Phase 1
Completed N=27
A Pharmacokinetic Study to Evaluate the Effect of Antacids on Raltegravir (MK-0518) in HIV-Infected Participants (MK-0518-247)
Source: ClinicalTrials.gov NCT01622673 ↗Enrolled (actual)
27
Serious AEs
0.0%
Results posted
Sep 2013
Primary outcomePrimary: Least Squares Mean Steady State Plasma Concentration (C12hrs) of Raltegravir After Coadministration of Antacid (Primary Hypothesis) — 132.30; 89.75; 49.38 nM
Summary
This study will evaluate: (1) the effect of co-administration of single doses of calcium carbonate antacid and magnesium/aluminum hydroxide antacid on the steady-state plasma pharmacokinetic profile of raltegravir in human immunodeficiency virus (HIV)-infected participants; and (2) the effect of staggered dosing of a single dose of a magnesium/aluminum hydroxide antacid 2 hours before and 2 hours after administration of raltegravir on the steady-state plasma pharmacokinetic profile of raltegravir in the same participants.
The study will determine whether (1) the C12hrs of steady-state raltegravir after co-administration of single doses of calcium carbonate antacid is decreased to a clinically meaningful degree compared with C12hrs after administration of raltegravir alone; and whether (2) the C12hrs of steady-state raltegravir after co-administration of a single dose of magnesium/aluminum hydroxide antacid is decreased to a clinically meaningful degree compared with the C12hrs after administration of raltegravir alone.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Least Squares Mean Steady State Plasma Concentration (C12hrs) of Raltegravir After Coadministration of Antacid (Primary Hypothesis) |
132.30; 89.75; 49.38 | — |
| PRIMARY Least Squares Mean Steady State Plasma Concentration (C12hrs) of Raltegravir After Staggered Administration of Antacid (Secondary Hypothesis) |
125.75; 54.92; 54.47 | — |
| PRIMARY Least Squares Mean Steady State Area Under the Plasma Concentration-time Curve (AUC0-12hrs) of Raltegravir After Coadministration of Antacid (Primary Hypothesis) |
16399.76; 7294.30; 8358.67 | — |
| PRIMARY Least Squares Mean Steady State Area Under the Plasma Concentration-Time (AUC0-12hrs) of Raltegravir After Staggered Administration of Antacid (Secondary Hypothesis) |
17577.15; 8521.95; 12226.11 | — |
| PRIMARY Least Squares Mean Maximum Plasma Concentration (Cmax) of Raltegravir After Coadministration of Antacid (Primary Hypothesis) |
5427.15; 2584.78; 3013.88 | — |
| PRIMARY Least Squares Mean Maximum Plasma Concentration (Cmax) of Raltegravir After Staggered Administration of Antacid (Secondary Hypothesis) |
5678.90; 2753.64; 4399.66 | — |
| PRIMARY Mean Time to Maximum Plasma Concentration (Tmax) of Raltegravir |
2.06; 2.08; 1.48; 1.52; 1.78 | — |
| PRIMARY Number of Participants With Any Clinical or Laboratory Adverse Event (AE) |
1; 2; 2; 2; 1 | — |
Eligibility Criteria
Inclusion Criteria
- HIV-infected participant on a stable raltegravir dose (400 mg every 12 hours) as part of a stable anti-retroviral regimen (ARV) for at least 1 month and will maintain current ARV therapy throughout the study
- Body Mass Index ≤32 kg/m^2
- Good general health
- Can be a current smoker and/or user of nicotine or nicotine-containing products, but use of nicotine-containing products will not be permitted during the stay at the clinical research site
Exclusion Criteria
- History of gastric bypass surgery
- Pregnant or nursing
- Mentally or legally incapacitated, has significant emotional problems, or has a history of a clinically significant psychiatric disorder; participants who have had situational depression may be enrolled at the discretion of the investigator.
- History of stroke, chronic seizures, or major neurological disorder
- History of clinically significant endocrine, gastrointestinal, cardiovascular, hematological, hepatic, immunological, renal, respiratory, or genitourinary abnormalities or diseases (excluding HIV); participants with a history of uncomplicated kidney stones or childhood asthma may be enrolled at the discretion of the investigator.
- Active neoplastic disease deemed unstable or progressing by the investigator
- Currently taking rifampin or unable to refrain from use of any proton pump inhibitor and any histamine-2 (H2)-blockers, over-the-counter antacids, calcium supplements, or multivitamins during the study
- Consumes excessive amounts of alcohol
- Consumes excessive amounts of coffee, tea, cola, or other caffeinated beverages
- Major surgery or blood donation within the past 4 weeks
- History of significant multiple and/or severe allergies or has had an anaphylactic reaction or significant intolerability to prescription or non-prescription drugs or food
- Regular user of any illicit drugs or history of drug (including alcohol) abuse within the past 6 months; current methadone or suboxone use is allowed.
Data sourced from ClinicalTrials.gov (NCT01622673). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.