Drug intelligence / Profile preview

silibinin

Development stage
Phase 4
Lead developer
MADAUS
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Silibinin is a flavonolignan and the principal active constituent of silymarin, an extract from the seeds of milk thistle (Silybum marianum). It is a mixture of two diastereomers, silybin A and silybin B, in approximately equal amounts. Silibinin exhibits hepatoprotective effects by stabilizing hepatocyte membranes, providing antioxidant activity, reducing fibrosis and inflammation, and inhibiting toxin entry into liver cells. It has been used clinically for toxic liver damage (including mushroom poisoning), as adjunct therapy in chronic hepatitis and cirrhosis, alcoholic liver disease (ALD), metabolic liver disease, viral hepatitis (B/C), and as an investigational agent in certain cancers such as prostate cancer. The water-soluble salt form—silibinin-C-2',3-dihydrogensuccinate disodium—is used intravenously for Amanita mushroom poisoning. Mechanistically, it acts through antioxidation, anti-inflammatory pathways (such as NF-kappaB inhibition), antifibrotic effects, modulation of lipid metabolism genes/pathways in the liver, inhibition of mitogenic/survival signaling including insulin-like growth factor receptor type 1 and epidermal growth factor receptor pathways[1][2][5][7].

Brand names
LegalonSiliphosSilybin-phytosome
Other names
silibininasilibininesilibininumsilymarin I
02

Targets

IGF-1R (Insulin-like growth factor 1 receptor)SLCO2B1 (Organic anion transporting polypeptide 2B1)OATP1B1 (Organic anion transporting polypeptide 1B1)EGFR (Epidermal growth factor receptor)SLCO1B3 (Organic anion transporting polypeptide 1B3)

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