compound 13 (GSK716)
mutant alpha-1-antitrypsin folding corrector sub-µM in cell, high predicted human %F from 2T component DEL + SBDD Bioorg. Med. Chem. Lett., Mar. 19, 2021 GlaxoSmithKline, Stevenage, UK / UCL
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NDI-101150
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inavolisib
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 RTK (receptor tyrosine kinase) signaling and is in several ongoing or planned Ph. III trials for breast cancer. In October 2024, it received FDA approval for use in combination with palbociclib and fulvestrant to treat adults with endocrine-resistant, PIK3CA-mutated, HR+/HER2- breast cancer. This article explains how it works, how it was discovered, and why it matters.
RMC-9805
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BMS-986408
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