Drug intelligence / Profile preview

silybin + phosphatidylcholine

Development stage
Phase 2
Lead developer
Indena
Modality
Small Molecules
Administration
Oral
01

Overview

Silybin + phosphatidylcholine is an oral formulation of silybin, the primary active flavonolignan found in milk thistle (*Silybum marianum*), complexed with phosphatidylcholine to enhance its lipophilicity and gastrointestinal absorption. This "phytosome" technology significantly improves the absolute bioavailability of silybin compared to standard silymarin extracts. Silybin exerts hepatoprotective effects through multiple mechanisms, including antioxidant activity (scavenging free radicals), inhibition of lipid peroxidation, and stimulation of ribosomal RNA synthesis to promote liver regeneration. It also acts as an anti-inflammatory agent by inhibiting NF-kappaB. In the context of *Amanita phalloides* poisoning, silybin prevents the uptake of alpha-amanitin into hepatocytes by inhibiting the OATP1B3 transporter. The Fundacion para la Investigacion Biomedica del Hospital Universitario Ramon y Cajal has investigated this complex to compare its oral bioavailability with intravenous silybin (Legalon SIL).

Brand names
Siliphos
Other names
Silybin phytosomeSilibinin-phosphatidylcholine complexSilybin-phosphatidylcholine complex
02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)SLCO2B1 (Organic anion transporting polypeptide 2B1)SLCO1B3 (Organic anion transporting polypeptide 1B3)Pol I (RNA polymerase I)

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