title: Practical preclinical model for assessing the potential for unconjugated hyperbilirubinemia produced by human immunodeficiency virus protease inhibitors.
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.
authors.affiliation: Global Pharmaceutical Research and Development, Abbott, Abbott Park, Illinois 60064, USA. dale.kempf@abbott.com
authors.forename: Dale J
authors.initials: DJ
authors.lastname: Kempf
authors.forename: Jeffrey F
authors.initials: JF
authors.lastname: Waring
authors.forename: David C
authors.initials: DC
authors.lastname: Morfitt
authors.forename: Paige
authors.initials: P
authors.lastname: Werner
authors.forename: Brian
authors.initials: B
authors.lastname: Ebert
authors.forename: Michael
authors.initials: M
authors.lastname: Mitten
authors.forename: Bach
authors.initials: B
authors.lastname: Nguyen
authors.forename: John T
authors.initials: JT
authors.lastname: Randolph
authors.forename: David A
authors.initials: DA
authors.lastname: DeGoey
authors.forename: Larry L
authors.initials: LL
authors.lastname: Klein
authors.forename: Kennan
authors.initials: K
authors.lastname: Marsh
mesh_terms: D000818:Animals; D004195:Disease Models, Animal; D017320:HIV Protease Inhibitors / Q000097:blood / Q000633:toxicity*; D006932:Hyperbilirubinemia / Q000139:chemically induced*; D051381:Rats; D011911:Rats, Gunn
chemical_list: D017320:HIV Protease Inhibitors