Mother-to-child transmission (MTCT) of the human immunodeficiency virus (HIV) is a global problem. HIV can be transmitted from mother-to-child at various stages of pregnancy including in utero, intrapartum and during breastfeeding. A number of interventions have, therefore, been aimed at effectively providing alternatives to breastfeeding and limiting the risk of newborn infection during delivery, by using caesarian section as the mode of delivery and administering antiretroviral (ARV) drugs prepartum and peripartum. However, these approaches are not always possible in developing countries and the use of ARV drugs, in particular nevirapine, zidovudine and zidovudine/lamivudine, have been investigated in both developing countries and developed countries. The studies have involved the administration of various ARV prophylaxis regimens to HIV-infected pregnant women perinatally, either as monotherapy or in various combinations. In some studies, infants have also received ARV prophylaxis. Although studies have enrolled different populations and utilized various ARV drugs and regimens, encouraging reductions in the MTCT rates have been reported. These interventions have raised concerns regarding the development of ARV-resistant HIV strains. Mutations that confer resistance to nevirapine have been detected in pregnant women who received this drug, but the emergence of these mutations was not associated with an increased risk of transmission of HIV-1 to their infants. Studies are ongoing to determine if the presence of these mutations has implications for the subsequent administration of nevirapine, either to prevent MTCT of HIV-1 or for the mother's own health. Effective interventions that can reduce MTCT of HIV are now available worldwide. However, a number of issues remain to be resolved, particularly methods to reduce the transmission of the virus during breastfeeding and to deliver effective treatment for the mothers' own HIV infection.