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GS-2121

Phase 1

Advanced Solid Tumors | Small molecule | Oncology |Gilead Sciences, Inc.|Last Updated: Apr 21, 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
CONTROLLEDBiomarker
Total Trials1
Total Enrollment154
FDA Designations
No designations recorded
Clinical Trials (1)
NCT IDTitlePhaseStatusEnrollmentVelocityDesignStartCompletionLast UpdatedSitesCountries
NCT06532565Study of GS-2121 Given Alone or in Combination in Adults With Advanced Solid TumorsPHASE1 RECRUITING 154Jul 26, 2024Jun 1, 2028Apr 21, 20266 United States, Canada
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Study Endpoints
Primary Endpoints
Parts A and B: Percentage of Participants with Adverse Events and Serious Adverse Events
First dose up to 90 days post last dose (up to approximately 118 weeks)
Parts A and B: Percentage of Participants with Laboratory Abnormalities
First dose up to 90 days post last dose (up to approximately 118 weeks)
Part A: Percentage of Participants with Dose-Limiting Toxicities (DLTs) During Dose Escalation
Day 1 up to Day 21

DLTs are defined as any of the protocol-specified treatment-emergent adverse events (AEs) with onset within the DLT-evaluation period for the corresponding dose.

Parts C and D: Percentage of Participants with Adverse Events and Serious Adverse Events
First dose up to 90 days post last dose (up to approximately 118 weeks)
Parts C and D: Percentage of Participants with Laboratory Abnormalities
First dose up to 90 days post last dose (up to approximately 118 weeks)
Part C: Percentage of Participants with DLTs During Dose Escalation
Day 1 up to Day 21

DLTs are defined as any of the protocol-specified treatment-emergent adverse events (AEs) with onset within the DLT-evaluation period for the corresponding dose.

Secondary Endpoints
Parts A and B: Plasma Concentration of GS-2121 and Active Metabolite
Predose and postdose up to end of treatment (up to 105 weeks)
Parts A and B: PK Parameter: AUC0-24 of GS-2121
Predose and postdose up to end of treatment (up to 105 weeks)
Parts A and B: PK Parameter: Cmax of GS-2121
Predose and postdose up to end of treatment (up to 105 weeks)
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Study Design & Arms
AllocationNON_RANDOMIZED
MaskingNONE
ModelSEQUENTIAL
PurposeTREATMENT
Treatment Arms
ArmTypeDescription
Part A: GS-2121 Monotherapy Dose EscalationEXPERIMENTALParticipants will receive escalating doses of GS-2121 monotherapy until disease progression, or until the participant meets other study drug discontinuation criteria as specified in protocol.
Part B: GS-2121 Monotherapy Dose ExpansionEXPERIMENTALParticipants with selected indications will receive GS-2121 monotherapy at the recommended dose for expansion.
Part C: Combination Dose Escalation of GS-2121 with ZimberelimabEXPERIMENTALParticipants will receive escalating doses of GS-2121 in combination with zimberelimab until disease progression, or until the participant meets other study drug discontinuation criteria as specified in protocol.
Part D: Combination Dose Expansion of GS-2121 with ZimberelimabEXPERIMENTALParticipants with selected indications will receive GS-2121 at the recommended dose for expansion in combination with zimberelimab.
Interventions
NameTypeDescription
GS-2121DRUGTablet administered orally
ZimberelimabDRUGAdministered intravenously
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Eligibility Criteria
Age Range18 Years — N/A
SexALL
Healthy VolunteersNo
Study Sites6

Key Inclusion Criteria: * Participants diagnosed with histologically or cytologically confirmed advanced solid tumors who have progressed despite standard therapy, are intolerant to standard therapy, or are ineligible for standard therapy. * Measurable disease per Response Evaluation Criteria in So...

Countries:United StatesCanada
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Recent Changes (Last 90 Days)
LOWMay 26, 2026NCT06532565primaryCompletionDate: changed
LOWMay 24, 2026NCT06532565studyFirstPostDate: changed