Entering the Clinic

Our investigational drug, OP-1250, is an estrogen receptor antagonist. It was developed to compete with estrogen for binding to the receptor and keep it in a completely inactive state.

Now that preclinical studies support advancing OP-1250 into the clinic, the clinical exploration of OP-1250’s potential has begun.

Our Pipeline

Target Patient Population



Phase I

Phase II

Phase III


First Clinical Phases of OP-1250

Olema has completed discovery and preclinical studies of OP-1250 required to file an IND and is currently in the Phase 1/2 development stages with OP-1250 as a single-agent treatment for estrogen receptor-positive, HER2-negative metastatic breast cancer (ER+, HER2- MBC). Initial data is anticipated in the second half of 2021.

Metastatic Breast Cancer

ER+, HER2- MBC (with and without CNS metastases)

ER+, HER2- MBC(1) (combination with CDK4/6i)(1, 2)

ER+, HER2- MBC with PIK3CA mutated (combination with PIK3αi)(1, 2)

ER+, Pre-menopausal(1)

ER+ with ESR1 mutation(1)

Programs and Biology Complementary to OP-1250

Olema is anticipating initiating clinical studies in ER+, HER2- MBC in combination with other therapies; in ER+ pre-menopausal MBC, and in ER+ MBC with ESR1 mutation during 2021. A clinical study in ER+, HER2+ MBC with CNS metastases is expected to begin in 2022.

HER2+ Metastatic Breast Cancer with CNS mets

ER+, HER2+ MBC with CNS metastases

Other Women’s Cancers

Clinical studies of OP-1250 in endometrial cancer in 2021 and other gynecologic malignancies.

Gynecology — Oncology

Endometrial Cancer(1)

Gynecologic malignancies

Clinical Trials

The first clinical trial is an ongoing Phase 1/2, open-label, multi-center, dose-escalation and expansion study evaluating the safety, pharmacokinetics, pharmacodynamics, and anti-tumor activity of daily oral administration of OP-1250.

Get in Touch

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