A Phase I, Single Centre, Open-Label, Non-Randomised Study to Evaluate the PK of Single and Optional Multiple Dosing Regimens of MR Formulations of PCS499 Compared to Trental® (Pentoxifylline) Administered to Healthy Subjects Under Fed Conditions
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 18
- 试验地点
- 1
- 主要终点
- Maximum plasma concentrations (Cmax) in Part 2
研究概览
简要总结
This was a Phase I, single centre, open-label, non-randomised study and was designed to be conducted in up to 2 parts. The purpose of Part 1 was to identify a MR formulation of PCS499 that would provide an optimal dosing regimen in patients. The purpose of Part 2 of the study was to generate repeat dose information for the selected MR formulation of PCS499 in order to provide additional PK information for future patient studies.
研究设计
- 研究类型
- Interventional
- 分配方式
- Non Randomized
- 干预模型
- Sequential
- 主要目的
- Basic Science
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 55 Years（Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Male or non-pregnant, non-lactating female subjects
- •Aged 18 to 55 years, inclusive
- •Subjects who were healthy as determined by no clinically relevant abnormalities identified by a detailed medical history, full physical examination, vital signs, 12-lead resting electrocardiogram (ECG; corrected QT interval [QTc] ≤450, QRS <120, PR <220; normal morphology) performed at the screening visit and prior to each dosing
- •Body mass index (BMI) of 18.0 to 35.0 kg/m2 inclusive or, if outside the range, considered not clinically significant by the investigator and body weight >50 kg
- •Subjects who were willing and able to be confined at the clinical research centre for the scheduled inpatient visits
- •Ability to swallow multiple tablets whole
排除标准
- •Subject had a clinically significant history of GI, cardiovascular, musculoskeletal, endocrine, hematologic, psychiatric, renal, hepatic, bronchopulmonary, neurologic, immunologic, and/or lipid metabolism disorders and/or drug hypersensitivity
- •Subject had a known or suspected malignancy with the exception of basal cell carcinoma
- •Subject had a positive blood screen for human immunodeficiency virus (HIV), hepatitis B surface antigen (HBsAg), or hepatitis C virus antibody (HCV Ab) at the screening visit
- •Female subjects who were pregnant or lactating (all female subjects required a negative serum pregnancy test at the screening and a negative urine pregnancy test at each admission).
- •Subject had active disease or symptoms within 7 days prior to Day -1, such as nausea, vomiting, diarrhoea, and infection
- •Subject had undergone a hospital admission or major surgery within 30 days prior to the Screening visit
- •Subjects who had taken part in Part 1 were not permitted to take part in Part 2
研究组 & 干预措施
PCS499 MR Tablet Prototype 4
600mg single dose
干预措施: PCS499 (Drug)
PCS499 MR Tablet Prototype 2
600 mg single dose
干预措施: PCS499 (Drug)
Trental MR tablet 400mg
single dose
干预措施: Trental (Drug)
PCS499 MR Tablet Prototype 1
600mg single dose
干预措施: PCS499 (Drug)
Trental MR Tablet
400 mg multiple dose
干预措施: Trental (Drug)
PCS499 MR Tablet 900mg
multiple dose
干预措施: PCS499 (Drug)
PCS499 MR Tablet 600mg
multiple dose
干预措施: PCS499 (Drug)
结局指标
主要结局
Maximum plasma concentrations (Cmax) in Part 2
时间窗: Blood sampling will be drawn prior to the single dose administration on Days 1 & 4 and at 11 other timepoints in the following 24 hours. In addition, pre-dose trough samples will be taken on Days 2 &3.
Serial blood sampling at specified time points for determination of plasma concentration-time profiles
Maximum plasma concentrations (Cmax) for Part 1
时间窗: Blood samples will be drawn prior to single dose administration of study drug and at 11 other timepoints in a 24 hour period.
Serial blood sampling at specified time points for determination of plasma concentration-time profiles
次要结局
未报告次要终点