Reformulated Imatinib Inhibits PDGFR-β, Eliminating Morphine Analgesic Tolerance in Rats

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(ChemotherapyAdvisor) – Inhibition of platelet-derived growth factor receptor-β (PDGFR-β) selectively eliminated morphine tolerance in rats, a study published in Nature Medicine online February 19 has found.

“PDGFR-β inhibitors are widely used and well tolerated, suggesting that clinical translation of our findings could reduce the suffering endured by individuals with intractable pain,” the investigators noted in the first study to identify the key role of cellular signaling in morphine tolerance.

In the study, the investigators reformulated imatinib (Gleevec) using a carrier molecule, Captisol, which increased drug delivery to the brain. The modified imatinib prevented morphine tolerance and was found to reverse tolerance in rats receiving high morphine doses continuously for several days.


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