Drug intelligence / Profile preview

Legalon SIL

Development stage
Phase 2
Lead developer
Rotta Research
Modality
Small Molecules
Administration
Intravenous
01

Overview

**Legalon SIL** is an intravenous formulation of silibinin-C-2',3-dihydrogensuccinate disodium salt, a flavonolignan derivative from milk thistle (Silybum marianum) standardized to deliver 350 mg silibinin per vial. It acts primarily by inhibiting OATP1B3-mediated uptake of amatoxins into hepatocytes, blocking enterohepatic recirculation of the toxin, and exhibits antioxidative, anti-inflammatory effects that mitigate TNF-mediated hepatocyte apoptosis in amatoxin-induced hepatic failure from Amanita phalloides poisoning. Administered as a 5 mg/kg loading dose followed by 20 mg/kg/day continuous IV infusion, it is registered in over a dozen European countries and has shown mortality reduction to <10% in nearly 1,500 documented cases compared to >20% with historical treatments; a Phase II trial (NCT00915681) assessed its efficacy in preventing liver transplantation/death.

Brand names
Legalon SILLegalon
Other names
Silibinin-C-2',3-dihydrogensuccinate disodium salt
02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)SLCO1B3 (Organic anion transporting polypeptide 1B3)SLCO2B1 (Organic anion transporting polypeptide 2B1)

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