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
調査の概要
詳細な説明
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.
研究の種類
入学 (推定)
段階
- フェーズ 1
連絡先と場所
研究連絡先
- 名前:jack zhang Clinical Trial Manager, bachelor
- メール:jack.zhang@inxmed.com
研究連絡先のバックアップ
- 名前:xiaofang liu Project Manager, Bachelor
- 電話番号:86+13308303078
- メール:xiaofang.liu@inxmed.com
研究場所
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Zhejiang
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Hangzhou、Zhejiang、中国、310005
- Zhejiang Cancer Hospital
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コンタクト:
- zhengbo song Chief Physician, MD
- 電話番号:86-13857153345
- メール:songzb@zjcc.org.cn
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参加基準
適格基準
就学可能な年齢
- 大人
- 高齢者
健康ボランティアの受け入れ
説明
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.
研究計画
研究はどのように設計されていますか?
デザインの詳細
- 主な目的:処理
- 割り当て:なし
- 介入モデル:単一グループの割り当て
- マスキング:なし(オープンラベル)
武器と介入
参加者グループ / アーム |
介入・治療 |
|---|---|
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実験的: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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この研究は何を測定していますか?
主要な結果の測定
結果測定 |
メジャーの説明 |
時間枠 |
|---|---|---|
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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).
時間枠: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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二次結果の測定
結果測定 |
メジャーの説明 |
時間枠 |
|---|---|---|
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PK:AUC0-24h of IN10028
時間枠: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
時間枠: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
時間枠: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
時間枠: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
時間枠: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
時間枠: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
時間枠: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
時間枠: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
時間枠: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
時間枠: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
時間枠: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
時間枠: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
時間枠: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
時間枠: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
時間枠: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
時間枠: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
時間枠: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
時間枠: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.
時間枠: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.
時間枠: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.
時間枠: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.
時間枠: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.
時間枠: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.
時間枠: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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協力者と研究者
研究記録日
主要日程の研究
研究開始 (推定)
一次修了 (推定)
研究の完了 (推定)
試験登録日
最初に提出
QC基準を満たした最初の提出物
最初の投稿 (実際)
学習記録の更新
投稿された最後の更新 (実際)
QC基準を満たした最後の更新が送信されました
最終確認日
詳しくは
本研究に関する用語
その他の研究ID番号
- IN10028-001
個々の参加者データ (IPD) の計画
個々の参加者データ (IPD) を共有する予定はありますか?
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