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Study identifier: NCT05216432 Synced from ClinicalTrials.gov · July 28, 2026
● Recruiting

First-in-Human Study of Mutant-selective PI3Kα Inhibitor, RLY-2608, as a Single Agent in Patients With Advanced Solid Tumors and in Combination With Endocrine Therapy +/- a CDK4/6 or CDK4 Inhibitor in Patients With Advanced Solid Tumors or Advanced Breast Cancer

Condition: PIK3CA Mutation · Solid Tumor, Adult · HER2-negative Breast Cancer  ·  Sponsor: Relay Therapeutics, Inc.

PhasePhase 1
Planned participants930
Who can joinAll sexes, 18 Years to no upper limit
Healthy volunteersNo

About this study

This is an open-label, FIH study designed to evaluate the maximum tolerated dose, recommended Phase 2 dose, safety, tolerability, PK, pharmacodynamics, and preliminary antineoplastic activity of RLY-2608, in advanced solid tumor patients with a Phosphatidylinositol-4,5-bisphosphate-3 kinase, catalytic subunit alpha (PIK3CA) mutation in blood and/or tumor per local assessment. The study will evaluate RLY-2608 as a single agent for patients with unresectable or metastatic solid tumors. It will also evaluate RLY-2608 in combination RLY-2608 + fulvestrant and in triple combination RLY-2608 + fulvestrant + CDK4/6 inhibitor (palbociclib or ribociclib) or CDK4 inhibitor (PF-07220060) for patients with HR+ HER2- locally advanced or metastatic breast cancer. The RLY-2608 single agent arm, RLY-2608 + fulvestrant combination arm, and triple combination arms will have 2 parts: a dose escalation (Part 1) and a dose expansion (Part 2).

This description comes directly from the study's public registry record.

Talk to the study team

Relay Therapeutics Inc  ·  617-322-0731  ·  ClinicalTrials@relaytx.com

Always discuss trial participation with your own doctor first.

Locations (37)

The University of Arizona Cancer CenterTucson, Arizona, United StatesRecruiting
University of California-San DiegoSan Diego, California, United StatesRecruiting
HealthONEDenver, Colorado, United StatesRecruiting
Yale UniversityNew Haven, Connecticut, United StatesRecruiting
Florida Cancer SpecialistsOrlando, Florida, United StatesRecruiting
Boca Raton Clinical Research (BRCR) GlobalPlantation, Florida, United StatesWithdrawn
University of Chicago Medical CenterChicago, Illinois, United StatesRecruiting
Community Health NetworkIndianapolis, Indiana, United StatesRecruiting
Massachusetts General HospitalBoston, Massachusetts, United StatesRecruiting
Dana-Farber Cancer InstituteBoston, Massachusetts, United StatesRecruiting
University of MichiganAnn Arbor, Michigan, United StatesRecruiting
Washington University School of Medicine St. LouisSt Louis, Missouri, United StatesRecruiting

+ 25 more locations — full list on the registry record.

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Source record: clinicaltrials.gov/study/NCT05216432