A Phase 1, Open-Label Study to Assess the Pharmacokinetics, Pharmacodynamics, Safety and Tolerability of Repeated Doses of Opicapone, and Effect on Levodopa Pharmacokinetics in Subjects With Parkinson's Disease
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 16
- 试验地点
- 1
- 主要终点
- Pharmacokinetic evaluation of opicapone and its metabolites: area under the curve (AUC 0-24)
研究概览
简要总结
This is a phase 1, open-label study to assess the pharmacokinetics, pharmacodynamics, safety, and tolerability of opicapone when administered orally once daily for 14 days as adjunctive therapy to carbidopa/levodopa in subjects with Parkinson's disease.
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 85 Years（Adult, Older Adult）
- 性别
- All
- 接受健康志愿者
- 否
入选标准
- •Have a clinical diagnosis of idiopathic Parkinson's Disease (PD) for at least 3 years with clear improvement with levodopa treatment
- •Be at a stable dose of maintenance medication(s) for PD, including stable doses of CD/LD
- •Subjects of childbearing potential who do not practice total abstinence must agree to use hormonal or two forms of nonhormonal contraception (dual contraception) consistently during the screening, treatment and follow-up periods of the study
- •Have a body mass index (BMI) of 18 to 40 kg/m2
- •Have a modified Hoehn and Yahr stage of ≤4 in the OFF state
- •Be able to tolerate an overnight period of 12 hours without CD/LD
- •Be in good general health and expected to complete the clinical study as designed
排除标准
- •Are currently pregnant or breastfeeding
- •More than 2 alcoholic beverages daily or more than 14 alcoholic beverages weekly within 7 days of Day -1 or consume any alcohol within 48 hours of Day -
- •Have motor fluctuations during the day (ie, effect of levodopa "wearing off" or having unpredictable "off" periods), or severe or intolerable levodopa-induced dyskinesia
- •Have had previous exposure to opicapone, or have an allergy, hypersensitivity, or intolerance to opicapone or other COMT inhibitor.
- •Have a history of a medical condition or surgical procedure that might interfere with absorption or metabolism.
- •Have a known history of neuroleptic malignant syndrome
- •Have an unstable medical condition or chronic disease
- •Have taken certain prohibited medications within 28 days of Day -
- •Have a known or suspected diagnosis of AIDS, or have tested seropositive for HIV
- •Have hepatitis A or B
- •Have a significant risk of suicidal or violent behavior
研究组 & 干预措施
Opicapone once daily with Carbidopa/Levodopa
Opicapone administered once daily for 14 days; carbidopa/levodopa administered at set frequency on Study Days 1, 2 & 15
干预措施: Opicapone (Drug)
Opicapone once daily with Carbidopa/Levodopa
Opicapone administered once daily for 14 days; carbidopa/levodopa administered at set frequency on Study Days 1, 2 & 15
干预措施: Carbidopa Levodopa (Drug)
结局指标
主要结局
Pharmacokinetic evaluation of opicapone and its metabolites: area under the curve (AUC 0-24)
时间窗: up to 19 days
Area under the plasma concentration versus time curve from 0 to 24 hours for analytes with quantifiable concentrations at 24 hours postdose
Pharmacokinetic evaluation of opicapone and its metabolites: area under the curve (AUC 0-tlast)
时间窗: up to 19 days
Area under the plasma concentration versus time curve from 0 hour to the time of the last measurable concentration for analytes below the limit of quantification at 24 hours postdose
Pharmacokinetic evaluation of opicapone and its metabolites: Maximum plasma concentration (Cmax)
时间窗: up to 19 days
Maximum plasma concentration
Pharmacokinetic evaluation of opicapone and its metabolites: Time to maximum plasma concentration (tmax)
时间窗: up to 19 days
Time to maximum plasma concentration
Pharmacokinetic evaluation of levodopa following administration of opicapone: area under the curve (AUC 0-tlast)
时间窗: up to 15 days
Area under the plasma concentration versus time curve from 0 hours to time before next levodopa dose
Pharmacokinetic evaluation of levodopa following administration of opicapone: maximum plasma concentration (cmax)
时间窗: up to 15 days
Maximum plasma concentration
次要结局
- Incidence of Treatment-Emergent Adverse Events (safety and tolerability)(up to 19 days)
- Pharmacodynamic evaluation of opicapone on S-COMT activity(up to 19 days)