Drug intelligence / Profile preview

desmethyl cariprazine

Development stage
Unknown
Lead developer
Gedeon Richter
Modality
Small Molecules
Administration
Oral
01

Overview

Desmethyl cariprazine (DCAR) is the primary active metabolite of the atypical antipsychotic drug cariprazine. It is formed in the liver primarily by the cytochrome P450 enzyme CYP3A4 and to a lesser extent by CYP2D6. DCAR, along with didesmethyl cariprazine, significantly contributes to the overall clinical efficacy of cariprazine. It acts as a partial agonist at dopamine D3 and D2 receptors, with a notable preference for D3 receptors, and also as a partial agonist at serotonin 5-HT1A receptors. Additionally, it functions as an antagonist at serotonin 5-HT2B and 5-HT2A receptors. This pharmacological profile allows it to modulate dopaminergic and serotonergic neurotransmission, contributing to the therapeutic effects observed in conditions such as schizophrenia and bipolar disorder.

02

Targets

DRD3 (Dopamine receptor D3)HTR2B (5-Hydroxytryptamine Receptor 2B)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))DRD2 (Dopamine D2 Receptor)

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