palazestrant + palbociclib

Palazestrant + palbociclib is an investigational oral combination therapy for the treatment of estrogen receptor-positive (ER+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. Palazestrant (OP-1250) is a novel, orally available complete estrogen receptor antagonist and selective estrogen receptor degrader (CERAN/SERD). It binds to the estrogen receptor and fully blocks its activity while promoting its degradation, thereby inhibiting ER-driven tumor cell proliferation. Palbociclib is a cyclin-dependent kinase 4/6 (CDK4/6) inhibitor that blocks cell cycle progression by inhibiting CDK4/6-mediated phosphorylation of the retinoblastoma protein, leading to G1 phase cell cycle arrest. The combination aims to provide dual blockade of ER signaling and cell cycle progression in hormone-driven breast cancers. Clinical studies have shown that this combination has an acceptable safety profile with no significant drug-drug interactions or increased toxicity compared to standard regimens[1][3][5]. The primary indication under investigation is ER+/HER2- advanced or metastatic breast cancer.

Other names

OP-1250 plus palbociclibOP1250 plus palbociclibOP 1250 plus palbociclibpalazestrant plus palbociclib