Aumolertinib: A Review in Non-Small Cell Lung Cancer

Aumolertinib (formerly almonertinib; Ameile(R)) is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (EGFR-TKI) that is selective for mutant EGFR over wild-type EGFR. It has been developed for the treatment of advanced EGFR mutation-positive non-small cell lung cancer (NSCLC). In the phase 3 AENEAS trial conducted in Chinese patients, aumolertinib as first-line treatment significantly prolonged progression-free survival (PFS) and duration of response (DoR) compared with gefitinib in patients with advanced EGFR mutation-positive NSCLC; overall survival (OS) data from this study are immature. In the phase 1/2 APOLLO trial, aumolertinib showed good clinical activity (based on objective response rate, PFS, DoR and OS) in Chinese patients with locally advanced or metastatic EGFR T790M mutation-positive NSCLC who had progressed on or after prior EGFR-TKI therapy. Aumolertinib has a generally manageable tolerability profile; adverse events associated with wild-type EGFR inhibition (e.g. rash and diarrhoea) were less frequent with aumolertinib than gefitinib in AENEAS. Thus, aumolertinib is a promising new option for both first-line and second-line treatment in patients with advanced EGFR mutation-positive NSCLC. Plain Language Summary Non-small cell lung cancer (NSCLC), the most common type of lung cancer, is associated with a poor prognosis. In up to 50% of Asian patients and approximate to 17% of Caucasian patients with NSCLC, specific mutations in the epidermal growth factor receptor (EGFR) gene are responsible for tumour growth. Drugs that block the effects of EGFR [known as EGFR tyrosine kinase inhibitors (EGFR-TKIs)] improve survival in patients with NSCLC and EGFR mutations. Aumolertinib (Ameile(R)) is a third-generation EGFR-TKI that has been developed in China. When given to patients with previously untreated, advanced EGFR mutation-positive NSCLC, aumolertinib delayed cancer progression by approximate to 9 months compared with gefitinib, a first-generation EGFR-TKI. Aumolertinib also showed good clinical activity as a second-line treatment in patients with advanced EGFR mutation-positive NSCLC who had developed resistance during or after treatment with earlier-generation EGFR-TKIs. Overall, the tolerability profile of aumolertinib was similar to that of gefitinib, with some adverse events such as rash and diarrhoea being less frequent. Aumolertinib is a promising new first- or second-line treatment option in patients with advanced EGFR mutation-positive NSCLC.