Remlifanserin

Pharmaceutical compound From Wikipedia, the free encyclopedia

Remlifanserin (INNTooltip International Nonproprietary Name;[5] developmental code name ACP-204) is a selective serotonin 5-HT2A receptor inverse agonist which is under development for the treatment of Alzheimer's disease psychosis.[1][6][7][8][9][10] It is taken by mouth.[1]

Other namesACP-204; ACP204
Routes of
administrationOral[1]
Drug classSerotonin 5-HT2A receptor inverse agonist
Onset of action4–6 hours (6 hours fasted, 9 hours fed) (TmaxTooltip time to peak levels)[2][3]
Quick facts Clinical data, Other names ...
Remlifanserin
Clinical data
Other namesACP-204; ACP204
Routes of
administration		Oral[1]
Drug classSerotonin 5-HT2A receptor inverse agonist
Pharmacokinetic data
Onset of action4–6 hours (6 hours fasted, 9 hours fed) (TmaxTooltip time to peak levels)[2][3]
Elimination half-life17.5–19.8 hours[2][4]
Identifiers
  • 3-[(4-cyclopropyloxyphenyl)methyl]-1-[(2,4-difluorophenyl)methyl]-1-(1-methylpiperidin-4-yl)urea
CAS Number
PubChem CID
UNII
KEGG
Chemical and physical data
FormulaC24H29F2N3O2
Molar mass429.512 g·mol−1
3D model (JSmol)
  • CN1CCC(CC1)N(CC2=C(C=C(C=C2)F)F)C(=O)NCC3=CC=C(C=C3)OC4CC4
  • InChI=1S/C24H29F2N3O2/c1-28-12-10-20(11-13-28)29(16-18-4-5-19(25)14-23(18)26)24(30)27-15-17-2-6-21(7-3-17)31-22-8-9-22/h2-7,14,20,22H,8-13,15-16H2,1H3,(H,27,30)
  • Key:UYRCLXJMWZFKDG-UHFFFAOYSA-N
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The drug is an improved follow-up compound to the earlier drug pimavanserin (Nuplaizid; ACP-103).[7] It is more potent and selective than pimavanserin as a serotonin 5-HT2A receptor inverse agonist.[11] Remlifanserin shows 32- to 123-fold selectivity for antagonism and inverse agonism of the serotonin 5-HT2A receptor over the serotonin 5-HT2C receptor depending on the bioassay.[11][12] For comparison, pimavanserin's selectivity was 8- to 37-fold depending on the assay.[11] Remlifanserin shows very low affinity for the serotonin 5-HT2B receptor compared to the serotonin 5-HT2A and 5-HT2C receptors.[11] It is expected to have less hERG inhibition and QT prolongation than pimavanserin.[11][12] The drug blocks the head-twitch response induced by the serotonergic psychedelic DOI and the hyperlocomotion induced by the NMDA receptor antagonist dizocilpine (MK-801) in rodents.[11] It has a several-fold shorter half-life than pimavanserin (17.5–19.8 hours vs. 57 hours, respectively).[12][2][4]

Remlifanserin is under development by Acadia Pharmaceuticals.[1][6] As of January 2025, it is in phase 3 clinical trials.[1][6] Some of its clinicaltrials.gov identifier(s) (nct number) are NCT06159673, NCT07029581, NCT06194799, NCT07095465.[13]

See also

References

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