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Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase
Increased Aurora A expression occurs in a variety of human cancers and induces chromosomal abnormalities during mitosis associated with tumor initiation and progression. MLN8054 is a selectiveExpand
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Effective dosing regimen of 1-aminobenzotriazole for inhibition of antipyrine clearance in rats, dogs, and monkeys.
1-Aminobenzotriazole (ABT) has been extensively used as a nonspecific inhibitor of cytochromes p450 (p450s) in animals for mechanistic studies, and antipyrine (AP) has been used as a probe forExpand
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Species differences in the pharmacokinetics and metabolism of indinavir, a potent human immunodeficiency virus protease inhibitor.
  • J. Lin, M. Chiba, +4 authors J. Nishime
  • Chemistry, Medicine
  • Drug metabolism and disposition: the biological…
  • 1 October 1996
Indinavir, a potent and specific inhibitor of human immunodeficiency virus protease, is undergoing clinical investigation for the treatment of acquired immunodeficiency syndrome. The studiesExpand
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Comparison of Intrinsic Clearance in Liver Microsomes and Hepatocytes from Rats and Humans: Evaluation of Free Fraction and Uptake in Hepatocytes
  • Chuang Lu, P. Li, +5 authors L. Gan
  • Chemistry, Medicine
  • Drug Metabolism and Disposition
  • 1 September 2006
Apparent intrinsic clearance (CLint,app) of 7-ethoxycoumarin, phenacetin, propranolol, and midazolam was measured using rat and human liver microsomes and freshly isolated and cryopreservedExpand
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Hepatic microsomal metabolism of montelukast, a potent leukotriene D4 receptor antagonist, in humans.
Montelukast (L-706,631, MK-0476, SINGULAIR), a potent and selective leukotriene D4 (CysLT1) receptor antagonist, is currently under development for the treatment of asthma. In vitro studies wereExpand
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Metabolic profiles of montelukast sodium (Singulair), a potent cysteinyl leukotriene1 receptor antagonist, in human plasma and bile.
  • S. Balani, X. Xu, +16 authors T. Baillie
  • Medicine, Chemistry
  • Drug metabolism and disposition: the biological…
  • 1 November 1997
Montelukast sodium [1-([(1(R)-(3-(2-(7-chloro-2-quinolinyl)-(E)- ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio]methyl)cyclopropylacetic acid sodium salt] (MK-476, Singulair) is aExpand
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Strategy of utilizing in vitro and in vivo ADME tools for lead optimization and drug candidate selection.
The high-throughput screening in drug discovery for absorption, distribution, metabolism and excretion (ADME) properties has become the norm in the industry. Only a few years ago it was ADMEExpand
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Role of cytochrome P450 3A4 in human metabolism of MK-639, a potent human immunodeficiency virus protease inhibitor.
MK-639 (L-735,524) is a potent human immunodeficiency virus protease inhibitor under investigation in the treatment of acquired immunodeficiency syndrome. Five in vitro approaches have been used toExpand
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A Novel Model for the Prediction of Drug-Drug Interactions in Humans Based on in Vitro Cytochrome P450 Phenotypic Data
Ketoconazole has generally been used as a standard inhibitor for studying clinical pharmacokinetic drug-drug interactions (DDIs) of drugs that are primarily metabolized by CYP3A4/5. However,Expand
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Disposition of indinavir, a potent HIV-1 protease inhibitor, after an oral dose in humans.
  • S. Balani, E. Woolf, +4 authors J. Lin
  • Chemistry, Medicine
  • Drug metabolism and disposition: the biological…
  • 1 December 1996
Indinavir, N-[2(R)-hydroxy-1(S)-indanyl]-5-[2(S)-tertiary- butylaminocarbonyl-4-(3-pyridylmethyl)piperazino]-4(S)- hydroxy-2(R)-phenylmethylpentanamide (L-735,524,MK-639, ayl-4- Crixivan), is aExpand
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