Acalabrutinib structural formula and pharmacological effects

Acalabrutinib) is a Bruton tyrosine kinase inhibitor used to treat mantle cell lymphoma, chronic lymphocytic leukemia (CLL) and small lymphocytic lymphoma. Acalabrutinibis 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.

Acalabrutinib(Acalabrutinib) is an inhibitor of Brutontyrosine kinase(BTK). The molecular formula of acalabrutinib is C26H23N7O2, and its molecular weight is 465.51. The chemical name is4-{ 8-Amino-3-[(2S)-1-(Butan-2-Acenoyl pan>)pyrrolidine-2-yl]imidazo[1,5-a]pyrazine-1-yl)}-N-(pyridine-2-yl)benzamide. The chemical structure of acalabrutinib is as follows:

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The geometric mean absolute bioavailability of acalabrutinib is 25%. For ACP-5862, the median peak acalabrutinib plasma concentration(Tmax) was achieved[Min, Max]Time is 0.9 [0.5, 1.9]hours and 1.6 [0.9, 2.7] hours. 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 effect of acalabrutinib on the QTc interval was evaluated in a randomized, double-blind, double-dummy, placebo and active control, 4-way crossover thorough study in 48 healthy adult subjects. Give a single dose of(44 times the maximum recommended single dose ofac Alabrutinibdoes not prolongQTcinterval to any clinically relevant degree(i.e.≥ 10 ms). Acalabrutinibis dose-proportional, with exposure to acalabrutiniband its active metabolite ACP-5862 ranging from 75 to 250 in patients with B cell malignancies mg increases with increasing doses over the range of ( is the approved recommended single dose of 0.75 to 2.5 times). at100 The geometric mean of the daily plasma drug concentration curve of acalabrutinib over time (AUC24h) and the maximum plasma concentration(Cmax) at the recommended dose of mgtwice daily The values (%Coefficient of variation[CV]) are 1843 (38%) ng/mL and 563 respectively (29%) ng/mL, ACP-5862 respectively3947 (43%) ng/mL and 451 (52%) ng/mL. The cost of generic drugs is about 6,000 to 8,000 per box. If you want to get more high-quality information, you can contact Yaode, and Yaode will do its best to learn more about high-quality overseas drugs for you.

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