The Effect of Intermittent Rifampicin on Raltegravir (RIFRAL)
Primary Purpose
HIV, Tuberculosis
Status
Completed
Phase
Phase 1
Locations
United Kingdom
Study Type
Interventional
Intervention
Raltegravir
Rifampicin
Raltegravir
Sponsored by
About this trial
This is an interventional treatment trial for HIV focused on measuring Healthy volunteers
Eligibility Criteria
Inclusion Criteria:
- The ability to understand and sign a written informed consent form, prior to participation in any screening procedures and must be willing to comply with all study requirements.
- ≥ 18 years
- Male or female subjects
- A female may be eligible to enter and participate in the study if she:
- Is of non-child-bearing potential defined as ether post-menopausal (12 months of spontaneous amenorrhea and ≥ 45 years of age)or physically incapable of becoming pregnant with documented tubal ligation, hysterectomy or bilateral oophorectomy or
- Is of child-bearing potential with a negative pregnancy test at screening and agrees to use one of the following methods of contraception to avoid pregnancy
- Complete abstinence from intercourse from 2 weeks prior to administration of IP, throughout the study and for at least 4 weeks after discontinuation of all study medication
- Double barrier method (male condom/spermicide, male condom/diaphragm, diaphragm/spermicide)
- Any intrauterine device (IUD) with published data showing that the expected failure rate is < 1 % per year
- Any other method with published data showing that the expected failure rate is < 1 % PER YEAR
- Hormonal contraception plus a barrier method. Hormonal contraception alone will not be considered adequate for inclusion into or participation in this study due to one of the study drugs being rifampicin.
All subjects participating in the study will be counseled on safer sexual practices including the use of effective barrier methods (e.g. male condom)
Exclusion Criteria:
- Any significant acute or chronic medical condition
- Pregnant or lactating women
- Women of childbearing age unless using non hormonal contraception
- Males who are not using contraception
- Evidence of organ dysfunction or any clinically significant deviation from normal during screening including laboratory determinations such as abnormal LFTs
- Positive blood screen for HIV-1 and 2 antibodies
- Positive blood screen for hepatitis B or C antibodies
- Positive IGRA screen for TB
- Current or recent (within 3 months) gastrointestinal disease
- Clinically relevant alcohol or drug use or history of alcohol or drug use that will hinder compliance with treatment, follow up procedures or evaluation of adverse effects
- Use of proton pump inhibitors
- Exposure to any investigational drug or placebo within 4 weeks of first dose of study drug
- Consumption of grapefruit and Seville oranges or products containing grapefruit or Seville oranges within 1 week of first study drug and for the duration of the study
- Use of any other drugs including over-the-counter medications and herbal preparations, within 2 weeks prior to first dose of study drug
- Previous allergy to any of the constituents of the pharmaceuticals in this trial
Sites / Locations
- Royal Liverpool & Broadgreen Univeristy Hospitals NHS Trust
Outcomes
Primary Outcome Measures
Change in raltegravir area under the curve (AUC) 0-12h
Secondary Outcome Measures
Number of participants with adverse events
Full Information
NCT ID
NCT01424826
First Posted
August 24, 2011
Last Updated
October 30, 2013
Sponsor
Helen Reynolds
Collaborators
Liverpool University Hospitals NHS Foundation Trust
1. Study Identification
Unique Protocol Identification Number
NCT01424826
Brief Title
The Effect of Intermittent Rifampicin on Raltegravir
Acronym
RIFRAL
Official Title
A Single Arm, 3 Phase Study to Determine the Effect of Intermittent Dosing of Rifampicin on the Pharmacokinetics of Raltegravir in Healthy Volunteers
Study Type
Interventional
2. Study Status
Record Verification Date
October 2013
Overall Recruitment Status
Completed
Study Start Date
January 2012 (undefined)
Primary Completion Date
June 2013 (Actual)
Study Completion Date
July 2013 (Actual)
3. Sponsor/Collaborators
Responsible Party, by Official Title
Sponsor-Investigator
Name of the Sponsor
Helen Reynolds
Collaborators
Liverpool University Hospitals NHS Foundation Trust
4. Oversight
Data Monitoring Committee
Yes
5. Study Description
Brief Summary
This study seeks to address the question of whether intermittent dosing of rifampicin influences the pharmacokinetics of raltegravir when co-administered. This study aims to look at what happens when rifampicin is taken 3 times a week with the standard dose and an increased dose of raltegravir. This is to find out the best dose of raltegravir to take when taking rifampicin 3 times a week. The study will be conducted in 18 healthy volunteers.
Detailed Description
The aim of this study is to optimise the dosing of raltegravir when coadministered intermittently with rifampicin. The co-administration of rifampicin and antiretrovirals (ARVs) is both complicated and problematic due to the potent induction of metabolism by rifampicin. Rifampicin induces cytochrome P450 (CYP) enzymes, which results in reduced plasma concentrations of two groups of ARVs, the protease inhibitors (PIs) and the non-nucleoside reverse transcriptase inhibitors (NNRTIs). This pharmacokinetic interaction precludes the use of PIs and severely compromises the effectiveness of the NNRTI, nevirapine, as it potentially results in the loss of antiviral activity due to sub-therapeutic concentrations which will also lead to antiretroviral resistance.
Rifampicin also induces phase II enzymes including UDP-glucuronosyl transferase. The HIV integrase inhibitor, raltegravir, is primarily metabolised by UGT1A1 and therefore, there is the potential for a pharmacokinetic drug interaction with rifampicin. In fact, previous studies have shown a decrease in raltegravir AUC, CMAX, and C12 when co-administered with daily rifampicin. During directly observed therapy (DOTs) for TB, rifampicin is often given intermittently (e.g. 3 times a week). Although several studies have examined the interaction between raltegravir and daily rifampicin, currently there are no data regarding the pharmacokinetics of raltegravir when rifampicin is co-administered intermittently.
6. Conditions and Keywords
Primary Disease or Condition Being Studied in the Trial, or the Focus of the Study
HIV, Tuberculosis
Keywords
Healthy volunteers
7. Study Design
Primary Purpose
Treatment
Study Phase
Phase 1
Interventional Study Model
Single Group Assignment
Masking
None (Open Label)
Allocation
N/A
Enrollment
18 (Actual)
8. Arms, Groups, and Interventions
Intervention Type
Drug
Intervention Name(s)
Raltegravir
Intervention Description
400 mg bd for minimum of 28 days and maximum 35 days
Intervention Type
Drug
Intervention Name(s)
Rifampicin
Intervention Description
< 50 kg 600 mg 3 times/week for a minimum of 27 days and maximum of 34 days > 50 kg 900 mg 3 times/week for a minimum of 27 days and maximum of 34 days
Intervention Type
Drug
Intervention Name(s)
Raltegravir
Intervention Description
800 mg bd for 4 days
Primary Outcome Measure Information:
Title
Change in raltegravir area under the curve (AUC) 0-12h
Time Frame
Day 28 and day 33
Secondary Outcome Measure Information:
Title
Number of participants with adverse events
Time Frame
40 days (up to + 7 days)
10. Eligibility
Sex
All
Minimum Age & Unit of Time
18 Years
Accepts Healthy Volunteers
Accepts Healthy Volunteers
Eligibility Criteria
Inclusion Criteria:
The ability to understand and sign a written informed consent form, prior to participation in any screening procedures and must be willing to comply with all study requirements.
≥ 18 years
Male or female subjects
A female may be eligible to enter and participate in the study if she:
Is of non-child-bearing potential defined as ether post-menopausal (12 months of spontaneous amenorrhea and ≥ 45 years of age)or physically incapable of becoming pregnant with documented tubal ligation, hysterectomy or bilateral oophorectomy or
Is of child-bearing potential with a negative pregnancy test at screening and agrees to use one of the following methods of contraception to avoid pregnancy
Complete abstinence from intercourse from 2 weeks prior to administration of IP, throughout the study and for at least 4 weeks after discontinuation of all study medication
Double barrier method (male condom/spermicide, male condom/diaphragm, diaphragm/spermicide)
Any intrauterine device (IUD) with published data showing that the expected failure rate is < 1 % per year
Any other method with published data showing that the expected failure rate is < 1 % PER YEAR
Hormonal contraception plus a barrier method. Hormonal contraception alone will not be considered adequate for inclusion into or participation in this study due to one of the study drugs being rifampicin.
All subjects participating in the study will be counseled on safer sexual practices including the use of effective barrier methods (e.g. male condom)
Exclusion Criteria:
Any significant acute or chronic medical condition
Pregnant or lactating women
Women of childbearing age unless using non hormonal contraception
Males who are not using contraception
Evidence of organ dysfunction or any clinically significant deviation from normal during screening including laboratory determinations such as abnormal LFTs
Positive blood screen for HIV-1 and 2 antibodies
Positive blood screen for hepatitis B or C antibodies
Positive IGRA screen for TB
Current or recent (within 3 months) gastrointestinal disease
Clinically relevant alcohol or drug use or history of alcohol or drug use that will hinder compliance with treatment, follow up procedures or evaluation of adverse effects
Use of proton pump inhibitors
Exposure to any investigational drug or placebo within 4 weeks of first dose of study drug
Consumption of grapefruit and Seville oranges or products containing grapefruit or Seville oranges within 1 week of first study drug and for the duration of the study
Use of any other drugs including over-the-counter medications and herbal preparations, within 2 weeks prior to first dose of study drug
Previous allergy to any of the constituents of the pharmaceuticals in this trial
Overall Study Officials:
First Name & Middle Initial & Last Name & Degree
Saye Khoo
Organizational Affiliation
University of Liverpool
Official's Role
Principal Investigator
Facility Information:
Facility Name
Royal Liverpool & Broadgreen Univeristy Hospitals NHS Trust
City
Liverpool
ZIP/Postal Code
L7 8XP
Country
United Kingdom
12. IPD Sharing Statement
Citations:
PubMed Identifier
25261424
Citation
Reynolds HE, Chrdle A, Egan D, Chaponda M, Else L, Chiong J, Back DJ, Khoo SH. Effect of intermittent rifampicin on the pharmacokinetics and safety of raltegravir. J Antimicrob Chemother. 2015 Feb;70(2):550-4. doi: 10.1093/jac/dku376. Epub 2014 Sep 26.
Results Reference
derived
Learn more about this trial
The Effect of Intermittent Rifampicin on Raltegravir
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