Study of OP-3136 in Advanced or Metastatic Solid Tumors

Clinicaltrials.gov ID: NCT06784193
db-list-check Status RECRUITING
b-loader Phase PHASE1
b-people Age ≥ 18 Years
b-bullseye-arrow Enrollments 90

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)

Drugs

OP-3136

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).

Detailed 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.

Locations

4 locations Found with status Recruiting

Status

  • RECRUITING

Central Contacts

  • There may be multiple sites in this clinical trial Olema Clinical Trial Lead
  • 415-651-7206

Status

  • RECRUITING

Central Contacts

  • There may be multiple sites in this clinical trial Olema Clinical Trial Lead
  • 415-651-7206

Status

  • RECRUITING

Central Contacts

  • There may be multiple sites in this clinical trial Olema Clinical Trial Lead
  • 415-651-7206

Status

  • RECRUITING

Central Contacts

  • There may be multiple sites in this clinical trial Olema Clinical Trial Lead
  • 415-651-7206

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 1 (Dose escalation): 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 2 (Dose Expansion in ER+ HER2- mBC): 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 2 (Dose Expansion in mCRPC): 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).

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.

Study Plan

Part 1 Dose Escalation

  • DRUG:

    OP-3136

    Description:

    OP-3136

Part 2 Dose Expansion - mBC

  • DRUG:

    OP-3136

    Description:

    OP-3136

Part 2 Dose Expansion - mCRPC

  • DRUG:

    OP-3136

    Description:

    OP-3136

Outcome Measures

Primary Outcome Measures

Number of participants with dose-limiting toxicities in the Dose Escalation Arms

Time Frame: Up to 28 days

Incidence of adverse events and laboratory abnormalities

Time Frame: Up to 26 months

Secondary Outcome Measures

Maximum observed concentration (Cmax)

Time Frame: Up to 26 months

Time to maximum concentration (Tmax)

Time Frame: Up to 26 months

Area under the curve from time zero to 24 hours (AUC0-24)

Time Frame: Up to 26 months

Overall Response Rate (ORR)

Time Frame: Up to 26 months

Duration of Response (DOR)

Time Frame: Up to 26 months

Clinical Benefit Rate (CBR)

Time Frame: Up to 26 months

Timeline

  • Last Updated
    March 6, 2025
  • Start Date
    January 20, 2025
  • Today
    May 12, 2025
  • Completion Date ( Estimated )
    August 30, 2027

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