Drug intelligence / Profile preview

posatirelin

Development stage
Discontinued
Lead developer
Gedeon Richter
Modality
Peptides, Small Molecules
Administration
Intramuscular, Oral
01

Overview

Posatirelin is a synthetic tripeptide analogue of thyrotropin-releasing hormone (TRH) with enhanced central nervous system effects relative to its hormonal effects. It possesses neurotrophic, cholinergic, and catecholaminergic properties. The drug acts as an agonist at TRH receptors (TRHR) and thyroid-stimulating hormone receptors (TSHR). Posatirelin has demonstrated neuroprotective effects through modulation of monoaminergic and cholinergic systems. The mechanism involves activation of the PI3K/Akt pathway and upregulation of Bcl-2 protein, contributing to its anti-apoptotic effects. Originally developed by Gedeon Richter for the treatment of dementia, particularly vascular dementia and cognitive disorders, the drug showed improvements in cognitive functions, memory, attention, and motivation in clinical studies. It is not currently available for treatment outside clinical trials.

Brand names
Pyladox
Other names
PosatirelinePosatirelinapAad-Leu-Pro-NH2pAad-Leu-Pro-NH-2pAad-Leu-Pro-NH 2L-pyro-2-aminoadipyl-L-leucyl-L-prolinamideL-pyro2-aminoadipyl-L-leucyl-L-prolinamideL-pyro 2-aminoadipyl-L-leucyl-L-prolinamide
02

Targets

TRHR (Thyrotropin-releasing hormone receptor)

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