Human biological monitoring is a powerful tool for scientists, policy makers, and occupational health‐care professionals, such as physicians and occupational hygienists, to assess and manage health risks associated with chemical exposures among the general population as well as at the workplace. This chapter will focus on using biological monitoring in occupational exposure assessments. It includes biological monitoring sampling strategies and practical approaches. Relevant biomarkers used in biomonitoring are derived based on fundamental understanding of absorption, distribution, metabolism, and excretion (ADME) of chemicals. Therefore, ADME will be discussed along with toxicokinetics and toxicodynamics. Individual susceptibility is a topic associated with biological monitoring as opposed to air monitoring. Monitoring variability associated with air and biological monitoring is compared. The biomonitoring strategy choice is dependent on the purpose, selected biomarker, matrix (urine, blood, saliva, hair, exhaled breath, exhaled breath condensate), sampling time, which is determined based on the selected biomarkers apparent elimination half‐life, and variability but also on the purpose of the biomonitoring program. Biological limit values are established on available scientific data. Their historic development and concepts are country specific. Biomonitoring of metals and inorganic compounds as well as organic compounds are extensively covered. Emerging biomarker fields as well as new chemical analytical methods are briefly discussed. Future trends in human biological monitoring are discussed as it is a current topic in public health policies, in occupational and environmental health and in science in general.