Aumolertinib

A third-generation EGFR tyrosine kinase inhibitor

Aumolertinib
[[File: Chemical structure of Aumolertinib |frameless|220px|alt=|]]
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Drug class	Tyrosine kinase inhibitor
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Aumolertinib, marketed under the brand name Alflutinib, is a tyrosine kinase inhibitor (TKI) used in the treatment of non-small cell lung cancer (NSCLC). It specifically targets the epidermal growth factor receptor (EGFR) with mutations that confer resistance to first- and second-generation EGFR inhibitors.

Mechanism of Action

Aumolertinib is a third-generation EGFR TKI that irreversibly binds to the ATP-binding site of the EGFR tyrosine kinase domain. It is designed to selectively inhibit both the activating EGFR mutations and the T790M resistance mutation, which is a common mechanism of acquired resistance to earlier EGFR inhibitors such as gefitinib and erlotinib.

Clinical Use

Aumolertinib is indicated for the treatment of patients with locally advanced or metastatic NSCLC with EGFR T790M mutation-positive tumors, as detected by an FDA-approved test, who have progressed on or after EGFR TKI therapy. It is administered orally and has shown efficacy in overcoming resistance in patients who have developed the T790M mutation.

Pharmacokinetics

Aumolertinib is well absorbed following oral administration. It undergoes extensive metabolism, primarily by the liver enzyme cytochrome P450 3A4 (CYP3A4). The drug and its metabolites are excreted primarily in the feces, with a minor amount excreted in the urine.

Adverse Effects

Common adverse effects of aumolertinib include diarrhea, rash, dry skin, and paronychia. Serious adverse effects may include interstitial lung disease, hepatotoxicity, and cardiac effects such as QT prolongation. Patients receiving aumolertinib should be monitored for these potential side effects.

Development and Approval

Aumolertinib was developed by Hansoh Pharma and received approval in China for the treatment of EGFR T790M mutation-positive NSCLC. It represents a significant advancement in the management of NSCLC, providing an option for patients who have developed resistance to earlier EGFR-targeted therapies.

Related Pages

• Non-small cell lung cancer
• Epidermal growth factor receptor
• Tyrosine kinase inhibitor
• Gefitinib
• Erlotinib