Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5 and 366 pM against genotype 6a. Ombitasvir has EC50s of 14.1 and 5.0 pM against genotype 1a-H77 and 1b-Con1 subgenomic replicons, respectively.
In GT1a, variants M28V, L31V, and H58D confers 58- to 243-fold resistance to Ombitasvir. Single variants M28T, Q30R, and Y93C/S confers 800- to 8965-fold resistance, while Y93H/N confers >40000-fold resistance to Ombitasvir.
|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: ≥ 60 mg/mL|
In vitro and in vivo antiviral activity and resistance profile of ombitasvir, an inhibitor of hepatitis C virus NS5A.
Krishnan P, et al. Antimicrob Agents Chemother. 2015 Feb;59(2):979-87. PMID: 25451055.
Discovery of ABT-267, a pan-genotypic inhibitor of HCV NS5A.
DeGoey DA, et al. J Med Chem. 2014 Mar 13;57(5):2047-57. PMID: 24400777.
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