First-in-human study of HM95573, a novel oral RAF inhibitor, in patients with solid tumors.

2570Background: HM95573 is a novel and selective RAF kinase inhibitor which showed potent anti-tumor activities in BRAF, KRAS and NRAS mutant model in vitro and in vivo. This phase 1 trial evaluated the safety, tolerability, pharmacokinetics (PK), and anti-tumor activity of HM95573 in patients with solid tumors. Interim results from the phase 1 study are presented here. Methods: Patients who had solid tumor with BRAF, KRAS or NRAS mutation were enrolled. HM95573 was administered everyday with 21-day cycle and treatment cycle has been repeated until disease progression or dose-limiting toxicity (DLT). Dose escalation was performed with PK-guided dose escalation method until target AUC achieved or the first DLT observed. Safety assessments include adverse events (AE), laboratory test, ophthalmologic and dermatological assessments, physical examination, vital signs, and ECG. Serial blood samples were collected on Cycle1Day1, Cycle2Day1, and Cycle3Day1 for PK analysis. Tumor responses were assessed every 6 we...