Merimepodib, also known as VX-497, is an orally bioavailable IMPDH inhibitor with broad spectrum antiviral activities. VX-497 has intermediate antiviral activity against a second group of viruses, which includes HSV-1, parainfluenza-3 virus, BVDV, VEEV, and dengue virus, with IC50s ranging from 6 to 19 μM.
In vivo, oral administration of VX-497 inhibits the primary IgM antibody response in a dose-dependent manner, with an ED(50) value of approximately 30-35 mg/kg in mice. Single daily dosing of VX-497 is observed to be as effective as twice-daily dosing in this model of immune activation.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 27 mg/mL|
The novel IMPDH inhibitor VX-497 prolongs skin graft survival and improves graft versus host disease in mice
C J Decker, et al. Dvrgs Exp Clin Res. 2001;27(3):89-95. PMID: 11447770.
VX-497: a novel, selective IMPDH inhibitor and immunosuppressive agent
J Jain, et al. J Pharm Sci. 2001 May;90(5):625-37. PMID: 11288107.
Broad-spectrum antiviral activity of the IMP dehydrogenase inhibitor VX-497: a comparison with ribavirin and demonstration of antiviral additivity with alpha interferon
W Markland, et al. Antimicrob Agents Chemother. 2000 Apr;44(4):859-66. PMID: 10722482.
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