Drug intelligence / Profile preview

abt-072 + ketoconazole

Development stage
Unknown
Lead developer
AbbVie
Modality
Small Molecules
Administration
Oral
01

Overview

ABT-072 + ketoconazole is a combination of two drugs: ABT-072, a direct-acting antiviral agent (non-nucleoside NS5B polymerase inhibitor) developed for hepatitis C virus (HCV) infection, and ketoconazole, an antifungal agent that is also a potent inhibitor of the cytochrome P450 3A4 (CYP3A4) enzyme. ABT-072 acts by inhibiting the RNA-dependent RNA polymerase (NS5B) of HCV, thereby impairing viral RNA synthesis[1][5]. Ketoconazole has been used to study and manipulate drug pharmacokinetics by inhibiting CYP3A4-mediated metabolism, which can potentially increase the plasma concentration of coadministered drugs that are CYP3A4 substrates. The combination is investigational and mainly used in a pharmacokinetic context to assess the impact of CYP3A4 inhibition on the disposition of ABT-072 (and potentially other drugs)[5].

02

Targets

CYP3A4 (Cytochrome P450 3A4)NS5B (Hepatitis C virus non-structural protein 5B (NS5B) RNA-dependent RNA polymerase)PXR (Pregnane X receptor)

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