Study of OP-3136 in Advanced or Metastatic Solid Tumors

Last updated: May 13, 2025
Sponsor: Olema Pharmaceuticals, Inc.
Overall Status: Active - Recruiting

Phase

1

Condition

N/A

Treatment

OP-3136

Clinical Study ID

NCT06784193
OP-3136-101
  • Ages > 18
  • All Genders

Study Summary

This is a first-in-human, open-label, multicenter phase 1 study to evaluate the safety, tolerability, pharmacokinetics (PK), pharmacodynamics (PD), and preliminary efficacy of OP-3136, a lysine acetyltransferases 6A and 6B (KAT6A/B) inhibitor, in participants with advanced solid tumors.

This study consists of 2 parts: a dose escalation part (Part 1) and dose expansion part (Part 2).

Eligibility Criteria

Inclusion

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 1 (Dose escalation): Participants must have a tumor that is unresectable ormetastatic and for which life prolonging measures do not exist or availabletherapies are intolerable or no longer effective.

  • Part 2 (Dose Expansion in ER+ HER2- mBC): Participants must have received up to 3prior lines of endocrine therapy (one of which must be in combination with CDK4/6inhibitor) and up to 1 prior line of chemotherapy or an antibody-drug conjugate.

  • Part 2 (Dose Expansion in mCRPC): Participants must have received up to 4 lines ofprior systemic therapy for prostate cancer. Prior therapy must include treatmentwith an androgen receptor pathway inhibitor(s).

Exclusion

Key Exclusion Criteria:

  • Prior therapy with KAT6A/B inhibitor in any treatment setting.

  • Participants with advanced/metastatic, symptomatic, visceral spread, that are atrisk of life-threatening complications in the short term.

  • Known active or symptomatic central nervous system (CNS) metastases, carcinomatousmeningitis, leptomeningeal disease, or a spinal cord compression that requireCNS-specific treatment, or participants who did not demonstrate clinical andradiologic stability during the last 2 months prior to the first dose of studytreatment or require or are currently on steroid therapy for CNS metastases.

  • History of cerebral vascular disease, including transient ischemic attack, within 6months prior to the first dose of study treatment.

  • History of or ongoing impaired cardiac function or clinically significant cardiacdisease within 6 months prior to the first dose of study treatment.

Note: Additional inclusion/exclusion criteria may apply.

Study Design

Total Participants: 90
Treatment Group(s): 1
Primary Treatment: OP-3136
Phase: 1
Study Start date:
December 16, 2024
Estimated Completion Date:
August 30, 2027

Study Description

Part 1 (Dose Escalation): 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 2 (Dose Expansion): This part will evaluate the recommended dose and regimen from Part 1 in the expansion cohorts of participants with ER+ HER2- mBC and participants with mCRPC.

Connect with a study center

  • Cancer Research South Australia

    Adelaide, South Australia 5000
    Australia

    Active - Recruiting

  • Florida Cancer Specialists

    Sarasota, Florida 34232
    United States

    Active - Recruiting

  • University Medical Center - New Orleans

    New Orleans, Louisiana 70112
    United States

    Active - Recruiting

  • START - Midwest

    Grand Rapids, Michigan 49546
    United States

    Active - Recruiting

  • SCRI Oncology Partners

    Nashville, Tennessee 37203
    United States

    Active - Recruiting

  • START - San Antonio

    San Antonio, Texas 78229
    United States

    Active - Recruiting

  • START - Mountain Region

    West Valley City, Utah 84119
    United States

    Active - Recruiting

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