A Study to Assess the Bioavailability and Pharmacokinetics of an Immediate Release Tablet Formulation of Lefamulin When Administered to Fed and Fasted Healthy Subjects in Comparison to an Intravenous Formulation and a Capsule Formulation
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 20
- 试验地点
- 1
- 主要终点
- The area under the concentration time curve (AUC) of an intravenous and oral formulation of lefamulin in the fasting state
研究概览
简要总结
A Phase 1 study to assess the bioavailability and pharmacokinetics of a 600 mg immediate release tablet formulation of lefamulin when administered to fed and fasted healthy subjects in comparison to an intravenous formulation and a capsule formulation.
详细描述
This is a single center, single cohort, open label, randomized, four- period cross-over study with healthy subjects receiving a single dose of lefamulin at four study sessions at least 4 days apart. Lefamulin will be taken: 1) as 600 mg IR tablet orally in the fasted state; 2) as 600 mg API in capsule (3 x 200 mg capsules) orally in the fasted state; 3) as 150 mg i.v. infusion in 250 mL citrate buffered saline over 1 h; 4) as 600 mg IR tablet orally one hour after breakfast.
The order will be randomized. A total of 20 healthy subjects will be enrolled in the study. The same subjects will take part in all study sessions.
After each study session, the Safety Monitoring Team will review the safety and tolerance data before the commencement of the subsequent session.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 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
- •Healthy subjects 18-55 years of age
- •Good state of health (mentally and physically) as determined by the investigator
- •Body mass index within the range 19 to 32 kg/m2 inclusive
- •A signed and dated written informed consent form
- •The subject is able to understand and willing to comply with protocol requirements and timetables, instructions and protocol-stated restrictions
排除标准
- •Any acute or chronic illness or clinically relevant abnormality identified on the screening medical assessment, laboratory tests or ECG (12-lead or Holter), unless in the opinion of the investigator, in consultation with the Nabriva medical monitor, it will not interfere with the study procedures, affect the outcome of the study or compromise the safety of the subject
- •A known history of chronic liver or biliary disease, history of Gilbert's syndrome or an elevated bilirubin level
- •History of gastritis, gastrointestinal tract disorders or other clinical condition or previous surgery that might affect the absorption, distribution, biotransformation, or excretion of lefamulin
- •Use of prescription or non-prescription drugs within 7 days or 10 times the elimination half-life (whichever is longer) prior to first dose of study medication
- •Any intake of prescription or non-prescription drugs known to induce or inhibit drug-metabolizing enzymes or transport system enzymes within a period of less than 10 times the respective elimination half-life, or intake of grapefruit juice or grapefruit containing products within 7 days prior to first dose of study drug.
研究组 & 干预措施
Treatment A
Lefamulin as a 600 mg IR tablet in the fasted state
干预措施: Lefamulin (Drug)
Treatment B
Lefamulin as 600 mg API in capsule (three 200 mg capsules) in the fasted state
干预措施: Lefamulin (Drug)
Treatment C
Lefamulin as 150 mg i.v. in 250 mL citrate buffered saline infused over 1 h
干预措施: Lefamulin (Drug)
Treatment D
Lefamulin as a 600 mg IR tablet one hour after breakfast
干预措施: Lefamulin (Drug)
结局指标
主要结局
The area under the concentration time curve (AUC) of an intravenous and oral formulation of lefamulin in the fasting state
时间窗: 36 hours
次要结局
- The area under the concentration time curve (AUC) of a 600 mg IR tablet of lefamulin in the fed state(36 hours)
- The area under the concentration time curve (AUC) of a tablet and capsule formulation of lefamulin in the fasting state(36 hours)
- Assessment of the safety and tolerability of lefamulin when administered, as single doses orally and i.v. to healthy subjects aged 18 to 55 years (adverse events, laboratory assessments, vital signs and electrocardiograms)(36 hours)