Teluron (terguride) / Pfizer, ErgoNex - LARVOL DELTA

5-HT2/5-HT2B receptor inhibition abrogate fibrotic potential of peritoneal fibroblasts by reducing the production of extracellular matrix proteins in PD patients (ISN-WCN 2024) - "We aimed to evaluate anti-fibrotic role of inhibitors of 5-HT2 and 5-HT2B (Terguride and SB204741), respectively in human peritoneal fibroblasts (HPFBs) isolated from peritoneum of PD patients... 5-HT receptor antagonists attenuate 5-HT/TGF-β1 mediated pro-fibrotic potential of HPFBs by attenuating the production of ECM proteins and alpha smooth muscle actin in HPFBs."

Clinical • Fibrosis • ACTA2 • COL1A1 • COL1A2 • CTGF • IL17A • IL1B • IL6 • MMP2 • TGFB1 • TIMP1

Challenges of Pituitary Apoplexy in Pregnancy. (PubMed, J Clin Med) - "Pre-pregnancy medication included dopamine agonists (15/43) and terguride (1/43) in addition to subsequent insulin therapy for gestational diabetes (N = 2) and type 1 diabetes mellitus (N = 1)...PAPP is exceptionally reported. To our knowledge, this sample-case series study is the largest of its kind that is meant to increase the awareness to the benefit of the maternal-fetal outcomes from multidisciplinary insights."

Journal • Review • CNS Disorders • Endocrine Cancer • Endocrine Disorders • Gestational Diabetes • Gynecology • Infectious Disease • Metabolic Disorders • Neuroendocrine Tumor • Oncology • Ophthalmology • Pain • Pituitary Gland Carcinoma • Solid Tumor • Type 1 Diabetes Mellitus

5-HT2 and 5-HT2B Receptor Antagonism Abrogates Fibrotic Potential of Human Renal Allograft Fibroblasts by Targeting STAT3 Pathway (KSN 2023) - "We aimed to evaluate the anti-fibrotic role of inhibitors of 5-HT and 5-HT (Terguride and SB204741), respectively in human renal fibroblasts (HRFB) isolated from renal allograft rejection patients... TGF-β1 mediated non-canonical pathways, ERK1/2 and STAT3 have been implicated in the development of fibrosis. 5-HT receptor antagonists might reduce the fibrotic potential of HRFB via suppression of TGF-β1 mediated non-canonical pathways."

Fibrosis • Transplant Rejection • Transplantation • ACTA2 • COL1A1 • COL1A2 • CTGF • MMP2 • SMAD3 • TGFB1 • TIMP1

"Terguride ameliorates monocrotaline-induced pulmonary hypertension in rats." R. Dumitrascu, C. Kulcke, M. Königshoff, et al. Eur Respir J 2011; 37: 1104-1118. (PubMed, Eur Respir J) - No abstract available

Journal • Preclinical • Hypertension • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases

Aggressive Pituitary Adenoma Not Fulfilling the New High-Risk Criteria with Progression after 18-Year Stable Clinical Course: Case Report. (PubMed, J Neurol Surg A Cent Eur Neurosurg) - " Pathologic confirmation for the present definition would be expected to assess the cutoff between typical adenomas and aggressive tumors."

Clinical • Journal • Endocrine Cancer • Oncology • Pituitary Gland Carcinoma • MRI

Pharmacological treatment strategies for lowering prolactin in people with a psychotic disorder and hyperprolactinaemia: A systematic review and meta-analysis. (PubMed, Schizophr Res) - "We aimed to examine the evidence from open-label studies and randomized clinical trials (RCTs) that studied four prolactin-lowering therapeutic strategies in people with psychotic disorders and hyperprolactinaemia: 1) switching to prolactin-sparing antipsychotics; 2) adding aripiprazole; 3) adding dopamine agonists; and 4) adding metformin...Nine studies explored switching antipsychotic treatment to aripiprazole (n = 4), olanzapine (n = 1), quetiapine (n = 2), paliperidone palmitate (n = 1) or blonanserin (n = 1)...Six studies explored the addition of cabergoline (n = 3), bromocriptine (n = 2) or terguride (n = 1)...The three placebo-controlled RCTs for aripiprazole addition showed similar withdrawal rates for aripiprazole (10.1%) and placebo (11.5%), without significant differences in the meta-analysis. Our study suggests that, in terms of levels of evidence, adding aripiprazole is the first..."

Journal • Retrospective data • Review • CNS Disorders • Schizophrenia

Effects of 2-bromoterguride, a dopamine D2 receptor partial agonist, on cognitive dysfunction and social aversion in rats. (PubMed, Psychopharmacology (Berl)) - "Our data support 2-bromoterguride as a promising APD candidate due to its beneficial effect on cognitive impairments and negative symptoms of schizophrenia."

Journal • Alzheimer's Disease • Biosimilar • CNS Disorders • Schizophrenia

The Serotonin Receptor 2 Inhibitor Terguride Has Beneficial Effects on Skin Fibrosis: Results from a Phase 2 Proof of Concept Study (ACR-ARHP 2016) - "Terguride was well tolerated in patients with dcSSc. Strong and consistent effects on fibrosis related skin biopsy biomarkers could be observed in this open-label controlled phase 2 proof of concept study, which was further supported by a significant improvement of the mRSS over the control group. These data justify further investigation in an upcoming randomized placebo controlled phase 3 study."

Adverse events • Retrospective data • Biosimilar • Fibrosis • Immunology • Systemic Sclerosis

Blocking properties of terguride at the 5-HT2 receptor subtypes mediating cardiovascular responses in the rat. (PubMed, Can J Physiol Pharmacol) - "These results, taken together, suggest that terguride behaved as an antagonist at the 5-HT2 receptors located, probably, in the central nervous system and/or the systemic vasculature. This is the first evidence demonstrating that terguride can block central/peripheral 5-HT2 receptors mediating cardiovascular responses in anaesthetized or pithed rats."

Journal • Preclinical • Anesthesia

5-HT2 AND 5-HT2B RECEPTOR INHIBITION ATTENUATE PERITONEAL FIBROSIS BY TARGETING NON-CANONICAL SIGNALING PATHWAYS INCLUDING STAT3 (ISN-WCN 2019) - "...We aimed to evaluate anti-fibrotic role of inhibitors of 5-HT2 and 5-HT2B (Terguride and SB204741), respectively in human peritoneal fibroblasts (HPFB) isolated from peritoneum of CAPD patients. Biopsy from parietal peritoneum (PB) of control patients (n=8) and CAPD patients (n=6) excised during laparotomy was incubated overnight in dispase (2.4 U/mL)/37°C... TGF-β1 mediated non-canonical pathways, ERK1/2 and STAT3 have been implicated in regulation of pro-fibrotic genes and in the development of fibrosis. 5-HT receptor antagonists might reduce fibrosis via suppression of TGF-β1 mediated non-canonical pathways."