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BPI-1178 + fulvestrant is an investigational combination therapy comprised of BPI-1178, a novel, orally administered cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor, and fulvestrant, a selective estrogen receptor degrader (SERD). BPI-1178 inhibits CDK4/6, blocking retinoblastoma protein (Rb) phosphorylation and causing G1 cell cycle arrest, thereby inhibiting tumor cell proliferation. This combination is being developed to treat hormone receptor positive (HR+), human epidermal growth factor receptor 2 negative (HER2-) advanced or recurrent breast cancer, particularly in patients who have progressed following non-fulvestrant first-line endocrine therapy[1][2][3][5]. Fulvestrant degrades and antagonizes estrogen receptors, disrupting hormone-driven cancer cell growth.
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