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

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

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01085123

Enrollment

Registered

2010-03-11

Start date

2010-05-31

Completion date

2010-10-31

Last updated

2010-11-03

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Migraine

Keywords

Migraine, ZOMIG® Rapimelt

Brief summary

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

Interventions

DRUGRapimelt

oral tablet , 2.5 and 5 mg, single dose. 10 mg (2x5 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

Study design

Allocation

NON_RANDOMIZED

Intervention model

SINGLE_GROUP

Primary purpose

BASIC_SCIENCE

Masking

NONE

Eligibility

Sex/Gender

MALE

Age

20 Years to 45 Years

Healthy volunteers

Yes

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

Design outcomes

Primary

Measure	Time frame
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

Measure	Time frame
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

Countries

Sweden

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026