Drug intelligence / Profile preview

PF-06649751 + trimethobenzamide hydrochloride

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

This is a combination of PF-06649751 (tavapadon), a novel, orally administered, non-catechol-based, highly selective dopamine D1/D5 receptor partial agonist, and trimethobenzamide hydrochloride, an antiemetic agent. PF-06649751 is under investigation for the symptomatic treatment of motor symptoms in Parkinson’s disease and acts by partially activating dopamine D1 and D5 receptors in the brain, possibly providing motor benefit while avoiding side effects of full agonists and older catechol-based D1 agonists[1][3][7]. Trimethobenzamide hydrochloride is used to manage nausea and vomiting, likely by acting on the chemoreceptor trigger zone in the medulla, though its mechanism is not precisely known; it does not primarily act on dopamine or serotonin receptors[2][6][8]. This combination may be investigated to address the nausea commonly associated with dopaminergic therapies.

Brand names
Tigan
Other names
trimethobenzamide HCl
02

Targets

DRD1 (Dopamine D1 Receptor)DRD5 (Dopamine D5 Receptor)H (Histamine receptors)

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