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Kinnate Doses First Patient in Phase I Trial of FGFR Inhibitor

NEW YORK – Kinnate Biopharma announced today that it has begun dosing patients in a Phase I trial of its small molecule kinase inhibitor KIN-3248. 

The trial will enroll around 120 patients with bile duct cancer, urothelial carcinoma, or certain other solid tumors whose cancers harbor alterations in fibroblast growth factor receptor 2 and 3 genes. The two-part trial will include a dose escalation study followed by a study of safety and efficacy in naïve and pretreated patients with FGFR inhibitors. 

Aberrations in FGFR1-4 are found in 5-10 percent of all human cancers. But in intrahepatic cholangiocarcinoma they represent 10 to 20 percent, and in urothelial cancer 20 to 35 percent. KIN-3248 is an irreversible pan-FGFR inhibitor that is designed to overcome acquired resistance to current FGFR-targeted therapies. The company reported that the drug had inhibitory activity across a broad range of clinically relevant FGFR mutations believed to drive both primary disease and acquired resistance. 

Kinnate presented preclinical data at the JCA-AACR Precision Cancer Medicine International Conference last year showing that KIN-3248 was active against wild-type FGFR1-4, but not against non-FGFR kinases. It also inhibited FGFRs with mutations associated with resistance to FGFR inhibitors including the FGFR2 and FGFR3 gatekeeper mutations, V565X and V555M, molecular brake mutations, N550X and N540X, and activation loop mutations, L618V and K650M. 

Kinnate is also preparing to begin a Phase I trial of its RAF inhibitor, KIN-2787, in patients with melanoma and non-small cell lung cancer carrying alterations in BRAF and NRAS-mutant melanoma.