Article
Mechanisms of Resistance to Noncovalent Bruton's Tyrosine Kinase Inhibitors.
The New England journal of medicine - 24 Feb 2022
Wang Eric, Mi Xiaoli, Thompson Meghan C, Montoya Skye, Notti Ryan Q, Afaghani Jumana, Durham Benjamin H, Penson Alex, Witkowski Matthew T, Lu Sydney X, Bourcier Jessie, Hogg Simon J, Erickson Caroline, Cui Dan, Cho Hana, Singer Michael, Totiger Tulasigeri M, Chaudhry Sana, Geyer Mark, Alencar Alvaro, Linley Adam J, Palomba M Lia, Coombs Catherine C, Park Jae H, Zelenetz Andrew, Roeker Lindsey, Rosendahl Mary, Tsai Donald E, Ebata Kevin, Brandhuber Barbara, Hyman David M, Aifantis Iannis, Mato Anthony, Taylor Justin, Abdel-Wahab Omar
Abstract excerpt
BACKGROUND: Covalent (irreversible) Bruton's tyrosine kinase (BTK) inhibitors have transformed the treatment of multiple B-cell cancers, especially chronic lymphocytic leukemia (CLL). However, resistance can arise through multiple mechanisms, including acquired mutations in BTK at residue C481, the binding site of covalent BTK inhibitors. Noncovalent (reversible) BTK inhibitors overcome this mechanism and other...
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