Background: This single-arm phase 1 study was conducted to define the PK of REG and its metabolites, M-2 and M-5, in Chinese patients with advanced solid tumors. Methods: Patients from China mainland with locally advanced/metastatic, refractory solid tumors were enrolled if they were not candidates for standard therapy or if they had metastatic CRC or advanced GIST and REG was a treatment option. The primary objective was PK; secondary objectives were safety, tolerability, and efficacy.