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J Acquir Immune Defic Syndr. 2014 Nov 1;67(3):310-5. doi: 10.1097/QAI.0000000000000316.

Raltegravir pharmacokinetics in neonates following maternal dosing.

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*Section of Pediatric Infectious Diseases, Boston Medical Center, Boston, MA; †Division of Clinical Pharmacology, University of Alabama at Birmingham, Birmingham, AL; ‡Merck & Co., Inc., Whitehouse Station, NJ; §Department of Pediatric Infectious Diseases, David Geffen School of Medicine at University of California at Los Angeles, Los Angeles, CA; ‖Department of Pediatrics, University of California, San Diego and Rady Children's Hospital San Diego, La Jolla, CA; ¶Eunice Kennedy Shriver National Institute of Child Health and Human Development, #Division of AIDS, National Institute of Health, Bethesda, MD; **Department of Pediatrics, Johns Hopkins University School of Medicine, Baltimore, MD; ††Statistical and Data Analysis Center, Harvard School of Public Health, Boston, MA; and ‡‡Department of Pediatrics, Boston University School of Medicine, Boston, MA.


: International Maternal Pediatric Adolescent AIDS Clinical Trials P1097 was a multicenter trial to determine washout pharmacokinetics and safety of in utero/intrapartum exposure to raltegravir in infants born to HIV-infected pregnant women receiving raltegravir-based antiretroviral therapy. Twenty-two mother-infant pairs were enrolled; evaluable pharmacokinetic data were available from 19 mother-infant pairs. Raltegravir readily crossed the placenta, with a median cord blood/maternal delivery plasma raltegravir concentration ratio of 1.48 (range, 0.32-4.33). Raltegravir elimination was highly variable and extremely prolonged in some infants; [median t1/2 26.6 (range, 9.3-184) hours]. Prolonged raltegravir elimination likely reflects low neonatal UGT1A1 enzyme activity and enterohepatic recirculation. Excessive raltegravir concentrations must be avoided in the neonate because raltegravir at high plasma concentrations may increase the risk of bilirubin neurotoxicity. Subtherapeutic concentrations, which could lead to inadequate viral suppression and development of raltegravir resistance, must also be avoided. Two ongoing International Maternal Pediatric Adolescent AIDS Clinical Trials studies are further investigating the pharmacology of raltegravir in neonates.

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