Aim: GW788388 is a selective and orally active TGF-β1 receptor inhibitor that shows potent activity in renal fibrosis. We aimed to establish and validate a simple and sensitive ultra-performance LC-MS/MS method for the determination of GW788388 in plasma samples. Methodology & results: GW788388 in rat plasma was processed with protein precipitation method and then separated on a C18 column. The calibration curve presented a good linearity in the range of 1.0-1200 ng/ml, with satisfactory accuracy (relative error, [-17.5% < relative error <11.7%) and precision (CV <8.9%) for all quality control samples. After oral administration, GW788388 was absorbed quickly and reached a peak concentration of 595.3 ± 60.2 ng/ml after 20 min. Conclusion: The validated method provides a quantification method of GW788388 in rat plasma in detail, and can be utilized to successfully describe the pharmacokinetic profile of GW788388.
Keywords: GW788388; UPLC–MS/MS; pharmacokinetics.