Effect of Food on Opicapone Bioavailability and Pharmacodynamics in Healthy Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- 入组人数
- 28
- 主要终点
- Time to occurrence of Emax (tEmax) - Day 9 (fasted state)
研究概览
简要总结
The purpose of this study is to investigate the effect of food on the catechol-O-Methyltransferase (COMT) activity after repeated doses of opicapone (OPC, development code BIA 9-1067) in healthy subjects and to characterize the effects of food on the pharmacokinetics (PK) and tolerability of OPC after repeated doses.
详细描述
Single-centre, open-label, single-arm study in 28 healthy subjects. Subjects received a single-dose of 50 mg OPC once-daily (QD) in the evening for 12 days. On Day 1 (D1), 50 mg OPC was orally administered in the evening (reference hour for all other administrations) after a minimum of 6 hours fast. From D2 to D8 subjects were in ambulatory and received 50 mg OPC once-daily (evening administration after 2 hours fast). On D9, 50 mg OPC was orally administered in the evening after a minimum of 6 hours fast. On D10, 50 mg OPC was orally administered in the evening, thirty minutes after the start of a moderate meal (with a previous 6 hours fast). On D11 and D12 subjects received the last doses of 50 mg OPC (evening administration after 2 hours fast).
研究设计
- 研究类型
- Interventional
- 分配方式
- Na
- 干预模型
- Single Group
- 主要目的
- Treatment
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 45 Years（Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Able and willing to give written informed consent and to comply with the study restrictions.
- •Male or female subjects aged between 18 and 45 years, inclusive.
- •Body mass index (BMI) between 19 and 30 kg/m2, inclusive.
- •Healthy as determined by pre-study medical history, physical examination, vital signs, complete neurological examination and 12-lead ECG.
- •Negative tests for HBsAg, anti-HCV Ab and HIV-1 and HIV-2 Ab at screening.
- •Clinical laboratory test results clinically acceptable at screening and admission.
- •Negative screen for alcohol and drugs of abuse at screening and admission.
- •Non-smokers or ex-smokers for at least 3 months.
- •If female:
- •Not of childbearing potential by reason of surgery or, if of childbearing potential, she uses an effective non-hormonal method of contraception (intrauterine device or intrauterine system; condom or occlusive cap [diaphragm or cervical or vault caps] with spermicidal foam or gel or film or cream or suppository; true abstinence; or vasectomized male partner, provided that he is the sole partner of that subject) for all the duration of the study.
- •Negative serum pregnancy test at screening and a negative urine pregnancy test on admission.
排除标准
- •Clinically relevant history or presence of respiratory, gastrointestinal, renal, hepatic, haematological, lymphatic, neurological, cardiovascular, psychiatric, musculoskeletal, genitourinary, immunological, dermatological, endocrine, connective tissue diseases or disorders.
- •Clinically relevant surgical history.
- •Clinically relevant abnormality in the coagulation tests.
- •Clinically relevant abnormality in the liver function tests.
- •History of relevant atopy or drug hypersensitivity, particularly to any COMT inhibitor.
- •History of alcoholism or drug abuse.
- •Consume more than 14 units of alcohol a week.
- •Significant infection or known inflammatory process at screening or admission.
- •Acute gastrointestinal symptoms (e.g., nausea, vomiting, diarrhoea, heartburn) at the time of screening or admission.
- •Used medicines within 2 weeks of admission that may affect the safety or other study assessments, in the investigator's opinion.
- •Previously received OPC.
- •Used any investigational drug or participated in any clinical trial within 90 days prior to screening.
- •Participated in more than 2 clinical trials within the 12 months prior to screening.
- •Donated or received any blood or blood products within the 3 months prior to screening.
- •Vegetarians, vegans or have medical dietary restrictions.
- •Cannot communicate reliably with the investigator.
- •Unlikely to co-operate with the requirements of the study.
- •If female:
- •Pregnant or breast-feeding.
- •Of childbearing potential and not used an approved effective contraceptive method or she uses oral contraceptives.
研究组 & 干预措施
50 mg OPC
Subjects received 50 mg OPC once-daily in the evening for 12 days. On D9 subjects were to receive 50 mg OPC in the evening after a minimum 6 hours fast. On D10 subjects were to receive the QD dose of 50 mg OPC thirty minutes after the start of moderate meal (with a previous 6 hours fast)
干预措施: Opicapone (OPC) (Drug)
结局指标
主要结局
Time to occurrence of Emax (tEmax) - Day 9 (fasted state)
时间窗: Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose
Pharmacodynamic parameters for opicapone
Maximum observed effect on COMT activity (Emax) - Day 9 (fasted state)
时间窗: Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose
Pharmacodynamic parameters for opicapone
Area under the effect-time curve (AUEC) - Day 9 (fasted state)
时间窗: Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose
Pharmacodynamic parameters for opicapone
Maximum observed effect on COMT activity (Emax) - Day 10 (fed state)
时间窗: Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose
Pharmacodynamic parameters for opicapone
Time to occurrence of Emax (tEmax) - Day 10 (fed state)
时间窗: Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose
Pharmacodynamic parameters for opicapone
Area under the effect-time curve (AUEC) - Day 10 (fed state)
时间窗: Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose
Pharmacodynamic parameters for opicapone
次要结局
- Maximum observed plasma concentration (Cmax) - Day 10 (fed state)(Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose)
- Time of occurrence of Cmax (tmax) - Day 10 (fed state)(Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose)
- Maximum observed plasma concentration (Cmax) - Day 9 (fasted state)(Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose)
- Time of occurrence of Cmax (tmax) - Day 9 (fasted state)(Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose)