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resibufogenin
- Development stage
- Preclinical
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral, Intraperitoneal
01
Overview
**Resibufogenin** is a bioactive bufadienolide steroid extracted primarily from the venom glands of certain toads of the Bufonidae family and is a main glycoside constituent in the traditional Chinese medicine Chan Su[1][7]. It exhibits **cardiotonic** properties similar to cardiac glycosides like digoxin by inhibiting the Na^+/K^+-ATPase[10]. Its mechanisms encompass induction of cell cycle arrest, apoptosis, and inhibition of cell proliferation and migration, including via proteasomal degradation of cyclin D1 and modulation of ATP1A1 signaling cascade[6][9]. Resibufogenin has demonstrated anticancer, anti-inflammatory, antiviral, vasopressor, and respiratory-therapeutic effects, and antiangiogenic activity through inhibition of VEGFR2 phosphorylation and downstream signaling[1][4]. Therapeutic areas include oncology (notably for multiple myeloma, triple-negative breast cancer, pancreatic and colorectal cancer), cardiovascular diseases (heart failure, hypertension), and respiratory disorders[1][3][4][7].
- Brand names
- Respigon
- Other names
- bufogeninbufogeninaResibufoginResibufogenin USP/EP/BPResibufogenin-RMResibufogenin 95%Resibufogenin 97%
02
Targets
ATP1A1 (Sodium/potassium-transporting ATPase subunit alpha-1)GSK3 (Glycogen synthase kinase 3 beta)IKK complexPRKCI (Protein kinase C iota)TAK1 (Transforming growth factor beta–activated kinase 1)VEGFR2 (Vascular endothelial growth factor receptor 2)NaV (Voltage-gated sodium channels)
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