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    DRUG:

    GSK2256098

    i
    Other names: GSK2256098, GSK 2256098, GTPL7939, GTPL-7939, GSK-2256098, GTPL 7939
    Company:
    GSK
    Drug class:
    FAK inhibitor
    Related drugs:
    17d
    Targeting focal adhesion kinase (FAK) in non-small cell lung cancer (NSCLC): Molecular mechanisms and combination therapeutic strategies. (PubMed, Biochem Pharmacol)
    Several FAK targeted inhibitors have advanced into clinical evaluation; for example, CEP-37440 is undergoing phase I trials, whereas GSK-2256098 has reached phase II trials. This review summarizes the structure and functional characteristics of FAK, its role in the pathogenesis of NSCLC, the research progress on FAK inhibitors, and the current status and prospects of combining FAK inhibitors with other therapies for NSCLC. The aim is to provide new insights for future clinical trial design and combination therapy strategies for NSCLC.
    Review • Journal
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    EGFR (Epidermal growth factor receptor) • ALK (Anaplastic lymphoma kinase)
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    GSK2256098 • CEP-37440
    25d
    A071401: Vismodegib, FAK Inhibitor GSK2256098, Capivasertib, and Abemaciclib in Treating Patients With Progressive Meningiomas (clinicaltrials.gov)
    P2, N=124, Recruiting, Alliance for Clinical Trials in Oncology | Trial primary completion date: Jan 2026 --> Jan 2027
    Trial primary completion date
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • AKT1 (V-akt murine thymoma viral oncogene homolog 1) • CCND1 (Cyclin D1) • CCNE1 (Cyclin E1) • PTCH1 (Patched 1) • CDK4 (Cyclin-dependent kinase 4) • NF2 (Neurofibromin 2) • SMO (Smoothened Frizzled Class Receptor) • CDK6 (Cyclin-dependent kinase 6) • CCND2 (Cyclin D2) • CCND3 (Cyclin D3)
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    PIK3CA mutation • PTEN mutation • AKT1 mutation
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    Verzenio (abemaciclib) • Truqap (capivasertib) • Erivedge (vismodegib) • GSK2256098
    over1year
    A071401: Vismodegib, FAK Inhibitor GSK2256098, Capivasertib, and Abemaciclib in Treating Patients with Progressive Meningiomas (clinicaltrials.gov)
    P2, N=124, Recruiting, Alliance for Clinical Trials in Oncology | Trial completion date: Oct 2024 --> Jan 2028 | Trial primary completion date: Oct 2024 --> Jan 2026
    Trial completion date • Trial primary completion date
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • AKT1 (V-akt murine thymoma viral oncogene homolog 1) • CCND1 (Cyclin D1) • CCNE1 (Cyclin E1) • PTCH1 (Patched 1) • CDK4 (Cyclin-dependent kinase 4) • NF2 (Neurofibromin 2) • SMO (Smoothened Frizzled Class Receptor) • CDK6 (Cyclin-dependent kinase 6) • CCND2 (Cyclin D2) • CCND3 (Cyclin D3)
    |
    PIK3CA mutation • PTEN mutation • CDKN2A mutation • PTCH1 mutation • NF2 mutation • AKT1 mutation • SMO mutation • PIK3CA mutation + PTEN mutation • CDK4 mutation
    |
    Verzenio (abemaciclib) • Truqap (capivasertib) • Erivedge (vismodegib) • GSK2256098
    3years
    A phase II trial of GSK2256098 and trametinib in patients with advanced pancreatic ductal adenocarcinoma. (PubMed, J Gastrointest Oncol)
    One response-inevaluable patient achieved clinical stability for 5 months with reduction in CA19-9 and ctDNA levels with a MAP2K1 treatment resistance mutation detected in ctDNA at clinical progression. The combination of GSK2256098 and trametinib was well tolerated but was not active in unselected advanced PDAC.
    P2 data • Journal • Metastases
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    KRAS (KRAS proto-oncogene GTPase) • CA 19-9 (Cancer antigen 19-9)
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    KRAS mutation
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    Mekinist (trametinib) • GSK2256098
    over3years
    Alliance A071401: Phase II Trial of Focal Adhesion Kinase Inhibition in Meningiomas With Somatic NF2 Mutations. (PubMed, J Clin Oncol)
    GSK2256098 was well tolerated and resulted in an improved PFS6 rate in patients with recurrent or progressive NF2-mutated meningiomas, compared with historical controls. The criteria for promising activity were met, and FAK inhibition warrants further evaluation for this patient population.
    P2 data • Journal
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    NF2 (Neurofibromin 2)
    |
    NF2 mutation
    |
    GSK2256098
    over4years
    Vismodegib, FAK Inhibitor GSK2256098, Capivasertib, and Abemaciclib in Treating Patients With Progressive Meningiomas (clinicaltrials.gov)
    P2, N=124, Recruiting, Alliance for Clinical Trials in Oncology | Suspended --> Recruiting | N=69 --> 124
    Clinical • Enrollment open • Enrollment change
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • AKT1 (V-akt murine thymoma viral oncogene homolog 1) • CCND1 (Cyclin D1) • CCNE1 (Cyclin E1) • PTCH1 (Patched 1) • CDK4 (Cyclin-dependent kinase 4) • SMO (Smoothened Frizzled Class Receptor) • CDK6 (Cyclin-dependent kinase 6) • CCND2 (Cyclin D2) • CCND3 (Cyclin D3)
    |
    PIK3CA mutation • PTEN mutation • CDKN2A mutation • PTCH1 mutation • NF2 mutation • AKT1 mutation • SMO mutation • PIK3CA mutation + PTEN mutation • CDK4 mutation
    |
    Verzenio (abemaciclib) • Truqap (capivasertib) • Erivedge (vismodegib) • GSK2256098
    over4years
    Vismodegib and FAK Inhibitor GSK2256098 in Treating Patients With Progressive Meningiomas (clinicaltrials.gov)
    P2, N=69, Suspended, Alliance for Clinical Trials in Oncology | Trial primary completion date: Aug 2021 --> Oct 2024
    Clinical • Trial primary completion date
    |
    PTCH1 (Patched 1)
    |
    PTCH1 mutation • NF2 mutation
    |
    Erivedge (vismodegib) • GSK2256098
    almost5years
    Crispr/Cas-based modeling of NF2 loss in meningioma cells. (PubMed, J Neurosci Methods)
    Our model based on Crispr/Cas-based gene editing provides paired meningioma cells suitable to study functional consequences and therapeutic accessibility of NF2/merlin loss.
    Journal
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    NF2 (Neurofibromin 2)
    |
    GSK2256098
    almost5years
    Discovery of antiproliferative and anti-FAK inhibitory activity of 1,2,4-triazole derivatives containing acetamido carboxylic acid skeleton. (PubMed, Bioorg Med Chem Lett)
    Compound 3d possessed significant FAK inhibitory activity with IC value of 18.10 nM better than the reference GSK-2256098 (IC = 22.14 nM)...This effect led to apoptosis induction and cell cycle arrest. Taken together, these results indicate that 3d could serve as a potent preclinical candidate for the treatment of cancers.
    Journal
    |
    STAT3 (Signal Transducer And Activator Of Transcription 3)
    |
    GSK2256098