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pembrolizumab + palazestrant
- Development stage
- Unknown
- Lead developer
- Olema Oncology
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous, Oral
01
Overview
pembrolizumab + palazestrant is a combination therapy being developed by Olema Pharmaceuticals in collaboration with Merck (MSD) for the treatment of advanced or metastatic estrogen receptor-positive (ER+), human epidermal growth factor receptor 2-negative (HER2-) breast cancer. The combination pairs pembrolizumab (Keytruda), a humanized monoclonal antibody that acts as a programmed death receptor-1 (PD-1) inhibitor to enhance anti-tumor immune responses, with palazestrant (OP-1250), an oral small molecule that functions as both a complete estrogen receptor antagonist (CERAN) and a selective estrogen receptor degrader (SERD). By simultaneously targeting the PD-1/PD-L1 immune checkpoint and the hormonal signaling pathway that drives ER+ breast cancer, this combination aims to overcome endocrine resistance and improve clinical outcomes in patients who have progressed on prior therapies.
- Brand names
- Keytruda
- Other names
- pembrolizumab and palazestrantKeytruda and palazestrantpembrolizumab and OP-1250
02
Targets
PDCD1 (Programmed cell death protein 1 receptor)ESR1 (ERα)
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