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

NCT01085123 | Completed Phase 1

• 1 other identifier: D1220C00005
• Study Type: interventional
• Target: 10
• Locations: 1 country
• Sites: 1

Brief Summary

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

Conditions

Migraine

Keywords

Migraine; ZOMIG® Rapimelt

Outcome Measures

Primary Outcomes (1)

• To determine zolmitriptan and/or its active metabolite 183C91 occupancy at 5-HT1B receptors in the living human brain

  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 Outcomes (2)

• To describe the relation between Zomig® Rapimelt dose and 5-HT1B receptor occupancy

  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

  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

Study Arms (1)

1

EXPERIMENTAL

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

Drug: Rapimelt; Drug: [11C]AZ10419369

Interventions

Rapimelt DRUG

oral tablet , 2.5 and 5 mg, single dose. 10 mg (2x5 mg) visit 3, 5 mg visit 4, 2.5 mg visit 5.

Also known as: ZOMIG®

1

[11C]AZ10419369 DRUG

solution for iv injection. Will be injected within 2 to 5 hours after administration of ZOMIG® Rapimelt

1

Eligibility Criteria

• Age: 20 Years - 45 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

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

You may not qualify if:

• 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

Sponsors & Collaborators

• AstraZeneca: lead

Study Sites (1)

Research Site

Uppsala, Sweden

Location

MeSH Terms

Conditions

Migraine Disorders

Interventions

zolmitriptan; 5-methyl-8-(4-methyl-piperazin-1-yl)-4-oxo-4H-chromene-2-carboxylic acid (4-morpholin-4-yl-phenyl)amide

Condition Hierarchy (Ancestors)

Headache Disorders, Primary; Headache Disorders; Brain Diseases; Central Nervous System Diseases; Nervous System Diseases

Study Officials

• Stephen Kanes

  AstraZeneca

  STUDY DIRECTOR

• Wolfgang Kühn

  Quintiles AB Phase I Services

  PRINCIPAL INVESTIGATOR

• Brendan Smyth

  AstraZeneca

  STUDY CHAIR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY

Study Record Dates

• First Submitted: March 10, 2010
• First Posted: March 11, 2010
• Study Start: May 1, 2010
• Primary Completion: October 1, 2010
• Study Completion: October 1, 2010
• Last Updated: November 3, 2010

Record last verified: 2010-11

Locations

SE (1)