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GSK239512

Phase 2

Alzheimer's Disease | Small molecule | Neurology |GSK plc|Trials Updated: Nov 8, 2017

GSK239512 development status

Highest phase Phase 2
Registered trials 6 across 1 sponsor since May 2007

GSK239512 target and mechanism

Molecular targetHRH3
Target classAntagonist
ModalitySmall molecule

Success Probability

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Market & Valuation

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Trial Design

RandomizedDouble-BlindPLACEBO_CONTROLLED
Total Trials6
Total Enrollment432

FDA Designations

No designations recorded

GSK239512 clinical trials

GSK239512 · 6 trials · 6 indications

Phase 2 3Phase 1 3
NCT01772199Study to Assess Whether GSK239512 Can Remyelinate Lesions in Subjects With Relapsing Remitting Multiple SclerosisMultiple Sclerosis, Relapsing-Remitting
COMPLETED131 Analytics
NCT01009060Study to Evaluate the Efficacy and Safety of GSK239512 in SchizophreniaSchizophrenia
COMPLETED50 Analytics
NCT01009255Study to Evaluate the Efficacy and Safety of GSK239512 in Alzheimer's DiseaseAlzheimer's Disease
COMPLETED196 Analytics
PHASE2COMPLETED
Study to Assess Whether GSK239512 Can Remyelinate Lesions in Subjects With Relapsing Remitting Multiple Sclerosis
Multiple Sclerosis, Relapsing-RemittingUnlock trial analytics
PHASE2COMPLETED
Study to Evaluate the Efficacy and Safety of GSK239512 in Schizophrenia
SchizophreniaUnlock trial analytics
PHASE2COMPLETED
Study to Evaluate the Efficacy and Safety of GSK239512 in Alzheimer's Disease
Alzheimer's DiseaseUnlock trial analytics

Study Endpoints

Primary Endpoints

Mean change in gadolinium (Gd) enhanced (GdE) lesion magnetization transfer ratio (MTR) differences (calibrated to reference scan) from before enhancement to stable recovery (>=3 months post new GdE lesion)
Up to Week 48

A single Baseline magnetic resonance image (MRI) prior to randomization. Following randomization, a total of 8 MRIs at approximate 6 week intervals: Week 6, Week 12, Week 18, Week 24, Week 30, Week 36, Week 42, Week 48. Reference MRI: In order to accommodate variations in MTR images acquired using different scanners, the images must be normalized to eliminate intensity shifts and contrast variations. For each scanner, images from a normal subject will be obtained and processed to serve as a calibration for each scanner prior to initiating scanning for subjects participating in the study

Mean change in Delta MTR lesion MTR differences (calibrated to reference scan) from before lesion appearance to stable recovery (>=3 months post lesion appearance)
Up to Week 48

A single Baseline MRI prior to randomization Following randomization, a total of 8 MRIs at approximate 6 week intervals: Week 6, Week 12, Week 18, Week 24, Week 30, Week 36, Week 42, Week 48. Reference MRI: In order to accommodate variations in MTR images acquired using different scanners, the images must be normalized to eliminate intensity shifts and contrast variations. For each scanner, images from a normal subject will be obtained and processed to serve as a calibration for each scanner prior to initiating scanning for subjects participating in the study

Change From Baseline in Composite Score of CSSB Following Dosing With GSK239512
Baseline and up to Week 7

The CSSB is a computerized battery with following domains (score range): Verbal memory (0-75), working memory (0-28), motor speed (0-100), verbal fluency, attention and speed of information processing (0-110) and executive functions with higher score representing better performance. Two Baseline CSSB testing were conducted; the first on the day prior to commencing dosing (Day -1) and the other test pre-dose on Day 1: the average of the two tests was used as Baseline. Change from Baseline was calculated as score at a given time minus score at Baseline. For each individual task from the CSSB, the Baseline was calculated as the mean of the second screening assessment and the Day 1 pre-dose assessment. A composite score was calculated by averaging all the measures, and then calculating a z-score of the composite. Higher the composite score, better is the performance. Z-score is the measure of standard deviation away from the mean score.

Change from Baseline (Day 1) in the executive function/working memory composite score in the Cog State battery at Week 16
Baseline (Day 1) and Week 16

Executive function/working memory composite score was calculated from the three tasks controlled oral word association (a measure of language fluency, planning and working memory where participants were instructed to generate as many as words as they could think of beginning with a specific letter in one minute. They were then requested to do exactly the same for two furthers letters and a score was given for this activity accuracy), category naming (a measure of semantic fluency, planning and working memory where participants were required to generate as many exemplars of the category 'animals' as they could in one minute), and one-back (a valid measure of working memory where participants were shown a single stimulus of a card in the center of the computer screen and were asked for YES" or "NO" to match the current card with the previous card and the accuracy was noted). Change from Baseline is the value at indicated time point minus the Baseline value.

Change from Baseline (Day 1) in the episodic memory composite score in the CogState battery at Week 16
Baseline (Day 1) and Week 16

Episodic memory composite score was calculated from the three tasks International Shopping List Task (ISLT) immediate recall, ISLT delayed recall, and Paired Associate Learning (PAL). The Total Score was calculated by taking the mean of all individual task scores. Change from Baseline is the value at indicated time point minus the Baseline value.

AUC of GSK239512
Predose and up to 120 hour post dose of GSK239512
Cmax of GSK239512
Predose and up to 120 hour post dose of GSK239512
Safety and tolerability as measured by adverse events, vital signs clinical laboratory measurements and validated clinical assessment scales.
Days 8, 15, 22 and 29
Receptor occupancy in the brain after receiving a dose of GSK239512, measured using calculations from PET images at 4 hours and 24 hours post dose

Secondary Endpoints

Change from baseline in T2 lesion MTR at Week 48
Baseline and Week 48
Cumulative new and enlarging Gd enhancing, T2 and Combined Unique Active lesions comparing placebo to GSK239512 treated subjects
Up to Week 48
Change from baseline at Week 48 in total brain volume, white matter volume and grey matter volume comparing placebo to GSK239512 treated subjects
Baseline and Week 48
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Study Design & Arms

AllocationRANDOMIZED
MaskingQUADRUPLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
GSK239512 ArmEXPERIMENTALGSK239512 once daily orally, started at 10 mcg and titrated to the maximum tolerated dose, Up to the highest dose of 80 mcg (10 mcg first week, 20 mcg second week, 40 mcg third week, 80 mcg fourth week) followed by 44 week maintenance treatment period
Placebo ArmPLACEBO_COMPARATORPlacebo once daily orally
GSK239512EXPERIMENTALRepeat dose.
PlaceboPLACEBO_COMPARATORRepeat dose. Placebo to match GSK239512
Session 1 or Session 2ACTIVE_COMPARATORSingle dose sessions without ketoconazole co-administration
Co-dose SessionACTIVE_COMPARATORSingle dose session with ketoconazole co-administration

Interventions

NameTypeDescription
GSK239512DRUGWhite to almost white, round tablets. Once daily orally, started at 10 mcg and titrated to the maximum tolerated dose, Up to the highest dose of 80 mcg (10 mcg first week, 20 mcg second week, 40 mcg third week, 80 mcg fourth week) followed by 44 week maintenance treatment period
PlaceboDRUGWhite to almost white, round tablets. Once daily orally.
ketoconazoleDRUGCYP3A4 inhibitor, potential perpetrator of drug-drug interaction
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Eligibility Criteria

Age Range18 Years to 50 Years
SexALL
Healthy VolunteersNo
Study Sites43

Inclusion Criteria: * 18 to 50 years of age * Diagnosed with a relapsing-remitting course of multiple sclerosis as defined by the appropriate McDonald criteria at the time of diagnosis. * Diagnosis of RRMS made within approximately 10 years prior to the screening visit (as documented by year of dia...

Countries:BulgariaCanadaCzechiaGermanySpainSwedenUkraineUnited KingdomUnited StatesChileRussiaSlovakiaSouth KoreaAustralia
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Frequently asked questions about GSK239512

What is GSK239512?

GSK239512 is an investigational small molecule developed by GSK plc for neurological conditions. It has been studied in Alzheimer's disease, mild cognitive impairment, schizophrenia, and relapsing-remitting multiple sclerosis. It is an HRH3 antagonist and remains in clinical development rather than being an approved medicine.

What is GSK239512 used for?

GSK239512 has been studied in Alzheimer's disease, mild cognitive impairment, schizophrenia, and relapsing-remitting multiple sclerosis. It is an investigational agent and is not an approved treatment for any of these conditions. All recorded trials of GSK239512 are completed, and no trials are currently active.

What does GSK239512 target?

GSK239512 targets HRH3, the histamine H3 receptor, and acts as an antagonist. Blocking this receptor is the proposed mechanism explored in its neurological development programs. GSK239512 is a small molecule and was studied in Alzheimer's disease, schizophrenia, and relapsing-remitting multiple sclerosis.

Who makes GSK239512?

GSK239512 is developed by GSK plc, which trades under the ticker GSK. The company sponsored the clinical trials of GSK239512 in Alzheimer's disease, schizophrenia, and relapsing-remitting multiple sclerosis. GSK239512 is an investigational small molecule and is not an approved product.

What phase is GSK239512 in?

GSK239512 is in Phase 2 development. Its Phase 2 trials covered Alzheimer's disease, schizophrenia, and relapsing-remitting multiple sclerosis, and a Phase 1 drug-drug interaction study was also conducted. All recorded GSK239512 trials are completed, and no trials are currently active.

What clinical trials is GSK239512 in?

GSK239512 has been evaluated in completed trials including NCT01772199 in relapsing-remitting multiple sclerosis, NCT01009255 in Alzheimer's disease, NCT01009060 in schizophrenia, and NCT01802931, a Phase 1 drug-drug interaction study in multiple sclerosis. These studies were randomized, double-blind, and placebo-controlled, with 224 participants in total.