Drug intelligence / Profile preview

apelin-13

Development stage
Phase 1
Modality
Peptides, Recombinant Proteins and Enzymes
Administration
Intravenous, Subcutaneous, Intraperitoneal, Intracerebroventricular, Intravitreal
01

Overview

Apelin-13 is a bioactive peptide and the predominant active isoform of the endogenous ligand for the G protein-coupled receptor APJ (also known as the apelin receptor). It exerts potent vasodilatory and antihypertensive effects, acts as a positive inotrope in cardiac tissue, and has demonstrated anti-inflammatory, antithrombotic, neuroprotective, and metabolic regulatory properties. Apelin-13 is widely distributed in both central nervous system tissues (notably hippocampus) and peripheral organs. Mechanistically, it binds to the APJ receptor to activate multiple intracellular signaling pathways including nitric oxide-cGMP signaling (inhibiting platelet aggregation), PI3K/Akt/mTOR pathway (metabolic regulation), ERK/MAPK pathway (cell survival), AMPK activation (glucose uptake/insulin sensitivity), and suppression of pro-inflammatory cytokines such as TNF-alpha and IL-1β. Preclinical studies suggest therapeutic potential for cardiovascular diseases (heart failure, myocardial infarction), metabolic syndrome/type 2 diabetes mellitus, neurodegenerative disorders like Alzheimer's disease via anti-neuroinflammatory actions, chronic kidney disease due to its renal hemodynamic effects, osteoporosis by modulating bone metabolism markers, hyponatremia through water/salt balance regulation via increased urinary excretion of sodium/water. Clinical trials are ongoing or planned for heart failure/pulmonary hypertension/chronic kidney disease/hyponatremia.

Other names
[Pyr1]-apelin-13Pyr-apelin-13Pyr-apelin13Pyr-apelin 13Apelin 13Apelin13Apelin-13
02

Targets

APLNR (Apelin receptor)

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