Cobicistat versus ritonavir boosting and differences in the drug-drug interaction profiles with co-medications



Marzolini, Catia, Gibbons, Sara, Khoo, Saye ORCID: 0000-0002-2769-0967 and Back, David
(2016) Cobicistat versus ritonavir boosting and differences in the drug-drug interaction profiles with co-medications. JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 71 (7). pp. 1755-1758.

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Abstract

Nearly all HIV PIs and the integrase inhibitor elvitegravir require a pharmacokinetic enhancer in order to achieve therapeutic plasma concentrations at the desired dose and frequency. Whereas ritonavir has been the only available pharmacokinetic enhancer for more than a decade, cobicistat has recently emerged as an alternative boosting agent. Cobicistat and ritonavir are equally strong inhibitors of cytochrome P450 (CYP) 3A4 and consequently were shown to be equivalent pharmacokinetic enhancers for elvitegravir and for the PIs atazanavir and darunavir. Since cobicistat is a more selective CYP inhibitor than ritonavir and is devoid of enzyme-inducing properties, differences are expected in their interaction profiles with some co-medications. Drugs whose exposure might be altered by ritonavir but unaltered by cobicistat are drugs primarily metabolized by CYP1A2, CYP2B6, CYP2C8, CYP2C9 and CYP2C19 or drugs undergoing mainly glucuronidation. Thus, co-medications should be systematically reviewed when switching the pharmacokinetic enhancer to anticipate potential dosage adjustments.

Item Type: Article
Uncontrolled Keywords: Humans, HIV-1, HIV Infections, Ritonavir, HIV Protease Inhibitors, Anti-HIV Agents, Drug Therapy, Combination, Drug Interactions, Cytochrome P-450 CYP3A, Cytochrome P-450 CYP3A Inhibitors, Darunavir, Atazanavir Sulfate, Cobicistat
Depositing User: Symplectic Admin
Date Deposited: 17 May 2017 06:30
Last Modified: 19 Jan 2023 07:04
DOI: 10.1093/jac/dkw032
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URI: https://livrepository.liverpool.ac.uk/id/eprint/3007496

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