Drug intelligence / Profile preview

zotepine

Development stage
Phase 4
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Zotepine is an atypical antipsychotic (neuroleptic) drug primarily indicated for the treatment of acute and chronic schizophrenia. It was first developed by Fujisawa Pharmaceutical (now part of Astellas Pharma) and has been marketed in Japan since 1982, Germany since 1990 (now discontinued there), and other countries including India and parts of Europe. It is not approved in the United States, Canada, UK, Australia, or New Zealand[2][1][7]. Mechanistically, zotepine acts as a dopamine antagonist with high affinity for D1 and D2 receptors. It also strongly antagonizes several serotonin receptors (notably 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7), inhibits noradrenaline reuptake via sodium-dependent noradrenaline transporter blockade, and blocks sodium-dependent serotonin transporters[1][3][7]. These actions contribute to its efficacy on both positive and negative symptoms of schizophrenia as well as cognitive symptoms. Off-label uses include acute mania in bipolar disorder, psychotic depression, Tourette's syndrome, agitation/aggression in dementia patients; however these are not widely approved indications[5].

Brand names
LodopinNipoleptZoleptilZotewinSetousLosizopilon
Other names
ZotepinaZotepinumZotepin
02

Targets

HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)DRD1 (Dopamine D1 Receptor)NET (Norepinephrine Transporter)HTR7 (5-hydroxytryptamine receptor 7)DRD2 (Dopamine D2 Receptor)HTR6 (5-hydroxytryptamine receptor 6)

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