Nelfinavir and its active metabolite, hydroxy-t-butylamidenelfinavir (M8), are transferred in small quantities to breast milk and do not reach biologically significant concentrations in breast-feeding infants whose mothers are taking nelfinavir

Abstract

Antiretroviral drugs cross from maternal plasma to breast milk and from breast milk to the infant in different concentrations. We measured concentrations of nelfinavir and its active metabolite (M8) in maternal plasma and breast milk from women and in dried blood spots collected from their infants at delivery and postnatal weeks 2, 6, 14, and 24 in the Kisumu Breastfeeding Study, Kisumu, Kenya. Nelfinavir-based antiretroviral regimens given to mothers as prevention of mother-to-child HIV transmission (PMTCT) do not expose the breast-feeding infant to biologically significant concentrations of nelfinavir or M8.

Fig. 1.

Concentrations of nelfinavir (NFV) and its active metabolite, hydroxyl-t-butylamidenelfinavir (M8), after dosing of nelfinavir mesylate (1,250 mg given orally twice daily) in maternal plasma (A) or breast milk (B) in the Kisumu Breastfeeding Study, Kenya, 2004 to 2007. Dashed lines are regression lines for nelfinavir, and solid lines are regression lines for M8. The P values represent the probability that the slope of the line is different from zero as calculated by Spearman-rank correlation statistics for trends. The changes in maternal plasma and breast milk concentrations of nelfinavir over a 12-h dosing interval were statistically significant at a significance level of 0.05.