Pimodivir

Pimodivir is an inhibitor of influenza virus polymerase basic protein 2 (PB2; K_D = <0.003 µM).¹ It also binds to glycogen synthase kinase 3β (GSK3β; K_i = ^~1.6 µM) and inhibits the activity of Axl and calcium/calmodulin-dependent protein kinase IIβ (CaMKIIβ) by greater than 50% in a panel of 65 human and rat kinases. Pimodivir decreases the replication of seven adamantine- and neuraminidase inhibitor-resistant strains of influenza virus A (EC₅₀s = <0.15-2.8 nM in a cell-based assay). It increases the antiviral activity of oseltamivir (Item No. 16070), zanamivir (Item No. 15123), and favipiravir (T-705; Item No. 23384) with 50% combination index (CI₅₀) values of 0.58, 0.64, and 0.89, respectively, in a cell-based assay.² Pimodivir increases survival in a mouse model of intranasal influenza A infection when administered at doses of 1, 3, and 10 mg/kg twice per day.

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1. Clark, M.P., Ledeboer, M.W., Davies, I., et al. Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2. J. Med. Chem. 57(15), 6668-6678 (2014).

2. Byrn, R.A., Jones, S.M., Bennett, H.B., et al. Preclinical activity of VX-787, a first-in-class, orally bioavailable inhibitor of the influenza virus polymerase PB2 subunit. Antimicrob. Agents Chemother. 59(3), 1569-1582 (2014).