inavolisib + abemaciclib + fulvestrant

This is a **combination therapy** consisting of inavolisib, abemaciclib, and fulvestrant, explored for the treatment of hormone receptor–positive, HER2-negative advanced or metastatic breast cancer, particularly in cases with *PIK3CA* mutation and endocrine resistance[4][5]. - **Inavolisib** is a highly selective PI3Kα inhibitor that both inhibits and degrades the mutated p110α subunit encoded by *PIK3CA*, targeting aberrant PI3K signaling responsible for tumor growth and resistance mechanisms[4]. - **Abemaciclib** is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which blocks cell cycle progression in cancer cells[5]. - **Fulvestrant** is an estrogen receptor antagonist that binds, blocks, and accelerates degradation of the estrogen receptor, eliminating estrogen-driven signaling[4][5]. This triplet combines targeted therapy against three fundamental drivers of breast cancer: PI3K signaling, cell cycle progression, and estrogen receptor signaling. Early phase data demonstrate synergistic anti-tumor activity, with objective response rates consistent with the profiles of the individual drugs[5]. The triplet is currently under clinical investigation and not yet approved for this combination.

Other names

inavolisib + abemaciclib + fulvestrant