An endothelin receptor antagonist (ERA) is a drug that blocks endothelin receptors.
Classes
Three main kinds of ERAs exist:
- Dual ET Receptor Antagonists, which affect both endothelin A (ET<sub>A</sub>) and B receptors (ET<sub>B</sub>) CPU0213 [821780-32-9] is an example of a dual receptor endothelin receptor antagonist.
- aprocitentan, bosentan, macitentan, tezosentan, Feloprentan (LU-302872 the HCl salt is called LU-420627) [204267-33-4],
- Selective ET<sub>A</sub> Receptor Antagonists, which affect endothelin A receptors
- sitaxentan, ambrisentan, atrasentan, BQ-123, sparsentan, zibotentan, avosentan, edonentan, clazosentan, Fandosentan
- Selective ET<sub>B</sub> Receptor Antagonists, which affect endothelin B receptors
- BQ-788 and A192621 are used in research but have not yet reached clinical trial stage
Macitentan, ambrisentan and bosentan are mainly used for the treatment of pulmonary arterial hypertension, while atrasentan is an experimental anti-cancer drug.
Further (unsorted) examples include: BMS-182874, BMS-193884, BQ-485 [141594-26-5] CI 1020 (PD 156707) [162256-50-0] Enrasentan [167256-08-8], J 104132 [198279-45-7], L-754142 [173450-67-4], PABSA [188710-94-3], PD-155080, SB 209670 [157659-79-5], ZD1611 [186497-38-1]
References