Study To Estimate The Relative Bioavailability of Ertugliflozin (PF-04971729, MK-8835) in Healthy Adult Participants (MK-8835-039)

Merck Sharp & Dohme (MSD)

Status and phase: Completed; Phase 1

Conditions: Healthy

Treatments: Drug: Ertugliflozin 10 mg tablet; Drug: Ertugliflozin OC Fast; Drug: Ertugliflozin OC Slow

Study type: Interventional

Funder types: Industry

Identifiers

NCT01114568

8835-039

Details and patient eligibility

About

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.

Enrollment: 12 patients

Sex: All

Ages: 21 to 65 years old

Volunteers: Accepts Healthy Volunteers

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.

Trial design

12 participants in 6 patient groups

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

Experimental group

Description:

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.

Treatment:

Drug: Ertugliflozin OC Slow

Drug: Ertugliflozin 10 mg tablet

Drug: Ertugliflozin OC Fast

Ertugliflozin 10 mg: tablet→OC slow→OC fast

Experimental group

Description:

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.

Treatment:

Drug: Ertugliflozin OC Slow

Drug: Ertugliflozin 10 mg tablet

Drug: Ertugliflozin OC Fast

Ertugliflozin 10 mg: OC fast→tablet→OC slow

Experimental group

Description:

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.

Treatment:

Drug: Ertugliflozin OC Slow

Drug: Ertugliflozin 10 mg tablet

Drug: Ertugliflozin OC Fast

Ertugliflozin 10 mg: OC fast→OC slow→tablet

Experimental group

Description:

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.

Treatment:

Drug: Ertugliflozin OC Slow

Drug: Ertugliflozin 10 mg tablet

Drug: Ertugliflozin OC Fast

Ertugliflozin 10 mg: OC slow→tablet→OC fast

Experimental group

Description:

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.

Treatment:

Drug: Ertugliflozin OC Slow

Drug: Ertugliflozin 10 mg tablet

Drug: Ertugliflozin OC Fast

Ertugliflozin 10 mg: OC slow→OC fast→tablet

Experimental group

Description:

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.

Treatment:

Drug: Ertugliflozin OC Slow

Drug: Ertugliflozin 10 mg tablet

Drug: Ertugliflozin OC Fast