Kaletra Sex/Gender Pharmacokinetics (PK) Study (LPVGenderPK)

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details. Identifier: NCT00148759
Recruitment Status : Completed
First Posted : September 8, 2005
Results First Posted : October 22, 2013
Last Update Posted : December 3, 2013
Information provided by (Responsible Party):
Ighovwerha Ofotokun, Emory University

September 6, 2005
September 8, 2005
November 24, 2009
October 22, 2013
December 3, 2013
June 2005
January 2007   (Final data collection date for primary outcome measure)
24-hr LPV AUC [ Time Frame: 24 hours ]
Steady state(2 weeks after therapy change)
To compare the 24-hour pharmacokinetic profile of LPV following a switch from LPV/r BID to QD dosing among HIV-infected men and women
Complete list of historical versions of study NCT00148759 on Archive Site
24-hr LPV Cmax [ Time Frame: 24 hours ]
LPV Cmax at Steady State
  • a) To compare the 24-hour pharmacokinetic profile of LPV following a switch from LPV/r BID to QD dosing among HIV-infected Caucasian and African American patients.
  • b) To evaluate the tolerability of LPV/r (measured as toxicity grade of diarrhea) dosed BID compared with LPV/r dosed QD.
  • c) To evaluate changes in quality of life from baseline and 2 weeks following a switch from LPV/r BID to QD dosing
Not Provided
Not Provided
Kaletra Sex/Gender Pharmacokinetics (PK) Study
A Switch From Twice Daily to Once Daily Lopinavir/Ritonavir: A 24-hour Pharmacokinetic Profile to Evaluate Sex Differences
The levels of lopinavir achieved in the blood following oral ingestion of standard doses of Kaletra (lopinavir/ritonavir) in HIV-infected men was compared with those achieved in HIV-infected women receiving the same dose of the drug.

The association between patient sex and the tolerability of antiretroviral drugs (ARVs) is increasingly being recognized. Several lines of evidence suggest that women are more likely than men to develop side effects to ARVs. On the other hand, it has been generally accepted that the efficacies of the ARVs are similar in both sexes. However, recent studies suggest that this may not always be the case. In addition to these observed sex-related differences in the effects of ARVs, there is growing evidence that the pharmacokinetic profile of some of these drugs may be different among male and female HIV infected patients.

The fact that female sex is a risk factor for enhanced antiretroviral effects (including toxicities) has an important implication, particularly from a global health perspective as women now represent the fastest growing segment of the HIV/AIDS epidemic. Therefore, an understanding of the magnitude, clinical significance, and the mechanisms underlying this phenomenon deserves further study. Knowledge acquired from such studies will likely contribute to improved survival among female HIV-infected patients, through optimization of antiretroviral therapeutic regimens in manners that minimize serious adverse effects and improve adherence.

Similarly, the influence of race on the pharmacological effects of ARVs deserves further investigation. Although, there is no reason to believe based on available evidence that racial differences exist in the pharmacological effects of ARVs, the need however exists to explore the influence of race on ARVs pharmacokinetics and treatment outcomes. This is so because data on race related differences on ARV effects is limited, and in addition, people of ethnic minority have been disproportionately under represented in clinical trials involving these drugs in spite of the fact that they bear a larger burden of the HIV epidemic.

Our study will examine the influence of race and sex on the 24-hr pharmacokinetics of lopinavir/ritonavir (an antiretroviral agent commonly used in naïve patients) following a switch from LPV/r 400/100 mg twice daily to 800/200 mg once daily dosing. Tolerability (measured by toxicity grade of diarrhea) and change in quality of life following switch from twice daily to once daily dosing will also be assessed using appropriate validated measurement tools.

Phase 4
Allocation: Non-Randomized
Intervention Model: Parallel Assignment
Masking: None (Open Label)
Primary Purpose: Treatment
HIV Infections
Drug: LPV/r
LPV/r 800/200 mg once daily
Other Names:
  • Daily LPV/r
  • Kaletra
  • Active Comparator: adult male subjects
    LPV/r 800/200 mg once daily
    Intervention: Drug: LPV/r
  • Experimental: Adult female subjects
    LPV/r 800/200 mg once daily
    Intervention: Drug: LPV/r
Ofotokun I, Chuck SK, Binongo JN, Palau M, Lennox JL, Acosta EP. Lopinavir/Ritonavir pharmacokinetic profile: impact of sex and other covariates following a change from twice-daily to once-daily therapy. J Clin Pharmacol. 2007 Aug;47(8):970-7. Epub 2007 Jul 5.

*   Includes publications given by the data provider as well as publications identified by Identifier (NCT Number) in Medline.
January 2007
January 2007   (Final data collection date for primary outcome measure)

Inclusion Criteria:

  • Age greater or equal to 18 years
  • Diagnosis of HIV infection as previously established by HIV Enzyme-Linked Immunosorbent Assay (ELISA) test and confirmed by Western blot analysis.
  • Must have been taking LPV/r as part of an antiretroviral regimen at a dose of 400/100 mg orally twice per day for at least 3 months.
  • Recent (within last 90 days) HIV-RNA copies must be less than 400 copies/ml

Exclusion Criteria:

  • Hepatic abnormality: alanine-aminotransferase (ALT), aspartate-aminotransferase (AST) or total bilirubin (TBR) ≥ 3 x upper limit of normal
  • Renal insufficiency: serum creatinine ≥ 2 mg/dl
  • Co-infection with hepatitis B and/or C viruses
  • Pregnant or breastfeeding
  • Use of concurrent medications known to affect lopinavir or ritonavir concentrations significantly.
Sexes Eligible for Study: All
18 Years and older   (Adult, Senior)
Contact information is only displayed when the study is recruiting subjects
United States
UPN 04092824 ( Other Grant/Funding Number: Abbott Virology )
GCRC0605G ( Other Identifier: Other )
Not Provided
Not Provided
Ighovwerha Ofotokun, Emory University
Emory University
Principal Investigator: Igho Ofotokun, MD, MSc Emory University
Emory University
November 2013

ICMJE     Data element required by the International Committee of Medical Journal Editors and the World Health Organization ICTRP