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)…