Acalabrutinib

acalabrutinib (uh-KA-luh-BROO-tih-nib) is a drug used to treat mantle cell lymphoma in patients who have already received at least one other treatment. It is also being studied in the treatment of other types of cancer. Acalabrutinib blocks a protein called Bruton’s tyrosine kinase (BTK) , which may help keep cancer cells from growing. It is a type of tyrosine kinase inhibitor. Also called Calquence.

Information about Acalabrutinib

Acalabrutinib is an oral inhibitor of Bruton’s tyrosine kinase that is used in the therapy of B cell malignancies including refractory mantle cell lymphoma.   

Liver safety of Acalabrutinib

Acalabrutinib has not been associated with serum enzyme elevations during therapy or with cases of idiosyncratic acute liver injury, but has been linked to cases of reactivation of hepatitis B. 

Mechanism of action of Acalabrutinib

Acalabrutinib (a kal" a broo' ti nib) is an orally available, small molecule inhibitor of Bruton’s tyrosine kinase (BTK), which is an essential component in the B cell receptor signaling pathway.  Inhibition of this pathway prevents B cell activation, differentiation and proliferation.  Deficiency of BTK is the cause of X linked (Bruton’s) agammaglobulinemia, and B cell receptor signaling through BTK has been shown to be critical for proliferation and survival of malignant B lymphocytes in mantle cell lymphoma and CLL.  Unlike ibrutinib, another BTK inhibitor, acalabrutinib has a high degree of specificity for BTK and has little or no activity against EGFR and other tyrosine kinases. 

FDA approval information for Acalabrutinib

Acalabrutinib was approved for use in the United States as therapy for refractory mantle cell lymphoma in 2017 and is under evaluation in other malignancies such as CLL, pancreatic and non-small cell lung cancer. 

Dosage and administration for Acalabrutinib

Acalabrutinib is available in capsules of 100 mg under the brand name Calquence.  The recommended dose is 100 mg once daily. 

Side effects of Acalabrutinib

Side effects are common, but usually mild-to-moderate in severity; they include myelosuppression, fatigue, diarrhea, nausea, vomiting, anorexia, constipation, peripheral edema, dyspnea, headache, arthralgia, myalgia, rash and fever.  Uncommon, but potentially serious side effects include severe bone marrow suppression, infections, bleeding, tumor lysis syndrome and renal toxicity.

 

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