On June 4, 2021 Kinnate Biopharma Inc. (Nasdaq: KNTE) ("Kinnate"), a biopharmaceutical company focused on the discovery and development of small molecule kinase inhibitors for difficult-to-treat, genomically defined cancers, reported that results from preclinical studies evaluating its lead RAF inhibitor candidate, KIN-2787 (Press release, Kinnate Biopharma, JUN 4, 2021, View Source [SID1234583524]). These data will be presented today during a virtual poster session at the 57th Annual Meeting of the American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper).
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KIN-2787, Kinnate’s most advanced product candidate, is an orally available small molecule pan-RAF inhibitor being developed for the treatment of patients with lung cancer, melanoma, and other solid tumors. Unlike currently available treatments that target only Class I BRAF kinase mutations, Kinnate has designed KIN-2787 to target Class II and Class III BRAF mutations, where it would be a first-line targeted therapy, in addition to covering Class I BRAF mutations. The U.S. Food and Drug Administration (FDA) has cleared Kinnate’s Investigational New Drug (IND) application for KIN-2787 and the company anticipates initiating a first-in-human Phase 1 clinical trial of the candidate in patients with mutant BRAF-driven solid tumors in mid-2021.
"These data are important, early signals of the potential anti-tumor activity of KIN-2787 and support our IND application recently cleared by the FDA," said Eric Murphy, PhD, Chief Scientific Officer, and co-founder of Kinnate. "Our approach targets dimer signaling in specific patient populations with BRAF mutations while minimizing MAPK paradoxical activation. KIN-2787 shows pronounced in vitro and in vivo activity against human cancers driven by Class I, II and III BRAF alterations, and these results support our phase 1 clinical trial initiating shortly in these defined molecular subtypes."
The poster presentation, delivered by Aleksandra Franovic, PhD, Senior Director of Translational Medicine at Kinnate, highlights data which show that treatment with KIN-2787 resulted in exposure-dependent inhibition of MEK-ERK phosphorylation and was accompanied by the successful suppression of MAPK transcriptional targets at the RNA and protein level. High selectivity was displayed for all three RAF family kinases in screens evaluating its activity against more than 600 kinases. Due to potent dimer inhibition, KIN-2787 did not demonstrate significant paradoxical activation in these studies. Twice daily (BID) dosing was well-tolerated and led to prolonged target coverage and a trend towards more frequent and deeper tumor responses in vivo.
Kinnate’s poster presentation (Abstract #3116), titled "The next-generation pan-RAF inhibitor, KIN-2787, is active in class II and class III BRAF Mutant models," will be available for on-demand viewing at 09:00AM ET today and can be accessed via: View Source