Ligand id: 3950

Name: sitaxsentan

Structure and Physico-chemical Properties

2D Structure
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Calculated Physico-chemical Properties
Hydrogen bond acceptors 4
Hydrogen bond donors 1
Rotatable bonds 6
Topological polar surface area 144.35
Molecular weight 454.01
XLogP 3.04
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Use of sitaxentan was indicated for the treatment of pulmonary hypertension, connective tissue diseases, hypertension and congestive heart failure. However, use of sitaxentan has been discontinued in most countries due to concerns about liver toxicity.
Mechanism Of Action and Pharmacodynamic Effects
Competitive antagonist of endothelin-1 at endothelin-A and -B receptors. The binding of endothelin-1 at these receptors causes pulmonary vaoconstriction therefore their antagonism by sitaxentan decreases pulmonary vascular resistance.