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Discovery of Sisunatovir (RV521), an Inhibitor of Respiratory Syncytial Virus Fusion. 2021
G Stuart Cockerill, and
Richard M Angell, and
Alexandre Bedernjak, and
Irina Chuckowree, and
Ian Fraser, and
Jose Gascon-Simorte, and
Morgan S A Gilman, and
James A D Good, and
Rachel Harland, and
Sara M Johnson, and
John H Ludes-Meyers, and
Edward Littler, and
James Lumley, and
Graham Lunn, and
Neil Mathews, and
Jason S McLellan, and
Michael Paradowski, and
Mark E Peeples, and
Claire Scott, and
Dereck Tait, and
Geraldine Taylor, and
Michelle Thom, and
Elaine Thomas, and
Carol Villalonga Barber, and
Simon E Ward, and
Daniel Watterson, and
Gareth Williams, and
Paul Young, and
Kenneth Powell
Reviral Ltd., Stevenage Bioscience Catalyst, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2FX, U.K.
RV521 is an orally bioavailable inhibitor of respiratory syncytial virus (RSV) fusion that was identified after a lead optimization process based upon hits that originated from a physical property directed hit profiling exercise at Reviral. This exercise encompassed collaborations with a number of contract organizations with collaborative medicinal chemistry and virology during the optimization phase in addition to those utilized as the compound proceeded through preclinical and clinical evaluation. RV521 exhibited a mean IC50 of 1.2 nM against a panel of RSV A and B laboratory strains and clinical isolates with antiviral efficacy in the Balb/C mouse model of RSV infection. Oral bioavailability in preclinical species ranged from 42 to >100% with evidence of highly efficient penetration into lung tissue. In healthy adult human volunteers experimentally infected with RSV, a potent antiviral effect was observed with a significant reduction in viral load and symptoms compared to placebo.
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