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][5][6] It is taken orally.[1] The drug has been found to increase cholinergic signaling in preclinical research.[2][3][7][8] The elimination half-life of E2511 is 3.2 hours in humans.[2][3][4] 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][4] The chemical structure of E2511 does not yet appear to have been disclosed.[1][3]
See also
References
- ^ a b c d e f g “E 2511”. AdisInsight. 26 September 2024. Retrieved 10 June 2026.
- ^ a b c d e f g “E2511”. ALZFORUM. 9 November 2023. Retrieved 10 June 2026.
- ^ a b c d e Forsell P, Parrado Fernández C, Nilsson B, Sandin J, Nordvall G, Segerdahl M (July 2024). “Positive Allosteric Modulators of Trk Receptors for the Treatment of Alzheimer’s Disease”. Pharmaceuticals. 17 (8). Basel, Switzerland: 997. doi:10.3390/ph17080997. PMC 11357672. PMID 39204102.
- ^ a b c Aceves P, Hall N, Dayal S, Yagi T, Chang J, Mikamoto M, et al. (2023). “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) e066208. doi:10.1002/alz.066208. ISSN 1552-5260.
- ^ Enkavi G (February 2026). “Molecular determinants of signal transduction in tropomyosin receptor kinases”. FEBS Open Bio. 16 (2): 252–267. doi:10.1002/2211-5463.70135. PMC 12871558. PMID 41053984.
- ^ Nordvall G, Forsell P, Sandin J (October 2022). “Neurotrophin-targeted therapeutics: A gateway to cognition and more?”. Drug Discovery Today. 27 (10) 103318. doi:10.1016/j.drudis.2022.07.003. PMID 35850433.
- ^ Tomioka T, Hiramatsu N, Moriyama Y, Kosasa T (2023). “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) e062590. doi:10.1002/alz.062590. ISSN 1552-5260.
- ^ Tomioka T, Moriyama Y, Hiramatsu N, Kosasa T, Kondo K, Wakita H (2021). “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) e051985. doi:10.1002/alz.051985. ISSN 1552-5260.