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

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

Condition Phase
Phase 1

Study Type: Observational
Study Design: Time Perspective: Prospective
Official Title: 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

Resource links provided by NLM:

Further study details as provided by Heidelberg University:

Estimated Enrollment: 12
Study Start Date: January 2005
Detailed Description:


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

Ages Eligible for Study:   18 Years to 50 Years   (Adult)
Sexes Eligible for Study:   All
Accepts Healthy Volunteers:   Yes

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
  Contacts and Locations
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Please refer to this study by its identifier: NCT00176033

Clinical Research Center, Department of Internal Medicine VI
Heidelberg, Germany, 69120
Sponsors and Collaborators
Heidelberg University
Principal Investigator: Gerd Mikus, MD, BSc Department of Internal Medicine VI
  More Information Identifier: NCT00176033     History of Changes
Other Study ID Numbers: K026
Study First Received: September 12, 2005
Last Updated: February 12, 2009

Keywords provided by Heidelberg University:
HIV Infections

Additional relevant MeSH terms:
HIV Protease Inhibitors
Protease Inhibitors
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action
Anti-HIV Agents
Anti-Retroviral Agents
Antiviral Agents
Anti-Infective Agents
Cytochrome P-450 CYP3A Inhibitors
Cytochrome P-450 Enzyme Inhibitors processed this record on May 24, 2017