CFT8919 is an orally bioavailable allosteric BiDAC™ degrader that is designed to be potent and selective against EGFR bearing an oncogenic L858R mutation. In preclinical studies, CFT8919 is active in in vitro and in vivo models of L858R driven non-small cell lung cancer. Importantly, in preclinical studies, CFT8919 retains full activity against additional EGFR mutations that confer resistance against approved EGFR inhibitors including L858R-C797S, L858R-T790M, and L858R-T790M-C797S. In 2023, C4T and Betta Pharmaceuticals entered into an exclusive licensing agreement for the development and commercialization of CFT8919 in Greater China, including Hong Kong SAR, Macau SAR and Taiwan.
CFT8919
Opportunity for Targeted Protein Degradation
Many patients with non-small cell lung cancer benefit from treatment with EGFR tyrosine kinase inhibitors, or TKIs. However, patients ultimately develop resistance to EGFR TKIs, often by acquisition of a secondary resistance mutation in EGFR. A third-generation covalent EGFR inhibitor, osimertinib, can overcome this resistance mechanism and is now approved in the first-line setting.
However, acquired resistance remains an issue. Additionally, patients with the EGFR L858R mutation experience a less durable response to approved EGFR inhibitors, including osimertinib. Patients who progress after osimertinib lack effective treatment options.
