Preclinical pharmacokinetics plays an important role in the Drug Discovery and Development process. Regulatory agencies require preclinical pharmacokinetic data to assess the efficacy and safety of new candidates before their approval for clinical trials.

Pharmacokinetics assessment is present throughout all the stages of the drug development process. Preclinical pharmacokinetics helps, among others, screen out compounds, understand the relationship between the pharmacological activity and exposure in plasma and tissue of action, identify the dosage range that achieves therapeutic levels while minimizing the risk of toxicity, and predict human pharmacokinetics.

Experiments can be designed for initial pharmacokinetic screening of compounds, renal excretion, in vivo tissue distribution or for assessment of the influence of different variables (dose, formulation, sex, food) at later stages.