Drug intelligence / Profile preview

Olanzapine + melatonin

Development stage
Phase 4
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Olanzapine + melatonin is a combination of two agents used together primarily in research and clinical practice to mitigate the metabolic side effects associated with antipsychotic therapy. Olanzapine is an atypical antipsychotic that acts as an antagonist at multiple neuronal receptors, including dopamine D1-D4, serotonin 5HT2A/2C/3/6, alpha-1 adrenergic, histamine H1, and muscarinic receptors. It is approved for the treatment of schizophrenia and bipolar disorder[4][6]. Melatonin is a hormone involved in regulating circadian rhythms and sleep-wake cycles; it also has antioxidant properties. When co-administered with olanzapine, melatonin has been shown in clinical studies to attenuate weight gain, abdominal obesity, hypertriglyceridemia[3], cholesterol increases[2][5], and systolic blood pressure rise induced by olanzapine therapy. This combination does not represent a fixed pharmaceutical product but rather concurrent use of two agents to improve tolerability of antipsychotic treatment.

02

Targets

ADRA1A (α1A)DRD2 (Dopamine D2 Receptor)HRH1 (Histamine H1 Receptor)MTNR1A (MT1)MTNR1B (Melatonin Receptor 2)M1 (Muscarinic acetylcholine receptor M1)HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)mAChR (Muscarinic acetylcholine receptors)

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