1
2
D. Lu et al.
Xenobiotica, Early Online: 1–13
Costa A, Sarmento B, Seabra V. (2014). An evaluation of the latest
in vitro tools for drug metabolism studies. Expert Opin Drug Metab
Toxicol 10:103–19.
Liu H, Sun H, Lu D, et al. (2014a). Identification of glucuronidation and
biliary excretion as the main mechanisms for gossypol clearance:
in vivo and in vitro evidence. Xenobiotica 44:696–707.
Court MH. (2005). Isoform-selective probe substrates for in vitro studies
of human UDP-glucuronosyltransferases. Methods Enzymol 400:
Mackenzie PI, Bock KW, Burchell B, et al. (2005). Nomenclature update
for the mammalian UDP glycosyltransferase (UGT) gene superfamily.
Pharmacogenet Genomics 15:677–85.
1
04–16.
Cubitt HE, Houston JB, Galetin A. (2011). Prediction of human drug
clearance by multiple metabolic pathways: integration of hepatic and
intestinal microsomal and cytosolic data. Drug Metab Dispos 39:
Manevski N, Moreolo PS, Yli-Kauhaluoma J, Finel M. (2011).
Bovine serum albumin decreases Km values of human
UDP-glucuronosyltransferases 1A9 and 2B7 and increases Vmax
values of UGT1A9. Drug Metab Dispos 39:2117–29.
8
64–73.
Dawson VK, Schreier TM, Boogaard MA, Gingerich WH. (1999).
Uptake, metabolism, and elimination of niclosamide by fish. In: Smith
DJ, Gingerich WH, Beconi-Barker MG, eds. Xenobiotics in fish.
Springer, 167–76.
Nagar S, Blanchard RL. (2006). Pharmacogenetics of uridine
diphosphoglucuronosyltransferase (UGT) 1A family members
and its role in patient response to irinotecan. Drug Metab Rev 38:
393–409.
Douch PG, Gahagan HM. (1977). The metabolism of niclosamide
and related compounds by Moniezia expansa, Ascaris
lumbricoides var suum, and mouse- and sheep-liver enzymes.
Xenobiotica 7:301–7.
Nakajima M, Nakamura S, Tokudome S, et al. (1999). Azelastine
N-demethylation by cytochrome P-450 (CYP)3A4, CYP2D6, and
CYP1A2 in human liver microsomes: evaluation of approach to
predict the contribution of multiple CYPs. Drug Metab Dispos 27:
Emoto C, Murayama N, Rostami-Hodjegan A, Yamazaki H. (2010).
Methodologies for investigating drug metabolism at the early drug
discovery stage: prediction of hepatic drug clearance and P450
contribution. Curr Drug Metab 11:678–85.
1
381–91.
Nakamura A, Nakajima M, Yamanaka H, et al. (2008). Expression of
UGT1A and UGT2B mRNA in human normal tissues and various cell
lines. Drug Metab Dispos 36:1461–4.
Evans WE, Relling MV. (1999). Pharmacogenomics: translating func-
tional genomics into rational therapeutics. Science 286:487–91.
Fang ZZ, Krausz KW, Nagaoka K, et al. (2014). In vivo effects of the
pure aryl hydrocarbon receptor antagonist GNF-351 after oral
Ohno S, Nakajin S. (2009). Determination of mRNA expression of
human UDP-glucuronosyltransferases and application for localization
in various human tissues by real-time reverse transcriptase-polymer-
ase chain reaction. Drug Metab Dispos 37:32–40.
Ortiz de Montellano PR. (2005). Cytochrome P450: structure, mechan-
ism, and biochemistry. Springer Science & Business Media.
Paine MF, Hart HL, Ludington SS, et al. (2006). The human intestinal
cytochrome P450 ‘‘pie’’. Drug Metab Dispos 34:880–6.
Pan JX, Ding K, Wang CY. (2012). Niclosamide, an old antihelminthic
agent, demonstrates antitumor activity by blocking multiple signaling
pathways of cancer stem cells. Chin J Cancer 31:178–84.
Park SJ, Shin JH, Kang H, et al. (2011). Niclosamide induces
mitochondria fragmentation and promotes both apoptotic and
autophagic cell death. BMB Rep 44:517–22.
Pastrakuljic A, Tang BK, Roberts EA, Kalow W. (1997). Distinction of
CYP1A1 and CYP1A2 activity by selective inhibition using fluvox-
amine and isosafrole. Biochem Pharmacol 53:531–8.
administration are limited to the gastrointestinal tract. Br
Pharmacol 171:1735–46.
J
Fonseca BD, Diering GH, Bidinosti MA, et al. (2012). Structure–activity
analysis of niclosamide reveals potential role for cytoplasmic pH in
control of mammalian target of rapamycin complex 1 (mTORC1)
signaling. J Biol Chem 287:17530–45.
Fujita
irinotecan disposition and toxicity: a review. Curr Clin Pharmacol 5:
09–17.
K,
Sparreboom
A.
(2010).
Pharmacogenetics
of
2
Gao H, Steyn SJ, Chang G, Lin J. (2010). Assessment of in silico models
for fraction of unbound drug in human liver microsomes. Expert Opin
Drug Metab Toxicol 6:533–42.
Gertz M, Houston JB, Galetin A. (2011). Physiologically based
pharmacokinetic modeling of intestinal first-pass metabolism of
CYP3A substrates with high intestinal extraction. Drug Metab
Dispos 39:1633–42.
Poulin P, Haddad S. (2011). Microsome composition-based model as a
mechanistic tool to predict nonspecific binding of drugs in liver
microsomes. J Pharm Sci 100:4501–17.
Griffiths LA, Facchini V. (1979). The major metabolites of niclosamide:
identification by mass spectrometry. In: Frigerio A, ed. Recent
developments in mass spectrometry in biochemistry and medicine.
Vol. 2. Springer, 121–6.
Hallifax D, Foster JA, Houston JB. (2010). Prediction of human
metabolic clearance from in vitro systems: retrospective analysis and
prospective view. Pharm Res 27:2150–61.
Hallifax D, Houston JB. (2006). Binding of drugs to hepatic microsomes:
comment and assessment of current prediction methodology with
recommendation for improvement. Drug Metab Dispos 34:724–6;
author reply 727.
Hutzler JM, Tracy TS. (2002). Atypical kinetic profiles in drug
metabolism reactions. Drug Metab Dispos 30:355–62.
Prentis RA, Lis Y, Walker SR. (1988). Pharmaceutical innovation by the
seven UK-owned pharmaceutical companies (1964–1985). Br J Clin
Pharmacol 25:387–96.
Reid JM, Kuffel MJ, Miller JK, et al. (1999). Metabolic
activation of dacarbazine by human cytochromes P450: the
role of CYP1A1, CYP1A2, and CYP2E1. Clin Cancer Res 5:
2
192–7.
Rowland A, Elliot DJ, Knights KM, et al. (2008). The ‘‘albumin effect’’
and in vitro–in vivo extrapolation: sequestration of long-chain
unsaturated fatty acids enhances phenytoin hydroxylation by human
liver microsomal and recombinant cytochrome P450 2C9. Drug
Metab Dispos 36:870–7.
Seo KA, Kim HJ, Jeong ES, et al. (2014). In vitro assay of six UDP-
glucuronosyltransferase isoforms in human liver microsomes, using
cocktails of probe substrates and liquid chromatography–tandem mass
spectrometry. Drug Metab Dispos 42:1803–10.
Shet MS, McPhaul M, Fisher CW, et al. (1997). Metabolism of the
antiandrogenic drug (Flutamide) by human CYP1A2. Drug Metab
Dispos 25:1298–303.
Shimada H, Eto M, Ohtaguro M, et al. (2010). Differential mechanisms
for the inhibition of human cytochrome P450 1A2 by apigenin and
genistein. J Biochem Mol Toxicol 24:230–4.
Imperi F, Massai F, Ramachandran Pillai C, et al. (2013). New life for an
old drug: the anthelmintic drug niclosamide inhibits Pseudomonas
aeruginosa quorum sensing. Antimicrob Agents Chemother 57:
9
96–1005.
Jin Y, Lu Z, Ding K, et al. (2010). Antineoplastic mechanisms of
niclosamide in acute myelogenous leukemia stem cells: inactivation of
the NF-kappaB pathway and generation of reactive oxygen species.
Cancer Res 70:2516–27.
Kassahun K, Mattiuz E, Franklin R, Gillespie T. (1998). Olanzapine
10-N-glucuronide: a tertiary N-glucuronide unique to humans. Drug
Metab Dispos 26:848–55.
Kola I, Landis J. (2004). Can the pharmaceutical industry reduce attrition
rates? Nat Rev Drug Discov 3:711–15.
Li Y, Li PK, Roberts MJ, et al. (2014). Multi-targeted therapy of cancer
by niclosamide: a new application for an old drug. Cancer Lett 349:
Sun H, Wang H, Liu H, et al. (2014). Glucuronidation of capsaicin by
liver microsomes and expressed UGT enzymes: reaction kinetics,
contribution of individual enzymes and marked species differences.
Expert Opin Drug Metab Toxicol 10:1325–36.
Tassaneeyakul W, Birkett DJ, Veronese ME, et al. (1993). Specificity of
substrate and inhibitor probes for human cytochromes P450 1A1 and
8
–14.
1
A2. J Pharmacol Exp Ther 265:401–7.
Liu W, Liu H, Sun H, et al. (2014b). Metabolite elucidation of the Hsp90
inhibitor SNX-2112 using ultraperformance liquid chromatography/
quadrupole time-of-flight mass spectrometry (UPLC-QTOF/MS).
Xenobiotica 44:455–64.
von Moltke LL, Weemhoff JL, Bedir E, et al. (2004). Inhibition of
human cytochromes P450 by components of Ginkgo biloba. J Pharm
Pharmacol 56:1039–44.