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Current Status of Endothelin Receptor Antagonists in Pulmonary Arterial Hypertension: A Combined Study Results and Pharmacology-Based Review

Pulmonary arterial hypertension (PAH) affects a wide range of people globally and has a poor prognosis despite many advancements in available treatment options. Among the available treatments, endothelin receptor antagonists (ERA) are among the most widely used drugs. These drugs have been evaluated...

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Autores principales: Nahar, Shamsun, Kanda, Srishti, Chatha, Uzair, Odoma, Victor A, Pitliya, Aakanksha, AlEdani, Esraa M, Bhangu, Japneet K, Javed, Khalid, Manshahia, Prabhleen Kaur, Yu, Ann Kashmer
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Cureus 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10467640/
https://www.ncbi.nlm.nih.gov/pubmed/37654961
http://dx.doi.org/10.7759/cureus.42748
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author Nahar, Shamsun
Kanda, Srishti
Chatha, Uzair
Odoma, Victor A
Pitliya, Aakanksha
AlEdani, Esraa M
Bhangu, Japneet K
Javed, Khalid
Manshahia, Prabhleen Kaur
Yu, Ann Kashmer
author_facet Nahar, Shamsun
Kanda, Srishti
Chatha, Uzair
Odoma, Victor A
Pitliya, Aakanksha
AlEdani, Esraa M
Bhangu, Japneet K
Javed, Khalid
Manshahia, Prabhleen Kaur
Yu, Ann Kashmer
author_sort Nahar, Shamsun
collection PubMed
description Pulmonary arterial hypertension (PAH) affects a wide range of people globally and has a poor prognosis despite many advancements in available treatment options. Among the available treatments, endothelin receptor antagonists (ERA) are among the most widely used drugs. These drugs have been evaluated in scientific trials. We included free full texts in the English language from the last ten years and reviewed them. We are writing this review to amalgamate the pharmacological aspects and the previous studies on ERAs to demonstrate a comprehensive overview of the current status of ERAs for PAH treatment. We focused on the structure, pharmacodynamics, pharmacokinetics, and efficacy and safety of the three most widely used ERAs: Bosentan, Ambrisentan, and Macitentan. These drugs have different receptor affinities, bioavailability, excretion routes, and different levels of safety profiles. There are three available studies, the RCT, the ARIES series, and the SERAPHIN studies, for assessing the safety and efficacy of Bosentan, Ambrisentan, and Macitentan, respectively. All the studies and some additional studies for combination therapy have proven all three drugs effective in treating PAH. The side effects (SE) varied from headache and hepatic enzyme elevation to worsening the PAH status of varied severities. Although these studies provided valuable insight into the role of ERAs, there is still enough scope for more studies on ERAs, both as monotherapy and combination therapy for PAH.
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spelling pubmed-104676402023-08-31 Current Status of Endothelin Receptor Antagonists in Pulmonary Arterial Hypertension: A Combined Study Results and Pharmacology-Based Review Nahar, Shamsun Kanda, Srishti Chatha, Uzair Odoma, Victor A Pitliya, Aakanksha AlEdani, Esraa M Bhangu, Japneet K Javed, Khalid Manshahia, Prabhleen Kaur Yu, Ann Kashmer Cureus Cardiology Pulmonary arterial hypertension (PAH) affects a wide range of people globally and has a poor prognosis despite many advancements in available treatment options. Among the available treatments, endothelin receptor antagonists (ERA) are among the most widely used drugs. These drugs have been evaluated in scientific trials. We included free full texts in the English language from the last ten years and reviewed them. We are writing this review to amalgamate the pharmacological aspects and the previous studies on ERAs to demonstrate a comprehensive overview of the current status of ERAs for PAH treatment. We focused on the structure, pharmacodynamics, pharmacokinetics, and efficacy and safety of the three most widely used ERAs: Bosentan, Ambrisentan, and Macitentan. These drugs have different receptor affinities, bioavailability, excretion routes, and different levels of safety profiles. There are three available studies, the RCT, the ARIES series, and the SERAPHIN studies, for assessing the safety and efficacy of Bosentan, Ambrisentan, and Macitentan, respectively. All the studies and some additional studies for combination therapy have proven all three drugs effective in treating PAH. The side effects (SE) varied from headache and hepatic enzyme elevation to worsening the PAH status of varied severities. Although these studies provided valuable insight into the role of ERAs, there is still enough scope for more studies on ERAs, both as monotherapy and combination therapy for PAH. Cureus 2023-07-31 /pmc/articles/PMC10467640/ /pubmed/37654961 http://dx.doi.org/10.7759/cureus.42748 Text en Copyright © 2023, Nahar et al. https://creativecommons.org/licenses/by/3.0/This is an open access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
spellingShingle Cardiology
Nahar, Shamsun
Kanda, Srishti
Chatha, Uzair
Odoma, Victor A
Pitliya, Aakanksha
AlEdani, Esraa M
Bhangu, Japneet K
Javed, Khalid
Manshahia, Prabhleen Kaur
Yu, Ann Kashmer
Current Status of Endothelin Receptor Antagonists in Pulmonary Arterial Hypertension: A Combined Study Results and Pharmacology-Based Review
title Current Status of Endothelin Receptor Antagonists in Pulmonary Arterial Hypertension: A Combined Study Results and Pharmacology-Based Review
title_full Current Status of Endothelin Receptor Antagonists in Pulmonary Arterial Hypertension: A Combined Study Results and Pharmacology-Based Review
title_fullStr Current Status of Endothelin Receptor Antagonists in Pulmonary Arterial Hypertension: A Combined Study Results and Pharmacology-Based Review
title_full_unstemmed Current Status of Endothelin Receptor Antagonists in Pulmonary Arterial Hypertension: A Combined Study Results and Pharmacology-Based Review
title_short Current Status of Endothelin Receptor Antagonists in Pulmonary Arterial Hypertension: A Combined Study Results and Pharmacology-Based Review
title_sort current status of endothelin receptor antagonists in pulmonary arterial hypertension: a combined study results and pharmacology-based review
topic Cardiology
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10467640/
https://www.ncbi.nlm.nih.gov/pubmed/37654961
http://dx.doi.org/10.7759/cureus.42748
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