PMID: 9430355Jan 1, 1997Paper

Liver targeting of antiviral nucleoside analogues through the asialoglycoprotein receptor

Journal of Viral Hepatitis
Luigi FiumeG B Gervasi

Abstract

In order to reduce the extrahepatic side-effects of antiviral nucleoside analogues in the treatment of chronic viral hepatitis, these drugs are conjugated with galactosyl-terminating macromolecules. The conjugates selectively enter hepatocytes after interaction of the carrier galactose residues with the asialoglycoprotein receptor present in large amounts and high affinity only on these cells. Within hepatocytes the conjugates are delivered to lysosomes where enzymes split the bond between the carrier and the drug, allowing the latter to become concentrated in the liver. The validity of this chemotherapeutic strategy has been endorsed by a clinical study. Adenine arabinoside monophosphate (ara-AMP), conjugated with lactosaminated human serum albumin (L-HSA) and administered to hepatitis B virus (HBV)-infected patients for 28 days, exerted an antiviral activity to the same extent as the free drug without producing any clinical side-effects, including the severe neurotoxicity caused by the free drug. Preclinical studies are now underway with conjugates obtained using lactosaminated poly-L-lysine (Lac-poly(Lys)) as the hepatotropic carrier. These new conjugates have some advantages over those prepared with L-HSA: they can be admin...Continue Reading

Citations

May 10, 2003·Journal of Controlled Release : Official Journal of the Controlled Release Society·Niren MurthyPatrick S Stayton
Jul 23, 2002·Digestive and Liver Disease : Official Journal of the Italian Society of Gastroenterology and the Italian Association for the Study of the Liver·G Di StefanoL Fiume
Jul 19, 2003·Digestive and Liver Disease : Official Journal of the Italian Society of Gastroenterology and the Italian Association for the Study of the Liver·G Di StefanoL Fiume
Nov 10, 2005·Journal of Drug Targeting·Kapil KhatriSuresh P Vyas
Mar 9, 2012·Drug Development and Industrial Pharmacy·Swati GuptaG P Agrawal
Feb 28, 2015·Journal of Drug Targeting· ParamjotNeeraj Mishra
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Oct 23, 2014·Journal of Pharmaceutical Sciences·Tsutomu IshiharaTohru Mizushima
Feb 24, 2015·Journal of Controlled Release : Official Journal of the Controlled Release Society·Anisha A D'Souza, Padma V Devarajan
Jun 28, 2008·Journal of Controlled Release : Official Journal of the Controlled Release Society·Felix Kratz
Jan 16, 2007·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Giuseppina Di StefanoAlessandro Mattioli
May 10, 2002·The Journal of Pharmacy and Pharmacology·Yoshinori KatoYoshiharu Machida
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Sep 18, 2003·Bioconjugate Chemistry·Michio AbeJanina Baranowska-Kortylewicz

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