About the functions and efficacy of acalatinib/acalatinib capsules

Acalabrutinib/Acalabrutinib is an oral drug and a second-generation BTK (Bruton's tyrosine kinase) inhibitor. Compared with the first-generation BTK inhibitor ibrutinib, acotinib has some advantages in pharmacological properties. First, acotinib can covalently bind to the Cys481 site in the ATP binding pocket of BTK more strongly and selectively, thereby achieving better targeting effects. Secondly, acotinib has the characteristics of good plasma exposure and rapid oral absorption, allowing the drug to achieve therapeutic effects faster. In addition, the half-life of acotinib is shorter, which is beneficial to reducing side effects and improving drug tolerance

Acotinib has demonstrated effective targeting and good efficacy in the treatment of chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma (SLL) and mantle cell lymphoma (MCL) and other disease models. By selectively inhibiting BTK, acotinib can block signaling pathways and inhibit the growth and proliferation of cancer cells, thereby achieving therapeutic effects.

Compared with ibrutinib, acotinib not only has higher selectivity forBTK, but also inhibits other kinases such as EGFR, TEC and ITK, which makes acotinib more comprehensive in inhibiting the growth of cancer cells. In addition, acotinib needs to be taken twice daily to ensure that the drug binds to BTK to a complete and continuous level (>95% within 24 hours) without increasing the inhibition of other kinases, thereby reducing toxic effects.

The full target coverage of acotinib can reduce drug resistance caused byBTK enzyme mutations and reduce the risk of Richter transformation (which refers to the development of CLL into highly malignant large B-cell lymphoma). Therefore, acotinib has potential efficacy in the treatment of relapsed CLL and other diseases.