Is Acalabrutinib developed and manufactured by AstraZeneca?

Acalabrutinib is developed and produced by the American pharmaceutical company AstraZeneca (AstraZeneca). Acalabrutinib was approved by the USFDA in 2017. Acalabrutinib is suitable for the treatment of adults with mantle cell lymphoma who have received at least one previous treatment. (MCL) and the treatment of adult chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL).

Acalabrutonis a Brutontyrosine kinase inhibitor that prevents B cell proliferation, trafficking, chemotaxis, and adhesion. Dosing every 12 hours may cause other effects such as atrial fibrillation, other malignancies, cytopenias, bleeding, and infection. Acalatinib is a small molecule inhibitor of BTK. Acalabrutiniband its active metabolite ACP-5862 both form covalent bonds with the cysteine u200bu200bresidue (Cys481) in the BTK active site, thereby inhibiting the enzyme activity of BTK. Therefore, acalatinibinhibits BTK-mediated activation of downstream signaling proteins CD86 and CD69, ultimately inhibiting malignant B cell proliferation and survival.

The reversible binding rate of acalabrutinib to human plasma proteins is approximately 97.5%. The average blood-to-plasma ratio in vitro is about0.7. Experiments at physiological concentrations in test tubes show that acalabrutinib can bind to human serum albumin by 93.7% and to α-1-acidic glycoprotein by 41.1%. Acalabrutinibis mainly metabolized byCYP3Aenzyme. ACP-5862 was identified as the major active metabolite in plasma, with a geometric mean exposure (AUC) of approximately2-3 times of the containing amount of acalabrutinib. ACP-5862 is approximately 50% less potent than acalabrutinib in inhibiting BTK. If you want to get more high-quality information, you can contact Yaode, and Yaode will do its best to help you learn more about high-quality overseas drugs.