Drug intelligence / Profile preview

Staccato prochlorperazine

Development stage
Unknown
Lead developer
Ferrer
Modality
Small Molecules
Administration
Inhalation
01

Overview

Staccato prochlorperazine is an investigational inhaled formulation of the dopamine D2‑receptor antagonist prochlorperazine delivered via Alexza’s single‑use, breath‑actuated Staccato thermal aerosol device for rapid systemic absorption, developed primarily for the acute treatment of nausea and vomiting, including chemotherapy‑induced or migraine‑associated nausea.[4][5][13][15] Prochlorperazine is a first‑generation phenothiazine antipsychotic that blocks D2 receptors in key brain regions such as the chemoreceptor trigger zone and mesolimbic pathways, and also exhibits antagonism at histaminergic, cholinergic, and alpha‑adrenergic receptors, providing potent antiemetic and antipsychotic activity but with a risk of extrapyramidal symptoms, sedation, orthostatic hypotension, and hyperprolactinemia.[4][13] The Staccato inhalation route is intended to provide very rapid onset and needle‑free parenteral‑like exposure for acute use situations, but the program has been limited to early clinical pharmacokinetic evaluation.

Brand names
CompazineStemetilBuccastemStemeticCompro
Other names
prochlorperazine
02

Targets

ADRA1A (α1A)DRD2 (Dopamine D2 Receptor)mAChR (Muscarinic acetylcholine receptors)HRH1 (Histamine H1 Receptor)

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