Remlifanserin

Last updated

Remlifanserin
Remlifanserin.svg
Clinical data
Other namesACP-204; ACP204
Routes of
administration 		Oral [1]
Drug class Serotonin 5-HT2A receptor inverse agonist
Identifiers
  • 3-[(4-cyclopropyloxyphenyl)methyl]-1-[(2,4-difluorophenyl)methyl]-1-(1-methylpiperidin-4-yl)urea
CAS Number
PubChem CID
UNII
Chemical and physical data
Formula C24H29F2N3O2
Molar mass 429.512 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

Remlifanserin (INN Tooltip International Nonproprietary Name; [2] 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] [3] [4] [5] [6] [7] It is taken by mouth. [1]

The drug is an improved follow-up compound to its developer's earlier drug pimavanserin (Nuplaizid; ACP-103). [4] It is more potent and selective than pimavanserin as a serotonin 5-HT2A receptor inverse agonist. [8] 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. [8] For comparison, pimavanserin's selectivity was 8- to 37-fold depending on the assay. [8] Remlifanserin shows very low affinity for the serotonin 5-HT2B receptor compared to the serotonin 5-HT2A and 5-HT2C receptors. [8] It is expected to have less QT prolongation than pimavanserin. [8] 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. [8]

Remlifanserin is under development by Acadia Pharmaceuticals. [1] [3] As of January 2025, it is in phase 3 clinical trials. [1] [3] Its clinicaltrials.gov identifier (nct number) is NCT06159673. [9]

See also

References

  1. 1 2 3 4 5 "ACP 204". AdisInsight. 23 January 2025. Retrieved 22 February 2025.
  2. ↑ "Proposed INN: List 131 International Nonproprietary Names for Pharmaceutical Substances (INN)" (PDF). WHO Drug Information. 38 (2): 421. 2024. remlifanserin N'-{[4-(cyclopropyloxy)phenyl]methyl}-N-[(2,4- difluorophenyl)methyl]-N-(1-methylpiperidin-4-yl)urea serotonin receptor (5-HT2A) inverse agonist [...] C24H29F2N3O2 2289704-13-6 [...]
  3. 1 2 3 "Delving into the Latest Updates on ACP-204 with Synapse". Synapse. 4 February 2025. Retrieved 22 February 2025.
  4. 1 2 "ACP-204". ALZFORUM. 5 February 2024. Retrieved 22 February 2025.
  5. ↑ Imbimbo C, Cotta Ramusino M, Leone S, Mazzacane F, De Franco V, Gatti A, et al. (February 2025). "Emerging Pharmacological Approaches for Psychosis and Agitation in Alzheimer's Disease". CNS Drugs. 39 (2): 143–160. doi:10.1007/s40263-024-01133-9. PMC   11769872 . PMID   39623197.
  6. ↑ IsHak WW, Meyer A, Freire L, Totlani J, Murphy N, Renteria S, et al. (2024). "Overview of Psychiatric Medications in the Pipeline in Phase III Trials as of June 1, 2024: A Systematic Review". Innovations in Clinical Neuroscience. 21 (7–9): 27–47. PMC   11424068 . PMID   39329027.
  7. ↑ Kwon KJ, Kim HY, Han SH, Shin CY (October 2024). "Future Therapeutic Strategies for Alzheimer's Disease: Focus on Behavioral and Psychological Symptoms". International Journal of Molecular Sciences. 25 (21) 11338. doi: 10.3390/ijms252111338 . PMC   11547068 . PMID   39518892.
  8. 1 2 3 4 5 6 Burstein E, Markus Dey P, Pathak S (December 2024). "ACNP 63rd Annual Meeting: Poster Abstracts P305-P608: P497. Nonclinical Characterization of ACP-204, a Novel Second Generation 5-HT2A Inverse Agonist" (PDF). Neuropsychopharmacology. 49 (Suppl 1): 236–417 (346–347). doi: 10.1038/s41386-024-02012-z . PMID   39643634.
  9. ↑ ACADIA Pharmaceuticals Inc. (2025-02-21). A Master Protocol for Three Independent, Seamlessly Enrolling, Double-blind, Placebo-controlled Efficacy and Safety Studies of ACP-204 in Adults with Alzheimer's Disease Psychosis (Report). clinicaltrials.gov.
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