Drug intelligence / Profile preview

Lastet + Aumolertinib combination

Development stage
Unknown
Lead developer
Hansoh Pharmaceutical Group
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding 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[6]. 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[1][2].\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[2].\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[8]. 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[2].\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[5][7].\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

EGFR T790M (Epidermal growth factor receptor T790M mutant)ABCB1 (P-glycoprotein)TOP2A (DNA topoisomerase II)

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