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    DRUG CLASS:

    TTK inhibitor

    Related drugs:
    6ms
    Targeting monopolar spindle kinase I (Mps1 or TTK) induces radiosensitization in syngeneic models of triple negative breast cancer (TNBC) and potentiates type I interferon (T1IFN) signaling. (PubMed, Neoplasia)
    Here, we extended those studies into syngeneic murine models of TNBC using two TTK inhibitors: empesertib and the novel TTK inhibitor CFI-402257 (also known as luvixasertib) that was recently granted FDA fast track approval in breast cancer. Taken together, these studies demonstrate that TTK inhibition enhances radiosensitivity and TTK inhibition with RT modulates the immune landscape of TNBC. Collectively, this combination may represent a novel therapeutic strategy to improve outcomes for patients with TNBC by both direct tumor cytotoxicity and by promoting an immune-responsive environment.
    Journal
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    TTK (TTK Protein Kinase)
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    luvixasertib (CFI-402257) • empesertib (BAY1161909)
    7ms
    TWT-203: CFI-402257, a Potent and Selective TTK Inhibitor, in Solid Tumors and With Fulvestrant in Breast Cancer (clinicaltrials.gov)
    P1/2, N=44, Active, not recruiting, Treadwell Therapeutics, Inc | Recruiting --> Active, not recruiting | Trial completion date: Aug 2025 --> Aug 2026 | Trial primary completion date: Aug 2025 --> Aug 2026
    Enrollment closed • Trial completion date • Trial primary completion date
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    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
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    fulvestrant • luvixasertib (CFI-402257)
    7ms
    Study on Safety and Efficacy of NMS-01940153E in Adult Patients With Unresectable Hepatocellular Carcinoma (HCC) Previously Treated With Systemic Therapy (clinicaltrials.gov)
    P1/2, N=31, Terminated, Nerviano Medical Sciences | Completed --> Terminated; In the Phase II part of the study, among the participants evaluable for efficacy, no objective (partial response or clinical response) was observed at the first futility analysis.
    Trial termination
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    NMS-153
    9ms
    CCTG IND.236: CFI-402257 in Combination With Paclitaxel in Patients With Advanced/Metastatic HER2-Negative Breast Cancer (clinicaltrials.gov)
    P1/2, N=37, Active, not recruiting, Canadian Cancer Trials Group | Trial completion date: Dec 2024 --> Dec 2025
    Trial completion date
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    paclitaxel • luvixasertib (CFI-402257)
    11ms
    Targeting TTK Inhibits Tumorigenesis of T-Cell Lymphoma Through Dephosphorylating p38α and Activating AMPK/mTOR Pathway. (PubMed, Adv Sci (Weinh))
    CFI-402257, a specific inhibitor of TTK, is found to exhibit anti-tumor effects and exerted synergistic efficacy with PI3K inhibitor, Duvelisib, in TCL. The study shows that TTK contributes to the development of TCL by regulating p38α-mediated AMPK/mTOR pathway. CFI-402257 is expected to be a promising strategy for TCL treatment.
    Journal
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    TTK (TTK Protein Kinase)
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    Copiktra (duvelisib) • luvixasertib (CFI-402257)
    1year
    Identifying Anti-Cancer Effects and Exploring the Mechanism of an MPS1/TTK Inhibitor in Gastric Cancer. (PubMed, Cancer Res Treat)
    The TP53MUT-resistant line can tolerate aneuploidy or polyploidy and exhibits drug resistance. Our study explores the potential of an MPS1/TTK inhibitor, compound-9, as a targeted therapy in gastric cancer cells and investigates its mechanism of action.
    Journal • MSi-H Biomarker
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    MSI (Microsatellite instability)
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    MSI-H/dMMR • TP53 wild-type
    1year
    The identification of potent dual-target monopolar spindle 1 (MPS1) and histone deacetylase 8 (HDAC8) inhibitors through pharmacophore modeling, molecular docking, molecular dynamics simulations, and biological evaluation. (PubMed, Front Pharmacol)
    Furthermore, MPH-5 showed potent inhibition of HepG2 xenograft tumor growth in mice with no apparent toxicity and presented favorable pharmacokinetics. The study suggests that MPH-5 is a potent, selective, high-efficacy, and low-toxicity antitumor candidate for the treatment of hepatocellular carcinoma.
    Journal • Epigenetic controller
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    PKM (Pyruvate Kinase M1/2)
    over1year
    Study on Safety and Efficacy of NMS-01940153E in Adult Patients With Unresectable Hepatocellular Carcinoma (HCC) Previously Treated With Systemic Therapy (clinicaltrials.gov)
    P1/2, N=31, Completed, Nerviano Medical Sciences | Active, not recruiting --> Completed | Trial completion date: Mar 2025 --> Aug 2024
    Trial completion • Trial completion date
    |
    NMS-153
    over1year
    BAL0891 in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=216, Recruiting, SillaJen, Inc. | N=120 --> 216
    Enrollment change • Combination therapy • Metastases
    |
    carboplatin • paclitaxel • BAL0891
    over1year
    CCTG IND.236: CFI-402257 in Combination With Paclitaxel in Patients With Advanced/Metastatic HER2-Negative Breast Cancer (clinicaltrials.gov)
    P1/2, N=37, Active, not recruiting, Canadian Cancer Trials Group | Phase classification: P2 --> P1/2 | Trial completion date: Dec 2023 --> Dec 2024
    Phase classification • Trial completion date • Combination therapy • Metastases
    |
    paclitaxel • luvixasertib (CFI-402257)
    over1year
    TTK inhibitor OSU13 promotes immunotherapy responses by activating tumor STING. (PubMed, JCI Insight)
    Combining a low-toxicity dose of OSU13 with anti-PD1 checkpoint blockade resulted in prominent STING- and CD8 T cell-dependent tumor inhibition and improved survival. These findings provide a rationale for utilizing TTK inhibitors in combination with immunotherapy in STING-proficient tumors.
    Journal
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    PD-L1 (Programmed death ligand 1) • CD8 (cluster of differentiation 8) • STING (stimulator of interferon response cGAMP interactor 1)
    over1year
    BAL0891 in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=120, Recruiting, SillaJen, Inc. | Trial primary completion date: Sep 2024 --> Jul 2025
    Trial primary completion date • Combination therapy • Metastases
    |
    carboplatin • paclitaxel • BAL0891