FDA Approves Macitentan for Pulmonary Arterial Hypertension


Macitentan 441798-33-0 FDA ApprovalOn October 19, 2013 the FDA approved Macitentan for the treatment of pulmonary arterial hypertension, also known as PAH. As the first oral drug approved as a potential reduction for patient hospitalizations, Macitentan is also being touted to delay disease progression in patients with PAH. Actelion markets the brand name of Macitentan, coined Opsumit, is an inventive product as it is a dual endothelin receptor antagonist. The clinical trial dubbed SERAPHIN was a definite catalyst for the FDA approval, which was an extensive, lengthy and randomized study that encompassed 742 patients with PAH. The SERAPHIN study {Study with an Endothelin Receptor Antagonist in Pulmonary arterial Hypertension to Improve clinical outcome} followed participants who received either 3 milligrams of Macitentan, 10 milligrams of Macitentan or a placebo pill. The doses were administered once daily and patients experienced minimal adverse effects. Sore throat, nasopharyngitis, headache and anemia occurred as side effects in a small number of patients. Macitentan is not intended for use by women who are pregnant or think they may be pregnant, as this medication carries a boxed warning for this patient population.

The 10 milligram dosage of Macitentan was approved by the FDA and was revealed to be successful in multiple studies. Overall results elicited a sizable reduction in the risk of death among patients with pulmonary arterial hypertension, as well as a reduction in cases of lung transplantation, atrial septostomy and the initiation of subcutaneous or intravenous prostanoids. The patients who received the 10 milligram daily doses of Macitentan as compared to the patients who received a placebo had a 45 percent reduction in the worsening of their PAH symptoms. Additionally, when comparing the placebo pill to the 10 milligram dosage of Macitentan there was a diminishment of hospitalization rates, with only 19 percent of patients dosed with Macitentan needing hospital care. In comparison, roughly 32 percent of patients who were given a placebo ended up needing hospitalization. The patients dosed with Macitentan 3 milligrams did display modest reductions in the study endpoints; however it was not approved by the FDA at this time.

Pulmonary Arterial Hypertension is a serious and debilitating condition which presents as ceaseless high blood pressure in the pulmonary artery. With the normal blood pressure  in the pulmonary artery of a healthy adult being about 14 mmHg  at rest, patients with PAH often experience a resting pressure if 25 mmHg or greater. Certain cases of PAH are familial, while other cases are due to preexisting conditions like heart disease or lung disease.

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