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Pharmacokinetic and Pharmacodynamic Interactions Between the Cholesterol-lowering Ezetimibe and the Non-nucleoside Reverse Transcriptase Inhibitor Efavirenz During Chronic Treatment in Healthy Volunteers With Reference to Intestinal Expression of CYP3A4, UGT1A1, ABCB1 and ABCC2

This study has been completed.
Sponsor:
Information provided by:
University Medicine Greifswald
ClinicalTrials.gov Identifier:
NCT00810303
First received: December 17, 2008
Last updated: September 23, 2010
Last verified: September 2010
History of Changes
Results First Received: June 21, 2010  
Study Type: Interventional
Study Design: Allocation: Non-Randomized;   Endpoint Classification: Pharmacokinetics/Dynamics Study;   Intervention Model: Single Group Assignment;   Masking: Open Label;   Primary Purpose: Basic Science
Conditions: Pharmacokinetics
Drug Interactions
Pharmacodynamics
Intestinal Transporter Expression
Interventions: Drug: Ezetrol (ezetimibe) multiple dose
Drug: Ezetrol (ezetimibe) multiple dose and Sustiva (efavirenz) single dose
Drug: Ezetrol (ezetimibe) and Sustiva (efavirenz) multiple dose
Drug: Sustiva (efavirenz) single dose

  Participant Flow
  Hide Participant Flow

Recruitment Details
Key information relevant to the recruitment process for the overall study, such as dates of the recruitment period and locations
No text entered.

Pre-Assignment Details
Significant events and approaches for the overall study following participant enrollment, but prior to group assignment
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Reporting Groups
  Description
Study Group whole study group: 12 healthy subjects

Participant Flow for 4 periods

 Period 1:   Efavirenz Alone - Day 1-5
    Study Group  
STARTED     12  
COMPLETED     12  
NOT COMPLETED     0  

Period 2:   Ezetimibe Alone - Day 6-15
    Study Group  
STARTED     12  
COMPLETED     12  
NOT COMPLETED     0  

Period 3:   Ezetimibe and Efavirenz - Day 16-20
    Study Group  
STARTED     12  
COMPLETED     12  
NOT COMPLETED     0  

Period 4:   Ezetimibe and Efavirenz - Day 21-30
    Study Group  
STARTED     12  
COMPLETED     12  
NOT COMPLETED     0  



  Baseline Characteristics
  Hide Baseline Characteristics

Reporting Groups
  Description
Study Group whole study group: 12 healthy subjects

Baseline Measures
    Study Group  
Number of Participants  
[units: participants]
 		  12  
Age  
[units: participants]
 		 
<=18 years     0  
Between 18 and 65 years     12  
>=65 years     0  
Age  
[units: years]
Mean ± Standard Deviation 		  26  ± 4.6  
Gender  
[units: participants]
 		 
Female     0  
Male     12  
Region of Enrollment  
[units: participants]
 		 
Germany     12  



  Outcome Measures
  Show All Outcome Measures

1.  Primary:   AUC0-24h of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15   [ Time Frame: study day 15 ]
  Show Outcome Measure 1

2.  Primary:   AUC0-24h of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16   [ Time Frame: study day 16 ]
  Show Outcome Measure 2

3.  Primary:   AUC0-24h of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30   [ Time Frame: study day 30 ]
  Show Outcome Measure 3

4.  Primary:   Cmax of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15   [ Time Frame: study day 15 ]
  Show Outcome Measure 4

5.  Primary:   Cmax of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16   [ Time Frame: study day 16 ]
  Show Outcome Measure 5

6.  Primary:   Cmax of Free Ezetimibe (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30   [ Time Frame: study day 30 ]
  Show Outcome Measure 6

7.  Primary:   AUC of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz) on Study Days 1-5   [ Time Frame: study days 1-5 ]
  Show Outcome Measure 7

8.  Primary:   AUC of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Days 16-20   [ Time Frame: study days 16-20 ]
  Show Outcome Measure 8

9.  Primary:   AUC0-24h of Efavirenz (Steady State Pharmacokinetic After Chronic Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Day 30   [ Time Frame: study day 30 ]
  Show Outcome Measure 9

10.  Primary:   Cmax of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz) on Study Days 1-5   [ Time Frame: study days 1-5 ]
  Show Outcome Measure 10

11.  Primary:   Cmax of Efavirenz (Single Dose Pharmacokinetic After Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Days 16-20   [ Time Frame: study days 16-20 ]
  Show Outcome Measure 11

12.  Primary:   Cmax of Efavirenz (Steady State Pharmacokinetic After Chronic Treatment With 400 mg Efavirenz and Concomitant Chronic Treatment of 10 mg Ezetimibe) on Study Day 30   [ Time Frame: study day 30 ]
  Show Outcome Measure 12

13.  Secondary:   AUC0-24h of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15   [ Time Frame: study day 15 ]
  Show Outcome Measure 13

14.  Secondary:   AUC0-24h of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16   [ Time Frame: study day 16 ]
  Show Outcome Measure 14

15.  Secondary:   AUC0-24h of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30   [ Time Frame: study day 30 ]
  Show Outcome Measure 15

16.  Secondary:   Cmax of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe) on Study Day 15   [ Time Frame: study day 15 ]
  Show Outcome Measure 16

17.  Secondary:   Cmax of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Single Dose Administration of 400 mg Efavirenz) on Study Day 16   [ Time Frame: study day 16 ]
  Show Outcome Measure 17

18.  Secondary:   Cmax of Ezetimibe Glucuronide (Steady-state Pharmacokinetic After Chronic Treatment With 10 mg Ezetimibe and Concomitant Chronic Treatment With 400 mg Efavirenz) on Study Day 30   [ Time Frame: study day 30 ]
  Show Outcome Measure 18


  Serious Adverse Events
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  Other Adverse Events
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  More Information
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Certain Agreements:  
All Principal Investigators ARE employed by the organization sponsoring the study.


Limitations and Caveats
Limitations of the study, such as early termination leading to small numbers of participants analyzed and technical problems with measurement leading to unreliable or uninterpretable data
No text entered.  


Results Point of Contact:  
Name/Title: Danilo Wegner
Organization: Department of Clinical Pharmacology
phone: +4903834865640
e-mail: dwegner@uni-greifswald.de


No publications provided


Responsible Party: Prof. Dr. W. Siegmund, MD, Organization: Department of Clinical Pharmacology
ClinicalTrials.gov Identifier: NCT00810303     History of Changes
Other Study ID Numbers: Efavirenz - 2008
Study First Received: December 17, 2008
Results First Received: June 21, 2010
Last Updated: September 23, 2010
Health Authority: Germany: Federal Institute for Drugs and Medical Devices