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Rivoceranib (Apatinib)

Rivoceranib Pipeline

Clinical Program

Rivoceranib (Apatinib)

Rivoceranib (Apatinib) is the first successful small-molecule tyrosine kinase inhibitor to be approved in gastric cancer (China, Dec 2014). It is important to note that in the United States and other jurisdictions, Rivoceranib is investigational and safety and efficacy have not been established.  Orphan Drug designation has been granted in the US, Europe and South Korea. It has been clinically tested with over 1,000 patients worldwide. Rivoceranib has also shown potential to improve outcomes in combination treatment with chemotherapeutics and immunotherapy, as well as for maintenance therapy. Additional studies and research will need to be conducted to verify the clinical applications in this context.

For Patients

Rivoceranib is an oral anti-cancer compound being studied for its ability to fight solid cancers including late stage stomach cancer, colorectal cancer, liver cancer, and adenoid cystic carcinoma. Although rivoceranib is already approved and marketed in China, it is not yet approved for patients in the rest of the world. Therefore, safety and efficacy have not been established outside of China. Rivoceranib is being studied outside of China as an investigational drug. If you and your physician decide that a clinical trial may be the right option for you, you may contact the research staff listed in clinicaltrials.gov (search term apatinib or rivoceranib).

Technical Description

Rivoceranib (Apatinib, YN968D1) is an orally bioavailable experimental drug candidate being developed outside of China by Elevar Therapeutics, for the treatment of solid tumors including advanced or metastatic gastric cancer, colorectal cancer, hepatocellular carcinoma, and adenoid cystic carcinoma. YN968D1 was first synthesized and patented by Advenchen Laboratories in Southern California. 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®. Elevar Therapeutics holds the global rights (excluding China) and has partnered for the development and marketing of rivoceranib in South Korea.

Rivoceranib is a potent inhibitor of vascular endothelial growth factor receptor-2 (known as VEGFR2) which mediates the primary pathway for tumor-mediated angiogenesis. It has been clinically tested in over 1,000 patients worldwide. It has also shown potential to improve outcomes in combination with chemotherapeutics and immunotherapy, as well as for maintenance therapy. Additional studies and research will need to be conducted to verify the clinical applications in this context.  It is important to note that in the United States, Rivoceranib is investigational and safety and efficacy have not been established.

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