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Medical > Therapy > Specific treatments

Endothelin receptor antagonists
Sitaxsentan

 

Selective antagonism of ETA receptors may be more beneficial than antagonism of both ETA and ETB receptors for the treatment of PAH by blocking only the vasoconstrictor effects of ETA receptors, but not the vasodilator and clearance function of ETB receptors. Sitaxsentan is about 6500 times more selective for the ETA compared with the ETB receptor. It has a high oral bioavailability and a long half-life time of 5-7 hours. The STRIDE-1 trial included 118 patients with different forms of PAH comparing sitaxsentan at a daily dose of 100mg in 55 patients, 300 mg in 63 patients and placebo in 60 patients (Barst et al. 2004). Both doses significantly increased peak VO2, 6-minute walking distance, functional class and hemodynamics. The incidence of elevated transaminases was 0 % and 10% for the 100-mg and the 300-mg regimen, respectively.

References

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