Advancing Palazestrant and OP-3136 Through Development

Palazestrant, our lead product candidate, is a novel, orally available complete estrogen receptor antagonist (CERAN) and selective estrogen receptor degrader (SERD) that blocks both transcriptional activation function domains, AF1 and AF2, resulting in complete inhibition of ER-driven transcription regardless of ESR1 mutation status. It is being evaluated as a single agent in the ongoing pivotal Phase 3 clinical trial, OPERA-01, and in combination with ribociclib in the ongoing pivotal Phase 3 clinical trial, OPERA-02. Palazestrant is also being evaluated in multiple Phase 1/2 studies in combination with ribociclib, palbociclib, alpelisib, everolimus, and atirmociclib.

OP-3136, our earlier-stage product candidate, is a novel, orally available small molecule that potently and selectively inhibits lysine acetyltransferase 6 (KAT6), an epigenetic target that is dysregulated in breast and other cancers. Patients are currently enrolling in the Phase 1 clinical trial.

Our Pipeline

Target Patient Population

Discovery

Nonclinical

Phase I

Phase II

Phase III

Clinical
Collaboration

Palazestrant (OP-1250) - ER+/HER2- Metastatic Breast Cancer

1st line combo with CDK 4/6i ribociclib

2/3 line monotherapy

Combo therapy with CDK4/6i ribociclib

Combo therapy with CDK4/6i palbociclib

Combo therapy with CDK4i atirmociclib

Combo therapy with PI3Ki alpelisib

Combo therapy with mTOR inhibitor everolimus

OP-3136 KAT6 Inhibitor - Breast Cancer and Other Solid Tumors

ER+/HER2- metastatic breast cancer/castrate-resistant prostate/lung cancer