Drug intelligence / Profile preview

hexarelin

Development stage
Preclinical
Lead developer
Mediolanum Farmaceutici
Modality
Peptides, Small Molecules
Administration
Oral, Intravenous, Subcutaneous, Intranasal
01

Overview

Hexarelin (also known as examorelin) is a synthetic hexapeptide and potent growth hormone secretagogue (GHS), developed by Mediolanum Farmaceutici. It acts as a highly selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR), stimulating the release of growth hormone from the pituitary gland by mimicking the action of endogenous ghrelin[1][6][8]. Hexarelin is centrally penetrant and orally active, with additional routes including intravenous, subcutaneous, and intranasal administration[1][7]. Beyond its GH-releasing effects, hexarelin has demonstrated cardioprotective activity in preclinical models—improving heart function and reducing cardiac fibrosis and ischemic injury—mediated through both GHSR 1a and CD36 receptors in cardiac tissue[3][4][5]. It also exhibits antioxidative properties by reducing reactive oxygen species production and enhancing antioxidant enzyme activity[4]. Secondary endocrine effects include mild stimulation of cortisol, prolactin, and ACTH secretion[6].

Other names
examorelinL-Histidyl-2-methyl-D-tryptophyl-L-alanyl-L-tryptophyl-D-phenylalanyl-L-lysinamideL-Histidyl2-methyl-D-tryptophyl-L-alanyl-L-tryptophyl-D-phenylalanyl-L-lysinamideL-Histidyl 2-methyl-D-tryptophyl-L-alanyl-L-tryptophyl-D-phenylalanyl-L-lysinamide
02

Targets

GHSR (Growth hormone secretagogue receptor)CD36 (CD36 antigen)

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