loading...| Preferred Name |
macitentan |
|
| Synonyms |
Actelion-1 ACT-064992 N-[5-(4-bromophenyl)-6-(2-(5-bromopyrimidin-2-yloxy)ethoxy)-pyrimidin-4-yl]-N'-propylaminosulfonamide |
|
| 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. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C87728" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C87728" NCI Thesaurus) |
|
| ID |
http://purl.bioontology.org/ontology/PDQ/CDR0000721764 |
|
| altLabel |
Actelion-1 ACT-064992 N-[5-(4-bromophenyl)-6-(2-(5-bromopyrimidin-2-yloxy)ethoxy)-pyrimidin-4-yl]-N'-propylaminosulfonamide |
|
| cui |
C2606557 C2606556 C4282250 |
|
| DATE FIRST PUBLISHED |
2011-12-31 |
|
| Date last modified |
2012-01-03 |
|
| 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. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C87728" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C87728" NCI Thesaurus) |
|
| LT |
TRD |
|
| NCI ID |
C87728 |
|
| notation |
CDR0000721764 |
|
| ORIG STY |
Drug/agent |
|
| prefLabel |
macitentan |
|
| tui |
T109 T121 |