Since the initial clinical approval in the late 1990s and remarkable anticancer effects for
certain types of cancer, molecular targeted therapy utilizing small molecule agents or …

Clinically acquired resistance is a major challenge in cancer therapies with small-molecule
kinase inhibitors (SMKIs). Gatekeeper mutations in the ATP-binding pocket of kinases are …

Bruton tyrosine kinase (BTK), a nonreceptor tyrosine kinase, is a major therapeutic target for
B-cell–driven malignancies. However, approved covalent BTK inhibitors (cBTKis) are …

Increasing use of covalent and noncovalent inhibitors of Bruton's tyrosine kinase (BTK) has
elucidated a series of acquired drug-resistant BTK mutations in patients with B cell …

Covalent inhibitors of Bruton tyrosine kinase (BTK) have transformed the therapy of chronic
lymphocytic leukemia (CLL), but continuous therapy has been complicated by the …

Abstract Pirtobrutinib (LOXO-305), a reversible inhibitor of Bruton's tyrosine kinase (BTK),
was designed as an alternative strategy to treat ibrutinib-resistant disease that develops due …

Simple Summary The availability of Bruton's tyrosine kinase (BTK) inhibitor ibrutinib has
undoubtedly reshaped the initial management of chronic lymphocytic leukemia (CLL) …

Bruton's tyrosine kinase (BTK) inhibition is one of the treatment standards for patients with
relapsed/refractory Waldenström's macroglobulinemia (WM) and for patients with WM who …

Despite significant efficacy, one of the major limitations of small-molecule Bruton's tyrosine
kinase (BTK) agents is the presence of clinically acquired resistance, which remains a major …

Low-molecular weight chemical compounds have a longstanding history as drugs. Target
specificity and binding efficiency represent major obstacles for small molecules to become …