ArticleDrugs2014
Macitentan: first global approval.
Article in Drugs, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers, 1 of them a synthesis that pooled it.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
25 citing papers in PubMed, 1 synthesis or guideline pooled it, 48 citations in OpenAlex.
- Efficacy and safety of macitentan for pulmonary hypertension: A meta-analysis.The clinical respiratory journal · 2023Pooled it
- Investigation of mutual pharmacokinetic interactions between macitentan, a novel endothelin receptor antagonist, and sildenafil in healthy subjects.British journal of clinical pharmacology · 2014Trial
- Disproportionality analysis of adverse events associated with endothelin receptor antagonists based on the FDA adverse event reporting system (FAERS).Frontiers in cardiovascular medicine · 2026Article
- Novel immunotargets in multiple myeloma: biological relevance and therapeutic potential.Biomarker research · 2025Review
- Drug Interactions of Imperatorin and Curcumin on Macitentan in vitro and in vivo.Drug design, development and therapy · 2025Article
- Structural basis of antagonist selectivity in endothelin receptors.Cell discovery · 2024Article
- Late-stage modification of bioactive compounds: Improving druggability through efficient molecular editing.Acta pharmaceutica Sinica. B · 2024Review
- Endothelin Receptor Antagonists in Kidney Disease.International journal of molecular sciences · 2023Review
- Effects of bergapten on the pharmacokinetics of macitentan in rats bothFrontiers in pharmacology · 2023Article
- Results of Macitentan in Japanese Patients With Chronic Thromboembolic Pulmonary Hypertension - A Prospective, Multicenter, Open-Label, Single-Arm, Phase 3 Study.Circulation reports · 2021Article
- Novel Targets in a High-Altitude Pulmonary Hypertension Rat Model Based on RNA-seq and Proteomics.Frontiers in medicine · 2021Article
- Safety and efficacy of the endothelin receptor antagonist macitentan in pediatric pulmonary hypertension.Cardiovascular diagnosis and therapy · 2020Article
- Endothelin-receptor antagonists in the management of pulmonary arterial hypertension: where do we stand?Vascular health and risk management · 2018Review
- Endothelin.Pharmacological reviews · 2016Review
- An Update on Pulmonary Arterial Hypertension.The journal for nurse practitioners : JNP · 2015Article
- Comparative safety and tolerability of endothelin receptor antagonists in pulmonary arterial hypertension.Drug safety · 2015Review
- Endothelin receptors and their antagonists.Seminars in nephrology · 2015Review
- The role of endothelin-1 and endothelin receptor antagonists in inflammatory response and sepsis.Archivum immunologiae et therapiae experimentalis · 2015Review
- A pathogenetic role for endothelin-1 in peritoneal dialysis-associated fibrosis.Journal of the American Society of Nephrology : JASN · 2015Article
- Erlotinib augmentation with dapsone for rash mitigation and increased anti-cancer effectiveness.SpringerPlus · 2015Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Macitentan (Opsumit®) is a novel dual endothelin receptor antagonist (ERA) with sustained receptor binding properties developed by Actelion Pharmaceuticals Ltd. In October 2013, oral macitentan 10 mg once daily received its first global approval in the US, followed closely by Canada, for the treatment of pulmonary arterial hypertension (PAH). The drug has also received a positive opinion in the EU from the Committee for Medicinal Products for Human Use for the treatment of PAH, and is under regulatory review in several other countries for the same indication. Endothelin (ET)-1 influences pathological changes via two ET receptor subtypes (ETA and ETB), to which it binds with high affinity. ET-1 is implicated in several forms of vascular disease making it a valid target for the treatment of pulmonary vascular diseases such as PAH. Clinical development is underway for other indications, including Eisenmenger syndrome, ischaemic digital ulcers secondary to systemic sclerosis, and glioblastoma. Macitentan was also evaluated in idiopathic pulmonary fibrosis; however, a phase 2 trial did not meet its primary endpoint and further investigation in this indication was discontinued. Macitentan was developed by modifying the structure of bosentan in the search for an optimal dual ERA with improved efficacy and tolerability compared with other ERAs. This article summarizes the milestones in the development of macitentan leading to this first approval for PAH.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.