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RLY-5836

Phase 1

PIK3CA Mutation | Small molecule | Oncology |Relay Therapeutics, Inc.|Last Updated: May 16, 2025

Success Probability

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Market & Valuation

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Trial Design

CONTROLLEDDMC
Total Trials1
Total Enrollment41

FDA Designations

No designations recorded

Clinical trial landscape

RLY-5836 · 1 trial · 8 indications

Phase 1 1
NCT05759949First-in-Human Study of RLY-5836 in Advanced Breast Cancer and Other Solid TumorsPIK3CA Mutation
COMPLETED41 Analytics
PHASE1COMPLETED
First-in-Human Study of RLY-5836 in Advanced Breast Cancer and Other Solid Tumors
PIK3CA MutationUnlock trial analytics

Study Endpoints

Primary Endpoints

Maximum Tolerated Dose (MTD) and Recommended Phase 2 Dose (RP2D) of RLY-5836
Cycle 1 (4-week cycle) of treatment for MTD and at the end of every cycle (4-week cycles) for RP2D until study discontinuation, approximately 24 months
Number of participants with any dose-limiting toxicity (DLT)
Cycle 1, up to 28 days.
Number of participants with adverse events (AEs)
Every cycle (4-week cycles) until study discontinuation, approximately 24 months
Number of participants with serious adverse events (SAEs)
Every cycle (4-week cycles) until study discontinuation, approximately 24 months

Secondary Endpoints

PIK3CA genotype in blood and tumor tissue by next generation nucleic acid sequencing
Every cycle (4-week cycles) through Cycle 3 and every other cycle thereafter until study discontinuation, approximately 24 months
PK of RLY-5836: area under the concentration-time curve (AUC)
Approximately every 2 weeks in Cycle 1 (4-week cycle) and every cycle through end of treatment (4-week cycles), approximately 24 months
PK of RLY-5836: maximum plasma concentration (Cmax)
Approximately every 2 weeks in Cycle 1 (4-week cycle) and every cycle through end of treatment (4-week cycles), approximately 24 months
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Study Design & Arms

AllocationNON_RANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
RLY-5836 Single Agent ArmEXPERIMENTALRLY-5836 single agent arm for participants with unresectable or metastatic solid tumors
RLY-5836 + Fulvestrant ArmEXPERIMENTALRLY-5836 + fulvestrant combination arm for participants with HR+, HER2- locally advanced or metastatic breast cancer
RLY-5836 + Palbociclib + Fulvestrant ArmEXPERIMENTALRLY-5836 + palbociclib + fulvestrant triple combination arm for participants with HR+, HER2- locally advanced or metastatic breast cancer
RLY-5836 + Ribociclib + Fulvestrant ArmEXPERIMENTALRLY-5836 + ribociclib + fulvestrant triple combination arm for participants with HR+, HER2- locally advanced or metastatic breast cancer
RLY-5836 + Abemaciclib + Fulvestrant ArmEXPERIMENTALRLY-5836 + abemaciclib + fulvestrant triple combination arm for participants with HR+, HER2- locally advanced or metastatic breast cancer

Interventions

NameTypeDescription
RLY-5836DRUGRLY-5836 is a mutant-selective, oral PI3Kα inhibitor.
FulvestrantDRUGFulvestrant (500 mg) is administered IM into the buttocks (gluteal area) slowly (1 to 2 minutes per injection) as 2×5 mL injections, 1 in each buttock, on Cycle 1 Day 1, Cycle 1 Day 15, and Day 1 of each subsequent cycle.
PalbociclibDRUGPalbociclib 125 mg once daily is taken orally in combination with RLY-5836 and fulvestrant for 28-day cycles that include 21 days of treatment followed by 7 days off treatment.
RibociclibDRUGRibociclib 600 mg once daily is taken orally in combination with RLY-5836 and fulvestrant for 28-day cycles that include 21 days of treatment followed by 7 days off treatment.
AbemaciclibDRUGAbemaciclib 150 mg BID will be taken orally in combination with RLY-5836 and fulvestrant for 28-day cycles.
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites7

Inclusion Criteria: Patient has ECOG performance status of 0-1 One or more documented primary oncogenic PIK3CA mutation(s) in blood and/or tumor per local assessment RLY-5836 single agent arm key inclusion criteria * Disease that is refractory to standard therapy, intolerant to standard therapy,...

Countries:United States
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Frequently asked questions about RLY-5836

What is RLY-5836 used for?

RLY-5836 is an investigational small molecule being developed for the treatment of cancers with PIK3CA mutations, including advanced breast cancer and other solid tumors. It is being studied in patients with HER2-negative, hormone receptor positive, metastatic or advanced breast cancer, as well as unresectable solid tumors.

What does RLY-5836 target?

RLY-5836 targets cancers that harbor PIK3CA mutations. It is designed to act on tumors with this specific genetic alteration, which is common in certain types of breast cancer and other solid tumors. The drug is being evaluated for its potential to treat these mutation-driven cancers.

Who makes RLY-5836?

RLY-5836 is being developed by Relay Therapeutics, Inc., a biopharmaceutical company. Relay Therapeutics is conducting clinical research on this investigational drug for the treatment of PIK3CA-mutated cancers, including advanced breast cancer and other solid tumors.

What phase is RLY-5836 in?

RLY-5836 is in Phase 1 clinical development. It is an investigational drug, meaning it has not been approved by regulatory authorities and is still being studied in clinical trials to evaluate its safety and efficacy in patients with PIK3CA-mutated advanced breast cancer and other solid tumors.

What clinical trials is RLY-5836 in?

RLY-5836 has been studied in a Phase 1 first-in-human clinical trial, identified as NCT05759949. This trial, titled 'First-in-Human Study of RLY-5836 in Advanced Breast Cancer and Other Solid Tumors,' enrolled 41 participants in the United States and has been completed.

Is RLY-5836 the same as other names?

RLY-5836 is the primary name for this investigational drug. No alternative names have been reported for this compound. It is being developed by Relay Therapeutics under this designation for the treatment of PIK3CA-mutated cancers.