Clinical data
Other namesMIN-101; CYR-101; MT-210
Routes of
By mouth
  • 2-[[1-[2-(4-Fluorophenyl)-2-oxoethyl]piperidin-4-yl]methyl]-3H-isoindol-1-one
CAS Number
PubChem CID
CompTox Dashboard (EPA)
Chemical and physical data
Molar mass385.435 g·mol−1
3D model (JSmol)
  • 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

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]

See also


  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. ^ a b 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".