Pirtobrutinib inhibits wild-type and mutant Bruton’s tyrosine kinase-mediated signaling in chronic lymphocytic leukemia

• Published in: Blood cancer journal (New York) Vol. 12; no. 5; pp. 80 - 12
• Main Authors: Aslan, Burcu, Kismali, Gorkem, Iles, Lakesla R., Manyam, Ganiraju C., Ayres, Mary L., Chen, Lisa S., Gagea, Mihai, Bertilaccio, Maria Teresa Sabrina, Wierda, William G., Gandhi, Varsha
• Format: Journal Article
• Language: English
• Published: London Nature Publishing Group UK 20.05.2022; Springer Nature B.V; Nature Publishing Group
• Subjects: 692/308/575; 692/700/565/1436/2185; Agammaglobulinaemia Tyrosine Kinase; Animals; Biomedical and Life Sciences; Biomedicine; Cancer Research; Clinical Studies as Topic; Hematology; Humans; Inhibitor drugs; Kinases; Leukemia, Lymphocytic, Chronic, B-Cell - drug therapy; Leukemia, Lymphocytic, Chronic, B-Cell - genetics; Leukemia, Lymphocytic, Chronic, B-Cell - metabolism; Mice; Mutation; Oncology; Protein Kinase Inhibitors - pharmacology; Protein Kinase Inhibitors - therapeutic use; Signal Transduction

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 to C481 kinase domain mutations. The clinical activity of pirtobrutinib has been demonstrated in CLL, but the mechanism o...