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Jan. 11, 2024

Inavolisib: An Isoform-Selective Mutant PI3Ka Monovalent Degrader with Positive Ph. III Data


isoform-selective mutant PI3Kα degrader oral <9 mg QD, Ph. III in HR+/HER2- BC from cellular characterization of PI3Ki and opt. J. Med. Chem., December 1, 2022 Genentech, South San Francisco, CA

Drug Hunter Team

Inavolisib is a PI3Kα isoform-selective kinase inhibitor and monovalent degrader of the mutant p110α catalytic subunit of mutant PI3Kα. The molecule selectively depletes mutant p110α in cancer cells with active receptor tyrosine kinase (RTK) signaling, and is in several ongoing or planned Ph. III trials for breast cancer. Recently, Genentech announced Ph. III results with the molecule showing that it could be a best-in-class treatment option for PI3Kα-driven cancers. This article explains how it works, how it was discovered, and why it matters.



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