Acalabrutinib is a small-molecule inhibitor of BTK (Bruton’s tyrosine kinase). Acalabrutinib and its active metabolite, ACP-5862, form a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK enzymatic activity. In nonclinical studies, acalabrutinib inhibited BTK-mediated activation of downstream signaling proteins CD86 and CD69 and inhibited malignant B-cell proliferation and tumor growth in mouse xenograft models.
This medicinal substance has been classified in the anatomical therapeutic chemical (ATC) classification according to its main therapeutic use as follows:
Acalabrutinib is the active ingredient of these drugs:
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Medicine agencies around the world have authorized marketing of this active ingredient according to these medication package inserts (MPIs):