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Solid phase extraction and high-performance liquid chromatographic determination of lazertinib in human plasma
1Department of Medicinal Therapy Research, Education and Research Unit for Comprehensive Clinical Pharmacy, Meiji Pharmaceutical University, Tokyo, Japan.
Abstract:
Lazertinib is a novel third-generation tyrosine kinase inhibitor (TKI) developed for the treatment of epidermal growth factor receptor (EGFR) mutant non-small cell lung cancer (NSCLC). Reports on previous EGFR-TKIs have detailed significant associations between blood drug concentration and efficacy. In addition, significantly elevated blood concentrations of lazertinib have been observed in Asians compared to Caucasians, suggesting the influence of interethnic variability. In this study, we developed and validated a method to determine lazertinib concentrations in human plasma for therapeutic drug monitoring (TDM). Lazertinib and its internal standard, sotorasib, were extracted by solid-phase extraction using an Oasis hydrophilic lipophilic balance cartridge. Chromatographic separation was performed on a reversed-phase column with 0.5% KH2PO4 (pH 4.5) and acetonitrile (52:48, v/v) as the mobile phases in an isocratic elution mode with a flow rate of 1.0 mL/min. The detection wavelength was 296 nm. The calibration curves were linear in the range of 25-2,000 ng/mL, with a coefficient of determination (r2) of 0.9997. The accuracy and precision of all validation experiments were within the criteria set by the Food and Drug Administration guidelines. This study represents the first development and validation of a method for quantifying lazertinib in human plasma. This study is expected to facilitate the widespread use of TDM in studies on lazertinib.
Insights
A new method accurately measures lazertinib drug levels in plasma, crucial for optimizing treatment of EGFR-mutant non-small cell lung cancer (NSCLC) and addressing interethnic variability in drug concentration.
Area of Science:
- Pharmacology
- Analytical Chemistry
- Oncology
Background:
- Lazertinib is a third-generation tyrosine kinase inhibitor (TKI) for EGFR-mutant non-small cell lung cancer (NSCLC).
- Previous EGFR-TKIs show links between blood concentration and efficacy.
- Interethnic differences in lazertinib blood concentration (e.g., Asians vs. Caucasians) are noted.
Purpose of the Study:
- To develop and validate a robust analytical method for quantifying lazertinib in human plasma.
- To enable therapeutic drug monitoring (TDM) for lazertinib treatment.
Main Methods:
- Solid-phase extraction (SPE) using Oasis HLB cartridges for sample preparation.
- Reversed-phase High-Performance Liquid Chromatography (RP-HPLC) with UV detection at 296 nm.
- Method validation according to FDA guidelines for accuracy, precision, and linearity (25–2,000 ng/mL, r²=0.9997).
Main Results:
- A validated method for lazertinib quantification in human plasma was successfully established.
- The method demonstrated high accuracy and precision, meeting regulatory standards.
- Linearity was confirmed across the specified concentration range.
Conclusions:
- This study presents the first validated method for measuring lazertinib plasma concentrations.
- The developed method is suitable for therapeutic drug monitoring (TDM).
- This facilitates further research and clinical application of lazertinib, especially considering interethnic variability.
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