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The purpose of this study is to assess safety, tolerability and pharmacokinetics after a single and repeated oral doses of TC-5214 (S-mecamylamine) in healthy male Japanese subjects.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Active | Experimental | Each cohort will have 9 volunteers that will receive TC-5214 |
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| Placebo | Placebo Comparator | Each cohort will have 3 volunteers that will receive placebo |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| TC-5214 | Drug | Four increasing doses levels of a single dose and two increasing dose levels of 6 days repeated dose of TC-5214 tablet |
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| Measure | Description | Time Frame |
|---|---|---|
| Safety by assessment of adverse events, brief neurological examinations, visual acuity test, vital signs, physical examinations, laboratory parameters, and electrocardiograms (ECGs), and Columbia Suicide Severity Rating Scale (C-SSRS). | Collected prior to treatment, during treatment and 7-10 days following discharge. Volunteers will be monitored througout the study for adverse events. |
| Measure | Description | Time Frame |
|---|---|---|
| Under Single Dosing conditions: Cmax, tmax, λz, t½λz, AUC(0-12), AUC(0-t), AUC, AUMC, MRT, % AUC extrapolated, CL/F, Vss/F, Ae fraction, Fe, (% of dose) Renal CLR. | Blood samples are taken repeatedly for 24 hours after dosing for 24 hours on Day 1 for SAD | |
| Under Multiple Dosing Conditions: Css, max, Cmin, Cmax (tss,max), λz, t½λz, AUCss, AUC(0-t), AUC, AUMC, MRT, % AUC extrapolated, CL/F, Vss/F, Ae, Fe % of dose,Renal CLR, Rac(Cmax), Rac(AUC), Rac(Cmin)), LI, % fluctuation, time to reach the steady state |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Hans Eriksson | AstraZeneca R&D Sodertalje, SE-151 85 Sodertalje, Sweden | Study Director |
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| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 24408516 | Derived | Xu H, Henningsson A, Alverlind S, Tummala R, Toler S, Beaver JS, Al-Huniti N. Population pharmacokinetics of TC-5214, a nicotinic channel modulator, in phase I and II clinical studies. J Clin Pharmacol. 2014 Jun;54(6):707-18. doi: 10.1002/jcph.264. Epub 2014 Jan 16. |
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| Placebo | Drug | Placebo tablet, single dose and 6 days repeated dose |
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| Blood samples are taken repeatedly for 24 hours after dosing for 24 hours on Day 1 for SAD and Day 6 (last dose) for MAD. |