Overview
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.
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
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2024/12/10 | Phase 1 | Not yet recruiting | |||
2024/04/25 | Phase 1 | Completed | Fore Biotherapeutics | ||
2024/03/29 | Phase 4 | Recruiting | |||
2023/08/28 | Phase 2 | Recruiting | Stichting Hemato-Oncologie voor Volwassenen Nederland | ||
2023/02/28 | Phase 4 | Recruiting | |||
2023/02/08 | Phase 1 | Completed | Food and Drug Administration (FDA) | ||
2023/01/20 | Phase 1 | Completed | Pyramid Biosciences | ||
2022/08/17 | Phase 2 | Recruiting | Fore Biotherapeutics | ||
2022/08/10 | Phase 1 | Terminated | |||
2022/07/14 | Phase 1 | Terminated |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Janssen Products LP | 59676-800 | ORAL | 150 mg in 1 1 | 8/18/2023 | |
| Avera McKennan Hospital | 69189-1201 | ORAL | 150 mg in 1 1 | 3/20/2017 | |
| State of Florida DOH Central Pharmacy | 53808-0887 | ORAL | 150 mg in 1 1 | 3/6/2014 | |
| Janssen Products LP | 59676-575 | ORAL | 150 mg in 1 1 | 8/15/2023 | |
| Gilead Sciences, Inc. | 61958-1901 | ORAL | 150 mg in 1 1 | 1/13/2022 | |
| Gilead Sciences, Inc. | 61958-1201 | ORAL | 150 mg in 1 1 | 9/16/2021 | |
| Gilead Sciences, Inc. | 61958-1401 | ORAL | 150 mg in 1 1 | 9/15/2021 | |
| A-S Medication Solutions | 50090-1723 | ORAL | 150 mg in 1 1 | 8/15/2023 | |
| Gilead Sciences, Inc. | 61958-1202 | ORAL | 150 mg in 1 1 | 11/24/2018 | |
| E.R. Squibb & Sons, L.L.C. | 0003-3641 | ORAL | 150 mg in 1 1 | 7/31/2020 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 9/19/2013 | ||
Authorised | 11/19/2015 | ||
Authorised | 7/13/2015 | ||
Authorised | 11/19/2014 | ||
Authorised | 9/21/2017 | ||
Authorised | 5/24/2013 | ||
Authorised | 9/19/2013 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| GENVOYA FILM COATED TABLET 150 MG/150 MG/200 MG/10 MG | SIN15165P | TABLET, FILM COATED | 150mg | 1/20/2017 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| PREZCOBIX darunavir/cobicistat 800 mg/150 mg film coated tablet bottle | 231198 | Medicine | A | 9/24/2015 | |
| STRIBILD tenofovir disoproxil fumarate 300mg, emtricitabine 200 mg, elvitegravir 150 mg, cobicistat 150 mg tablet bottle | 194081 | Medicine | A | 2/22/2013 | |
| GENVOYA elvitegravir (150mg), cobicistat (150mg), emtricitabine (200mg) and tenofovir alafenamide (as fumarate) (10mg) fixed dose combination tablets | 233398 | Medicine | A | 1/15/2016 | |
| EVOTAZ atazanavir/cobicistat 300 mg/150 mg film coated tablets bottle | 229476 | Medicine | A | 9/23/2015 | |
| TYBOST 150 mg cobicistat tablets, bottle | 200445 | Medicine | A | 10/23/2013 | |
| SYMTUZA 800/150/200/10 darunavir/cobicistat/emtricitabine/tenofovir alafenamide 800/150/200/10 mg film-coated tablets | 312623 | Medicine | A | 11/22/2019 |