Aim The guideline is meant to standardize the principles, procedures, and methods for developing therapeutic drug monitoring (TDM) guidelines and promoting open, transparent, scientific, and credible TDM guidelines. Methods Division of Therapeutic Drug Monitoring, Chinese Pharmacological Society established guideline working groups, declared and managed conflicts of interest. The guideline working groups used the Delphi method to formulate the purpose and scope of the guidelines and questions in the PICO format, searched and synthesized evidence, and integrated with the current situation in China and TDM characteristics to preliminarily develop recommendations for the guideline for TDM guideline development in China. Through internal discussions of the guideline working groups and external peer review, the content was improved, and we eventually formulated a guideline suitable for guiding TDM-related guidelines. Results The guideline provides suggestions for problems to be identified and solved in the planning, development, publishing, and updating stages of TDM guidelines, including forming guideline working groups, planning guidelines, declaration and management of interests, formulating questions and selecting outcomes, preparing the planning proposal, evidence retrieval and synthesis, evidence assessment, developing recommendations, drafting guidelines, external review guidelines, publishing and disseminating guidelines, postevaluation of guidelines, and updating guidelines. Conclusions This guideline can provide methodological guidance and reference for the development of TDM guidelines.