TABLE 5

Clinical trials of ET antagonists

CompoundClassCompanyConditions Studied
AmbrisentanSelective ETAGilead SciencesPulmonary arterial hypertension (licensed in Europe & USA)
LU208075Scleroderma
BSF208075Pulmonary fibrosis
Atrasentan ABT-627/Selective ETAAbbottProstate cancer
A147627/Diabetic nephropathy
A127722Ischemic heart disease
AvosentanSelective ETASpeedelDiabetic nephropathy
SPP301
Bosentan RO470203Mixed ETA/BActelionPulmonary arterial hypertension (licensed in Europe & USA)
Scleroderma
Hypertension
Chronic heart failure
Melanoma
ClazosentanSelective ETAActelionSubarachnoid hemorrhage
AXV034343
VML588
Ro611790
DarusentanSelective ETAGilead SciencesHypertension
LU125252Chronic heart failure
BSF135252
EdonentanSelective ETABristol-Myers SquibbChronic heart failure
BMS207940
EnrasentanMixed ETA/BGlaxoSmithKlineChronic heart failure
SB217242
MacitentanMixed ETA/BActelionPulmonary arterial hypertension (licensed in Europe & USA)
ACT-064992Pulmonary fibrosis
SitaxsentanSelective ETA Selective ETAEncysive (acquired by Pfizer)Pulmonary arterial hypertension Chronic heart failure
TBC11251RetrophinChronic kidney disease
Sparsentan*Hypertension
RE021Focal & segmental glomerulosclerosis
TezosentanMixed ETA/B Selective ETAActelion AstraZenecaChronic heart failure
Ro 61-0612Acute coronary syndrome
ZibotentanHepatorenal syndrome
ZD4054Prostate cancer
Ovarian cancer

  • ↵* Dual ETA and angiotensin receptor antagonist (Murugesan et al., 2005)