Administration of antiviral drugs to pregnant women with influenza, human immunodeficiency virus (HIV), and herpes simplex virus (HSV) infections is widely accepted as an effective treatment to safeguard the health of the mother and fetus. This review deals with the transfer of antiviral drugs to the fetus across the placental barrier, which is formed by an epithelial layer of syncytiotrophoblasts. First, the structure, function, and developmental change of the placenta and the placental barrier are briefly presented. We then review the transplacental permeability of antiviral drugs, such as oseltamivir for influenza, antiretrovirals (e.g., zidovudine, didanosine, and saquinavir) for HIV, and acyclovir for HSV, focusing on the involvement of ATP-binding cassette, organic anion/cation, and nucleoside transporters. The increasing evidence that is becoming available about transport mechanisms operating at the placental barrier is expected to be useful in the development of techniques to control fetal and placental transfer of antiviral drugs, and thereby to obtain maximum therapeutic benefit while minimizing potential fetal toxicity.
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