Influence of Drug Transporter Expression on the Pharmacokinetics of the HIV Protease Inhibitor Kaletra

This study has been completed.
Sponsor:
Information provided by:
Heidelberg University
ClinicalTrials.gov Identifier:
NCT00176033
First received: September 12, 2005
Last updated: February 12, 2009
Last verified: February 2009

September 12, 2005
February 12, 2009
January 2005
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Complete list of historical versions of study NCT00176033 on ClinicalTrials.gov Archive Site
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Influence of Drug Transporter Expression on the Pharmacokinetics of the HIV Protease Inhibitor Kaletra
Influence of Drug Transporter Expression on the Pharmacokinetics of the HIV Protease Inhibitor Kaletra (Lopinavir/Ritonavir) and on the Concentration Relations Between Plasma, Blood Cells, Saliva and Urine

The aim of this study is to determine the pharmacokinetics of Kaletra™ (HIV protease inhibitors lopinavir and ritonavir) in different body compartments and to assess the role of four different drug transporters (MDR, MRP1, MRP2 and BCRP) in the tissue distribution of the two protease inhibitors. The latter will be studied by comparing intracellular concentrations of peripheral blood mononuclear cells (PBMCs) with total and free plasma concentrations in healthy individuals. These effects will be studied after single dose (day 1), during steady state (day 3), and during chronic treatment (day 14).

Objective:

Measurement of AUC, Cmax, tmax, t1/2 and clearance (Cl) of the protease inhibitor Kaletra™ (lopinavir and ritonavir) each in the plasma of healthy individuals

  • establish free and total plasma - blood cell concentration-relationship
  • establish free and total plasma - saliva concentration-relationship
  • establish blood cell concentration - drug transporter expression-relationship
Observational
Time Perspective: Prospective
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  • Healthy
  • Pharmacokinetics
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*   Includes publications given by the data provider as well as publications identified by ClinicalTrials.gov Identifier (NCT Number) in Medline.
 
Completed
12
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Inclusion Criteria:

  • Good state of health

Exclusion Criteria:

  • Drug treatment with known inhibitors or inducers of cytochrome P450 isozymes or ABC-transporters within the preceding 2 months
  • Any acute or chronic illness
  • Smoking
  • Pregnancy
  • Alcohol or drug abuse
Both
18 Years to 50 Years
Yes
Contact information is only displayed when the study is recruiting subjects
Germany
 
NCT00176033
K026
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Heidelberg University
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Principal Investigator: Gerd Mikus, MD, BSc Department of Internal Medicine VI
Heidelberg University
February 2009

ICMJE     Data element required by the International Committee of Medical Journal Editors and the World Health Organization ICTRP