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GSK1521498

Phase 2

Obesity | Small molecule | Metabolic |GSK plc|Last Updated: Jul 21, 2017

Success Probability

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Trial Design

RandomizedDouble-BlindPLACEBO_CONTROLLED
Total Trials1
Total Enrollment60

FDA Designations

No designations recorded

Clinical trial landscape

GSK1521498 · 3 trials · 2 indications

Phase 2 1Phase 1 2
NCT01195792A 35 Day Study to Investigate the Effects of GSK1521498 on Bodyweight in Obese Subjects With Over-Eating Behaviours.Obesity
COMPLETED60 Analytics
PHASE2COMPLETED
A 35 Day Study to Investigate the Effects of GSK1521498 on Bodyweight in Obese Subjects With Over-Eating Behaviours.
ObesityUnlock trial analytics

Study Endpoints

Primary Endpoints

Clinically and statistically significant weight loss
35 days
Brain activation within the reward circuitry in response to consumption of food and alcohol cues, as measured by functional magnetic resonance imaging (fMRI)
Day 5 in each treatment period

To test that the OPRM1 A118G polymorphism modulates the effects of GSK1521498 10 mg on brain reward function and processing

Adverse events as a measure of safety and tolerability
Throughout the study, from Day 1 to Day 67

Number of subjects with any adverse events during the treatment periods

Blood pressure (BP) as a measure of safety and tolerability
Screening (Up to 30 days prior to Day 1), Day 1, Day 2, Day 5 in each treatment period and Follow-up visit.

Systolic and diastolic BP will be measured

12-lead ECG and heart rate as a measure of safety and tolerability
Screening (Up to 30 days prior to Day 1), Day 1, Day 2, Day 5 in each treatment period and Follow-up visit.

12-lead electrocardiograph (ECG) will be measured

Clinical chemistry including liver enzymes and hematology as a measure of safety and tolerability
Screening (Up to 30 days prior to Day 1), Day 5 of each of the 3 treatment periods and Follow-up visit

Hematology/Chemistry assessments to be done at screening (fasted) and day 5 for each treatment session (un-fasted).

Psychiatric symptom questionnaires-Becks Depression & Anxiety Inventory (BDI-II & BAI)
Screening (Up to 30 days prior to Day 1), Day 1 (pre-dose and approximately 4 hours post dose), Day 2 (prior to discharge), Day 3 (prior to discharge), Day 5 (prior to discharge), in each treatment period and Follow-up visit

Mood anxiety will be assessed by The Beck Anxiety Inventory (BAI), The Beck Depression Inventory (BDI-II).

Psychiatric symptom questionnaires- Columbia Suicide Severity Rating Scale (C-SSRS)
Screening (Up to 30 days prior to Day 1), Day 1 (pre-dose and approximately 4 hours post dose), Day 2 (prior to discharge), Day 5 (prior to discharge), in each treatment period and Follow-up visit

Suicidality will be assessed by C-SSRS.

Psychiatric symptom questionnaires- Bond and Lader Visual Analogue Scales (VAS).
Screening (Up to 30 days prior to Day 1), Day 1 (pre-dose and approximately 4 hours post dose), Day 2 (prior to discharge), Day 3 (prior to discharge), Day 4 (prior to discharge), Day 5 (prior to discharge), in each treatment period and Follow-up visit

Mood anxiety and suicidality will be assessed by VAS.

Computerized tests of reaction time (CANTAB)
Approximately 1 hour pre-dose on Day 1 and approximately 4 hours post dose on Day 1, Day 2 and Day 5 in each treatment period

CANTAB attention tasks comprising of Simple Reaction Time (SRT), Choice Reaction Time (CRT) and Rapid Visual Information Processing (RVP) will be done to measure the power of attention

Pharmacokinetic interaction
GSK1521498 PK sampling; pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 7, 8, 9, 12, 13, 24, 48 and 72 hr post-dose.

AUC and Cmax of GSK1521498 and alcohol

Secondary Endpoints

To see if effects on bodyweight are associated with effects on fat mass, eating behaviour brain function and blood and urine markers
35 days
To see if effects on bodyweight correlate with over-eating behaviour at baseline
35 days
Safety: adverse events,blood pressure, heart rate, ECG, clinical chemistry, hematology, urinalysis, change in cognition (eg reaction times), change in mood scales, change in neuropsychiatric symptoms
35 days
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Study Design & Arms

AllocationRANDOMIZED
MaskingDOUBLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
2 mg GSK1521498EXPERIMENTALApproximately 20 subjects will be randomised to receive 2 mg GSK1521498. The drug is being developed for the treatment of obesity due to excessive consumption of high calorie foods
5 mg GSK1521498EXPERIMENTALApproximately 20 subjects will be randomised to receive 5 mg GSK1521498. The drug is being developed for the treatment of obesity due to excessive consumption of high calorie foods
PlaceboPLACEBO_COMPARATORApproximately 20 subjects will be randomised to receive matching placebo.
Treatment APLACEBO_COMPARATORSubject will receive oral dose of matching placebo once daily for 5 days in one of the 3 treatment periods.
Treatment BEXPERIMENTALSubject will receive 25 mg orally once daily for the first two days and 50 mg once daily for 3 days in one of the 3 treatment periods.
Treatment CEXPERIMENTALSubject will receive 10 mg orally once daily for 5 days in one of the 3 treatment periods.
GSK1521498 & alcoholEXPERIMENTALGSK1521498 20 mg and alcohol (0.5g/kg ethanol mixed with orange juice)
GSK1521498 & orange juiceEXPERIMENTALGSK1521498 20 mg and orange juice approximately matching alcoholic beverage for volume and colour
Placebo & alcoholEXPERIMENTALPlacebo and alcohol (0.5g/kg ethanol mixed with orange juice)
Placebo & orange juicePLACEBO_COMPARATORPlacebo and orange juice approximately matching alcoholic beverage for volume and colour

Interventions

NameTypeDescription
GSK1521498DRUGGSK1521498 2mg or 5mg will be given for up to 35 days and subjects will be assessed weekly
PlaceboDRUGPlacebo will be given for up to 35 days and subjects will be assessed weekly
Naltrexone (NTX)DRUGSwedish orange gelatin capsule containing 25mg of NTX or 50mg of NTX
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Eligibility Criteria

Age Range18 Years to 60 Years
SexALL
Healthy VolunteersNo
Study Sites3

Inclusion Criteria: * Obese but essentially healthy male or female between 18 and 60 years of age inclusive. * Body Mass Index greater than or equal to 30 kg/m2. * Binge Eating Scale (BES) score that is greater than or equal to 19 at screening assessment. * A female subject of child-bearing potenti...

Countries:United KingdomUnited States
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Frequently asked questions about GSK1521498

What is GSK1521498 used for?

GSK1521498 is an investigational small molecule being studied for alcoholism and obesity. It is in Phase 1 clinical development and has not been approved by the FDA. The drug is being developed by GSK plc.

What does GSK1521498 target?

GSK1521498 targets the mu opioid receptor, as indicated by a clinical trial evaluating the influence of the A118G polymorphism in the mu opioid receptor gene (OPRM1) on its effects. This suggests the drug works by interacting with this receptor.

Who makes GSK1521498?

GSK1521498 is being developed by GSK plc, a pharmaceutical company listed on the stock exchange under the ticker GSK. The drug is currently in Phase 1 clinical trials for alcoholism and obesity.

What phase is GSK1521498 in?

GSK1521498 is in Phase 1 clinical development. It is an investigational drug and has not been approved by regulatory authorities. Clinical trials have been completed for both alcoholism and obesity indications.

What clinical trials is GSK1521498 in?

GSK1521498 has been studied in clinical trials including NCT01195792 for obesity, NCT01366573 for alcoholism, and NCT01738867 for alcoholism in healthy social drinkers. All trials are completed, with the obesity trial being Phase 2 and the others Phase 1.

Is GSK1521498 the same as naltrexone?

No, GSK1521498 is not the same as naltrexone. However, a clinical trial (NCT01738867) compared the effects of GSK1521498 and naltrexone on brain function in healthy social drinkers, indicating they are distinct drugs being studied for similar conditions.