Where it comes from
- Made in
- Endothelium, heart, fat tissue, hypothalamus and stomach
- Sent out by
- Hypoxia, insulin and exercise raise it; cut from the precursor into several lengths
- Acts on
- Vascular endothelium and smooth muscle
- Heart muscle
- Hypothalamus (vasopressin neurons)
- Kidney
What it does
In medicine
- No medicine acts on the apelin receptor. Short infusions in people with heart failure raised cardiac output and lowered blood pressure, which is as far as the clinic has gone 1
- Blood apelin is not a clinical test: it falls in pulmonary arterial hypertension and in advanced heart failure, but the assays disagree with each other and none is standardised
Beyond the body’s own use
- AMG 986, a small-molecule apelin receptor agonist taken by mouth, was given to 182 people including 20 with heart failure. It was tolerated, but no clinically meaningful effect on the heart was seen 2
- Stabilised apelin analogues are still early work. The peptide is destroyed by ACE2 and neprilysin within minutes, so every programme is a chemistry problem before it is a cardiology one 3
- It is studied in diabetes, where it improves insulin sensitivity in mice; no human study has looked at glucose
- A thirteen-residue peptide is digested if swallowed, so no route to the receptor avoids either an injection or a redesigned molecule 2
Sources
- Japp et al., Acute cardiovascular effects of apelin in humans, Circulation 2010
- Winkle et al., A first-in-human study of AMG 986, a novel apelin receptor agonist, Cardiovascular Drugs and Therapy 2023
- Tatemoto et al., Isolation of a novel endogenous peptide ligand for the human APJ receptor, Biochemical and Biophysical Research Communications 1998
This card describes what a medicine is for and what the evidence says; it recommends nothing. Talk to your clinician about anything you read here.