Discovery of the RSV Inhibitor TMC353121

Bonfanti, Jean‐François; Ispas, Gabriela; Velsen, Frans Van; Olszewska, Wieslawa; Gevers, Tom; Roymans, Dirk

doi:10.1002/9780470929353.ch24

Cited by 2 publications

(2 citation statements)

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“…44,45 The discovery of BMS-433771 and TMC-353121 in particular have been reviewed in depth and provoked greater interest in the discovery of RSV fusion inhibitors. 43,46 The benzodiazepine urea RSV604 disclosed by Arrow Therapeutics was the only compound to achieve any sort of clinical proof of concept (5-4, Figure 5). 42 5.1.…”

Section: Preclinical Rsv Inhibitor Programsmentioning

confidence: 99%

“… BMS-433771 ( 5 - 1 , Figure ), identified by scientists at Bristol-Myers Squib (BMS; New York, NY), was the first fusion inhibitor described with oral bioavailability . Subsequently the structurally distinct TMC-353121 ( 5 - 2 ; Johnson & Johnson, New Brunswick, NJ) progressed into nonhuman primate models of RSV infection, while the polycyclic fusion inhibitor BT-9881 ( 5 - 3 ) was evaluated in phase 1 clinical trials. , The discovery of BMS-433771 and TMC-353121 in particular have been reviewed in depth and provoked greater interest in the discovery of RSV fusion inhibitors. , The benzodiazepine urea RSV604 disclosed by Arrow Therapeutics was the only compound to achieve any sort of clinical proof of concept ( 5 - 4 , Figure ). …”

Section: Preclinical Rsv Inhibitor Programsmentioning

confidence: 99%

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State of the Art in Respiratory Syncytial Virus Drug Discovery and Development

2018

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Respiratory syncytial virus (RSV) is a globally prevalent viral infection with limited treatment options which hospitalizes millions each year. Treatment options have been limited to palivizumab, a monoclonal antibody, approved for prophylaxis in high-risk infants and ribavirin with very limited efficacy and significant safety concerns. This Perspective surveys the range of direct acting antiviral agents (DAAs) that target key steps in the viral life cycle. A number of approaches to DAAs have produced landmark clinical studies over the past few years, notably in fusion and nucleoside inhibitors, and an update of the clinical status of these compounds is provided. Non-nucleoside inhibitors of replication are reviewed in addition to inhibitors of other mechanisms, notably the RSV N and G proteins. This article will provide an informative perspective of the current status of drug discovery targeted at providing an effective therapy for RSV infection.

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