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





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