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

Primary Purpose

HIV Infections

Status
Completed
Phase
Phase 4
Locations
Spain
Study Type
Interventional
Intervention
Raltegravir
Sponsored by
Germans Trias i Pujol Hospital
About
Eligibility
Locations
Arms
Outcomes
Full info

About this trial

This is an interventional treatment trial for HIV Infections focused on measuring Raltegravir, intracellular concentration, plasmatic concentration, HIV, Treatment experienced

Eligibility Criteria

18 Years - 65 Years (Adult, Older Adult)All SexesDoes not accept healthy volunteers

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.

Sites / Locations

  • Hospital Germans Trias i Pujol
  • Hospital de la Santa Creu i Sant Pau

Arms of the Study

Arm 1

Arm Type

Experimental

Arm Label

Raltegravir 800 mg / 24 hours

Arm Description

Raltegravir 800 mg / 24 hours

Outcomes

Primary Outcome Measures

Plasmatic and intracellular concentration of raltegravir

Secondary Outcome Measures

Clearance, CL/F
Volume of distribution, V/F
Elimination half-life, t1/2
Area under the plasma concentration-time curve during the dosing interval AUC0-24
Maximum concentration
Time to maximum concentration, Tmax
Minimum concentration

Full Information

First Posted
October 7, 2009
Last Updated
December 3, 2019
Sponsor
Germans Trias i Pujol Hospital
Collaborators
Fundación FLS de Lucha Contra el Sida, las Enfermedades Infecciosas y la Promoción de la Salud y la Ciencia
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1. Study Identification

Unique Protocol Identification Number
NCT00995241
Brief Title
Pilot Study to Compare the Pharmacokinetics Parameters in Plasma and Intracellular of Raltegravir Administered Once a Day in Adult Patients Infected With HIV
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
Study Type
Interventional

2. Study Status

Record Verification Date
December 2019
Overall Recruitment Status
Completed
Study Start Date
November 2009 (undefined)
Primary Completion Date
December 2009 (Actual)
Study Completion Date
December 2009 (Actual)

3. Sponsor/Collaborators

Responsible Party, by Official Title
Sponsor
Name of the Sponsor
Germans Trias i Pujol Hospital
Collaborators
Fundación FLS de Lucha Contra el Sida, las Enfermedades Infecciosas y la Promoción de la Salud y la Ciencia

4. Oversight

Data Monitoring Committee
No

5. Study Description

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

6. Conditions and Keywords

Primary Disease or Condition Being Studied in the Trial, or the Focus of the Study
HIV Infections
Keywords
Raltegravir, intracellular concentration, plasmatic concentration, HIV, Treatment experienced

7. Study Design

Primary Purpose
Treatment
Study Phase
Phase 4
Interventional Study Model
Single Group Assignment
Masking
None (Open Label)
Allocation
N/A
Enrollment
5 (Actual)

8. Arms, Groups, and Interventions

Arm Title
Raltegravir 800 mg / 24 hours
Arm Type
Experimental
Arm Description
Raltegravir 800 mg / 24 hours
Intervention Type
Drug
Intervention Name(s)
Raltegravir
Other Intervention Name(s)
N/P
Intervention Description
Raltegravir 800 mg / 24 hours.
Primary Outcome Measure Information:
Title
Plasmatic and intracellular concentration of raltegravir
Time Frame
10 days
Secondary Outcome Measure Information:
Title
Clearance, CL/F
Time Frame
10 days
Title
Volume of distribution, V/F
Time Frame
10 days
Title
Elimination half-life, t1/2
Time Frame
10 days
Title
Area under the plasma concentration-time curve during the dosing interval AUC0-24
Time Frame
10 days
Title
Maximum concentration
Time Frame
10 days
Title
Time to maximum concentration, Tmax
Time Frame
10 days
Title
Minimum concentration
Time Frame
10 days

10. Eligibility

Sex
All
Minimum Age & Unit of Time
18 Years
Maximum Age & Unit of Time
65 Years
Accepts Healthy Volunteers
No
Eligibility Criteria
Inclusion Criteria: Age > 18 years. HIV documented infection. Stable antiretroviral treatment for at least 4 weeks. HIV viral load in plasma <50 copies / mL for at least 12 weeks Voluntary written informed consent. Exclusion Criteria: AIDS-defining illness in the previous 4 weeks Suspicion of inadequate adherence to antiretroviral therapy In the case of women, pregnant or breastfeeding, or non-use of contraceptives History or suspicion of failure to cooperate adequately 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.
Overall Study Officials:
First Name & Middle Initial & Last Name & Degree
Jose Molto, MD,PhD
Organizational Affiliation
Germans Trias i Pujol Hospital
Official's Role
Principal Investigator
First Name & Middle Initial & Last Name & Degree
Marta Valle, MD,PhD
Organizational Affiliation
Fundació Institut de Recerca de l'Hospital de la Santa Creu i Sant Pau
Official's Role
Principal Investigator
Facility Information:
Facility Name
Hospital Germans Trias i Pujol
City
Badalona
State/Province
Barcelona
ZIP/Postal Code
08916
Country
Spain
Facility Name
Hospital de la Santa Creu i Sant Pau
City
Barcelona
ZIP/Postal Code
08025
Country
Spain

12. IPD Sharing Statement

Learn more about this trial

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

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