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Raltegravir In Vitro Effect on Bilirubin Binding

Clarke, Diana F. PharmD*; Wong, Ronald J. PhD; Wenning, Larissa PhD; Stevenson, David K. MD; Mirochnick, Mark MD*

Pediatric Infectious Disease Journal: September 2013 - Volume 32 - Issue 9 - p 978–980
doi: 10.1097/INF.0b013e31829044a8
HIV Reports

Drugs that displace bilirubin from albumin may increase the risk of kernicterus in neonates. We evaluated the effect of raltegravir on bilirubin–albumin binding in pooled neonatal serum using the peroxidase method. Raltegravir had minimal effect on bilirubin–albumin binding at concentrations of 5 and 10 µM, caused a small but statistically significant increase in unbound bilirubin at 100 µM and caused potentially harmful increases at 500 and 1000 µM. Our data suggest that the effect of raltegravir on neonatal bilirubin binding is unlikely to be clinically significant at typical peak concentrations reached with usual dosing.

From the *Department of Pediatrics, Boston University School of Medicine/Boston Medical Center, Boston, MA; Department of Pediatrics, Division of Neonatal and Developmental Medicine, Stanford University School of Medicine, Stanford, CA; and Merck & Co., Inc., Whitehouse Station, NJ.

Accepted for publication March 04, 2013.

This work was supported, in part, by the Clinical and Translational Science Award 1UL1 RR025744 for the Stanford Center for Clinical and Translational Education and Research (Spectrum) from the National Center for Research Resources, National Institutes of Health, the Mary L. Johnson Research Fund, the Christopher Hess Research Fund, the H.M. Lui Research Fund, the National Institute of Allergy and Infectious Diseases [U01 AI068632] and the Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) [contract NO1-HD33345]. Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc., provided raltegravir and financial support for the conduct of the study. The study involved members of the International Maternal Pediatric Adolescent AIDS Clinical Trials P1097 team: overall support for the International Maternal Pediatric Adolescent AIDS Clinical Trials Group was provided by the National Institute of Allergy and Infectious Diseases [U01 AI068632], the Eunice Kennedy Shriver NICHD and the National Institute of Mental Health [AI068632]. The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institute of Health. This work was supported by the Statistical and Data Analysis Center at Harvard School of Public Health, under the National Institute of Allergy and Infectious Diseases cooperative agreement no.5 U01 AI41110 with the Pediatric AIDS Clinical Trials Group and no.1 U01 AI068616 with the International Maternal Pediatric Adolescent AIDS Clinical Trials Group. Support of the sites was provided by the National Institute of Allergy and Infectious Diseases and the NICHD International and Domestic Pediatric and Maternal HIV Clinical Trials Network funded by NICHD (contract number N01-DK-9-001/HHSN267200800001C). The authors have no other funding or conflicts of interest to disclose.

Address for correspondence: Diana F. Clarke, PharmD, Section of Pediatric Infectious Diseases, Boston Medical Center, 670 Albany Street, 6th Floor, Boston, MA 02118. E-mail: diana.clarke@bmc.org.

© 2013 by Lippincott Williams & Wilkins, Inc.