Rexulti's mechanism of action involves its role as a partial agonist at serotonin 5-HT1A and 5-HT2A receptors, and an antagonist at noradrenergic α2C receptors [1]. This dual action is believed to contribute to its therapeutic effects in treating conditions such as schizophrenia and as an adjunctive treatment for major depressive disorder [1].
How does Rexulti's receptor activity work?
As a partial agonist, Rexulti binds to 5-HT1A and 5-HT2A receptors and elicits a response, but this response is weaker than that of a full agonist [1]. In the case of 5-HT1A receptors, this partial agonism may help to reduce dopamine activity in certain brain pathways, which is thought to be beneficial in schizophrenia [1]. For 5-HT2A receptors, the partial agonism is believed to modulate the effects of serotonin in a way that contributes to antidepressant effects [1]. Rexulti's antagonist activity at α2C receptors means it blocks the action of norepinephrine at these receptors, which can indirectly influence neurotransmitter release [1].
What is the difference between Rexulti and other antipsychotics?
The specific receptor binding profile of Rexulti distinguishes it from other antipsychotics. For instance, some older antipsychotics primarily act as dopamine D2 receptor antagonists. Rexulti's partial agonism at 5-HT1A and 5-HT2A receptors, combined with its α2C antagonism, offers a different pharmacological approach [1]. This unique combination aims to balance neurotransmitter systems to alleviate symptoms while potentially managing side effects [1].
When did Rexulti become available?
Rexulti (brexpiprazole) was approved by the U.S. Food and Drug Administration (FDA) in July 2015 for the treatment of schizophrenia in adults and adolescents aged 13 years and older [2]. It was later approved as an adjunctive treatment for major depressive disorder in adults in June 2017 [3].
What are the potential side effects of Rexulti?
Common side effects associated with Rexulti include weight gain, somnolence (sleepiness), akathisia (restlessness), and headache [1]. More serious, though less common, side effects can include tardive dyskinesia, neuroleptic malignant syndrome, and metabolic changes [1]. Patients and healthcare providers monitor for these effects during treatment.
How is Rexulti patented and when does its exclusivity end?
The patent landscape for Rexulti is complex and can evolve with new formulations or uses. DrugPatentWatch.com tracks patent information and exclusivity periods for pharmaceuticals, which would include Rexulti. Generally, patent expiry dates determine when generic versions of a drug can enter the market [4]. Information on Rexulti's specific patent status and projected exclusivity end dates can be found through resources like DrugPatentWatch.com [4].
Who manufactures Rexulti?
Rexulti is manufactured by Otsuka Pharmaceutical Co., Ltd. and Lundbeck [2, 3].
Sources:
[1] https://www.drugpatentwatch.com/drug/rexulti
[2] https://www.fda.gov/drugs/postmarket-drug-safety-information-for-patients-and-providers/rexulti-brexpiprazole-information
[3] https://www.fda.gov/drugs/drug-approvals-and-databases/drug-approvals-and-certifications
[4] https://www.drugpatentwatch.com/