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