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[gerry]

ORLANDO, Florida—A new potent, specific inhibitor of BCR-ABL with a distinct mechanism of action shows rapid anti-tumor activity in heavily pretreated patients with chronic myeloid leukemia (CML), according to data reported here at the American Society of Hematology Annual Meeting (Abstract 138).

 

ABL001 is a small molecule designed to inhibit BCR-ABL in a different way than other tyrosine kinase inhibitors (TKIs) as it binds to a unique region of BCR-ABL, forcing a conformational change that disables the protein's active site, explained Oliver G. Ottmann, MD, of the Department of Hematology, School of Medicine, at Cardiff University in the UK.

In an interview, Ottmann said: "This new class of drug, allosteric inhibitor, inhibits TKI activity not through the classic mode, but instead to a physically remote area of the BCR-ABL protein, inducing changes in the kinase. The idea is to overcome resistance mediated by classic TKIs and point mutations."

 

http://journals.lww....Heavily.11.aspx

[gerry]

A New Use for Nilotinib...

 

Tyrosine kinase inhibitors (TKIs) have changed the treatment paradigm for patients with chronic myelogenous leukemia (CML), and new research suggests one of the agents could potentially do the same for patients with Parkinson's disease. Researchers found that nilotinib (marketed as Tasigna by Novartis)—approved by the U.S. Food and Drug Administration for the treatment of patients with CML (OT 7/10/10 issue)—improved cognition, motor skills, and non-motor function for patients with Parkinson's disease and Lewy body dementia. Complete data from the Phase I clinical trial were presented at the Annual Meeting of the Society for Neuroscience in October (Program 12, Poster 1).

http://journals.lww....inib___.12.aspx