Exarafenib (KIN-2787) is an orally administered, potent and selective investigational small molecule pan-RAF inhibitor. KN-8701 is an ongoing, global Phase 1 clinical trial (NCT04913285) evaluating exarafenib in patients with advanced solid tumors harboring BRAF-altered and/or who have NRAS mutant melanoma. KN-8701 contains a two-part dose escalation: Part A1 evaluated exarafenib as a monotherapy across BRAF alterations and tumor types, and Part A2 is evaluating exarafenib in combination with binimetinib, a MEK inhibitor. Part B, dose expansion, is evaluating exarafenib monotherapy at 300 mg bid in patients with BRAF-altered cancers including lung cancer, melanoma and other solid tumors. Watch: Exarafenib Mechanism of Action
As of September 18, 2023, exarafenib plus binimetinib was generally well-tolerated in two dose cohorts and cleared by a dose review committee. In the fourth quarter of 2023, the Company intends to select two doses for further development.