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Ref Type Journal Article
PMID (21443688)
Authors Tian S, Quan H, Xie C, Guo H, Lü F, Xu Y, Li J, Lou L
Title YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo.
Journal Cancer science
Vol 102
Issue 7
Date 2011 Jul
URL
Abstract Text Angiogenesis is an important process in cell development, especially in cancer. Vascular endothelial growth factor (VEGF) signaling is an important regulator of angiogenesis. Several therapies that act against VEGF signal transduction have been developed, including YN968D1, which is a potent inhibitor of the VEGF signaling pathway. This study investigated the antitumor activity of YN968D1 (apatinib mesylate) in vitro and in vivo. YN968D1 potently suppressed the kinase activities of VEGFR-2, c-kit and c-src, and inhibited cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ. YN968D1 effectively inhibited proliferation, migration and tube formation of human umbilical vein endothelial cells induced by FBS, and blocked the budding of rat aortic ring. In vivo, YN968D1 alone and in combination with chemotherapeutic agents effectively inhibited the growth of several established human tumor xenograft models with little toxicity. A phase I study of YN968D1 has shown encouraging antitumor activity and a manageable toxicity profile. These findings suggest that YN968D1 has promise as an antitumor drug and might have clinical benefits.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Rivoceranib Rivoceranib 11 3
Drug Name Trade Name Synonyms Drug Classes Drug Description
Rivoceranib YN968D1|Apatinib KIT Inhibitor 50 RET Inhibitor 39 SRC Inhibitor 29 VEGFR2 Inhibitor 35 Rivoceranib (Apatinib) is an inhibitor of receptor tyrosine kinases, including KDR (VEGFR2), RET, c-KIT, Src, and PDGFRa, which may result in reduced cell proliferation and inhibition of tumor growth (PMID: 21443688, PMID: 32669874).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown lung cancer not applicable Rivoceranib Preclinical - Cell line xenograft Actionable In a preclinical study, Apatinib (YN968D1) inhibited tumor growth in lung cancer cell line xenograft models (PMID: 21443688). 21443688
Unknown unknown stomach cancer not applicable Rivoceranib Preclinical - Cell line xenograft Actionable In a preclinical study, Apatinib (YN968D1) inhibited tumor growth in gastric cancer cell line xenograft models (PMID: 21443688). 21443688
Unknown unknown colon cancer not applicable Rivoceranib Preclinical - Cell line xenograft Actionable In a preclinical study, Apatinib (YN968D1) inhibited tumor growth in colon cancer cell line xenograft models (PMID: 21443688). 21443688