Oseltamivir: A First Line Defense Against Swine Flu

Ritesh      Agrawal; Prarthana      V. Rewatkar; Ganesh      R. Kokil; Arunima      Verma; Atin      Kalra

Abstract

Oseltamivir (has known by its brand name Tamiflu) is a prodrug, requiring ester hydrolysis for conversion to the active form, Oseltamivir carboxylate. Oseltamivir was the first orally active neuraminidase inhibitor commercially developed by US based Gilead Sciences and is currently marketed by F. Hoffmann-La Roche (Roche). Oseltamivir is an antiviral drug which works by blocking the function of the viral neuraminidase protein. US FDA approved Oseltamivir for prophylaxis of uncomplicated influenza A and B. Currently, Oseltamivir is the only first line defense drug available for the treatment of Swine Flu. Orally Oseltamivir is well tolerated and effective in treatment of influenza in adolescents and adults, including the elderly and patients with chronic cardiac and/or respiratory disease. Many of the pharmaceutical companies targeted Oseltamivir as a block buster molecule. In present review, we have tried to cover chemistry, mode of binding, total synthesis, current patent status, adverse effect and clinical status of Oseltamivir giving emphasis on medicinal chemistry aspect.

Keywords: Oseltamivir, tamiflu, neuraminidase inhibitors, swine flu, Oseltamivir carboxylate, active neuraminidase inhibitor, influenza, Influenza A virus subtype H5N1, zanamivir (Relenza), avian flu Pandemic, Peramivir, Oseltamivir phosphate, C16H28N2O4, hemagglutinin, cellular-receptor sialic acid, Glu276 residue, His274Tyr, Patent No. 5,763,483, Patent No. 5,866,601, Patent No. 5,952,375, butadiene, acrylic acid, Prophylaxis of influenza, hepatic esterases, sore throat, live attenuated influ-enza vaccine, P450, glucuronyl transferases, Acetaminophen, Cimetidine, Antacids, aluminum hydroxides, calcium carbonates, Antivirals, Amantadine, Rimantadine