Influence of Drug Transporter Expression on the Pharmacokinetics of the HIV Protease Inhibitor Kaletra
Information source: University of Heidelberg
Information obtained from ClinicalTrials.gov on November 03, 2008
Link to the current ClinicalTrials.gov record.
Condition(s) targeted: Healthy; Pharmacokinetics
Phase: Phase 1
Status: Recruiting
Sponsored by: University of Heidelberg Official(s) and/or principal investigator(s):
Gerd Mikus, MD, BSc, Principal Investigator, Affiliation: Department of Internal Medicine VI
Overall contact:
Brigitte Tubach, RN, Email: brigitte.tubach@med.uni-heidelberg.de
Summary
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).
Clinical Details
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
Study design: Screening, Cross-Sectional, Defined Population, Prospective Study
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 â blood cell concentration-relationship
- establish free and total plasma â saliva concentration-relationship
- establish blood cell concentration â drug transporter expression-relationship
Eligibility
Minimum age: 18 Years.
Maximum age: 50 Years.
Gender(s): Both.
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
Locations and Contacts
Brigitte Tubach, RN, Email: brigitte.tubach@med.uni-heidelberg.de
Clinical Research Center, Department of Internal Medicine VI, Heidelberg 69120, Germany; Recruiting
Brigitte Tubach, RN, Email: brigitte.tubach@med.uni-heidelberg.de
Additional Information
Starting date: January 2005
Last updated: March 12, 2007
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