loading...| Preferred Name | apalutamide | |
| Synonyms |
4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide AR antagonist ARN-509 JNJ-56021927 ARN-509 androgen receptor antagonist ARN-509 Erleada |
|
| Definitions |
A small molecule and androgen receptor (AR) antagonist with potential antineoplastic activity. Apalutamide binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes. This ultimately inhibits the expression of genes that regulate prostate cancer cell proliferation and may lead to an inhibition of cell growth in AR-expressing tumor cells. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C92574" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C92574" NCI Thesaurus) |
|
| ID |
http://purl.bioontology.org/ontology/PDQ/CDR0000683082 |
|
| altLabel |
4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide AR antagonist ARN-509 JNJ-56021927 ARN-509 androgen receptor antagonist ARN-509 Erleada |
|
| CAS Registry |
956104-40-8 |
|
| cui |
C4329353 C2985183 C4331906 C4551002 |
|
| DATE FIRST PUBLISHED |
2010-08-03 |
|
| Date last modified |
2018-02-15 |
|
| definition |
A small molecule and androgen receptor (AR) antagonist with potential antineoplastic activity. Apalutamide binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes. This ultimately inhibits the expression of genes that regulate prostate cancer cell proliferation and may lead to an inhibition of cell growth in AR-expressing tumor cells. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C92574" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C92574" NCI Thesaurus) |
|
| LT |
TRD |
|
| NCI ID |
C92574 |
|
| notation |
CDR0000683082 |
|
| ORIG STY |
Drug/agent |
|
| prefLabel |
apalutamide |
|
| tui |
T109 T121 |