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Feb. 9, 2022

Inavolisib: an PI3Kα Isoform-Selective Kinase Inhibitor and Mutant PI3Kα Degrader

Genentech mPI3Kα Degrader

isoform-selective mutant PI3Kα degrader oral <9 mg QD, Ph. III in HR+/HER2- BC from cellular characterization of PI3Ki and opt. inovalisib (GDC-0077) Genentech, South San Francisco, CA

Drug Hunter Team

The Genentech PI3Kα isoform-selective kinase inhibitor and mutant PI3Kα degrader inavolisib selectively depletes the oncogenic mutant p110α catalytic subunit of PI3Kα in cancer cells with active receptor tyrosine kinase (RTK) signaling. The gene encoding p110α, PIK3CA, is one of the most frequently mutated oncogenes, with over 2M cancer [...]



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