RWJ-270201 (BCX-1812): a novel neuraminidase inhibitor for influenza

Author:

Young Diane1,Fowler Cynthia1,Bush Karen1

Affiliation:

1. The R.W. Johnson Pharmaceutical Research Institute, Route 202, PO Box 300, Raritan, NJ 08869, USA

Abstract

The influenza virus neuraminidase (NA) is important in the pathogenesis of infection and, thus, is an attractive target for agents used in the treatment and prophylaxis of influenza. This article describes preclinical and early clinical data related to RWJ–270201 (BCX–1812), a novel, orally active NA inhibitor that was rationally designed for having potent and selective activity against influenza A and B viruses. RWJ–270201 is a unique NA inhibitor with a cyclopentane ring structure and high selectivity for the influenza NA. RWJ–270201 has efficacy comparable to or better than earlier NA inhibitors against a wide range of influenza A and B isolates, including recently emerged and avian strains, both in vitro and in a lethal murine model of influenza. Based on the high selectivity and efficacy of RWJ–270201 against both type A and B influenza strains in preclinical studies as well as murine pharmacodynamic studies supporting the potential for once–daily administration, clinical trials were initiated in order to determine the tolerability and antiviral activity of RWJ–270201 in humans. To date, clinical studies have indicated that RWJ–270201 is well tolerated and has antiviral activity in human experimental influenza models when administered orally once daily.

Publisher

The Royal Society

Subject

General Agricultural and Biological Sciences,General Biochemistry, Genetics and Molecular Biology

Reference43 articles.

1. BCX-1812 (RWJ-270201):  Discovery of a Novel, Highly Potent, Orally Active, and Selective Influenza Neuraminidase Inhibitor through Structure-Based Drug Design

2. Generation and characterization of a mutant of in£uenza A virus selected with the neuraminidase inhibitor WJ-270201;Bantia S.;Antiviral Res.,2000

3. Bantia S. (and 13 others) 2001 Comparison of the anti-in£uenza virus activity of WJ-270201 with those of oseltamivir and zanamivir. Antimicrob. Agents Chemother. 45 1162^1167.

4. Boivin G. & Goyette N. 2000 Susceptibility of in£uenza A (H3N2) A (H1N1) and B viruses to the neuraminidase inhibitor WJ-270201 during the 1999^2000 £u season in Canada. In Third Int. Symp. on the Respiratory Viral Infections.

5. Three-dimensional Structure of Influenza A N9 Neuraminidase and Its Complex with the Inhibitor 2-Deoxy 2,3-Dehydro-N-Acetyl Neuraminic Acid

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