Indications
Acalabrutinib is a kinase inhibitor used to treat adults with mantle cell lymphoma (MCL) who have already received at least one prior therapy. This use is approved under accelerated approval, based on overall response rate. Continued approval for MCL may depend on verification and description of clinical benefit in confirmatory trials. Acalabrutinib is also used to treat adults with chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL).
⚠️ Always consult a registered physician before taking any medicine.
Pharmacology
Acalabrutinib is a small-molecule inhibitor of BTK. The medicine and its active metabolite, ACP-5862, form a covalent bond with a cysteine residue in the BTK active site, and this stops the enzyme from working. BTK is a signaling molecule in the B cell antigen receptor (BCR) pathway and in the cytokine receptor pathways. In B cells, BTK signaling switches on the pathways needed for B-cell proliferation, trafficking, chemotaxis and adhesion.
In nonclinical studies, acalabrutinib blocked BTK-mediated activation of the downstream signaling proteins CD86 and CD69. It also inhibited malignant B-cell proliferation and tumor growth in mouse xenograft models.
Pregnancy & Breastfeeding
Pregnancy: Animal findings suggest that Acalabrutinib may cause fetal harm if a pregnant woman takes it. There are no data in pregnant women to show what the risk is. In animal studies, pregnant rabbits given Acalabrutinib during organogenesis had reduced fetal growth. This happened at maternal exposures (AUC) about 4 times the exposure seen in patients taking the recommended dose of 100 mg twice daily. Pregnant women should be told about the potential risk to the fetus. The background risk of major birth defects and miscarriage for the people this medicine is meant for is unknown. Every pregnancy carries a background risk of birth defect, loss or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively.
Lactation: No data are available on whether Acalabrutinib or its active metabolite passes into human milk, what effect it has on a breastfed child, or what effect it has on milk production. Both Acalabrutinib and its active metabolite were found in the milk of lactating rats. Because a breastfed child could have adverse reactions from Acalabrutinib, women who are breastfeeding should be advised not to breastfeed while taking it and for at least 2 weeks after the final dose.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Dosage Reference
⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.
Side Effects & Interactions
Side Effects
No side-effect data recorded yet.