An Open-label, Fixed-sequence Phase I Clinical Trial to Evaluate the Effect of HS-10504 on the Pharmacokinetics of Midazolam in Patients With Non-small Cell Lung Cancer
研究概览
详细说明
This study consists of two stages: Stage 1 (DDI evaluation period, C0D1 to C2D21) and Stage 2 (drug donation period, from C3D1 onward). Each cycle contains 21 days, except for Cycle 0.
Stage 1 (DDI evaluation period, C0D1 to C2D21): Enrolled participants receive a single oral dose of midazolam oral solution 1 mg (2 mg/mL, 0.5 mL) on C0D1 and C2D20, respectively; and receive HS-10504 tablets 400 mg (100 mg/tablet, 4 tablets) once daily from C1D1 to C2D21.
Stage 2 (drug donation period, from C3D1 onward): After completing Stage 1, participants may decide, based on the investigator's judgment and their own willingness, whether to enter Stage 2 (the extended drug donation period, which is optional and not mandatory). This stage continues until the participant voluntarily requests discontinuation, is lost to follow-up, experiences disease progression, develops intolerable toxicity, is judged by the investigator to no longer derive benefit from the treatment, or the drug has been approved for marketing, whichever occurs first.
研究类型
注册 (估计的)
阶段
- 阶段1
参与标准
资格标准
适合学习的年龄
- 成人
- 年长者
接受健康志愿者
描述
Inclusion Criteria:
- Histologically or cytologically confirmed locally advanced or metastatic NSCLC
- Disease progression or intolerance to prior third-generation EGFR TKI therapy in patients with mNSCLC
- Confirmed EGFR mutation positivity in participants before enrollment.
- At least one target lesion according to RECIST 1.1
- Eastern Cooperative Oncology Group (ECOG) performance status (PS) 0-1 with no deterioration in the 2 weeks prior to the first dose
- Minimum life expectancy greater than 12 weeks
- Female participants of childbearing potential must agree to use appropriate contraception (refer to section 12.5) from the time of signing informed consent until 6 months after the last dose, and should not breastfeed; male participants must agree to use barrier contraception (i.e., condoms) from the time of signing informed consent until 6 months after the last dose
- Willing to participate in this clinical trial, understand the study procedures, and be able to provide written informed consent.
Exclusion Criteria:
Has received or is currently receiving the following treatments:
- Prior or current treatment with a fourth-generation EGFR tyrosine kinase inhibitor.
- Use of strong/moderate inhibitors or strong/moderate inducers of CYP3A4, CYP3A5, CYP2C8, and/or CYP2D6, or narrow therapeutic index drugs that are sensitive substrates of CYP3A4, CYP3A5, P-gp, and BCRP within 14 days or 5 half-lives (whichever is longer) prior to the first dose of investigational product; or need to continue these medications during the study period.
- Use of drugs that affect gastric acid secretion or intragastric pH within 7 days prior to the first dose of investigational product.
- Currently receiving treatment with drugs known to prolong the QT interval or that may cause torsade de pointes; or need to continue these medications during the study period
- Presence of toxicities from prior anti-tumor therapy that have not resolved to < Grade 2 according to the Common Terminology Criteria for Adverse Events (CTCAE) version 5.0.
- History of other primary malignancies.
- Inadequate bone marrow reserve or hepatic/renal organ function.
Meets any of the following cardiac criteria:
- Mean Fridericia-corrected QT interval (QTcF) > 470 msec on resting electrocardiogram (ECG);
- Resting ECG shows any clinically significant rhythm, conduction, or ECG morphological abnormality deemed important by the investigator (e.g., complete left bundle branch block, third-degree atrioventricular block, second-degree atrioventricular block, and PR interval > 250 msec, etc.);
- Presence of any factors that increase the risk of QT prolongation or arrhythmic events, such as heart failure, refractory hypokalemia, congenital long QT syndrome, family history of long QT syndrome, unexplained sudden death in a first-degree relative under 40 years of age, or any concomitant medication that prolongs the QT interval;
- Left ventricular ejection fraction (LVEF) < 50%.
- Severe, uncontrolled, or active cardiovascular disease.
- Severe or poorly controlled diabetes mellitus.
- Severe or poorly controlled hypertension.
- Clinically significant bleeding symptoms or obvious bleeding tendency within 1 month prior to the first dose.
- Severe arterial thrombotic event within 3 months prior to the first dose.
- Severe infection within 4 weeks prior to the first dose.
- Continuous corticosteroid therapy for more than 30 days within 30 days prior to the first dose, or need for long-term corticosteroid therapy, or other acquired or congenital immunodeficiency diseases, or history of organ transplantation
- Known active infectious disease.
- Clinically severe gastrointestinal abnormalities that may affect drug intake, transport, or absorption.
- Hepatic encephalopathy, hepatorenal syndrome, or ≥C (incomplete in original).
- Other moderate to severe pulmonary diseases that seriously impair respiratory function and may interfere with the detection or management of drug-related pulmonary toxicity.
- Previous history of severe neurological or psychiatric disorders.
- Female participants who are pregnant, breastfeeding, or planning to become pregnant during the study period.
- History of severe allergies, or hypersensitivity to any component of HS-10504 tablets or midazolam oral solution, or history of hypersensitivity to drugs with a similar chemical structure or of the same class as HS-10504.
- History of ventilation difficulty or severe airway obstruction.
- Any severe or uncontrolled ocular condition that, in the physician's judgment, may increase the patient's risk; or ocular abnormalities requiring surgery or expected to require surgical treatment during the study period.
- Participants who, in the investigator's judgment, may have poor compliance with study procedures and requirements.
- In the investigator's judgment, presence of any life-threatening complication.
学习计划
研究是如何设计的?
设计细节
- 主要用途:治疗
- 分配:不适用
- 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:实验组
药物相互作用组
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HS-10504:Participants receive HS-10504 tablets 400 mg (100 mg/tablet, 4 tablets) once daily Midazolam:Participants receive a single oral dose of midazolam oral solution 1 mg (2 mg/mL, 0.5 mL) on C0D1 and C2D20, respectively。
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研究衡量的是什么?
主要结果指标
结果测量 |
措施说明 |
大体时间 |
|---|---|---|
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Evaluation of PK parameters of Midazolam: Cmax
大体时间:24 hours after administration of Midazolam
|
To evaluate the Cmax of Midazolam administered alone and in combination with HS-10504
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24 hours after administration of Midazolam
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Evaluation of PK parameters of Midazolam: AUC0-t
大体时间:24 hours after administration of Midazolam
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To evaluate the AUC0-t of Midazolam administered alone and in combination with HS-10504
|
24 hours after administration of Midazolam
|
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Evaluation of PK parameters of Midazolam: AUC0-∞
大体时间:24 hours after administration of Midazolam
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To evaluate the AUC0-∞ of Midazolam administered alone and in combination with HS-10504
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24 hours after administration of Midazolam
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次要结果测量
结果测量 |
措施说明 |
大体时间 |
|---|---|---|
|
Evaluation of PK parameters of Midazolam: Tmax
大体时间:24 hours after administration of Midazolam
|
To evaluate the Tmax of Midazolam administered alone and in combination with HS-10504
|
24 hours after administration of Midazolam
|
|
Evaluation of PK parameters of Midazolam: t1/2z
大体时间:24 hours after administration of Midazolam
|
To evaluate the t1/2z of Midazolam administered alone and in combination with HS-10504
|
24 hours after administration of Midazolam
|
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Evaluation of PK parameters of Midazolam: λz
大体时间:24 hours after administration of Midazolam
|
To evaluate the λz of Midazolam administered alone and in combination with HS-10504
|
24 hours after administration of Midazolam
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Evaluation of PK parameters of Midazolam: CLz/F
大体时间:24 hours after administration of Midazolam
|
To evaluate the CLz/F of Midazolam administered alone and in combination with HS-10504
|
24 hours after administration of Midazolam
|
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Evaluation of PK parameters of Midazolam: Vz/F.
大体时间:24 hours after administration of Midazolam
|
To evaluate the Vz/F of Midazolam administered alone and in combination with HS-10504
|
24 hours after administration of Midazolam
|
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Evaluation of PK parameters of 1-OH Midazolam: Cmax
大体时间:24 hours after administration of Midazolam
|
To evaluate the Cmax of 1-OH Midazolam administered alone and in combination with HS-10504
|
24 hours after administration of Midazolam
|
|
Evaluation of PK parameters of 1-OH Midazolam: AUC0-t
大体时间:24 hours after administration of Midazolam
|
To evaluate the AUC0-t of 1-OH Midazolam administered alone and in combination with HS-10504
|
24 hours after administration of Midazolam
|
|
Evaluation of PK parameters of 1-OH Midazolam: AUC0-∞
大体时间:24 hours after administration of Midazolam
|
To evaluate the AUC0-∞ of 1-OH Midazolam administered alone and in combination with HS-10504
|
24 hours after administration of Midazolam
|
|
Evaluation of PK parameters of 1-OH Midazolam: Tmax
大体时间:24 hours after administration of Midazolam
|
To evaluate the Tmax of 1-OH Midazolam administered alone and in combination with HS-10504
|
24 hours after administration of Midazolam
|
|
Evaluation of PK parameters of 1-OH Midazolam: t1/2z.
大体时间:24 hours after administration of Midazolam
|
To evaluate the t1/2z of 1-OH Midazolam administered alone and in combination with HS-10504
|
24 hours after administration of Midazolam
|
|
Evaluation of PK parameters of HS-10504 and metabolite M6-2: Cmin
大体时间:24 hours after administration of HS-10504
|
To evaluate the Cmin of HS-10504 and metabolite M6-2
|
24 hours after administration of HS-10504
|
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Evaluation of PK parameters of HS-10504 and metabolite M6-2: Cmax
大体时间:24 hours after administration of HS-10504
|
To evaluate the Cmax of HS-10504 and metabolite M6-2
|
24 hours after administration of HS-10504
|
|
Evaluation of PK parameters of HS-10504 and metabolite M6-2: AUC0-24 h
大体时间:24 hours after administration of HS-10504
|
To evaluate the AUC0-24 h of HS-10504 and metabolite M6-2
|
24 hours after administration of HS-10504
|
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Evaluation of PK parameters of HS-10504 and metabolite M6-2: Tmax.
大体时间:24 hours after administration of HS-10504
|
To evaluate the Tmax of HS-10504 and metabolite M6-2
|
24 hours after administration of HS-10504
|
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Adverse events
大体时间:through study completion, an average of 43 days
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To evaluate the adverse events (AEs) of Midazolam administered alone and in combination with HS-10504.
|
through study completion, an average of 43 days
|
|
blood pressure
大体时间:through study completion, an average of 43 days
|
To evaluate the blood pressure of Midazolam administered alone and in combination with HS-10504.
|
through study completion, an average of 43 days
|
|
Pulse
大体时间:through study completion, an average of 43 days
|
To evaluate the Puls of Midazolam administered alone and in combination with HS-10504.
|
through study completion, an average of 43 days
|
|
body temperature
大体时间:through study completion, an average of 43 days
|
To evaluate the body temperature of Midazolam administered alone and in combination with HS-10504.
|
through study completion, an average of 43 days
|
|
respiratory rate
大体时间:through study completion, an average of 43 days
|
To evaluate the respiratory rate of Midazolam administered alone and in combination with HS-10504.
|
through study completion, an average of 43 days
|
|
complete blood count (CBC)
大体时间:through study completion, an average of 43 days
|
To evaluate the complete blood count (CBC) of Midazolam administered alone and in combination with HS-10504.
|
through study completion, an average of 43 days
|
|
urinalysis
大体时间:through study completion, an average of 43 days
|
To evaluate the urinalysis of Midazolam administered alone and in combination with HS-10504.
|
through study completion, an average of 43 days
|
|
blood chemistry
大体时间:through study completion, an average of 43 days
|
To evaluate the blood chemistry of Midazolam administered alone and in combination with HS-10504.
|
through study completion, an average of 43 days
|
|
coagulation tests
大体时间:through study completion, an average of 43 days
|
To evaluate the coagulation tests of Midazolam administered alone and in combination with HS-10504.
|
through study completion, an average of 43 days
|
|
12-lead electrocardiogram(heart rate)
大体时间:through study completion, an average of 43 days
|
To evaluate the 12-lead electrocardiogram(heart rate) of Midazolam administered alone and in combination with HS-10504
|
through study completion, an average of 43 days
|
|
12-lead electrocardiogram(PR)
大体时间:through study completion, an average of 43 days
|
To evaluate the 12-lead electrocardiogram(PR) of Midazolam administered alone and in combination with HS-10504
|
through study completion, an average of 43 days
|
|
12-lead electrocardiogram(RR)
大体时间:through study completion, an average of 43 days
|
To evaluate the 12-lead electrocardiogram(RR) of Midazolam administered alone and in combination with HS-10504
|
through study completion, an average of 43 days
|
|
12-lead electrocardiogram(QRS duration)
大体时间:through study completion, an average of 43 days
|
To evaluate the 12-lead electrocardiogram(QRS duration) of Midazolam administered alone and in combination with HS-10504
|
through study completion, an average of 43 days
|
|
12-lead electrocardiogram(QTcF)
大体时间:through study completion, an average of 43 days
|
To evaluate the 12-lead electrocardiogram(QTcF) of Midazolam administered alone and in combination with HS-10504
|
through study completion, an average of 43 days
|
|
physical examination of Midazolam administered alone and in combination with HS-10504.
大体时间:through study completion, an average of 43 days
|
To evaluate the abnormal of the physical examination(1) Eyes; 2) Ear, nose, throat; 3) Cardiovascular system; 4) Chest and respiratory system; 5) Abdominal examination; 6) Skin and mucous membranes; 7) Spine and limbs; 8) Musculoskeletal system; 9) Nervous system; 10) Lymph nodes; 11) Genitourinary system; 12) Others.) of Midazolam administered alone and in combination with HS-10504.
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through study completion, an average of 43 days
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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 (估计的)
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
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