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EC50: 5.4 nM for RSV fusion

VP-14637 is an inhibitor of RSV.

Respiratory syncytial virus (RSV) is the leading cause of respiratory tract infections in humans. RSV F protein that mediates fusion of the viral envelope with the host cell membrane has become a target of anti-RSV treatment.

In vitro: Previous study demonstrated that VP-14637 did not block RSV adsorption but inhibited RSV-induced cell-cell fusion and specifically bound to RSV-infected cells. VP-14637 was capable of specifically interacting with the RSV fusion protein. RSV variants resistant to VP-14637 were selected, in which no mutations arose in HR1, indicating a mechanism other than direct disruption of the heptad repeat interaction. The F proteins containing the resistance mutations exhibited greatly reduced binding of VP-14637 [1].

In vivo: In cotton rats, animals given as little as 126 microg/kg of VP-14637 by small droplet aerosol starting 1 day after experimental virus infection with either a RSV A or B subtype consistently had significantly lower mean pulmonary RSV titers and reduced histopathological findings than mock-treated animals or cotton rats given placebo. In addition, no cotton rat treated with VP14637 had any evident untoward responses [2].

Clinical trial: So far, no clinical study has been conducted.

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