OncoSignal
Live from Open Targets Platform, fetched 2026-11-12 03:51 UTC. Every row links to its source record.

ADORA2A adenosine A2a receptor

ENSG00000128271 · protein coding · Open Targets profile

Receptor for adenosine (By similarity). The activity of this receptor is mediated by G proteins which activate adenylyl cyclase (By similarity). .

10 of the 27 drugs recorded against ADORA2A are approved, and 4 more reached Phase 3

Each band is a group of drugs. It runs from the kind of drug on the left to the furthest stage that drug has reached in any disease on the right. Thicker bands mean more drugs.

7 small molecule drugs at Approved: REGADENOSON, OXTRIPHYLLINE, PENTOXIFYLLINE, ISTRADEFYLLINE, ADENOSINE, CAFFEINE CITRATE, CAFFEINE4 small molecule drugs at Phase 3: APADENOSON, BINODENOSON, TOZADENANT, PRELADENANT12 small molecule drugs at Phase 2: UK432097, SONEDENOSON, REGADENOSON ANHYDROUS, VIPADENANT, SIPAGLADENANT, IMARADENANT, AMP579, ETRUMADENANT, BVT.115959, PBF-509, EVODENOSON, CIFORADENANT1 small molecule drug at Phase 1: PBF-9992 protein drugs at Approved: THEOPHYLLINE, AMINOPHYLLINE1 unknown drug at Approved: DEFIBROTIDESmall molecule 24Protein 2Unknown 1Approved 10Phase 3 4Phase 2 12Phase 1 1

Approved bands are highlighted. Withdrawn means the drug was pulled from the market or from development. A combined phase counts as the later one (Phase 1/2 is shown as Phase 2). Hover a band for the drug names. Source: Open Targets Platform, fetched live.

ADORA2A: inherited and tumour-mutation evidence across 15 cancers

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)
00.250.50.751acute lymphoblastic leukemiaacute lymphoblastic leukemiabreast cancerbreast cancernon-small cell lung carcinomanon-small cell lung carcinomaprostate cancerprostate cancertriple-negative breast carcinomatriple-negative breast carcinomapancreatic ductal adenocarcinomapancreatic ductal adenocarcinomahepatocellular carcinomahepatocellular carcinomafibrosisfibrosisB-cell chronic lymphocytic leukemiaB-cell chronic lymphocytic leukemiacolorectal carcinomacolorectal carcinomahead and neck squamous cell carcinomahead and neck squamous cell carcinomacolorectal cancercolorectal cancercentral nervous system cancercentral nervous system cancergliomagliomaastrocytoma (excluding glioblastoma)astrocytoma (excluding glioblastoma)

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
Approved Drug, Structure with Ligand, High-Quality Ligand, High-Quality Pocket, Druggable Family
Antibody
GO CC high conf, UniProt loc med conf, UniProt SigP or TMHMM
PROTAC
UniProt Ubiquitination, Small Molecule Binder

gnomAD loss of function constraint: o/e 0.5971900224685669 (upper bound 0.9884899854660034). 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 400 registry trials, updated in the last three years, of the most advanced drugs against ADORA2A (regadenoson, defibrotide, oxtriphylline, theophylline, pentoxifylline, istradefylline, aminophylline, adenosine, caffeine, apadenoson, binodenoson, tozadenant), ranked by Phase 2+ trials. Live from ClinicalTrials.gov.

159 of 384 trials of drugs against ADORA2A have sites only in United States

Registry trials of regadenoson, defibrotide, oxtriphylline, theophylline, pentoxifylline, istradefylline, aminophylline, adenosine, caffeine, apadenoson, binodenoson, tozadenant 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; 341 of 384 have all sites in one country.

Sites only in this groupSites here and elsewhere
United StatesUnited States: 159 trials with sites only hereUnited States: 31 trials with sites here and elsewhere190ChinaChina: 19 trials with sites only hereChina: 8 trials with sites here and elsewhere27EuropeEurope: 81 trials with sites only hereEurope: 23 trials with sites here and elsewhere104JapanJapan: 0 trials with sites only hereJapan: 9 trials with sites here and elsewhere9OtherOther: 93 trials with sites only hereOther: 29 trials with sites here and elsewhere122

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. 16 trials list no sites and are left out. Source: ClinicalTrials.gov, fetched live.

269 trials of drugs against ADORA2A were stopped early; 5 of the 200 most recent give no reason

Terminated, withdrawn and suspended interventional trials of regadenoson, defibrotide, oxtriphylline, theophylline, pentoxifylline, istradefylline, aminophylline, adenosine, caffeine, apadenoson, binodenoson, tozadenant, 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 25 most recent of 269.

  • terminated · 2026-11-03 · Philips Clinical & Medical Affairs Global · matched by the registry's drug synonyms
    “The study was stopped due to ongoing enrollment challenges.”
  • terminated · 2026-10-21 · Medical College of Wisconsin · matched by the registry's drug synonyms
    “No longer have funding support to complete the pharmacogenetics component.”
  • suspended · 2026-10-20 · City of Hope Medical Center · 8-Chloroadenosine
    “Safety Issues, status is being updated per PI due to safety issues. Study is now Temporarily Closed to Accrual.”
  • suspended · 2026-09-28 · Weill Medical College of Cornell University · matched by the registry's drug synonyms
    “Study is paused for interim analysis.”
  • terminated · 2026-08-20 · Jules Bordet Institute · matched by the registry's drug synonyms
    “Study logistics or limited study population, as defined by the iclusion/exclusion criteria, leading to a poor recruitment”
  • terminated · 2026-08-04 · Genzyme, a Sanofi Company · matched by the registry's drug synonyms
    “Enrolment formally closed earlier than planned due to recruitment challenges.”
  • terminated · 2026-07-30 · M.D. Anderson Cancer Center · matched by the registry's drug synonyms
    “Slow participant enrollment”
  • terminated · 2026-07-10 · Donald Basel · matched by the registry's drug synonyms
    “data analysis unequivocal - requires study methodology re-evaluation”
  • terminated · 2026-07-06 · Marissa Jarosinski · matched by the registry's drug synonyms
    “Poor recruitment”
  • terminated · 2026-06-30 · Hoffmann-La Roche · matched by the registry's drug synonyms
    “Sponsor decision to discontinue lebrikizumab development for the treatment of asthma.”
  • terminated · 2026-06-22 · University Hospital, Bordeaux · matched by the registry's drug synonyms
    “target number of subjects not reached”
  • terminated · 2026-06-09 · Regeneron Pharmaceuticals · matched by the registry's drug synonyms
    “Sponsor Decision related to study drug supply”
  • terminated · 2026-05-22 · Henry Ford Health System · matched by the registry's drug synonyms
    “Slow recruitment and interim analysis results”
  • terminated · 2026-05-07 · Christoph Grimm · matched by the registry's drug synonyms
    “slow recruitment during COVID pandemia”
  • terminated · 2026-05-06 · Ottawa Heart Institute Research Corporation · matched by the registry's drug synonyms
    “Testing supplies unavailable.”
  • terminated · 2026-04-22 · EMD Serono Research & Development Institute, Inc. · matched by the registry's drug synonyms
    “Overarching portfolio-level review of the company's oncology pipeline resulted in early termination of the study. The study was not terminated due to safety.”
  • withdrawn · 2026-04-08 · Assistance Publique - Hôpitaux de Paris · matched by the registry's drug synonyms
    “Lack of financing”
  • withdrawn · 2026-03-11 · HealthPartners Institute · matched by the registry's drug synonyms
    “The trial was deemed to be unfeasible to commence at this site.”
  • terminated · 2026-03-03 · Novartis Pharmaceuticals · matched by the registry's drug synonyms
    “Business decision and not related to safety concerns”
  • withdrawn · 2026-02-23 · University of Michigan · matched by the registry's drug synonyms
    “Device development took longer than anticipated and the study needed to be redesigned to not include device testing.”
  • terminated · 2026-02-04 · The Guthrie Clinic · matched by the registry's drug synonyms
    “Researcher stopped study due to slow accrual rate”
  • terminated · 2026-01-22 · Delta-Fly Pharma, Inc. · matched by the registry's drug synonyms
    “The data met the protocol-specified criteria for futility of the investigational treatment.”
  • terminated · 2026-01-12 · Sinotau Pharmaceutical Group · matched by the registry's drug synonyms
    “The main objective of this study has been achieved. Following internal discussions, the sponsor has decided to terminate this study early.”
  • terminated · 2025-12-01 · Gustave Roussy, Cancer Campus, Grand Paris · matched by the registry's drug synonyms
    “Abandon of the partner, GSK”
  • terminated · 2025-12-01 · Gustave Roussy, Cancer Campus, Grand Paris · matched by the registry's drug synonyms
    “Bankruptcy of partner: Clovis”
Paediatric incentives and obligations for ADORA2A's drugs

For regadenoson, defibrotide, oxtriphylline, theophylline, pentoxifylline, istradefylline, aminophylline, adenosine, caffeine, apadenoson, binodenoson, tozadenant: 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.

  • EU paediatric investigation plan: yes · EMEA-000410-PIP01-08-M07 (regadenoson, Diagnosis of myocardial perfusion disturbances): PM: decision on the application for modification of an agreed PIP, 18 Jul 2024; EMEA-002540-PIP01-18 (Istradefylline, Treatment of Parkinson's disease): W: decision granting a waiver in all age groups for all conditions or indications, 14 Aug 2019; EMEA-001537-PIP01-13 (Caffeine;Ibuprofen, Treatment of pain): W: decision granting a waiver in all age groups for all conditions or indications, 22 Jan 2014
    Rule: An EMA PIP decision (agreement, modification or waiver) lists the drug as its active substance, exact name. Source: EMA data download (dated snapshot), 2026-11-11
  • EU orphan designation: yes · EU/3/04/211 withdrawn 29 Jul 2004: Prevention of hepatic veno-occlusive disease; EU/3/13/1201 withdrawn 13 Nov 2013: Prevention of graft-versus-host disease; EU/3/03/132 expired 18 Feb 2003: Treatment of primary apnoea of premature newborns; EU/3/04/212 positive 29 Jul 2004: Treatment of hepatic veno-occlusive disease; +1 more
    Rule: An EU orphan designation lists the drug as its active substance (exact name) or belongs to a medicine that does; withdrawn and expired designations are listed with their status. Source: EMA data download (dated snapshot), 2026-11-11
  • Authorised in the EU: yes · Rapiscan: authorised since 6 Sept 2010; Gencebok: authorised since 19 Aug 2020; Peyona (previously Nymusa): authorised since 2 Jul 2009; Defitelio: authorised since 18 Oct 2013, exceptional circumstances; +2 more
    Rule: An EMA medicine record lists the drug as its active substance or INN, exact name; national-only authorisations are not in this file. Source: EMA data download (dated snapshot), 2026-11-11
  • FDA orphan designation: not published · FDA's orphan designation database turns away automated requests, so this app does not read it; search it by hand at the link
    Rule: Would be: an FDA orphan designation names the drug. Source: FDA orphan designations search
  • FDA pediatric oncology approval: no · FDA's table lists no pediatric approval of regadenoson, defibrotide, oxtriphylline, theophylline, pentoxifylline, istradefylline, aminophylline, adenosine, caffeine, apadenoson, binodenoson, tozadenant
    Rule: FDA's Pediatric Oncology Drug Approvals table names the drug. Source: FDA Pediatric Oncology Drug Approvals (content current as of 2026-03-03), 2026-11-12
  • Registered studies open to children: yes · 344 interventional studies of regadenoson, defibrotide, oxtriphylline, theophylline, pentoxifylline, istradefylline, aminophylline, adenosine, caffeine, apadenoson, binodenoson, tozadenant include patients under 18; 61 are recruiting, not yet recruiting or active
    Rule: The registry's age group includes Child (birth to 17 years), which also counts studies that set no minimum age. Source: ClinicalTrials.gov search, 2026-11-12

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 27 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
REGADENOSONSmall moleculeapprovalcardiovascular disorder, COVID-19, sickle cell disease, ischemia reperfusion injury, lung transplantation, type 2 diabetes mellitusOpen Targets · ChEMBL
DEFIBROTIDEUnknownapprovalRecurrent thrombophlebitis, hepatic veno-occlusive disease, diabetic kidney disease, acute chest syndrome, respiratory failure, Kawasaki disease, plasma cell myeloma, acute respiratory distress syndrome, +1 moreOpen Targets · ChEMBL
OXTRIPHYLLINESmall moleculeapprovalCough, Airway obstructionOpen Targets · ChEMBL
THEOPHYLLINEProteinphase 4asthma, chronic bronchitis, chronic obstructive pulmonary disease, Airway obstruction, smoking behavior, nicotine dependence, gastroesophageal reflux disease, B-cell chronic lymphocytic leukemia, +17 moreOpen Targets · ChEMBL
PENTOXIFYLLINESmall moleculephase 4cardiovascular disorder, intermittent vascular claudication, liver failure, cirrhosis of liver, chronic kidney disease, kidney disorder, rapidly progressive glomerulonephritis, Proteinuria, +80 moreOpen Targets · ChEMBL
ISTRADEFYLLINESmall moleculephase 4Parkinson disease, Dyskinesia, restless legs syndrome, spinal cord injury, amyotrophic lateral sclerosis, ApathyOpen Targets · ChEMBL
AMINOPHYLLINEProteinphase 4asthma, Airway obstruction, Headache, B-cell chronic lymphocytic leukemia, acute kidney injury, kidney injury, chronic obstructive pulmonary disease, atrial fibrillation, +1 moreOpen Targets · ChEMBL
ADENOSINESmall moleculephase 4paroxysmal tachycardia, Wolff-Parkinson-White syndrome, cardiovascular disorder, Paroxysmal supraventricular tachycardia, gas gangrene, myocardial infarction, combined immunodeficiency, atrial fibrillation, +15 moreOpen Targets · ChEMBL
CAFFEINE CITRATESmall moleculephase 4Apnea, cerebral palsy, intracranial hemorrhage, bronchopulmonary dysplasia, Patent ductus arteriosus, perinatal asphyxia, Respiratory distress, Bradycardia, +9 moreOpen Targets · ChEMBL
CAFFEINESmall moleculephase 4migraine disorder, Pain, Apnea, Headache, orthostatic hypotension, drug dependence, attention deficit-hyperactivity disorder, peripheral arterial disease, +40 moreOpen Targets · ChEMBL
APADENOSONSmall moleculephase 3coronary artery disorderOpen Targets · ChEMBL
BINODENOSONSmall moleculephase 3hypertensive disorderOpen Targets · ChEMBL
TOZADENANTSmall moleculephase 3Parkinson diseaseOpen Targets · ChEMBL
PRELADENANTSmall moleculephase 3Parkinson diseaseOpen Targets · ChEMBL
UK432097Small moleculephase 2chronic obstructive pulmonary diseaseOpen Targets · ChEMBL
SONEDENOSONSmall moleculephase 2diabetic footOpen Targets · ChEMBL
REGADENOSON ANHYDROUSSmall moleculephase 2sickle cell disease, acute chest syndromeOpen Targets · ChEMBL
VIPADENANTSmall moleculephase 2Parkinson diseaseOpen Targets · ChEMBL
SIPAGLADENANTSmall moleculephase 2Parkinson diseaseOpen Targets · ChEMBL
IMARADENANTSmall moleculephase 2prostate cancer, renal cell carcinoma, non-small cell lung carcinoma, colorectal carcinoma, head and neck carcinomaOpen Targets · ChEMBL
AMP579Small moleculephase 2familial hyperlipidemiaOpen Targets · ChEMBL
ETRUMADENANTSmall moleculephase 2prostate cancer, non-small cell lung carcinoma, rectal cancer, cancer, urothelial carcinoma, dedifferentiated liposarcoma, pancreatic ductal adenocarcinoma, metastatic colorectal cancer, +8 moreOpen Targets · ChEMBL
BVT.115959Small moleculephase 2Pain, neuropathic painOpen Targets · ChEMBL
PBF-509Small moleculephase 1 2non-small cell lung carcinomaOpen Targets · ChEMBL
EVODENOSONSmall moleculephase 1 2arteriosclerosis, open-angle glaucoma, ocular hypertensionOpen Targets · ChEMBL
CIFORADENANTSmall moleculephase 1 2Parkinson disease, attention deficit-hyperactivity disorder, non-small cell lung carcinoma, renal cell adenocarcinoma, renal cell carcinoma, plasma cell myeloma, neoplasmOpen Targets · ChEMBL
PBF-999Small moleculephase 1Huntington diseaseOpen Targets · ChEMBL