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References in periodicals archive ?
Opsumit, an orally available endothelin receptor antagonist, resulted from a tailored drug discovery process in Actelion's laboratories.
Antivascular therapy for multidrug-resistant ovarian tumors by macitentan, a dual endothelin receptor antagonist. Transl Oncol.
(5-8) Bosentan is a dual endothelin receptor antagonist, which binds to ET-A and B receptors, thereby inhibiting endothelin-1.
Pittrow, "Role of endothelin and endothelin receptor antagonists in renal disease," European Journal of Clinical Investigation, vol.
The results of the observational studies and randomized controlled trials revealed that endothelin receptor antagonists (ERAs) compared with conventional medication may improve exercise tolerance and functional status, quality of life, right ventricular function and pulmonary hemodynamics and may lengthen the time to clinical worsening and survival in patients with PAH.
The multicenter, double-blinded trial randomized 67 adults with PAH to 12 weeks of treatment with the endothelin receptor antagonist alone or in combination with the inhaled prostacyclin derivative.
In two studies that were the basis of approval, the most common side effects associated with the drug were peripheral edema (a known class effect of endothelin receptor antagonists), which was usually mild to moderate; nasal congestion; sinusitis; and flushing, according to an Food and Drug Administration statement announcing the approval.
"Off-label anticoagulants, diuretics and calcium-channel blockers are often used to treat PAH, with more targeted therapies (such as endothelin receptor antagonists) also used extensively to treat this debilitating disease," says Datamonitor.
Based on the properties of the compound and the results of our Phase 2 trial, we believe ambrisentan's efficacy and safety profile may position it as the best-in-class among endothelin receptor antagonists. We are excited by the progress of our ambrisentan clinical program and look forward to sharing the results of the ARIES-2 trial later this year."
* Therapeutic modalities now include parenteral prostanoids, oral endothelin receptor antagonists, PDE5 inhibitors, and lung transplantation (SOR: A; for PDE5 inhibitors, SOR: B)
Compared with patients on placebo, those on Letairis had significant improvements in the primary end point, the 6-minute walk distance at 12 weeks, and had a significant delay in the time to clinical worsening of PAH Endothelin receptor antagonists block the receptor for endothelin, which is overproduced in the lungs of patients with pulmonary hypertension, thus stimulating the growth and proliferation of the blood vessels in the pulmonary endothelium, Dr.
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