仏Amolyt社による、欧州内分泌学会(ECE)での当社からのライセンス品であるAZP-3813の研究成果の発表資料

2022/05/24　ペプチドリーム　株式会社　

AZP-3813, a Bicyclic 16-Amino Acid Pep7de Antagonist of the
Human Growth Hormone Receptor as a Poten7al New
Treatment for Acromegaly

Stéphane Milano1, Haruaki Kurasaki2, Tatsuya Tomiyama2, Patrick Reid2, Aart Jan Van der Lely3, Michael D. Culler41Amolyt Pharma, Ecully, France, 2Pep4Dream, Inc., Kawasaki-Shi, Kanagawa , Japan, 3Erasmus University Medical Center, RoGerdam, Netherlands, 4
Amolyt Pharma, Cambridge, MassachuseGs, United States

INTRODUCTION: Acromegaly is typically caused by an adenoma of thesomatotroph cells of the pituitary that hyper-secretes growth hormone(GH), which in turn sEmulates excess insulin-like growth factor 1 (IGF1)producEon and the resulEng overgrowth of Essues and diseasemanifestaEons. Suppression and control of IGF1 levels in acromegalythrough medical therapy is based on either suppressing GH secreEonfrom the pituitary or inhibiEng GH acEon by prevenEng interacEon withits receptor (Figure 1). AZP-3813 is a 16-amino acid, bicyclic pepEdeantagonist of the GH receptor (GHR) that was derived from pepEdesequences discovered using a unique, cell-free in vitro transcripEon-translaEon system screened against the human GHR, and that wasopEmized by raEonal design to increase binding a？nity, solubility andhalf-life. To determine if the potent GH receptor antagonism displayedin vitro translates to in vivo e？cacy, the ability of AZP-3813 to suppressIGF1 levels in normal juvenile rats was examined.

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