Drug intelligence / Profile preview

Lastet + Aumolertinib combination

Development stage
Unknown
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

The combination of Lastet (also known as etoposide capsules) and aumolertinib is being investigated for the treatment of EGFR-positive non-small cell lung cancer (NSCLC). This combination therapy is currently being studied in clinical trials, particularly for patients with EGFR mutations.\n\nAumolertinib (formerly known as almonertinib) is a third-generation EGFR tyrosine kinase inhibitor that selectively targets both EGFR-sensitizing mutations and the T790M resistance mutation. It was recently approved by the MHRA (UK) on June 3, 2025, for treating NSCLC in patients with EGFR mutations. Aumolertinib works by blocking EGFR, which may help slow or stop lung cancer growth and potentially reduce tumor size.\n\nLastet (oral etoposide) is administered in a specific dosing regimen - typically 25-50 mg/day orally in a 28-day cycle, with two weeks of continuous administration followed by two weeks off.\n\nThe combination is being studied in clinical trials such as the EVOLUTION trial, a multicentre Phase II clinical trial conducted across three tertiary hospitals in China. This trial is enrolling patients with locally advanced or metastatic lung cancer harboring EGFR-sensitive mutations who haven't previously undergone systemic therapy.\n\nAccording to the search results, aumolertinib selectively inhibits the transport function of ABCB1 (MDR1/p-glycoprotein), suppressing drug efflux and potentially restoring sensitivity to chemotherapy agents in multidrug-resistant cancer cells. This provides a theoretical basis for combining conventional cytotoxic anticancer drugs like Lastet with aumolertinib.\n\nThe primary endpoint in the EVOLUTION trial is progression-free survival, with secondary endpoints including overall survival, objective response rate, disease control rate, and duration of response.\n\nAumolertinib as a single agent has shown promising efficacy with a favorable safety profile compared to first-generation EGFR TKIs like gefitinib, with lower incidence of rash and diarrhea.\n\nThe combination therapy is currently in Phase II clinical development for EGFR-positive non-small cell lung cancer.

Other names
Etoposide + AumolertinibEtoposideAlmonertinib
02

Targets

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