Discovery and clinical translation of ceperognastat, an O‐GlcNAcase (OGA) inhibitor, for the treatment of Alzheimer's disease
Ceperognastat is a highly potent, CNS-penetrant OGA inhibitor.Ceperognastat is both orally available and CNS-penetrant even when given at low doses.Ceperognastat can achieve > 95% OGA enzyme occupancy in the animal and human brain.Ceperognastat had an acceptable safety profile in Phase 1 clinical studies.
Authors
- David Russell (ORCID: https://orcid.org/0000-0002-9105-2943)
- Mirosław Bryś (ORCID: https://orcid.org/0000-0003-3682-117X)
- Feiyu Fred Zhang
- Hugh Nuthall
- Susan L. DuBois
- Nicolas Dreyfus
- Sergey Shcherbinin
- Jeremy Gilmore (ORCID: https://orcid.org/0000-0003-2551-5839)
- J. Hendle (ORCID: https://orcid.org/0000-0001-8857-0216)
- Eric M. Woerly (ORCID: https://orcid.org/0009-0000-2425-7597)
- Emily C. Collins
- Adam Fleisher (ORCID: https://orcid.org/0000-0002-2556-0878)
- William Kielbasa
- Dustin J. Mergott (ORCID: https://orcid.org/0000-0003-1802-0758)
- Roger N. Gunn (ORCID: https://orcid.org/0000-0003-1181-5769)
- Kevin B. Donnelly (ORCID: https://orcid.org/0000-0002-1073-2593)
- Paul Goldsmith (ORCID: https://orcid.org/0000-0003-2977-1055)
- Michele Mancini (ORCID: https://orcid.org/0000-0003-0845-2813)
- David Evans (ORCID: https://orcid.org/0000-0001-5217-0368)
- Cristian C. Constantinescu
- Michael Hutton
- Stephen L. Lowe
Institutions
- Eli Lilly (United States) (US)
- Invicro (United Kingdom) (GB)
- Invicro (United States) (US)
Publication Details
- Journal
- Alzheimer s & Dementia Translational Research & Clinical Interventions
- Published
- 2024-10-01
- DOI
- https://doi.org/10.1002/trc2.70020
- Citations
- 18
- Primary Topic
- Glycosylation and Glycoproteins Research
- Type
- article
- Field-Weighted Citation Impact
- 4.21
Funders
- Eli Lilly and Company