Article
Chemistry, Medicinal
Francois Dufrasne
Summary: Baloxavir marboxil is a new drug developed in Japan that treats seasonal flu and has been marketed in multiple countries. It is effective against both influenza A and B viruses, although the B strain is more resistant. The drug is currently undergoing post-marketing surveillance and may be used for treating COVID-19.
Article
Immunology
Masatoki Sato, Emi Takashita, Masahiko Katayose, Kenji Nemoto, Nobuko Sakai, Seiichiro Fujisaki, Koichi Hashimoto, Mitsuaki Hosoya
Summary: This study aimed to detect influenza variants with reduced susceptibility to baloxavir marboxil and oseltamivir, and to determine differences in clinical course in children with and without these variants post-antiviral treatment. The results showed that while the emergence of baloxavir-resistant variants may affect the clinical course of patients, oseltamivir-resistant variants had no clinical impact.
JOURNAL OF INFECTIOUS DISEASES
(2021)
Article
Microbiology
Guichan Liao, Muye Xia, Yuanhui Jiang, Hongjie Chen, Wei Liao, Jie Peng, Shaohang Cai
Summary: In this study, baloxavir demonstrated comparable clinical benefits to oseltamivir, establishing its efficacy as an effective antiviral therapy for Chinese patients with influenza. There were no significant differences between the two groups in terms of duration of fever and symptoms, positive rate of viral antigen, and improvements in health-related quality of life.
FRONTIERS IN MICROBIOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Brendan Todd, Egor P. Tchesnokov, Matthias Gotte
Summary: Baloxavir marboxil is an FDA-approved antiviral prodrug for influenza treatment, with its active form baloxavir acid showing high potency in inhibiting the nuclease activity of the influenza virus. Research reveals that BXA acts as a tight binding inhibitor and the I38T mutation reduces this property.
JOURNAL OF BIOLOGICAL CHEMISTRY
(2021)
Article
Immunology
Takuji Komeda, Takahiro Takazono, Naoki Hosogaya, Taiga Miyazaki, Eriko Ogura, Shinpei Iwata, Hideyuki Miyauchi, Keiichi Honda, Masakazu Fujiwara, Yoshikazu Ajisawa, Hideaki Watanabe, Yoshitake Kitanishi, Kanae Hara, Hiroshi Mukae
Summary: This study compared the incidence of hospitalization in patients treated with baloxavir versus oseltamivir and zanamivir for influenza. The results suggest that baloxavir treatment may be more effective in reducing hospitalization rates compared to the other two drugs.
CLINICAL INFECTIOUS DISEASES
(2021)
Article
Microbiology
Laura Seldeslachts, Cato Jacobs, Birger Tielemans, Eliane Vanhoffelen, Lauren Van der Sloten, Stephanie Humblet-Baron, Lieve Naesens, Katrien Lagrou, Erik Verbeken, Joost Wauters, Greetje Vande Velde
Summary: The study found that baloxavir marboxil has a therapeutic effect on influenza-associated pulmonary aspergillosis, improving body weight, survival, and viral clearance in a mouse model. It also reduces lung lesions and fungal burden, suggesting that baloxavir marboxil can mitigate severe influenza and decrease the risk of lethal invasive Aspergillus superinfection.
Review
Virology
Yacine Abed, Amel Saim-Mamoun, Guy Boivin
Summary: Neuraminidase inhibitors (NAIs) are important antiviral drugs recommended for seasonal influenza A and B infections. While currently targeting the surface NA protein, future development of additional anti-influenza agents may focus on internal proteins such as PA, PB1, and PB2.
REVIEWS IN MEDICAL VIROLOGY
(2021)
Article
Crystallography
Xinbo Zhou, Kaxi Yu, Jiyong Liu, Zhiping Jin, Xiurong Hu
Summary: This study focused on the crystallization and dissolution behaviors of three polymorphs of Baloxavir marboxil (BXM), a new FDA-approved anti-influenza agent. The results suggested that Form II, with a larger surface area of exposed hydrogen bond acceptors, demonstrated increased solubility and dissolution rate compared to Form I.
Article
Infectious Diseases
Yoshinori Ando, Takeshi Noshi, Kenji Sato, Toru Ishibashi, Yuki Yoshida, Takahiro Hasegawa, Motoyasu Onishi, Mitsutaka Kitano, Ryoko Oka, Makoto Kawai, Ryu Yoshida, Akihiko Sato, Takao Shishido, Akira Naito
Summary: The relationship between pharmacokinetic parameters and antiviral activity of baloxavir acid was investigated based on virus titre reduction in lungs of infected mice. The results showed dose-dependent virus titre reductions with oral baloxavir marboxil, suggesting its potential for maximizing virological outcomes in clinical settings.
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
(2021)
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
Hazem Hamza, Mahmoud M. Shehata, Ahmed Mostafa, Stephan Pleschka, Oliver Planz
Summary: The MEK inhibitor ATR-002 shows significant inhibitory effects on replication of different influenza virus strains, including those resistant to BXA. The combination of ATR-002 and BXA demonstrates synergistic potency in reducing virus titers, suggesting their potential as a combined therapy for treating BXA-resistant IAV infections.
FRONTIERS IN MICROBIOLOGY
(2021)
Article
Chemistry, Medicinal
Lin Tang, Haiyan Yan, Weibin Wu, Dawei Chen, Zhenxiong Gao, Jinqiang Hou, Cunlong Zhang, Yuyang Jiang
Summary: A series of novel substituted polycyclic pyridone derivatives were synthesized and found to exhibit potent anti-influenza activity, including inhibiting the replication of influenza A virus at picomolar concentrations. These compounds showed low cytotoxicity and promising potential as anti-influenza drug candidates.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Hidekazu Osada, Irina Chon, Wint Wint Phyu, Keita Wagatsuma, Nobuo Nagata, Takashi Kawashima, Isamu Sato, Tadashi Saito, Naoki Kodo, Hironori Masaki, Norichika Asoh, Yoshiko Tsuchihashi, Yutaka Shirahige, Yasuhiko Ono, Yasushi Shimada, Hirotsune Hamabata, Kousuke Saito, Reiko Saito
Summary: The study established a rapid real-time PCR system for detecting the PA/I38T variant in influenza viruses, with high sensitivity and the ability to distinguish between PA/I38T and wild type viruses. The prevalence of PA/I38T in clinical samples was found to be limited, highlighting the usefulness of the cycling probe-PCR system for antiviral surveillance.
ANTIVIRAL RESEARCH
(2021)
Article
Virology
Naoki Takizawa, Fumitaka Momose
Summary: Baloxavir acid (BXA), the active compound in baloxavir marboxil (BXM), reduces the propagation of influenza A and B viruses by inhibiting the activity of the polymerase acidic (PA) subunit. A novel PA subunit substitution, PA E198K, has been identified that reduced susceptibility to BXA.
ARCHIVES OF VIROLOGY
(2022)
Article
Immunology
Shogo Miyazawa, Takahiro Takazono, Naoki Hosogaya, Kazuko Yamamoto, Hideaki Watanabe, Masakazu Fujiwara, Satoki Fujita, Hiroshi Mukae
Summary: This study compared the impact of Baloxavir marboxil and oseltamivir treatments on intra-familial influenza transmission using a simulation model. The results showed that treating the first family member with Baloxavir marboxil may contribute to a greater reduction in intra-familial influenza transmission compared to oseltamivir.
CLINICAL INFECTIOUS DISEASES
(2022)
Article
Microbiology
Shashank Tripathi, Marie O. Pohl, Yingyao Zhou, Ariel Rodriguez-Frandsen, Guojun Wang, David A. Stein, Hong M. Moulton, Paul DeJesus, Jianwei Che, Lubbertus C. F. Mulder, Emilio Yangueez, Dario Andenmatten, Lars Pache, Balaji Manicassamy, Randy A. Albrecht, Maria G. Gonzalez, Quy Nguyen, Abraham Brass, Stephen Elledge, Michael White, Sagi Shapira, Nir Hacohen, Alexander Karlas, Thomas F. Meyer, Michael Shales, Andre Gatorano, Jeffrey R. Johnson, Gwen Jang, Tasha Johnson, Erik Verschueren, Doug Sanders, Nevan Krogan, Megan Shaw, Renate Koenig, Silke Stertz, Adolfo Garcia-Sastre, Sumit K. Chanda
CELL HOST & MICROBE
(2015)
Article
Virology
Nicole B. Glennon, Omar Jabado, Michael K. Lo, Megan L. Shaw
JOURNAL OF VIROLOGY
(2015)
Article
Chemistry, Medicinal
Megan R. Edwards, Colette Pietzsch, Thibaut Vausselin, Megan L. Shaw, Alexander Bukreyev, Christopher F. Basler
ACS INFECTIOUS DISEASES
(2015)
Editorial Material
Chemistry, Medicinal
Megan L. Shaw
ACS INFECTIOUS DISEASES
(2017)
Article
Virology
Maria T. Sanchez-Aparicio, Leighland J. Feinman, Adolfo Garcia-Sastre, Megan L. Shaw
JOURNAL OF VIROLOGY
(2018)
Article
Multidisciplinary Sciences
Dominik Dornfeld, Alexandra H. Dudek, Thibaut Vausselin, Sira C. Guenther, Judd F. Hultquist, Sebastian Giese, Daria Khokhlova-Cubberley, Yap C. Chew, Nevan J. Krogan, Adolfo Garcia-Sastre, Martin Schwemmle, Megan L. Shaw
SCIENTIFIC REPORTS
(2018)
Article
Chemistry, Medicinal
Kris M. White, Pablo Abreu, Hui Wang, Paul D. De Jesus, Balaji Manicassamy, Adolfo Garcia-Sastre, Sumit K. Chanda, Robert J. DeVita, Megan L. Shaw
ACS INFECTIOUS DISEASES
(2018)
Article
Biochemistry & Molecular Biology
Sven Heinz, Lorane Texari, Michael G. B. Hayes, Matthew Urbanowski, Max W. Chang, Ninvita Givarkes, Alexander Rialdi, Kris M. White, Randy A. Albrecht, Lars Pache, Ivan Marazzi, Adolfo Garcia-Sastre, Megan L. Shaw, Christopher Benner
Article
Biochemical Research Methods
Cameron A. Smurthwaite, Brett J. Hilton, Ryan O'Hanlon, Zachary D. Stolp, Bryan M. Hancock, Darin Abbadessa, Aleksandr Stotland, Larry A. Sklar, Roland Wolkowicz
Article
Chemistry, Medicinal
Kris M. White, Paul De Jesus, Zhong Chen, Pablo Abreu, Elisa Barile, Puiying A. Mak, Paul Anderson, Quy T. Nguyen, Atsushi Inoue, Silke Stertz, Renate Koenig, Maurizio Pellecchia, Peter Palese, Kelli Kuhen, Adolfo Garcia-Sastre, Sumit K. Chanda, Megan L. Shaw
ACS INFECTIOUS DISEASES
(2015)
Article
Microbiology
Grant Beyleveld, Daniel J. Chin, Elena Moreno Del Olmo, Jade Carter, Isabel Najera, Cristian Cilloniz, Megan L. Shaw
Article
Chemistry, Medicinal
Ryan O'Hanlon, Victor H. Leyva-Grado, Marion Sourisseau, Matthew J. Evans, Megan L. Shaw
ACS INFECTIOUS DISEASES
(2019)