Cariprazine hydrochloride

Description

Cariprazine hydrochloride (IX) is an oral, brain-penetrant, atypical antipsychotic developed by the Hungarian pharmaceutical firm Gedeon Richter. It was approved by the FDA in September 2015 for treatment of schizophrenia and for the acute treatment of manic or mixed episodes of bipolar I disorder. While the precise mechanism of action of cariprazine is unknown, its antipsychotic and procognitive effects may be mediated through partial agonism at dopamine D2/D3 and serotonin 5-HT1A receptors as well as antagonism at serotonin 5-HT2A receptors. Unlike many antipsychotics, cariprazine displays particular selectivity for the D3 receptor (D3, Ki = 0.085 nM; D2L, Ki = 0.49 nM; D2S, Ki = 0.69 nM). Cariprazine is extensively metabolized by CYP3A4 and, to a lesser extent, CYP2D6; desmethyl and didesmethyl cariprazine, the primary metabolites, are pharmacologically equipotent to the parent drug. In clinical trials, cariprazine demonstrated improvement compared to placebo as measured by Young Mania Rating Scale (YMRS) total scores in patients with bipolar mania and by Positive and Negative Syndrome Scale (PANSS) total scores in patients with schizophrenia. Forest Laboratories (now Allergan) has exclusive rights to cariprazine in the U.S. and Canada, while Mitsubishi Pharma Corporation has exclusive rights to the sale of the drug in Japan and Asia.

The Uses of Cariprazine hydrochloride

Cariprazine is used to treat schizophrenia (a mental illness that causes disturbed or unusual thinking, loss of interest in life, and strong or inappropriate emotions). Cariprazine is also used to treat episodes of depression in people with bipolar I disorder (manic depressive disorder; a disease that causes episodes of mania, episodes of depression and other abnormal moods). It is also used as a short term treatment for episodes of mania or mixed episodes (symptoms of mania and depression that happen together) in people with bipolar I disorder. Cariprazine is in a class of medications called atypical antipsychotics. It works by changing the activity of certain natural substances in the brain.