Acalabrutinib (2 brand names, 1 dosage form, 1 route)
Available dosage forms: CAPSULE.
Routes of administration: ORAL.
Brand Names
- ACALABRUTINIB
- CALQUENCE
Contraindications
None.
Adverse Reactions
The following clinically significant adverse reactions are discussed in greater detail in other sections of the labeling: •Serious and Opportunistic Infections [see Warnings and Precautions (5.1) ] •Hemorrhage [see Warnings and Precautions (5.2) ] •Cytopenias [see Warnings and Precautions (5.3) ] •Second Primary Malignancies [see Warnings and Precautions (5.4) ] •Cardiac Arrhythmias [see Warnings and Precautions (5.5) ] •Hepatotoxicity, including DILI [see Warnings and Precautions (5.6) ]
Mechanism of Action
Acalabrutinib is a small-molecule inhibitor of BTK. 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. BTK is a signaling molecule of the B cell antigen receptor (BCR) and cytokine receptor pathways. In B cells, BTK signaling results in activation of pathways necessary for B-cell proliferation, trafficking, chemotaxis, and adhesion. 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.