Drug intelligence / Profile preview

LEAP238-47

Development stage
Preclinical
Modality
Peptides, Small Molecules
Administration
Intravenous
01

Overview

LEAP238-47 is a synthetic peptide fragment corresponding to amino acids 38–47 of liver-expressed antimicrobial peptide 2 (LEAP2), an endogenous human gut hormone. This fragment has demonstrated robust insulinotropic properties, stimulating insulin release in human pancreatic islets at levels comparable to glucagon-like peptide-1. Mechanistically, LEAP238-47 acts as an inverse agonist and antagonist of the growth hormone secretagogue receptor (GHSR, also known as the ghrelin receptor), thereby attenuating tonic GHSR activity. While it shows strong effects on insulin secretion in vitro, intravenous infusion in healthy humans did not produce significant glucoregulatory effects at tested doses. The compound is being explored for its potential metabolic and anti-obesity applications due to its modulation of appetite-regulating pathways[1][6][8].

Other names
LEAP2(38-47)
02

Targets

GHSR (Growth hormone secretagogue receptor)

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