What is the mechanism of action of acalabrutinib?

Acalabrutinib is an orally active, irreversible and highly selective second-generation drugBTK inhibitor. Acalabrutinibis suitable for patients with mantle cell lymphoma(MCL)who have received ≥1 treatments in the past span>, also suitable for the treatment of chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL).

Acalabrutini(Acalabrutinib)What is its mechanism of action?

Acalabrutinib is a small molecule inhibitor of BTK. Acalabrutiniband its active metabolite ACP-5862 form covalent bonds with the cysteine u200bu200bresidues in the BTK active site, resulting in the inhibition of BTK enzyme activity. BTKis a signaling molecule for the Bcell antigen receptor(BCR) and cytokine receptor pathways. In B cells, BTK signaling leads to the activation of pathways necessary for B cell proliferation, trafficking, chemotaxis, and adhesion. In nonclinical studies, acalabrutinib inhibits BTK-mediated activation of downstream signaling proteins CD86 and CD69 and suppresses malignant B cell proliferation and tumor growth in mouse xenograft models. In patients with Bcell malignancies, steady-state median BTK occupancy in peripheral blood was maintained at ≥ 95%over 12 hours, resulting in BTK being inactivated throughout the recommended dosing interval.The geometric mean absolute bioavailability of acalabrutinib is 25%. For ACP-5862, the median [minimum, maximum]time to peak acalabrutinib plasma concentration(Tmax) is 0.9 [0.5, 1.9] hours and 1.6 [0.9, 2.7] hours. Generic drugs cost about six to seven thousand per box. 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.