General Information

Macitentan Impurities and Macitentan 

For evaluating the purity and safety of Macitentan, an essential active pharmaceutical ingredient, Daicel Pharma offers a customized synthesis of Macitentan impurity standards. These impurity standards include crucial compounds such as HN-MCTRCO1, HN-MCTRCO2, N-Despropyl Macitentan, HN-MCTRCO3, and more. Additionally, Daicel Pharma provides worldwide delivery options for Macitentan impurity standards.

Macitentan [CAS: 441798-33-0] has antihypertensive and antineoplastic properties and is a dual endothelin receptor (ETR) antagonist. It treats pulmonary arterial hypertension (PAH). Acting as an endothelin receptor antagonist, Macitentan functions as an antihypertensive agent by blocking the effects of endothelin, a hormone involved in blood vessel constriction.

Macitentan: Use and Commercial Availability 

Opsumit, which contains the active ingredient Macitentan, is a medication for the long-term treatment of patients with pulmonary arterial hypertension (PAH) classified as World Health Organization (WHO) Functional Class II or III. It reduces morbidity in PAH cases associated with idiopathic or heritable factors and those linked to connective tissue disease or congenital heart disease. Opsumit can be used alone or in combination with phosphodiesterase-5 (PDE-5) inhibitors as a part of the treatment regimen.

Macitentan Structure and Mechanism of Action

The chemical name of Macitentan is N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N′-propylsulfamide. Its chemical formula is C₁₉H₂₀Br₂N₆O₄S, and its molecular weight is approximately 588.3 g/mol.

Macitentan prevents the binding of Endothelin (ET)-1 to ET_A and ET_B receptors in smooth muscle cells.

Macitentan Impurities and Synthesis

The analysis and control of impurities in Macitentan¹, an endothelin receptor antagonist used for pulmonary arterial hypertension, are critical for ensuring its safety and efficacy. Impurities in Macitentan may include related compounds and degradation products. Analytical techniques such as high-performance liquid chromatography (HPLC) and mass spectrometry (MS) help identify and quantify these impurities. Stringent control measures and specifications limit the presence of impurities in Macitentan, following regulatory guidelines.

Daicel Pharma strictly adheres to cGMP standards and operates an analytical facility for preparing Macitentan impurity standards, which include HN-MCTRCO1, HN-MCTRCO2, N-Despropyl Macitentan, HN-MCTRCO3, and more. In addition, we offer deuterium-labeled Macitentan standard, Macitentan-D4, which is essential for conducting bioanalytical research and BA/BE studies. Our Macitentan impurity standards have a detailed Certificate of Analysis (CoA) that provides a comprehensive characterization report. This report includes data obtained through techniques, 1H NMR, 13C NMR, IR, MASS, and HPLC purity analysis². Upon request, we give additional data like 13C-DEPT. Moreover, we can synthesize unknown Macitentan impurity standards, degradation products, and labeled compounds to evaluate the effectiveness of generic Macitentan. Each delivery has a comprehensive characterization report.