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GS-3242

Phase 2

HIV-1-infection | Small molecule | Infectious Disease |Gilead Sciences, Inc.|Last Updated: Sep 4, 2026

Target and mechanism

Molecular targetintegrase
Target classProtein
ModalitySmall molecule

Also known as GS-3242 Tablet

Success Probability

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Market & Valuation

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Trial Design

RandomizedCONTROLLEDDMC
Total Trials3
Total Enrollment902

FDA Designations

No designations recorded

Clinical trial landscape

GS-3242 · 3 trials · 1 indication

Phase 2 2Phase 1 1
NCT07708727Study of an Injectable Regimen of GS-3242 With Lenacapavir Compared to Biktarvy in People New to HIV-1 TreatmentHIV-1-infection
RECRUITING700 Analytics
NCT07645287A Study of GS-3242 in Combination With Lenacapavir Versus Biktarvy in Virologically Suppressed People With HIV-1HIV-1-infection
RECRUITING175 Analytics
PHASE2RECRUITING
Study of an Injectable Regimen of GS-3242 With Lenacapavir Compared to Biktarvy in People New to HIV-1 Treatment
HIV-1-infectionUnlock trial analytics
PHASE2RECRUITING
A Study of GS-3242 in Combination With Lenacapavir Versus Biktarvy in Virologically Suppressed People With HIV-1
HIV-1-infectionUnlock trial analytics

Study Endpoints

Primary Endpoints

Phase 2: Part A: Proportion of Participants With HIV-1 RNA < 50 Copies/mL at Week 35 as Determined by the United States (US) Food and Drug Administration (FDA) Snapshot Algorithm
Week 35
Phase 2: Part B: Proportion of Participants With HIV-1 RNA < 50 Copies/mL at Week 26 as Determined by the US FDA Snapshot Algorithm
Week 26
Phase 3: Proportion of Participants With HIV-1 RNA < 50 Copies/mL at Week 52 as Determined by the US FDA Snapshot Algorithm
Week 52
Part A: Proportion of Participants With HIV-1 RNA ≥ 50 Copies/mL at Week 35 as Determined by the United States (US) Food and Drug Administration (FDA) Snapshot Algorithm
Week 35
Part B: Proportion of Participants With HIV-1 RNA ≥ 50 Copies/mL at Week 26 as Determined by the US FDA Snapshot Algorithm
Week 26
Change From Baseline in Plasma Human Immunodeficiency Virus (HIV)-1 Ribonucleic Acid (RNA) (log10 Copies/mL) at Day 11 Relative to Historical Placebo Data
Baseline, Day 11

Secondary Endpoints

Phase 2: Parts A and B: Proportion of Participants With HIV-1 RNA < 50 Copies/mL at Week 12 as Determined by the US FDA Snapshot Algorithm
Week 12
Phase 2: Parts A and B: Proportion of Participants With HIV-1 RNA < 50 Copies/mL at Week 52 as Determined by the US FDA Snapshot Algorithm
Week 52
Phase 2: Parts A and B: Change From Baseline in Clusters of Differentiation 4 (CD4) Cell Count at Week 12
Baseline, Week 12
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Phase 2: Part A: Group 1 of GS-3242 + LENEXPERIMENTALParticipants will be randomized to receive oral loading doses of GS-3242 in combination with LEN oral tablets, followed by intramuscular (IM) injections of GS-3242 and LEN for at least 52 weeks.
Phase 2: Part A: Group 2 of GS-3242 + LENEXPERIMENTALParticipants will be randomized oral loading doses of GS-3242 in combination with LEN oral tablets, followed by IM injections of GS-3242 (at a different dose than Group 1) and LEN for at least 52 weeks.
Phase 2: Part A: Group 3 of B/F/TAFEXPERIMENTALParticipants will be randomized to receive 50/200/25 mg of B/F/TAF daily for at least 52 weeks.
Phase 2: Part B: Group 4 of GS-3242 + LENEXPERIMENTALParticipants will be enrolled (non-randomized) to receive oral loading doses of GS-3242 in combination with LEN oral tablets, followed IM injections of GS-3242 and LEN (at different doses than Group 1 and 2) for at least 52 weeks.
Phase 3: Group 1 of GS-3242 + LENEXPERIMENTALParticipants will be randomized to receive oral loading doses of GS-3242 in combination with LEN oral tablets, followed by IM injections of GS-3242 and LEN for at least 104 weeks.
Phase 3: Group 2 of B/F/TAFEXPERIMENTALParticipants will be randomized to receive 50/200/25 mg of B/F/TAF daily for at least 104 weeks.
Part A: Group 1 of GS-3242 + LENEXPERIMENTALParticipants will be randomized to receive oral loading doses of GS-3242 in combination with LEN oral tablets, followed by intramuscular (IM) injections of GS-3242 and LEN up to 52 weeks.
Part A: Group 2 of GS-3242 + LENEXPERIMENTALParticipants will be randomized to receive oral loading doses of GS-3242 in combination with LEN oral tablets, followed by a IM injections of GS-3242 (at a different dose than Group 1) and LEN up to 52 weeks.
Part A: Group 3 of B/F/TAFEXPERIMENTALParticipants will be randomized to continue to receive 50/200/25 mg of B/F/TAF daily for up to 52 weeks.
Part B: Group 4 (Conditional) of GS-3242 + LENEXPERIMENTALParticipants will be enrolled (non-randomized) to receive oral loading doses of GS-3242 in combination with LEN oral tablets, followed IM injection of GS-3242 and LEN (at different doses than Groups 1 and 2) up to 52 weeks.
Cohort 1: Single Dose of GS-3242EXPERIMENTALParticipants in cohort 1 will receive single dose of GS-3242 450 mg on Days 1 and 2 in the fasted condition. After assessments on Day 11 or upon early termination (ET), the participants initiate a regimen of bictegravir/emtricitabine/tenofovir alafenamide (Biktarvy®) (BVY), or an alternative standard of care (SOC) antiretroviral (ART) regimen (example INSTI + NRTIs: dolutegravir (DTG)/abacavir (ABC)/3TC or DTG/3TC) up to Day 39. Following the completion of Cohort 1, additional cohorts may be opened for enrollment if further data are needed. Doses of GS-3242 will be based on safety and pharmacokinetic (PK) data from ongoing Phase 1a studies.

Interventions

NameTypeDescription
GS-3242 TabletDRUGAdministered orally
GS-3242 InjectionDRUGAdministered intramuscularly (IM)
Lenacapavir TabletDRUGAdministered orally
Lenacapavir InjectionDRUGAdministered IM
B/F/TAFDRUGAdministered orally
GS-3242DRUGAdministered orally
BVYDRUGAdministered orally
Standard of CareDRUGAntiretroviral therapy, administered orally Non-NNRTIs, examples: ABC/ DTG/3TC; DTG plus (TAF or TDF) plus (FTC or 3TC)
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites8

Key Inclusion Criteria: * HIV-1 ribonucleic acid (RNA) ≥ 500 copies/mL at screening. * Antiretroviral (ARV) treatment-naive, except for prior use of oral daily pre-exposure prophylaxis (PrEP) or postexposure prophylaxis (PEP) up to 1 month prior to screening. Key Exclusion Criteria: * Prior usage...

Countries:United StatesPuerto RicoAustraliaCanadaMexicoThailand
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Recent Changes (Last 90 Days)

LOWSep 4, 2026NCT07645287lastUpdatePostDate: changed
LOWAug 14, 2026NCT07708727Status: NOT_YET_RECRUITING → RECRUITING
LOWAug 14, 2026NCT07708727Status: NOT_YET_RECRUITING → RECRUITING
LOWAug 6, 2026NCT07645287lastUpdatePostDate: changed
LOWAug 6, 2026NCT07645287lastUpdatePostDate: changed
LOWJul 17, 2026NCT07708727NEW_TRIAL: changed
LOWJul 17, 2026NCT07708727NEW_TRIAL: changed
LOWJul 17, 2026NCT07708727NEW_TRIAL: changed
LOWJul 10, 2026NCT07645287Status: NOT_YET_RECRUITING → RECRUITING
LOWJul 10, 2026NCT07645287Status: NOT_YET_RECRUITING → RECRUITING
LOWJun 12, 2026NCT07645287NEW_TRIAL: changed
LOWJun 12, 2026NCT07645287NEW_TRIAL: changed
MEDIUMJun 11, 2026NCT07001319TRIAL_REMOVED: changed
MEDIUMJun 11, 2026NCT07001319TRIAL_REMOVED: changed
MEDIUMJun 11, 2026NCT07001319TRIAL_REMOVED: changed

Frequently asked questions about GS-3242

What is GS-3242 used for?

GS-3242 is an investigational small molecule being developed for the treatment of HIV-1 infection. It is currently in Phase 2 clinical trials, where it is being studied in combination with other antiretroviral agents for both virologically suppressed and treatment-naive people living with HIV-1.

What does GS-3242 target?

GS-3242 targets integrase, a viral protein essential for HIV-1 replication. By inhibiting integrase, GS-3242 is designed to block the integration of viral DNA into the host cell genome, a critical step in the HIV-1 life cycle.

Who makes GS-3242?

GS-3242 is being developed by Gilead Sciences, Inc., a biopharmaceutical company traded on the NASDAQ under the ticker symbol GILD. Gilead is conducting multiple clinical trials to evaluate the safety and efficacy of GS-3242 in people with HIV-1 infection.

What phase is GS-3242 in?

GS-3242 is in Phase 2 clinical development. It has completed one Phase 1 study and is currently being evaluated in two Phase 2 trials, both of which are recruiting participants. GS-3242 is not yet approved and remains an investigational agent.

What clinical trials is GS-3242 in?

GS-3242 is being studied in three clinical trials. NCT07001319 is a completed Phase 1 study. NCT07645287 is a Phase 2 trial combining GS-3242 with lenacapavir versus Biktarvy in virologically suppressed people. NCT07708727 is a Phase 2 trial of an injectable GS-3242 and lenacapavir regimen in treatment-naive individuals.

Is GS-3242 the same as GS-3242 Tablet?

Yes, GS-3242 Tablet is another name for GS-3242. The tablet formulation is the oral dosage form of this investigational integrase inhibitor being developed by Gilead Sciences for the treatment of HIV-1 infection.