Apelin
Also known as: [Pyr1]apelin-13, apelin-13, apelin-17, apelin-36, Apelin‑13, Apelin‑36, APJ ligand, APLN, ELABELA
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Summary
Apelin is a 36‑amino‑acid endogenous peptide (with shorter active fragments such as Apelin‑13) that serves as the natural ligand for the APJ receptor. It regulates blood pressure, cardiac contractility, angiogenesis, and glucose homeostasis. Synthetic analogues are under investigation for heart‑failure, pulmonary arterial hypertension and metabolic disease.
Mechanism of Action
binds the APJ (APELA) G‑protein‑coupled receptor, activating downstream PI3K/Akt, MAPK, and nitric‑oxide pathways that modulate cardiovascular tone, fluid balance and metabolic signaling
Routes of Administration
Goals & Uses
- Heart failureCardiovascularModerate
- Heart failure treatmentCardiovascularModerate
- Metabolic syndrome / obesityMetabolicLow
- Cardioprotection / ischemia-reperfusion injuryCardiovascularLow
- Fluid balance / hyponatremiaEndocrine / RenalLow
- Pulmonary arterial hypertension (PAH)Cardiovascular / PulmonaryModerate
- Pulmonary arterial hypertensionCardiovascular / PulmonaryModerate
- Type 2 diabetes mellitusMetabolicLow
Contraindications
- PregnancyPopulationModeratePotential fetal risk or insufficient safety data
- Known hypersensitivity to apelin or formulation componentsImmunologicHigh
- Severe hypotensionCardiovascularHigh
Adverse Effects
- Injection site reactionsLocalUncommon
- HypotensionCardiovascularCommonLow blood pressure
- FlushingVascularUncommonWarmth and redness of the skin
- TachycardiaCardiovascularUncommonAbnormally fast heart rate
- NauseaGastrointestinalRareFeeling of sickness or urge to vomit
Drug Interactions
- Beta‑blockersLow
- ACE2 inhibitors / substratesLow
- ACE inhibitorsModerate
- AntihypertensivesModerateMay potentiate hypotensive effects in some contexts
- Vasopressin / AVP analogues (e.g., desmopressin)Moderate
Population Constraints
- PregnancyReproductive SafetyRelative
- Elderly with hemodynamic instabilityAge / CardiovascularRelative
- Renal impairmentOrgan ImpairmentRelative
- Severe renal impairmentOrgan ImpairmentRelative
- Pediatric populationsAgeRelative
- Pregnant womenReproductiveRelative
Regulatory Status
- European UnionUnapprovedNo marketing authorization; clinical research ongoing
- United StatesUnapprovedInvestigational New Drug (IND) status for early‑phase trials
- United KingdomInvestigationalUniversity of Edinburgh and collaborators have conducted Phase I/II trials with apelin-13 and analogs in heart failure and PAH.
No approved pharmaceutical product containing apelin; investigational use only in early‑phase clinical trials.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Apelin?
Apelin is a 36‑amino‑acid endogenous peptide (with shorter active fragments such as Apelin‑13) that serves as the natural ligand for the APJ receptor. It regulates blood pressure, cardiac contractility, angiogenesis, and glucose homeostasis. Synthetic analogues are under investigation for heart‑failure, pulmonary arterial hypertension and metabolic disease.
What is Apelin used for?
Apelin is educationally associated with: Heart failure, Heart failure treatment, Metabolic syndrome / obesity, Cardioprotection / ischemia-reperfusion injury, Fluid balance / hyponatremia, Pulmonary arterial hypertension (PAH), Pulmonary arterial hypertension, Type 2 diabetes mellitus. Educational only — not medical advice.
How is Apelin administered?
Recorded routes of administration: Intranasal, Intravenous, Subcutaneous.
What are the potential side effects of Apelin?
Reported adverse effects include: Injection site reactions, Hypotension, Flushing, Tachycardia, Nausea. This list is not exhaustive — consult a qualified clinician.
Who should avoid Apelin?
Recorded contraindications: Pregnancy, Known hypersensitivity to apelin or formulation components, Severe hypotension. Consult a qualified clinician before use.