Gene Accession

Q06187

Gene Alias

Protein names Recommended name Tyrosine-protein kinase BTK EC number EC:2.7.10.2 (UniProtKB | ENZYME | Rhea) Alternative names Agammaglobulinemia tyrosine kinase (ATK) B-cell progenitor kinase (BPK) Bruton tyrosine kinase Gene names Name BTK Synonyms AGMX1, ATK, BPK

Background

Acalabrutinib (A) is a selective, second-generation irreversible Bruton's Tyrosine Kinase inhibitor (BTKi) that has shown outstanding clinical activity in chronic lymphocytic leukemia (CLL) and other hematologic malignancies. Acquired resistance to the first-generation BTKi, ibrutinib (I), is mediated most commonly by C481S mutations in BTK, which decrease binding affinity and change binding from irreversible to reversible.