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NCT01315847

Positron Emission Tomography (PET) Study of Brain Calcitonin Gene-Related Peptide (CGRP) Receptor Occupancy After Telcagepant Administration (MK-0974-067)

Completed Phase 1 Results posted Last updated 2 April 2019
What this trial tests

Phase 1 trial testing telcagepant in Migraine in 10 participants. Completed in 26 July 2011.

Timeline
14 January 2010
Primary endpoint
26 July 2011
26 July 2011

Quick facts

Lead sponsorMerck Sharp & Dohme LLC
PhasePhase 1
StatusCompleted
Study typeINTERVENTIONAL
Allocationnon randomized
Designparallel
Maskingnone
Primary purposetreatment
Enrollment10
Start date14 January 2010
Primary completion26 July 2011
Estimated completion26 July 2011

Drugs / interventions tested

Conditions studied

Sponsor

Merck Sharp & Dohme LLC — full company profile →

Who can join

Adults 18 to 65, any sex, with Migraine. Patients with the condition only — healthy volunteers not accepted.

Results — posted to ClinicalTrials.gov

Per-arm endpoint measurements with 95% confidence intervals where reported. Source: trial results section.

Number of Participants With Adverse Events (AEs) (Part I) Primary · Up 14 days after the last dose of telcagepant and/or [11C]MK-4232 in Part I of study (Up to approximately 14 weeks)

Any AEs occurring among participants (all were healthy subjects) in Part I of study were recorded. An AE was defined as any unfavorable and unintended change in the structure, function or chemistry of the body temporally associated with study drug administration, whether or not considered related to the study drug. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition which was temporally associated with the administration of the study drug, was also an AE.

GroupValue95% CI
Telcagepant and [11C]MK-4232 (Part I): Healthy Participants4
Number of Participants With AEs (Part III) Primary · Up 14 days after the last dose of telcagepant and/or [11C]MK-4232 in Part III of study (Up to approximately 6 months)

Any AEs occurring among participants (all were migraine patients) in Part III of study were recorded. An AE was defined as any unfavorable and unintended change in the structure, function or chemistry of the body temporally associated with study drug administration, whether or not considered related to the study drug. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition which was temporally associated with the administration of the study drug, was also an AE.

GroupValue95% CI
Telcagepant and [11C]MK-4232 (Part III): Migraineurs4
Brain Calcitonin Gene-related Peptide (CGRP) Receptor Occupancy (RO) Post Telcagepant Obtained by PET Imaging Using [11C]MK-4232 Tracer at Baseline and After a Maximum Dose of Telcagepant (1120 mg) in Healthy Participants (Part I, Period 1) Primary · Part I Baseline, at ~0-90 minutes after [11C]MK-4232 dose; and Part I, Period 1 post telcagepant, at ~0-90 minutes after [11C]MK-4232 dose

Brain CGRP RO post telcagepant was determined by change in \[11C\]MK-4232 PET tracer biokinetics at baseline and post telcagepant administration. Using PET brain images acquired over \~0-90 minutes after \[11C\]MK-4232 dose, regions of interest (ROIs) were drawn throughout cerebral cortex and white matter, striatum, thalamus, cerebellum and pons. The ROIs were projected onto all frames of the dynamic PET scans in order to generate \[11C\]MK-4232 tissue time-activity curves (TACs). Serial arterial blood samples for measurement of plasma radioactivity and \[11C\]MK-4232 concentrations were colle

Subject 04
GroupValue95% CI
Telcagepant and [11C]MK-4232 (Part I): Healthy Participants43
Subject 01
GroupValue95% CI
Telcagepant and [11C]MK-4232 (Part I): Healthy Participants48
Subject 103
GroupValue95% CI
Telcagepant and [11C]MK-4232 (Part I): Healthy Participants58
Average Telcagepant Plasma Concentration During PET Imaging Using [11C]MK-4232 Tracer After a Maximum Dose of Telcagepant (1120 mg) in Healthy Participants (Part I, Period 1) Primary · Part I, Period 1 post telcagepant, at ~0-90 minutes after [11C]MK-4232 dose

In Part I, Period 1 blood samples for determination of plasma telcagepant concentrations were obtained prior to the telcagepant dose (time 0) and at 2, 3, 4 and 5 hours post telcagepant dose. The average plasma telcagepant concentration during the PET scan was determined, calculated as the area under the plasma telcagepant concentration versus time curve during the PET scanning interval divided by the duration of the PET scanning interval.

Subject 04
GroupValue95% CI
Telcagepant and [11C]MK-4232 (Part I): Healthy Participants16.3± 1.84
Subject 01
GroupValue95% CI
Telcagepant and [11C]MK-4232 (Part I): Healthy Participants20.2± 3.93
Subject 103
GroupValue95% CI
Telcagepant and [11C]MK-4232 (Part I): Healthy Participants22.2± 4.43
Brain CGRP RO Post Telcagepant Obtained by PET Imaging Using [11C]MK-4232 Tracer at Baseline and After a Therapeutic Dose of Telcagepant (140 mg) in Healthy Participants (Part I, Period 2) Primary · Part I Baseline, at ~0-90 minutes after [11C]MK-4232 dose; and Part I, Period 2 post telcagepant, at ~0-90 minutes after [11C]MK-4232 dose

Brain CGRP RO post telcagepant was determined by change in \[11C\]MK-4232 PET tracer biokinetics at baseline and post telcagepant administration. Using PET brain images acquired over \~0-90 miniutes after \[11C\]MK-4232 dose, ROIs were drawn throughout the cerebral cortex and white matter, striatum, thalamus, cerebellum and pons. The ROIs were projected onto all frames of the dynamic PET scans in order to generate \[11C\]MK-4232 tissue TACs. Serial arterial blood samples for measurement of plasma radioactivity and \[11C\]MK-4232 concentrations were collected during the PET scans. These samples

Subject 02
GroupValue95% CI
Telcagepant and [11C]MK-4232 (Part I): Healthy Participants5
Subject 04
GroupValue95% CI
Telcagepant and [11C]MK-4232 (Part I): Healthy Participants10
Subject 101
GroupValue95% CI
Telcagepant and [11C]MK-4232 (Part I): Healthy Participants4
Average Telcagepant Plasma Concentration During PET Imaging Using [11C]MK-4232 Tracer After a Therapeutic Dose of Telcagepant (140 mg) in Healthy Participants (Part I, Period 2) Primary · Part 1, Period 2 post telcagepant, at ~0-90 minutes after [11C]MK-4232 dose

In Part I, Period 2 blood samples for determination of plasma telcagepant concentrations were obtained prior to the telcagepant dose (time 0) and at 1, 2, 3 and 4 hours post telcagepant dose. The average plasma telcagepant concentration during the PET scan was determined, calculated as the area under the plasma telcagepant concentration versus time curve during the PET scanning interval divided by the duration of the PET scanning interval.

Subject 02
GroupValue95% CI
Telcagepant and [11C]MK-4232 (Part I): Healthy Participants0.254± 0.140
Subject 04
GroupValue95% CI
Telcagepant and [11C]MK-4232 (Part I): Healthy Participants0.859± 0.305
Subject 101
GroupValue95% CI
Telcagepant and [11C]MK-4232 (Part I): Healthy Participants0.424± 0.187

Adverse events — posted to ClinicalTrials.gov

Time frame: Up 14 days after the last dose of telcagepant and/or [11C]MK-4232 (Up to approximately 14 weeks for Part I, Up to approximately 6 months for Part III). Reporting threshold: 5%. Adverse-event reports describe events observed during the trial — not all are caused by the drug.

Telcagepant and [11C]MK-4232 (Part I): Healthy Participants
Serious: 0/6 (0%)
Deaths:
Telcagepant and [11C]MK-4232 (Part III): Migraineurs
Serious: 0/4 (0%)
Deaths:
Other adverse events (16 terms — click to expand)

ReactionSystemTelcagepant and [11C]MK-42…Telcagepant and [11C]MK-42…
MigraineNervous system disorders
White blood cells urine positiveInvestigations
HeadacheNervous system disorders
EcchymosisSkin and subcutaneous tissue disorders
Sinus tachycardiaCardiac disorders
Eye pruritusEye disorders
Ocular hyperaemiaEye disorders
Abdominal pain upperGastrointestinal disorders
General physical health deteriorationGeneral disorders
CystitisInfections and infestations
NasopharyngitisInfections and infestations
Blood urine presentInvestigations
Back painMusculoskeletal and connective tissue disorders
PresyncopeNervous system disorders
InsomniaPsychiatric disorders
DysphoniaRespiratory, thoracic and mediastinal disorders

Data from ClinicalTrials.gov NCT01315847 adverse events section.

Sponsor's own description

The purpose of this study is to determine the receptor occupancy (RO) associated with telcagepant (MK-0974) administration based on displacement of \[11C\]MK-4232 from the CGRP receptors in the brain using PET. The study enrolled healthy participants (Part I) and migraine patients (Part III). Due to a protocol amendment, study Part II was not conducted.

Publications & conference data

No peer-reviewed publications indexed yet for this trial. Completed trials usually publish results within 12-18 months.

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Other trials of telcagepant

Trials testing the same drug.

Other recruiting trials for Migraine

Currently open trials in the same condition.

Other Merck Sharp & Dohme LLC trials

Trials by the same sponsor.

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