Article
Pirtobrutinib targets BTK C481S in ibrutinib-resistant CLL but second-site BTK mutations lead to resistance.
Blood advances - 9 May 2023
Naeem Aishath, Utro Filippo, Wang Qing, Cha Justin, Vihinen Mauno, Martindale Stephen, Zhou Yinglu, Ren Yue, Tyekucheva Svitlana, Kim Annette S, Fernandes Stacey M, Saksena Gordon, Rhrissorrakrai Kahn, Levovitz Chaya, Danysh Brian P, Slowik Kara, Jacobs Raquel A, Davids Matthew S, Lederer James A, Zain Rula, Smith C I Edvard, Leshchiner Ignaty, Parida Laxmi, Getz Gad, Brown Jennifer R
Abstract excerpt
Covalent inhibitors of Bruton tyrosine kinase (BTK) have transformed the therapy of chronic lymphocytic leukemia (CLL), but continuous therapy has been complicated by the development of resistance. The most common resistance mechanism in patients whose disease progresses on covalent BTK inhibitors (BTKis) is a mutation in the BTK 481 cysteine residue to which the inhibitors bind covalently. Pirtobrutinib is a...
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