Drug intelligence / Profile preview

cinobufotalin

Development stage
Unknown
Lead developer
Research institutes/hospitals in China
Modality
Small Molecules
Administration
Intravenous, Intraperitoneal
01

Overview

Cinobufotalin is a bufadienolide compound isolated from the skin secretions of giant toads and has been used in traditional Chinese medicine for its cardiotonic (heart-strengthening), diuretic (promoting urine production), and hemostatic (stopping bleeding) effects. In recent years it has gained attention for its antitumor properties. Preclinical studies show that cinobufotalin induces apoptosis and inhibits proliferation in various cancer cell lines including lung cancer cells and lymphoma cells. It exerts anticancer effects by downregulating vascular endothelial growth factor (VEGF) and epidermal growth factor receptor (EGFR), disrupting DNA structure in tumor cells via increased reactive oxygen species production and mitochondrial dysfunction. Network pharmacology analyses suggest that cinobufotalin targets key signaling molecules such as SRC kinase family members and PI3K/AKT/MAPK pathways involved in cell survival and proliferation[1][4][5][6]. Clinical studies have evaluated injectable formulations of cinobufotalin as an adjuvant to chemotherapy or transcatheter hepatic arterial chemoembolization for hepatocellular carcinoma or gastric cancer[6][10].

Brand names
cinobufotalin
Other names
CINOBUFOTLINCinobufagin metabolite m-2UNII-L0QBZ37386UNII-L-0QBZ37386UNII-L 0QBZ37386CINOBUFOTALIN [MI]CINOBUFOTALIN [WHO-DD]5-beta-Bufa-20,22-dienolide, 14,15-beta-epoxy-3-beta,5,16-beta-trihydroxy-, 16-acetateBufa-20,22-dienolide, 16-(acetyloxy)-14,15-epoxy-3,5-dihydroxy-, (3beta,5beta,15beta,16beta)-
02

Targets

PIK3CA (Phosphoinositide 3-kinase alpha)VEGFR2 (Vascular endothelial growth factor receptor 2)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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