biostudies-literatureOswald SNIGMS NIH HHS506-13https://www.ebi.ac.uk/biostudies/studies/S-EPMC3667671biostudies-literatureUnknown91(3)Hypercholesterolemia frequently occurs in patients treated with efavirenz who cannot be treated adequately with statins because of drug interactions. These patients may benefit from cholesterol-lowering therapy with ezetimibe. This study determined the influence of single-dose and multiple-dose efavirenz (400 mg/day for 9 days) on the pharmacokinetics and sterol-lowering of ezetimibe (10 mg) in 12 healthy subjects. In addition, the influence of efavirenz on genome-wide intestinal expression and in vitro function of ABCB1, ABCC2, UGT1A1, and OATP1B1 was studied. Efavirenz (multiple dose) had no influence on the pharmacokinetics and lipid-lowering functions of ezetimibe. Intestinal expression of enzymes and transporters (e.g., ABCB1, ABCC2, and UGT1A1) was not affected by chronic efavirenz. Clinical pharmacology and therapeuticsImpact of efavirenz on intestinal metabolism and transport: insights from an interaction study with ezetimibe in healthy volunteers.PMC3667671R01GM078501R01 GM078501Keiser MMarinova MLutjohann DRunge DNassif AJia JOgburn ETDesta ZMostertz JSiegmund WMeyer zu Schwabedissen HEHubeny AUlrich AOswald SModess CKroemer HKfalseImpact of efavirenz on intestinal metabolism and transport: insights from an interaction study with ezetimibe in healthy volunteers.Hypercholesterolemia frequently occurs in patients treated with efavirenz who cannot be treated adequately with statins because of drug interactions. These patients may benefit from cholesterol-lowering therapy with ezetimibe. This study determined the influence of single-dose and multiple-dose efavirenz (400 mg/day for 9 days) on the pharmacokinetics and sterol-lowering of ezetimibe (10 mg) in 12 healthy subjects. In addition, the influence of efavirenz on genome-wide intestinal expression and in vitro function of ABCB1, ABCC2, UGT1A1, and OATP1B1 was studied. Efavirenz (multiple dose) had no influence on the pharmacokinetics and lipid-lowering functions of ezetimibe. Intestinal expression of enzymes and transporters (e.g., ABCB1, ABCC2, and UGT1A1) was not affected by chronic efavirenz. 2012-01-01T00:00:00Z2012 Mar2025-06-01T12:29:54.365Z2025-06-01T12:29:54.365ZS-EPMC36676712229738710.1038/clpt.2011.255