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

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).

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Key information

Conditions

Healthy Blood-Borne Infections Communicable Diseases Genital Diseases HIV Infections Immune System Diseases Immunologic Deficiency Syndromes Infections Lentivirus Infections Pharmacokinetics RNA Virus Infections Retroviridae Infections Sexually Transmitted Diseases Sexually Transmitted Diseases, Viral Urogenital Diseases Virus Diseases

Age range

18 year–50 year

Sex eligibility

All sexes

Study type

Observational

Primary location

Clinical Research Center, Department of Internal Medicine VI

Heidelberg, 69120, Germany

About this study

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

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

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

Sponsors and collaborators

Lead sponsor

Heidelberg University

Other

Registry information

Official study 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

Important dates

Study start: 2005
First posted: Sep 15, 2005
Registry last updated: Feb 13, 2009

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

Published trials that share one or more normalized conditions with this study.

Completed