Drug intelligence / Profile preview

LEAP2 fragment

Development stage
Unknown
Lead developer
Herlev & Gentofte Hospital
Modality
Peptides
Administration
Intravenous
01

Overview

LEAP2 fragment (specifically LEAP2(38-47)) is a 10-residue N-terminal fragment of liver-expressed antimicrobial peptide 2 (LEAP2), an endogenous peptide hormone. It acts as an antagonist and inverse agonist of the growth hormone secretagogue receptor (GHSR), also known as the ghrelin receptor. LEAP2 is upregulated in human enteroendocrine cells following Roux-en-Y gastric bypass (RYGB) surgery. The LEAP2 fragment has been shown to increase glucose-stimulated insulin secretion (GSIS) in isolated human pancreatic islets in vitro, suggesting a potential role in improving glucose metabolism and treating type 2 diabetes and obesity. However, in clinical studies, intravenous infusion of the fragment in healthy individuals did not demonstrate significant glucoregulatory effects, likely due to its low potency and rapid degradation in vivo.

Other names
LEAP-2 fragmentLEAP2 fragmentLEAP 2 fragmentLEAP-2(38-47)LEAP2 38-47LEAP-2 38-47LEAP 2 38-47LEAP2(38-47)LEAP238-47LEAP-238-47LEAP 238-47LEAP238–47
02

Targets

GHRL (Ghrelin)GHSR (Growth hormone secretagogue receptor)

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