Azeliragon Explained

Azeliragon (TTP488 or PF-04494700) is a small-molecule RAGE inhibitor. It is developed by vTv Therapeutics for various cancers, including triple-negative breast cancer,[1] [2] pancreatic cancer.[3]

The chemical reached Phase III trials in slowing cognitive deterioration in early stage Alzheimer's disease patients.[4] [5] [6] It was also tested in people with diabetic neuropathy[7] and animal models of graft-vs-host disease.[8]

Notes and References

  1. Magna . Melinda . Hwang . Gyong Ha . McIntosh . Alec . Drews-Elger . Katherine . Takabatake . Masaru . Ikeda . Adam . Mera . Barbara J. . Kwak . Taekyoung . Miller . Philip . Lippman . Marc E. . Hudson . Barry I. . RAGE inhibitor TTP488 (Azeliragon) suppresses metastasis in triple-negative breast cancer . npj Breast Cancer . 13 July 2023 . 9 . 1 . 59 . 10.1038/s41523-023-00564-9 . 37443146 . 10344964 . en . 2374-4677.
  2. Xie . Jizhao . Xu . Huanji . Wu . Xinduo . Xie . Yunfeng . Lu . Xiuhong . Wang . Lisheng . Design, synthesis and anti-TNBC activity of Azeliragon triazole analogues . Bioorganic & Medicinal Chemistry Letters . December 2021 . 54 . 128444 . 10.1016/j.bmcl.2021.128444. 34763082 . 243976660 .
  3. Kong . Weikang . Zhu . Lingxia . Li . Tian . Chen . Jiao . Fan . Bo . Ji . Wenjing . Zhang . Chunli . Cai . Xueting . Hu . Chunping . Sun . Xiaoyan . Cao . Peng . Azeliragon inhibits PAK1 and enhances the therapeutic efficacy of AKT inhibitors in pancreatic cancer . European Journal of Pharmacology . June 2023 . 948 . 175703 . 10.1016/j.ejphar.2023.175703. 37028543 . 258019889 .
  4. Burstein . A.H. . Sabbagh . M. . Andrews . R. . Valcarce . C. . Dunn . I. . Altstiel . L. . DEVELOPMENT OF AZELIRAGON, AN ORAL SMALL MOLECULE ANTAGONIST OF THE RECEPTOR FOR ADVANCED GLYCATION ENDPRODUCTS, FOR THE POTENTIAL SLOWING OF LOSS OF COGNITION IN MILD ALZHEIMER'S DISEASE . The Journal of Prevention of Alzheimer's Disease . 2018 . 5 . 2 . 149–154 . 10.14283/jpad.2018.18. 29616709 . 4592148 .
  5. Yang . Lijuan . Liu . Yepei . Wang . Yuanyuan . Li . Junsheng . Liu . Na . Azeliragon ameliorates Alzheimer's disease via the Janus tyrosine kinase and signal transducer and activator of transcription signaling pathway . Clinics . 2021 . 76 . e2348 . 10.6061/clinics/2021/e2348. 33681944 . 7920406 .
  6. Burstein . Aaron H. . Dunn . Imogene . Gooch . Ann M. . Valcarce . Carmen . Effects of azeliragon on ADAS‐cog and CDR domains and individual items in patients with mild Alzheimer's disease and type 2 diabetes (T2D): Human/Human trials: Other . Alzheimer's & Dementia . December 2020 . 16 . S9 . 10.1002/alz.041198. 227500289 . free .
  7. Ma . Simeng . Nakamura . Yoki . Hisaoka-Nakashima . Kazue . Morioka . Norimitsu . Blockade of receptor for advanced glycation end-products with azeliragon ameliorates streptozotocin-induced diabetic neuropathy . Neurochemistry International . February 2023 . 163 . 105470 . 10.1016/j.neuint.2022.105470. 36581174 . 255113751 .
  8. Joshi . Aditi A. . Wu . Ying . Deng . Songyan . Preston-Hurlburt . Paula . Forbes . Josephine M. . Herold . Kevan C. . RAGE antagonism with azeliragon improves xenograft rejection by T cells in humanized mice. . Clinical Immunology . December 2022 . 245 . 109165 . 10.1016/j.clim.2022.109165. 36257528 . 252979084 .

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