Calcent

Acalabrutinib is a kinase inhibitor indicated for the treatment of adult patients with:

• Mantle cell lymphoma (MCL) who have received at least one prior therapy
• This indication is approved under accelerated approval based on overall response rate Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trials
• Chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL)

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.

Most common adverse reactions (incidence ≥30%) were: anemia, neutropenia, upper respiratory tract infection, thrombocytopenia, headache, diarrhea, and musculoskeletal pain.

Based on findings in animals, Acalabrutinib may cause fetal harm and dystocia when administered to a pregnant woman. There are no available data in pregnant women to inform the drug-associated risk. No data are available regarding the presence of Acalabrutinib or its active metabolite in human milk, its effects on the breastfed child, or on milk production.

Tyrosine Kinase Inhibitor

Do not store above 30⁰C. Keep away from light and out of the reach of children.