VX-222 is a small molecule non-nucleoside inhibitor of HCV NS5B polymerase that is being investigated for the treatment of hepatitis C virus infection. While the protease inhibitors (telaprevir and boceprevir) are the directly-targeted anti-HCV agents furthest along in the development pipeline, HCV polymerase - an enzyme responsible for copying viral genetic material-is also a promising target. VX-222 is a novel non-nucleoside HCV NS5B polymerase inhibitor with potent in vitro activity.
|Cell lines||Huh7.5 cells|
|Preparation method||Trypsinizing Huh7.5 cells harboring HCV RNA replicons and plating into 48-well plates at a concentration of 4 × 104 cells/well. Changing the medium and adding VX-222in 200 μL of complete medium the next day. 48 hours later, total RNA is extracted and viral RNAs are quantiﬁed by real-time reverse transcription-PCR (RT-PCR). The effective drug concentrations that reduced HCV RNA replicon levels by 50% (EC50) are calculated by nonlinear regression analysis with log curve ﬁtting|
|Concentrations||0.01 nM -10 μM|
|Incubation time||48 hours|
|Animal models||Rats or dogs|
|Formulation||Dissolved in 30% PEG|
|Dosages||5 mg/kg for rats or 10 mg/kg for dogs|
|Administration||By oral gavage|
|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 80 mg/mL|
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