Drug intelligence / Profile preview

lergotrile mesylate

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

Overview

Lergotrile mesylate is a **synthetic nonpeptide ergot alkaloid derivative** and a **direct-acting dopamine receptor agonist**. It was developed primarily for the treatment of **Parkinson’s disease**, particularly for patients experiencing insufficient response or complications from levodopa therapy. The drug acts by stimulating dopamine receptors, leading to improvement in parkinsonian symptoms such as tremor, rigidity, bradykinesia, although its greatest benefit is seen in tremor reduction. Lergotrile mesylate also acts as a **prolactin secretion inhibitor**. However, its use was halted due to concerns over liver toxicity observed in clinical trials[1][3][4][8][10].

Other names
lergotrile mesylate2-chloro-6-methylergoline-8β-acetonitrile methanesulfonate
02

Targets

ADRA1A (α1A)DRD2 (Dopamine D2 Receptor)

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