Phase I/II Study of TSU-68 for Advanced Hepatocellular Carcinoma
As HCC is a highly vascular tumor, a number of antiangiogenic agents have been tested for
the treatment of HCC. Orantinib is an orally administered, small-molecule, multiple receptor
tyrosine kinase inhibitor that targets vascular endothelial growth factor receptor-2
(VEGFR-2), platelet-derived growth factor receptor (PDGFR), and fibroblast growth factor
receptor (FGFR). Phase I studies that have been conducted in Japan for patients with solid
tumors recommended a dosage of 400 mg bid. As a potent antiangiogenic agent, Orantinib is
also expected to be effective against HCC. However, because most HCC patients have
accompanying liver cirrhosis or hepatitis, its safety must be reevaluated in the presence of
liver function impairment.
Allocation: Non-Randomized, Endpoint Classification: Safety/Efficacy Study, Intervention Model: Single Group Assignment, Masking: Open Label, Primary Purpose: Treatment
Step 1(Phase I) Safety
Masao Omata, M.D.
Yamanashi Prefectural Central Hospital
Japan: Ministry of Health, Labor and Welfare