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Objective: Optimal therapeutic drug monitoring (TDM), including clinical pharmacokinetics, appropriate interpretation, and dose adjustment of drugs, is required to effectively monitor specific therapeutic drugs. Hospital pharmacists (HPs), being the most qualified healthcare professionals to implement TDM, must understand its applications to determine and adjust drug doses and avoid adverse drug reactions and toxicity. Therefore, in this knowledge, attitude, and practice (KAP) study, we assessed TDM level among HPs in Saudi Arabia. Methods: This cross‐sectional study was conducted with 414 HPs in the Makkah region with a valid pharmacy license from the Saudi Commission for Health Specialties. An overall score of 50% or higher of the total responses in each section was considered good, whereas an overall score lower than 50% was considered poor. Categorical data are expressed as frequency and percentage. Correlations were measured using Pearson's correlation coefficient (r). Results: The TDM‐KAP levels of the participants were 50%, 80%, and 62% for KAP, respectively. Significant positive linear correlations were found between knowledge and attitude, knowledge and practice, attitude and practice, knowledge and classification, practice and classification, practice and experience, and knowledge and experience. The participants showed acceptable knowledge and practice of TDM levels with elevated attitude levels. Conclusion: As a lack of TDM knowledge directly contributes to reduced practice levels, increasing TDM knowledge and practice by introducing more intensive pharmaceutical programs that illustrate TDM clinical applications in hospitals is recommended, which will enhance HP integration. [ABSTRACT FROM AUTHOR]