Laninamivir Prodrug CS-8958, a Long-Acting Neuraminidase Inhibitor, Shows Superior Anti-Influenza Virus Activity after a Single Administration▿
Identifieur interne : 000E55 ( Main/Exploration ); précédent : 000E54; suivant : 000E56Laninamivir Prodrug CS-8958, a Long-Acting Neuraminidase Inhibitor, Shows Superior Anti-Influenza Virus Activity after a Single Administration▿
Auteurs : Shuku Kubo [Japon] ; Takanori Tomozawa [Japon] ; Masayo Kakuta [Japon] ; Akane Tokumitsu [Japon] ; Makoto Yamashita [Japon]Source :
- Antimicrobial Agents and Chemotherapy [ 0066-4804 ] ; 2010.
Abstract
Two neuraminidase (NA) inhibitors, zanamivir (Relenza) and oseltamivir phosphate (Tamiflu), have been licensed for use for the treatment and prophylaxis of influenza. We have reported on laninamivir (code name, R-125489), a novel neuraminidase inhibitor, and have discovered that the laninamivir prodrug CS-8958 worked as a long-acting neuraminidase inhibitor in a mouse influenza virus infection model when it is intranasally administered. In this study, CS-8958 was administered just once 7 days before infection and showed significant efficacy
Url:
DOI: 10.1128/AAC.01311-09
PubMed: 20047917
PubMed Central: 2825999
Affiliations:
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Le document en format XML
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<front><div type="abstract" xml:lang="en"><p>Two neuraminidase (NA) inhibitors, zanamivir (Relenza) and oseltamivir phosphate (Tamiflu), have been licensed for use for the treatment and prophylaxis of influenza. We have reported on laninamivir (code name, R-125489), a novel neuraminidase inhibitor, and have discovered that the laninamivir prodrug CS-8958 worked as a long-acting neuraminidase inhibitor in a mouse influenza virus infection model when it is intranasally administered. In this study, CS-8958 was administered just once 7 days before infection and showed significant efficacy <italic>in vivo</italic>
. The efficacy of a single administration of CS-8958 after viral infection was then compared with that of repeated administrations of oseltamivir phosphate or zanamivir in mice and ferrets. CS-8958 showed efficacy superior or similar to the efficacies of the two licensed NA inhibitors. CS-8958 also significantly reduced the titers of an oseltamivir-resistant H1N1 virus with a neuraminidase H274Y substitution in a mouse infection model. These results suggest that since CS-8958 is characteristically long lasting in the lungs, it may be ideal for the prophylaxis and treatment of influenza.</p>
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<name sortKey="Yamashita, Makoto" sort="Yamashita, Makoto" uniqKey="Yamashita M" first="Makoto" last="Yamashita">Makoto Yamashita</name>
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