A Phase I Trial to Investigate the Pharmacokinetics and ECG Effects of Single Doses of Linaprazan Glurate Administered as Oral Tablets to Healthy Participants
试验速览
- 阶段
- 1 期
- 状态
- 招募中
- 入组人数
- 121
- 试验地点
- 2
- 主要终点
- Measurement of pharmacokinetic profile of linprazan glurate and linaprazan (AUClast)
研究概览
简要总结
This is a Phase I, single-center, double blind, placebo-controlled, parallel-group, randomized trial designed to evaluate the PK, cardiodynamic ECG effects, safety, and tolerability of single oral doses of linaprazan glurate. The trial will explore the PK properties of linaprazan glurate and linaprazan as well as the cardiodynamic ECG effects, safety, and tolerability after the administration of single doses: 300 mg and 600 mg in Part I of the trial, using formulation A of linaprazan glurate, as well as 150 mg, 275 mg, and up to 2 additional dose levels, using formulation C of linaprazan glurate to reach target linaprazan mean Cmax exposure (5222 nmol/L).
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Parallel
- 主要目的
- Basic Science
- 盲法
- Quadruple (Participant, Care Provider, Investigator, Outcomes Assessor)
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
- •Main inclusion Criteria:
- •Willing and able to give written informed consent for participation in the study.
- •Healthy male or female aged 18 to 65 years
- •Body mass index ≥18.5 and ≤35.0 kg/m
- •Prospective subjects, as well as their partners, must agree to contraception requirements
排除标准
- •Female subjects of childbearing potential unless they agree to use highly effective methods of contraception (failure rate of <1%) from 2 weeks prior to dosing until the end-of-study visit.
- •Male subjects with a partner of childbearing potential, unless they agree to use method of contraception from 2 weeks prior to dosing until the end-of-study visit.History of or current clinically significant disease as defined in the protocol
- •History of or current clinically significant disease as defined in the protocol.
- •History of GERD, significant acid reflux.
- •Subjects who are pregnant, currently breastfeeding, or intend to become pregnant (female subjects) or father a child (male subjects) during the course of the study (i.e., from screening to end of study visit).
研究组 & 干预措施
Placebo
Oral administration as a singel dose
干预措施: Placebo (Drug)
Linaprazan glurate
Oral administration as a single dose of 300 mg, 600 mg, 150 mg, 275 mg, and up to 2 additional dose levels.
干预措施: Linaprazan glurate (Drug)
结局指标
主要结局
Measurement of pharmacokinetic profile of linprazan glurate and linaprazan (AUClast)
时间窗: Up to 24 hours
To assess the AUC from time 0 to the last measurable concentration (AUClast)
Measurement of Cardiodynamic ECG (QTcF)
时间窗: Up to 24 hours
To assess the change from baseline in QTcF
Measurement of Cardiodynamic ECG (PR interval)
时间窗: Up to 24 hours
To assess the change from baseline in PR interval
Measurement of Cardiodynamic ECG (placebo-corrected QRS interval)
时间窗: Up to 24 hours
To assess the change from baseline in placebo-corrected QRS interval
Measurement of Cardiodynamic ECG (changes of T-wave)
时间窗: Up to 24 hours
Frequency of treatment emergent changes of T-wave abnormalities
Measurement of Cardiodynamic ECG (placebo-corrected PR interval)
时间窗: Up to 24 hours
To assess the change from baseline in placebo-corrected PR interval
Measurement of pharmacokinetic profile of linprazan glurate and linaprazan (Cmax)
时间窗: Up to 24 hours
To assess the Maximum plasma concentration (Cmax)
Measurement of pharmacokinetic profile of linprazan glurate and linaprazan (T1/2)
时间窗: Up to 24 hours
To assess the Terminal elimination half-life (T1/2)
Measurement of Cardiodynamic ECG (placebo-corrected QTcF)
时间窗: Up to 24 hours
To assess the change from baseline in placebo-corrected QTcF
Measurement of Cardiodynamic ECG (placebo-corrected heart rate)
时间窗: Up to 24 hours
To assess the change from baseline in placebo-corrected heart rate
Measurement of pharmacokinetic profile of linprazan glurate and linaprazan (AUCinf)
时间窗: Up to 24 hours
To assess the Area under the plasma concentration vs. time curve (AUC) from time 0 to infinity (AUCinf)
Measurement of Cardiodynamic ECG (heart rate)
时间窗: Up to 24 hours
To assess the change from baseline in heart rate
Measurement of Cardiodynamic ECG (QRS interval)
时间窗: Up to 24 hours
To assess the change from baseline in QRS interval
Measurement of Cardiodynamic ECG (categorical outliers)
时间窗: Up to 24 hours
Number of categorical outliers for ECG parameters (QTcF, HR, PR interval, QRS interval)
Measurement of Cardiodynamic ECG (changes of U-wave)
时间窗: Up to 24 hours
Frequency of treatment emergent changes of U-wave abnormalities
次要结局
未报告次要终点