Rivoceranib is the first small-molecule tyrosine kinase inhibitor to be approved in gastric cancer under the name Apatinib in China (December 2014). Rivoceranib is a highly potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2), the primary pathway for tumor angiogenesis. VEGFR-2 inhibition is a clinically validated approach to limit tumor growth and disease progression. Rivoceranib has been studied in over 1,000 patients worldwide and was well tolerated in clinical trials with a comparable safety profile to other TKIs. Rivoceranib is currently being studied as a monotherapy and in combination with chemotherapy and immunotherapy.
Clinical studies are underway in multiple tumor types including, gastric cancer, hepatocellular carcinoma (combo w/camrelizumab), adenoid cystic carcinoma, and colorectal cancer (combo w/Lonsurf®). Orphan drug designations for rivoceranib have been granted in gastric cancer (U.S., EU, and South Korea) in adenoid cystic carcinoma (U.S.), and hepatocellular carcinoma (U.S.). Elevar Therapeutics holds the global rights (excluding China) and has partnered for the development and marketing of rivoceranib with HLB-LS in South Korea. Apatinib is currently marketed in China for advanced gastric cancer by the Chinese-territory license-holder, Jiangsu Hengrui Medicine Co., Ltd under the brand name Aitan®.