Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
GSK239512 · 6 trials · 6 indications
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
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
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.
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.
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.
| Arm | Type | Description |
|---|---|---|
| GSK239512 Arm | EXPERIMENTAL | GSK239512 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 Arm | PLACEBO_COMPARATOR | Placebo once daily orally |
| GSK239512 | EXPERIMENTAL | Repeat dose. |
| Placebo | PLACEBO_COMPARATOR | Repeat dose. Placebo to match GSK239512 |
| Session 1 or Session 2 | ACTIVE_COMPARATOR | Single dose sessions without ketoconazole co-administration |
| Co-dose Session | ACTIVE_COMPARATOR | Single dose session with ketoconazole co-administration |
| Name | Type | Description |
|---|---|---|
| GSK239512 | DRUG | White 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 |
| Placebo | DRUG | White to almost white, round tablets. Once daily orally. |
| ketoconazole | DRUG | CYP3A4 inhibitor, potential perpetrator of drug-drug interaction |
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...
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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.
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.
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.
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.
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.
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.