ErgoNex Pharma has licensed the development rights on Terguride. Oral formulations of terguride have been approved in the treatment of hyperprolactinemic pituitary adenoma, ovulation disorders due to hyperprolactinemia, galactorrhea and suppression of puerperal lactation. Terguride has a benign side effect profile, which is well established in clinical use and confirmed by post-marketing surveillance studies.
ErgoNex Pharma is presently studying the clinical utilities of Terguride PAH in clinical proof-of-concept studies.
Terguride modulates a spectrum of neurotransmitter receptors including dopamine, serotonin, and alpha2-adrenergic receptors with high affinity.
Terguride is a strong anti-serotoninergic drug and acts as an antagonist of the 5-HT2 receptors. 5-HT2 receptor isoforms have been implicated in trophic effects of serotonin (5-HT). Excessive vascular remodeling processes or fibrosis, respectively, in a number of tissues including liver, kidney, heart valve and lung have been associated with altered 5-HT signalling or metabolism. In pulmonary arterial hypertension (PAH) and idiopathic pulmonary fibrosis (IPF) 5-HT has been implicated in excessive wound healing processes with extensive proliferation of arterial smooth muscle cells in PAH, or transformation of fibroblasts into an extracellular matrix depositing fibromyoblast phenotype in lung parenchyma. In pulmonary hypertension 5-HT receptor signalling plays a key role in pulmonary vascular remodelling processes, which are the main driving force for the advanced stages of the disease. Excessive proliferative effects of 5-HT also manifest in cardiomyocytes and contribute directly to progression to heart failure. Terguride has potent anti-proliferative and anti-fibrotic activity and thereby drives reverse remodelling processes.
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Pharmacological Profile of Terguride | View larger version |
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5-HT2 receptor activation stimulates cell proliferation and fibrosis | View larger version |










