RECRUITING Phase 1 ClinicalTrials.gov

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

Sponsor: Olema Pharmaceuticals, Inc. • ClinicalTrials.gov ID: NCT06784193

Registry updated: 2026-10-05

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Description

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).

Interventions

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

Eligibility criteria

Key Inclusion Criteria: * Participants with advanced or metastatic ER+HER2- breast cancer, mCRPC, or NSCLC (Part 1) or advanced or metastatic ER+HER2- BC or mCRPC (Part 2). * Part 1A (Dose escalation for OP-3136 monotherapy): Participants must have a tumor that is unresectable or metastatic and for which life prolonging measures do not exist or available therapies are intolerable or no longer effective. * Part 1B (Dose escalation for OP-3136 in combination with fulvestrant): Participants with advanced or metastatic ER+ HER2- breast cancer that have progressed on or after at least 1 prior line of treatment that included endocrine therapy and CDK 4/6 inhibitor in advanced or metastatic setting and must have received no more than 2 prior lines of endocrine therapy (one of which must be in combination with CDK4/6 inhibitor) and no more than 1 prior line of chemotherapy or an antibody-drug conjugate in the advanced or metastatic setting. * Part 1C (Dose escalation for OP-3136 in combination with palazestrant): Participants with advanced or metastatic ER+ HER2- breast cancer that have progressed on or after at least 1 prior line of treatment that included endocrine therapy and CDK 4/6 inhibitor in advanced or metastatic setting and must have received no more than 2 prior lines of endocrine therapy (one of which must be in combination with CDK4/6 inhibitor) and no more than 1 prior line of chemotherapy or an antibody-drug conjugate in the advanced or metastatic setting. * Part 2A (Dose Expansion in ER+ HER2- mBC for OP-3136 monotherapy): Participants must have received up to 3 prior lines of endocrine therapy (one of which must be in combination with CDK4/6 inhibitor) and up to 1 prior line of chemotherapy or an antibody-drug conjugate. * Part 2A (Dose Expansion in mCRPC for OP-3136 monotherapy): Participants must have received up to 4 lines of prior systemic therapy for prostate cancer. Prior therapy must include treatment with an androgen receptor pathway inhibitor(s). * Part 2B (Dose Expansion in ER+ HER2- mBC for OP-3136 in combination with fulvestrant OR Dose Expansion in ER+ HER2- mBC for OP-3136 in combination with palazestrant): Participants must have progressed on or after at least 1 prior line of treatment that included endocrine therapy and CDK 4/6 inhibitor in advanced or metastatic setting. Participants must have received no more than 2 prior lines of endocrine therapy in the advanced or metastatic setting and no more than 1 prior line of chemotherapy or an antibody-drug conjugate in the advanced or metastatic setting. Key Exclusion Criteria: * Prior therapy with KAT6A/B inhibitor in any treatment setting. * Participants with advanced/metastatic, symptomatic, visceral spread, that are at risk of life-threatening complications in the short term. * Known active or symptomatic central nervous system (CNS) metastases, carcinomatous meningitis, leptomeningeal disease, or a spinal cord compression that require CNS-specific treatment, or participants who did not demonstrate clinical and radiologic stability during the last 2 months prior to the first dose of study treatment or require or are currently on steroid therapy for CNS metastases. * History of cerebral vascular disease, including transient ischemic attack, within 6 months prior to the first dose of study treatment. * History of or ongoing impaired cardiac function or clinically significant cardiac disease within 6 months prior to the first dose of study treatment. Note: Additional inclusion/exclusion criteria may apply.

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

Locations

Banner MD Anderson Cancer Center — Gilbert, Arizona, United States
University of Colorado — Aurora, Colorado, United States
Florida Cancer Specialists — Sarasota, Florida, United States
University Medical Center - New Orleans — New Orleans, Louisiana, United States
Massachusetts General Hospital — Boston, Massachusetts, United States
Dana-Farber Cancer Institute — Boston, Massachusetts, United States
START - Midwest — Grand Rapids, Michigan, United States
Memorial Sloan Kettering Cancer Center — New York, New York, United States
The Ohio State University — Columbus, Ohio, United States
SCRI Oncology Partners — Nashville, Tennessee, United States
Tennessee Oncology — Nashville, Tennessee, United States
START - San Antonio — San Antonio, Texas, United States
START - Mountain Region — West Valley City, Utah, United States
The Kinghorn Cancer Centre — Darlinghurst, New South Wales, Australia
Liverpool Hospital — Liverpool, New South Wales, Australia
Macquarie University Clinical Trials Unit — Macquarie, New South Wales, Australia
Cancer Research South Australia — Adelaide, South Australia, Australia
Institut De Cancerologie De L'ouest — Saint-Herblain, Loire-Atlantique, France
Hôpital Paris Saint-Joseph — Paris, Paris, France
Institut Gustave Roussy — Villejuif, Val-de-Marne, France
Queen Mary Hospital — Hong Kong, Hong Kong, Hong Kong
START Dublin — Dublin, Dublin, Ireland
START - Barcelona — Barcelona, Barcelona, Spain
Start - Fjd — Madrid, Madrid, Spain
START Madrid - CIOCC — Madrid, Madrid, Spain

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Official Source

Data sourced from ClinicalTrials.gov, a service of the U.S. National Institutes of Health.

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