Bexicaserin (INNTooltip International Nonproprietary Name; developmental code names LP352 and AN352) is a selective serotonin 5-HT2C receptor agonist which is under development for the treatment of seizures in developmental disabilities such as Dravet syndrome and Lennox-Gastaut syndrome.[1][3][2] It is taken by mouth.[2][1]

Bexicaserin
Clinical data
Other namesLP352; LP-352; AN352; AN-352
Routes of
administration
Oral[1]
Drug classSerotonin 5-HT2C receptor agonist[1][2]
Pharmacokinetic data
Elimination half-life5–7 hours[2]
Identifiers
  • (3R)-N-(2,2-difluoroethyl)-3-methyl-1,10-diazatricyclo[6.4.1.04,13]trideca-4,6,8(13)-triene-5-carboxamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC15H19F2N3O
Molar mass295.334 g·mol−1
3D model (JSmol)
  • C[C@H]1CN2CCNCC3=C2C1=C(C=C3)C(=O)NCC(F)F
  • InChI=1S/C15H19F2N3O/c1-9-8-20-5-4-18-6-10-2-3-11(13(9)14(10)20)15(21)19-7-12(16)17/h2-3,9,12,18H,4-8H2,1H3,(H,19,21)/t9-/m0/s1
  • Key:KGOOOHQKLRUVSF-VIFPVBQESA-N

The drug is highly selective for the serotonin 5-HT2C receptor, with negligible affinity for the serotonin 5-HT2A and 5-HT2B receptors.[2] Because it does not activate the serotonin 5-HT2B receptor, bexicaserin is not expected to pose a risk of cardiac valvulopathy, unlike the existing agent fenfluramine.[2]

As of October 2024, bexicaserin is in phase 3 clinical trials for treatment of developmental disabilities.[1][3] It is being developed by Longboard Pharmaceuticals.[1][3]

See also

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References

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  1. ^ a b c d e f "Bexicaserin - Longboard Pharmaceuticals". AdisInsight. 16 October 2024. Retrieved 29 October 2024.
  2. ^ a b c d e f Dell'isola GB, Verrotti A, Sciaccaluga M, Roberti R, Parnetti L, Russo E, et al. (June 2024). "Evaluating bexicaserin for the treatment of developmental epileptic encephalopathies". Expert Opinion on Pharmacotherapy. 25 (9): 1121–1130. doi:10.1080/14656566.2024.2373350. PMID 38916481.
  3. ^ a b c "Delving into the Latest Updates on Bexicaserin with Synapse". Synapse. 28 October 2024. Retrieved 29 October 2024.