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Purpose <p>Lanreotide, a long-acting somatostatin analog, is widely used in the management of acromegaly and neuroendocrine neoplasms. This study aimed to develop an environmentally friendly analytical method for Lanreotide and to identify and characterize its degradation products (DPs). A further objective was to evaluate the structural elucidation of these products using Orbitrap mass spectrometry and assess their potential toxicity.</p> Methods <p>Lanreotide was subjected to ICH-recommended stress conditions, including acidic, basic, oxidative, thermal, and photolytic environments. Chromatographic separation of the resulting DPs was achieved using an X-Select C18 column with gradient elution employing 0.1% formic acid in water and 0.075% formic acid in acetonitrile. High-resolution Orbitrap MS/MS was used for structural elucidation, while toxicity prediction of DPs was performed using CASE Ultra software. The greenness of the developed method was assessed using the Eco-Scale, AGREE, and GAPI metrics.</p> Results <p>Lanreotide exhibited significant degradation under acidic, basic, oxidative, thermal, and visible-light stress conditions, whereas it remained stable under neutral and UV light exposure conditions. Seven new DPs were detected, separated, and structurally characterized by HR-MS/MS. Toxicity assessment revealed no major structural alerts for most products. Greenness evaluations confirmed strong environmental sustainability of the developed method.</p> Conclusion <p>The developed green analytical method provides a reliable approach for routine batch analysis of Lanreotide in bulk and dosage forms, even in the presence of DPs. The insights generated also support improved storage and stability management for manufacturers.</p> Graphical Abstract <p>x</p>

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High-Resolution LC–MS Approach for Structural Elucidation and (Q)SAR-Based Toxicity Assessment of Cyclic Peptide Lanreotide Acetate Degradation Products

  • 期刊论文

  • 发表日期：

    2026年2月1日

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  • Sachin Chaturvedi,
  • Raju Choudhary,
  • Nitish Sharma

摘要

Purpose

Lanreotide, a long-acting somatostatin analog, is widely used in the management of acromegaly and neuroendocrine neoplasms. This study aimed to develop an environmentally friendly analytical method for Lanreotide and to identify and characterize its degradation products (DPs). A further objective was to evaluate the structural elucidation of these products using Orbitrap mass spectrometry and assess their potential toxicity.

Methods

Lanreotide was subjected to ICH-recommended stress conditions, including acidic, basic, oxidative, thermal, and photolytic environments. Chromatographic separation of the resulting DPs was achieved using an X-Select C18 column with gradient elution employing 0.1% formic acid in water and 0.075% formic acid in acetonitrile. High-resolution Orbitrap MS/MS was used for structural elucidation, while toxicity prediction of DPs was performed using CASE Ultra software. The greenness of the developed method was assessed using the Eco-Scale, AGREE, and GAPI metrics.

Results

Lanreotide exhibited significant degradation under acidic, basic, oxidative, thermal, and visible-light stress conditions, whereas it remained stable under neutral and UV light exposure conditions. Seven new DPs were detected, separated, and structurally characterized by HR-MS/MS. Toxicity assessment revealed no major structural alerts for most products. Greenness evaluations confirmed strong environmental sustainability of the developed method.

Conclusion

The developed green analytical method provides a reliable approach for routine batch analysis of Lanreotide in bulk and dosage forms, even in the presence of DPs. The insights generated also support improved storage and stability management for manufacturers.

Graphical Abstract

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