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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

NCT05216432 · Status: RECRUITING · Phase: PHASE1 · Type: INTERVENTIONAL · Enrollment: 930

Last updated 2025-09-22

No results posted yet for this study

Summary

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).

Conditions

Interventions

DRUG

RLY-2608

RLY-2608 is a mutant-selective, oral PI3Kα inhibitor.

DRUG

Fulvestrant

500 mg fulvestrant is administered intramuscularly on Cycle 1 Day 1, Day 15, and Day 1 of each subsequent cycle (where a cycle is 28 days).

DRUG

Palbociclib 125mg

125mg palbociclib is taken orally once daily for 28-day cycles that include 21 days of treatment followed by 7 days off treatment.

DRUG

Ribociclib 400mg

400mg ribociclib is taken orally once daily for 28-day cycles that include 21 days of treatment followed by 7 days off treatment.

DRUG

Ribociclib 600mg

600mg ribociclib is taken orally once daily for 28-day cycles that include 21 days of treatment followed by 7 days off treatment.

DRUG

PF-07220060 100mg

PF-07220060 100 mg is taken orally twice daily at the same time with RLY-2608 during each 28-day cycle.

DRUG

PF-07220060 300 mg

PF-07220060 300 mg is taken orally twice daily at the same time with RLY-2608 during each 28-day cycle.

Sponsors & Collaborators

  • Relay Therapeutics, Inc.

    lead INDUSTRY

Study Design

Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Model
PARALLEL

Eligibility

Min Age
18 Years
Sex
ALL
Healthy Volunteers
No

Timeline & Regulatory

Start
2021-12-08
Primary Completion
2027-04-30
Completion
2027-04-30
FDA Drug
Yes

Countries

  • United States
  • Australia
  • France
  • Italy
  • Spain

Study Locations

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Entities

Drugs
Diseases

Read the full study record

This page highlights key information. For complete eligibility criteria, study locations, investigator contacts, and the full protocol, visit the original record on ClinicalTrials.gov.

View NCT05216432 on ClinicalTrials.gov