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This study is to investigate the safety, tolerability and pharmacokinetics of single ascending oral doses of PF-04991532 in Japanese healthy subjects. The secondary objective is to investigate the pharmacokinetics and safety of single ascending oral doses of PF-04991532 in Western healthy subjects and to compare the pharmacokinetics between Japanese and Western healthy subjects.
Safety/Tolerability and Pharmacokinetics
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Japanese cohort | Experimental | A total of 12 Japanese healthy subjects will be allocated to receive 3 ascending single doses (100 mg, 300 mg and 750 mg) of PF-04991532 or placebo through 3 dosing periods in a randomization ratio of 3:1. |
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| Weterner Cohort | Experimental | 9 western healthy subjects will be enrolled to receive 2 single ascending doses (300 mg and 750 mg) of PF-04991532 through 2 dosing periods. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| PF-04991532 | Drug | Single dose administration of PF-04991532 (100 mg, 300 mg and 750 mg) in tablet formulation under fasted condition. |
|
| Measure | Description | Time Frame |
|---|---|---|
| Maximum Plasma Concentration (Cmax) | Pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 10,12 and 16, 24, 36 and 48 hours post dose | |
| Time for Cmax (Tmax) | Pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 10,12 and 16, 24, 36 and 48 hours | |
| Area under the plasma concentration-time profile from time zero to the time of the last quantifiable concentration (AUClast) | Pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 10,12 and 16, 24, 36 and 48 hours | |
| Area under the plasma concentration-time profile from time zero to 24 hours (AUC0-24) | Pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 10,12 and 16, 24, 36 and 48 hours | |
| Total amount of unchanged drug excreted in the urine over 24 hours, expressed as percent of dose (Ae24%) | Urine collection from 0 to 24 hours post dose | |
| Renal clearance (CLr) | Urine collection from 0 to 24 hours post dose |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Pfizer CT.gov Call Center | Pfizer | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Pfizer Investigational Site | New Haven | Connecticut | 06511 | United States |
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| Label | URL |
|---|---|
| To obtain contact information for a study center near you, click here. | View source |
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| Placebo | Drug | Single dose administration of matching placebo in tablet formulation at the fasted state |
|
| PF-04991532 | Drug | Single dose administration of PF-04991532 (300 mg and 750 mg) in tablet formulation under fasted condition. |
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| ID | Term |
|---|---|
| D003920 | Diabetes Mellitus |
| D003924 | Diabetes Mellitus, Type 2 |
| D044882 | Glucose Metabolism Disorders |
| ID | Term |
|---|---|
| D008659 | Metabolic Diseases |
| D009750 | Nutritional and Metabolic Diseases |
| D004700 | Endocrine System Diseases |
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| ID | Term |
|---|---|
| C571532 | 6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid |
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