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molecules of the month

mobocertinib

EGFR exon 20 mutant inhibitor, oral once-daily

FDA-approved for EGFR ex20+ NSCLC

from cellular screening + SBDD

Bioorg. Med. Chem. Lett., 21 November 2022

ARIAD/Takeda, Cambridge, MA

mobocertinib chemical structure EGFR exon 20 mutant inhibitor, oral once-daily- ARIAD/Takeda, Cambridge, MA
6 mins read

The first approved EGFR exon 20 mutant inhibitor. While there are now three generations of EGFR inhibitors approved, patients harboring the common EGFR exon 20 insertion resistance mutations haven’t responded well to previously approved drugs. This mutation class makes up 4-12% of all mutant EGFR-positive NSCLC cases and has the highest incidence beyond the most common EGFR mutations, illustrating this unmet medical need. Mobocertinib (Exkivity) is a Breakthrough Therapy that we highlighted as a Molecule of the Month in February 2021 and was recently approved for NSCLC as the first EGFR exon 20 inhibitor. Details around its discovery have finally been disclosed, warranting this update. EGFR exon 20 mutants are hard to drug. Unlike active site mutations like EGFR T790M,…


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