Celgosivir

INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
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Legal status	Investigational
CAS Number
PubChem	60734
DrugBank
ChemSpider	54737
KEGG

Celgosivir, in development by Migenix for the treatment of hepatitis C virus (HCV) infection, is an oral prodrug of the natural product castanospermine that inhibits alpha-glucosidase I, an enzyme that plays a critical role in viral maturation by initiating the processing of the N-linked oligosaccharides of viral envelope glycoproteins. Celgosivir is well absorbed in vitro and in vivo, and is rapidly converted to castanospermine. Celgosivir has a novel mechanism of action (preventing the glycosylation of viral proteins by the host), and demonstrates broad antiviral activity in vitro.<ref name=Durantel>,

 Celgosivir, an alpha-glucosidase I inhibitor for the potential treatment of HCV infection, 
 Current Opinion in Investigational Drugs, 
 2009,
 Vol. 10(Issue: 8),
 pp. 860–70,
 
 PMID: 19649930,</ref>

Clinical trials

Celgosivir is not efficient as a monotherapy for the treatment of HCV, but has demonstrated a synergistic effect in combination with pegylated interferon alfa-2b plus ribavirin, both in vitro and in phase II clinical trials that last up to 1 year in patients with chronic HCV infection. Celgosivir may prove to be a valuable component for combination therapy and may help to prevent the apparition of drug resistance. Long-term toxicity studies are necessary to confirm the safety of celgosivir in humans.<ref name=Durantel/>

Although generally safe and well tolerated, celgosivir does not seem to reduce viral load or fever burden in patients with dengue fever.<ref>,

 Efficacy and safety of celgosivir in patients with dengue fever (CELADEN): A phase 1b, randomised, double-blind, placebo-controlled, proof-of-concept trial, 
 The Lancet Infectious Diseases, 
 2014,
 Vol. 14(Issue: 8),
 pp. 706,
 DOI: 10.1016/S1473-3099(14)70730-3,
 PMID: 24877997,</ref>

External links

• KEGG DRUG: Celgosivir Hydrochloride

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