マシテンタン

Also known as ACT-064992, ACT064992, ACT 064992

Macitentan, sold under the brand name Opsumit, is an endothelin receptor antagonist developed by Actelion and approved for the treatment of pulmonary arterial hypertension (PAH). Macitentan is a dual endothelin receptor antagonist, meaning that it acts as an antagonist of two endothelin (ET) receptor subtypes, ETA and ETB. However, macitentan has a 50-fold increased selectivity for the ETA subtype compared to the ETB subtype.

In the Vinony graph

Within Vinony's link graph, マシテンタン is referenced by 159 other articles, and connects out to digital object identifier, chemical formula and integral.

It is catalogued under topics including 4-Bromophenyl compounds, Bromoarenes and Drugs developed by Johnson & Johnson.

Its subject is documented across 11 Wikipedia language editions.

Chemical data

Formula: C19H20Br2N6O4S
Molecular weight: 588.3 g/mol
IUPAC name: 5-(4-bromophenyl)-6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-N-(propylsulfamoyl)pyrimidin-4-amine
SMILES: CCCNS(=O)(=O)NC1=C(C(=NC=N1)OCCOC2=NC=C(C=N2)Br)C3=CC=C(C=C3)Br
InChIKey: JGCMEBMXRHSZKX-UHFFFAOYSA-N
XLogP: 3.7
Polar surface area: 137 Å²
H-bond donors: 2
H-bond acceptors: 10
Formal charge: 0

via PubChem

Drug data · ChEMBL

Max clinical phase: Approved
Molecule type: Small molecule
First approval: 2010
Admin. routes: oral
Indications: pulmonary arterial hypertension, idiopathic pulmonary fibrosis, systemic scleroderma, glioblastoma multiforme

via ChEMBL · EBI

Wikidata facts

Subclass of: chemical compound
Mass: 585.9633483200003
Has use: medication

Show 7 more facts

chemical formula: C₁₉H₂₀Br₂N₆O₄S
canonical SMILES: CCCNS(=O)(=O)NC1=C(C(=NC=N1)OCCOC2=NC=C(C=N2)Br)C3=CC=C(C=C3)Br
World Health Organisation international non-proprietary name: macitentan
defined daily dose: 10
medical condition treated: pulmonary hypertension
Commons category: Macitentan
legal status (medicine): boxed warning

Sources (7)

via Wikidata · CC0

Article · 日本語

マシテンタン（Macitentan）は（ERA）の一つであり、肺高血圧（PAH）の治療に使用される。デュアルエンドセリン受容体拮抗薬であり、2種類のエンドセリン（ET）受容体（および）に結合するが、ETBへの結合力に比べてETAへの結合力は50倍強い。米国では2013年10月に承認された。商品名オプスミット。日本では2015年2月に薬事・食品衛生審議会が審議、承認了承し、2015年3月に厚生労働省に承認された。開発コードACT-064992。

Abstract from DBpedia / Wikipedia · CC BY-SA