Roluperidone

Roluperidone (former developmental code names MIN-101, CYR-101, MT-210) is a 5-HT2A and σ2 receptor antagonist 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] Pre-clinical findings provide evidence of the effect of roluperidone on Brain-Derived Neurotrophic Factor (“BDNF”), which has been associated with neurogenesis, neuroplasticity, neuroprotection, synapse regulation, learning and memory.[5] As of May 2018, the drug was in phase III clinical trials.[6] 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."[7] However, in August of 2022 Minerva submitted a New Drug Application (NDA) to the Food and Drug Administration (FDA) for the approval of roluperidone for the treatment of schizophrenia.[8] The NDA submission in 2022 followed successful completion of a phase III clinical trial which was published in early 2022. Minerva believed that the findings of this second trial supported the claim that the drug was an effective agent for the treatment of negative symptoms in schizophrenia. However, in October 2022, FDA sent Minerva a refusal to file letter pertaining to the New Drug Application for roluperidone for treating negative symptoms in schizophrenia patients. [9]

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

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. 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 (MIN-101) • Minerva Neurosciences".
  6. "Roluperidone - Minerva Neurosciences". Adis Insight. Springer Nature Switzerland AG.
  7. Kilgore, Tomi. "Minerva Neurosciences' stock plummets after schizophrenia treatment disappoints in phase 3 study". MarketWatch. Retrieved 2021-03-21.
  8. "Minerva Neurosciences Submits New Drug Application to FDA for Roluperidone for the Treatment of Negative Symptoms in Patients with Schizophrenia".
  9. "Minerva Neurosciences Receives Refusal to File Letter from FDA for its New Drug Application for Roluperidone for the Treatment of Negative Symptoms in Schizophrenia".
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