TABLE 5.
Clinical trials of ET antagonists
| Compound | Class | Company | Conditions Studied |
|---|---|---|---|
| Ambrisentan | Selective ETA | Gilead Sciences | Pulmonary arterial hypertension (licensed in Europe & USA) |
| LU208075 | Scleroderma | ||
| BSF208075 | Pulmonary fibrosis | ||
| Atrasentan ABT-627/ | Selective ETA | Abbott | Prostate cancer |
| A147627/ | Diabetic nephropathy | ||
| A127722 | Ischemic heart disease | ||
| Avosentan | Selective ETA | Speedel | Diabetic nephropathy |
| SPP301 | |||
| Bosentan RO470203 | Mixed ETA/B | Actelion | Pulmonary arterial hypertension (licensed in Europe & USA) |
| Scleroderma | |||
| Hypertension | |||
| Chronic heart failure | |||
| Melanoma | |||
| Clazosentan | Selective ETA | Actelion | Subarachnoid hemorrhage |
| AXV034343 | |||
| VML588 | |||
| Ro611790 | |||
| Darusentan | Selective ETA | Gilead Sciences | Hypertension |
| LU125252 | Chronic heart failure | ||
| BSF135252 | |||
| Edonentan | Selective ETA | Bristol-Myers Squibb | Chronic heart failure |
| BMS207940 | |||
| Enrasentan | Mixed ETA/B | GlaxoSmithKline | Chronic heart failure |
| SB217242 | |||
| Macitentan | Mixed ETA/B | Actelion | Pulmonary arterial hypertension (licensed in Europe & USA) |
| ACT-064992 | Pulmonary fibrosis | ||
| Sitaxsentan | Selective ETA Selective ETA | Encysive (acquired by Pfizer) | Pulmonary arterial hypertension Chronic heart failure |
| TBC11251 | Retrophin | Chronic kidney disease | |
| Sparsentan* | Hypertension | ||
| RE021 | Focal & segmental glomerulosclerosis | ||
| Tezosentan | Mixed ETA/B Selective ETA | Actelion AstraZeneca | Chronic heart failure |
| Ro 61-0612 | Acute coronary syndrome | ||
| Zibotentan | Hepatorenal syndrome | ||
| ZD4054 | Prostate cancer | ||
| Ovarian cancer |
*
Dual ETA and angiotensin receptor antagonist (Murugesan et al., 2005)