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Vol. 29, Issue 2, 100-102, February 2001
Departments of Pharmacology and Since antiretroviral drugs are known to inhibit many cytochrome
P450 isoforms, the inhibition of CYP2B6 by non-nucleoside reverse
transcriptase inhibitors and viral protease inhibitors was studied in
vitro in human liver microsomes using bupropion hydroxylation as the
CYP2B6 index reaction. Mean IC50 values (µM) for
inhibition of bupropion hydroxylation were: nelfinavir (2.5), ritonavir
(2.2), and efavirenz (5.5). The reaction was only weakly inhibited by
indinavir, saquinavir, amprenavir, delavirdine, and nevirapine. The
inhibition of bupropion hydroxylation in vitro by nelfinavir,
ritonavir, and efavirenz indicates inhibitory potency versus CYP2B6 and
suggests the potential for clinical drug interactions.
Experimental Therapeutics
and of Biochemistry,
Tufts University School of Medicine
and
the Division of Clinical Pharmacology,
New England Medical
Center,
Boston, Massachusetts
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