Practical Preclinical Model for Assessing the Potential for Unconjugated Hyperbilirubinemia Produced by Human Immunodeficiency Virus Protease Inhibitors
Author(s) -
Dale J. Kempf,
Jeffrey F. Waring,
David C. Morfitt,
Paige Werner,
Brian Ebert,
Michael J. Mitten,
Bach Nguyen,
John T. Randolph,
David A. DeGoey,
Larry L. Klein,
Kennan C. Marsh
Publication year - 2006
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.50.2.762-764.2006
Subject(s) - amprenavir , ritonavir , indinavir , atazanavir , protease , virology , protease inhibitor (pharmacology) , unconjugated hyperbilirubinemia , medicine , pharmacology , darunavir , human immunodeficiency virus (hiv) , biology , antiretroviral therapy , hiv 1 protease , enzyme , viral load , biochemistry , jaundice
A practical preclinical model for the hyperbilirubinemia produced by human immunodeficiency virus protease inhibitors has been developed. Indinavir and atazanavir produced significant hyperbilirubinemia, whereas amprenavir, the negative control, was indistinguishable from the ritonavir booster dose. This model was used to disqualify an exploratory protease inhibitor from development.
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