Pharmacokinetic Study on Raltegravir and Lamotrigine (GRANOLA)
Primary Purpose
HIV Infection
Status
Completed
Phase
Phase 1
Locations
Netherlands
Study Type
Interventional
Intervention
lamotrigine
Raltegravir
Sponsored by

About this trial
This is an interventional treatment trial for HIV Infection focused on measuring interactions, neuropathic pain, pharmacokinetics
Eligibility Criteria
Inclusion Criteria:
- Between 18 and 55 years of age
- Subject does not smoke more than 10 cigarettes, 2 cigars or 2 pipes per day
- Subject has a Quetelet Index of 18 to 30 kg/m2
- Subject is able and willing to sign informed consent
- Subject is in good age-appropriate health condition
- Subject has a normal blood pressure and pulse rate
Exclusion Criteria:
- History of sensitivity/idiosyncrasy to medicinal products or excipients
- Positive HIV test
- Positive hepatitis B or C test
- Therapy with any drug (2 weeks preceding dosing) except for paracetamol
- Relevant history or presence of pulmonary disorders, cardiovascular
- History of or current abuse of drugs, alcohol or solvents
- Inability to understand the nature and extent of the trial and procedures
- Participation in a drug trial within 60 days prior to the first dose
- Donation of blood within 60 days prior to the first dose
- Febrile illness within 3 days before the first dose
Sites / Locations
- Radboud University Medical Center
Arms of the Study
Arm 1
Arm 2
Arm Type
Experimental
Active Comparator
Arm Label
A
B
Arm Description
Group A: day 1-5 Raltegravir 400 mg oral BD (twice daily). Lamotrigine one oral dose 100 mg on day 4. Wash-out 6-31. Followed by one oral dose Lamotrigine 100 mg on day 34. 5 days Raltegravir 400 mg oral BD. Lamotrigine one oral dose 100mg on day 34.
Group B: day 4 Lamotrigine one oral dose on day 4. Wash-out day 6-28 followed by Raltegravir 400 mg oral BD day 29-33. One dose Lamotrigine 100 mg oral on day 32. One dose Lamotrigine 100 mg oral.
Outcomes
Primary Outcome Measures
Plasma concentrations of lamotrigine, lamotrigine-2N-glucuronide, and raltregravir
Secondary Outcome Measures
Determination of pharmacokinetic parameters (AUC, Cmax, Tmax, Cmin and T 1/2) by noncompartmental analysis
Full Information
NCT ID
NCT00618241
First Posted
February 5, 2008
Last Updated
October 16, 2020
Sponsor
Radboud University Medical Center
Collaborators
Merck Sharp & Dohme LLC
1. Study Identification
Unique Protocol Identification Number
NCT00618241
Brief Title
Pharmacokinetic Study on Raltegravir and Lamotrigine
Acronym
GRANOLA
Official Title
The Influence of Raltegravir (MK-0518) on the Pharmacokinetics of Single-dose Lamotrigine in Healthy Male Subjects (GRANOLA)
Study Type
Interventional
2. Study Status
Record Verification Date
May 2011
Overall Recruitment Status
Completed
Study Start Date
February 2008 (undefined)
Primary Completion Date
October 2008 (Actual)
Study Completion Date
October 2008 (Actual)
3. Sponsor/Collaborators
Name of the Sponsor
Radboud University Medical Center
Collaborators
Merck Sharp & Dohme LLC
4. Oversight
Data Monitoring Committee
No
5. Study Description
Brief Summary
The purpose of this study is to determine whether interactions between raltegravir and lamotrigine take place and to study the safety of the combination raltegravir/lamotrigine before used in HIV patients.
Detailed Description
Lamotrigine is an anticonvulsive drug that is used both for the treatment of HIV-associated neuropathic pain and the treatment of epilepsy in HIV-infected individuals. Lamotrigine is metabolized via glucuronidation.
Raltegravir is a newly developed integrase inhibitor that is also metabolized via glucuronidation.
Since both agents are metabolized via glucuronidation, there is a possibility of competition for glucuronidation, leading to drug-drug interactions between raltegravir and lamotrigine.
This primary objective of this study is to determine the effect of raltegravir on the pharmacokinetics of single dose lamotrigine (by intrasubject comparison). A secondary objective is to determine the effect of single dose lamotrigine on the pharmacokinetics of raltegravir when compared to historical controls. Another secondary objective is to evaluate the safety of combined use of single dose lamotrigine and raltegravir.
6. Conditions and Keywords
Primary Disease or Condition Being Studied in the Trial, or the Focus of the Study
HIV Infection
Keywords
interactions, neuropathic pain, pharmacokinetics
7. Study Design
Primary Purpose
Treatment
Study Phase
Phase 1
Interventional Study Model
Crossover Assignment
Masking
None (Open Label)
Allocation
Randomized
Enrollment
24 (Actual)
8. Arms, Groups, and Interventions
Arm Title
A
Arm Type
Experimental
Arm Description
Group A: day 1-5 Raltegravir 400 mg oral BD (twice daily). Lamotrigine one oral dose 100 mg on day 4. Wash-out 6-31. Followed by one oral dose Lamotrigine 100 mg on day 34.
5 days Raltegravir 400 mg oral BD. Lamotrigine one oral dose 100mg on day 34.
Arm Title
B
Arm Type
Active Comparator
Arm Description
Group B: day 4 Lamotrigine one oral dose on day 4. Wash-out day 6-28 followed by Raltegravir 400 mg oral BD day 29-33. One dose Lamotrigine 100 mg oral on day 32.
One dose Lamotrigine 100 mg oral.
Intervention Type
Drug
Intervention Name(s)
lamotrigine
Other Intervention Name(s)
Lamictal
Intervention Description
100 mg
Intervention Type
Drug
Intervention Name(s)
Raltegravir
Intervention Description
400 mg BD
Primary Outcome Measure Information:
Title
Plasma concentrations of lamotrigine, lamotrigine-2N-glucuronide, and raltregravir
Time Frame
just before dosing, at 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 24 hours and 48 hours after dosing on study days 4-5 and 32-33.
Secondary Outcome Measure Information:
Title
Determination of pharmacokinetic parameters (AUC, Cmax, Tmax, Cmin and T 1/2) by noncompartmental analysis
Time Frame
at each sampling time
10. Eligibility
Sex
Male
Minimum Age & Unit of Time
18 Years
Maximum Age & Unit of Time
55 Years
Accepts Healthy Volunteers
Accepts Healthy Volunteers
Eligibility Criteria
Inclusion Criteria:
Between 18 and 55 years of age
Subject does not smoke more than 10 cigarettes, 2 cigars or 2 pipes per day
Subject has a Quetelet Index of 18 to 30 kg/m2
Subject is able and willing to sign informed consent
Subject is in good age-appropriate health condition
Subject has a normal blood pressure and pulse rate
Exclusion Criteria:
History of sensitivity/idiosyncrasy to medicinal products or excipients
Positive HIV test
Positive hepatitis B or C test
Therapy with any drug (2 weeks preceding dosing) except for paracetamol
Relevant history or presence of pulmonary disorders, cardiovascular
History of or current abuse of drugs, alcohol or solvents
Inability to understand the nature and extent of the trial and procedures
Participation in a drug trial within 60 days prior to the first dose
Donation of blood within 60 days prior to the first dose
Febrile illness within 3 days before the first dose
Overall Study Officials:
First Name & Middle Initial & Last Name & Degree
David M. Burger, PharmD PhD
Organizational Affiliation
Radboud University Medical Center
Official's Role
Principal Investigator
Facility Information:
Facility Name
Radboud University Medical Center
City
Nijmegen
State/Province
Gelderland
Country
Netherlands
12. IPD Sharing Statement
Citations:
PubMed Identifier
19717722
Citation
van Luin M, Colbers A, Verwey-van Wissen CP, van Ewijk-Beneken-Kolmer EW, van der Kolk M, Hoitsma A, da Silva HG, Burger DM. The effect of raltegravir on the glucuronidation of lamotrigine. J Clin Pharmacol. 2009 Oct;49(10):1220-7. doi: 10.1177/0091270009345689. Epub 2009 Aug 28.
Results Reference
result
Links:
URL
https://pubmed.ncbi.nlm.nih.gov/19717722/
Description
Results published in The Journal of Clinical Pharmacology; 2009; 49; 1220
Learn more about this trial
Pharmacokinetic Study on Raltegravir and Lamotrigine
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