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Lepetegravir

Phase 2

HIV-1-Infection | Small molecule | Infectious Disease |Gilead Sciences, Inc.|Last Updated: Apr 17, 2026

Success Probability

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Trial Design

RandomizedDouble-BlindACTIVE_CONTROLLEDDMC
Total Trials1
Total Enrollment675

FDA Designations

No designations recorded

Clinical trial landscape

Lepetegravir · 1 trial · 1 indication

Phase 2 1
NCT06544733Study of Oral Weekly Lepetegravir (Formerly GS-1720) and Lenacapavir Pacfosacil (Formerly GS-4182) Versus Biktarvy in People With HIV-1 Who Are Virologically SuppressedHIV-1-Infection
ACTIVE NOT_RECRUITING675 Analytics
PHASE2ACTIVE NOT_RECRUITING
Study of Oral Weekly Lepetegravir (Formerly GS-1720) and Lenacapavir Pacfosacil (Formerly GS-4182) Versus Biktarvy in People With HIV-1 Who Are Virologically Suppressed
HIV-1-InfectionUnlock trial analytics

Study Endpoints

Primary Endpoints

Phase 2: Proportion of Participants With HIV-1 RNA ≥ 50 Copies/mL at Week 24 as Determined by the United States (US) Food and Drug Administration (FDA)-defined Snapshot Algorithm
Week 24
Phase 3: Proportion of Participants With HIV-1 RNA ≥ 50 Copies/mL at Week 48 as Determined by the US FDA-defined Snapshot Algorithm
Week 48

Secondary Endpoints

Phase 2: Proportion of Participants With HIV-1 RNA ≥ 50 copies/mL at Week 12 as Determined by the US FDA-defined Snapshot Algorithm
Week 12
Phase 2: Proportion of Participants With HIV-1 RNA ≥ 50 copies/mL at Week 48 as Determined by the US FDA-defined Snapshot Algorithm
Week 48
Phase 2: Proportion of Participants With HIV-1 RNA < 50 Copies/mL at Week 12 as Determined by the US FDA-defined Snapshot Algorithm
Week 12
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Study Design & Arms

AllocationRANDOMIZED
MaskingDOUBLE
ModelSEQUENTIAL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Phase 2: Lepetegravir + Lenacapavir pacfosacil (Treatment Group 1)EXPERIMENTALParticipants who have been virologically suppressed on bictegravir/emtricitabine/tenofovir alafenamide (BVY) will switch to lepetegravir (650 mg tablet) and lenacapavir pacfosacil (300 mg tablet) coadministered. Participants will receive a 1-day loading dose of lepetegravir (1300 mg) and lenacapavir pacfosacil (600 mg) on Day 1. Thereafter, participants will take weekly doses of single agent lepetegravir (650 mg) and lenacapavir pacfosacil (300 mg) coadministered for at least 48 weeks.
Phase 2: Bictegravir/emtricitabine/tenofovir alafenamide (BVY) (Treatment Group 2)ACTIVE_COMPARATORParticipants who have been virologically suppressed on bictegravir/emtricitabine/tenofovir alafenamide (BVY) will continue receiving BVY daily for at least 48 weeks.
Phase 2 Extension Phase: Lepetegravir /Lenacapavir pacfosacil Fixed-dose Combination (FDC)EXPERIMENTALAt the end of the randomized treatment, Phase 2 participants will be given the option to participate in the Extension Phase. Phase 2 Treatment Group 1 will switch to lepetegravir /lenacapavir pacfosacil FDC weekly. Phase 2 Treatment Group 2 will receive a loading dose of lepetegravir /lenacapavir pacfosacil FDC on Extension Phase Day 1 then, lepetegravir/lenacapavir pacfosacil FDC weekly. Participants who choose to enter the Extension Phase will receive lepetegravir /lenacapavir pacfosacil FDC tablets until the product becomes available or until Gilead Sciences elects to discontinue the study, whichever occurs first.
Phase 3: Lepetegravir /Lenacapavir pacfosacil FDC + Placebo to Match (PTM) BVY (Treatment Group 1)EXPERIMENTALParticipants who have been virologically suppressed on BVY will switch from BVY to lepetegravir/lenacapavir pacfosacil FDC tablets weekly + placebo-to-match (PTM) BVY once daily. In addition, participants will receive a 1-day loading dose regimen of lepetegravir /lenacapavir pacfosacil FDC on Day 1. Participants will receive treatment for at least 96 weeks.
Phase 3: BVY Placebo to Match Lepetegravir /Lenacapavir pacfosacil FDC + BVY (Treatment Group 2)ACTIVE_COMPARATORParticipants who have been virologically suppressed on BVY will continue receiving oral BVY daily. In addition, participants will receive a 1-day loading dose of PTM lepetegravir /lenacapavir pacfosacil on Day 1 and weekly PTM thereafter. Participants will receive treatment for at least 96 weeks.
Phase 3 Extension Phase: Lepetegravir/Lenacapavir pacfosacil Fixed-dose Combination (FDC)EXPERIMENTALAfter the end of blinded treatment, Phase 3 participants will be given the option to participate in the Extension Phase. Phase 3 Treatment Group 1 will switch to lepetegravir/lenacapavir pacfosacil FDC weekly. Phase 3 Treatment Group 2 will receive a 1-day loading dose of lepetegravir/lenacapavir pacfosacil FDC on Extension Phase Day 1, then lepetegravir/lenacapavir pacfosacil FDC weekly. Participants who choose to enter the Extension Phase will receive lepetegravir/lenacapavir pacfosacil FDC tablets until the product becomes available or until Gilead Sciences elects to discontinue the study, whichever occurs first.

Interventions

NameTypeDescription
LepetegravirDRUGTablets administered orally without regard to food
Lenacapavir pacfosacilDRUGTablets administered orally without regard to food
Placebo to Match BVYDRUGTablets administered orally without regard to food
Bictegravir/emtricitabine/tenofovir alafenamideDRUGTablets administered orally without regard to food
Lepetegravir/Lenacapavir pacfosacil FDCDRUGTablets administered orally without regard to food
Placebo to Match GS1720/GS-4182 FDCDRUGTablets administered orally without regard to food
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites39

Key Inclusion Criteria: * Documented plasma HIV-1 RNA \< 50 copies/mL for ≥ 24 weeks before and at screening. * Receiving BVY for ≥ 24 weeks prior to screening. Key Exclusion Criteria: * Prior use of, or exposure to LEN, lepetegravir, or lenacapavir pacfosacil. * History of virologic failure whil...

Countries:United StatesPuerto Rico
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Frequently asked questions about Lepetegravir

What is Lepetegravir used for in HIV-1 infection?

Lepetegravir is an investigational small molecule being developed for the treatment of HIV-1 infection. It is currently in Phase 2 clinical development, studied in combination with lenacapavir pacfosacil as an oral weekly regimen for people with HIV-1 who are virologically suppressed.

What does Lepetegravir target?

Lepetegravir is an integrase inhibitor, targeting the HIV-1 integrase enzyme to block viral integration into host DNA. This mechanism is being evaluated in a Phase 2 trial for HIV-1 infection, where it is administered orally once weekly in combination with lenacapavir pacfosacil.

Who makes Lepetegravir?

Lepetegravir is being developed by Gilead Sciences, Inc., a biopharmaceutical company traded on NASDAQ under the ticker GILD. The drug is currently in Phase 2 clinical development for the treatment of HIV-1 infection.

What phase is Lepetegravir in?

Lepetegravir is in Phase 2 clinical development. It is an investigational drug, not yet approved by regulatory authorities, and is being studied in an active, not recruiting Phase 2 trial for HIV-1 infection.

What clinical trials is Lepetegravir in?

Lepetegravir is being evaluated in one Phase 2 clinical trial, NCT06544733, which is active but not recruiting. The study compares oral weekly lepetegravir and lenacapavir pacfosacil versus Biktarvy in 675 participants with HIV-1 who are virologically suppressed, conducted in the United States and Puerto Rico.

Is Lepetegravir the same as GS-1720?

Lepetegravir was formerly known as GS-1720. The Phase 2 trial NCT06544733 references the drug as 'Lepetegravir (Formerly GS-1720)', indicating that both names refer to the same investigational compound.