Conditions: Pharmacokinetics Drug Interactions Pharmacodynamics Intestinal Transporter Expression
Allocation: NON_RANDOMIZED | Intervention model: SINGLE_GROUP
Enrollment: 12
Healthy volunteers: yes

Brief summary:
The purpose of this study is to evaluate the effects of a chronic co-medication of efavirenz on pharmacokinetics and sterol-lowering effects of ezetimibe at steady-state in healthy subjects genotyped for ABCB1, ABCC2, CYP2B6 and UGT1A1.

Detailed description:

Arms:
arm 1: A study with a duration of 34 days with 4 periods (= 4 pharmakokinetics) on 12 healthy subjects.

Interventions: intervention 1: Ezetrol (ezetimibe) multiple dose intervention 2: Ezetrol (ezetimibe) multiple dose and Sustiva (efavirenz) single dose intervention 3: Ezetrol (ezetimibe) and Sustiva (efavirenz) multiple dose intervention 4: Sustiva (efavirenz) single dose
Intervention descriptions: intervention 1: administration of 1 tablet/day Ezetrol (10 mg ezetimibe) on study day 6-15 and a pharmakokinetic on study day 15 (0-24 h blood sampling, 0-24 h urine sampling and 5 d feces sampling (study day 11-15)) intervention 2: administration of 1 tablet/day Ezetrol(R) (10 mg ezetimibe) on study day 16-20 and 2 capsules Sustiva(R) (2x200 mg efavirenz) on study day 16 with a pharmakokinetic (0-120 h blood sampling, urine sampling (24 h intervals) and feces sampling on study days 16-20) intervention 3: administration of 1 tablet/day Ezetrol(R) (10 mg ezetimibe) and 2 capsules/day Sustiva(R) (2x200 mg efavirenz) on study day 21-30 and with a pharmakokinetic (0-120 h blood sampling, urine sampling (24 h intervals) on study day 30 and feces sampling on study day 26-30) intervention 4: administration of 2 capsules Sustiva(R) (2x200 mg efavirenz) on study day 1 with a pharmakokinetic (0-120 h blood sampling, urine sampling (24 h intervals) and feces sampling on study days 1-5)

Protocol document: