TAS2940

TAS2940 is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor developed by Otsuka for the treatment of cancers with HER2 (ERBB2) and EGFR (ERBB1) aberrations. It potently inhibits both wild-type and mutant forms of HER2 and EGFR, including clinically relevant mutations such as HER2 V777L, A775_G776insYVMA, and various EGFR exon 20 insertions. TAS2940 has demonstrated strong preclinical efficacy in models of breast cancer, non-small cell lung cancer (NSCLC), glioblastoma (GBM), and other solid tumors with ERBB pathway alterations—especially those involving brain metastases or primary brain tumors—due to its improved ability to penetrate the blood-brain barrier. The drug acts by inhibiting phosphorylation of HER2/EGFR/HER3 signaling pathways as well as downstream effectors like AKT and ERK. Clinical development is ongoing in advanced solid tumors with documented HER2 or EGFR aberrations.