Drug name
Last update: Mar 2026GS-3242
Developer(s)
Drug information
Not provided
GS-3242
Not provided
Small molecule
Integrase Strand Transfer Inhibitors (INSTIs)
GS-3242 is a long-acting injectable (LAI) under development for the treatment of people living with HIV with plasma HIV-1 RNA levels of 5,000–400,000 copies/mL. In vitro data predict a dosing interval of ≥3 months. Two clinical studies (Phase 1a/1b) are ongoing. In Phase 1a, intramuscular doses of 400 mg (n=9), 800 mg (n=8), or 1200 mg (n=9) were administered. In Phase 1b, participants received GS-3242 250 mg orally on Days 1 and 2. Interim results showed treatment-emergent adverse events limited to injection-site reactions (Grade 1: 58%; Grade 2: 42%). Mean plasma HIV-1 RNA reduction was −2.31 log10 copies/mL. The terminal half-life was 47–56 days, with dose-proportional Cmax values of 5,062 μg/mL (400mg) , 9,640 μg/mL (800 mg), and 14,580 μg/mL (1200mg), respectively.
Not approved yet.
Not approved yet.
Therapeutic area(s)
- HIV
- Treatment
Administration route
Oral, Intramuscular
Associated long-acting platforms
Not provided
Use of drug
- Administered by a community health worker
- Administered by a nurse
- Administered by a specialty health worker
- Self-administered
- Once
- Every 4 months
- Every 3 months
Phase 1b trial interim results show that the TEAEs are: Grade 1 Injection site pain - 58%; Grade 2 Injection site pain - 42%; Headache; Nausea & Malaise. The formulation needs cold chain.
Dosage
400 mg, 800 mg and 1200mg IM & 450 mg PO
1200 mg IM
Based on clinical trial dosing plan: 1) 400 mg IM (possible dosing interval of Q3M or longer) 2) 800 mg IM (possible dosing interval of Q3M or longer) 3) 1200 mg IM (possible dosing interval of Q3M or longer) 4) 450 mg PO
Approved dosing regimen is not available (as of March 2026)
Not provided
Associated technologies
Not provided
Comment & Information
Developer(s)
Gilead Sciences, Inc.
Gilead Sciences, Inc. is a leading American biopharmaceutical company headquartered in Foster City, California. Founded in 1987 by Michael L. Riordan, the company has grown into a global powerhouse in the development of antiviral drugs and has significantly expanded its presence in oncology and inflammatory diseases. In Feb 2026, Gilead announced its intention to acquire Arcellx for $7.8 billion.
Drug structure
Scale-up and manufacturing prospects
Not provided
Not provided
Not provided
Not provided
Excipients
Not provided
Not provided
Not provided
Delivery device(s)
Not provided
There are either no relevant patents or these were not yet submitted to LAPaL
Publications
Arens, Y., & Gulick, R. M. (2025). Future options for long-acting HIV treatment and prevention. Current Opinion in HIV and AIDS, 20(1), 39-47.
Purpose of review
The aim of this review was to describe future options for long-acting HIV treatment and preexposure prophylaxis (PrEP) regimens featuring both innovations with currently approved antiretrovirals and a profile of investigational agents in the pipeline.
Recent findings
Newer formulations and modes of delivery for existing antiretroviral drugs and a number of investigational agents are under study for long-acting HIV treatment and PrEP. Regimens with weekly oral dosing for HIV treatment, monthly oral dosing for HIV PrEP, and injectable agents with longer dosing intervals (every 3 months or longer) for treatment and PrEP are in clinical development. Newer agents with novel mechanisms of action and newer modes of administration including vaginal rings, implants, patches, and rectal douches also are under investigation.
Summary
Despite the success of current antiretroviral therapy and PrEP with one-pill, once-daily regimens, there is a continuing need for new formulations, investigational agents, and novel modes of delivery to overcome barriers to implementation and ensure real-world effectiveness. Newer long-acting antiretroviral regimens for HIV treatment and PrEP using novel preparations and strategies will offer choice, enhance adherence, decrease toxicity, and improve patient and provider satisfaction.
Additional documents
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Useful links
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