OncoSignal
Live from Open Targets Platform, fetched 2026-11-12 01:11 UTC. Every row links to its source record.

APLNR apelin receptor

ENSG00000134817 · protein coding · Open Targets profile

G protein-coupled receptor for peptide hormones apelin (APLN) and apelin receptor early endogenous ligand (APELA/ELA), that plays a role in the regulation of normal cardiovascular function and fluid homeostasis (PubMed:11090199, PubMed:22810587, PubMed:25639753, PubMed:28137936, PubMed:35817871, PubMed:38428423). When acting as apelin receptor, activates both G(i) protein pathway that inhibits adenylate cyclase activity, and the beta-arrestin pathway that promotes internalization of the receptor (PubMed:11090199, PubMed:25639753, PubMed:28137936, PubMed:35817871, PubMed:38428423). APLNR/APJ also functions as mechanoreceptor that is activated by pathological stimuli in a G protein-independent fashion to induce beta-arrestin signaling, hence eliciting cardiac hypertrophy (PubMed:22810587, PubMed:38428423). However, the presence of apelin ligand blunts cardiac hypertrophic induction from APLNR/APJ on response to pathological stimuli (PubMed:22810587, PubMed:38428423). Plays a key role in early development such as gastrulation, blood vessels formation and heart morphogenesis by acting as a APELA receptor (By similarity). May promote angioblast migration toward the embryonic midline, i.e. the position of the future vessel formation, during vasculogenesis (By similarity). Promotes sinus venosus (SV)-derived endothelial cells migration into the developing heart to promote coronary blood vessel development (By similarity). Also plays a role in various processes in adults such as regulation of blood vessel formation, blood pressure, heart contractility and heart failure (PubMed:25639753, PubMed:28137936). {ECO:0000250|UniProtKB:Q7SZP9, ECO:0000250|UniProtKB:Q9WV08, ECO:0000269|PubMed:11090199, ECO:0000269|PubMed:22810587, ECO:0000269|PubMed:25639753, ECO:0000269|PubMed:28137936, ECO:0000269|PubMed:35817871, ECO:0000269|PubMed:38428423}.

In 1 of 15 cancers, the evidence for APLNR comes mainly from inherited variants

Each row is a cancer, strongest overall evidence first. The two dots show how strong the inherited (germline) and tumour-mutation (somatic) evidence is; the line between them is the gap.

Inherited (germline) variantsMutations in tumours (somatic)
00.250.50.751glioblastomaglioblastomahepatocellular carcinomahepatocellular carcinomanasopharyngeal carcinomanasopharyngeal carcinomamelanomamelanomacentral nervous system cancercentral nervous system cancernonpapillary renal cell carcinomanonpapillary renal cell carcinomagliomagliomavein of Galen aneurysmvein of Galen aneurysmpancreatic ductal adenocarcinomapancreatic ductal adenocarcinomamalignant mesotheliomamalignant mesotheliomapleural mesotheliomapleural mesotheliomacervical carcinomacervical carcinomacervical carcinoma: germline 0.06blue rubber bleb nevusblue rubber bleb nevuscolon carcinomacolon carcinomaliver dysplastic noduleliver dysplastic nodule

Scores run from 0 (no evidence) to 1 (strongest). A missing dot at 0 means Open Targets holds no evidence of that kind. Source: Open Targets Platform, fetched live.

Tractability

Small molecule
Structure with Ligand, High-Quality Ligand, Druggable Family
Antibody
UniProt loc high conf, GO CC high conf, UniProt SigP or TMHMM
PROTAC
Small Molecule Binder
Other modalities
Advanced Clinical

gnomAD loss of function constraint: o/e 0.5561400055885315 (upper bound 0.8841999769210815). Low values mean loss of function is poorly tolerated, a safety flag for inhibition.

Who runs trials of these drugs

Principal investigators and study chairs on 9 registry trials, updated in the last three years, of the most advanced drugs against APLNR (apelin), ranked by Phase 2+ trials. Live from ClinicalTrials.gov.

6 of 9 trials of drugs against APLNR have sites only in Europe

Registry trials of apelin updated in the last three years, counted by the country group of their listed sites. A trial with sites in several groups counts in each; 9 of 9 have all sites in one country.

Sites only in this groupSites here and elsewhere
EuropeEurope: 6 trials with sites only hereEurope: 0 trials with sites here and elsewhere6OtherOther: 3 trials with sites only hereOther: 0 trials with sites here and elsewhere3

Site counts are not patients per country, and trials registered only outside ClinicalTrials.gov are not covered. Where sites are is a fact about the record, not a judgement of its quality. Europe is the EU and EEA, the UK and Switzerland. Source: ClinicalTrials.gov, fetched live.

1 trials of drugs against APLNR were stopped early

Terminated, withdrawn and suspended interventional trials of apelin, newest update first, live from ClinicalTrials.gov. Each reason is quoted exactly as the registry gives it; we do not sort reasons into safety, efficacy or business. Dates are the last registry update. Showing the 1 most recent of 1.

  • withdrawn · 2012-08-23 · University of Aarhus · matched by the registry's drug synonyms
    “As a single center, it was not possible to recruit enough patients with pulmonary hypertension”
Paediatric incentives and obligations for APLNR's drugs

For apelin: what EMA and FDA publish about paediatric plans, orphan status and pediatric approvals, and how many registered studies take children. Each line is a yes, no or not published fact from the record linked under it; none of it is a forecast.

Rare pediatric disease voucher. FDA, content current as of 29 Apr 2026: “As of February 3, 2026, enactment of the Consolidated Appropriations Act, 2026, the rare pediatric disease PRV program will sunset after September 30, 2029. FDA may not award any PRVs under this program after September 30, 2029.” Voucher sale prices are not shown here; they appear only as company-reported news. FDA: Rare Pediatric Disease Designation and Priority Review Voucher Programs

All 1 drugs and clinical candidates as a table

Each drug, stage and indication links to its Open Targets record, where the trials and approvals behind it are listed. Salt forms (for example a mesylate) are listed as Open Targets records them, as separate entries.

DrugTypeHighest stageIndicationsSource records
APELINUnknownphase 2type 2 diabetes mellitus, heart failure, pulmonary arterial hypertension, pulmonary hypertension, HyponatremiaOpen Targets · ChEMBL