Roluperidone (former developmental code names MIN-101, CYR-101, MT-210) is a
5-HT2A and
σ2 receptor antagonist under development by
Minerva Neurosciences
Minerva (; ett, Menrva) is the Roman goddess of wisdom, justice, law, victory, and the sponsor of arts, trade, and strategy. Minerva is not a patron of violence such as Mars, but of strategic war. From the second century BC onward, the R ...
for the treatment of
schizophrenia
Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of psychosis. Major symptoms include hallucinations (typically hearing voices), delusions, and disorganized thinking. Other symptoms include social wi ...
.
One of its
metabolite
In biochemistry, a metabolite is an intermediate or end product of metabolism.
The term is usually used for small molecules. Metabolites have various functions, including fuel, structure, signaling, stimulatory and inhibitory effects on enzymes, ...
s also has some
affinity
Affinity may refer to:
Commerce, finance and law
* Affinity (law), kinship by marriage
* Affinity analysis, a market research and business management technique
* Affinity Credit Union, a Saskatchewan-based credit union
* Affinity Equity Part ...
for the
H1 receptor.
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. As of May 2018, the drug was in
phase III clinical trial
Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...
s.
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." However, in August of 2022 Minerva submitted a New Drug Application (NDA) to the
Food and Drug Administration
The United States Food and Drug Administration (FDA or US FDA) is a federal agency of the Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food ...
(FDA) for the approval of roluperidone for the treatment of
schizophrenia
Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of psychosis. Major symptoms include hallucinations (typically hearing voices), delusions, and disorganized thinking. Other symptoms include social wi ...
. 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.
See also
*
List of investigational antipsychotics
This is a list of investigational antipsychotics, or antipsychotics that are currently under development for clinical use but are not yet approved. ''Chemical/generic names are listed first, with developmental code names, synonyms, and brand names ...
*
Risperidone
Risperidone, sold under the brand name Risperdal among others, is an atypical antipsychotic used to treat schizophrenia and bipolar disorder. It is taken either by mouth or by injection (subcutaneous or intramuscular). The injectable versions ...
*
Paliperidone
Paliperidone, sold under the trade name Invega among others, is an atypical antipsychotic. It is mainly used to treat schizophrenia and schizoaffective disorder.
It is marketed by Janssen Pharmaceuticals. An extended release formulation is ...
*
Iloperidone
Iloperidone, commonly known as Fanapt and previously known as Zomaril, is an atypical antipsychotic for the treatment of schizophrenia.
Medical uses
Iloperidone is indicated for the treatment of schizophrenia. In a 2013 study in a comparison o ...
*
Glemanserin
*
Pruvanserin
*
Volinanserin
Volinanserin (INN) (developmental code name MDL-100,907) is a highly selective 5-HT2A receptor antagonist that is frequently used in scientific research to investigate the function of the 5-HT2A receptor. It was also tested in clinical trials ...
*
Lenperone
*
Lidanserin
Lidanserin ( INN; ZK-33,839) is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist. It was developed as an antihypertensive agent but was never marketed.
See also
* Glemanserin
* Pruvanserin
* Roluperidone
* Volin ...
*
MIN-117
MIN-117 (known formerly as WF-516) is an investigational antidepressant which is under development by Minerva Neurosciences for the clinical treatment of major depressive disorder (MDD). It is described as a 5-HT1A and 5-HT2A receptor antagoni ...
*
MIN-202
Seltorexant, also known by its developmental code names MIN-202 and JNJ-42847922, is an orexin receptor antagonist, orexin antagonist medication which is under development for the treatment of depression (mood), depression and insomnia. It is a b ...
References
5-HT2A antagonists
Antipsychotics
Isoindoles
Ketones
Organofluorides
Piperidines
Sigma antagonists
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