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The other way of classifying drug transporters is from a pharmacodynamic or pharmacokinetic point of view. In such a classification, the transporter that transfers its substrates into the systemic blood circulation is called an absorptive transporter, whereas the transporter that excretes its substrates from the blood circulation into bile, urine, or the gut lumen is known as a secretory transporter. However, when absorptive or secretory transporters in the blood‐brain‐barrier and placenta are discussed, the definition needs to be modified. The brain and fetus have been traditionally considered as two “isolated” compartments in the human body. In drug therapy, many strategies have been utilized to achieve either enhanced or reduced penetration of drugs into these two compartments. Conventionally, the transporters facilitating drug penetration into the brain or fetus are referred to absorptive transporters.