First Study in Humans With GSK424887

A Single Blind, Randomised, Placebo Controlled, Single Ascending Dose Study to Evaluate the Safety, Tolerability and Pharmacokinetics of GSK424887 in Healthy Male Subjects and an Open Label Positron Emission Tomography Study to Evaluate the Serotonin Transporter and Neurokinin- Receceptor Occupancy

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01059591

Enrollment

Registered

2010-02-01

Start date

2006-05-25

Completion date

2007-01-25

Last updated

2017-08-11

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

Conditions

Depressive Disorder and Anxiety Disorders

Keywords

NK1 antagonist and SSRI, Healthy subjects, Safety, First time in Human

Brief summary

This is the first study in Humans with GSK424887 to evaluate what effects, good or bad, the drug has on human health (safety and tolerability) and the amount of drug which gets into the bloodstream and is eliminated from the body (pharmacokinetics). Also the study aims to investigate the penetration of the drug in the human brain by using PET (Positron Emission Tomography) imaging technology

Interventions

DRUGGSK424887

GSK424887 2mg, 10mg, 50mg, 100mg capsule

DRUGPlacebo

Placebo to match GSK424887 2mg, 10mg,50mg, 100mg capsule

RADIATIONPET

Each subject will undergo 3 PET scans : one at Baseline and the others following dosing with GSK424887 at approximately 2h post-dose and aproximately 24 hours post-dose

Study design

Allocation

RANDOMIZED

Intervention model

CROSSOVER

Primary purpose

BASIC_SCIENCE

Masking

DOUBLE (Subject, Investigator)

Eligibility

Sex/Gender

MALE

Age

18 Years to 45 Years

Healthy volunteers

Yes

Inclusion criteria

* Healthy males aged 18-45 years, limited to 25-40 years for PET section

Exclusion criteria

* The subject has a positive: drug/alcohol, Hepatitis, HIV screen * The subject has a history of psychiatric illness suicidal attempts or behaviour. * Abuse of alcohol. * Clinically significant laboratory, ECG abnormality; * The subject has recently received an investigational. * Use of prescription or non-prescription drugs, * History or presence of allergy to the study drug or drugs of this class,. * Donation of more than 500 mL blood within the 90 days before dosing. * An unwillingness of male subjects to comply with contraceptive requirements * Average daily caffeine intake exceeding Protocol requirements.

Design outcomes

Primary

Measure	Time frame
Adverse event monitoring, vital signs (blood pressure, heart rate, ECGs, clinical laboratory assessments (standard laboratory parameters); Area under the concentration-time curve (AUC), Maximum observed concentration (Cmax) , tmax	12 weeks

Secondary

Measure	Time frame
Brain receptor occupancy	2 weeks

Countries

United Kingdom

Outcome results

None listed

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