On November 6, 2024 C4 Therapeutics, Inc. (C4T) (Nasdaq: CCCC), a clinical-stage biopharmaceutical company dedicated to advancing targeted protein degradation science, reported its partner Betta Pharmaceuticals has dosed the first patient in the Phase 1 clinical trial of CFT8919, an orally bioavailable allosteric degrader of EGFR L858R for non-small cell lung cancer (NSCLC), in Greater China (Press release, C4 Therapeutics, NOV 6, 2024, View Source [SID1234648576]).

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"We are pleased to see CFT8919, our fourth small molecule degrader to enter the clinic, begin the journey through clinical development in Greater China with our partner Betta Pharmaceuticals," said Len Reyno, M.D., chief medical officer of C4 Therapeutics. "CFT8919 may offer an exciting advancement in treating non-small cell lung cancer driven by an EGFR mutation, which is currently treated with EGFR tyrosine kinase inhibitors (TKIs) that offer a less durable response for patients with the EGFR L858R driver mutation than those with other driver mutations. We, along with our partner Betta Pharmaceuticals, believe CFT8919 may offer a novel targeted therapy for patients and physicians searching for treatment options."

C4T designed CFT8919 to be potent and selective against EGFR bearing an oncogenic L858R mutation and capable of overcoming common EGFR secondary mutations that render patients refractory to EGFR TKIs. The EGFR mutation is particularly common in NSCLC patients of Asian heritage. In China, where approximately 693,000 patients are diagnosed with NSCLC annually, approximately 50 percent of diagnoses are driven by the EGFR mutation. The EGFR L858R mutation is the second most common EGFR mutation, found in approximately 40 percent of patients diagnosed with an EGFR mutation in the U.S. and China.

In 2023, C4T and Betta Pharmaceuticals entered into a strategic collaboration to develop, manufacture and commercialize CFT8919 in Greater China, including Hong Kong SAR, Macau SAR and Taiwan. Under the terms of the agreement, C4T is eligible for up to $357 million in potential milestones plus royalties on net sales. C4T retains development and commercialization rights for CFT8919 in the United States, European Union and rest of the world.

About CFT8919
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, CFT8919 retains full activity against additional EGFR mutations that confer resistance against approved EGFR inhibitors including L858R-C797S, L858R-T790M, and L858R-T790M-C797S.