Zorifertinib

A tyrosine kinase inhibitor used in cancer treatment

Zorifertinib
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Zorifertinib is a tyrosine kinase inhibitor (TKI) that is primarily used in the treatment of certain types of cancer, particularly non-small cell lung cancer (NSCLC) with specific genetic mutations. It is designed to target and inhibit the activity of the epidermal growth factor receptor (EGFR), which is often overexpressed or mutated in various cancers.

Mechanism of Action

Zorifertinib functions by selectively inhibiting the epidermal growth factor receptor (EGFR) tyrosine kinase. EGFR is a transmembrane protein that, when activated by binding to its specific ligands, triggers a cascade of downstream signaling pathways that promote cell proliferation and survival. In many cancers, mutations in the EGFR gene lead to its constant activation, driving uncontrolled cell division and tumor growth. Zorifertinib binds to the ATP-binding site of the EGFR tyrosine kinase domain, thereby blocking its activity and inhibiting tumor cell proliferation.

Clinical Use

Zorifertinib is primarily indicated for the treatment of patients with advanced or metastatic non-small cell lung cancer (NSCLC) that harbor specific EGFR mutations. These mutations are typically identified through genetic testing of tumor samples. The drug is administered orally and is often used in patients who have developed resistance to first-generation EGFR inhibitors.

Side Effects

Common side effects of Zorifertinib include skin rash, diarrhea, and fatigue. More serious adverse effects can include interstitial lung disease, liver enzyme abnormalities, and cardiac effects. Patients undergoing treatment with Zorifertinib require regular monitoring to manage these potential side effects effectively.

Development and Approval

Zorifertinib was developed as part of ongoing efforts to improve targeted cancer therapies, particularly for patients with specific genetic profiles. Its development involved extensive clinical trials to assess its efficacy and safety in comparison to existing treatments. The drug received regulatory approval after demonstrating significant benefits in progression-free survival in patients with EGFR-mutant NSCLC.

Research and Future Directions

Ongoing research is focused on understanding the mechanisms of resistance to Zorifertinib and developing combination therapies to enhance its efficacy. Studies are also exploring its potential use in other types of cancer with similar genetic mutations.

Related Pages

• Epidermal growth factor receptor
• Non-small cell lung cancer
• Tyrosine kinase inhibitor
• Cancer treatment