Searchable abstracts of presentations at key conferences in endocrinology

ea0081p148 | Pituitary and Neuroendocrinology | ECE2022

AZP-3813, a bicyclic 16-amino acid peptide antagonist of the human growth hormone receptor as a potential new treatment for acromegaly

Milano Stephane , Kurasaki Haruaki , Tomiyama Tatsuya , Reid Patrick , Jan Van der Lely Aart , Culler Michael D.

Medical treatment of acromegaly is based on either suppressing pituitary GH secretion or inhibiting GH action by preventing interaction with its receptor in order to suppress the elevated levels of IGF1. AZP-3813 is a 16-amino acid, bicyclic peptide antagonist of the GH receptor (GHR) derived from peptide sequences discovered using a unique, cell-free in vitro transcription-translation system screened against the human GHR, and that was optimized by rational design to increase...

ea0063oc6.1 | Obesity | ECE2019

Impaired glucose homeostasis in leptin-deficient ob/ob mice is corrected by AZP-3404, a 9-amino acid peptide analog derived from insulin-like growth factor-binding protein 2, a key mediator of leptin action

Culler Michael D , Delale Thomas , Milano Stephane , van der Lely Aart Jan , Abribat Thierry , Clemmons David

The key metabolic hormone, leptin, acts in part through the liver to regulate glucose homeostasis, as well as the maturation of both adipocytes and osteoblasts. These actions have been demonstrated to be mediated by insulin-like growth factor binding protein 2 (IGFBP-2), independent of its ability to bind IGF1. The effects of IGFBP-2 on adipocyte and osteoblast maturation can be localized to a short peptide sequence within the unique heparin binding domain (HBD-1) of IGFBP-2. ...

ea0063p621 | Diabetes, Obesity and Metabolism 2 | ECE2019

Nonclinical development of livoletide (AZP-531), a peptide analog of unacylated ghrelin for the treatment of hyperphagia in Prader-Willi syndrome

Milano Stephane , Allas Soraya , Cade Didier , Briffaux Jean-Paul , Spencer Andrew

Prader-Willi syndrome (PWS) is a rare complex endocrine disease characterized by hyperphagia and abnormal food-related behaviors that contribute to severe morbidity and early mortality and to a significant burden on patients and caregivers. There are no approved treatments for hyperphagia in PWS. Patients with PWS have increased circulating levels of the orexigenic hormone acylated ghrelin (AG) with a relative deficit of unacylated ghrelin (UAG). These abnormalities in AG and ...

ea0099oc2.3 | Oral Communications 2: Calcium and Bone | Part I | ECE2024

A translational approach to investigate the mechanism whereby eneboparatide induces prolonged calcium normalization in patients with chronic hypoparathyroidism

Ravel Guillaume , Datta Rakesh , Milano Stephane , Ovize Michel , Allas Soraya , Aouadi Myriam , Culler Michael

Maintaining normal serum and urinary calcium in patients with chronic hypoparathyroidism (cHP) remains a therapeutic challenge. Parathyroid hormone (PTH) replacement therapy is not ideal due to its short half-life and transient activation of the PTH 1 receptor (PTH1R). Eneboparatide is a hybrid analog of PTH and PTH-related peptide specifically designed to induce prolonged activation of the PTH1R. Despite a short half-life, eneboparatide is able to normalize serum and urinary ...

ea0090oc8.2 | Oral Communications 8: Calcium and Bone | ECE2023

Eneboparatide, a Novel PTH-1 Receptor Agonist, Has No Impact on Bone Parameters Following Chronic Treatment of Non-Human Primates

Ravel Guillaume , Delale Thomas , Milano Stephane , Chirat Sophie , Verset Michael , Latronico Emilie , Allas Soraya , Culler Michael D.

Eneboparatide (AZP-3601) is a novel, synthetic, 36-amino-acid peptide agonist of the parathyroid hormone type 1 receptor (PTHR1), with potent selectivity for the R0 conformation. This results in prolonged calcemic responses, while having a short circulating half-life. Eneboparatide is being developed for the treatment of chronic hypoparathyroidism (cHP). Studies in hypoparathyroid animal models and, most recently, in hypoparathyroid patients, have demonstrated that eneboparati...