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Curr Med Chem. 2019;26(33):6033-6052. doi: 10.2174/0929867325666180607092451.

A Chemical Approach to Overcome Tyrosine Kinase Inhibitors Resistance: Learning from Chronic Myeloid Leukemia.

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Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Padova, Italy.



The possibilities of treatment for oncological diseases are growing enormously in the last decades. Unfortunately, these developments have led to the onset of resistances with regards to the new treatments. This is particularly true if we face with the therapeutic field of Tyrosine Kinase Inhibitors (TKIs). This review gives an overview of possible TKI resistances that can occur during the treatment of an oncologic diesease and available strategies that can be adopted, taking cues from a successful example such as CML.


We performed a literature search for peer-reviewed articles using different databases, such as PubMed and Scopus, and exploiting different keywords and different logical operators.


68 papers were included in the review. Twenty-four papers give an overview of the causes of TKIs resistances in the wide oncologic field. The remaining papers deal CML, deeply analysing the TKIs Resistances present in this pathology and the strategies adopted to overcome them.


The aim of this review is to furnish an overview and a methodological guideline for the approach and the overcoming of TKIs Resistances.


Bcr-Abl; Cancer; TKI; asciminib; chronic myeloid leukemia; imatinib; kinase; resistance.

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