NCT01998672已完成1 期
A Double-blind, Randomised, Placebo-controlled, Dose-escalation Study of the Safety, Tolerability and Pharmacokinetics of Increasing Multiple Oral Doses of Px-102 to Healthy Subjects
适应症
干预措施
相关药物
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 42
- 试验地点
- 1
- 主要终点
- Safety and tolerability of Px-102
研究概览
简要总结
The purpose of this study is to assess the safety and tolerability of the FXR agonist Px-102 in healthy subjects after 7 days multiple oral dosing.
详细描述
The study is a single-centre, double-blind, randomized, placebo-controlled, parallel group phase I study with healthy male subjects receiving ascending multiple oral oral doses of Px-102 to assess the safety and tolerability, pharmacokinetics and pharmacodynamics.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Parallel
- 主要目的
- Treatment
- 盲法
- Triple (Participant, Care Provider, Investigator)
入排标准
- 年龄范围
- 18 Years 至 45 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Healthy male subject of Caucasian origin 18 to 45 years of age (inclusive).
- •Good state of health (mentally and physically) as determined by medical history, physical examination, vital signs, ECG recording and clinical lab results.
- •BMI in between 20-29 kg/m² (inclusive); with absolute weight in between 70 to 120 kg.
- •Total cholesterol and liver enzyme levels [alanine aminotransferase (ALT), aspartate aminotransferase (AST), gamma-glutamyltransferase (GGT), alkaline phosphatase (AP)] strictly within the normal ranges at screening and on Day -
- •Serum triglyceride not exceeding the upper limit of normal range.
- •HbA1c ≤ 6.5%
- •Subject has been informed both verbally and in writing and has given written consent to participation in the study prior to start and any study-related procedure.
- •Negative results for HIV- and Hepatitis-B and -C serology at screening.
- •Subject (including female partners of childbearing potential) has to use a highly effective method of birth control (failure rate less than 1% per year when used consistently and correctly), e.g. implants, injectables, combined oral contra-ceptives in combination with a barrier method, some intrauterine contraceptive devices or sexual abstinence.
排除标准
- •Female gender
- •Use of prescription or non-prescription drugs within 7 days (30 if the drug is a possible enzyme inducer) prior to administration of study medication. Use of drugs known to induce steatosis (e.g. valproate, amiodarone or prednisone) or to affect body weight and carbohydrate metabolism
- •Any acute or chronic illness or clinically relevant finding at screening and at base-line examination which may jeopardize the subject's participation in the study
- •History or presence of biliary obstruction or biliary disease, hepatic encephalopathy, advanced ascites, portal hypertension, esophageal/gastric variceal bleeding, hepatocellular carcinoma, previous liver transplantation or any other chronic liver disease
- •Renal dysfunction, e.g. glomerular filtration rate ≤ 80 ml/min/1.73 m2 (as determined by the formula of Cockroft-Gault)
- •Type I or II Diabetes
- •Any clinically relevant abnormality on screening medical assessment, laboratory examination, 12-lead ECG
- •Any clinically relevant finding in the baseline telemetry within the pre-dose evaluated observation period of at least 20 hours
- •Marked baseline prolongation of QT/QTc interval (QTc interval > 440 ms) in the 12-lead ECG using the Fridericia method for QTc analysis
- •Heart rate < 50 bpm.
- •History of pathological cardiovascular symptoms or a severe cardiovascular event
- •History of severe chronic autoimmune diseases such as severe allergy, atopic eczema, chronic dermatitis, severe psoriasis, multiple sclerosis, severe asthma, lupus or related disorders
- •Allergies (except for mild forms of hay fever) or history of hypersensitivity reactions
- •Smoking (regular or irregular) > 5 cigarettes (or equivalent) per day
- •Excessive alcohol drinking (more than approximately 20 g alcohol per day), unable to refrain from alcohol drinking from 48 hours prior to dosing until the last pharmacokinetic blood sample has been withdrawn
- •Positive test for drugs or alcohol at screening or prior to the dosing session
- •History of alcoholism or drug/chemical/substance abuse within past 2 years
- •Investigator deems the subject unable or unwilling to comply fully with the study protocol
- •Has received clinical study medication within the last 30 days prior to this study
- •Donation or loss of 400 ml or more of blood within eight (8) weeks prior to dosing
- •Allergic to any of the active or inactive ingredients in the study medication
- •Any other reason which the Investigator considers unsuitable for the subject to participate
- •Any condition or previous disease leading to pruritus or itching of the skin.
研究组 & 干预措施
Px-102
Active Comparator
Px-102 drinking solution, 0.5 mg/kg, 1.0 mg/kg and 1.5 mg/kg
干预措施: Px-102 (Drug)
Placebo
Placebo Comparator
Oral drinking solution
干预措施: Placebo (Drug)
结局指标
主要结局
Safety and tolerability of Px-102
时间窗: 7 days
Adverse event monitoring, laboratory values, cardiovascular monitoring. Comparison active vs. placebo
次要结局
- Pharmacokinetics of Px-102 and metabolites(Day 1: 0 min, 15 min, 30 min, 60 min, 1.5 h, 2 h, 3 h, 4 h, 5 h, 6 h, 7 h, 8 h, 12 h, 22 h, 24 h; Day 5 and 6: pre-dose; Day 7: 0 min, 15 min, 30 min, 60 min, 1.5 h, 2 h, 3 h, 4 h, 5 h, 6 h, 7 h, 8 h, 12 h, 22 h, 24 h, 30 h.)
- Pharmacodynamics(Pre-dose, 1, 2, 4, 8 and 10 hours after administration on Days 1 and 7; Pre-dose, 2 hours and 8 hours after administration on Days 2 to 6; at 22 hours after the last administration)
研究者
研究点 (1)
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