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GSK1018921 · 2 trials · 1 indication
| Arm | Type | Description |
|---|---|---|
| GSK1018921 | EXPERIMENTAL | All subjects will received a dose of GSK1018921 and will peforme three PET scans using the ligand \[11C\]GSK931145, but in order to obtain adequate sampling of the exposure-time-occupancy curves, a range of doses will be evaluated, and the timing of the post-dose scans will differ between subjects. |
| Part A: Subjects receiving treatment in cohort A | EXPERIMENTAL | Eligible subjects will be randomized to receive GSK101892 and placebo. Subjects will receive escalated doses of GSK101892 with a starting dose of 0.5 milligrams. Each subject will receive no more than 4 doses of GSK1018921 in a maximum of 5 dosing sessions. Within each cohort, each session will be separated by a washout period of at least 7 days. |
| Part A: Subjects receiving treatment in cohort B | EXPERIMENTAL | Eligible subjects will be randomized to receive GSK101892 and placebo. Subjects will receive escalated doses of GSK101892 with a starting dose of 0.5 milligrams. Each subject will receive no more than 4 doses of GSK1018921 in a maximum of 5 dosing sessions. Within each cohort, each session will be separated by a washout period of at least 7 days. |
| Part A: Subjects receiving treatment in cohort C | EXPERIMENTAL | Eligible subjects will be randomized to receive GSK101892 and placebo. Subjects will receive escalated doses of GSK101892 with a starting dose of 0.5 milligrams. Each subject will receive no more than 4 doses of GSK1018921 in a maximum of 5 dosing sessions. Within each cohort, each session will be separated by a washout period of at least 7 days. |
| Part B: Subjects in 5 period crossover period | EXPERIMENTAL | Eligible subjects (first 14 subjects) will be randomized to one of the following 14 sequences as a 5 period crossover with sequences; LMNOQ, MNOLQ, NOLMQ, OLMNQ, ONMLQ, NMLOQ, MLONQ, LONMQ, LNMOQ, NMOLQM MOLNQ, OLNMQ, OMNLQ and MNLOQ) (L= 80 milligrams GSK1018921 given in fasted state, M= 200 milligrams GSK1018921 given in fasted state, N= nicotine lozenge, O= placebo and Q= 80 milligrams GSK1018921 in fed state). |
| Part B: Subjects in 4 period crossover period | EXPERIMENTAL | Eligible subjects (last 7 subjects) will be randomized to one of the following 7 sequences as a 4 period crossover with sequences; NLOM, LOMN, OLNM, LNMO, NMOL, MOLN, and MNLO. |
| Name | Type | Description |
|---|---|---|
| GSK1018921 | DRUG | GSK1018921 is a GT1 recepor antagonist |
| Nicotine Lozenges | DRUG | Nicotine Lozenges will be supplied as 4 milligrams lozenges. |
| Placebo | DRUG | Placebo tablets will be given to the subjects. |
* Inclusion criteria: * Healthy male subjects * Age: 18-55 years * No history of physical, neurological or mental illness * Exclusion criteria * History of claustrophobia or inability to lie still in the PET camera for at least 2 hours * Cardiac pacemakers or metal implants in the body t...
GSK1018921 is an investigational small molecule being developed by GSK plc for the treatment of schizophrenia. It is currently in Phase 1 clinical development, meaning it has not yet been approved by regulatory authorities and remains under study to evaluate its safety, tolerability, and pharmacological effects in humans.
GSK1018921 is a small molecule that targets the GlyT1 transporter, as indicated by a positron emission tomography (PET) study designed to describe the relationship between plasma concentrations and brain Gly-T1 occupancy. This mechanism is being explored for its potential role in treating schizophrenia.
GSK1018921 is being developed by GSK plc, a global pharmaceutical company listed on the stock exchange under the ticker GSK. The company is conducting clinical trials to evaluate the drug's safety and effects in healthy volunteers, with the goal of understanding its potential for treating schizophrenia.
GSK1018921 is in Phase 1 clinical development. It has completed two Phase 1 trials, both of which are finished, and there are no active trials currently ongoing. The drug remains investigational and is not yet approved for any use.
GSK1018921 has been studied in two completed Phase 1 clinical trials. The first, NCT00527020, was a first-time-in-human study with 27 participants in Germany. The second, NCT00945503, was a PET study with 12 male participants in Spain, examining brain Gly-T1 occupancy. Both trials involved healthy volunteers.
GSK1018921 is not the same as Gly-T1; rather, Gly-T1 is the molecular target that GSK1018921 acts on. The drug is designed to interact with the Gly-T1 transporter, and a PET study was conducted to measure how much of the drug occupies this target in the brain over time.