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| Name | Class |
|---|---|
| Pfizer | INDUSTRY |
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This study is to characterize the pharmacokinetics, safety, tolerability, and pharmacodynamics of single and multiple oral doses (SD, MD) of ertugliflozin (PF-04971729, MK-8835) in Japanese healthy participants. The secondary objective is to investigate the safety, tolerability, pharmacokinetics, and pharmacodynamics of single doses of ertugliflozin in Western healthy participants as compared to Japanese healthy participants.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Single Dose Japanese Cohort | Experimental | This will be a single dose Cohort in which Japanese healthy participants will receive 3 ascending single doses (1 mg, 5 mg, and 25 mg) of ertugliflozin or placebo through 3 dosing periods. A minimum wash out period of 7-days will be set between each dose administration. |
|
| Single dose Western cohort | Experimental | This will be a single dose Cohort in which Western healthy participants will receive 3 ascending single doses (1 mg, 5 mg, and 25 mg) of ertugliflozin through 3 dosing periods. A minimum wash out period of 7-days will be set between each dose administration. |
|
| Multiple Dose Japanese Cohort | Experimental | This will be a multiple dose Cohort in which Japanese healthy participants will receive once-daily 25 mg ertugliflozin or placebo for 7 days. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Ertugliflozin | Drug | Dose escalation of 1, 5, and 25 mg Ertugliflozin administered in the fasted state |
|
| Measure | Description | Time Frame |
|---|---|---|
| Maximum plasma concentration (Cmax) of ertugliflozin for the Single Dose Cohort | Up to Day 4 of each treatment period | |
| Time taken to reach the maximum observed plasma concentration (Tmax) of ertugliflozin for the Single Dose Cohort | Up to Day 4 of each treatment period | |
| Area under the plasma concentration-time curve (AUC) from time 0 to time of the last quantifiable concentration (AUClast) for ertugliflozin for the Single Dose Cohort | Up to Day 4 of each treatment period | |
| AUC from Hour 0 to infinity (AUCinf) for ertugliflozin for the Single Dose Cohort | Up to Day 4 of each treatment period | |
| Ertugliflozin half life (t1/2) for the Single Dose Cohort | Up to Day 4 of each treatment period | |
| Apparent clearance (CL/F) of ertugliflozin for the Single Dose Cohort | Up to Day 4 of each treatment period | |
| Apparent volume of distribution (Vz/F) for the Single Dose Cohort | Up to Day 4 of each treatment period | |
| Accumulation Ratio of Area Under the Curve for the dosing interval of ertugliflozin (Rac) for the Single Dose Cohort | Up to Day 4 of each treatment period | |
| Number of participants who experienced an adverse event (AE) for the Single Dose Cohort |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Medical Director | Merck Sharp & Dohme LLC | Study Director |
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| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 34213819 | Derived | Fediuk DJ, Sahasrabudhe V, Dawra VK, Zhou S, Sweeney K. Population Pharmacokinetic Analyses of Ertugliflozin in Select Ethnic Populations. Clin Pharmacol Drug Dev. 2021 Nov;10(11):1297-1306. doi: 10.1002/cpdd.970. Epub 2021 Jul 2. | |
| 33813736 | Derived | Marshall JC, Liang Y, Sahasrabudhe V, Tensfeldt T, Fediuk DJ, Zhou S, Krishna R, Dawra VK, Wood LS, Sweeney K. Meta-Analysis of Noncompartmental Pharmacokinetic Parameters of Ertugliflozin to Evaluate Dose Proportionality and UGT1A9 Polymorphism Effect on Exposure. J Clin Pharmacol. 2021 Sep;61(9):1220-1231. doi: 10.1002/jcph.1866. Epub 2021 Jun 19. |
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| Placebo | Drug | Placebo tablets to Ertugliflozin administered in the fasted state |
|
| Ertugliflozin | Drug | Ertugliflozin 25 mg tablets administered once daily in the fed state for 7 days |
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| Placebo | Drug | Placebo tablets administered once daily in the fed state for 7 days |
|
| Up to 10 days after the final dose of study drug (Up to Day 11) |
| Number of participants who discontinued study drug due to an AE for the Single Dose Cohort | Up to Day 1 of each treatment period |
| Urinary Glucose Excretion over 24 hours for the Single Dose Cohort | Up to 24 hours postdose (Up to Day 2) |
| Cmax of ertugliflozin for the Multiple Dose Cohort | Up to Day 10 |
| Tmax of ertugliflozin for the Multiple Dose Cohort | Up to Day 10 |
| AUClast for ertugliflozin for the Multiple Dose Cohort | Up to Day 10 |
| AUCinf for ertugliflozin for the Multiple Dose Cohort | Up to Day 10 |
| t1/2 for the Multiple Dose Cohort | Up to Day 10 |
| CL/F of ertugliflozin for the Multiple Dose Cohort | Up to Day 10 |
| Vz/F for the Multiple Dose Cohort | Up to Day 10 |
| Rac for the Single Dose Cohort | Up to Day 10 |
| Number of participants who experienced an AE for the Multiple Dose Cohort | Up to 10 days after the final dose of study drug (Up to Day 17) |
| Number of participants who discontinued study drug due to an AE for the Multiple Dose Cohort | Up to Day 7 |
| Urinary Glucose Excretion over 24 hours for the Multiple Dose Cohort | Up to 24 hours postdose (Up to Day 8) |
| 33434408 | Derived | Li Y, Nucci G, Yamamoto Y, Fediuk DJ, Sahasrabudhe V. Pharmacokinetics and Pharmacodynamics of Ertugliflozin in Healthy Japanese and Western Subjects. Clin Pharmacol Drug Dev. 2021 Jul;10(7):765-776. doi: 10.1002/cpdd.908. Epub 2021 Jan 12. |
| ID | Term |
|---|---|
| D003924 | Diabetes Mellitus, Type 2 |
| ID | Term |
|---|---|
| D003920 | Diabetes Mellitus |
| D044882 | Glucose Metabolism Disorders |
| D008659 | Metabolic Diseases |
| D009750 | Nutritional and Metabolic Diseases |
| D004700 | Endocrine System Diseases |
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| ID | Term |
|---|---|
| C570288 | ertugliflozin |
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