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Limitations of BTK Inhibitors in Cancer Treatment

The evolution of Bruton's tyrosine kinase (BTK) inhibitors has highlighted several challenges, including the need for improved selectivity to reduce off-target toxicities, overcoming covalent dependencies that create predictable bottlenecks, and addressing the limitations of reversible binding. Additionally, the role of BTK as a structural scaffold, not just an enzyme, poses a challenge for effective treatment. The 'treat-to-progression' paradigm also guarantees clonal evolution, leading to treatment resistance.

Science, Chemistry, Medicinal Chemistry