Effect of Antacids on the Pharmacokinetics of Raltegravir

Effect of Antacids on the Pharmacokinetics of Raltegravir in Healthy Volunteers

The purpose of this study is to test whether there is a drug interaction between raltegravir (a medicine used to treat the human immunodeficiency virus or HIV) and antacids.

Study Overview

• Status: Completed
• Conditions: HIV Infections
• Intervention / Treatment: Drug: raltegravir; Drug: antacid

Detailed Description

This study will determine if an interaction occurs between the HIV medicine raltegravir and an antacid. A prior study found an interaction with another medicine like raltegravir called elvitegravir and an antacid. The elvitegravir levels were reduced by half. The same interaction may occur with raltegravir and an antacid based on the structure of this medicine and how it works. When the levels of HIV medications are reduced, people with HIV can "fail" their treatment. The virus can multiply when the drug levels are too low and the medications can stop working. We need to be sure that antacids will not cause this problem with raltegravir.

• Study Type: Interventional
• Enrollment (Actual): 17
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Colorado
    • Aurora, Colorado, United States, 80045
      • University of Colorado Denver

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 60 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Absence of HIV-1 infection as documented by any licensed ELISA test kit within 21 days prior to study entry.
• Age greater than or equal to 18 but less than or equal to 60 years.
• Ability and willingness to give written informed consent.
• Within 30% (+/-) of ideal body weight and total body weight of ≥ 50 kg.
• Hematology, Metabolic Profile, Renal, and Hepatic Function tests all within normal limits.
• Creatine kinase (CK) less than 3 times the upper limit of normal

Exclusion Criteria:

• Pregnancy or breast-feeding.
• Women and men of reproductive potential who are actively engaging in sexual activity or assisted reproductive technology with the intent of pregnancy.
• Allergy/sensitivity to raltegravir.
• Allergy/sensitivity to antacids.
• Active drug or alcohol abuse or dependence that, in the opinion of the investigator, would interfere with adherence to study requirements. While on study, subjects will be instructed not to consume alcohol for 48 hours prior the screening visit, and for the 24 hours preceding the intensive pharmacokinetic (PK) study visits and for 24 hours following the completion of the study visits.
• Any medical condition that, in the opinion of the investigator, would interfere with the subject's ability to participate in this protocol.
• Participation in any investigational drug studies within 30 days prior to study entry.
• History of or active cardiovascular, renal, hematologic, hepatic, neurologic, gastrointestinal, psychiatric, endocrine, or immunologic disease(s). This is inclusive of chronic illnesses such as hypertension, coronary artery disease, arthritis, diabetes, any chronic gastrointestinal conditions that might interfere with drug absorption.
• Use of investigational, prescription, and over-the-counter medications within 14 days of study entry with the following exceptions: aspirin, acetaminophen, ibuprofen, and oral contraceptives

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Active Comparator: raltegravir alone; Subjects will receive a single dose of 400 mg raltegravir orally	Drug: raltegravir; raltegravir 400mg orally once; Other Names: Isentress
Experimental: raltegravir plus antacid; Subjects will receive a single dose of 400mg raltegravir orally simultaneously with an antacid	Drug: raltegravir; raltegravir 400mg orally once; Other Names: Isentress; Drug: antacid; aluminum, magnesium, simethicone-containing antacid 30mL orally once; Other Names: Isentress, Maalox Plus Extra Strength

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Raltegravir AUC with and without an antacid	0-48 hours

Secondary Outcome Measures

Outcome Measure	Time Frame
Raltegravir Cmax with and without an antacid	0-48 hours

Collaborators and Investigators

• Sponsor: University of Colorado, Denver

Study record dates

Study Major Dates

• Study Start: July 1, 2009
• Primary Completion (Actual): December 1, 2009
• Study Completion (Actual): December 1, 2009

Study Registration Dates

• First Submitted: July 20, 2009
• First Submitted That Met QC Criteria: July 21, 2009
• First Posted (Estimate): July 23, 2009

Study Record Updates

• Last Update Posted (Actual): June 28, 2017
• Last Update Submitted That Met QC Criteria: June 26, 2017
• Last Verified: June 1, 2017

More Information

Terms related to this study

• Keywords: HIV; drug interaction; antiretroviral; human immunodeficiency virus
• Additional Relevant MeSH Terms: RNA Virus Infections; Virus Diseases; Infections; Blood-Borne Infections; Communicable Diseases; Sexually Transmitted Diseases, Viral; Sexually Transmitted Diseases; Lentivirus Infections; Retroviridae Infections; Immunologic Deficiency Syndromes; Immune System Diseases; HIV Infections; Physiological Effects of Drugs; Molecular Mechanisms of Pharmacological Action; Anti-Infective Agents; Antiviral Agents; Enzyme Inhibitors; Anti-HIV Agents; Anti-Retroviral Agents; Gastrointestinal Agents; Protective Agents; HIV Integrase Inhibitors; Integrase Inhibitors; Antioxidants; Raltegravir Potassium; TEMPO; Antacids; Aluminum hydroxide, magnesium hydroxide, simethicone drug combination
• Other Study ID Numbers: 09-0475

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: No