Endothelin Receptor Antagonists

Name
Endothelin Receptor Antagonists
Accession Number
DBCAT000972
Description

Compounds and drugs that bind to and inhibit or block the activation of ENDOTHELIN RECEPTORS.

Drugs
DrugDrug Description
BosentanA dual endothelin receptor antagonist used to treat pulmonary arterial hypertension.
MacitentanAn endothelin receptor antagonist used to manage pulmonary arterial hypertension to delay disease progression.
DarusentanFor the treatment of congestive heart failure and hypertension.
Actelion-1Investigated for use/treatment in cardiovascular disorders, hypertension, and pulmonary hypertension.
TBC-3711Investigated for use/treatment in congestive heart failure, hypertension, and pulmonary hypertension.
AtrasentanInvestigated for use/treatment in prostate cancer and cancer/tumors (unspecified).
SitaxentanInvestigated for use/treatment in pulmonary hypertension, connective tissue diseases, hypertension, and congestive heart failure.
EnrasentanInvestigated for use/treatment in congestive heart failure, chronic obstructive pulmonary disease (COPD), and benign prostatic hyperplasia.
BQ-123BQ-123 has been investigated for the basic science and treatment of Coronary Artery Disease, Aorto-coronary Bypass Grafting, and ST-Elevation Myocardial Infarction.
AmbrisentanA selective type A endothelin receptor antagonist used to treat primary pulmonary arterial hypertension and pulmonary arterial hypertension based on diagnostic classifications.
SparsentanAn endothelin and angiotensin II receptor antagonist indicated to reduce proteinuria in adults with primary immunoglobulin A nephropathy at risk of rapid disease progression.
BQ-788Not Annotated
AprocitentanAn endothelin receptor antagonist used for the treatment of uncontrolled hypertension in patients inadequately controlled on other treatments.
Drugs & Drug Targets
DrugTargetType
BosentanEndothelin receptor type Btarget
BosentanEndothelin-1 receptortarget
BosentanCytochrome P450 3A4enzyme
BosentanCytochrome P450 2C9enzyme
BosentanBile salt export pumptransporter
MacitentanCytochrome P450 3A4enzyme
MacitentanCytochrome P450 2C19enzyme
MacitentanEndothelin-1 receptortarget
MacitentanEndothelin receptor type Btarget
MacitentanAlbumincarrier
MacitentanCytochrome P450 2C9enzyme
MacitentanCytochrome P450 2C8enzyme
Macitentanalpha1-acid glycoproteincarrier
DarusentanEndothelin-1 receptortarget
Actelion-1Endothelin-1 receptortarget
TBC-3711Endothelin-1target
TBC-3711Endothelin-1 receptortarget
AtrasentanEndothelin-1 receptortarget
SitaxentanCytochrome P450 2C19enzyme
SitaxentanCytochrome P450 2C9enzyme
SitaxentanCytochrome P450 3A4enzyme
SitaxentanEndothelin-1 receptortarget
SitaxentanEndothelin receptor type Btarget
EnrasentanEndothelin-1 receptortarget
EnrasentanEndothelin receptor type Btarget
BQ-123Endothelin-1 receptortarget
AmbrisentanEndothelin receptor type Btarget
AmbrisentanEndothelin-1 receptortarget
AmbrisentanCytochrome P450 2C19enzyme
AmbrisentanCytochrome P450 3A4enzyme
AmbrisentanUDP-glucuronosyltransferase 1A9enzyme
AmbrisentanUDP-glucuronosyltransferase 1A3enzyme
AmbrisentanUDP-glucuronosyltransferase 2B7enzyme
AmbrisentanATP-dependent translocase ABCB1transporter
AmbrisentanSolute carrier organic anion transporter family member 1B1transporter
AmbrisentanSolute carrier organic anion transporter family member 1B3transporter
AmbrisentanCytochrome P450 3A5enzyme
SparsentanEndothelin-1 receptortarget
SparsentanType-2 angiotensin II receptortarget
SparsentanCytochrome P450 3A4enzyme
SparsentanCytochrome P450 2B6enzyme
SparsentanCytochrome P450 2C9enzyme
SparsentanCytochrome P450 2C19enzyme
SparsentanATP-dependent translocase ABCB1transporter
SparsentanBroad substrate specificity ATP-binding cassette transporter ABCG2transporter
SparsentanSolute carrier organic anion transporter family member 1B3transporter
SparsentanOrganic anion transporter 3transporter
SparsentanType-1 angiotensin II receptortarget
BQ-788Endothelin receptor type Btarget
AprocitentanEndothelin-1 receptortarget
AprocitentanEndothelin receptor type Btarget
AprocitentanUDP-glucuronosyltransferase 1A1enzyme
AprocitentanUDP-glucuronosyltransferase 2B7enzyme
AprocitentanAlbumincarrier
AprocitentanCytochrome P450 3A4enzyme
AprocitentanCytochrome P450 2C8enzyme
AprocitentanCytochrome P450 2C9enzyme
AprocitentanCytochrome P450 2C18enzyme
AprocitentanCytochrome P450 2C19enzyme
AprocitentanATP-dependent translocase ABCB1transporter
AprocitentanBroad substrate specificity ATP-binding cassette transporter ABCG2transporter
AprocitentanBile salt export pumptransporter
AprocitentanHepatic sodium/bile acid cotransportertransporter