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
Drugs & Drug Targets
DrugTargetType
BosentanEndothelin B receptortarget
BosentanEndothelin-1 receptortarget
BosentanCytochrome P450 3A4enzyme
BosentanCytochrome P450 2C9enzyme
BosentanBile salt export pumptransporter
MacitentanCytochrome P450 3A4enzyme
MacitentanCytochrome P450 2C19enzyme
MacitentanEndothelin-1 receptortarget
MacitentanEndothelin B receptortarget
MacitentanSerum albumincarrier
MacitentanCytochrome P450 2C9enzyme
MacitentanCytochrome P450 2C8enzyme
Macitentanalpha1-acid glycoproteincarrier
DarusentanEndothelin-1 receptortarget
Actelion-1Endothelin-1 receptortarget
TBC-3711Endothelin-1target
AtrasentanEndothelin-1 receptortarget
SitaxentanCytochrome P450 2C19enzyme
SitaxentanCytochrome P450 2C9enzyme
SitaxentanCytochrome P450 3A4enzyme
SitaxentanEndothelin-1 receptortarget
SitaxentanEndothelin B receptortarget
EnrasentanEndothelin-1 receptortarget
EnrasentanEndothelin B receptortarget
AmbrisentanEndothelin B receptortarget
AmbrisentanEndothelin-1 receptortarget
AmbrisentanCytochrome P450 2C19enzyme
AmbrisentanCytochrome P450 3A4enzyme
AmbrisentanUDP-glucuronosyltransferase 1-9enzyme
AmbrisentanUDP-glucuronosyltransferase 1-3enzyme
AmbrisentanUDP-glucuronosyltransferase 2B7enzyme
AmbrisentanP-glycoprotein 1transporter
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
SparsentanP-glycoprotein 1transporter
SparsentanATP-binding cassette sub-family G member 2transporter
SparsentanSolute carrier organic anion transporter family member 1B3transporter
SparsentanSolute carrier family 22 member 8transporter