loading...| Preferred Name |
Macitentan |
|
| Synonyms |
N-(5-(4-Bromophenyl)-6-(2-((5-Bromopyrimidin-2-Yl)Oxi)Ethoxy)Pyrimidin-4-Yl)-N'-Propylsulfuric Diamide ACT-064992 Actelion-1 MACITENTAN Macitentan |
|
| Definitions |
An orally available dual endothelin receptor (ETR) antagonist with potential antihypertensive and antineoplastic activity. Upon administration, macitentan and its metabolites block the binding of endothelin isoform 1 (ET-1) to type-A and type-B ETR on both the tumor cells and the endothelial cells in the tumor vasculature. This prevents ET-1 mediated signaling transduction which may decrease tumor cell proliferation, progression, and angiogenesis in tumor tissue. ET-1, a potent vasoconstrictor that plays an important role in inflammation and tissue repair, is, together with its receptors, overexpressed varyingly in many tumor cell types. |
|
| ID |
http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C87728 |
|
| Accepted_Therapeutic_Use_For |
Pulmonary arterial hypertension, idiopathic pulmonary fibrosis, oncology |
|
| CAS_Registry |
441798-33-0 |
|
| Chemical_Formula |
C19H20Br2N6O4S |
|
| code |
C87728 |
|
| Concept_In_Subset |
http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C176424 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157711 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157712 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116978 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116977 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C128784 |
|
| Contributing_Source |
CTRP FDA GDC |
|
| DEFINITION |
An orally available dual endothelin receptor (ETR) antagonist with potential antihypertensive and antineoplastic activity. Upon administration, macitentan and its metabolites block the binding of endothelin isoform 1 (ET-1) to type-A and type-B ETR on both the tumor cells and the endothelial cells in the tumor vasculature. This prevents ET-1 mediated signaling transduction which may decrease tumor cell proliferation, progression, and angiogenesis in tumor tissue. ET-1, a potent vasoconstrictor that plays an important role in inflammation and tissue repair, is, together with its receptors, overexpressed varyingly in many tumor cell types. |
|
| Display_Name |
Macitentan |
|
| FDA_UNII_Code |
Z9K9Y9WMVL |
|
| FULL_SYN |
N-(5-(4-Bromophenyl)-6-(2-((5-Bromopyrimidin-2-Yl)Oxi)Ethoxy)Pyrimidin-4-Yl)-N'-Propylsulfuric Diamide ACT-064992 Actelion-1 MACITENTAN Macitentan |
|
| Has_Target | ||
| Is_Value_For_GDC_Property | ||
| label |
Macitentan |
|
| Maps_To |
Macitentan |
|
| NCI_Drug_Dictionary_ID |
721764 |
|
| PDQ_Closed_Trial_Search_ID |
721764 |
|
| PDQ_Open_Trial_Search_ID |
721764 |
|
| Preferred_Name |
Macitentan |
|
| prefixIRI |
Thesaurus:C87728 |
|
| Semantic_Type |
Pharmacologic Substance |
|
| UMLS_CUI |
C2606556 |
|
| subClassOf |