"目錄號(hào): HY-14184
Macitentan 是一種可口服的非肽類的ETA和ETB receptor的雙重拮抗劑，能有有效治療特發(fā)性肺纖維化和肺動(dòng)脈高壓癥狀。
相關(guān)產(chǎn)品
Atrasentan hydrochloride-BQ-788 sodium salt-Bosentan-Ambrisentan-Avosentan-BQ-123-ACT-132577-Sitaxsentan sodium-Sulfisoxazole-Zibotentan-Endothelin 1 swine, human-Aminaftone-Macitentan n-butyl analogue-PD-159020-Ro 46-2005-
生物活性
Description
Macitentan is an orally active, non-peptide dual endothelinETAandETB receptorantagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
In Vitro
Tube formation ability is restored when microvascular endothelial cells are preincubated with BOS or macitentan, also reducing the expression of mesenchymal markers and restoring CD31 expression and the imbalance between VEGF-A and VEGF-A165b[1]. Macitentan inhibits OATP1B1-mediated uptake of atorvastatin and OATP1B3-mediated uptake of estrone-3-sulfate with IC50?±?SE values of 6.3?±?0.7 and 11.8?±?5.0?μM, respectively[3]. Treatment with macitentan or with ACT-132577 does not lead to intracellular accumulation of R123 in HeyA8-MDR, showing that these compounds are not P-gp inhibitors[4].
In Vivo
Macitentan (25 mg/kg/day, p.o.) prevents increased production of vasoactive and fibrogenic factors, NF-κB activation, structural and functional changes, and increases extracellular matrix protein production in type 2 diabetes in type 2 diabetes[2]. Macitentan (10 mg/kg, p.o.) coupled with once-per-week 5 mg/kg taxol, significantly reduces the weight (size) of HeyA8-MDR tumors in mice. Combination therapy with macitentan (10 or 50 mg/kg, but not 5 mg/kg) and taxol or macitentan (10 mg/kg) and cisplatinum significantly reduces the number of proliferating Ki-67-positive cells[4].
Clinical Trial
Actelion
Pulmonary Arterial Hypertension
May 2008
Phase 3
Actelion
Idiopathic Pulmonary Fibrosis
May 2009
Phase 2
Actelion
Pulmonary Arterial Hypertension
May 2008
Phase 3
Actelion
Idiopathic Pulmonary Fibrosis
May 2009
Phase 2
Boston University-Actelion
Pulmonary Hypertension-Sickle Cell Disease
July 2015
Phase 1
Actelion
Pulmonary Arterial Hypertension
April 2013
Phase 3
Actelion
Glioblastoma
October 2014
Phase 1
Actelion
Pulmonary Arterial Hypertension
September 1, 2013
Phase 3
Actelion
Pulmonary Arterial Hypertension
June 1, 2015
Phase 4
Actelion
Pulmonary Arterial Hypertension
September 2013
Phase 3
Actelion
Chronic Thromboembolic Pulmonary Hypertension
February 9, 2015
Phase 2
Actelion
Pulmonary Arterial Hypertension
March 2014
Phase 3
Actelion
Pulmonary Arterial Hypertension
May 2013
Phase 3
Actelion
Pulmonary Arterial Hypertension
July 15, 2017
Phase 3
Actelion
Chronic Thromboembolic Pulmonary Hypertension
August 2014
Phase 2
Actelion
Digital Ulcers
December 2011
Phase 3
Actelion
Systemic Sclerosis-Ulcers
December 2011
Phase 3
University of California, Los Angeles
Lung Transplant Rejection
September 2016
Phase 4
Actelion
Idiopathic Pulmonary Fibrosis
July 2011
Phase 2
Actelion
Portopulmonary Hypertension
June 1, 2015
Phase 4
Actelion
Pulmonary Arterial Hypertension
April 1, 2014
Actelion
Healthy Subjects
August 3, 2017
Phase 1
Actelion
Pulmonary Arterial Hypertension
October 1, 2008
Phase 3
Actelion
Pulmonary Arterial Hypertension
June 1, 2014
Phase 3
Actelion
Pulmonary Hypertension
December 2015
Phase 2
Actelion
Pulmonary Hypertension
July 2014
Phase 2
Actelion
Healthy
August 2011
Phase 1
Actelion
Congenital Heart Disease
August 15, 2017
Phase 3
Actelion
Pulmonary Arterial Hypertension
September 2015
Phase 4
Actelion
Heart Failure With Preserved Ejection Fraction
July 31, 2017
Phase 2
Actelion
Pulmonary Arterial Hypertension
May 2016
Phase 3
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References
