Endothelin receptor antagonist

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An endothelin receptor antagonist (ERA) is a drug that blocks endothelin receptors.

Three main kinds of ERAs exist:

Dual ET Receptor Antagonists, which affect both endothelin A (ET_A) and B receptors (ET_B) ^[1]
- aprocitentan, bosentan, macitentan, tezosentan
Selective ET_A Receptor Antagonists, which affect endothelin A receptors
- sitaxentan, ambrisentan, atrasentan, BQ-123, sparsentan, zibotentan, avosentan, edonentan, clazosentan
Selective ET_B 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.

References

v t e Medications used in the management of pulmonary arterial hypertension (B01, C02)
Prostacyclin analogues	Beraprost Epoprostenol Iloprost Selexipag Treprostinil
Endothelin receptor antagonists	Ambrisentan Bosentan Macitentan Sitaxentan
PDE5 inhibitors	Sildenafil Tadalafil
sGC stimulators	Riociguat Vericiguat
Adjunctive therapy	Calcium channel blockers Diuretics Digoxin Oxygen therapy Warfarin

Central

α₂-Adrenergic receptor agonists	Clonidine Guanabenz Guanfacine Guanoxabenz Methyldopa^# Tiamenidine^‡
Adrenergic release inhibitors	Bethanidine Bretylium Debrisoquine Guanadrel Guanazodine Guancydine Guanethidine Guanoclor Guanoxan
Imidazoline receptor agonists	Moxonidine Rilmenidine Tolonidine
Ganglion-blocking/nicotinic antagonists	Hexamethonium^‡ Mecamylamine Pentolinium Trimethaphan

Peripheral

Indirect

Monoamine oxidase inhibitors	Pargyline^‡
VMAT inhibitors	Bietaserpine Deserpidine Methoserpidine Reserpine Syrosingopine
Tyrosine hydroxylase inhibitors	Metirosine

Direct

α₁-Adrenergic receptor blockers	Doxazosin Ketanserin Indoramin Prazosin Trimazosin Urapidil
Non-selective α-adrenergic receptor blockers	Phentolamine

Serotonin receptor antagonists	Ketanserin Lidanserin
Endothelin receptor antagonists (for PHTooltip Pulmonary hypertension)	dual (Aprocitentan, Bosentan, Macitentan (+tadalafil), Riociguat) selective (Ambrisentan (+tadalafil), Sitaxentan, Sotatercept)

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