Aim: Naloxegol is an oral peripherally acting μ-opioid receptor antagonist approved for the treatment of opioid-induced constipation. Sensitive, robust, bioanalytical methods were required to quantitate naloxegol in human biological matrices as part of the clinical development program. Methodology/results: Analytical plasma samples were prepared using Solid Phase Extraction (SPE) coupled with concentration. The method’s linearity was established at 0.1–50 ng/ml with up to 100-fold dilution. Urine samples were analyzed directly postdilution; dialysate samples were extracted by supported liquid extraction. Sensitive liquid chromatography/mass spectrometry (LC–MS/MS) assays were developed and validated, and demonstrated acceptable precision, accuracy and selectivity for naloxegol in the appropriate matrices. Conclusion: Methods for quantifying naloxegol in human biological matrices have been successfully validated.
Keywords:
- clinical
- LC–MS
- naloxegol