Drug intelligence / Profile preview

boceprevir + ritonavir

Development stage
Discontinued
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Boceprevir + ritonavir is a combination of two small molecule drugs: boceprevir, an oral NS3/4A protease inhibitor formerly used for the treatment of chronic hepatitis C virus (HCV) genotype 1 infection, and ritonavir, an HIV protease inhibitor primarily used as a pharmacokinetic booster for other protease inhibitors in HIV therapy. Both drugs are substrates and inhibitors of cytochrome P450 3A and P-glycoprotein, leading to significant potential for drug-drug interactions. The use of this combination is primarily studied and discussed in the context of patients co-infected with HIV and HCV, where ritonavir is often used to boost other HIV protease inhibitors. Boceprevir acts by inhibiting the HCV NS3/4A protease, thereby blocking viral replication. Ritonavir, at low doses, inhibits CYP3A activity, boosting concentrations of co-administered protease inhibitors, but also impacts the pharmacokinetics of drugs like boceprevir. Boceprevir has been marketed under the brand name Victrelis. Use of this combination is associated with complex pharmacokinetic interactions, often resulting in decreased concentrations of both boceprevir and ritonavir-boosted protease inhibitors, which can lead to reduced therapeutic effectiveness for both HCV and HIV. Due to these risks, this combination is not routinely recommended outside of specific investigational or co-infection settings[1][2][3][4][5].

02

Targets

CYP3A (CYP3A family)NS3/4A (Hepatitis C virus nonstructural protein 3/4A serine protease)PR (Progesterone receptor)

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