Description

• General description: A stable-labeled internal standard for the immunosuppressant Everolimus, marketed as Zortress® and Certican for use in organ transplantation and Afinitor® for treatment of kidney and pancreatic cancers. Clinical laboratories quantitate everolimus levels in patient whole blood samples using LC-MS/MS. While many everolimus LC-MS/MS methods use 32-desmethoxyrapamycin or ascomycin as an internal standard, higher levels of variability / lower levels of reproducibility may occur in the analysis along with the potential for interferences. Use of a stable-labeled analog of everolimus is the best choice to minimize variability or mitigate any potential interference in LC-MS/MS analysis.
• Application: Quantitative Bioanalysis in Therapeutic Drug Monitoring: Everolimus-D₄ is utilized as an internal standard in LC-MS/MS methods for the quantification of everolimus, highlighting its application in the pharmacokinetic studies of mTOR inhibitors. This method ensures accuracy and precision in therapeutic drug monitoring, crucial for optimizing dosages in cancer treatments and immunosuppressive therapies (Heideloff et al., 2013).Multi-Drug Analysis in Transplantation Medicine: The use of Everolimus-D₄ as a deuterated internal standard supports ultra-fast liquid chromatography-tandem mass spectrometry methods for simultaneously measuring multiple immunosuppressants in whole blood. This technique is vital for managing drug interactions and therapeutic levels in patients undergoing organ transplantation, which involves targeted therapy and mTOR inhibitors (Meinitzer et al., 2010).
• Legal Information: Afinitor is a registered trademark of Novartis AG