Acalabrutinib Powder is an experimental anticancer drug that is a selective inhibitor of Bruton's tyrosine kinase (BTK). This kinase transmits signals from the B cell receptor (BCR), so any inherited BTK mutation will lead to B cell immunodeficiency. Therefore, BTK inhibitors targeting B cell signaling have shown great promise in treating chronic lymphocytic leukemia (CLL).
Acamprosate is a drug used to treat alcohol dependence.
The following is the preparation method of acalabrutinib:
1. The main raw materials for synthesizing acalabrutinib are alanine (L-proline) and acetamide
(acetic anhydride).
2. First, react acetyl-L-prolinc with acetamide in a solvent to produce N-acetylactine (N-acctyl-L-prolinc).
3. React N-acetylalanine with ammonia to produce acetylalanine (acetyl-L-proline).
4. React acetylalanine with butyl isocyanate under alkaline conditions to produce acetylalanine isocyanate butyl ester (acetyl-L-proline-4-butyl ester).
5. React acetylalanine isocyanate butyl ester with n-butanol under alkaline conditions to produce acalabrutinib.
6. Acalabrutinib can be obtained in pure form through steps such as crystallization and purification.
Acalabrutinib is a second-generation small molecule Bruton's tyrosine kinase inhibitor. Acalabrutinib and its metabolite ACP-5862 form a covalent bond with the 481st cysteine residue in the BTK active site, inhibiting the activity of the BTK enzyme; and BTK is a signaling molecule for the B cell antigen receptor and cytokine receptor channels. In B cells, the activation of BTK signaling is a channel signal necessary to promote B cell proliferation, transport, chemotaxis and adhesion. Acalabrutinib and its metabolites selectively block the BTK pathway without destroying other molecular pathways important for platelets and immune function, thereby avoiding or reducing the occurrence of adverse reactions related to cancer therapy.
1. Common dose for adult lymphoma: 100 mg orally every 12 hours until disease progression or unacceptable toxicity occurs.
2. Common dose for adult leukemia:
3. Monotherapy: 100 mg orally every 12 hours until disease progression or unacceptable toxicity occurs.
4. Combination with obinutuzumab:
1) 100 mg orally every 12 hours until disease progression or unacceptable toxicity occurs;
2) Start using the drug in the first cycle (each cycle is 28 days);
3) Start using obinutuzumab in the second cycle for a total of 6 cycles, and refer to the dose recommended in the prescribing information of obinutuzumab, and administer acalabrutinib before taking obinutuzumab on the same day.
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