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FAK Inhibitor in Patients With Advanced Solid Tumors

12 mai 2026 mis à jour par: InxMed (Shanghai) Co., Ltd.

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

This is A Phase I/Ib Study,aimed 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.

Aperçu de l'étude

Statut

Pas encore de recrutement

Les conditions

Intervention / Traitement

Description détaillée

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.

Type d'étude

Interventionnel

Inscription (Estimé)

75

Phase

  • La phase 1

Contacts et emplacements

Cette section fournit les coordonnées de ceux qui mènent l'étude et des informations sur le lieu où cette étude est menée.

Coordonnées de l'étude

Sauvegarde des contacts de l'étude

  • Nom: xiaofang liu Project Manager, Bachelor
  • Numéro de téléphone: 86+13308303078
  • E-mail: xiaofang.liu@inxmed.com

Lieux d'étude

    • Zhejiang
      • Hangzhou, Zhejiang, Chine, 310005
        • Zhejiang Cancer Hospital
        • Contact:
          • zhengbo song Chief Physician, MD
          • Numéro de téléphone: 86-13857153345
          • E-mail: songzb@zjcc.org.cn

Critères de participation

Les chercheurs recherchent des personnes qui correspondent à une certaine description, appelée critères d'éligibilité. Certains exemples de ces critères sont l'état de santé général d'une personne ou des traitements antérieurs.

Critère d'éligibilité

Âges éligibles pour étudier

  • Adulte
  • Adulte plus âgé

Accepte les volontaires sains

Non

La description

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.

Plan d'étude

Cette section fournit des détails sur le plan d'étude, y compris la façon dont l'étude est conçue et ce que l'étude mesure.

Comment l'étude est-elle conçue ?

Détails de conception

  • Objectif principal: Traitement
  • Répartition: N / A
  • Modèle interventionnel: Affectation à un seul groupe
  • Masquage: Aucun (étiquette ouverte)

Armes et Interventions

Groupe de participants / Bras
Intervention / Traitement
Expérimental: 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.
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.

Que mesure l'étude ?

Principaux critères de jugement

Mesure des résultats
Description de la mesure
Délai
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).
Délai: Approximately 6 months
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).
Approximately 6 months

Mesures de résultats secondaires

Mesure des résultats
Description de la mesure
Délai
PK:AUC0-24h of IN10028
Délai: Approximately 6 months
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.
Approximately 6 months
PK: AUC0-t of IN10028
Délai: Approximately 6 months
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.
Approximately 6 months
PK: AUC0-∞ of IN10028
Délai: Approximately 6 months
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.
Approximately 6 months
PK: AUCextrap(%) of IN10028
Délai: Approximately 6 months
To evaluate percent of aucinf attributed to extrapolation (AUCextrap(%) )profile following single-dose and multiple-dose administration of IN10028.
Approximately 6 months
PK: Cmax of IN10028
Délai: Approximately 6 months
Maximum plasma concentration (Cmax) profile following single-dose administration of IN10028.
Approximately 6 months
PK: Tmax of IN10028
Délai: Approximately 6 months
Time to reach maximum plasma concentration (Tmax) profile following single-dose administration of IN10028.
Approximately 6 months
PK: t1/2 of IN10028
Délai: Approximately 6 months
Elimination half-life (t1/2) profile following single-dose and multiple-dose administration of IN10028.
Approximately 6 months
PK: λz of IN10028
Délai: Approximately 6 months
Terminal elimination rate constant (λz) profile following single-dose and multiple-dose administration of IN10028.
Approximately 6 months
PK: Vz/F of IN10028
Délai: Approximately 6 months
Apparent volume of distribution during the terminal phase(Vz/F) following single-dose administration of IN10028.
Approximately 6 months
PK: CL/F of IN10028
Délai: Approximately 6 months
Apparent total clearance during the elimination phase(CL/F) following single-dose administration of IN10028.
Approximately 6 months
PK: Cmax,ss of IN10028
Délai: Approximately 6 months
To evaluate the maximum steady-state plasma drug concentration(Cmax,ss)following the multiple-dose administration of IN10028.
Approximately 6 months
PK: Cmin,ss of IN10028
Délai: Approximately 6 months
To evaluate the minimum steady-state plasma drug concentration(Cmin,ss)following the multiple-dose administration of IN10028.
Approximately 6 months
PK: Cav,ss of IN10028
Délai: Approximately 6 months
To evaluate the average steady-state plasma drug concentration(Cav,ss)following the multiple-dose administration of IN10028.
Approximately 6 months
PK: AUC0-tau of IN10028
Délai: Approximately 6 months
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.
Approximately 6 months
PK: CLss/F of IN10028
Délai: Approximately 6 months
To evaluate the apparent total clearance at steady state (CLss/F) following the multiple-dose administration of IN10028.
Approximately 6 months
PK: Vz,ss/F of IN10028
Délai: Approximately 6 months
To evaluate the apparent steady-state volume of distribution during the terminal phase (Vz,ss/F) following the multiple-dose administration of IN10028.
Approximately 6 months
PK: Flu% of IN10028
Délai: Approximately 6 months
To evaluate the percentage of fluctuation at steady state (Flu%) following the multiple-dose administration of IN10028.
Approximately 6 months
PK: Rac of IN10028
Délai: Approximately 6 months
To evaluate the percent fluctuation at steady state (Rac) following the multiple-dose administration of IN10028.
Approximately 6 months
To evaluate the rate of Objective Response Rate (ORR) of IN10028 in solid tumors.
Délai: Approximately 1 year
Defined as the proportion of subjects with complete response (CR) or partial response (PR).
Approximately 1 year
To evaluate the time of Duration of Response (DoR) of IN10028 in solid tumors.
Délai: Approximately 1 year
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.
Approximately 1 year
To evaluate the rate of Disease Control Rate (DCR) of IN10028 in solid tumors.
Délai: Approximately 1 year
Defined as the proportion of patients with CR, PR, or stable disease (SD).
Approximately 1 year
To evaluate the Time To Response (TTR) of IN10028 in solid tumors.
Délai: Approximately 1 year
To preliminarily evaluate the antitumor activity of IN10028 time to response (TTR).
Approximately 1 year
To evaluate the duration of Progression-free Survival (PFS) of IN10028 in solid tumors.
Délai: Approximately 1 year
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.
Approximately 1 year
To Evaluate the duration of Overall survival (OS) of IN10028 in solid tumors.
Délai: Approximately 1 year
Defined as the time from the first dose of study treatment to the date of death due to any cause.
Approximately 1 year

Collaborateurs et enquêteurs

C'est ici que vous trouverez les personnes et les organisations impliquées dans cette étude.

Dates d'enregistrement des études

Ces dates suivent la progression des dossiers d'étude et des soumissions de résultats sommaires à ClinicalTrials.gov. Les dossiers d'étude et les résultats rapportés sont examinés par la Bibliothèque nationale de médecine (NLM) pour s'assurer qu'ils répondent à des normes de contrôle de qualité spécifiques avant d'être publiés sur le site Web public.

Dates principales de l'étude

Début de l'étude (Estimé)

30 mai 2026

Achèvement primaire (Estimé)

28 février 2027

Achèvement de l'étude (Estimé)

28 février 2028

Dates d'inscription aux études

Première soumission

1 mai 2026

Première soumission répondant aux critères de contrôle qualité

12 mai 2026

Première publication (Réel)

19 mai 2026

Mises à jour des dossiers d'étude

Dernière mise à jour publiée (Réel)

19 mai 2026

Dernière mise à jour soumise répondant aux critères de contrôle qualité

12 mai 2026

Dernière vérification

1 mai 2026

Plus d'information

Termes liés à cette étude

Autres numéros d'identification d'étude

  • IN10028-001

Plan pour les données individuelles des participants (IPD)

Prévoyez-vous de partager les données individuelles des participants (DPI) ?

NON

Informations sur les médicaments et les dispositifs, documents d'étude

Étudie un produit pharmaceutique réglementé par la FDA américaine

Non

Étudie un produit d'appareil réglementé par la FDA américaine

Non

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