2682003-36-5

BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50= 5 nM. BI-4142 showed efficacy against HER2 exon 20 insertion-driven tumors, while preserving EGFR wt signaling.

BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50 of 5 nM[1].

HER2: 5 nM (IC₅₀)

[1] Wilding B, et al. Discovery of potent and selective HER2 inhibitors with efficacy against HER2 exon 20 insertion-driven tumors, which preserve wild-type EGFR signaling. Nat Cancer. 2022 Jul;3(7):821-836. DOI:10.1038/s43018-022-00412-y