Role of placental ATP-binding cassette (ABC) transporters in antiretroviral therapy during pregnancy

Highly active anti-retroviral therapy (HAART) is used to treat HIV-infected patients and involves administration of multiple antiretroviral drugs acting at different steps of the HIV life cycle. In treating HIV-infected pregnant patients, the aim of therapy is not only to treat the mother but also to prevent the transmission of the virus to the fetus. Among the antiretroviral drugs used, there are differences in the extent of transfer of these drugs across the placenta; HIV protease inhibitors are particularly poorly transferred. Activities of ABC transporters expressed in the human placenta as well as differences in plasma protein binding may account for the poor transplacental transfer of certain drugs. This review discusses factors affecting the extent of placental transfer of antiretroviral drugs during pregnancy. These issues may also apply to drugs in other therapeutic categories. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:2317-2335, 2009