Article
Pharmacology & Pharmacy
Andrei A. Ivashchenko, Jeremy C. Jones, Dmitry O. Shkil, Yan A. Ivanenkov, Philippe Noriel Q. Pascua, Melissa K. Penaflor, Ruben N. Karapetian, Elena A. Govorkova, Alexandre V. Ivachtchenko
Summary: In this study, the efficacy of a new orally-dosed neuraminidase inhibitor (NAI) AV5080 against different subtypes of influenza viruses was examined. AV5080 showed superior in vitro efficacy compared to currently approved NAIs, oseltamivir and zanamivir. However, it exhibited reduced inhibition against certain viral variants, such as NA-E119G and NA-R292K. These findings suggest that AV5080 is a promising orally-dosed NAI.
ANTIVIRAL RESEARCH
(2023)
Article
Medicine, General & Internal
Sofia Tejada, Miia Jansson, Candela Sole-Lleonart, Jordi Rello
Summary: Neuraminidase inhibitors (NAIs) therapy significantly reduced the time to clinical resolution, total influenza-related complications, acute otitis media and need for antibiotic treatment. While reductions in mortality, pneumonia, asthma exacerbations, and hospitalization rates only demonstrated a trend benefit with NAIs treatment. The most significant adverse event associated with NAIs was an increase in nausea and vomiting.
EUROPEAN JOURNAL OF INTERNAL MEDICINE
(2021)
Article
Public, Environmental & Occupational Health
Thiago das Chagas Sousa, Jessica Santa Cruz Carvalho Martins, Milene Dias Miranda, Cristiana Couto Garcia, Paola Cristina Resende, Cliomar A. A. Santos, Maria do Carmo Debur, Rodrigo Ribeiro Rodrigues, Andrea Cony Cavalcanti, Tatiana Schaffer Gregianini, Felipe Campos de Melo Iani, Felicidade Mota Pereira, Sandra Bianchini Fernandes, Jessylene de Almeida Ferreira, Katia Correa de Oliveira Santos, Fernando Motta, David Brown, Walquiria Aparecida Ferreira de Almeida, Marilda Mendonca Siqueira, Aline da Rocha Matos
Summary: This study evaluated the antiviral resistance of Brazilian influenza A virus strains and found a low prevalence of resistance markers, indicating that antiviral drugs are still effective. However, there is a need for strengthened surveillance of influenza resistance.
FRONTIERS IN PUBLIC HEALTH
(2022)
Article
Chemistry, Medicinal
Ruifang Jia, Jian Zhang, Chiara Bertagnin, Srinivasulu Cherukupalli, Wei Ai, Xiao Ding, Zhuo Li, Jiwei Zhang, Han Ju, Xiuli Ma, Arianna Loregian, Bing Huang, Peng Zhan, Xinyong Liu
Summary: The structural modifications at the 150-cavity of influenza virus neuraminidases can result in more potent oseltamivir derivatives, with compound 5c showing the most promising activity. In vitro and in vivo studies demonstrated low cytotoxicity and no acute toxicity of 5c, indicating its potential as a drug candidate.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Medicine, General & Internal
Jen-Wei Liu, Shen-Hua Lin, Lin-Chien Wang, Hsiao-Yean Chiu, Jen-Ai Lee
Summary: This study compared the efficacy and safety of neuraminidase inhibitors and the endonuclease inhibitor for the treatment of seasonal influenza among healthy adults and children. The results showed that zanamivir was associated with the shortest time to alleviation of influenza symptoms, while baloxavir was associated with reduced rate of influenza-related complications.
Article
Immunology
Takuji Komeda, Takahiro Takazono, Naoki Hosogaya, Eriko Ogura, Masakazu Fujiwara, Hideyuki Miyauchi, Yoshikazu Ajisawa, Shinpei Iwata, Hideaki Watanabe, Keiichi Honda, Yoshitake Kitanishi, Kanae Hara, Hiroshi Mukae
Summary: The study found that baloxavir may help reduce household transmission of influenza compared to oseltamivir. However, no similar reduction was shown in comparison to inhalant medications, which may be due to unmeasured confounding factors related to differences in administration route.
CLINICAL INFECTIOUS DISEASES
(2021)
Article
Microbiology
Chiara Medaglia, Arnaud Charles-Antoine Zwygart, Paulo Jacob Silva, Samuel Constant, Song Huang, Francesco Stellacci, Caroline Tapparel
Summary: Influenza viruses have high genetic variability and can quickly develop resistance mutations. Combination therapy with two drugs can reduce the risk of resistance emergence. Combining interferon lambda with oseltamivir can delay the emergence of drug-resistant influenza virus variants.
Article
Pharmacology & Pharmacy
Sofia Tejada, Alexandre M. Tejo, Yolanda Pena-Lopez, Carlos G. Forero, Xavier Corbella, Jordi Rello
Summary: The study found that baloxavir and neuraminidase inhibitors (NAIs) have a significant reduction effect on complications of uncomplicated influenza, especially in reducing antibiotic prescriptions. Single-dose baloxavir is non-inferior to NAIs in terms of safety and efficacy.
EXPERT REVIEW OF CLINICAL PHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Jiwei Zhang, Chuanfeng Liu, Ruifang Jia, Xujie Zhang, Jian Zhang, Chiara Bertagnin, Anna Bonomini, Laura Guizzo, Yuanmin Jiang, Huinan Jia, Shuzhen Jia, Xiuli Ma, Arianna Loregian, Bing Huang, Peng Zhan, Xinyong Liu
Summary: Introducing structurally diverse benzyl side chains at the C5-NH2 position of oseltamivir improves its binding affinity with neuraminidase and anti-influenza activity. We designed and synthesized novel oseltamivir derivatives with different N-heterocycle substituents that induce opening of the 150-loop of group-2 neuraminidases. Compound 6k showed broad-spectrum activity against wild-type neuraminidases and enhanced activity against H3N2 compared to oseltamivir carboxylate and zanamivir.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Review
Chemistry, Medicinal
Kuanglei Wang, Huicong Zhang, Yongshou Tian
Summary: This review covers influenza drugs, mutation types of neuraminidase, molecular mechanisms of drug resistance, strategies to enhance drug susceptibility, and alternative therapies.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Ruifang Jia, Jiwei Zhang, Fangyuan Shi, Anna Bonomini, Camilla Lucca, Chiara Bertagnin, Jian Zhang, Chuanfeng Liu, Huinan Jia, Yuanmin Jiang, Xiuli Ma, Arianna Loregian, Bing Huang, Peng Zhan, Xinyong Liu
Summary: Two series of oseltamivir derivatives were designed, synthesized, and evaluated for their ability to inhibit neuraminidase. Compound 43b showed weaker or slightly improved inhibitory activity against wild-type neuraminidases compared to oseltamivir carboxylate. However, it displayed significantly more potent activity against mutant neuraminidases and exhibited equivalent or more potent antiviral activities in cellular assays. Additionally, 43b possessed improved physicochemical properties and ADMET properties compared to oseltamivir carboxylate. Therefore, it is considered a promising lead compound for further investigation.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Infectious Diseases
Naoki Tani, Naoki Kawai, Yong Chong, Takuma Bando, Norio Iwaki, Seizaburo Kashiwagi, Hideyuki Ikematsu
Summary: This study investigated the susceptibility of epidemic influenza viruses to neuraminidase inhibitors and the emergence of resistant viruses after treatment. The results suggest the continued effectiveness of these inhibitors for epidemic influenza in Japan. Treatment-emergent resistant viruses were detected after oseltamivir treatment.
JOURNAL OF INFECTION
(2022)
Article
Environmental Sciences
Magdalena Swierczynska, Dagmara M. Mirowska-Guzel, Edyta Pindelska
Summary: This article presents the possibilities of using all available antiviral drugs specific for influenza A and B, and compares the currently recommended anti-influenza medications. It highlights the promising new drug baloxavir marboxil, and suggests further research on combination therapy.
INTERNATIONAL JOURNAL OF ENVIRONMENTAL RESEARCH AND PUBLIC HEALTH
(2022)
Article
Chemistry, Medicinal
Hongqian Zhao, Siyuan Jiang, Zhifan Ye, Hongxi Zhu, Baichun Hu, Peipei Meng, Yanmei Hu, Huicong Zhang, Kuanglei Wang, Jun Wang, Yongshou Tian
Summary: The study designed a series of oseltamivir derivatives bearing hydrazide fragment, successfully targeting the 150 cavity, showing potent activity and satisfactory metabolic stability. This provides an important reference for potent inhibition against the H274Y mutant of NAs.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Immunology
Chia-Ping Su, K. Arnold Chan, Ching-Tai Huang, Chi-Tai Fang
Summary: The study shows that inhaled zanamivir is as effective as oral oseltamivir in preventing influenza-related hospitalization or death for outpatients.
CLINICAL INFECTIOUS DISEASES
(2022)