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Abstract

Aim: Aur0101 is a cytotoxic and small-molecule microtubule depolymerizing agent, and is the payload conjugated to antibody–drug conjugate PYX-201. Developing and validating a sensitive bioanalytical method to quantitate Aur0101 was novel and crucial in preclinical PYX-201 studies. Materials & methods: Reference standard Aur0101 and its stable isotope labelled internal standard Aur0101-d8 were used in this LC–MS/MS method. Results: This sensitive assay was validated at a lower limit of quantitation of 15 pg/ml and successfully applied to support preclinical rat and monkey toxicology studies. Preclinical plasma toxicokinetic parameters were presented. Conclusion: A sensitive and robust LC–MS/MS assay was validated for Aur0101 in rat and monkey plasma.

Keywords:

  • ADC
  • Aur0101
  • LC–MS/MS
  • microtubule inhibitor
  • oncology
  • preclinical
  • small molecule
  • toxicokinetic
  • validation
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