Drug-Interaction Assessment of GSK3772701 in Healthy Male and Female Participants Aged 18 to 55 Years
A Phase 1, Open-Label Study in Healthy Participants Aged 18 to 55 Years to Investigate the CYP3A4 Interaction Potential of GSK3772701
研究概览
研究类型
注册 (估计的)
阶段
- 阶段1
联系人和位置
学习联系方式
- 姓名:US GSK Clinical Trials Call Center
- 电话号码:877-379-3718
- 邮箱:GSKClinicalSupportHD@gsk.com
研究联系人备份
- 姓名:EU GSK Clinical Trials Call Center
- 电话号码:+44 (0) 20 89904466
- 邮箱:GSKClinicalSupportHD@gsk.com
学习地点
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Florida
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Miami、Florida、美国、33143
- 招聘中
- GSK Investigational Site
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首席研究员:
- Sandra Pagnussat
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接触:
- US GSK Clinical Trials Call Center
- 电话号码:877-379-3718
- 邮箱:GSKClinicalSupportHD@gsk.com
-
接触:
- EU GSK Clinical Trials Call Centre
- 电话号码:+44 (0) 20 8990 4466
- 邮箱:GSKClinicalSupportHD@gsk.com
-
-
参与标准
资格标准
适合学习的年龄
- 成人
接受健康志愿者
描述
Inclusion Criteria:
- Aged 18 to 55 years (inclusive), at the time of signing the informed consent form (ICF).
- Weight of at least 50 kg with a body-mass index <=18.0 and <=30.0 kg/m².
- Written informed consent obtained from the participant prior to performance of any study specific procedure, and which includes agreement to compliance, with the requirements and restrictions listed in the ICF and in this protocol.
- Participants, who, in the opinion of the investigator, can and will comply with the requirements of the protocol (e.g., completion of study assessments, return for follow-up visits).
Participants who are healthy as established by medical evaluation including medical history, physical examination, cardiac monitoring, and clinical laboratory assessment before entering into the study.
Contraception:
- Male participants are eligible to participate.
- A female participant is eligible to participate if they are not pregnant or breastfeeding, and one of the following conditions applies:
- Is a participant of non-childbearing potential (PONCBP). OR
- Is a POCBP and using a contraceptive method that is highly effective, with a failure rate of <1%, for 30 days prior to and during the study intervention period and for at least 7 days after the last dose of GSK3772701 and at least 2 days after the last dose of MDZ.
- A POCBP must have a negative highly sensitive pregnancy test (urine or serum as required by local regulations) at Screening and within 24 hours before the first dose of study intervention.
- A blood sample for simultaneous follicle-stimulating hormone (FSH) may be collected, and estradiol levels may be included at investigator's discretion to confirm non-reproductive potential when menopausal status is uncertain according to the local laboratory reference range.
Exclusion Criteria:
- History or presence/significant history of or current cardiovascular, respiratory, hepatic, renal, urological, gastrointestinal, immunological, dermatological, endocrine, hematologic, neurological, or psychiatric disorders capable of significantly altering the absorption, metabolism, or elimination of drugs; constituting a risk when taking the study intervention or interfering with the interpretation of data.
- Any condition where the administration of MDZ could be contraindicated, including but not limited to, hypersensitivity (MDZ, any of its excipients, or to any benzodiazepines), sleep apnea, glaucoma (narrow-angle glaucoma, acute or open angle glaucoma, untreated), myasthenia gravis, respiratory insufficiency, impaired pulmonary function, or severe hepatic impairment.
- History of any malignancy within the past 5 years. Exceptions are squamous and basal cell carcinomas of the skin and carcinoma in situ of the cervix, or malignancy which is considered cured with minimal risk of recurrence. Participants under evaluation for possible malignancy are not eligible.
- History of any reaction or hypersensitivity likely to be exacerbated by any component (formulation, capsule, or excipients) of the study intervention(s) (including hypromellose [hydroxypropyl methylcellulose] for GSK3772701) or allergies to cherries (as per MDZ USPI).
- Acute or chronic clinically significant pulmonary, endocrinological, cardiovascular, muscular, neurological, hepatic, or renal functional abnormality, as determined by physical examination or laboratory screening tests.
- Participants should have baseline clinical laboratory values (renal, hepatic, and hematological) within normal limits or clinically acceptable to the investigator. A participant with a clinical abnormality or laboratory parameter(s) which is/are not specifically listed in the inclusion or exclusion criteria, or outside the normal reference range for the population being studied, may be included only if the investigator considers that the finding is unlikely to introduce additional risk factors for the participant and will not interfere with the study procedures or endpoints.
- Participants with supine blood pressure (BP) >=140 mm Hg (systolic) or >=90 mm Hg (diastolic).
- Estimated glomerular filtration rate (eGFR) of <80 mL/min/1.73 m2 calculated using the Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI) Creatinine Equation (2021).
- The participant must agree to and adhere to the concomitant therapy (including non-drug therapies) restrictions from the Screening Visit through to the end of the study.
- Any other clinical condition that, in the opinion of the investigator, might pose an additional risk to the participant due to participation in the study or would make adhering to study procedures for the duration of the study difficult.
- Sensitivity to heparin or heparin-induced thrombocytopenia.
- Past or intended use of over-the-counter or prescription medication (including herbal medications, vitamins and supplements) within 7 days (or 14 days if the drug is a potential enzyme inducer), or 5 times the half-life (whichever is longer) prior to dosing.
- Treatment with biologic agents (such as monoclonal antibodies including marketed drugs) or investigational drugs or non-registered product (drug, vaccine, or medical device) within 3 months or 5 times the half-life (whichever is longer) prior to dosing.
- Exposure to more than 4 new chemical entities within 12 months prior to the first dosing day.
Current or prior enrolment in this or any other clinical study involving an investigational study intervention, or any other type of medical research, within the last 30 days or 5 half-lives, whichever is longer, prior to signing of the ICF.
Participants who screen fail for the current study are not eligible for re-screening or enrollment.
- Positive drug/alcohol screen, including tetrahydrocannabinol at Screening or Admission.
- Cotinine levels indicative of smoking or history or regular use of tobacco- or nicotine containing products within 6 months prior to Screening.
- Positive human immunodeficiency virus (HIV) antibody test.
- Regular alcohol consumption within 6 months prior to the clinical study defined as: An average weekly alcohol intake of 14 units for males or 7 units for females. One unit is equivalent to 8 g of alcohol: a half-pint. (approximately 240 mL) of beer, 1 glass (125 mL) of wine or 1 measure (25 mL) of spirits.
- Regular use of combustible tobacco products, and non-combustible nicotine delivery systems, inclusive of cigarettes, cigars, pipes, and materials used to "vape".
- Participants who have lost or donated over 500 mL of blood within 90 days prior to enrollment or intend to donate blood or blood products during the study.
- Participants who have donated plasma within 7 days prior to enrollment.
- Any study personnel or their immediate dependents, family, or household members.
- Regular use of known drugs of abuse, including tetrahydrocannabinol.
The following liver safety criteria are exclusionary:
- Alanine aminotransferase (ALT) >1.5 × the upper limit of normal (ULN).
- Total bilirubin >1.5 × ULN. Participants with Gilbert's syndrome can be included with total bilirubin >1.5 × ULN if direct bilirubin is <=1.5 × ULN.
- Current or chronic history of liver disease or known hepatic or biliary abnormalities (with the exception of Gilbert's syndrome or asymptomatic gallstones).
- Presence of hepatitis B surface antigen (HBsAg) and/or hepatitis B core antibody (HBcAb) at Screening or within 3 months prior to first dose of study intervention.
- Positive hepatitis C antibody test results at Screening or within 3 months prior to first dose of study intervention.
- Positive hepatitis C RNA test results at Screening or within 3 months prior to first dose of study intervention.
- QT interval corrected for heart rate according to Fridericia's formula (QTcF) >450 msec.
- The participant has congenital long QT syndrome or known prolongation of the QTc interval.
- The participant has a family history of QT prolongation or sudden death.
- The participant has any current or previous history of episodes of symptomatic bradycardia or bradyarrhythmia.
学习计划
研究是如何设计的?
设计细节
- 主要用途:基础科学
- 分配:非随机化
- 介入模型:单组作业
- 屏蔽:无(打开标签)
武器和干预
参与者组/臂 |
干预/治疗 |
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实验性的:Study participants
Healthy participants receive Midazolam (MDZ) on days 1, 3, 6 and 10, and GSK3772701 on days 3, 4 and 5.
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Participants receive MDZ orally.
Participants receive GSK3772701 orally.
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研究衡量的是什么?
主要结果指标
结果测量 |
大体时间 |
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Maximum observed concentration (Cmax) of MDZ
大体时间:At 0 hours (h) (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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At 0 hours (h) (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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Area under the concentration-time curve. from time 0 to the last measurable concentration [AUC(0-t)] of MDZ
大体时间:At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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Area under the plasma concentration-time curve from time 0 extrapolated to infinity [AUC(0-inf)] of MDZ
大体时间:At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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次要结果测量
结果测量 |
措施说明 |
大体时间 |
|---|---|---|
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Cmax of 1-hydroxymidazolam (OH-MDZ)
大体时间:At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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AUC(0-t) of 1-OH-MDZ
大体时间:At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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AUC(0-inf) of 1-OH-MDZ
大体时间:At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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Metabolite-to-parent ratios (1-OH-MDZ/MDZ) based on Cmax
大体时间:At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
|
|
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Metabolite-to-parent ratios (1-OH-MDZ/MDZ) based on AUC(0-t)
大体时间:At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
|
At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
|
|
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Metabolite-to-parent ratios (1-OH-MDZ/MDZ) based on AUC(0-inf)
大体时间:At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
|
At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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Time to maximum observed concentration (Tmax) of MDZ and 1-OH-MDZ
大体时间:At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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Terminal half-life (t1/2) of MDZ and 1-OH-MDZ
大体时间:At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
|
At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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Apparent oral plasma clearance (CL/F) of MDZ
大体时间:At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
|
At 0h (pre-dose) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose for each MDZ administration on days 1, 3, 6 and 10
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Cmax of GSK3772701
大体时间:At 0h (pre-dose) and at 0.5, 1, 2, 3, 4, 6, 12, 20 and 24 hours post-dose on days 3 and 5
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At 0h (pre-dose) and at 0.5, 1, 2, 3, 4, 6, 12, 20 and 24 hours post-dose on days 3 and 5
|
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AUC(0-t) of GSK3772701
大体时间:At 0h (pre-dose) and at 0.5, 1, 2, 3, 4, 6, 12, 20 and 24 hours post-dose on days 3 and 5
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At 0h (pre-dose) and at 0.5, 1, 2, 3, 4, 6, 12, 20 and 24 hours post-dose on days 3 and 5
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Area under the plasma concentration-time curve from time zero to 24 hours [AUC(0-24)] of GSK3772701
大体时间:At 0h (pre-dose) and at 0.5, 1, 2, 3, 4, 6, 12, 20 and 24 hours post-dose on days 3 and 5
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At 0h (pre-dose) and at 0.5, 1, 2, 3, 4, 6, 12, 20 and 24 hours post-dose on days 3 and 5
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Tmax of GSK3772701
大体时间:At 0h (pre-dose) and at 0.5, 1, 2, 3, 4, 6, 12, 20 and 24 hours post-dose on days 3 and 5
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At 0h (pre-dose) and at 0.5, 1, 2, 3, 4, 6, 12, 20 and 24 hours post-dose on days 3 and 5
|
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Concentration at 24 hours post dose (C24h) of GSK3772701
大体时间:At Day 4 pre-dose (24 hours post Day 3 dose), Day 5 pre-dose (24 hours post Day 4 dose) and Day 6 (24 hours post Day 5 dose)
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At Day 4 pre-dose (24 hours post Day 3 dose), Day 5 pre-dose (24 hours post Day 4 dose) and Day 6 (24 hours post Day 5 dose)
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Incidence of adverse events (AEs) overall, by severity and relationship to GSK3772701
大体时间:From Day 1 to Day 12
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An AE is defined as any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention.
The severity of AEs is determined by the investigator using the Division of Acquired Immunodeficiency Syndrome (DAIDS) Table for Grading of Severity of Adult and Pediatric Adverse Events, corrected version 2.1.
Grades are defined based on numeric criteria as follows Grade 1: mild; Grade 2: moderate; Grade 3: severe; Grade 4: potentially life-threatening; Grade 5: death.
Higher grades indicate greater severity.
The incidence rate describes the rate at which an event occurs.
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From Day 1 to Day 12
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Incidence of serious adverse events (SAEs) overall, by severity and relationship to GSK3772701
大体时间:From Day -30 to Day 12
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An SAE is defined as any untoward medical occurrence that results in death, is life-threatening, requires inpatient hospitalization or extends existing hospitalization, causes persistent or significant disability/incapacity, involves a congenital anomaly/birth defect in a participants offspring, includes an abnormal pregnancy outcome, or occurs in any other situation per the investigators judgement.
The severity of SAEs is determined by the investigator using the DAIDs Table for Grading of Severity of Adult and Pediatric Adverse Events, corrected version 2.1.
Grades are defined based on numeric criteria as follows Grade 1: mild; Grade 2: moderate; Grade 3: severe; Grade 4: potentially life-threatening; Grade 5: death.
Higher grades indicate greater severity.
The incidence rate describes the rate at which an event occurs.
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From Day -30 to Day 12
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合作者和调查者
研究记录日期
研究主要日期
学习开始 (实际的)
初级完成 (估计的)
研究完成 (估计的)
研究注册日期
首次提交
首先提交符合 QC 标准的
首次发布 (实际的)
研究记录更新
最后更新发布 (实际的)
上次提交的符合 QC 标准的更新
最后验证
更多信息
与本研究相关的术语
其他研究编号
- 300294
计划个人参与者数据 (IPD)
计划共享个人参与者数据 (IPD)?
IPD 计划说明
IPD 共享时间框架
IPD 共享访问标准
IPD 共享支持信息类型
- 研究方案
- 树液
- 国际碳纤维联合会
- 企业社会责任
药物和器械信息、研究文件
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