loading...| Preferred Name |
venetoclax |
|
| Synonyms |
Bcl-2 inhibitor GDC-0199 |
|
| Definitions |
An orally bioavailable, selective small molecule inhibitor of the anti-apoptotic protein Bcl-2, with potential antineoplastic activity. Venetoclax mimics BH3-only proteins, the native ligands of Bcl-2 and apoptosis activators, by binding to the hydrophobic groove of Bcl-2 proteins thereby repressing Bcl-2 activity and restoring apoptotic processes in tumor cells. Bcl-2 protein is overexpressed in some cancers and plays an important role in the regulation of apoptosis; its expression is associated with increased drug resistance and tumor cell survival. Compared to the Bcl-2 inhibitor navitoclax, this agent does not inhibit bcl-XL and does not cause bcl-XL-mediated thrombocytopenia. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C103147" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C103147" NCI Thesaurus) |
|
| ID |
http://purl.bioontology.org/ontology/PDQ/CDR0000698675 |
|
| altLabel |
Bcl-2 inhibitor GDC-0199 Venclexta GDC-0199 ABT199 ABT-0199 ABT-199 RG7601 |
|
| cui |
C3641087 C4079830 C4224858 C3641088 C4282411 |
|
| DATE FIRST PUBLISHED |
2011-04-07 |
|
| Date last modified |
2016-04-11 |
|
| definition |
An orally bioavailable, selective small molecule inhibitor of the anti-apoptotic protein Bcl-2, with potential antineoplastic activity. Venetoclax mimics BH3-only proteins, the native ligands of Bcl-2 and apoptosis activators, by binding to the hydrophobic groove of Bcl-2 proteins thereby repressing Bcl-2 activity and restoring apoptotic processes in tumor cells. Bcl-2 protein is overexpressed in some cancers and plays an important role in the regulation of apoptosis; its expression is associated with increased drug resistance and tumor cell survival. Compared to the Bcl-2 inhibitor navitoclax, this agent does not inhibit bcl-XL and does not cause bcl-XL-mediated thrombocytopenia. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C103147" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C103147" NCI Thesaurus) |
|
| LT |
TRD |
|
| NCI ID |
C103147 |
|
| notation |
CDR0000698675 |
|
| ORIG STY |
Drug/agent |
|
| prefLabel |
venetoclax |
|
| tui |
T109 T121 |