RLY-2608

DRUG5 trials

Sponsors

Relay Therapeutics Inc., Relay Therapeutics, Inc.

Conditions

Advanced Breast CancerBreast CancerCLOVES SyndromeHER2- Negative Breast CancerHER2-negative Breast CancerHormone Receptor Positive TumorHuman Epidermal Growth Factor Receptor 2 Negative (HR+/HER2-) Locally Advanced or Metastatic Breast CancerKlippel Trenaunay Syndrome

Phase 1

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

RecruitingNCT05216432

Relay Therapeutics, Inc.Advanced Breast Cancer, Breast Cancer, HER2-negative Breast Cancer +4

Start: 2021-12-08End: 2027-04-30Target: 930Updated: 2025-09-22

Phase 2

A Phase 2 Study of Mutant-selective PI3Kα Inhibitor, RLY-2608, in Adults and Children With PIK3CA Related Overgrowth Spectrum and Malformations Driven by PIK3CA Mutation

RecruitingNCT06789913

Relay Therapeutics, Inc.CLOVES Syndrome, Klippel Trenaunay Syndrome, Lymphatic Malformations +4

Start: 2025-06-13End: 2031-10-31Target: 277Updated: 2026-01-08

A Phase 2 Study of Mutant-selective PI3Kα Inhibitor, RLY-2608, in Adults and Children with PIK3CA Related Overgrowth Spectrum and Malformations Driven by PIK3CA Mutation

RecruitingCTIS2024-518895-30-00

Relay Therapeutics Inc.PIK3CA Related Overgrowth Spectrum and Malformations Driven by PIK3CA Mutation

Start: 2025-11-21Target: 52Updated: 2026-01-23

Phase 3

Phase 3 Study of RLY-2608 + Fulvestrant vs Capivasertib + Fulvestrant as Treatment for Locally Advanced or Metastatic PIK3CA-mutant HR+/HER2- Breast Cancer

RecruitingNCT06982521

Relay Therapeutics, Inc.Advanced Breast Cancer, Breast Cancer, HER2- Negative Breast Cancer +3

Start: 2025-08-26End: 2031-12-31Target: 540Updated: 2026-04-02

A Phase 3 Open-label Randomized Study Assessing the Efficacy and Safety of RLY-2608 + Fulvestrant Versus Capivasertib + Fulvestrant as Treatment for PIK3CA-mutant Hormone Receptor Positive, Human Epidermal Growth Factor Receptor 2 Negative (HR+/HER2-) Locally Advanced or Metastatic Breast Cancer Following Recurrence or Progression On or After Treatment with a CDK4/6 Inhibitor

RecruitingCTIS2025-523083-21-00

Relay Therapeutics Inc.Human Epidermal Growth Factor Receptor 2 Negative (HR+/HER2-) Locally Advanced or Metastatic Breast Cancer, PIK3CA-mutant Hormone Receptor Positive

Start: 2025-12-08Target: 272Updated: 2025-11-17

Related Papers

Abstract 5130: Identification and characterization of pan-mutant selective PI3Kα inhibitors with the capability of PI3Kα H1047R protein degradation

Cancer Research2026-04-03

Abstract PD10-07: Efficacy of mutant-selective PI3Kα inhibitor RLY-2608 in combination with fulvestrant in patient (pt) subset populations, including pts with PIK3CA-mutant HR+/HER2- advanced breast cancer (BC) pre-treated with fulvestrant or other SERD

Clinical Cancer Research2026-02-17

Abstract PS5-08-25: ReDiscover-2, a phase 3 study of RLY-2608 + fulvestrant versus capivasertib + fulvestrant as treatment for locally advanced or metastatic PIK3CA-mutant HR+/ HER2- breast cancer following recurrence or progression on or after treatment with a CDK4/6 inhibitor (trial in progress)

Clinical Cancer Research2026-02-17

ReInspire: A phase 2 study of mutant-selective PI3Kα inhibitor, RLY-2608, in adults and children with PIK3CA-related overgrowth spectrum and malformations driven by PIK3CA mutation

Blood2025-11-03

Abstract PS7-01: Efficacy of RLY-2608, a mutant-selective PI3Kα inhibitor in patients with PIK3CA-mutant HR+HER2- advanced breast cancer: ReDiscover trial

Clinical Cancer Research2025-06-13

Updated efficacy of mutant-selective PI3Kα inhibitor RLY-2608 in combination with fulvestrant in patients with <i>PIK3CA</i> -mutant HR+HER2- advanced breast cancer: ReDiscover trial.

Journal of Clinical Oncology2025-05-282 citations

Abstract 5977: Identification and characterization of an allosteric and mutant-selective PI3Kα inhibitor

Cancer Research2025-04-21

First-in-human study of RLY-2608, a pan-mutant and isoform selective PI3Kα inhibitor, as a single agent in patients (pts) with advanced solid tumors and in combination with fulvestrant in pts with advanced breast cancer.

Journal of Clinical Oncology2024-06-016 citations

Abstract PO3-20-03: First-in-human global study of RLY-2608, a pan-mutant and isoform selective PI3Kα inhibitor, as a single agent in patients with advanced solid tumors and in combination with fulvestrant in patients with advanced breast cancer

Cancer Research2024-05-02

Abstract CT017: Pan-mutant and isoform selective PI3Kα inhibitor, RLY-2608, demonstrates selective targeting in a first-in-human study of <i>PIK3CA-</i>mutant solid tumor patients, ReDiscover trial

Cancer Research2023-05-296 citations

Abstract OT3-22-01: First-in-human global multi-center study of RLY-2608, a pan mutant and isoform selective PI3Kα inhibitor, as a single agent in advanced solid tumor patients and in combination with fulvestrant in patients with advanced breast cancer

Cancer Research2023-03-011 citations

First-in-human global multi-center study of RLY-2608, a pan-mutant and isoform-selective PI3Kα inhibitor, as a single agent in patients with advanced solid tumors and in combination with fulvestrant in patients with advanced breast cancer.

Journal of Clinical Oncology2022-06-014 citations