alexa A Comprehensive Drug Review on Macitentan: A Preeminent Inclusion to Pulmonary Arterial Hypertension Therapy

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Research Article

A Comprehensive Drug Review on Macitentan: A Preeminent Inclusion to Pulmonary Arterial Hypertension Therapy

Dherya Bahl1, Rakesh K. Jaiswal1, Manzar Ahsan1, Farha Bano1, Monika Anand1, Danish Khan1 Asif Husain1*, Aftab Ahmad2*, Fahad A. Al-Abbasi3, Shah Alam Khan4

1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), New Delhi-110062, India

2Health Information Technology Department, Jeddah Community College, King Abdulaziz University, P.O. Box-80283, Jeddah-21589, Kingdom of Saudi Arabia

3Department of Biochemistry, Faculty of Sciences, King Abdulaziz University, Jeddah 21589, Kingdom of Saudi Arabia

4Department of Pharmacy, Oman Medical College, Muscat, Sultanate of Oman

*Corresponding Author:
Dr. Asif Husain
Sr. Asst. Professor, Department of Pharmaceutical Chemistry
Faculty of Pharmacy, Hamdard University, New Delhi-110 062, India
Tel: +91-11-26059681, 26059688, Ext. 5647; Mobile- +91-989-1116086
E-mails: [email protected], [email protected]

Dr. Aftab Ahmad
Health Information Technology Department, Jeddah Community College
King Abdulaziz University, P.O. Box-80283, Jeddah-21589, Kingdom of Saudi Arabia
Tel: +966-02-2870026, Extn.102; Mobile: +966–507243943
Fax: +966-02-2870024
E-mails: [email protected], [email protected]

Received date: 02 April 2015; Accepted date: 11 June 2015; Published date: 18 June 2015



Macitentan is a radically novice oral orphan drug which was approved by FDA in Oct 2013 (under trade name Opsumit®). It belongs to the class of the endothelin receptor antagonist (ETRA) and is indicated for the treatment of pulmonary arterial hypertension (PAH). PAH is a chronic disorder of raising blood pressure in the artery between the aisle of heart and lung. Till the date, the disease remains incurable and possesses a poor prognosis. A ray of hope in this direction is shown by Macitentan, which has been proved beneficial in decreasing disease progression symptoms and reducing hospitalization. Phase III SERAPHIN trials clearly indicate that it improves morbidity, mortality and 6MWD data compared with other drugs of the same class. Furthermore, its use is seemingly increasing for the treatment of other cardiovascular disorders related to ET system. However, the pharmacokinetics dose adjustments of Macitentan in patients with renal or hepatic impairment are extraneous. Drug–drug interactions are occult, and one circulating pharmacologically active metabolite (ACT-132577) is omnipresent. The safety profile of Macitentan is superior to other drugs of same ETRA’s class with prolonged receptor binding properties, greater tissue penetration, hepatic safety, edema/fluid retention and easy dosing, but it is similar when the decrease in hemoglobin concentration is taken into account. Macitentan attributes, hence, are appended and revolutionary important in the therapeutic long-term treatment and a better alternative remedy for PAH. The present review thus delineates the complete drug profile of Macitentan from the data of studies carried out till date and alleges it as a sanguine future for an overall improved CVS healthcare contributor.


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