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emtricitabine, darunavir/cobicistat, maraviroc
This is a three-drug combination that inhibits HIV replication through multiple mechanisms: emtricitabine and darunavir block reverse transcriptase and protease respectively, cobicistat enhances darunavir levels, and maraviroc blocks the CCR5 co-receptor.
This is a three-drug combination that inhibits HIV replication through multiple mechanisms: emtricitabine and darunavir block reverse transcriptase and protease respectively, cobicistat enhances darunavir levels, and maraviroc blocks the CCR5 co-receptor. Used for HIV-1 infection in treatment-experienced patients with CCR5-tropic virus.
At a glance
| Generic name | emtricitabine, darunavir/cobicistat, maraviroc |
|---|---|
| Sponsor | Giovanni Di Perri |
| Drug class | Antiretroviral combination (NRTI + PI + pharmacokinetic booster + CCR5 antagonist) |
| Target | HIV reverse transcriptase, HIV protease, CYP3A4, CCR5 co-receptor |
| Modality | Small molecule |
| Therapeutic area | Infectious Disease / Virology |
| Phase | FDA-approved |
Mechanism of action
Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) that blocks HIV reverse transcriptase. Darunavir is a protease inhibitor that prevents HIV protease from cleaving viral polyproteins. Cobicistat is a pharmacokinetic booster that inhibits CYP3A4, increasing darunavir plasma concentrations. Maraviroc is a CCR5 antagonist that blocks the CCR5 co-receptor on CD4+ T cells, preventing viral entry.
Approved indications
- HIV-1 infection in treatment-experienced patients with CCR5-tropic virus
Common side effects
- Diarrhea
- Nausea
- Headache
- Rash
- Elevated liver enzymes
- Lipid abnormalities
Key clinical trials
- Study of Cobicistat-Boosted Atazanavir (ATV/co), Cobicistat-Boosted Darunavir (DRV/co) and Emtricitabine/Tenofovir Alafenamide (F/TAF) in Children With HIV (PHASE2, PHASE3)
- Trial to Evaluate the Interest of a Reductive Anti Retroviral Strategy Using Dual Therapy Inspite of Triple Therapy (PHASE3)
- Pharmacokinetic Study of Antiretroviral Drugs and Related Drugs During and After Pregnancy
- Study to Evaluate Switching From a Regimen of Two Nucleos(t)Ide Reverse Transcriptase Inhibitors (NRTI) Plus a Third Agent to a Fixed Dose Combination (FDC) of Bictegravir/Emtricitabine/Tenofovir Alafenamide (B/F/TAF), in Virologically-Suppressed, HIV-1 Infected African American Participants (PHASE3)
- Using Less Neurotoxic Drugs in Patients With HAND (MARAND-X) (PHASE4)
- Switch Study to Evaluate F/TAF in HIV-1 Infected Adults Who Are Virologically Suppressed on Regimens Containing ABC/3TC (PHASE3)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
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