Description:
This clinical trial is a Phase 1-2, open-label, multi-center, dose-escalation and expansion study evaluating the safety, pharmacokinetics, pharmacodynamics, and antitumor activity of daily oral administration of OP-1250.
This clinical trial is a Phase 1-2, open-label, multi-center, dose-escalation and expansion study evaluating the safety, pharmacokinetics, pharmacodynamics, and antitumor activity of daily oral administration of OP-1250.
Recruiting
Phase 1/Phase 2
Drug | Synonyms | Arms |
---|---|---|
OP-1250 | OP-1250 Dose Escalation |
OP-1250 is a small molecule Complete Estrogen Receptor ANtagonist (CERAN). OP-1250 potently competes with the endogenous activating estrogenic ligand 17-beta estradiol for binding in the ligand binding pocket. OP-1250 blocks estrogen-driven transcriptional activity, inhibits estrogen-driven breast cancer cell growth, and induces degradation of the estrogen receptor.
Name | Type | Description | Interventions |
---|---|---|---|
OP-1250 Dose Escalation | Experimental | This portion of the study will evaluate the safety and pharmacology of a range of OP-1250 doses administered daily in subjects with advanced and/or metastatic hormone receptor (HR)-positive, HER2-negative breast cancer and to determine the RP2D |
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OP-1250 Expansion | Experimental | This portion of the study further explores the clinical activity, safety and pharmacology of OP-1250 monotherapy at the RP2D and to estimate preliminary data of anti-tumor efficacy |
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Inclusion Criteria: - Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1 - Must not have received prior oral endocrine therapy > 2 weeks prior to first dose - Must not have received prior fulvestrant, chemotherapy, antibody therapy, or investigational therapy ≤ 4 weeks prior to the first dose - Adequate hepatic function - Adequate renal function - Normal coagulation panel - Willingness to use effective contraception Exclusion Criteria: - Gastrointestinal disease - Significant renal disease - Significant cardiovascular disease - Significant ECG abnormalities - Ongoing systemic bacterial, fungal, or viral infection (requiring antimicrobial therapy) - Pregnancy or breastfeeding
Maximum Eligible Age: | N/A |
Minimum Eligible Age: | 18 Years |
Eligible Gender: | All |
Healthy Volunteers: | No |
Measure: | Determine MTD and/or RP2D of OP-1250 when used as a single agent |
Time Frame: | Up to one year |
Safety Issue: | |
Description: | Number of patients with DLT as defined in the protocol |
Phase: | Phase 1/Phase 2 |
Primary Purpose: | Interventional |
Overall Status: | Recruiting |
Lead Sponsor: | Olema Pharmaceuticals, Inc. |
May 5, 2021