Journal of Microbiology

Journal Article

Comparison of anti-influenza virus activity and pharmacokinetics of oseltamivir free base and oseltamivir phosphate: Jin Soo Shin , Keun Bon Ku , Yejin Jang , Yi-Seul Yoon , Daeho Shin , Oh Seung Kwon , Yun Young Go , Seong Soon Kim , Myoung Ae Bae , Meehyein Kim; J. Microbiol. 2017;55(12):979-983. Published online December 7, 2017; DOI: https://doi.org/10.1007/s12275-017-7371-x

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Abstract: Influenza viruses are major human respiratory pathogens that cause high morbidity and mortality worldwide. Currently, prophylactic vaccines and therapeutic antiviral agents are used to prevent and control influenza virus infection. Oseltamivir free base (OSV-FB), a modified generic antiviral drug of Tamiflu (oseltamivir phosphate, OSV-P), was launched in the Republic of Korea last year. Here, we examine the bioequivalence of these two compounds by assessing their antiviral efficacy in infected cells and in a mouse model. It was observed that both antivirals showed comparable efficacy against 11 different influenza A and B viruses in vitro. Moreover, in mice infected with influenza A virus (mouse-adapted A/Puerto Rico/8/34), they showed a dose-dependent therapeutic activity and alleviated infection-mediated reductions in body weight, leading to significantly better survival. There was histopathological disappearance of virus-induced inflammatory cell infiltration of the lung after oral treatment with either antiviral agent (at 10 mg/kg). Pharmacokinetic analysis also exhibited similar plasma concentrations of the active drug, oseltamivir carboxylate, metabolised from both OSVB and OSV-P. This is the first report showing bioequivalence of OSV-FB to its phosphate salt form in the mouse system. The free base drug has some beneficial points including simple drug formulation process and reduced risk of undesirable cation-phosphate precipitation within solution. The long term stability of OSV-FB requires further monitoring when it is provided as a national stock in readiness for an influenza pandemic.

Research Support, Non-U.S. Gov't

NOTE] Susceptibility of Human H3N2 Influenza Virus to Oseltamivir in South Korea, 2009–2011: Sehee Park , Jin Il Kim , Ilseob Lee , Sangmoo Lee , Min-Woong Hwang , Joon-Yong Bae , Jun Heo , Eun-Joo Lim , Won-Seok Seok , Hee Jin Cheong , Joon Young Song , Woo Joo Kim , Man-Seong Park; J. Microbiol. 2012;50(6):1067-1070. Published online December 30, 2012; DOI: https://doi.org/10.1007/s12275-012-2541-3

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Abstract: During the 2009–2011 influenza seasons, 10.26% of the specimens isolated from patients in South Korea were subtyped as H3N2 viruses. Some oseltamivir-sensitive H3N2 samples exhibited different plaque morphologies, and were found to have novel mutations in the neuraminidase gene. In a subsequent analysis using NA mutant viruses, viral compensation against oseltamivir treatment was observed only in the N2 mutant virus. All things considered, these novel mutations may account for the exclusive characteristics of selected H3N2 viruses observed in plaque reduction assays.

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