NCT06784193

Phase 1 Study of OP-3136 in Advanced or Metastatic Solid Tumors

A Phase 1 First-in-Human, Open-Label, Multicenter Study of OP-3136 in Adult Participants With Advanced or Metastatic Solid Tumors

• Status: Recruiting
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 180 (estimated)
• Sponsor: Olema Pharmaceuticals, Inc. · Industry
• Sex: All
• Age: 18 Years
• Healthy volunteers: Not accepted

Summary

This is a first-in-human, open-label, multicenter phase 1 study to evaluate safety, tolerability, pharmacokinetics (PK), pharmacodynamics (PD), and preliminary efficacy of OP-3136, a lysine acetyltransferases 6A and 6B (KAT6A/B) inhibitor, as monotherapy and in combination with other anticancer agents in participants with advanced solid tumors. This study consists of 2 parts: a dose escalation part (Part 1) and dose expansion part (Part 2).

Detailed description

Part 1A (Dose Escalation for OP-3136 Monotherapy): This part of the study will evaluate the safety, tolerability, and PK in a range of doses of OP-3136, a lysine acetyltransferases 6A and 6B (KAT6A/B) inhibitor, administered orally once daily to participants with ER+ HER2- advanced or metastatic breast cancer (mBC), advanced or metastatic castration resistant prostate cancer (mCRPC), or advanced or metastatic non-small cell lung cancer (mNSCLC), and determine the maximum tolerated dose (MTD) and the recommended dose/regimen for expansion (RDE). Part 1B (Dose Escalation for OP-3136 in Combination with Fulvestrant): This part of the study will evaluate the safety and PK of OP-3136 administered in combination with fulvestrant in participants with ER+ HER2- mBC, and determine MTD and RDE for this combination. Part 1C (Dose Escalation for OP-3136 in Combination with Palazestrant): This part of the study will evaluate the safety and PK of OP-3136 administered in combination with palazestrant in participants with ER+ HER2- mBC, and determine MTD and RDE for this combination. Part 2A (Dose Expansion for OP-3136 Monotherapy): This part will evaluate two expansion cohorts at the monotherapy RDE from part 1 in participants with ER+ HER2- mBC and participants with mCRPC. Part 2B (Dose Expansion for OP-3136 in Combination with Fulvestrant OR Palazestrant): This part will evaluate the RDEs for OP-3136 in combination with fulvestrant from Part 1B OR the RDEs of OP-3136 in combination with palazestrant in an expansion cohort in participants with ER+ HER2- mBC.

Conditions

• Advanced or Metastatic ER+ HER2- Breast Cancer (mBC)
• Advanced or Metastatic Non-Small Cell Lung Cancer (NSCLC)
• Advanced or Metastatic Castration-Resistant Prostate Cancer (mCRPC)
• Metastatic Breast Cancer
• Fulvestrant
• Palazestrant

Interventions

Type	Name	Description
DRUG	OP-3136	Selective inhibitor of HAT enzymes KAT6A and KAT6B
DRUG	Fulvestrant	Selective estrogen receptor degrader (SERD)
DRUG	Palazestrant	Complete estrogen receptor antagonist (CERAN)

Timeline

• Start date: 2024-12-16
• Primary completion: 2027-05-30
• Completion: 2027-08-30
• First posted: 2025-01-20
• Last updated: 2025-10-10

Locations

8 sites across 2 countries: United States, Australia

Regulatory

• FDA-regulated drug study