Drug intelligence / Profile preview

palazestrant + atirmociclib

Development stage
Phase 1
Lead developer
Olema Oncology
Modality
Small Molecules
Administration
Oral
01

Overview

palazestrant + atirmociclib is an investigational oral combination therapy being evaluated for the treatment of estrogen receptor-positive (ER+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. The combination consists of palazestrant (OP-1250), an orally available complete estrogen receptor antagonist (CERAN) and selective estrogen receptor degrader (SERD) developed by Olema Oncology, and atirmociclib (PF-07220060), a highly selective cyclin-dependent kinase 4 (CDK4) inhibitor developed by Pfizer. By simultaneously degrading and blocking the estrogen receptor and selectively inhibiting CDK4, this combination aims to overcome endocrine resistance and inhibit tumor cell proliferation with a potentially improved safety profile compared to dual CDK4/6 inhibitors.

Other names
OP-1250 + PF-07220060OP-1250 + atirmociclibpalazestrant + PF-07220060
02

Targets

CDK4 (Cyclin-dependent kinase 4)ER (Estrogen receptor)

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