WBZ-4: Re-engineered Gleevec™, Reduces Cardio Risks
The powerful anti-cancer drug imatinib (Gleevec™) has been re-engineered by researchers at Rice University and the University of Texas M. D. Anderson Cancer Center.
Developed by Novartis Pharmaceuticals, Gleevec is approved by the U.S. Food and Drug Administration for the treatment of chronic myeloid leukemia (CML), Philadelphia-chromosome positive acute lymphoblastic leukemia and GIST.
The drug targets two proteins that have been linked with cancer. One of its targets is the C-Kit kinase, a protein that has been tied to gastrointestinal cancer, and another is Bcr-Abl kinase, a key protein controlling CML.
Not just for kicks, mind you, but to more specifically target one type of cancer while potentially curbing a rare life-threatening cardiotoxic side effect.
In a new study, it has been reported that the re-engineered Gleevec™ is just as effective as the original version against gastrointestinal stromal tumor (GIST) but carrying significantly less risk of heart failure.
Designed at Rice, using a new bottom-up approach for rational drug design (based on a rational strategy developed by Ariel Fernandez, professor of bioengineering), the re-engineered version of imatinib is now a new drug dubbed WBZ-4.
Said Ariel Fernandez:
“Our bottom-up design strategy is also broadly applicable to drugs other than imatinib and enables a rational control and reduction of side effects. For example, WBZ-4 was designed to target C-Kit without inhibiting the function of Bcr-Abl, which recent imatinib studies have associated with increased risk for heart failure.
We were successful in our three basic goals in redesigning the drug — we refocused the primary impact on C-Kit, we reduced the impact on Bcr-Abl, and we reduced cardiotoxicitity. Our results corroborate previous findings about the role that Bcr-Abl plays in the cardiotoxicity of imatinib.”
WBZ-4 is not yet available for human testing and dates for clinical trials have not been set.
But for sure, the endeavor will be pursued in the near future.
Find more details from Rice University.
Tags: Gleevec, imatinib, re-engineered-imatinib, WBZ-4Related Stories
POSTED IN: ~ Anti-cancer treatments ~
1 opinion for WBZ-4: Re-engineered Gleevec™, Reduces Cardio Risks
matt
Dec 7, 2007 at 10:23 pm
All the Gleevac that people get for label and off-label use I have never seen a cardiac toxicity. I know the toxicity is heart failure but I never really see it.
http://professional.cancerconsultants.com/oncology_leukemia_news.aspx?id=37864
this article makes it seem more anecdotal, then a large percent
Matt RN, BSN, MEd, OCN
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