Pharmacyclics announces preclinical data indicating potential use of Novel Selective B-Cell Inhibitor

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Pharmacyclics: announces preclinical data publication indicating potential

use of Novel Selective B-Cell Tyrosine Kinase Inhibitor

http://news.moneycentral.msn.com/provider/providerarticle.aspx?Feed=BCOM & Date=20\

061213 & ID=6271777

Co announces publication of data characterizing its compounds designed to

inhibit Bruton's Tyrosine Kinase or B.T.K..

B.T.K. is a tyrosine kinase signaling molecule expressed in multiple immune

cell types, including B-cells, macrophages and mast cells, and is required

for B-cell activation, which plays a major role in autoimmune diseases and

lymphomas.

Structure-based design was used to synthesize small molecule drug candidates

that demonstrated potent selectivity for Btk versus other tyrosine kinase

binding sites.

In animal models of rheumatoid arthritis, these compounds demonstrated a

dose-dependent ability to inhibit disease development, with a greater than

95% decrease in arthritis score.

" These results show our proprietary compounds bind to the active site of Btk

and block the function of this B-cell signaling molecule, " said Lee

Honigberg, Ph.D., co-author on the paper and principal scientist at

Pharmacyclics.

" In addition, we found that these compounds are orally active in a

rheumatoid arthritis animal model, which validates BT.K. as a potentially

important clinical target in autoimmune disorders. "