus Type 1 (HIV-1)
Interventions
Drug: Atazanavir/Cobicistat FDC
Drug: Atazanavir
Drug: Cobicistat
First Posted Date
2013-04-23
Last Posted Date
2014-08-29
Lead Sponsor
Bristol-Myers Squibb
Target Recruit Count
64
Registration Number
NCT01837719
Locations
🇺🇸

Ppd Development, Inc., Austin, Texas, United States

A Study to Assess the Bioequivalence of Darunavir When Co-Administrated With Cobicistat Under Fed and Fasted Conditions

Phase 1
Completed
Conditions
Healthy Participants
Interventions
First Posted Date
2012-06-14
Last Posted Date
2013-03-04
Lead Sponsor
Janssen R&D Ireland
Target Recruit Count
133
Registration Number
NCT01619527
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