Chemistry:E2511

From HandWiki

E2511, or E-2511, is a selective biased tropomyosin receptor kinase A (TrkA) positive allosteric modulator which is under development for the treatment of Alzheimer's disease.[1][2][3][4][5] It is taken orally.[1] The drug has been found to increase cholinergic signaling in preclinical research.[2][3][6][7] The elimination half-life of E2511 is 3.2 hours in humans.[2][3][8] E2511 is under development by Eisai.[1][2] As of September 2024, it is in phase 1 clinical trials for Alzheimer's disease.[1][2] A phase 1 clinical trial has been completed.[1][2][8] The chemical structure of E2511 does not yet appear to have been disclosed.[1][3]

See also

  • Tropomyosin receptor kinase A § Ligands

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 1.5 "E 2511". 26 September 2024. https://adisinsight.springer.com/drugs/800060467. 
  2. ↑ 2.0 2.1 2.2 2.3 2.4 2.5 "E2511". 9 November 2023. https://www.alzforum.org/therapeutics/e2511. 
  3. ↑ 3.0 3.1 3.2 3.3 "Positive Allosteric Modulators of Trk Receptors for the Treatment of Alzheimer's Disease". Pharmaceuticals (Basel, Switzerland) 17 (8): 997. July 2024. doi:10.3390/ph17080997. PMID 39204102. 
  4. ↑ "Molecular determinants of signal transduction in tropomyosin receptor kinases". FEBS Open Bio 16 (2): 252–267. February 2026. doi:10.1002/2211-5463.70135. PMID 41053984. 
  5. ↑ "Neurotrophin-targeted therapeutics: A gateway to cognition and more?". Drug Discovery Today 27 (10). October 2022. doi:10.1016/j.drudis.2022.07.003. PMID 35850433. 
  6. ↑ "E2511, a novel small compound TrkA biased positive allosteric modulator, reinnervates cholinergic neuron and activates cholinergic functions in non-clinical studies". Alzheimer's & Dementia 19 (S7). 2023. doi:10.1002/alz.062590. ISSN 1552-5260. 
  7. ↑ "E2511, a novel small compound TrkA allosteric modulator, induces a specific trophic signaling via direct binding to TrkA, and can reverse the loss of choline acetyltransferase (ChAT) positive neurons in transgenic models of AD". Alzheimer's & Dementia 17 (S9). 2021. doi:10.1002/alz.051985. ISSN 1552-5260. 
  8. ↑ 8.0 8.1 "First-in-Human (FIH), Single- and Multiple-Ascending-Dose (SAD/MAD) studies in healthy subjects of E2511, a novel tropomyosin receptor kinase a (TrkA) positive allosteric modulator (PAM)". Alzheimer's & Dementia 19 (S7). 2023. doi:10.1002/alz.066208. ISSN 1552-5260. 



Retrieved from "https://handwiki.org/wiki/index.php?title=Chemistry:E2511&oldid=4644341"