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

CDK2 (Cyclin-dependent kinase 2)EGFR (Epidermal growth factor receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)GSK3 (Glycogen synthase kinase 3 beta)MOR (Mu opioid receptor)NF-κBSTAT3 (Signal Transducer and Activator of Transcription 3)ATP1A (Sodium/potassium-transporting ATPase)STAR (Steroidogenic acute regulatory protein)

Beyond the preview

Go deeper on cinobufagin.

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Clinical trials

Follow clinical development from study design and recruitment through results.

  • Trial phase
  • Status
  • Readouts

Indications & development

Explore development by indication, patient population, and geography.

  • Indications
  • Development status
  • Countries

Licensing & deals

Trace asset ownership, licensing agreements, and commercial partnerships.

  • Partners
  • Deal terms
  • Milestones

Patents & exclusivity

Explore the patent landscape and regulatory exclusivity around an asset.

  • Patents
  • Expiration dates
  • Exclusivity

Competitive landscape

Compare development programs by target, modality, and indication.

  • Competing assets
  • Targets
  • Development stage

Research & analysis

Connect source evidence and development news to your research questions.

  • Publications
  • News
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on cinobufagin.

Gosset Free

Get started with Gosset.

Enter your corporate email.

Work email preferred.

Book a call