Simultaneous quantitation of befotertinib (D-0316) and its metabolite D-0865 in human plasma by LC-MS/MS method

•Determination of befotertinib in human plasma is valuable in assessing its toxicity and efficacy in patients.•A rapid and sensitive quantitative method was established using LC-MS/MS technique and was validated for quantitative analysis of befotertinib in its phase I clinical study.•The method provided good and broad linearity, short runtime, and rapid analysis.