Evaluation of Pharmacokinetics, Safety, And Tolerability Of Ertugliflozin (PF-04971729, MK-8835) In Japanese And Western Healthy Participants (MK-8835-041)

A Phase 1, Randomized, Double Blind, Placebo-Controlled, Parallel Cohort, Single Dose Escalation And Multiple Dose Study In Japanese Healthy Subjects, And Open Label, Single Dose Escalation Study In Western Healthy Subjects To Investigate The Safety, Tolerability, Pharmacokinetics, And Pharmacodynamics Of PF-04971729

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01223339

Enrollment

Registered

2010-10-19

Start date

2010-10-31

Completion date

2011-02-28

Last updated

2016-05-20

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Diabetes Mellitus, Type 2

Keywords

Ertugliflozin, Japanese and Western population, pharmacokinetics, pharmacodynamics

Brief summary

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.

Interventions

DRUGErtugliflozin

Dose escalation of 1, 5, and 25 mg Ertugliflozin administered in the fasted state

DRUGPlacebo

Placebo tablets to Ertugliflozin administered in the fasted state

Study design

Allocation

RANDOMIZED

Intervention model

PARALLEL

Primary purpose

TREATMENT

Masking

DOUBLE (Subject, Investigator)

Eligibility

Sex/Gender

ALL

Age

18 Years to 55 Years

Healthy volunteers

Yes

Inclusion criteria

* Healthy male and/or female subjects of non-childbearing potential, between the ages of 18 and 55 years, inclusive * Body Mass Index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight \>50 kg (110 lbs). * Japanese subjects must have four Japanese grandparents who were born in Japan. * Mean body weight and the body weight range of Western subjects are similar to those of Japanese subjects with a 10% plus and minus error. * An informed consent document signed and dated by the subject. * Subjects who are willing and able to comply with scheduled visits, treatment plan,laboratory tests, and other study procedures.

Exclusion criteria

* Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease * Asian or Polynesian subjects in Western subject groups. * Any condition possibly affecting drug absorption (eg, gastrectomy). * A positive urine drug screen. * History of regular alcohol consumption exceeding 7 drinks/week for females or 14 drinks/week for males within 6 months of screening. * History or evidence of habitual use of tobacco or nicotine containing products within 3 months of Screening, with the exception of light smoking (up to 5 cigarettes per day or the equivalent). * Treatment with an investigational drug within 30 days or 5 half-lives preceding the first dose of study medication. * 12-lead ECG demonstrating QTc \>450 msec at screening. * Subjects with ANY of the following abnormalities on safety laboratory tests): * Evidence of glycosuria, as defined by a positive urine dipstick test; * Fasting serum triglyceride \>300 mg/dL; * Fasting LDL-cholesterol \> than or equal to 190 mg/dL. * Fasting serum glucose \>125 mg/dL.

Design outcomes

Primary

Measure	Time frame
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
Maximum plasma concentration (Cmax) of 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	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)

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026