Roluperidone

Roluperidone
Clinical data
Other namesMIN-101; CYR-101; MT-210
Routes of
administration		By mouth
Identifiers
IUPAC name
  • 2-[[1-[2-(4-Fluorophenyl)-2-oxoethyl]piperidin-4-yl]methyl]-3H-isoindol-1-one
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC22H23F2N2O2
Molar mass385.435 g·mol−1
3D model (JSmol)
SMILES
  • C1CN(CCC1CN2CC3=CC=CC=C3C2=O)CC(=O)C4=CC=C(C=C4)F
InChI
  • InChI=1S/C22H23FN2O2/c23-19-7-5-17(6-8-19)21(26)15-24-11-9-16(10-12-24)13-25-14-18-3-1-2-4-20(18)22(25)27/h1-8,16H,9-15H2
  • Key:RNRYULFRLCBRQS-UHFFFAOYSA-N

Roluperidone (former developmental code names MIN-101, CYR-101, MT-210) is a 5-HT2A and σ2 receptor antagonist that is under development by Minerva Neurosciences for the treatment of schizophrenia.[1][2][3][4] One of its metabolites also has some affinity for the H1 receptor.[2] As of May 2018, the drug is in phase III clinical trials.[5] In May 2020, the shares of Minerva Neurosciences plummeted 67% after the trial "failed to meet its primary endpoint of reduction in negative symptoms, and key secondary endpoints of improvement in personal and social performance measurements".[6]

See also

References

  1. ↑ Mestre TA, Zurowski M, Fox SH (April 2013). "5-Hydroxytryptamine 2A receptor antagonists as potential treatment for psychiatric disorders". Expert Opinion on Investigational Drugs. 22 (4): 411–21. doi:10.1517/13543784.2013.769957. PMID 23409724.
  2. 1 2 Ebdrup BH, Rasmussen H, Arnt J, Glenthøj B (September 2011). "Serotonin 2A receptor antagonists for treatment of schizophrenia". Expert Opinion on Investigational Drugs. 20 (9): 1211–23. doi:10.1517/13543784.2011.601738. PMID 21740279.
  3. ↑ Köster LS, Carbon M, Correll CU (December 2014). "Emerging drugs for schizophrenia: an update". Expert Opinion on Emerging Drugs. 19 (4): 511–31. doi:10.1517/14728214.2014.958148. PMID 25234340.
  4. ↑ "Drug Development in Schizophrenia: Summary and Table". Pharmaceutical Medicine. 28 (5): 265–271. 2014. doi:10.1007/s40290-014-0070-6. ISSN 1178-2595.
  5. ↑ "Roluperidone - Minerva Neurosciences". Adis Insight. Springer Nature Switzerland AG.
  6. ↑ Kilgore, Tomi. "Minerva Neurosciences' stock plummets after schizophrenia treatment disappoints in phase 3 study". MarketWatch. Retrieved 2021-03-21.
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