Clinical trial NCT01114568: Study To Estimate The Relative Bioavailability of Ertugliflozin (PF-04971729, MK-8835) in Healthy Adult Participants (MK-8835-039)
Official title: A Phase 1, Cross-Over, Single-Dose, Open-Label Study To Estimate The Relative Bioavailability Of Three Different Formulations Of PF-04971729 in Lean To Obese, Otherwise Healthy Adult Subjects
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Keywords: Relative Bioavailability
Pharmacokinetics
Pharmacodynamics
Lead sponsor: Merck Sharp & Dohme LLC
Sponsor class: INDUSTRY
Collaborators: name: Pfizer
First posted: 2010-05-03
Enrollment: 12
Sex: ALL
Minimum age (years): 21
Maximum age (years): 65
Standard ages: ADULT
OLDER_ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: CROSSOVER

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.


Eligibility criteria: Inclusion Criteria:

* 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.

Exclusion Criteria:

* 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.

Primary outcomes:
measure: Area under the plasma concentration-time curve (AUC) from time 0 to time of the last quantifiable concentration (AUClast) for ertugliflozin
timeFrame: Up to 48 hr. postdose (Up to Day 3 in each dosing period)
measure: AUC from Hour 0 to infinity (AUCinf) for ertugliflozin
timeFrame: Up to 48 hr. postdose (Up to Day 3 in each dosing period)
measure: Maximum plasma concentration (Cmax) of ertugliflozin
timeFrame: Up to 48 hr. postdose (Up to Day 3 in each dosing period)
measure: Time taken to reach the maximum observed plasma concentration (Tmax) of ertugliflozin
timeFrame: Up to 48 hr. postdose (Up to Day 3 in each dosing period)
measure: Ertugliflozin half life (t1/2)
timeFrame: Up to 48 hr. postdose (Up to Day 3 in each dosing period)
measure: Number of Participants Experiencing an Adverse Event (AE)
timeFrame: Up to 28 days postdose (Up to 49 days)
measure: Number of Participants Discontinuing Study Drug Due to an AE
timeFrame: Up to Day 21
measure: Urinary glucose excretion
timeFrame: Up to 48 hr. postdose (Up to Day 3 in each dosing period)
Secondary outcomes:
Other outcomes:
Locations:
Study officials:
affiliation: Merck Sharp & Dohme LLC
name: Medical Director
role: STUDY_DIRECTOR
References:
citation: 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.