STX-721 is an oral, covalent, mutant-selective inhibitor of EGFR and HER2 Exon 20 insertion (ex20ins) mutants, a well-validated target that saw its first approval with mobocertinib in 2022. Inhibition of wild-type (WT) EGFR is well-established to cause skin and gut toxicities, and selective inhibition of EGFR ex20ins mutants over WT may also allow greater efficacy to be seen at tolerated doses. This is an excellent case study for PK optimization with a covalent inhibitor, and [...]
STX-721: EGFR Ex20ins Inhibitor with Potential Best-in-Class Selectivity.
STX-721
oral covalent EGFR ex20ins mutant-selective inhibitor Ph. I for NSCLC with EGFR ex20ins mutations opt. from screen of TKI's for EGFR ex20ins selectivity First Disclosures, ACS Fall 2023 Scorpion Therapeutics, Boston, MA
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