isoform-selective mutant PI3K_ degrader

oral <9 mg QD, Ph. III in HR+/HER2- BC

from cellular characterization of PI3Ki and opt.

bioRxiv, May 13, 2021

Genentech, South San Francisco, CA

The Genentech PI3Kα isoform-selective kinase inhibitor and mutant PI3Kα degrader GDC-0077 (inavolisib) selectively depletes the oncogenic mutant p110α catalytic subunit of PI3Kα in cancer cells with active receptor tyrosine kinase (RTK)…

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