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    DRUG:

    ifebemtinib (IN10018)

    i
    Company:
    Boehringer Ingelheim, InxMed
    Drug class:
    FAK inhibitor
    Related drugs:
    10d
    Study to Evaluate D-1553 in Combination With IN10018 in Subjects With Solid Tumors (clinicaltrials.gov)
    P1/2, N=92, Active, not recruiting, InventisBio Co., Ltd | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    garsorasib (D-1553) • ifebemtinib (IN10018)
    1m
    Targeting FAK improves the tumor uptake of antibody-drug conjugates to strengthen the anti-cancer responses. (PubMed, iScience)
    Antibody-drug conjugates (ADCs), exemplified by HER2-targeted Enhertu and TROP2-targeted Trodelvy, have demonstrated significant therapeutic potential in cancers. Combination therapy with IN10018 and ADCs targeting either HER2 or TROP2 consistently yielded superior antitumor outcomes compared to monotherapies in animal models. These findings provide compelling preclinical evidence supporting the clinical evaluation of IN10018 in combination with ADCs.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    Enhertu (fam-trastuzumab deruxtecan-nxki) • Trodelvy (sacituzumab govitecan-hziy) • ifebemtinib (IN10018)
    2ms
    HX009+ IN10018 with or Without Standard Chemotherapy for Advanced Solid Tumours (clinicaltrials.gov)
    P1/2, N=124, Recruiting, Hangzhou Hanx Biopharmaceuticals, Ltd. | Not yet recruiting --> Recruiting | Trial completion date: Dec 2027 --> Dec 2028 | Trial primary completion date: Dec 2025 --> Dec 2027
    Enrollment open • Trial completion date • Trial primary completion date
    |
    ifebemtinib (IN10018) • HX-009
    5ms
    IN10018 Monotherapy and Combination Therapy for Metastatic Melanoma (clinicaltrials.gov)
    P1, N=120, Active, not recruiting, InxMed (Shanghai) Co., Ltd. | Recruiting --> Active, not recruiting | Trial completion date: Sep 2024 --> Dec 2025 | Trial primary completion date: Jun 2024 --> Jun 2025
    Enrollment closed • Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation • NRAS Q61 • NRAS G12 • NRAS G13
    |
    Tecentriq (atezolizumab) • Cotellic (cobimetinib) • ifebemtinib (IN10018)
    5ms
    HX009+ IN10018 With or Without Standard Chemotherapy for Advanced Solid Tumours (clinicaltrials.gov)
    P1/2, N=124, Not yet recruiting, Hangzhou Hanx Biopharmaceuticals, Ltd.
    New P1/2 trial • Metastases
    |
    ifebemtinib (IN10018) • HX-009
    6ms
    IN10018 with Nab-Paclitaxel and Cadonilimab for Metastatic or Recurrent Gastric-Type Cervical Adenocarcinoma: Phase 2 Trial (clinicaltrials.gov)
    P2, N=25, Not yet recruiting, Wuhan Union Hospital, China
    New P2 trial • Metastases
    |
    albumin-bound paclitaxel • Kaitanni (cadonilimab) • ifebemtinib (IN10018)
    6ms
    Study to Evaluate D-1553 in Combination With IN10018 in Subjects With Solid Tumors (clinicaltrials.gov)
    P1/2, N=92, Recruiting, InventisBio Co., Ltd | Trial completion date: Dec 2024 --> Dec 2025 | Trial primary completion date: Jun 2024 --> Jun 2025
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    garsorasib (D-1553) • ifebemtinib (IN10018)
    1year
    Simultaneous inhibition of FAK and ROS1 synergistically repressed triple-negative breast cancer by upregulating p53 signalling. (PubMed, Biomark Res)
    Our study demonstrates that the combination of IN10018 and crizotinib shows synergistic antitumor effects in TNBC. Mechanistically, this combination inhibits cell proliferation, enhances apoptosis, and induces ferroptosis, which is associated with increased p53 levels.
    Journal • PARP Biomarker • IO biomarker
    |
    ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • BCL2 (B-cell CLL/lymphoma 2) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • GPX4 (Glutathione Peroxidase 4) • CASP9 (Caspase 9) • CDK1 (Cyclin-dependent kinase 1) • CCNB1 (Cyclin B1)
    |
    ROS1 expression
    |
    Xalkori (crizotinib) • ifebemtinib (IN10018)
    1year
    a Study to Evaluate the Safety and Efficacy of D-1553 Combined With IN10018 in KRAS G12C Mutant Solid Tumors (clinicaltrials.gov)
    P1/2, N=140, Recruiting, InxMed (Shanghai) Co., Ltd. | Enrolling by invitation --> Recruiting
    Enrollment status • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    garsorasib (D-1553) • ifebemtinib (IN10018)
    over1year
    IN10018 Monotherapy and Combination Therapy for Metastatic Melanoma (clinicaltrials.gov)
    P1, N=120, Recruiting, InxMed (Shanghai) Co., Ltd. | Trial completion date: Jun 2024 --> Sep 2024 | Trial primary completion date: Dec 2023 --> Jun 2024
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation • NRAS Q61 • NRAS G12 • NRAS G13
    |
    Tecentriq (atezolizumab) • Cotellic (cobimetinib) • ifebemtinib (IN10018)
    over1year
    a Phase Ib/II Study to Evaluate the Safety and Efficacy of D-1553 Combined With IN10018 in KRAS G12C Mutant Solid Tumors (clinicaltrials.gov)
    P1/2, N=140, Enrolling by invitation, InxMed (Shanghai) Co., Ltd.
    New P1/2 trial
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    garsorasib (D-1553) • ifebemtinib (IN10018)
    over1year
    IN10018 Combination Therapy in Treatment-naïve ES-SCLC (clinicaltrials.gov)
    P1/2, N=120, Recruiting, InxMed (Shanghai) Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Combination therapy
    |
    carboplatin • Tevimbra (tislelizumab-jsgr) • etoposide IV • ifebemtinib (IN10018)
    over1year
    Study to Evaluate D-1553 in Combination With IN10018 in Subjects With Solid Tumors (clinicaltrials.gov)
    P1/2, N=92, Recruiting, InventisBio Co., Ltd | Not yet recruiting --> Recruiting
    Enrollment open • Combination therapy • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    garsorasib (D-1553) • ifebemtinib (IN10018)
    over1year
    IN10018 in Combination With Pegylated Liposomal Doxorubicin (PLD) vs. Placebo in Combination With PLD for the Treatment of Platinum-resistant Recurrent Ovarian Cancer (clinicaltrials.gov)
    P2, N=168, Recruiting, InxMed (Shanghai) Co., Ltd.
    New P2 trial • Combination therapy
    |
    MUC16 (Mucin 16, Cell Surface Associated)
    |
    MUC16 elevation
    |
    pegylated liposomal doxorubicin • ifebemtinib (IN10018)
    over2years
    IN10018 Monotherapy and Combination Therapy for Metastatic Melanoma (clinicaltrials.gov)
    P1, N=120, Recruiting, InxMed (Shanghai) Co., Ltd. | N=52 --> 120 | Trial completion date: Jun 2023 --> Jun 2024 | Trial primary completion date: Dec 2022 --> Dec 2023
    Enrollment change • Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    NRAS mutation • NRAS Q61 • NRAS G12 • NRAS G13
    |
    Tecentriq (atezolizumab) • Cotellic (cobimetinib) • ifebemtinib (IN10018)
    over2years
    Study to Evaluate D-1553 in Combination With IN10018 in Subjects With Solid Tumors (clinicaltrials.gov)
    P1/2, N=92, Not yet recruiting, InventisBio Co., Ltd | Initiation date: Jun 2022 --> Sep 2022
    Trial initiation date • Combination therapy
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    garsorasib (D-1553) • ifebemtinib (IN10018)
    almost3years
    Study to Evaluate D-1553 in Combination With IN10018 in Subjects With Solid Tumors (clinicaltrials.gov)
    P1/2, N=92, Not yet recruiting, InventisBio Co., Ltd
    New P1/2 trial • Combination therapy
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    garsorasib (D-1553) • ifebemtinib (IN10018)
    4years
    Inhibition of focal adhesion kinase enhances antitumor response of radiation therapy in pancreatic cancer through CD8+ T cells. (PubMed, Cancer Biol Med)
    In this study we showed that IN10018, a small molecular FAKi, enhanced antitumor response to RT...FAKi in combination with radiation inhibited the infiltration of granulocytes but enhanced the infiltration of macrophages and T regs in comparison with the radiation or FAKi treatment alone (P < 0.01). These results support the clinical development of FAKi as a radiosensitizer for PDAC and combining FAKi with RT to prime the tumor microenvironment of PDAC for immunotherapy.
    Journal
    |
    CD8 (cluster of differentiation 8)
    |
    ifebemtinib (IN10018)