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
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 12
- 主要终点
- Ertugliflozin half life (t1/2)
研究概览
简要总结
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.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 盲法
- None
入排标准
- 年龄范围
- 21 Years 至 65 Years（Adult, Older Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •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.
排除标准
- •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
- •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.
研究组 & 干预措施
Ertugliflozin 10 mg: tablet→osmotic capsule (OC) fast→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.
干预措施: Ertugliflozin 10 mg tablet (Drug)
Ertugliflozin 10 mg: tablet→osmotic capsule (OC) fast→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.
干预措施: Ertugliflozin OC Fast (Drug)
Ertugliflozin 10 mg: tablet→osmotic capsule (OC) fast→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.
干预措施: Ertugliflozin OC Slow (Drug)
Ertugliflozin 10 mg: tablet→OC slow→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.
干预措施: Ertugliflozin 10 mg tablet (Drug)
Ertugliflozin 10 mg: tablet→OC slow→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.
干预措施: Ertugliflozin OC Fast (Drug)
Ertugliflozin 10 mg: tablet→OC slow→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.
干预措施: Ertugliflozin OC Slow (Drug)
Ertugliflozin 10 mg: OC fast→tablet→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.
干预措施: Ertugliflozin 10 mg tablet (Drug)
Ertugliflozin 10 mg: OC fast→tablet→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.
干预措施: Ertugliflozin OC Fast (Drug)
Ertugliflozin 10 mg: OC fast→tablet→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.
干预措施: Ertugliflozin OC Slow (Drug)
Ertugliflozin 10 mg: OC fast→OC slow→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.
干预措施: Ertugliflozin 10 mg tablet (Drug)
Ertugliflozin 10 mg: OC fast→OC slow→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.
干预措施: Ertugliflozin OC Fast (Drug)
Ertugliflozin 10 mg: OC fast→OC slow→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.
干预措施: Ertugliflozin OC Slow (Drug)
Ertugliflozin 10 mg: OC slow→tablet→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.
干预措施: Ertugliflozin 10 mg tablet (Drug)
Ertugliflozin 10 mg: OC slow→tablet→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.
干预措施: Ertugliflozin OC Fast (Drug)
Ertugliflozin 10 mg: OC slow→tablet→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.
干预措施: Ertugliflozin OC Slow (Drug)
Ertugliflozin 10 mg: OC slow→OC fast→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.
干预措施: Ertugliflozin 10 mg tablet (Drug)
Ertugliflozin 10 mg: OC slow→OC fast→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.
干预措施: Ertugliflozin OC Fast (Drug)
Ertugliflozin 10 mg: OC slow→OC fast→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.
干预措施: Ertugliflozin OC Slow (Drug)
结局指标
主要结局
Ertugliflozin half life (t1/2)
时间窗: 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
时间窗: Up to 48 hr. postdose (Up to Day 3 in each dosing period)
AUC from Hour 0 to infinity (AUCinf) for ertugliflozin
时间窗: Up to 48 hr. postdose (Up to Day 3 in each dosing period)
Maximum plasma concentration (Cmax) of ertugliflozin
时间窗: Up to 48 hr. postdose (Up to Day 3 in each dosing period)
Number of Participants Discontinuing Study Drug Due to an AE
时间窗: Up to Day 21
Urinary glucose excretion
时间窗: Up to 48 hr. postdose (Up to Day 3 in each dosing period)
Number of Participants Experiencing an Adverse Event (AE)
时间窗: Up to 28 days postdose (Up to 49 days)
Time taken to reach the maximum observed plasma concentration (Tmax) of ertugliflozin
时间窗: Up to 48 hr. postdose (Up to Day 3 in each dosing period)
次要结局
未报告次要终点