A package of toxicokinetic and disposition studies is generally conducted in support of reproductive toxicology studies in the development of new drugs. The content of the package often varies between companies and sometimes either insufficient data or inappropriate/over-interpreted data are presented. This paper was written to aid investigators in the design of toxicokinetic and disposition studies in support of reproductive toxicology. It offers: (1) an overview on the regulatory guidelines for toxicokinetics, (2) methods for the derivation of toxicokinetic parameters, (3) suggestions on general toxicokinetic study design, (4) suggestions on the specific design of toxicokinetic support for reproductive toxicology studies, and (5) an overview of species differences in placental transfer and the applicability (or otherwise) of transfer studies in drug development. Toxicokinetic and drug disposition studies should be carefully designed in order to gather relevant information, and consideration should be given to the usefulness of any data before embarking on a series of supporting or routine experiments.