Drug intelligence / Profile preview

cinobufagin

Development stage
Preclinical
Modality
Small Molecules
Administration
Unknown
01

Overview

Cinobufagin is a **bufanolide steroid** and the major active ingredient derived from the venom of the Asiatic toad (Bufo gargarizans). It acts primarily as a **Na+/K+-ATPase inhibitor**, similar in activity to cardiac glycosides such as ouabain, and displays cardiotoxic as well as pharmacological effects. Cinobufagin has demonstrated **antineoplastic** activity in various preclinical cancer models, particularly for glioblastoma, lung cancer, colorectal cancer, and liver cancer, often by blocking **epidermal growth factor receptor (EGFR)** signaling and its downstream pathways (e.g., STAT3, Akt), leading to cell cycle arrest and **apoptosis**. Other reported actions include inhibition of steroidogenesis (by affecting StAR protein transcription), immunomodulation (altering cytokine secretion and stimulating T cell/macrophage proliferation), and analgesic effects (via up-regulation of mu opioid receptor and β-endorphin synthesis). Cinobufagin may also induce endoplasmic reticulum stress and caspase-mediated cell death in cancer cells[1][3][4][5][7][10].

Other names
cinobufagincinobufagine16-beta)-betcinobufagin-RMcinobufagin std.cinobufagin (6CI)FEMA 2288FEMA2288FEMA-2288T9PSN4R8IRT-9PSN4R8IRT 9PSN4R8IRCino-bufaginAKOS 233-01AKOS233-01AKOS-233-01AKOS B004228
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)CDK2 (Cyclin-dependent kinase 2)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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