An ultra-performance LC-MS/MS method for determination of JRF103 in human plasma: application in first in-patient study.

JRF103, a novel pan-HER inhibitor, has shown potent activity against HER1, HER2, HER4 and EGFR . To support its first in-patient trial, a sensitive and rapid method was developed and validated using ultra-performance LC-MS/MS. JRF103 was extracted from plasma using protein precipitation. Extracts were subjected to ultra-performance LC-MS/MS with electrospray ionization. Separation of analyte was achieved using a 1.7-μm C column (2.1 × 50-mm internal diameter) with a gradient elution. The developed method was fully validated following the international guides. The developed method was sensitive, specific and suitable for measuring JRF103 concentration in patients with advanced solid tumors in the first in-patient study of JRF103.