Tracleer™ (bosentan): Mode of Action

Tracleer (bosentan) is a dual endothelin receptor antagonist (ERA) with affinity for both endothelin receptors ET_A and ET_B. Tracleer competes with the binding of endothelin (ET-1) and other ET peptides to both receptors, with a slightly higher affinity for ET_A receptors than for ET_B receptors. Tracleer has demonstrated an ability to block the detrimental effects of endothelin mediated by ET_A and ET_B, such as vasoconstriction, fibrosis, inflammation and neurohormonal activation.

In animal models of pulmonary hypertension, chronic oral administration of Tracleer reduced pulmonary vascular resistance and reversed pulmonary vascular and right ventricular hypertrophy. In an animal model of pulmonary fibrosis, Tracleer reduced collagen deposition in the lungs.

In pre-clinical models Tracleer demonstrated an ability to:

• Decrease inflammatory reactions

• Prevent fibrosis development

• Decrease permeability of the pulmonary vessels

• Reverse existing pulmonary arterial hypertension

• Reverse pulmonary vascular remodeling and cardiac hypertrophy in models of pulmonary hypertension.

See how Tracleer works: