Study To Estimate The Relative Bioavailability of Ertugliflozin (PF-04971729, MK-8835) in Healthy Adult Participants (MK-8835-039)
Phase 1
Completed
- Conditions
- Healthy
- Interventions
- Registration Number
- NCT01114568
- Lead Sponsor
- Merck Sharp & Dohme LLC
- 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.
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- All
- Target Recruitment
- 12
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.
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- CROSSOVER
- Arm && Interventions
Group Intervention Description Ertugliflozin 10 mg: OC slow→OC fast→tablet Ertugliflozin OC Fast 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. Ertugliflozin 10 mg: OC fast→OC slow→tablet Ertugliflozin OC Slow 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. Ertugliflozin 10 mg: OC slow→tablet→OC fast Ertugliflozin OC Fast 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. Ertugliflozin 10 mg: tablet→osmotic capsule (OC) fast→OC slow Ertugliflozin OC Slow 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. Ertugliflozin 10 mg: OC fast→OC slow→tablet Ertugliflozin OC Fast 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. Ertugliflozin 10 mg: tablet→osmotic capsule (OC) fast→OC slow Ertugliflozin 10 mg tablet 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. Ertugliflozin 10 mg: tablet→OC slow→OC fast Ertugliflozin 10 mg tablet 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. Ertugliflozin 10 mg: OC fast→tablet→OC slow Ertugliflozin 10 mg tablet 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. Ertugliflozin 10 mg: OC fast→OC slow→tablet Ertugliflozin 10 mg tablet 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. Ertugliflozin 10 mg: OC slow→tablet→OC fast Ertugliflozin 10 mg tablet 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. Ertugliflozin 10 mg: OC slow→OC fast→tablet Ertugliflozin 10 mg tablet 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. Ertugliflozin 10 mg: OC fast→tablet→OC slow Ertugliflozin OC Slow 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. Ertugliflozin 10 mg: OC slow→tablet→OC fast Ertugliflozin OC Slow 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. Ertugliflozin 10 mg: OC slow→OC fast→tablet Ertugliflozin OC Slow 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. Ertugliflozin 10 mg: tablet→osmotic capsule (OC) fast→OC slow Ertugliflozin OC Fast 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. Ertugliflozin 10 mg: tablet→OC slow→OC fast Ertugliflozin OC Fast 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. Ertugliflozin 10 mg: tablet→OC slow→OC fast Ertugliflozin OC Slow 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. Ertugliflozin 10 mg: OC fast→tablet→OC slow Ertugliflozin OC Fast 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.
- Primary Outcome Measures
Name Time Method Ertugliflozin half life (t1/2) Up to 48 hr. postdose (Up to Day 3 in each dosing period) 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) 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) Number of Participants Experiencing an Adverse Event (AE) Up to 28 days postdose (Up to 49 days) 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)
- Secondary Outcome Measures
Name Time Method