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Lepetegravir

Phase 2

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

Success Probability
Approval Probability 71%
TA Base Rate26%
Adjusted LOA41%
ML RiskLOW_RISK
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Market & Valuation
rNPV $3.2B
Market Size $9.4B
Revenue Basis $1.6B
Competitors 6
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Trial Design
RandomizedDouble-BlindACTIVE_CONTROLLEDDMCBiomarker
Total Trials1
Total Enrollment675
FDA Designations
No designations recorded
Clinical Trials (1)
NCT IDTitlePhaseStatusEnrollmentVelocityDesignStartCompletionLast UpdatedSitesCountries
NCT06544733Study of Oral Weekly Lepetegravir (Formerly GS-1720) and Lenacapavir Pacfosacil (Formerly GS-4182) Versus Biktarvy in People With HIV-1 Who Are Virologically SuppressedPHASE2 ACTIVE NOT_RECRUITING 675Aug 20, 2024Jun 1, 2029Apr 17, 202639 United States, Puerto Rico
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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 — 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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Recent Changes (Last 90 Days)
MEDIUMMay 26, 2026NCT06544733primaryCompletionDate: changed
LOWMay 24, 2026NCT06544733studyFirstPostDate: changed