Lead as a toxic environmental metal has been an issue of concern for 30-40 years. Even though the exposures experienced by the general public have been significantly reduced, so have the acceptable blood lead concentrations assessed to safeguard health (specifically of children). The impact of these concurrent changes are reviewed and discussed in terms of the following: blood lead as the primary biomarker of exposure; pertinent toxicokinetic issues including modelling; legacy and newer sources of this toxic metal; improvements in lead quantification techniques and its characterization (chemical forms) in exposure media; and in vivo markers of lead sources. It is concluded that the progress in the quantification of lead and its characterization in exposure media have supported the efforts to identify statistical associations of lead in blood and tissues with adverse health outcomes, and have guided strategies to reduce human exposure (especially for children). To clarify the role of lead as a causative factor in disease, greater research efforts in biomarkers of effect and susceptibility seem timely.