Drug intelligence / Profile preview

iloperidone

Development stage
Approved
Lead developer
Vanda Pharmaceuticals
Modality
Small Molecules
01

Overview

Iloperidone is a second-generation (atypical) antipsychotic of the piperidinyl-benzisoxazole class, approved for the treatment of schizophrenia and manic or mixed episodes associated with bipolar I disorder in adults. It acts primarily as an antagonist at central dopamine D2 and serotonin 5‑HT2A receptors, with additional antagonism at D3 and α1‑adrenergic receptors. It has moderate affinity for D4, 5‑HT6, and 5‑HT7 receptors, low affinity for D1, 5‑HT1A, and histamine H1 receptors, and negligible activity at muscarinic cholinergic receptors. The drug was first FDA-approved in May 2009. Its efficacy is thought to result from rebalancing dopamine and serotonin neurotransmission in the brain[2][4][7][8].

Brand names
FanaptFanaptumFiaptaZomaril
Other names
IloperidonaIlopéridoneIloperidonum
02

Targets

HTR6 (5-hydroxytryptamine receptor 6)HTR2A (Serotonin receptor 5-HT2A)DRD3 (Dopamine receptor D3)DRD2 (Dopamine D2 Receptor)HTR7 (5-hydroxytryptamine receptor 7)DRD4 (Dopamine D4 Receptor)ADRA1A (α1A)ADRA2C (α2C)

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