loading...| Preferred Name |
ibrutinib |
|
| Synonyms |
Bruton's tyrosine kinase inhibitor PCI-32765 CRA-032765 PCI-32765 BTK inhibitor PCI-32765 2-propen-1-one, 1-((3R)-3-(4-amino-3-(4-phenoxyphenyl)-1h-pyrazolo(3,4-d)pyrimidin-1-yl)-1-piperidinyl)- Imbruvica |
|
| Definitions |
An orally bioavailable, small-molecule inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon oral administration, ibrutinib binds to and irreversibly inhibits BTK activity, thereby preventing both B-cell activation and B-cell-mediated signaling. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is required for B cell receptor signaling, plays a key role in B-cell maturation, and is overexpressed in a number of B-cell malignancies. The expression of BTK in tumor cells is also associated with increased proliferation and survival. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C81934" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C81934" NCI Thesaurus) |
|
| ID |
http://purl.bioontology.org/ontology/PDQ/CDR0000638648 |
|
| altLabel |
Bruton's tyrosine kinase inhibitor PCI-32765 CRA-032765 PCI-32765 BTK inhibitor PCI-32765 2-propen-1-one, 1-((3R)-3-(4-amino-3-(4-phenoxyphenyl)-1h-pyrazolo(3,4-d)pyrimidin-1-yl)-1-piperidinyl)- Imbruvica |
|
| cui |
C3692993 C2830052 C3501358 |
|
| DATE FIRST PUBLISHED |
2009-03-19 |
|
| Date last modified |
2013-11-13 |
|
| definition |
An orally bioavailable, small-molecule inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon oral administration, ibrutinib binds to and irreversibly inhibits BTK activity, thereby preventing both B-cell activation and B-cell-mediated signaling. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is required for B cell receptor signaling, plays a key role in B-cell maturation, and is overexpressed in a number of B-cell malignancies. The expression of BTK in tumor cells is also associated with increased proliferation and survival. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C81934" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C81934" NCI Thesaurus) |
|
| LT |
TRD |
|
| NCI ID |
C81934 |
|
| notation |
CDR0000638648 |
|
| ORIG STY |
Drug/agent |
|
| prefLabel |
ibrutinib |
|
| tui |
T109 T121 |