Drug intelligence / Profile preview

pergolide

Development stage
Phase 3
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

Pergolide is a long-acting ergot-derived dopamine agonist that acts primarily on dopamine D2 and D1 receptors, as well as several serotonin (5-HT) receptor subtypes and alpha-adrenergic receptors. It was originally developed for the treatment of Parkinson's disease as adjunct therapy with levodopa/carbidopa, where it works by directly stimulating post-synaptic dopamine receptors in the nigrostriatal system to improve motor symptoms. Pergolide also inhibits prolactin secretion and affects other pituitary hormones. Due to an increased risk of cardiac valvulopathy associated with 5-HT2B receptor activation, pergolide was withdrawn from human markets in the US (2007) and Canada but remains available for veterinary use—most notably under the brand name Prascend for treating Equine Cushing’s syndrome (pituitary pars intermedia dysfunction) in horses[1][3][4][8].

Brand names
PermaxPrascend
Other names
pergolide mesylate
02

Targets

HTR2A (Serotonin receptor 5-HT2A)ADRA1A (α1A)DRD1 (Dopamine D1 Receptor)HTR2B (5-Hydroxytryptamine Receptor 2B)DRD2 (Dopamine D2 Receptor)

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