Also known as: Sitaxentan sodium

Active ingredient description

Sitaxentan is a potent (Ki 0.43 nM) and highly selective ETA antagonist (approximately 6,500-fold more selective for ETA as compared to ETB). Endothelin-1 (ET-1) is a potent vascular paracrine and autocrine peptide in the lung, and can also promote fibrosis, cell proliferation, cardiac hypertrophy, and remodelling and is pro-inflammatory. ET-1 actions are mediated through endothelin A (ETA) and endothelin B receptors (ETB). ET-1 concentrations are elevated in plasma and lung tissue of patients with pulmonary arterial hypertension (PAH), as well as other cardiovascular disorders and connective tissue diseases.

Medicine classification

This medicinal substance has been classified in the anatomical therapeutic chemical (ATC) classification according to its main therapeutic use as follows:

ATC code
Group title
C Cardiovascular system → C02 Antihypertensives → C02K Other antihypertensives → C02KX Antihypertensives for pulmonary arterial hypertension
Discover more medicines within C02KX03

Product monographs

Competent medicine agencies globally have authorized commercialization of this active ingredient according to these medication package inserts (MPIs):

Summary of Product Characteristics (SPC)

Structural formula

Graphic representation of the active ingredient's molecular structure

Chemical formula: C₁₈H₁₅ClN₂O₆S₂
Molecular mass: 454.905 g/mol

External identifiers

CAS Substance: 184036-34-8
DrugBank Drug: DB06268
KEGG Drug: D07171
PubChem Compound: 216235
SNOMED-CT Concept: 428709002
Sitaxentan (substance)
UNII Identifier: J9QH779MEM