Enbezotinib

Enbezotinib

Chemical structure of Enbezotinib

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

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

Enbezotinib is primarily used in the treatment of B-cell malignancies, including:

• Chronic lymphocytic leukemia (CLL)
• Mantle cell lymphoma (MCL)
• Waldenström's macroglobulinemia (WM)

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

Common side effects of Enbezotinib include:

• Fatigue
• Nausea
• Diarrhea
• Headache
• Rash

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

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

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.

Related Pages

• Tyrosine kinase inhibitor
• Bruton’s tyrosine kinase
• Chronic lymphocytic leukemia
• Mantle cell lymphoma
• Waldenström's macroglobulinemia