TRH agonists(thyrotropin releasing hormone agonists), TRHR agonists(Thyrotropin releasing hormone receptor agonists), TSHR agonists(Thyroid stimulating hormone receptor agonists)

Therapeutic Areas

Nervous System Diseases

Active Indication

Nervous System Diseases

Inactive Indication

Cognition DisordersDementia

Originator Organization

Gedeon Richter USA, Inc.

Active Organization

Chemical Works of Gedeon Richter Plc

Inactive Organization

Gedeon Richter USA, Inc.Gedeon Richter Pharma GmbH

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC17H28N4O4

InChIKeyDPNGIIPSQYKWQA-AVGNSLFASA-N

CAS Registry78664-73-0

100 Clinical Results associated with Posatirelin

100 Translational Medicine associated with Posatirelin

100 Patents (Medical) associated with Posatirelin

Literatures (Medical) associated with Posatirelin

01 Dec 2010·NeuropeptidesQ3 · MEDICINE

Protective effects of TRH and its analogues against various cytotoxic agents in retinoic acid (RA)-differentiated human neuroblastoma SH-SY5Y cells

Q3 · MEDICINE

Article

Author: W. Lason ; M. Leskiewicz ; B. Budziszewska ; M. Kubera ; L. Jaworska-Feil ; D. Jantas ; A. Basta-Kaim ; A.W. Lipkowski

TRH (thyroliberin) and its analogues were reported to possess neuroprotective effects in cellular and animal experimental models of acute and chronic neurodegenerative diseases. In the present study we evaluated effects of TRH and its three stable analogues, montirelin (CG-3703), RGH-2202 and Z-TRH (N-(carbobenzyloxy)-pGlutamyl-Histydyl-Proline) on the neuronally differentiated human neuroblastoma SH-SY5Y cell line, which is widely accepted for studying potential neuroprotectants. We found that TRH and all the tested analogues at concentrations 0.1-50 μM attenuated cell damage induced by MPP(+) (2 mM), 3-nitropropionate (10 mM), hydrogen peroxide (0.5 mM), homocysteine (250 μM) and beta-amyloid (20μM) in retinoic acid differentiated SH-SY5Y cells. Furthermore, we demonstrated that TRH and its analogues decreased the staurosporine (0.5 μM)-induced LDH release, caspase-3 activity and DNA fragmentation, which indicate the anti-apoptotic proprieties of these peptides. The neuroprotective effects of TRH (10 μM) and RGH-2202 (10 μM) on St-induced cell death was attenuated by inhibitors of PI3-K pathway (wortmannin and LY294002), but not MAPK/ERK1/2 (PD98059 and U0126). Moreover, TRH and its analogues at neuroprotective concentrations (1 and 10 μM) increased expression of Bcl-2 protein, as confirmed by Western blot analysis. All in all, these results extend data on neuroprotective properties of TRH and its analogues and provide evidence that mechanism of anti-apoptotic effects of these peptides in SH-SY5Y cell line involves induction of PI3K/Akt pathway and Bcl-2. Furthermore, the data obtained on human cell line with a dopaminergic phenotype suggest potential utility of TRH and its analogues in the treatment of some neurodegenerative diseases including Parkinson's disease.

01 Nov 2004·Journal of the Neurological SciencesQ4 · MEDICINE

Treatment of vascular dementia: evidence from trials with non-cholinergic drugs

Q4 · MEDICINE

Review

Author: Pantoni, Leonardo

A considerable number of therapeutic trials have been performed in vascular dementia (VaD). The results of these trials have generally been considered as disappointing and no drug treatment has been so far approved for the treatment of VaD by regulatory agencies. The aim of the present paper is to critically review the results of randomized clinical trials performed with non-cholinergic drugs in VaD. The conclusions of the present review are that: (1) some drugs such as nicergoline, memantine, posatirelin, propentofylline, and pentoxifylline have shown some, although partly limited, benefits in VaD patients; (2) besides a lack of efficacy of the tested drugs, possible causes of the negative results of many randomized clinical trials in VaD are the enrollment of patients with heterogeneous subtypes of VaD, the small sample size, and the use of end-points and cognitive tests inadequate for the VaD setting because derived from previous experience in the field of Alzheimer disease. Preliminary analyses show that focusing therapeutic trials on specific forms of VaD such as the subcortical type may lead to results different from those obtained in a heterogeneous VaD group. This selective focus seems to be better suited for disclosing specific treatments in the field of VaD.

01 Jan 2002·Acta pharmaceutica Hungarica

[TRH analogs at Gedeon Richter Ltd.: highlights of experimental and clinical efficacy of posatirelin].

Article

Author: Sarkadi, Adám ; Kárpáti, Egon

The chemical research for dissociation of the central nervous system effects of thyrotropin-releasing hormone (TRH) from its hormonal activity resulted in the selection of RGH-2202 (posatirelin) for further development. Posatirelin showed stronger vigilance enhancing effect than TRH in a variety of commonly used neuro-psychopharmacological model in mice, rats and cats. This drug had positive effects in animal models of disturbed consciousness, and counteracted the decline of learning and memory capacity shown by aged or memory impaired rats. Posatirelin had a trophic effect on neurons both 'in vitro' and 'in vivo' as well. Activation of various neurotransmission systems has been demonstrated, but the "modulatory" action of this neuropeptide-like compound is too complex to be explained by a single mechanism. Posatirelin practically had no hormonal activity or other significant side effects either in animal studies or in clinical trials. The arousal level increasing and the neuronotrophic effects appeared in part in trials of human brain injuries and cerebral infarction. Patients suffering in dementia syndromes of either vascular or degenerative origin and treated chronically with posatirelin showed significant improvement in intellectual performance, in orientation, motivation and memory function in all well controlled trials.

100 Deals associated with Posatirelin

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Dementia	Phase 1	HU	Gedeon Richter Pharma GmbH	01 Jan 2002
Cognition Disorders	Phase 1	-	Gedeon Richter USA, Inc.	-
Nervous System Diseases	Preclinical	HU	Chemical Works of Gedeon Richter Plc	01 May 2002

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