Clinical Trials


Pilot Study to Compare the Pharmacokinetics Parameters in Plasma and Intracellular of Raltegravir Administered Once a Day in Adult Patients Infected With HIV

This study has been completed
Germans Trias i Pujol Hospital

Fundacio Lluita Contra la SIDA

Information provided by (Responsible Party)
Germans Trias i Pujol Hospital Identifier

First received: October 7, 2009
Last updated: December 3, 2019
Last Verified: December 2019
History of Changes


The purpose of this study is to compare plasma and intracellular pharmacokinetic parameters of raltegravir 800 mg administered once daily in HIV infected patients.

Condition Intervention Phase
HIV Infections

Drug : Raltegravir
Phase 4

Study Type: Interventional
Study Design: Allocation: N/A
Intervention Model: Single Group Assignment
Masking: None (Open Label)
Primary Purpose: Treatment
Official Title: Pilot Study to Compare the Pharmacokinetics Parameters in Plasma and Intracellular of Raltegravir Administered Once a Day in Adult Patients Infected With HIV

Further study details as provided by Germans Trias i Pujol Hospital:

Primary Outcome Measures

  • Plasmatic and intracellular concentration of raltegravir [ Time Frame: 10 days ]
Secondary Outcome Measures:
  • Clearance, CL/F [ Time Frame: 10 days ]
  • Volume of distribution, V/F [ Time Frame: 10 days ]
  • Elimination half-life, t1/2 [ Time Frame: 10 days ]
  • Area under the plasma concentration-time curve during the dosing interval AUC0-24 [ Time Frame: 10 days ]
  • Maximum concentration [ Time Frame: 10 days ]
  • Time to maximum concentration, Tmax [ Time Frame: 10 days ]
  • Minimum concentration [ Time Frame: 10 days ]

Enrollment: 5
Study Start Date: November 2009
Study Completion Date: December 2009
Primary Completion Date: December 2009 (Final data collection date for primary outcome measure)

Arms Assigned Interventions
Experimental: Raltegravir 800 mg / 24 hours
Raltegravir 800 mg / 24 hours
Drug: Raltegravir

Raltegravir 800 mg / 24 hours.

Other Name: N/P

Detailed Description:

HIV integrase is the enzyme responsible for transferring the DNA encoded by HIV to host chromosomes, a necessary step for the replication of retroviruses. Raltegravir (RAL) is the first integrase inhibitor approved for HIV treatment of patients infected by this virus. RAL has demonstrated a marked antiretroviral activity against HIV strains resistant to other antiretroviral drug families and high virological efficacy in patients pre-treated so as naïve to antiretroviral treatment. In addition, its safety profile is very favourable.
Unlike what happens with other antiretrovirals such as protease inhibitors, there is not a relationship between the virological response to antiretroviral treatment with RAL and the trough concentration of drug in plasma. Similarly, in vitro studies have shown that, after infection of cultured cells, the rate of viral replication measured by p24 antigen production was continuing inhibited even when RAL was washed from the culture medium from the 8 hours after infection, suggesting the possibility of a post-antibiotic effect of the drug. Either way, as in the case of transcriptase inhibitor nucleoside analogues, this lack of correlation between pharmacokinetics and pharmacodynamics of RAL may only be the result of intracellular accumulation of drug in blood lymphocytes peripheral, which in turn could be explained either by setting the RAL to the pre-integration complex or through the saturation of certain cellular transporters responsible for pumping the RAL from the inside out-cell (efflux transporters). Anyway, the result would be a greater RAL intracellular half-life than plasmatic, which would translate into a clinically persistent antiretroviral effect compared with its concentration in plasma.
Based on the above is possible to suggest that the average life of RAL was longer in the peripheral blood lymphocytes than in plasma, and that this intracellular increased half-life could explain the absence of relationship between trough RAL concentration and its virological efficacy, post-antibiotic effect of RAL found in some studies in vitro which, on the other hand, could be relevant to the possible once-daily administration of raltegravir.



Ages Eligible for Study: 18 Years to 65 Years  
Sexes Eligible for Study: All  
Accepts Healthy Volunteers: No  


Inclusion Criteria:

    1. Age > 18 years.
    2. HIV documented infection.
    3. Stable antiretroviral treatment for at least 4 weeks.
    4. HIV viral load in plasma <50 copies / mL for at least 12 weeks
    5. Voluntary written informed consent.

Exclusion Criteria:
    1. AIDS-defining illness in the previous 4 weeks
    2. Suspicion of inadequate adherence to antiretroviral therapy
    3. In the case of women, pregnant or breastfeeding, or non-use of contraceptives
    4. History or suspicion of failure to cooperate adequately
    5. Concomitant therapy in the two weeks prior to inclusion in the study with atazanavir,
    tenofovir, NNRTI, rifampicin, inhibitors of proton pump or other drugs with known interactions with raltegravir.

contacts and locations

Contacts and Locations

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Please refer to this study by its identifier: NCT00995241


Hospital Germans Trias i Pujol
Badalona, Barcelona, Spain, 08916
Hospital de la Santa Creu i Sant Pau
Barcelona, Spain, 08025

Sponsors and Collaborators

Germans Trias i Pujol Hospital
Fundacio Lluita Contra la SIDA


Principal Investigator: Jose Molto, MD,PhD Germans Trias i Pujol Hospital
Principal Investigator: Marta Valle, MD,PhD Fundació Institut de Recerca de l'Hospital de la Santa Creu i Sant Pau
More Information

More Information

Responsible Party: Germans Trias i Pujol Hospital Identifier: NCT00995241   History of Changes  
Other Study ID Numbers: RAL-IC  
Study First Received: October 7, 2009  
Last Updated: December 3, 2019  

Keywords provided by Germans Trias i Pujol Hospital:

intracellular concentration
plasmatic concentration
Treatment experienced

Additional relevant MeSH terms:
HIV Infections
Raltegravir Potassium processed this data on May 28, 2020
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