FAK Inhibitor in Patients With Advanced Solid Tumors
A Phase I/Ib Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Preliminary Antitumor Efficacy of Focal Adhesion Kinase Inhibitor IN10028 as Monotherapy and Combination Therapy in Patients With Advanced Solid Tumors
研究概览
详细说明
Same-target drugs of IN10028 include Ifebemtinib (a first-generation focal adhesion kinase [FAK] inhibitor), defactinib (Verastem Oncology), VS-4748 (Verastem Oncology), and GSK2256098 (GlaxoSmithKline [GSK] plc). IN10028 is a potent, highly selective, orally available second-generation focal adhesion kinase (FAK, also known as protein tyrosine kinase 2 [PTK2]) inhibitor . It binds to the kinase domain of FAK to block activation of downstream oncogenic PI3K/AKT and RAS/MAPK signaling pathways, thus suppressing tumor cell proliferation, inducing apoptosis, and markedly attenuating tumor cell migration and invasion.Based on the clinically validated target value of the first-generation FAK inhibitor Ifebemtinib (Ifebe, IN10018, original development code BI 853520) and its associated limitation of proteinuria, IN10028 has been specifically optimized to achieve more potent target inhibition and a potentially superior safety profile. Given the well-established clinical value of the FAK target and successful clinical experience with other same-target agents,there is a robust, well-supported clinical development rationale for IN10028.
A Phase I/Ib clinical trial is planned by the sponsor to evaluate the safety, tolerability, pharmacokinetics, and preliminary antitumor activity of FAK inhibitor IN10028 as monotherapy and in combination with other anticancer agents in patients with advanced solid tumors.
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:jack zhang Clinical Trial Manager, bachelor
- 邮箱:jack.zhang@inxmed.com
研究联系人备份
- 姓名:xiaofang liu Project Manager, Bachelor
- 电话号码:86+13308303078
- 邮箱:xiaofang.liu@inxmed.com
学习地点
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Zhejiang
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Hangzhou、Zhejiang、中国、310005
- Zhejiang Cancer Hospital
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接触:
- zhengbo song Chief Physician, MD
- 电话号码:86-13857153345
- 邮箱:songzb@zjcc.org.cn
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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:
- Able to understand and voluntarily sign the written Informed Consent Form (ICF), which must be signed prior to conducting the study-specific procedures required by the trial.
- At the time of signing the ICF, subjects are aged 18 to 75 years, inclusive, male and female.
- Subjects must have a histologically or cytologically confirmed diagnosis of advanced or metastatic malignant solid tumor.Monotherapy dose-escalation and dose expansion: Patients with solid tumors who failed prior standard systemic therapy, have no standard treatment options, or are intolerant to standard regimens.
- Prior systemic antitumor therapy must be completed at least 3 weeks before the first study drug treatment; prior small molecule TKIs or oral fluoropyrimidines require a minimum 2-week washout period.
- Subjects must have at least one measurable tumor lesion per RECIST v1.1. Previously irradiated lesions should not be selected as target lesions, unless such irradiated lesion is the only measurable lesion and has documented radiological disease progression, and may then be selected as a target lesion.
- Eastern Cooperative Oncology Group (ECOG) performance status score of 0 or 1.
- Subjects have an estimated expected survival time of at least 3 months.
- Has adequate organ function.
- Urine protein negative or trace (±); or urine protein 1+, but urine protein to creatinine ratio (UPCR) of random morning urine < 0.5, or 24-hour urine protein quantitation < 0.5 g/24 h.
- Female subjects of childbearing potential must have a negative serum pregnancy test and agree to use effective contraception during the study drug treatment period and for 120 days after the last dose of study drug administration. Male subjects with female partners of childbearing potential must agree to use effective contraception during the study drug treatment period and for 120 days after the last dose of study drug administration. In this protocol, a woman of childbearing potential is defined as a sexually mature female.
Exclusion Criteria:
- Subjects unable to receive oral administration or with conditions that severely affect drug digestion and absorption (e.g., subtotal gastrectomy or duodenectomy, severe sinus tract affecting digestion and absorption, and other related diseases.
- Subjects with known central nervous system (CNS) metastases, excluding those with asymptomatic CNS metastases or asymptomatic brain metastases following prior treatment, provided that the lesions have been confirmed to be stable for more than 3 months by computed tomography (CT) or magnetic resonance imaging (MRI), and no steroid therapy has been required for at least 4 weeks.
- Subjects with known hypersensitivity to any components of the study drug or its analogues.
- Subjects with prior treatment of focal adhesion kinase inhibitors (FAKi).
- Subjects with a history of any other malignancy within 5 years prior to screening, excluding cured cervical carcinoma in situ and completely resected basal cell carcinoma of the skin.
- Subjects with uncontrolled cardiac clinical symptoms or diseases, including:(1) Heart failure classified as New York Heart Association (NYHA) Class Ⅱ or above; (2) unstableangina; (3) Myocardial infarction within the past 1 year;(4) Clinically significant supraventricular or ventricular arrhythmia requiring treatment or intervention; (5) Corrected QT interval (QTc) > 450 ms in males and QTc > 470 ms in females. The QTc interval is calculated using Fridericia's correction formula: QTcF = QT/(RR^0.33); (6) Left ventricular ejection fraction (LVEF) < 50%.
- Subjects with known hereditary or acquired bleeding and thrombotic predispositions (e.g., hemophilia, coagulation disorders, thrombocytopenia, etc.)
- Subjects with an active infection within 4 weeks prior to enrollment, or those with other chronic medical conditions deemed unsuitable for study participation by the Investigator.
- Subjects with congenital or acquired immunodeficiency disorders (e.g., human immunodeficiency virus [HIV] infection), or those with a history of organ transplantation.
- Hepatitis B surface antigen (HBsAg) positive with hepatitis B virus DNA (HBV DNA) ≥ 2500 copies/mL (or 500 IU/mL); or positive for hepatitis C virus RNA (HCV RNA).
- Have received a live vaccine within 30 days prior to the first dose of administration.
- Women of childbearing potential who are pregnant-planning or lactating.
- Subjects who are inability to comply with protocol requirements or who is otherwise considered unsuitable for study participation by the investigator's judgment.
- Subjects receiving concomitant intravenous or oral medications that affect CYP isoenzymes (strong inducers or strong inhibitors of CYP3A4), or who have used such medications within at least 1 week prior to the first dose of administration.
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:IN10028
The monotherapy dose-escalation will adopt an accelerated titration design combined with the conventional 3+3 dose-escalation method.
The starting dose of IN10028 is 25 mg, with a total of 5 planned dose cohorts: 25 mg, 50 mg, 100 mg, 200 mg and 300 mg, administered orally once daily (QD) continuously.The DLT observation period is 14 days at the 25 mg dose level, and 21 days at the 50 mg, 100 mg, 200 mg and 300 mg dose levels, respectively.
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The starting dose of IN10028 is 25 mg, with a total of 5 planned dose cohorts: 25 mg, 50 mg, 100 mg, 200 mg and 300 mg, administered orally once daily (QD) continuously with a cycle of 21 days.
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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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To explore the incidence of dose-limiting toxicities (DLTs) of IN10028, identify the maximum tolerated dose (MTD), and determine the recommended phase 2 dose (RP2D).
大体时间:Approximately 6 months
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To evaluate the safety and tolerability of IN10028 in patients with advanced malignant solid tumors, characterize the incidence of dose limiting toxicities (DLTs), identify the maximum tolerated dose (MTD), and determine the recommended phase 2 dose (RP2D).
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Approximately 6 months
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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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PK:AUC0-24h of IN10028
大体时间:Approximately 6 months
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To evaluate area under the plasma concentration-time curve from 0 to 24 hours (AUC0-24h) profile following single- and multiple-dose administration of IN10028.
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Approximately 6 months
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PK: AUC0-t of IN10028
大体时间:Approximately 6 months
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To evaluate the area under the plasma concentration-time curve from 0 to the last measurable time point (AUC₀-t) profile following single- and multiple-dose administration of IN10028.
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Approximately 6 months
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PK: AUC0-∞ of IN10028
大体时间:Approximately 6 months
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To evaluate area under the plasma concentration-time curve from time 0 to infinity (AUC₀-∞) profile following single-dose and multiple-dose dosing of IN10028.
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Approximately 6 months
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PK: AUCextrap(%) of IN10028
大体时间:Approximately 6 months
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To evaluate percent of aucinf attributed to extrapolation (AUCextrap(%) )profile following single-dose and multiple-dose administration of IN10028.
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Approximately 6 months
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PK: Cmax of IN10028
大体时间:Approximately 6 months
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Maximum plasma concentration (Cmax) profile following single-dose administration of IN10028.
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Approximately 6 months
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PK: Tmax of IN10028
大体时间:Approximately 6 months
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Time to reach maximum plasma concentration (Tmax) profile following single-dose administration of IN10028.
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Approximately 6 months
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PK: t1/2 of IN10028
大体时间:Approximately 6 months
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Elimination half-life (t1/2) profile following single-dose and multiple-dose administration of IN10028.
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Approximately 6 months
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PK: λz of IN10028
大体时间:Approximately 6 months
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Terminal elimination rate constant (λz) profile following single-dose and multiple-dose administration of IN10028.
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Approximately 6 months
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PK: Vz/F of IN10028
大体时间:Approximately 6 months
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Apparent volume of distribution during the terminal phase(Vz/F) following single-dose administration of IN10028.
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Approximately 6 months
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PK: CL/F of IN10028
大体时间:Approximately 6 months
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Apparent total clearance during the elimination phase(CL/F) following single-dose administration of IN10028.
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Approximately 6 months
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PK: Cmax,ss of IN10028
大体时间:Approximately 6 months
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To evaluate the maximum steady-state plasma drug concentration(Cmax,ss)following the multiple-dose administration of IN10028.
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Approximately 6 months
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PK: Cmin,ss of IN10028
大体时间:Approximately 6 months
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To evaluate the minimum steady-state plasma drug concentration(Cmin,ss)following the multiple-dose administration of IN10028.
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Approximately 6 months
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PK: Cav,ss of IN10028
大体时间:Approximately 6 months
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To evaluate the average steady-state plasma drug concentration(Cav,ss)following the multiple-dose administration of IN10028.
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Approximately 6 months
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PK: AUC0-tau of IN10028
大体时间:Approximately 6 months
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To evaluate the time-concentration curve from time zero to the end of the dosing interval (tau)(AUC0-tau)following the multiple-dose administration of IN10028.
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Approximately 6 months
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PK: CLss/F of IN10028
大体时间:Approximately 6 months
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To evaluate the apparent total clearance at steady state (CLss/F) following the multiple-dose administration of IN10028.
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Approximately 6 months
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PK: Vz,ss/F of IN10028
大体时间:Approximately 6 months
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To evaluate the apparent steady-state volume of distribution during the terminal phase (Vz,ss/F) following the multiple-dose administration of IN10028.
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Approximately 6 months
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PK: Flu% of IN10028
大体时间:Approximately 6 months
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To evaluate the percentage of fluctuation at steady state (Flu%) following the multiple-dose administration of IN10028.
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Approximately 6 months
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PK: Rac of IN10028
大体时间:Approximately 6 months
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To evaluate the percent fluctuation at steady state (Rac) following the multiple-dose administration of IN10028.
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Approximately 6 months
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To evaluate the rate of Objective Response Rate (ORR) of IN10028 in solid tumors.
大体时间:Approximately 1 year
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Defined as the proportion of subjects with complete response (CR) or partial response (PR).
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Approximately 1 year
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To evaluate the time of Duration of Response (DoR) of IN10028 in solid tumors.
大体时间:Approximately 1 year
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Defined as the time from start of the first documentation of CR or PR to the first documentation of disease progression or to death due to any cause, whichever comes first.
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Approximately 1 year
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To evaluate the rate of Disease Control Rate (DCR) of IN10028 in solid tumors.
大体时间:Approximately 1 year
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Defined as the proportion of patients with CR, PR, or stable disease (SD).
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Approximately 1 year
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To evaluate the Time To Response (TTR) of IN10028 in solid tumors.
大体时间:Approximately 1 year
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To preliminarily evaluate the antitumor activity of IN10028 time to response (TTR).
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Approximately 1 year
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To evaluate the duration of Progression-free Survival (PFS) of IN10028 in solid tumors.
大体时间:Approximately 1 year
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Defined as the time from the first dose of study treatment to first documentation of disease progression or to death due to any cause, whichever comes first.
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Approximately 1 year
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To Evaluate the duration of Overall survival (OS) of IN10028 in solid tumors.
大体时间:Approximately 1 year
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Defined as the time from the first dose of study treatment to the date of death due to any cause.
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Approximately 1 year
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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
与本研究相关的术语
其他研究编号
- IN10028-001
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