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Apatinib, sold as rivoceranib outside China, was the first pill of its kind approved for stomach cancer and is now the partner of camrelizumab in first-line liver cancer.
Hengrui's apatinib was approved by the CFDA in October 2014 for advanced gastric or gastro-oesophageal junction adenocarcinoma after two or more lines, the first oral VEGFR2 inhibitor approved for gastric cancer anywhere, and in December 2020 for hepatocellular carcinoma after prior systemic therapy. Combined with camrelizumab it beat sorafenib in first-line HCC (CARES-310, Lancet 2023) and was approved in China in January 2023; the same combination has drawn three complete response letters from the FDA over manufacturing inspections and trial conduct rather than efficacy. Elevar Therapeutics (HLB) holds ex-China rights.
Selective ATP-competitive inhibitor of VEGFR2 (KDR) with weaker activity on RET, KIT and SRC; blocks tumour angiogenesis. Connects to VEGF / VEGFR.
1.Rivoceranib (apatinib) slips into a pocket on VEGF / VEGFR.
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| Region | Year | Indication |
|---|---|---|
| China | 2014 | Advanced gastric or gastro-oesophageal junction adenocarcinoma after two or more lines |
| China | 2020 | Advanced hepatocellular carcinoma after prior systemic therapy |
| China | 2023 | First-line unresectable hepatocellular carcinoma with camrelizumab (CARES-310) |
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Query for this drug: (TITLE:"Rivoceranib" OR ABSTRACT:"Rivoceranib" OR TITLE:"apatinib" OR ABSTRACT:"apatinib" OR TITLE:"Aitan" OR ABSTRACT:"Aitan" OR TITLE:"YN968D1" OR ABSTRACT:"YN968D1" OR TITLE:"Apatinib" OR ABSTRACT:"Apatinib") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Rivoceranib (apatinib), not a curated reading list.
Shares Shukui Qin, Hepatocellular carcinoma (KEGG map), VEGF angiogenesis, VEGF / VEGFR and the tag china.
Shares Shukui Qin, Hepatocellular carcinoma, Small-molecule kinase inhibitors and the tag china.
Shares Camrelizumab, Jiangsu Hengrui Pharmaceuticals and the tag china.
Shares VEGF angiogenesis, VEGF / VEGFR, Anti-angiogenic therapy, Small-molecule kinase inhibitors and the tag china.
Shares Anti-angiogenic therapy, Small-molecule kinase inhibitors and the tag china.
Shares Anti-angiogenic therapy, Hepatocellular carcinoma and the tag china.
Shares Hepatocellular carcinoma, Gastric & gastro-oesophageal junction cancer and the tag china.
Shares Jiangsu Hengrui Pharmaceuticals, Small-molecule kinase inhibitors and the tag china.