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Drug intelligence / Profile preview
Zyprexa Relprevv
- Development stage
- Approved
- Lead developer
- Eli Lilly
- Modality
- Small Molecules
- Administration
- Intramuscular
01
Overview
Zyprexa Relprevv is a long-acting intramuscular depot formulation of **olanzapine pamoate monohydrate** developed by Eli Lilly for the treatment of schizophrenia in adults. It is a **small molecule** atypical antipsychotic formulated as an extended-release injectable suspension for deep gluteal administration every 2 to 4 weeks, providing sustained exposure to olanzapine. Olanzapine exerts antipsychotic effects through multi-receptor antagonism in the central nervous system, with clinically important activity at **dopamine D2** and **serotonin 5-HT2A** receptors, along with additional antagonism at histamine H1, muscarinic acetylcholine, and adrenergic alpha1 receptors. The product was approved in the United States for schizophrenia and is associated with a boxed safety concern for post-injection delirium/sedation syndrome, requiring administration in registered healthcare settings with post-injection observation.
- Brand names
- Zyprexa Relprevv
- Other names
- olanzapine pamoate monohydrateintramuscular olanzapine depotolanzapine long-acting injectionolanzapine extended-release injectable suspension
02
Targets
ADRA1A (α1A)ADRB1 (β1)DRD1 (Dopamine D1 Receptor)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)DRD4 (Dopamine D4 Receptor)GABRR (GABA-A receptor subunit rho)HRH1 (Histamine H1 Receptor)M1 (Muscarinic acetylcholine receptor M1)CHRM2 (M2)CHRM3 (M3)CHRM4 (M4)CHRM5 (M5)HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)HTR3A (5-hydroxytryptamine receptor 3A)HTR6 (5-hydroxytryptamine receptor 6)
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