Sevabertinib

Sevabertinib (BAY 2927088) is an oral, reversible tyrosine kinase inhibitor (TKI) developed for the treatment of non-small cell lung cancer (NSCLC). It is specifically designed to target tumours harbouring activating mutations in the HER2 (ERBB2) tyrosine kinase domain (TKD), a genetic driver found in a subset of NSCLC patients. The drug is active against a broad spectrum of HER2 alterations, including exon 20 insertions and various point mutations.

Sevabertinib functions as a dual inhibitor that targets both HER2 and the epidermal growth factor receptor (EGFR). By reversibly binding to these kinases, sevabertinib inhibits the phosphorylation of HER2, thereby blocking the activation of downstream signalling pathways critical for tumor growth and survival. In vitro studies demonstrate that this inhibition suppresses the proliferation of cancer cells that either over-express wild-type HER2 or harbor specific HER2 mutations.