Drug intelligence / Profile preview

bicalutamide + palbociclib

Development stage
Unknown
Lead developer
Memorial Sloan Kettering Cancer Center
Modality
Small Molecules
Administration
Oral
01

Overview

Bicalutamide + palbociclib is an investigational oral combination therapy being studied primarily for the treatment of androgen receptor (AR) positive, triple-negative metastatic breast cancer. Bicalutamide is a non-steroidal antiandrogen that acts as an antagonist of the androgen receptor, blocking androgen-driven tumor growth. Palbociclib is a selective cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor that prevents cell cycle progression from G1 to S phase by inhibiting phosphorylation of retinoblastoma protein (Rb), thereby suppressing tumor cell proliferation. The rationale for combining these agents is based on preclinical and early clinical evidence suggesting synergistic activity in AR+ breast cancer subtypes, particularly those with intact Rb protein expression[1][3][8][10].

02

Targets

CDK6 (Cyclin-dependent kinase 6)AR (Adrenergic receptors)CDK4 (Cyclin-dependent kinase 4)

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