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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:
    2ms
    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
    almost2years
    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
    |
    KRAS (KRAS proto-oncogene GTPase) • CA 19-9 (Cancer antigen 19-9)
    |
    KRAS mutation
    |
    Mekinist (trametinib) • GSK2256098
    2years
    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
    |
    NF2 (Neurofibromin 2)
    |
    NF2 mutation
    |
    GSK2256098
    3years
    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
    over3years
    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
    over3years
    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
    |
    NF2 (Neurofibromin 2)
    |
    GSK2256098
    over3years
    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