Detailed explanation of the functions and efficacy of acalatinib/acalatinib capsules

Acalabrutinib/Acalabrutinib is a drug used to treat malignant tumors and belongs to a class of drugs called BTK inhibitors. BTK is a protease in the body that participates in the regulation of B cell signal transduction pathways. Acotinib inhibits the proliferation and viability of cancer cells by inhibiting the activity of BTK. Acotinib is primarily used to treat adults with certain types of non-Hodgkin lymphoma (including small cell lymphoma and mantle cell lymphoma) and chronic lymphocytic leukemia. It is often used as a maintenance treatment option when other treatments fail to control disease progression or have failed.

Bruton's tyrosine kinase (BTK) is a signaling molecule in the B cell antigen receptor and cytokine receptor pathways. This BTK signaling activates pathways necessary for B cell proliferation, trafficking, chemotaxis, and adhesion. Acotinib is a small molecule inhibitor of BTK. Acotinib and its active metabolite ACP-5862 form covalent bonds with the cysteine u200bu200bresidue (Cys481) in the active site of BTK, thereby inhibiting BTK enzyme activity. Therefore, acotinib inhibits BTK-mediated activation of downstream signaling proteins CD86 and CD69, ultimately inhibiting malignant B cell proliferation and survival.

Ibrutinib is generally considered a first-in-class BTK inhibitor, and acotinib is considered a second-generation BTK inhibitor, mainly because it has higher selectivity and inhibitory effect on the targeting activity of BTK, while having higher IC50 or almost no inhibitory effect on the kinase activities of ITK, EGFR, ERBB2, ERBB4, JAK3, BLK, FGR, FYN, HCK, LCK, LYN, SRC and YES. In fact, acotinib is rationally designed to be more potent and selective than ibrutinib, while theoretically exhibiting fewer side effects because the drug's off-target effects are minimized.