Determine Central 5-HT1B Receptor Occupancy of ZOMIG® Rapimelt (Zolmitriptan) in Healthy Male Volunteers

Overview

The purpose of this study is to determine the central 5-HT1B receptor occupancy of ZOMIG® Rapimelt (zolmitriptan) in healthy male volunteers.

Full Title of Study: “An Open Label, Positron Emission Tomography (PET) Study With [11C]AZ10419369 to Determine Central 5-HT1B Receptor Occupancy of ZOMIG® Rapimelt (Zolmitriptan) in Healthy Male Volunteers”

Study Type

  • Study Type: Interventional
  • Study Design
    • Allocation: Non-Randomized
    • Intervention Model: Single Group Assignment
    • Primary Purpose: Basic Science
    • Masking: None (Open Label)
  • Study Primary Completion Date: October 2010

Interventions

  • Drug: Rapimelt
    • oral tablet , 2.5 and 5 mg, single dose. 10 mg (2×5 mg) visit 3, 5 mg visit 4, 2.5 mg visit 5.
  • Drug: [11C]AZ10419369
    • solution for iv injection. Will be injected within 2 to 5 hours after administration of ZOMIG® Rapimelt

Arms, Groups and Cohorts

  • Experimental: 1
    • PET 1: baseline, PET 2: 10 mg Zomig® Rapimelt, PET 3: 5 mg ZOMIG® Rapimelt, PET 4 2.5 mg ZOMIG® Rapimelt

Clinical Trial Outcome Measures

Primary Measures

  • To determine zolmitriptan and/or its active metabolite 183C91 occupancy at 5-HT1B receptors in the living human brain
    • Time Frame: The first PET measurement will serve as a baseline assessment. The second, third and fourth PET measurements will be performed after oral administration of ZOMIG® Rapimelt (10 mg, 5 mg and 2.5 mg, respectively).

Secondary Measures

  • To describe the relation between Zomig® Rapimelt dose and 5-HT1B receptor occupancy
    • Time Frame: The second, third and fourth PET measurements will be performed after oral administration of ZOMIG® Rapimelt (10 mg, 5 mg and 2.5 mg, respectively). Imaging data analysis will be performed after each PET measurement
  • To describe the relation between plasma concentrations of zolmitriptan and 183C91 and 5-HT1B receptor occupancy
    • Time Frame: For each of 3 visits venous blood for zolmitriptan and 183C91 PK analyses taken before drug administration and at 3 time points during PET examination: start, middle and end, ie, at 0, +30 and + 63 minutes relative to injection of the radioli

Participating in This Clinical Trial

Inclusion Criteria

  • Body mass index between ≥19 and ≤30 kg/m2. Exclusion Criteria:

  • A history or presence of neurological, haematological, psychiatric, gastrointestinal, hepatic, pulmonary, renal disease – Use of drugs that induce the liver drug metabolising enzymes within 4 weeks before first PET

Gender Eligibility: Male

Minimum Age: 20 Years

Maximum Age: 45 Years

Are Healthy Volunteers Accepted: Accepts Healthy Volunteers

Investigator Details

  • Lead Sponsor
    • AstraZeneca
  • Provider of Information About this Clinical Study
    • MSD, AstraZeneca
  • Overall Official(s)
    • Stephen Kanes, Study Director, AstraZeneca
    • Wolfgang Kühn, Principal Investigator, Quintiles AB Phase I Services
    • Brendan Smyth, Study Chair, AstraZeneca

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