Literature DB >> 16436740

Practical preclinical model for assessing the potential for unconjugated hyperbilirubinemia produced by human immunodeficiency virus protease inhibitors.

Dale J Kempf1, Jeffrey F Waring, David C Morfitt, Paige Werner, Brian Ebert, Michael Mitten, Bach Nguyen, John T Randolph, David A DeGoey, Larry L Klein, Kennan Marsh.   

Abstract

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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Year:  2006        PMID： 16436740      PMCID： PMC1366866          DOI： 10.1128/AAC.50.2.762-764.2006

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  5 in total

1.  In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin glucuronidation.

Authors:  Donglu Zhang; Theodore J Chando; Donald W Everett; Christopher J Patten; Shangara S Dehal; W Griffith Humphreys
Journal:  Drug Metab Dispos       Date:  2005-08-23       Impact factor: 3.922

2.  Pharmacokinetic enhancement of inhibitors of the human immunodeficiency virus protease by coadministration with ritonavir.

Authors:  D J Kempf; K C Marsh; G Kumar; A D Rodrigues; J F Denissen; E McDonald; M J Kukulka; A Hsu; G R Granneman; P A Baroldi; E Sun; D Pizzuti; J J Plattner; D W Norbeck; J M Leonard
Journal:  Antimicrob Agents Chemother       Date:  1997-03       Impact factor: 5.191

3.  Inhibition of human organic anion transporting polypeptide OATP 1B1 as a mechanism of drug-induced hyperbilirubinemia.

Authors:  Scott D Campbell; Sonia M de Morais; Jinghai J Xu
Journal:  Chem Biol Interact       Date:  2004-11-20       Impact factor: 5.192

4.  The 3-methylcholanthrene-inducible UDP-glucuronosyltransferase deficiency in the hyperbilirubinemic rat (Gunn rat) is caused by a -1 frameshift mutation.

Authors:  T Iyanagi; T Watanabe; Y Uchiyama
Journal:  J Biol Chem       Date:  1989-12-15       Impact factor: 5.157

5.  Mechanism of indinavir-induced hyperbilirubinemia.

Authors:  S D Zucker; X Qin; S D Rouster; F Yu; R M Green; P Keshavan; J Feinberg; K E Sherman
Journal:  Proc Natl Acad Sci U S A       Date:  2001-10-16       Impact factor: 11.205
  5 in total
  3 in total

1.  Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.

Authors:  Tatyana Dekhtyar; Teresa I Ng; Liangjun Lu; Sherie Masse; David A DeGoey; William J Flosi; David J Grampovnik; Larry L Klein; Dale J Kempf; Akhteruzzaman Molla
Journal:  Antimicrob Agents Chemother       Date:  2008-01-22       Impact factor: 5.191

Review 2.  Biomarkers, metabonomics, and drug development: can inborn errors of metabolism help in understanding drug toxicity?

Authors:  Subrahmanyam Vangala; Alfred Tonelli
Journal:  AAPS J       Date:  2007-07-20       Impact factor: 4.009

3.  Hyperbilirubinaemia in HIV-HCV co-infected patients on antiretroviral therapy: drug effect or liver disease severity?

Authors:  Matthew B Kaspar; Richard K Sterling
Journal:  BMJ Open Gastroenterol       Date:  2016-03-02
  3 in total

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