Document Detail

Ibrutinib (PCI-32765), the first BTK (Bruton's tyrosine kinase) inhibitor in clinical trials.
MedLine Citation:
PMID:  23296407     Owner:  NLM     Status:  MEDLINE    
Ibrutinib is a potent covalent kinase inhibitor that targets BTK. BTK, or Bruton's tyrosine kinase, is an obvious target for therapy of B cell diseases because inactivating mutations lead to B cell aplasia in humans and the disease X-linked agammaglobulinemia. Ibrutinib has modest cytotoxicity against CLL cells in vitro but also blocks trophic stimuli from the microenvironment. As with other inhibitors of the BCR pathway, ibrutinib causes rapid nodal reduction and response associated with rapid increase in lymphocytosis, which then returns to baseline over time. The ORR of ibrutinib in relapsed refractory CLL is 67 % with PFS 88 % at 15 months. In a cohort of untreated patients 65 years and over, the estimated 15 month PFS is 96 %. Registration trials have been initiated, and the difficult task that remains is to determine where in the course of CLL therapy this drug will have the greatest impact and benefit for patients.
Jennifer R Brown
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Review    
Journal Detail:
Title:  Current hematologic malignancy reports     Volume:  8     ISSN:  1558-822X     ISO Abbreviation:  Curr Hematol Malig Rep     Publication Date:  2013 Mar 
Date Detail:
Created Date:  2013-02-22     Completed Date:  2013-07-16     Revised Date:  2014-03-07    
Medline Journal Info:
Nlm Unique ID:  101262565     Medline TA:  Curr Hematol Malig Rep     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1-6     Citation Subset:  IM    
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MeSH Terms
Antineoplastic Agents / therapeutic use*
Clinical Trials as Topic
Leukemia, Lymphocytic, Chronic, B-Cell / drug therapy*,  enzymology
Protein-Tyrosine Kinases / antagonists & inhibitors*
Pyrazoles / therapeutic use*
Pyrimidines / therapeutic use*
Grant Support
Reg. No./Substance:
0/Antineoplastic Agents; 0/PCI 32765; 0/Pyrazoles; 0/Pyrimidines; EC tyrosine kinase; EC Kinases

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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