Theseus Pharma: FDA Clears Application for Treatment of Gastrointestinal Stromal Tumors

 Theseus Pharmaceuticals, Inc. ("Theseus"), a biopharmaceutical company focused on improving the lives of cancer patients through the discovery, development and commercialization of transformative targeted therapies, today announced U.S. Food and Drug Administration (FDA) clearance of an investigational new drug (IND) application to evaluate THE-630, the company's lead development candidate, in patients with gastrointestinal stromal tumors (GIST). THE-630 is a pan-variant inhibitor of the receptor tyrosine kinase KIT designed for patients with advanced GIST whose cancer has developed resistance to earlier lines of therapy.

"The IND clearance for THE-630 marks an important milestone for Theseus as we transition into a clinical-stage company," said Tim Clackson, Ph.D., president and CEO of Theseus Pharmaceuticals. "Patients with previously-treated GIST often have tumors that have developed more than one mutation in KIT that causes resistance to treatment, and we believe treatment with a kinase inhibitor that is active against all relevant mutations—that is, a pan-variant inhibitor—is a promising approach to address this key mechanism of resistance. We look forward to initiating the Phase 1/2 clinical trial and evaluating the potential that THE-630 may offer for patients with advanced GIST who have developed resistance to prior therapy."

THE-630 exhibits potent in vitro activity against all known classes of KIT activating and resistance mutations in GIST. In preclinical studies, THE-630 achieved predicted pan-variant KIT inhibitory blood concentrations at tolerable doses and induced significant anti-tumor activity. Theseus plans to initiate a Phase 1/2 dose escalation and expansion clinical trial of THE-630 in patients with previously treated advanced GIST between late fourth quarter 2021 and mid-first quarter 2022.

https://www.biospace.com/article/releases/theseus-pharmaceuticals-announces-fda-clearance-of-investigational-new-drug-application-for-the-630-a-pan-variant-kit-inhibitor-in-development-for-the-treatment-of-gastrointestinal-stromal-tumors-gist-/