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buparlisib + fulvestrant

Development stage: Unknown
Lead developer: Novartis
Modality: Small Molecules
Administration: Oral, Intramuscular

Overview

Buparlisib + fulvestrant is a combination therapy consisting of buparlisib, an oral pan-class I PI3K inhibitor, and fulvestrant, a selective estrogen receptor degrader. This combination is used primarily for the treatment of hormone receptor-positive (HR+), HER2-negative metastatic breast cancer, particularly in patients who have progressed on prior endocrine therapy. The combination works by simultaneously targeting the PI3K signaling pathway (buparlisib) and degrading estrogen receptors (fulvestrant), addressing two key mechanisms of resistance in hormone receptor-positive breast cancer.

Targets

PI3K (Phosphoinositide-3-kinase regulatory subunit 6)ESR1 (ERα)

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