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4 results on '"Palmiotti, Christopher A."'

2. Prodrugs of a 1′-CN-4-Aza-7,9-dideazaadenosineC-Nucleoside Leading to the Discovery of Remdesivir (GS-5734) as a Potent Inhibitor of Respiratory Syncytial Virus with Efficacy in the African Green Monkey Model of RSV

Author

Mackman, Richard L., primary, Hui, Hon C., additional, Perron, Michel, additional, Murakami, Eisuke, additional, Palmiotti, Christopher, additional, Lee, Gary, additional, Stray, Kirsten, additional, Zhang, Lijun, additional, Goyal, Bindu, additional, Chun, Kwon, additional, Byun, Daniel, additional, Siegel, Dustin, additional, Simonovich, Scott, additional, Du Pont, Venice, additional, Pitts, Jared, additional, Babusis, Darius, additional, Vijjapurapu, Arya, additional, Lu, Xianghan, additional, Kim, Cynthia, additional, Zhao, Xiaofeng, additional, Chan, Julie, additional, Ma, Bin, additional, Lye, Diane, additional, Vandersteen, Adelle, additional, Wortman, Sarah, additional, Barrett, Kimberly T., additional, Toteva, Maria, additional, Jordan, Robert, additional, Subramanian, Raju, additional, Bilello, John P., additional, and Cihlar, Tomas, additional

Published
2021
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3. Broad-spectrum antiviral GS-5734 inhibits both epidemic and zoonotic coronaviruses

Author

Sheahan, Timothy P., primary, Sims, Amy C., additional, Graham, Rachel L., additional, Menachery, Vineet D., additional, Gralinski, Lisa E., additional, Case, James B., additional, Leist, Sarah R., additional, Pyrc, Krzysztof, additional, Feng, Joy Y., additional, Trantcheva, Iva, additional, Bannister, Roy, additional, Park, Yeojin, additional, Babusis, Darius, additional, Clarke, Michael O., additional, Mackman, Richard L., additional, Spahn, Jamie E., additional, Palmiotti, Christopher A., additional, Siegel, Dustin, additional, Ray, Adrian S., additional, Cihlar, Tomas, additional, Jordan, Robert, additional, Denison, Mark R., additional, and Baric, Ralph S., additional

Published
2017
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4. Prodrugs of a 1′-CN-4-Aza-7,9-dideazaadenosine C-Nucleoside Leading to the Discovery of Remdesivir (GS-5734) as a Potent Inhibitor of Respiratory Syncytial Virus with Efficacy in the African Green Monkey Model of RSV

Author

Mackman, Richard L., Hui, Hon C., Perron, Michel, Murakami, Eisuke, Palmiotti, Christopher, Lee, Gary, Stray, Kirsten, Zhang, Lijun, Goyal, Bindu, Chun, Kwon, Byun, Daniel, Siegel, Dustin, Simonovich, Scott, Du Pont, Venice, Pitts, Jared, Babusis, Darius, Vijjapurapu, Arya, Lu, Xianghan, Kim, Cynthia, Zhao, Xiaofeng, Chan, Julie, Ma, Bin, Lye, Diane, Vandersteen, Adelle, Wortman, Sarah, Barrett, Kimberly T., Toteva, Maria, Jordan, Robert, Subramanian, Raju, Bilello, John P., and Cihlar, Tomas

Abstract

A discovery program targeting respiratory syncytial virus (RSV) identified C-nucleoside 4(RSV A2 EC50= 530 nM) as a phenotypic screening lead targeting the RSV RNA-dependent RNA polymerase (RdRp). Prodrug exploration resulted in the discovery of remdesivir (1, GS-5734) that is >30-fold more potent than 4against RSV in HEp-2 and NHBE cells. Metabolism studies in vitro confirmed the rapid formation of the active triphosphate metabolite, 1-NTP, and in vivo studies in cynomolgus and African Green monkeys demonstrated a >10-fold higher lung tissue concentration of 1-NTPfollowing molar normalized IV dosing of 1compared to that of 4. A once daily 10 mg/kg IV administration of 1in an African Green monkey RSV model demonstrated a >2-log10reduction in the peak lung viral load. These early data following the discovery of 1supported its potential as a novel treatment for RSV prior to its development for Ebola and approval for COVID-19 treatment.

Published
2021
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