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Drug intelligence / Profile preview
Staccato loxapine
- Development stage
- Approved
- Lead developer
- Ferrer
- Modality
- Small Molecules
- Administration
- Inhalation
01
Overview
**Staccato loxapine** is an inhaled formulation of the antipsychotic loxapine delivered via Alexza's proprietary hand-held Staccato system, which generates a thermally produced aerosol for rapid deep-lung absorption and intravenous-like pharmacokinetics with peak plasma levels within minutes. Developed by Alexza Pharmaceuticals for acute treatment of agitation in adults with schizophrenia or bipolar I disorder, it acts primarily through high-affinity antagonism of dopamine D2 and serotonin 5-HT2A receptors, providing rapid onset of action (as early as 10 minutes) superior to placebo in phase III trials, with a number needed to treat for response of 3-4. Approved by the FDA in 2012 and EMA in 2013, it requires administration in a hospital setting under healthcare supervision with bronchodilator availability due to bronchospasm risk, and is available only via the Adasuve REMS program.
- Brand names
- Adasuve
- Other names
- Staccato Loxapine for Inhalation
02
Targets
HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)ADRA1A (α1A)DRD1 (Dopamine D1 Receptor)DRD2 (Dopamine D2 Receptor)DRD4 (Dopamine D4 Receptor)DRD5 (Dopamine D5 Receptor)HRH1 (Histamine H1 Receptor)M1 (Muscarinic acetylcholine receptor M1)
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