Study of OP-3136 in Advanced or Metastatic Solid Tumors
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-3136Summary
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
- [email protected]
Status
- RECRUITING
Central Contacts
- There may be multiple sites in this clinical trial Olema Clinical Trial Lead
- 415-651-7206
- [email protected]
Status
- RECRUITING
Central Contacts
- There may be multiple sites in this clinical trial Olema Clinical Trial Lead
- 415-651-7206
- [email protected]
Status
- RECRUITING
Central Contacts
- There may be multiple sites in this clinical trial Olema Clinical Trial Lead
- 415-651-7206
- [email protected]
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-3136Description:
OP-3136
Part 2 Dose Expansion - mBC
DRUG:
OP-3136Description:
OP-3136
Part 2 Dose Expansion - mCRPC
DRUG:
OP-3136Description:
OP-3136
Outcome Measures
Primary Outcome Measures
Number of participants with dose-limiting toxicities in the Dose Escalation Arms
Incidence of adverse events and laboratory abnormalities
Secondary Outcome Measures
Maximum observed concentration (Cmax)
Time to maximum concentration (Tmax)
Area under the curve from time zero to 24 hours (AUC0-24)
Overall Response Rate (ORR)
Duration of Response (DOR)
Clinical Benefit Rate (CBR)
Timeline
Last Updated
March 6, 2025Start Date
January 20, 2025Today
May 12, 2025Completion Date ( Estimated )
August 30, 2027
Sponsors of this trial
Lead Sponsor
Olema Pharmaceuticals, Inc.