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.