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molecules of the month

BI-4142

oral HER2 exon 20 mutants selective inhibitor

tumor regression in the HER2YVMA xenograft model

from 12k compounds in-house library screening and opt

Nat. Cancer

Boehringer Ingelheim RCV, Vienna, AT

BI-4142 Chemical Structure oral HER2 exon 20 mutants selective inhibitor - Boehringer Ingelheim RCV, Vienna, AT
5 mins read

Context. BI-4142 (Boehringer Ingelheim) is a HER2 exon 20 insertion mutant inhibitor being developed for non-small cell lung cancer (NSCLC). Despite the general advances made in HER2-targeted therapy and the existence of several agents targeting HER2-positive breast cancer, a high unmet need exists for patients with HER2 mutant NSCLC characterized by oncogenic mutations in exon 20. Approved agents include current EGFR TKIs as well as pan-HER2 TKIs, which are limited in their efficacy due to a lack of selectivity vs. EGFR and EGFR-WT–mediated toxicities which limit effective dosing. In September 2021, the FDA granted accelerated approval to Takeda’s mobocertinib (Exkivity®, a February 2021 MOTM), which targets the related EGFR exon 20 insertion positive NSCLC. BI-4142 was developed as a selective…


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