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    DRUG:

    azeliragon (TTP488)

    i
    Other names: TTP488, PF 4494700 , PF-04494700, TTP-488
    Associations

    News

    Trials
    Company:
    Cantex Pharma, vTv Therapeutics
    Drug class:
    AGEs inhibitor
    Associations

    News

    Trials
    18d
    CAN-201 NDG: Azeliragon and Chemoradiotherapy in Newly Diagnosed Glioblastoma (clinicaltrials.gov)
    P1/2, N=18, Active, not recruiting, Cantex Pharmaceuticals | Trial completion date: Dec 2025 --> Dec 2026 | Trial primary completion date: Dec 2024 --> Dec 2026
    Trial completion date • Trial primary completion date
    |
    S100A9 (S100 Calcium Binding Protein A9)
    |
    IDH wild-type
    |
    temozolomide • azeliragon (TTP488)
    2ms
    RAGE Inhibition to Decrease Cardiotoxicity in Women With Early Breast Cancer (clinicaltrials.gov)
    P1/2, N=48, Recruiting, Georgetown University | Trial completion date: Oct 2025 --> Dec 2026 | Trial primary completion date: Oct 2025 --> Dec 2026
    Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    Keytruda (pembrolizumab) • Herceptin (trastuzumab) • carboplatin • paclitaxel • docetaxel • Perjeta (pertuzumab) • doxorubicin hydrochloride • cyclophosphamide • azeliragon (TTP488)
    2ms
    Azeliragon attenuates cerebral infarction aggravation in diabetic rats: Receptor for advanced glycation end-product as a novel therapeutic target. (PubMed, Exp Neurol)
    Specifically, the phosphorylated to total NF-κB p65 ratio was significantly lower (p = 0.030), along with the levels of tumor necrosis factor-α and interleukin-1β, in the azeliragon group compared with the vehicle group (p < 0.001 for each). Therefore, RAGE antagonism significantly reduced ischemic brain damage and neuroinflammation in diabetic cerebral ischemia, offering a promising therapeutic strategy.
    Preclinical • Journal
    |
    TNFA (Tumor Necrosis Factor-Alpha) • NFKB1 (Nuclear factor of kappa light polypeptide gene enhancer in B-cells 1) • IL1B (Interleukin 1, beta)
    |
    azeliragon (TTP488)
    3ms
    Neoadjuvant Chemoradiotherapy With or Without Concurrent Azeliragon in Patients With Newly Diagnosed Glioblastoma (clinicaltrials.gov)
    P1, N=12, Recruiting, Washington University School of Medicine | Not yet recruiting --> Recruiting
    Enrollment open
    |
    temozolomide • azeliragon (TTP488)
    4ms
    RAGE signaling pathway in glioblastoma and cognitive decline: Insights into inflammatory mechanisms and therapeutic implications. (PubMed, Brain Res)
    Small-molecule inhibitors such as FPS-ZM1 and Azeliragon, biologics including sRAGE and RAGE antagonistic peptides, and phytochemicals such as curcumin, Tanshinone IIA, and berberine demonstrate the feasibility of modulating this pathway in preclinical models. Collectively, the evidence highlights the RAGE signaling as one of the central modulators of GBM progression and RT-induced cognitive decline through NF-κB, JAK/STAT, and MAPK activation. Future strategies that selectively disrupt pathological RAGE signaling, while sparing physiological functions, may provide transformative therapeutic avenues for patients facing the dual burden of glioblastoma and radiation-induced neurotoxicity.
    Journal
    |
    HMGB1 (High Mobility Group Box 1)
    |
    azeliragon (TTP488)
    8ms
    Neoadjuvant Chemoradiotherapy With or Without Concurrent Azeliragon in Patients With Newly Diagnosed Glioblastoma (clinicaltrials.gov)
    P1, N=12, Not yet recruiting, Washington University School of Medicine | Trial completion date: May 2029 --> Apr 2030 | Trial primary completion date: Oct 2027 --> Oct 2028
    Trial completion date • Trial primary completion date
    |
    temozolomide • azeliragon (TTP488)
    9ms
    RAGE Inhibition to Decrease Cardiotoxicity in Women With Early Breast Cancer (clinicaltrials.gov)
    P1/2, N=48, Recruiting, Georgetown University | Trial completion date: Apr 2025 --> Oct 2025 | Trial primary completion date: Mar 2025 --> Oct 2025
    Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    Keytruda (pembrolizumab) • Herceptin (trastuzumab) • carboplatin • paclitaxel • docetaxel • Perjeta (pertuzumab) • doxorubicin hydrochloride • cyclophosphamide • azeliragon (TTP488)
    12ms
    Concurrent Azeliragon With Craniospinal Irradiation (clinicaltrials.gov)
    P1, N=32, Recruiting, NYU Langone Health | Not yet recruiting --> Recruiting
    Enrollment open
    |
    azeliragon (TTP488)
    12ms
    A Randomized, Double-Blind, Placebo-Controlled Phase 2/3 Study to Determine the Safety and Effectiveness of Azeliragon in the Treatment of Patients Hospitalized for Coronavirus Disease 2019 (COVID-19) or Pneumonia (clinicaltrials.gov)
    P2/3, N=144, Active, not recruiting, The University of Texas Medical Branch, Galveston | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    azeliragon (TTP488)
    1year
    Neoadjuvant Chemoradiotherapy With or Without Concurrent Azeliragon in Patients With Newly Diagnosed Glioblastoma (clinicaltrials.gov)
    P1, N=12, Not yet recruiting, Washington University School of Medicine
    New P1 trial
    |
    temozolomide • azeliragon (TTP488)
    1year
    The RAGE Inhibitor TTP488 (Azeliragon) Demonstrates Anti-Tumor Activity and Enhances the Efficacy of Radiation Therapy in Pancreatic Cancer Cell Lines. (PubMed, Cancers (Basel))
    Additionally, Azeliragon modulated the immune suppressive tumor microenvironment in pancreatic cancer by reducing immunosuppressive cells, including M2 macrophages, regulatory T cells, and myeloid-derived suppressor cells, while enhancing CD8+ T cell infiltration. These findings suggest that Azeliragon, by inhibiting RAGE-mediated signaling and modulating immune response, may serve as an effective anti-cancer agent in pancreatic cancer.
    Preclinical • Journal
    |
    CD8 (cluster of differentiation 8)
    |
    azeliragon (TTP488)
    1year
    RAGE Inhibition to Decrease Cardiotoxicity in Women With Early Breast Cancer (clinicaltrials.gov)
    P1/2, N=48, Recruiting, Georgetown University | Trial completion date: Nov 2024 --> Apr 2025 | Trial primary completion date: Nov 2024 --> Mar 2025
    Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    Keytruda (pembrolizumab) • Herceptin (trastuzumab) • carboplatin • paclitaxel • docetaxel • Perjeta (pertuzumab) • doxorubicin hydrochloride • cyclophosphamide • azeliragon (TTP488)