Metabolism and Pharmacokinetics of Primaquine Enantiomers in Human Volunteers Receiving a Seven Day Dose Regimen
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- 入组人数
- 36
- 试验地点
- 1
- 主要终点
- Change in Methemoglobin concentration in blood from baseline
研究概览
简要总结
To investigate the comparative tolerability, metabolism and pharmacokinetics of individual enantiomers of PQ in healthy human volunteers, receiving study drug over the course of 7 days.
详细描述
The primary objective of this project is to investigate the comparative tolerability, metabolism and pharmacokinetics of individual enantiomers of PQ in healthy human volunteers. Based on the results of this study, if one enantiomer seems to show a better safety profile (in terms of hematological effects), an analogous study will be carried out in G6PD deficient individuals (under a separate protocol). The studies are primarily aimed at understanding the tolerability and safety of the enantiomers in G6PD deficiency. If one shows a better safety profile, ultimately the evaluation of its efficacy will be required.
研究设计
- 研究类型
- Interventional
- 分配方式
- Non Randomized
- 干预模型
- Crossover
- 主要目的
- Basic Science
- 盲法
- Single (Participant)
盲法说明
Participants will not be able to know the sequence of the drug adminstration
入排标准
- 年龄范围
- 18 Years 至 65 Years（Adult, Older Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Normal, healthy adults aged 18 to 65 years
排除标准
- •Known history of liver, kidney or hematological disease
- •Known history of cardiac disease, Non Sinus Rhythm arrhythmia or QT prolongation
- •Autoimmune disorders
- •Report of an active infection
- •Evidence of G6PD deficiency
- •Participant is pregnant or breast-feeding, or is expecting to conceive during the study.
研究组 & 干预措施
RPQ (-) enantiomer
Cohort 1 will receive 15 mg of RPQ (3A) every day for 7 days Cohort 2 will receive 22.5 mg of RPQ (3A) every day for 7 days
干预措施: RPQ (Drug)
SPQ (+) enantiomer
Cohort 1 will receive 15 mg of SPQ (2A) every day for 7 days Cohort 2 will receive 22.5 mg of SPQ (2A) every day for 7 days
干预措施: SPQ (Drug)
Primaquine Phosphate
Cohort 1 will receive 30 mg of RSPQ (1A) every day for 7 days Cohort 2 will receive 45 mg of RSPQ (1A) every day for 7 days
干预措施: Primaquine Phosphate (Drug)
Placebo
Cohort 1 will receive placebo (4A) capsules everyday for seven days Cohort 2 will receive placebo (4A) capsules everyday for seven days
干预措施: Placebo (Drug)
结局指标
主要结局
Change in Methemoglobin concentration in blood from baseline
时间窗: Days 0, 3, 5, 7
Change in Methemoglobin concentration in blood from baseline (% hemoglobin)
次要结局
- Change in Hematocrit (%) Compared to baseline(Days 0, 3, 5, 7)
- Primaquine Plasma concentration, ng/mL(Days 0, 3, 5, 7)
- Change in Hemoglobin (g/dL) Compared to baseline(Days 0, 3, 5, 7)
- Change in AST (U/L) Compared to baseline(Days 0, 3, 5, 7)
- Carboxy- Primaquine Plasma concentration, ng/mL(Days 0, 3, 5, 7)
- Primaquine N-carbamoyl-glucuronide Plasma concentration, ng/mL(Days 0, 3, 5, 7)
- Change in Total Bilirubin (mg/dL) Compared to baseline(Days 0, 3, 5, 7)
- Primaquine Orthoquinone Plasma concentration, ng/mL(Days 0, 3, 5, 7)
- Change in ALT (U/L) Compared to baseline(Days 0, 3, 5, 7)