azeliragon (TTP488) / Cantex Pharma 
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 21 Diseases   8 Trials   8 Trials   156 News 


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  • ||||||||||  Trial completion date, Trial primary completion date:  RAGE Inhibition to Decrease Cardiotoxicity in Women With Early Breast Cancer (clinicaltrials.gov) -  May 23, 2025   
    P1/2,  N=48, Recruiting, 
    The role of RAGE in EMT was studied in cells pretreated with RAGE antagonists (FPS-ZM1 or azeliragon), followed by cotreatment with TGF-?2 for 48 Trial completion date: Apr 2025 --> Oct 2025 | Trial primary completion date: Mar 2025 --> Oct 2025
  • ||||||||||  Trial completion date, Trial primary completion date:  RAGE Inhibition to Decrease Cardiotoxicity in Women With Early Breast Cancer (clinicaltrials.gov) -  Dec 26, 2024   
    P1/2,  N=48, Recruiting, 
    Compound 2g exhibits potent inhibition of the AGE2-BSA/sRAGE interaction (IC50 = 22 Trial completion date: Nov 2024 --> Apr 2025 | Trial primary completion date: Nov 2024 --> Mar 2025
  • ||||||||||  azeliragon (TTP488) / Cantex Pharma
    Enrollment closed:  CAN-201 NDG: Azeliragon and Chemoradiotherapy in Newly Diagnosed Glioblastoma (clinicaltrials.gov) -  Nov 12, 2024   
    P1/2,  N=18, Active, not recruiting, 
    Trial completion date: Nov 2024 --> Apr 2025 | Trial primary completion date: Nov 2024 --> Mar 2025 Recruiting --> Active, not recruiting
  • ||||||||||  azeliragon (TTP488) / Cantex Pharma
    Enrollment closed:  Azeliragon in MGMT Unmethylated Glioblastoma (clinicaltrials.gov) -  Sep 5, 2024   
    P2,  N=30, Active, not recruiting, 
    N=21 --> 0 | Not yet recruiting --> Withdrawn Recruiting --> Active, not recruiting
  • ||||||||||  azeliragon (TTP488) / Cantex Pharma
    Journal:  Involvement of RAGE in radiation-induced acquisition of malignant phenotypes in human glioblastoma cells. (Pubmed Central) -  Jul 28, 2024   
    Both phenotypes were suppressed by specific inhibitors of RAGE (FPS-ZM1 and TTP488) or by knockdown of RAGE...In addition, ?-irradiation-induced phosphorylation of STAT3 was suppressed by RAGE inhibitors, and a STAT3 inhibitor suppressed ?-irradiation-induced enhancement of cell migration, indicating that STAT3 is involved in the migration enhancement downstream of RAGE. Our results suggest that HMGB1-RAGE-STAT3 signaling is involved in radiation-induced enhancement of GBM cell migration, and may contribute to GBM recurrence by promoting metastasis and invasion.
  • ||||||||||  azeliragon (TTP488) / Cantex Pharma
    Enrollment change, Trial completion date, Trial primary completion date, Metastases:  Study of Effect of Azeliragon in Patients Refractory to Prior Treatment of Metastatic Pancreatic Cancer (clinicaltrials.gov) -  Jun 13, 2024   
    P1/2,  N=30, Recruiting, 
    Our results suggest that HMGB1-RAGE-STAT3 signaling is involved in radiation-induced enhancement of GBM cell migration, and may contribute to GBM recurrence by promoting metastasis and invasion. N=18 --> 30 | Trial completion date: Nov 2024 --> May 2025 | Trial primary completion date: Oct 2024 --> Feb 2025
  • ||||||||||  Herceptin (trastuzumab) / Roche, azeliragon (TTP488) / Cantex Pharma, Perjeta (pertuzumab) / Roche
    RAGE inhibition to decrease cancer therapy related cardiotoxicity in women with early breast cancer (RAGE). (Hall A; Poster Bd #: 207a) -  Apr 24, 2024 - Abstract #ASCO2024ASCO_1347;    
    P1/2
    In Cohort 4, 6 patients will receive dose dense doxorubicin and cyclophosphamide (ddAC)...As of 2/1/24, 4 patients have been enrolled, with 4 undergoing screening. At the completion of this trial, we plan a randomized trial to evaluate the role of TTP488 to decrease cardiotoxicity, cancer related cognitive decline and disease recurrence.
  • ||||||||||  azeliragon (TTP488) / Cantex Pharma
    Trial primary completion date:  CAN-201 NDG: Azeliragon and Chemoradiotherapy in Newly Diagnosed Glioblastoma (clinicaltrials.gov) -  Feb 15, 2024   
    P1/2,  N=18, Recruiting, 
    Our results provide novel insights into the role of the AGE-RAGE axis in skeletal muscle aging, and future work is warranted on the potential application of S100b as a pro-regenerative factor in aged skeletal muscle. Trial primary completion date: Dec 2023 --> Dec 2024
  • ||||||||||  azeliragon (TTP488) / Cantex Pharma
    Journal:  Macrophage RAGE activation is proinflammatory in NASH. (Pubmed Central) -  Jan 4, 2024   
    FFC mice that received a pharmacological inhibitor of RAGE (TTP488), and myeloid-specific RAGE KO mice (RAGE-MKO) had attenuated liver injury associated with a reduced accumulation of RAGE+ recruited macrophages...Correspondingly, the secretome of ligand-stimulated bone marrow derived macrophages from RAGE-MKO mice had an attenuated capacity to activate CD8+ T cells. Our data implicate RAGE as what we propose to be a novel and potentially targetable mediator of the proinflammatory signaling of recruited macrophages in NASH.
  • ||||||||||  azeliragon (TTP488) / Cantex Pharma
    Enrollment open:  Azeliragon in MGMT Unmethylated Glioblastoma (clinicaltrials.gov) -  Oct 27, 2023   
    P2,  N=30, Recruiting, 
    Our data implicate RAGE as what we propose to be a novel and potentially targetable mediator of the proinflammatory signaling of recruited macrophages in NASH. Not yet recruiting --> Recruiting
  • ||||||||||  azeliragon (TTP488) / Cantex Pharma
    Enrollment open, Trial initiation date:  CAN-201 NDG: Azeliragon and Chemoradiotherapy in Newly Diagnosed Glioblastoma (clinicaltrials.gov) -  Sep 15, 2023   
    P1/2,  N=18, Recruiting, 
    Not yet recruiting --> Recruiting Not yet recruiting --> Recruiting | Initiation date: Mar 2023 --> Sep 2023
  • ||||||||||  azeliragon (TTP488) / Cantex Pharma
    New P2 trial:  Azeliragon in MGMT Unmethylated Glioblastoma (clinicaltrials.gov) -  Aug 14, 2023   
    P2,  N=30, Not yet recruiting, 
  • ||||||||||  azeliragon (TTP488) / Cantex Pharma
    Journal:  RAGE inhibitor TTP488 (Azeliragon) suppresses metastasis in triple-negative breast cancer. (Pubmed Central) -  Jul 14, 2023   
    These results show that TTP488 impairs metastasis of TNBC and further clarifies the signaling and cellular mechanisms through which RAGE mediates metastasis. Importantly, as TTP488 displays a favorable safety profile in human studies, our study provides the rationale for evaluating TTP488 in clinical trials to treat or prevent metastatic TNBC.
  • ||||||||||  azeliragon (TTP488) / Cantex Pharma
    Review, Journal:  RAGE Inhibitors in Neurodegenerative Diseases. (Pubmed Central) -  May 16, 2023   
    Some of the RAGE antagonists, such as Azeliragon, are currently in clinical development for treating neurological diseases, including AD, although currently there have been no FDA-approved therapeutics based on the RAGE antagonists. This review outlines the AGE-RAGE interactions as a leading cause of the onset of neurological diseases and the current efforts on developing therapeutics for neurological diseases based on the RAGE antagonists.
  • ||||||||||  azeliragon (TTP488) / Cantex Pharma
    RAGE EXPRESSING MACROPHAGE SUBSETS MEDIATE INFLAMMATION IN NASH (South Hall A, Poster Hall - McCormick Place) -  Mar 23, 2023 - Abstract #DDW2023DDW_1520;    
    FFC-RLMC-KO and RAGE-i mice had significant attenuation of liver injury compared to FFC-WT and vehicle treated controls respectively, assessed by NAS-grading and ALT. Further, RLMC-KO mice had significantly lower RAGE expression by IHC of liver sections and fibrosis compared to FFC fed WT-mice.
  • ||||||||||  azeliragon (TTP488) / Cantex Pharma
    Trial initiation date:  CAN-201 NDG: Azeliragon and Chemoradiotherapy in Newly Diagnosed Glioblastoma (clinicaltrials.gov) -  Mar 10, 2023   
    P1/2,  N=18, Not yet recruiting, 
    Further, RLMC-KO mice had significantly lower RAGE expression by IHC of liver sections and fibrosis compared to FFC fed WT-mice. Initiation date: Dec 2022 --> Mar 2023
  • ||||||||||  Enrollment open, Trial completion date, Trial primary completion date:  RAGE Inhibition to Decrease Cardiotoxicity in Women With Early Breast Cancer (clinicaltrials.gov) -  Jan 9, 2023   
    P1/2,  N=48, Recruiting, 
    Initiation date: Dec 2022 --> Mar 2023 Not yet recruiting --> Recruiting | Trial completion date: Nov 2023 --> Nov 2024 | Trial primary completion date: Nov 2023 --> Nov 2024
  • ||||||||||  Trial initiation date:  RAGE Inhibition to Decrease Cardiotoxicity in Women With Early Breast Cancer (clinicaltrials.gov) -  Sep 29, 2022   
    P1/2,  N=48, Not yet recruiting, 
    Importantly, as TTP488 displays a high safety profile in human trials, this study provides the rationale for evaluating TTP488 in clinical trials to treat or prevent metastatic breast cancer. Initiation date: Aug 2022 --> Nov 2022