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Darusentan is a selective endothelin ETA receptor antagonist. It is being evaluated as a treatment for congestive heart failure and hypertension.
- Mechanism
- Curator reviewed
The mode of action by which the endothelin receptor antagonists cause a decrease of the BP is not yet totally elucidated; however, peripheral vasodilatation due to blockade of the vasoconstrictor effects of endothelin is the most likely explanation. A reduction of cardiac contractility is considered unlikely. Several studies have been published that investigated the effects of either selective or nonselective endothelin receptor blockade in patients with heart failure. In these studies, application of endothelin antagonists, while decreasing both systemic and pulmonary BP increased cardiac index and did not alter cardiac contractility or heart rate.
- Primary indication
- For the treatment of congestive heart failure and hypertension.Curator reviewed
- Formula / weight
- C22H22N2O6 · 410.4199 g/mol (avg)
- Code names
- LU-135252
Resolves to
FEJVSJIALLTFRP-LJQANCHMSA-NSMILESCOC1=CC(OC)=NC(O[C@H](C(O)=O)C(OC)(C2=CC=CC=C2)C2=CC=CC=C2)=N1What you can answer from here — as of June 15, 2026
Which drugs share a target with Darusentan, and which of those have an active Phase 3 trial?