Preferred Name |
Venetoclax |
|
Synonyms |
|
|
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. |
|
ID |
http://purl.obolibrary.org/obo/NCIT_C103147 |
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Accepted_Therapeutic_Use_For |
chronic lymphocytic leukemia (CLL) with 17p deletion and or small lymphocytic lymphoma (SLL) |
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CAS_Registry |
1257044-40-8 |
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code |
C103147 |
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Contributing_Source |
CTRP FDA |
|
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. |
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Display_Name |
Venetoclax |
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FDA_UNII_Code |
N54AIC43PW |
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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 |
Venetoclax |
|
Maps_To |
Venetoclax |
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NCI_Drug_Dictionary_ID |
698675 |
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PDQ_Closed_Trial_Search_ID |
698675 |
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PDQ_Open_Trial_Search_ID |
698675 |
|
Preferred_Name |
Venetoclax |
|
prefixIRI |
NCIT:C103147 |
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prefLabel |
Venetoclax |
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Semantic_Type |
Pharmacologic Substance |
|
UMLS_CUI |
C3659811 |
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subClassOf |