Rivoceranib

Rivoceranib

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^®.

Elevar Therapeutics conducts clinical trials for others in the field of cancer therapeutics, distributed primarily in promotion of cancer treatments to healthcare professionals.

Rivoceranib Pipeline

Technical Description

Rivoceranib is an orally bioavailable experimental drug candidate being developed by Elevar Therapeutics for the treatment of solid tumors including advanced or metastatic gastric cancer, colorectal cancer, hepatocellular carcinoma, and adenoid cystic carcinoma. Rivoceranib is a potent inhibitor of vascular endothelial growth factor receptor-2 (known as VEGFR2) which mediates the primary pathway for tumor-mediated angiogenesis.

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. Rivoceranib is being studied outside of China as an investigational drug. Although rivoceranib is already approved and marketed in China, it is not yet approved for patients in the rest of the world. It is important to note that in the United States and other jurisdictions outside of China, rivoceranib safety and efficacy have not been established. 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), or if treating physicians believe expanded access may be the only option for their patients, they may contact Elevar’s Expanded Access Program at 1-801-303-7440 x300.

Publications and Posters

• Updated Phase I study to evaluate the safety and efficacy of rivoceranib (apatinib) and nivolumab in patients with unresectable or metastatic cancer. Connective Tissue Oncology Society (CTOS) Annual Meeting (2020).
• A phase 2 open-label, multicenter study to evaluate efficacy and safety of rivoceranib in recurrent or metastatic adenoid cystic carcinoma. ASCO Annual Meeting (2020).
• Randomized phase 3 ANGEL study of rivoceranib (apatinib) + best supportive care (BSC) vs placebo + BSC in patients with advanced/metastatic gastric cancer who failed ≥2 prior chemotherapy regimens, ESMO Annual Meeting (2019).
• Phase I study to evaluate the safety and efficacy of rivoceranib (apatinib) and nivolumab in patients with unresectable or metastatic cancer. ASCO-SITC Clinical Immuno-Oncology Symposium (2019).
• Synergistic tumor-suppressive effect of apatinib, a selective VEGFR-2 inhibitor, in combination with immunotherapy in a syngeneic murine lung cancer model. American Association for Cancer Research (AACR) Annual Meeting (2018).
• A Phase I study evaluating the pharmacokinetics of rivoceranib (apatinib) in healthy Caucasian, Japanese, and Chinese subjects. American College of Clinical Pharmacology (2017).
• A prospective, randomized, double-blinded, placebo-controlled, phase III study to evaluate the efficacy and safety of apatinib plus best supportive care (BSC) compared to placebo plus BSC in patients with advanced or metastatic gastric cancer: The ANGEL study – ASCO Annual Meeting (2017).