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Second-generation BTK inhibitors in CLL

Thursday, August 3, 2017

Richard R. Furman, M.D., the Morton Coleman, M.D. Distinguished Associate Professor of Medicine, Joan and Sanford I. Weill Department of Medicine, Weill Cornell Medicine/NewYork-Presbyterian Hospital, spoke to OncLive about second-generation BTK inhibitors, such as acalabrutinib and BGB-3111 in chronic lymphocytic leukemia (CLL).

BGB-3111 and acalabrutinib are second-generation BTK inhibitors with some interesting differences between the 2 of them, Furman explains. Studies show that there have been sustained serum levels far more with BGB-3111 versus acalabrutinib. Acalabrutinib has a very short half-life that lasts approximately 30 minutes. Additionally, it is only due to the covalent bond that it is able to have 24-hour coverage that sees any benefit.

Researchers are unsure whether or not both drugs have certain advantages over the other. Both do have less EGFR inhibition than ibrutinib (Imbruvica), which Furman says affords a benefit in terms of diminished risk of diarrhea, rash, and other adverse events.