Pleconaril (VP 63843)

Pleconaril is an antipicornaviral agent.^1,2 It inhibits Picornaviridae viral replication by binding to a hydrophobic pocket in the major VP1 capsid protein, which prevents uncoating of the viral RNA genome. Pleconaril inhibits replication of the rhinoviruses HRV-A2 and HRV-B14 in HeLa Rh cells (EC₅₀s = 0.1 and 0.3 μM, respectively) and is not cytotoxic to HeLa Rh cells with a 50% cytotoxic concentration (CC₅₀) of greater than 131 μM.³ It also inhibits replication of enterovirus 71 (EV71) in human rhabdomyosarcoma (RD) cells (EC₅₀ = 15 μM) and is not cytotoxic to RD cells (CC₅₀ = >131 μM). Pleconaril (80 mg/kg per day) increases survival of EV71-infected mouse pups from 20 to 80%.⁴

1.Florea, N.R., Maglio, D., and Nicolau, D.P.Pleconaril, a novel antipicornaviral agentPharmacotherapy23(3)339-348(2003) 2.Bernard, A., Lacroix, C., Cabiddu, M.G., et al.Exploration of the anti-enterovirus activity of a series of pleconaril/pirodavir-like compoundsAntivir. Chem. Chemother.24(2)56-61(2015) 3.Bernard, A., Lacroix, C., Cabiddu, M.G., et al.Exploration of the anti-enterovirus activity of a series of pleconaril/pirodavir-like compoundsAntivir. Chem. Chemother.24(2)56-61(2015) 4.Zhang, G., Zhou, F., Gu, B., et al.In vitro and in vivo evaluation of ribavirin and pleconaril antiviral activity against enterovirus 71 infectionArch. Virol.157(4)669-679(2012)