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Sustiva (EFAVIRENZ)
Sustiva works by binding to the reverse transcriptase enzyme, preventing the replication of viral RNA.
Sustiva (Efavirenz) is a small molecule non-nucleoside reverse transcriptase inhibitor developed by Bristol Myers Squibb. It targets the cholesterol 24-hydroxylase enzyme and is used to treat human immunodeficiency virus (HIV) infection. Originally approved by the FDA in 1998, Sustiva is now off-patent and has multiple generic manufacturers. As a non-nucleoside reverse transcriptase inhibitor, Sustiva works by binding to the reverse transcriptase enzyme, preventing the replication of viral RNA. It is a key component in combination antiretroviral therapy (cART) regimens.
At a glance
| Generic name | EFAVIRENZ |
|---|---|
| Sponsor | Bristol-Myers Squibb |
| Drug class | Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor [EPC] |
| Target | Cholesterol 24-hydroxylase |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
| First approval | 1998 |
Mechanism of action
Efavirenz is an antiviral drug[see Clinical Pharmacology (12.4) ].
Approved indications
- Human immunodeficiency virus infection
Common side effects
- Rash
- Nausea
- Vomiting
- Dizziness
- Headache
- Fatigue
- Insomnia
- Pain
- Diarrhea
- Dyspepsia
- Anxiety
- Depression
Drug interactions
- alprazolam
- boceprevir
- ethinylestradiol
- etravirine
- fosamprenavir
- indinavir
- levomethadyl acetate
- maraviroc
- methadone
- methylergometrine
- methysergide
- midazolam
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)
- Efavirenz for the Treatment of Creutzfeldt-Jakob Disease (PHASE3)
- The T Cell Activator of Cell Killing ("TACK") IT ON" STUDY (NA)
- A Study to Provide Continued Access to Study Drug to Children and Adolescents Who Have Completed Clinical Studies Involving Gilead HIV Treatments (PHASE4)
- Interaction of CYP2B6 Genotype and Efavirenz With Methadone and Tizanidine PK (EARLY_PHASE1)
- A Single-center, Randomized, Open-label, Parallel-design Clinical Study to Evaluate the Pharmacokinetic Effects of Itraconazole, Fluconazole or Efavirenz on a Single Dose of Clifutinib in Healthy Participants (PHASE1)
- Trial to Evaluate the Interest of a Reductive Anti Retroviral Strategy Using Dual Therapy Inspite of Triple Therapy (PHASE3)
- Safety and Virologic Effect of a Human Monoclonal Antibody (VRC01) Administered Intravenously to Adults During Early Acute HIV Infection (PHASE1)
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 |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Sustiva CI brief — competitive landscape report
- Sustiva updates RSS · CI watch RSS
- Bristol-Myers Squibb portfolio CI