ABT-333 is a nonnucleoside NS5B polymerase inhibitor for the treatment of HCV infection. An interferon-free combination of the protease inhibitor ABT-450 with ritonavir (ABT-450/r), the nonnucleoside polymerase inhibitor ABT-333, and ribavirin showed efficacy against the hepatitis C virus (HCV) in a pilot study involving patients with HCV genotype 1 infection. ABT-333 is currently under clinical trials for the treatment of Hepatitis C.
Cell Experiment | |
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Cell lines | HCV replicon cells |
Preparation method | MTT analysis Both replicon-containing cell lines were maintained in Dulbecco’s modified Eagle’s medium (DMEM) containing 100 IU/ml penicillin, 100 g/ml streptomycin, and 200 g/ml G418 (all from Invitrogen, Carlsbad, CA) with 10% (vol/vol) fetal bovine serum (FBS).TheinhibitoryeffectsofdasabuvironHCVRNAreplication were determined in DMEM containing 5% FBS, with or without 40% human plasma (Bioreclamation, Westbury, NY), by measuring the activity of the luciferase reporter gene. The cells were incubated for 3 days in the presence of dasabuvir and subsequently were lysed and processed according to the manufacturer’s instructions (Promega, Madison, WI). The luciferase activity in the cells was measured using a Victor II luminometer (Perkin-Elmer, Waltham, MA); 50% effective concentration (EC50) values were calculated using nonlinear regression curve fitting to a 4-parameter logistic equation with GraphPad Prism 4 software. EC50s and standard deviations (SDs) were calculated from at least 3 experiments conducted in duplicate. The cytotoxicity of dasabuvir was determined with the colorimetric assay using MTT. |
Concentrations | Dasabuvir inhibited replication of HCV subgenomic replicons in cell culture assays, with EC50 values of 7.7 and 1.8 nM against genotype 1a (H77) and 1b (Con1), respectively. |
Incubation time | 3 days |
Animal Experiment | |
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Animal models | none |
Formulation | |
Dosages | |
Administration |
Molecular Weight | 493.57 |
Formula | C26H27N3O5S |
CAS Number | 1132935-63-7 |
Solubility (25°C) | DMSO 26 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
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.
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