Betta Pharmaceuticals CFT8919 approved for clinical trials in the United States

Betta Pharmaceuticals and C4 Therapeutics have jointly developed CFT8919, an orally bioavailable BiDAC™ degrader designed to selectively combat EGFRL858R in non-small cell lung cancer (NSCLC) patients.

Recently, C4 Therapeutics announced that its application for clinical trials of CFT8919 has been approved by the US Food and Drug Administration. CFT8919 has demonstrated activity in in vitro and in vivo models of EGFR L858R-driven NSCLC, targeting a wide range of on-target resistance mutations and exhibiting intracranial activity with potential for preventing or treating brain metastases in patients. CFT8919 has shown good selectivity by binding to the mutated conformational site of L858R while effectively targeting secondary EGFR resistance mutations such as T790M or C797S.

Additionally, CFT8919 has exhibited strong cell proliferation inhibition activity against both L858R single mutations and L858R secondary resistance mutations that arise after resistance to drugs such as osimertinib and erlotinib, demonstrating good selectivity for the wild-type EGFR.