Introduction
cancer
CANCER, SOLID TUMORS, METASTATIC BREAST CANCER
Fruquintinib (HMPL-013) is a highly selective, potent, oral, small-molecule tyrosine kinase inhibitor of vascular endothelial growth factor receptors (VEGFR) -1, -2, and -3 [The phase 3, multicenter, randomized, double-blind, placebo-controlled FRESCO study conducted in China demonstrated that fruquintinib significantly improved overall survival (OS) in patients with mCRC in a third-line or later setting compared to placebo. The median OS was 9.30 vs. 6.57 months (hazard ratio [HR] = 0.65, p < 0.001), and median progression-free survival (PFS) was 3.71 vs. 1.84 months (HR = 0.26, p < 0.001) [The primary objective of the dose escalation phase of this phase 1/1b study was to evaluate the safety and tolerability of fruquintinib at 2 dose levels, 3 and 5 mg, orally (PO) QD, 3/1, and to confirm the RP2D in United States (U.S.) patients with advanced solid tumors. Secondary objectives were to evaluate the pharmacokinetics (PK) and preliminary anticancer activity of fruquintinib. In the dose expansion phase of this study, the primary objective was to assess fruquintinib anticancer activity at the RP2D. Here we report the dose escalation phase of the study, including the 3 and 5 mg dose cohorts, and the dose expansion cohort in patients with solid tumors of any type treated with the confirmed 5 mg dose of fruquintinib (Cohort A). The other 5 mg dose cohorts in the dose expansion phase included specific cancer types such as refractory mCRC and metastatic breast cancer and will be reported separately.