NCT00621699

Pharmacokinetic Drug Interaction Between Ezetimibe and Tacrolimus After Single Dose Administration in Healthy Subjects

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 24 (actual)
• Sponsor: University Medicine Greifswald · Academic / Other
• Sex: All
• Age: 18 Years – 45 Years
• Healthy volunteers: Accepted

Summary

The purpose of this study is to confirm a significant influence of ezetimibe and tacrolimus on each others pharmacokinetics

Detailed description

Hypercholesterolemia is a frequent finding in organ transplant recipients receiving immunosuppressive drugs such as tacrolimus. To prevent increased cardiovascular morbidity and mortality in these patients, co-medication with lipid-lowering statins is recommended. However, treatment with statins is limited in many patients by insufficient cholesterol-lowering efficacy, drug interactions and serious adverse drug reactions (e.g. rhabdomyolysis). These patients may benefit from comedication with the cholesterol absorption inhibitor ezetimibe. Since tacrolimus and ezetimibe were shown to be substrates of the efflux transporter ABCB1 (P-glycoprotein), drug interactions between both compounds may occur. Therefore, this clinical study in healthy subjects was initiated to evaluate the clinical relevance of drug/drug interactions between tacrolimus and ezetimibe according to the accepted bioequivalence approach.

Conditions

• Pharmacokinetics
• Drug Interactions
• Hypercholesterolemia
• Immunosuppression

Interventions

Type	Name	Description
DRUG	1 tablet Ezetrol(R) (ezetimibe), MSD Sharp & Dohme GmbH, Germany	administration of 1 tablet Ezetrol(R) (10 mg ezetimibe), 0-144 h blood sampling, 0-5 d urine sampling (24 h intervals) and 0-10 d feces sampling
DRUG	1 capsule Prograf(R) (tacrolimus), Astellas Pharma GmbH, Germany	administration of 1 capsule Prograf(R) (5 mg tacrolimus), 0-144 h blood sampling
DRUG	1 tablet Ezetrol(R) + 1 capsules Prograf(R)	administration of 1 tablet Ezetrol(R) (10 mg ezetimibe) and 1 capsule Prograf(R) (5 mg Tacrolimus), 0-144 h blood sampling, 0-5 d urine sampling (24 h intervals) and 0-10 d feces sampling

Timeline

• Start date: 2007-09-01
• Primary completion: 2007-11-01
• Completion: 2007-11-01
• First posted: 2008-02-22
• Last updated: 2008-02-22

Locations

1 site across 1 country: Germany