Drug intelligence / Profile preview

inavolisib + palbociclib + letrozole

Development stage: Unknown
Lead developer: Genentech
Modality: Small Molecules
Administration: Oral

Overview

A combination therapy consisting of inavolisib (a potent and selective PI3Kα inhibitor that promotes degradation of mutated p110α), palbociclib (a CDK4/6 inhibitor), and letrozole (an aromatase inhibitor). This combination targets multiple pathways involved in breast cancer progression, including the PI3K/AKT pathway and cell cycle regulation. It has shown promising antitumor activity in PIK3CA-mutated, hormone receptor-positive, HER2-negative locally advanced or metastatic breast cancer, with a median progression-free survival of 23.3 months in Phase I/Ib trials.

Targets

CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)PIK3CA (Phosphoinositide 3-kinase alpha)CYP19A1 (Aromatase)

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