NCT01114568

Brief Summary

The purpose of this study is to examine the rate and extent of absorption of three oral formulations of ertugliflozin (PF 04971729, MK-8835) administered in lean to obese healthy volunteers.

Trial Health

100
On Track

Trial Health Score

Automated assessment based on enrollment pace, timeline, and geographic reach

Enrollment
12

participants targeted

Target at below P25 for phase_1 healthy

Timeline
Completed

Started May 2010

Shorter than P25 for phase_1 healthy

Status
completed

Health score is calculated from publicly available data and should be used for screening purposes only.

Trial Relationships

Click on a node to explore related trials.

Study Timeline

Key milestones and dates

First Submitted

Initial submission to the registry

April 27, 2010

Completed
4 days until next milestone

Study Start

First participant enrolled

May 1, 2010

Completed
2 days until next milestone

First Posted

Study publicly available on registry

May 3, 2010

Completed
29 days until next milestone

Primary Completion

Last participant's last visit for primary outcome

June 1, 2010

Completed
Same day until next milestone

Study Completion

Last participant's last visit for all outcomes

June 1, 2010

Completed
Last Updated

March 17, 2016

Status Verified

March 1, 2016

Enrollment Period

1 month

First QC Date

April 27, 2010

Last Update Submit

March 16, 2016

Conditions

Healthy

Keywords

Relative BioavailabilityPharmacokineticsPharmacodynamics

Outcome Measures

Primary Outcomes (8)

  • Area under the plasma concentration-time curve (AUC) from time 0 to time of the last quantifiable concentration (AUClast) for ertugliflozin

    Up to 48 hr. postdose (Up to Day 3 in each dosing period)

  • AUC from Hour 0 to infinity (AUCinf) for ertugliflozin

    Up to 48 hr. postdose (Up to Day 3 in each dosing period)

  • Maximum plasma concentration (Cmax) of ertugliflozin

    Up to 48 hr. postdose (Up to Day 3 in each dosing period)

  • Time taken to reach the maximum observed plasma concentration (Tmax) of ertugliflozin

    Up to 48 hr. postdose (Up to Day 3 in each dosing period)

  • Ertugliflozin half life (t1/2)

    Up to 48 hr. postdose (Up to Day 3 in each dosing period)

  • Number of Participants Experiencing an Adverse Event (AE)

    Up to 28 days postdose (Up to 49 days)

  • Number of Participants Discontinuing Study Drug Due to an AE

    Up to Day 21

  • Urinary glucose excretion

    Up to 48 hr. postdose (Up to Day 3 in each dosing period)

Study Arms (6)

Ertugliflozin 10 mg: tablet→osmotic capsule (OC) fast→OC slow

EXPERIMENTAL

The three treatments are A) a single dose of 10 mg administered as 2x5 mg material sparing formulation tablets B) a single dose of 10 mg extemporaneously prepared osmotic capsule with target release rate of approximately 6 hours (EP-Osmotic Capsule-Fast) and C) a single dose of 10 mg extemporaneously prepared osmotic capsule with target release rate of approximately 14 hours (EP-Osmotic Capsule-Slow). Treatment are administered on Day 1, Hour 0 of each dosing period with a minimum of 7-days wash-out between treatments A, B, and C.

Drug: Ertugliflozin 10 mg tabletDrug: Ertugliflozin OC FastDrug: Ertugliflozin OC Slow

Ertugliflozin 10 mg: tablet→OC slow→OC fast

EXPERIMENTAL

The three treatments are A) a single dose of 10 mg administered as 2x5 mg material sparing formulation tablets B) a single dose of 10 mg EP-Osmotic Capsule-Fast and C) a single dose of 10 mg EP-Osmotic Capsule-Slow. Treatment are administered on Day 1, Hour 0 of each dosing period with a minimum of 7-days wash-out between treatments A, B, and C.

Drug: Ertugliflozin 10 mg tabletDrug: Ertugliflozin OC FastDrug: Ertugliflozin OC Slow

Ertugliflozin 10 mg: OC fast→tablet→OC slow

EXPERIMENTAL

The three treatments are A) a single dose of 10 mg administered as 2x5 mg material sparing formulation tablets B) a single dose of 10 mg EP-Osmotic Capsule-Fast and C) a single dose of 10 mg EP-Osmotic Capsule-Slow. Treatment are administered on Day 1, Hour 0 of each dosing period with a minimum of 7-days wash-out between treatments A, B, and C.

Drug: Ertugliflozin 10 mg tabletDrug: Ertugliflozin OC FastDrug: Ertugliflozin OC Slow

Ertugliflozin 10 mg: OC fast→OC slow→tablet

EXPERIMENTAL

The three treatments are A) a single dose of 10 mg administered as 2x5 mg material sparing formulation tablets B) a single dose of 10 mg EP-Osmotic Capsule-Fast and C) a single dose of 10 mg EP-Osmotic Capsule-Slow. Treatment are administered on Day 1, Hour 0 of each dosing period with a minimum of 7-days wash-out between treatments A, B, and C.

Drug: Ertugliflozin 10 mg tabletDrug: Ertugliflozin OC FastDrug: Ertugliflozin OC Slow

Ertugliflozin 10 mg: OC slow→tablet→OC fast

EXPERIMENTAL

The three treatments are A) a single dose of 10 mg administered as 2x5 mg material sparing formulation tablets B) a single dose of 10 mg EP-Osmotic Capsule-Fast and C) a single dose of 10 mg EP-Osmotic Capsule-Slow. Treatment are administered on Day 1, Hour 0 of each dosing period with a minimum of 7-days wash-out between treatments A, B, and C.

Drug: Ertugliflozin 10 mg tabletDrug: Ertugliflozin OC FastDrug: Ertugliflozin OC Slow

Ertugliflozin 10 mg: OC slow→OC fast→tablet

EXPERIMENTAL

The three treatments are A) a single dose of 10 mg administered as 2x5 mg material sparing formulation tablets B) a single dose of 10 mg EP-Osmotic Capsule-Fast and C) a single dose of 10 mg EP-Osmotic Capsule-Slow. Treatment are administered on Day 1, Hour 0 of each dosing period with a minimum of 7-days wash-out between treatments A, B, and C.

Drug: Ertugliflozin 10 mg tabletDrug: Ertugliflozin OC FastDrug: Ertugliflozin OC Slow

Interventions

Ertugliflozin 10 mg tabletDRUG

A single dose of 10 mg ertugliflozin administered as 2x5 mg material sparing formulation tablets.

Ertugliflozin 10 mg: OC fast→OC slow→tabletErtugliflozin 10 mg: OC fast→tablet→OC slowErtugliflozin 10 mg: OC slow→OC fast→tabletErtugliflozin 10 mg: OC slow→tablet→OC fastErtugliflozin 10 mg: tablet→OC slow→OC fastErtugliflozin 10 mg: tablet→osmotic capsule (OC) fast→OC slow
Ertugliflozin OC FastDRUG

Formulation B) Ertugliflozin 10 mg OC Fast

Ertugliflozin 10 mg: OC fast→OC slow→tabletErtugliflozin 10 mg: OC fast→tablet→OC slowErtugliflozin 10 mg: OC slow→OC fast→tabletErtugliflozin 10 mg: OC slow→tablet→OC fastErtugliflozin 10 mg: tablet→OC slow→OC fastErtugliflozin 10 mg: tablet→osmotic capsule (OC) fast→OC slow
Ertugliflozin OC SlowDRUG

Formulation C) Ertugliflozin 10 mg OC Slow

Ertugliflozin 10 mg: OC fast→OC slow→tabletErtugliflozin 10 mg: OC fast→tablet→OC slowErtugliflozin 10 mg: OC slow→OC fast→tabletErtugliflozin 10 mg: OC slow→tablet→OC fastErtugliflozin 10 mg: tablet→OC slow→OC fastErtugliflozin 10 mg: tablet→osmotic capsule (OC) fast→OC slow

Eligibility Criteria

Age21 Years - 65 Years
Sexall
Healthy VolunteersYes
Age GroupsAdult (18-64), Older Adult (65+)

You may qualify if:

  • Healthy male and/or female subjects between the ages of 21 and 65 years, inclusive (Healthy is defined as no clinically relevant abnormalities identified by a detailed medical history, full physical examination, including blood pressure and pulse rate measurement, 12 lead ECG and clinical laboratory tests). Women must be of non childbearing potential
  • Body Mass Index (BMI) of 18.5 to 35.4 kg/m2; and a total body weight \>50 kg (110 lbs).
  • 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.

You may not qualify if:

  • Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at time of screening).
  • Any condition possibly affecting drug absorption (eg, gastrectomy).
  • A positive urine drug screen at Screening or prior to dosing in Period 1.
  • History of regular alcohol consumption exceeding 14 drinks/week for females or 21 drinks/week for males (1 drink = 5 ounces (150 mL) of wine or 12 ounces (360 mL) of beer or 1.5 ounces (45 mL) of hard liquor) within 6 months of screening.

Contact the study team to confirm eligibility.

Sponsors & Collaborators

Related Publications (1)

  • 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.

    PMID: 33813736DERIVED

MeSH Terms

Interventions

ertugliflozinTablets

Intervention Hierarchy (Ancestors)

Dosage FormsPharmaceutical Preparations

Study Officials

  • Medical Director

    Merck Sharp & Dohme LLC

    STUDY DIRECTOR

Study Design

Study Type
interventional
Phase
phase 1
Allocation
RANDOMIZED
Masking
NONE
Intervention Model
CROSSOVER
Sponsor Type
INDUSTRY
Responsible Party
SPONSOR

Study Record Dates

First Submitted

April 27, 2010

First Posted

May 3, 2010

Study Start

May 1, 2010

Primary Completion

June 1, 2010

Study Completion

June 1, 2010

Last Updated

March 17, 2016

Record last verified: 2016-03