Influence of Drug Transporter Expression on the Pharmacokinetics of the HIV Protease Inhibitor Kaletra - Full Text View

Sponsored by:	University of Heidelberg
Information provided by:	University of Heidelberg
ClinicalTrials.gov Identifier:	NCT00176033

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 I

MedlinePlus related topics: AIDS

Drug Information available for: Ritonavir Lopinavir

U.S. FDA Resources

Study Type:	Observational
Study Design:	Screening, Cross-Sectional, Defined Population, Prospective Study
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

Further study details as provided by University of Heidelberg:

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

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

Contacts

Contact: Brigitte Tubach, RN

brigitte.tubach@med.uni-heidelberg.de

Locations

Germany
Clinical Research Center, Department of Internal Medicine VI	Recruiting
Heidelberg, Germany, 69120
Contact: Brigitte Tubach, RN brigitte.tubach@med.uni-heidelberg.de

Sponsors and Collaborators

University of Heidelberg

Investigators

Principal Investigator:

Gerd Mikus, MD, BSc

Department of Internal Medicine VI

More Information

Study ID Numbers:	K026
Study First Received:	September 12, 2005
Last Updated:	March 12, 2007
ClinicalTrials.gov Identifier:	NCT00176033
Health Authority:	Germany: Federal Institute for Drugs and Medical Devices

Keywords provided by University of Heidelberg:

ritonavir
lopinavir
HIV Infections

Study placed in the following topic categories:

Lopinavir
Ritonavir
HIV Infections
Acquired Immunodeficiency Syndrome
Healthy

ClinicalTrials.gov processed this record on January 16, 2009