Macitentan: An important addition to the treatment of pulmonary arterial hypertension
Anjan Khadka1★, Dick B Singh Brashier1, Anantharamu Tejus1, Ashok Kumar Sharma1★ Corresponding author
- 1Department of Pharmacology, Armed Forces Medical College (AFMC), Pune, Maharashtra, India Molecules of the Millennium.
CORRESPONDENCE
Anjan Khadka
Department of Pharmacology, Armed Forces Medical College (AFMC), Pune, Maharashtra, India Molecules of the Millennium.
Received: 30-05-2014; Revised: 08-08-2014; Accepted: 31-10-2014.
Volume 6, Issue 1 · pp. 53–57 · PUBLISHED 2015 · DOI: 10.4103/0976-500X.149151
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ABSTRACT
Macitentan is an orphan drug for the treatment of pulmonary arterial hypertension (PAH). Endothelin‑1 (ET‑1) plays a critical role of pathophysiology of PAH. Macitentan, a new dual endothelin receptor antagonist, has reportedly improved prognosis of PAH patients by delaying the progression of disease. It prevents the binding of ET‑1 to both endothelin A (ETA) and endothelin B (ETB) receptors. Macitentan displays higher efficacy, lesser adverse effects and drug interactions. It has completed phase III trials in 2012 for treatment of PAH and has been tried for ischemic digital ulcers in systemic sclerosis, recurrent glioblastoma and combination with chemotherapeutic agents against various cancers. Safety data for macitentan were obtained primarily from a placebo‑controlled clinical study in 742 patients with PAH. The Food and Drug Administration (FDA) approved the drug on 13 October 2013. It is an important addition to long‑term treatment of PAH.
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Khadka, A., Brashier, D. B. S., Tejus, A., & Sharma, A. K. (2015). Macitentan: An important addition to the treatment of pulmonary arterial hypertension. Journal of Pharmacology and Pharmacotherapeutics, 6(1), 53–57. https://doi.org/10.4103/0976-500X.149151