zipalertinib + chemotherapy

Zipalertinib + chemotherapy is a combination drug regimen currently under investigation for the treatment of advanced or metastatic non-small cell lung cancer (NSCLC) harboring epidermal growth factor receptor (EGFR) exon 20 insertion mutations. Zipalertinib (CLN-081/TAS6417) is an orally available, next-generation, irreversible EGFR tyrosine kinase inhibitor with a novel pyrrolopyrimidine scaffold, offering potent and selective inhibition of mutant EGFR while sparing wild-type EGFR. In the pivotal REZILIENT3 Phase 3 trial, zipalertinib is combined with first-line standard-of-care platinum-based chemotherapy (pemetrexed plus cisplatin or carboplatin). The aim of this combination is to increase anti-tumor efficacy compared to chemotherapy or EGFR TKI therapy alone, as supported by prior clinical evidence in EGFR-mutant NSCLC. Zipalertinib has demonstrated favorable tolerability, with a low frequency of high-grade rash and diarrhea, and has received Breakthrough Therapy Designation from the FDA for this indication[2][1][3][5][6][9].

Other names

zipalertinib + chemotherapy