loading...| Preferred Name |
Macitentan |
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| Synonyms |
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|
| 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. |
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| ID |
http://purl.obolibrary.org/obo/NCIT_C87728 |
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| Accepted_Therapeutic_Use_For |
Pulmonary arterial hypertension, idiopathic pulmonary fibrosis, oncology |
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| CAS_Registry |
441798-33-0 |
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| Chemical_Formula |
C19H20Br2N6O4S |
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| code |
C87728 |
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| Contributing_Source |
CTRP FDA |
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| 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. |
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| Display_Name |
Macitentan |
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| FDA_UNII_Code |
Z9K9Y9WMVL |
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| Has_Target | ||
| in_subset |
http://purl.obolibrary.org/obo/NCIT_C63923 http://purl.obolibrary.org/obo/NCIT_C177537 http://purl.obolibrary.org/obo/NCIT_C176424 http://purl.obolibrary.org/obo/NCIT_C116977 http://purl.obolibrary.org/obo/NCIT_C116978 http://purl.obolibrary.org/obo/NCIT_C128784 |
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| Is_Value_For_GDC_Property | ||
| label |
Macitentan |
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| Maps_To |
Macitentan |
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| NCI_Drug_Dictionary_ID |
721764 |
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| PDQ_Closed_Trial_Search_ID |
721764 |
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| PDQ_Open_Trial_Search_ID |
721764 |
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| Preferred_Name |
Macitentan |
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| prefixIRI |
NCIT:C87728 |
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| prefLabel |
Macitentan |
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| Semantic_Type |
Pharmacologic Substance |
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| UMLS_CUI |
C2606556 |
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| subClassOf |