Table 4.
Therapeutic drugs, imaging agents, and clinical candidates that act through adenosine receptors.
| Compound | Selectivity | Company | Indication or use (phase)a |
|---|---|---|---|
| Agonists | |||
| Adenosine (1) (Adenocard, Adenoscan) | A1, A2A | Astellas | Paroxysmal supraventricular tachycardia (approved), myocardial perfusion imaging (approved), other uses in testing |
| AMP579 (12) | A1, A2 | Aventis | Myocardial infarction (discontinued) |
| Apadenoson (16, Stedivaze, BMS068645, ATL146e) | A2A | Clinical Data | Myocardial perfusion imaging (III) |
| ATL-1222 | A2A | Clinical Data | Acute inflammatory conditions (preclinical) |
| ATL-313 (17) | A2A | Clinical Data | Ophthalmic disease (preclinical) |
| BAY 60-6583 (28) | A2B | Bayer | Atherosclerosis (preclinical) |
| Binodenoson (23, WRC-0470, MRE-0470) | A2A | Aderis, King | Myocardial perfusion imaging (III) |
| BVT.115959 | A2A | Biovitrum | Diabetic neuropathic pain (II) |
| Capadenoson (6, BAY68-4986, nonnucleoside) | A1 | Bayer Schering | Atrial fibrillation, chronic treatment (II) |
| Cl-IB-MECA (30, CF102) | A3 | Can-Fite | Liver cancer (I–II) |
| CP608,039 (36) | A3 | Pfizer | Cardiac ischemia (discontinued) |
| GS 9667 (11, CVT-3619) | A1 | Gilead | Hypertriglyceridemia associated with diabetes (I) |
| GR79236 (9) | A1 | GlaxoSmithKline | Pain, hyperlipidemia (I, discontinued) |
| GW493838 (7) | A1 | GlaxoSmithKline | Peripheral neuropathic pain (II, discontinued) |
| IB-MECA (29, CF101) | A1 | Can-Fite | Rheumatoid arthritis, psoriasis, dry eye, and other autoimmune inflammatory diseases (II), glaucoma (II) |
| MRS3558 (34, CF502) | A3 | Can-Fite | Autoimmune inflammatory diseases (preclinical) |
| NNC-21-0136 (14) | A1 | Novo Nordisk | Stroke, neurodegeneration (discontinued) |
| INO 8875 (PJ-875) | A1 | Inotek Pharmaceuticals | Glaucoma (II); atrial fibrillation (discontinued) |
| Regadenoson (19, Lexiscan, CV-3146) | A2A | Gilead and Astellas | Myocardial perfusion imaging (approved) |
| RPR749 | A1 | Aventis | Hyperlipidemia (I) |
| SDZ WAG 94 (13) | A1 | Sandoz/Novartis | Diabetes |
| Selodenoson (8) | A1 | Aderis | Atrial fibrillation (II) |
| Sonedenoson (22, MRE-0094) | A2A | King | Diabetic foot ulcers, wound healing (II) |
| Tecadenoson (10, CVT-510) | A1 | Gilead | Paroxysmal supraventricular tachycardia (III) |
| UK 432097 (18) | A2A | Pfizer | COPD (II) |
| Antagonists | |||
| ATL 844 | A2B | Clinical Data and Novartis | Asthma and/or diabetes |
| Naxifylline (43, BG-9719) | A1 | Biogen-Idec | Heart failure (renal function) (discontinued) |
| Caffeine (38) | McMaster University | Apnea | |
| CPFPX (88) | A1 | Research Center Jülich, Germany | PET imaging (18F) |
| FK-453 (45) | A1 | Astellas | Acute renal failure |
| GS 6201 (67, CVT-6883) | A2B | Gilead | Asthma (I) |
| Istradefylline (49, KW6002) | A2A | Kyowa-Hakko Kogyo | Parkinson’s disease (III, discontinued) |
| KF26777 (80) | A3 | Kyowa-Hakko Kogyo | Asthma (preclinical) |
| LAS38096 (69) | A2B | Almirall | Anti-inflammatory (preclinical) |
| LAS101057 [192] | A2B | Almirall | Antiasthmatic (I) |
| L-97-1 (48) | A1 | Endacea | Sepsis (preclinical) |
| MRE2029-F20 (66) | A2B | King | Anti-inflammatory (preclinical) |
| OSIP339391 (74) | A2B | OSI | Asthma (preclinical) |
| OT-7999 (87) | A3 | Otsuka | Glaucoma (preclinical) |
| Preladenant (58, SCH-420814) | A2A | Schering-Plough | Parkinson’s disease (III) |
| SCH-442416 (55) | A2A | Schering-Plough | PET imaging (11C) |
| QAF805 (75) | A2B, A3 | Novartis | Asthma (I) |
| Rolofylline (41, KW3902, NAX) | A1 | NovaCardia and Merck | Heart failure (renal function) (discontinued) |
| SLV320 (46) | A1 | Solvay | Heart failure (renal function) |
| ST-1535 (59) | A2A | Sigma-Tau | Parkinson’s disease (I) |
| SYN-115 (60) | A2A | Synosia Therapeutics/UCB (after Synosia Therapeutics) | Parkinson’s disease (II), addiction |
| Theophylline/aminophylline (39) | A1 | King Faisal University | Recovery after anaesthesia |
| Toponafylline (42, BG-9928) | A1 | Biogen-Idec | Heart failure (renal function) (IIb) |
| Vipadenant (54, BIIB014, V2006) | A2A | Vernalis and Biogen-Idec | Parkinson’s disease (II) |
a
Many of the clinical trials indicated are no longer current.