Simultaneous quantitation of abiraterone, enzalutamide, N-desmethyl enzalutamide, and bicalutamide in human plasma by LC-MS/MS.

ABSTRACT: Inhibiting the androgen receptor (AR) pathway is an important clinical strategy in metastatic prostate cancer. Novel agents including abiraterone acetate and enzalutamide have been shown to prolong life in men with metastatic, castration-resistant prostate cancer (mCRPC). To evaluate the pharmacokinetics of AR-targeted agents, we developed and validated an LC-MS/MS assay for the quantitation of enzalutamide, N-desmethyl enzalutamide, abiraterone and bicalutamide in 0.05mL human plasma. After protein precipitation, chromatographic separation was achieved with a Phenomenex Synergi Polar-RP column and a linear gradient of 0.1% formic acid in methanol and water. Detection with an ABI 4000Q mass spectrometer utilized electrospray ionization in positive multiple reaction monitoring mode. The ass

SUBMITTER: Kim KP 

PROVIDER: S-EPMC5357460 | biostudies-literature | 2017 May

REPOSITORIES: biostudies-literature