Research ArticlesMetabolism of Amprenavir in Liver Microsomes: Role of CYP3A4 Inhibition for Drug Interactions
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2017, Journal of Pharmaceutical SciencesCitation Excerpt :Therefore, the slight exposure decrease (23%-24%) in etoposide and saquinavir when co-administered with grapefruit juice (100 mL single dose) and quercetin (500 mg 3 times daily for 8 days), respectively, could be caused by intestinal inhibition of OATPs. It should be noted that intestinal inhibition of CYP3A by grapefruit juice and quercetin could not be ruled out, based on the observations that both etoposide and saquinavir are substrates of CYP3A in vitro.110,149-170 Interestingly, quercetin also induced CYP3A, with a 24% reduction in exposure of co-administered midazolam, a CYP3A probe substrate,171 likely through pregnane X receptor activation.172
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2012, Journal of Pharmaceutical SciencesCitation Excerpt :It is responsible for oxidative biotransformation of more than 50% of drugs in humans and rats.6 SQV is metabolized primarily by CYP3A4 to mono- and dihydroxylated metabolites with negligible antiviral activity in humans.7–9 Mean Cmax (maximum concentration in body) and AUC (area under the curve) values were significantly elevated when SQV hard-gel formulation was coadministered with other CYP3A4 inhibitors, that is, ritonavir or indinavir.10,11
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