Bosentan is a dual endothelin receptor antagonist used to treat pulmonary arterial hypertension. A medication used to treat certain heart conditions.
- Mechanism
- Curator reviewed
Endothelin-1 (ET-1) is a neurohormone, the effects of which are mediated by binding to ETA and ETB receptors in the endothelium and vascular smooth muscle. It displays a slightly higher affinity towards ETA receptors than ETB receptors. ET-1 concentrations are elevated in plasma and lung tissue of patients with pulmonary arterial hypertension, suggesting a pathogenic role for ET-1 in this disease. Bosentan is a specific and competitive antagonist at endothelin receptor types ETA and ETB.
- Primary indication
- Used in the treatment of pulmonary arterial hypertension (PAH), to improve exercise ability and to decrease the rate of clinical worsening (in patients with WHO Class III or IV symptoms).Curator reviewed · 5 structured indications
- Formula / weight
- C27H29N5O6S · 551.614 g/mol (avg)
- First approval
- Canada, 2012 · United States, 2001 · European Union, 2016
- Brand names
Resolves to
GJPICJJJRGTNOD-UHFFFAOYSA-NSMILESCOC1=CC=CC=C1OC1=C(NS(=O)(=O)C2=CC=C(C=C2)C(C)(C)C)N=C(N=C1OCCO)C1=NC=CC=N1What you can answer from here — as of September 23, 2026
Which drugs share a target with Bosentan, and which of those have an active Phase 3 trial?
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