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Experimental study of a Phase III SERAPHIN, Macitentan(http://www.medchemexpress.com/product/Macitentan.html) can significantly reduce pulmonary arterial hypertension (PAH) patient morbidity and mortality. Dr. Lewis Rubin, University of California, San Diego, reported at the annual meeting of the American College of Physicians in 2012, the latest summary of its findings.
Dr. Rubin said, bosentan An Lisheng Tanzania both endothelial receptor antagonists (ERAs) for the treatment of PAH, and randomized clinical trials have proven its short-term efficacy. Approved by the U.S. Food and Drug Administration in the short-term follow-up test on the basis of athletic ability as the primary outcome measure, the oral drug for PAH treatment. Using Macitentan the treatment of patients with PAH analysis disease morbidity and mortality outcome study. Dr. Rubin pointed out that the end point of the event, "including the clinically relevant events reflect the real progress of the disease.
"Endothelin have both paracrine and autocrine activity Thus, endothelin receptor antagonists have greater tissue penetration ability, and can be more widely blocks endothelin, and can be transformed into a greater efficacy. Macitentan is a new dual endothelin receptor antagonist, has confirmed that the drug may enhance tissue penetration of bile salts, may reduce the incidence of adverse events hepatic dysfunction, "said Dr. Rubin.
Study, symptomatic PAH patients were randomized to the daily doses Macitentan 3 mg group Macitentan 10 mg group and the placebo group. The main findings from the start of treatment to the first morbidity or mortality events. The "event" is defined as all causes of death, atrial septal ostomy, lung transplantation, start intravenous or subcutaneous injection of prostaglandin or PAH deterioration. Compared with the placebo group, 3 mg group mortality and morbidity risks reduce%, 10 mg was reduced by 45%. The Macitentan also greatly reduce the risk of secondary outcomes, including functional classification of the World Health Organization, PAH time of death, all-cause hospitalization due to PAH and death. In addition, compared with the placebo group, Macitentan increase the 6-minute walk distance.
Dr. Rubin pointed endothelin receptor antagonists have anticipated that there will be adverse reactions, such as the occurrence of dose-related effect of hemoglobin. Application maximum dose of Macitentan of 4.3% in patients with significant symptoms of anemia. The placebo group with Macitentan of group elevated aminotransferases rate similar to the incidence of peripheral edema treatment effect Macitentan 10 mg group to accept or not to accept the treatment of PAH background of patients.
Not involved in the study, the University of Tokyo, Japan Atsushi Yao, MD, said the data obtained support PAH patients treated with the ERA. Medscape Medical News, he said that non-selective ERA Macitentan is a good tissue penetration, no serious adverse reaction, therefore, the results look very attractive. "
According to Dr. Yao explore how Macitentan with other treatment measures joint applications and determine Macitentan for the PAH specific effect of each type is very important, such as PAH related to systemic sclerosis and pulmonary hypertension. Bosentan sometimes improve the level of liver enzymes, its dose titration can not; However, to obtain the best Macitentan efficacy is promising, "he added.
Macitentan
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