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
  Purpose

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
Healthy
Pharmacokinetics
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:

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
  Eligibility

Ages Eligible for Study:   18 Years to 50 Years
Genders Eligible for Study:   Both
Accepts Healthy Volunteers:   Yes
Criteria

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
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the Contacts provided below. For general information, see Learn About Clinical Studies.

Please refer to this study by its ClinicalTrials.gov identifier: NCT00176033

Locations
Germany
Clinical Research Center, Department of Internal Medicine VI
Heidelberg, Germany, 69120
Sponsors and Collaborators
Heidelberg University
Investigators
Principal Investigator: Gerd Mikus, MD, BSc Department of Internal Medicine VI
  More Information

No publications provided

ClinicalTrials.gov Identifier: NCT00176033     History of Changes
Other Study ID Numbers: K026
Study First Received: September 12, 2005
Last Updated: February 12, 2009
Health Authority: Germany: Federal Institute for Drugs and Medical Devices

Keywords provided by Heidelberg University:
ritonavir
lopinavir
HIV Infections

Additional relevant MeSH terms:
Protease Inhibitors
HIV Protease Inhibitors
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action
Pharmacologic Actions
Anti-HIV Agents
Anti-Retroviral Agents
Antiviral Agents
Anti-Infective Agents
Therapeutic Uses

ClinicalTrials.gov processed this record on October 02, 2014