Enbezotinib
Enbezotinib[edit | edit source]
Enbezotinib is a tyrosine kinase inhibitor (TKI) used in the treatment of certain types of cancer. It is specifically designed to target and inhibit the activity of the Bruton’s tyrosine kinase (BTK), which plays a crucial role in the signaling pathways that regulate the growth and survival of B cells.
Mechanism of Action[edit | edit source]
Enbezotinib functions by binding to the active site of BTK, thereby preventing its activation. This inhibition disrupts the downstream signaling pathways that are essential for the proliferation and survival of malignant B cells. By blocking BTK, Enbezotinib effectively induces apoptosis in these cancerous cells, leading to a reduction in tumor growth.
Clinical Applications[edit | edit source]
Enbezotinib is primarily used in the treatment of B-cell malignancies, including:
These conditions are characterized by the overproduction of abnormal B cells, and Enbezotinib helps to manage these diseases by targeting the BTK pathway.
Side Effects[edit | edit source]
Common side effects of Enbezotinib include:
More serious adverse effects can include cytopenias, infections, and cardiac arrhythmias. Patients undergoing treatment with Enbezotinib require regular monitoring to manage these potential complications.
Pharmacokinetics[edit | edit source]
Enbezotinib is administered orally and is absorbed through the gastrointestinal tract. It undergoes hepatic metabolism, primarily via the cytochrome P450 enzyme system, and is excreted in both urine and feces. The drug has a half-life that allows for once-daily dosing, which is convenient for patients.
Development and Approval[edit | edit source]
Enbezotinib was developed as part of a new generation of BTK inhibitors, designed to improve upon the efficacy and safety profiles of earlier drugs in this class. It has undergone extensive clinical trials to establish its effectiveness and safety in treating B-cell malignancies.
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