Ibrutinib

• PCI - 32765
• IUPAC: 1 - [( 3R ) -3 - [4- amino-3- (4- phenoxyphenyl) pyrazolo [3,4- d] pyrimidin- 1-yl] piperidin- 1-yl] prop-2- en-1 -on

Cytostatic

Tyrosine kinase inhibitor

Template: Infobox chemical / molecular formula search available

Ibrutinib (formerly PCI - 32765, Pharmacyclics and Janssen Pharmaceutica company ) is a drug from the group of tyrosine kinase inhibitors, which is used under the trade name Imbruvica for the treatment of mantle cell lymphoma.

Development and clinical trials

Ibrutinib is an oral tyrosine kinase inhibitor that inhibits the Bruton's tyrosine kinase ( BTK). This plays a central role in intracellular signaling in B lymphocytes. The intended clinical application of Ibrutinib are therefore malignant B- cell malignancies, in the strict sense B- cell non -Hodgkin's lymphomas, but also autoimmune diseases in which B cells play a role, such as rheumatoid arthritis.

Ibrutinib (then under the name of PCI - 32765 ) was a designer drug for the inhibition of BTK first synthesized in 2007. The substance shows a high in vitro activity against lymphoma cells, and finally reached the clinical testing. In two large treatment studies, which were published in high-ranking New England Journal of Medicine, Ibrutinib demonstrated activity in heavily pretreated patients with refractory chronic lymphocytic leukemia (CLL ) or mantle cell lymphoma. Based on these study results assessed the U.S. Food and Drug Administration ( FDA) drug containing the predicate breakthrough ( "breakthrough" ), which has accelerated approval result. Ibrutinib was authorized on November 13, 2013 by the FDA for the treatment of mantle cell lymphoma. The trade name in the United States is Imbruvica.