LY3372689 explained

LY3372689 is a drug candidate molecule under investigation to treat Alzheimer's disease. It targets the enzyme O-GlcNAcase.[1] [2] Its result is to reduce formation of tau protein tangles.

A molecule containing radioactive fluorine was used with a PET scan to show that LY3372689 binds in the human brain.[3]

Eli Lilly and Company is recruiting subjects for a clinical trial.[4] Some hospitals in Australia: St Vincent's Hospital, SydneyHornsby Ku-Ring-Gai Hospital, The Prince Charles Hospital, The Queen Elizabeth Hospital, Adelaide, Box Hill Hospital, and Delmont Private Hospital are involved.[5] Results of the trial were expected by June 2024.[6] Primary completion of the study occurred on 9th July 2024, with full completion expected in August 2024. In an investor call, it was disclosed that LY3372689 missed the primary endpoint of improvement on the Integrated Alzheimer's Disease Rating Scale. The detailed results of this study are expected to be disclosed at a conference in late 2024.[7]

Chemical

The molecule contains three rings: thiazole, piperidine and oxadiazole. Other functional groups included are an ether, acetamide, and a fluoride.[8]

Notes and References

  1. Web site: LY3372689 . www.alzforum.org.
  2. Cheng . Steven S. . Mody . Alison C. . Woo . Christina M. . 2024-11-07 . Opportunities for Therapeutic Modulation of O-GlcNAc . Chemical Reviews . en . 10.1021/acs.chemrev.4c00417 . 0009-2665.
  3. Shcherbinin . Sergey . Kielbasa . William . Dubois . Susan . Lowe . Stephen L . Phipps . Krista M . Tseng . James . Kevin . Donnelly B . Natanegara . Fanni . Warner . Susan . Dreyfus . Nicolas . Lindsay-Scott . Peter . Hawk . Mai Khanh . McDonald . Nicholas . Zhang . Xiaoyu . Gilmore . Julie A . Biglan . Kevin . Mergott . Dustin J . Russell . David . Gunn . Roger N . Constantinescu . Cristian . Nuthall . Hugh Norman . Collins . Emily C . Brain target occupancy of LY3372689, an inhibitor of the O-GlcNAcase (OGA) enzyme: Translation from rat to human: Neuroimaging / evaluating treatments . Alzheimer's & Dementia . December 2020 . 16 . S4 . 10.1002/alz.040558. 227501893 . free .
  4. Web site: Assessment of Safety, Tolerability, and Efficacy of LY3372689 in Early Symptomatic Alzheimer's Disease . clinicaltrials.gov . 31 March 2022 . 22 March 2022.
  5. Web site: A Study of LY3372689 to Assess the Safety, Tolerability, and Efficacy in Participants With Alzheimer's Disease . 31 March 2022.
  6. Krietsch Boerner . Leigh . Hybrid meeting divulges structures of drug candidates . Chemical & Engineering News . 25 March 2022 . 0009-2347.
  7. Web site: https://edge.media-server.com/mmc/p/3kqnwjy6/ . 2024-10-06 . edge.media-server.com.
  8. Web site: Dreyfus . Nicolas Jacques Francois . Lindsay-Scott . Peter James . N-[4-Fluoro-5-{{!((}}(2''S'',4''S'')-2-Methyl-4-[(5-Methyl-1,2,4-Oxadiazol-3-Yl)methoxy]-1-Piperidyl]methyl]thiazol-2-Yl]acetamide as Oga Inhibitor ]. 31 March 2022 . en . 2 August 2018.

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "LY3372689".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2025, A B Cryer, All Rights Reserved. Cookie policy.