A Phase 1, Open Label, Randomized, Parallel-group, Single Center Study to Investigate Pharmacokinetics and Pharmacodynamics (Intragastric pH) of Linaprazan Glurate/Linaprazan After Single and 14 Days'Repeated Oral Administration of Linaprazan Glurate to Healthy Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 75
- 试验地点
- 1
- 主要终点
- AUC0-24h Linaprazan (QD)
研究概览
简要总结
This is a Phase I, single-center, open label parallel-group, randomized study designed to evaluate the pharmacokinetics (PK), pharmacodynamics (PD, by continuous intragastric pH measurment), safety and tolerability of single and repeated oral doses of linaprazan glurate in 3 different dose levels given once- (QD) or twice daily (BID), for 14 days, with an additional single dose after 2, 4 or 6 days of drug holiday. The population will include healthy male and female subjects.
The subjects will be followed up to 28 days post IMP dosing.
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
- None
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
- •Willing and able to give written informed consent for participation in the study.
- •Healthy male or female subject aged 18 to 65 years, inclusive.
- •Body mass index ≥ 18.5 and ≤ 30.0 kg/m
- •Medically healthy, without abnormal clinically significant medical history, physical findings, vital signs, ECGs, or laboratory values at the time of screening, as judged by the Investigator.
排除标准
- •Female subjects of childbearing potential (defined as all subjects physiologically capable of becoming pregnant)
- •Male subjects with a partner of childbearing potential
- •History of any clinically significant disease or disorder which, in the opinion of the Investigator, may either put the subject at risk because of participation in the study, or influence the results or the subject's ability to participate in the study.
- •History of GERD or clinically significant acid reflux, as judged by the Investigator.
研究组 & 干预措施
Group 1: 25 mg linaprazan glurate QD
25 mg (one 25 mg oral tablet) linaprazan glurate once daily (QD) for 14 days
干预措施: linaprazan glurate 25 mg QD (Drug)
Group 2: 50 mg Linaprazan Glurate QD
50 mg (two 25 mg oral tablets) linaprazan glurate once daily (QD) for 14 days
干预措施: linaprazan glurate 50 mg QD (Drug)
Group 3: 75 mg Linaprazan Glurate QD
75 mg (three 25 mg oral tablet) linaprazan glurate once daily (QD) for 14 days
干预措施: linaprazan glurate 75 mg QD (Drug)
Group 4: 25 mg Linaprazan Glurate BID
25 mg (one 25mg oral tablet) linaprazan glurate twice daily (BID) for 14 days
干预措施: linaprazan glurate 25 mg BID (Drug)
Group 5: 50 mg Linaprazan Glurate BID
50 mg (two 25 mg oral tablets) linaprazan glurate twice daily (BID) for 14 days
干预措施: linaprazan glurate 50 mg BID (Drug)
Group 6: 75 mg Linaprazan Glurate BID
75 mg (three 25 mg oral tablet) linaprazan glurate twice daily (BID) for 14 days
干预措施: linaprazan glurate 75 mg BID (Drug)
结局指标
主要结局
AUC0-24h Linaprazan (QD)
时间窗: Day 1 and Day 14
Linaprazan area under the plasma concentration curve, from 0 to 24h post dose on Day 1 and Day 14. QD groups only.
AUC0-24h Linaprazan Glurate (QD)
时间窗: Day 1 and day 14
Linaprazan glurate area under the plasma concentration curve, from 0-24h post dose on Day 1 and Day 14. QD groups only.
AUC0-12, 12-24h Linaprazan (BID)
时间窗: Day 1 and Day 14
Linaprazan area under the plasma concentration curve, from 0 to 12h and 12-24h post dose on Day 1 and Day 14. BID groups only.
Cmax Linaprazan (QD)
时间窗: Day 1 and day 14
Linaprazan maximum plasma concentration 0-24h post dose for QD groups, at day 1 and day 14.
Cmax Linaprazan (BID)
时间窗: Day 1 and day 14
Linaprazan maximum plasma concentration 0-12h, and 12-24h post dose for BID groups, at day 1 and day 14.
AUC0-12h, 12-24h Linaprazan Glurate (BID)
时间窗: Day 1 and Day 14
Linaprazan glurate area under the plasma concentration curve, from 0 to 12h and 12-24h post dose on Day 1 and Day 14. BID groups only.
Cmax Linaprazan Glurate (QD)
时间窗: Day 1 and day 14
Linaprazan glurate maximum plasma concentration 0-24h post dose for QD groups, at day 1 and day 14.
Cmax Linaprazan Glurate (BID)
时间窗: Day 1 and day 14
Linaprazan glurate maximum plasma concentration 0-12h and 12-24h post dose for BID groups, at day 1 and day 14.
Percentage of Time Gastric pH >4 Over a 24-hour Monitoring Period (Holding Time Ratio, HTR)
时间窗: Day 1 and day 14
Percentage of time gastric pH \>4 at Days 1 and 14 over a 24-hour monitoring period following linaprazan glurate administration. Intragastric pH was measured every second with an intragastric probe. The measurements were compressed into 10-minute median intervalls before calculating the % of time with intragastric \>pH 4 (HTR). The HTR is presented with descriptive statistics, by dosing group.
次要结局
未报告次要终点