Pharmacokinetics Distribution of Raltegravir by PET/MR

Pharmacokinetics Distribution of Raltegravir Using Radiolabeling in HIV-infected Patients by PET/MR: a Pilot Study.

This is a single-center drug distribution and pharmacokinetic study of a single microdose of 18F-raltegravir given to 10 HIV-infected subjects who are either taking or not taking a raltegravir-containing ART regimen. After administration of IV 18F-raltegravir, subjects will undergo PET/MRI in order to determine the distribution of radiolabeled drug through the lymphoreticular system and other tissues throughout the entire body.

Study Overview

• Status: Recruiting
• Conditions: HIV-1-infection
• Intervention / Treatment: Drug: 18F-Raltegravir

• Study Type: Interventional
• Enrollment (Estimated): 10
• Phase: Early Phase 1

Contacts and Locations

• Study Contact: Name: Timothy J Henrich, MD; Phone Number: 415-206-5518; Email: timothy.henrich@ucsf.edu

Study Locations

• United States
  • California
    • San Francisco, California, United States, 94110
      • Recruiting
      • University of California, San Francisco
      • Sub-Investigator: Francesca Aweeka, PharmD
      • Contact: Timothy J Henrich, MD; Phone Number: 415-206-5518; Email: timothy.henrich@ucsf.edu
      • Principal Investigator: Timothy J Henrich, MD
      • Sub-Investigator: Henry F Vanbrocklin, PhD
      • Sub-Investigator: Steven J Deeks, MD
      • Sub-Investigator: Benajamin Franc, MD

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years and older (Adult, Older Adult)
• Accepts Healthy Volunteers: No

Description

Inclusion Criteria:

• Age ≥18 years
• HIV infection
• Initiated a combination ART (HAART) regimen

Exclusion Criteria:

• Screening absolute neutrophil count <1,000 cells/mm3, platelet count <70,000 cells/mm3, hemoglobin < 8 mg/dL, estimated creatinine clearance <40 mL/minute, aspartate aminotransferase >100 units/L, alanine aminotransferase >100 units/L.
• Serious illness requiring hospitalization or parental antibiotics within the preceding 3 months.
• Any vaccination 2 weeks prior to baseline (Day 0) visit and throughout the study period.
• Concurrent treatment with immunomodulatory drugs, or exposure to any immunomodulatory drug in the preceding 16 weeks (e.g. corticosteroid therapy equal to or exceeding a dose of 15 mg/day of prednisone for more than 10 days, IL-2, interferon-alpha, methotrexate, cancer chemotherapy). NOTE: Use of inhaled or nasal steroid use is not exclusionary.
• Pregnant or breastfeeding women. Females of childbearing potential must have a negative serum pregnancy test at screening and agree to use a double-barrier method of contraception throughout the study period.
• Have a cardiac pacemaker or other indwelling foreign object that are contraindicated for MR imaging.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Other
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: 18F-Raltegravir	Drug: 18F-Raltegravir; A single microdose of 18F-Raltegravir will be given to individuals currently being treated for HIV-1 with antiretroviral therapy.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Number of patients with microdose (<2.5 millicurie; mCi) 18F-Raltegravir-related adverse events as measured by clinical observation during single intravenous dose administration and PET/MR imaging	One imaging session within 1 to 6 hours following administration of 18F-Raltegravir
Whole-body distribution (coronal through pelvis) of radiolabeled 18F-Raltegravir as determined by PET-MR scanning and quantification of radiographic regions of interest (ROI) immediately following and up to 4 hours after drug administration.	One imaging session within 1 to 6 hours following administration of 18F-Raltegravir

Collaborators and Investigators

• Sponsor: University of California, San Francisco
• Collaborators: Merck Sharp & Dohme LLC
• Investigators: Principal Investigator: Timothy J Henrich, MD, University of California, San Francisco

Study record dates

Study Major Dates

• Study Start (Actual): April 1, 2018
• Primary Completion (Estimated): November 1, 2024
• Study Completion (Estimated): January 1, 2025

Study Registration Dates

• First Submitted: March 3, 2017
• First Submitted That Met QC Criteria: May 31, 2017
• First Posted (Actual): June 5, 2017

Study Record Updates

• Last Update Posted (Actual): June 18, 2024
• Last Update Submitted That Met QC Criteria: June 14, 2024
• Last Verified: June 1, 2024

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Molecular Mechanisms of Pharmacological Action; Anti-Infective Agents; Antiviral Agents; Enzyme Inhibitors; Anti-HIV Agents; Anti-Retroviral Agents; HIV Integrase Inhibitors; Integrase Inhibitors; Raltegravir Potassium
• Other Study ID Numbers: 15-17586

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