Gumarontinib

A third-generation EGFR inhibitor used in cancer treatment

Gumarontinib
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Gumarontinib is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) used in the treatment of certain types of non-small cell lung cancer (NSCLC). It is specifically designed to target and inhibit the activity of the EGFR with the T790M mutation, which is a common mechanism of resistance to first- and second-generation EGFR inhibitors.

Mechanism of Action

Gumarontinib works by selectively binding to the mutated form of the EGFR, particularly the T790M mutation, which is often responsible for acquired resistance in patients who have been treated with earlier generation EGFR inhibitors. By inhibiting the kinase activity of the mutated receptor, gumarontinib effectively blocks the downstream signaling pathways that promote cancer cell proliferation and survival.

Clinical Use

Gumarontinib is indicated for the treatment of patients with metastatic NSCLC who have developed resistance to previous EGFR TKI therapy due to the T790M mutation. It is administered orally and has shown efficacy in shrinking tumors and prolonging progression-free survival in clinical trials.

Pharmacokinetics

Gumarontinib is absorbed orally and undergoes hepatic metabolism. It has a half-life that allows for once-daily dosing, which is convenient for patients. The drug is primarily excreted through the feces, with a smaller portion eliminated via the urine.

Side Effects

Common side effects of gumarontinib include diarrhea, rash, nausea, and fatigue. More serious adverse effects can include interstitial lung disease, hepatotoxicity, and cardiac effects. Patients are monitored regularly to manage these potential side effects.

Development

Gumarontinib was developed as part of an effort to overcome resistance mechanisms in EGFR-mutant NSCLC. Its development involved extensive research into the structure and function of the EGFR and the mutations that confer drug resistance.

Related Pages

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