API Macitentan Raw Material Macitentan

• Overview
• Product Description
• Product Details
• Application&Function
• Specification

Overview

Basic Info.

Model NO.	XMHT-macitentan
Certification	GMP, HSE, ISO 9001, USP, BP
Suitable for	Elderly, Children, Adult
State	Powder
Purity	>99%
Product Name	Macitentan
Name	Macitentan Powder
Appearance	White Powder
Color	White
CAS	441798-33-0
Mf	C19h20br2n6o4s
MW	588.27
Melting Point	134-136°C
Boiling Point	692.397 °C at 760 Mmhg
Assay	99%
Grade	Pharmaceutical Grade
Application	Pharmaceutical
Specific	COA
Test Method	HPLC
Shelf Life	2 Years
Transport Package	Negotiable
Specification	99%
Trademark	XMHT
Origin	Xi'an
Production Capacity	500kg/Month

Product Description

API Macitentan Raw Material MacitentanProduct Description

Product Details

Product Name	Macitentan
Appearance	White Powder
CAS	441798-33-0
MF	C19H20Br2N6O4S
MW	588.27

Macitentan is an advanced oral endothelin receptor antagonist (ERA) specifically developed for the long-term management of pulmonary arterial hypertension (PAH). Its clinical efficacy and safety profile are robustly supported by the landmark SERAPHIN study, a large-scale, multicenter, double-blind, placebo-controlled Phase III clinical trial. This pivotal study demonstrated that macitentan significantly reduces the risk of morbidity and mortality events in PAH patients.Application&Function

The primary mechanism of action involves dual blockade of both endothelin-A (ET-A) and endothelin-B (ET-B) receptors. Endothelin-1 (ET-1) is a potent vasoconstrictor and mitogen, whose pathological overexpression is a key driver in PAH. By antagonizing both receptor subtypes, macitentan comprehensively inhibits the detrimental effects of ET-1. Blocking ET-A receptors in vascular smooth muscle cells leads to potent and sustained vasodilation of the pulmonary arteries, reducing pulmonary vascular resistance (PVR). Concurrently, antagonism of ET-B receptors, which are also involved in vasoconstriction and fibrosis, further contributes to the therapeutic effect and may help modulate ET-1 clearance. This dual action not only improves hemodynamics but also directly counteracts the pathogenic processes of vascular remodeling and proliferation of smooth muscle cells, which are characteristic of PAH progression.The clinical benefits of macitentan are multi-faceted and significant. The most compelling evidence from the SERAPHIN trial showed a 45% reduction in the composite endpoint of morbidity and mortality compared to placebo over a median treatment duration of approximately two years. This morbidity/mortality endpoint included disease progression, initiation of intravenous or subcutaneous prostanoid therapy, lung transplantation, atrial septostomy, or death. A key efficacy parameter, the six-minute walk distance (6MWD), was significantly improved and maintained in patients treated with macitentan. Furthermore, treatment with macitentan led to a substantial delay in clinical worsening. Clinical worsening was defined as the first occurrence of death, a start of intravenous or subcutaneous prostanoid therapy, lung transplantation, atrial septostomy, or worsening of PAH. The time to this event was significantly prolonged, underscoring the drug's capacity to stabilize the disease over the long term.Specification