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Bosutinib Fairly Safe For Chronic Myelogenous Leukemia
December 13, 2007 at 6:50 PM
Drug News
The most common side effects were low-grade nausea, vomiting and diarrhea, which improved greatly three or four weeks into therapy. Higher grade side effects such as low counts of platelets, white or red blood cells ranged from 1 to 9 percent of patients. Fluid build-up in the lungs and other organs occurred in only 12 patients and was of low grade.
Cortes says the researchers suspect that the low grade and frequency of side effects is probably a result of the drug's specificity in the proteins that it targets. Bosutinib inhibits SRC and ABL proteins but does not affect platelet derived growth factor receptor or C-Kit, two similar kinases that are affected by other CML drugs.
CML is caused by the Bcr-Abl protein, which results from a chromosomal abnormality called the Philadelphia Chromosome. Bcr-Abl is a tyrosine kinase that fuels an overabundance of white blood cells and immature stem cells called blasts that crowd out red blood cells and platelets.
Tyrosine kinases are a specialized subgroup of protein kinases, which regulate protein behavior by attaching phosphate groups to proteins or small molecules. Bosutinib, like imatinib (Gleevec(r)), dasatinib (Sprycel(r)) and nilotinib (Tasigna(r)), is a tyrosine kinase inhibitor.
The researchers also found that bosutinib is effective against a variety of Bcr-Abl mutants that cause CML and conclude that the drug is effective in imatinib-resistant patients with chronic CML across a range of mutations and after the failure of other tyrosine kinase inhibitors.
Source-Eurekalert
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