-
1
-
-
9544225260
-
The present status and problems of bacterial chemotherapy
-
Marshall Jr, EK. The present status and problems of bacterial chemotherapy. Science 1940; 91: 345-50.
-
(1940)
Science
, vol.91
, pp. 345-350
-
-
Marshall Jr, E.K.1
-
2
-
-
69249105627
-
The toxicity of atabrine to the central nervous system
-
Newell HW, Lidz T. The toxicity of atabrine to the central nervous system. Am J Psychiatry 1946; 102: 805-18.
-
(1946)
Am J Psychiatry
, vol.102
, pp. 805-818
-
-
Newell, H.W.1
Lidz, T.2
-
3
-
-
0000106650
-
The pharmacological basis for the rational use of atabrine in the treatment of malaria
-
Shannon JA, Earle DP, Brodie BB, Taggart JV, Berliner RW. The pharmacological basis for the rational use of atabrine in the treatment of malaria. J Pharmacol Exp Ther 1944; 81: 307-30.
-
(1944)
J Pharmacol Exp Ther
, vol.81
, pp. 307-330
-
-
Shannon, J.A.1
Earle, D.P.2
Brodie, B.B.3
Taggart, J.V.4
Berliner, R.W.5
-
5
-
-
0016411409
-
Analgesic abuse and renal disease
-
Murray T, Goldberg M. Analgesic abuse and renal disease. Ann Rev Med 1975; 26: 537-50.
-
(1975)
Ann Rev Med
, vol.26
, pp. 537-550
-
-
Murray, T.1
Goldberg, M.2
-
6
-
-
69249129523
-
-
Parkinson A. In: Klaassen CD, Ed. Biotransformation of xenobiotics. Casarett & Doull's Toxicology: The basic science of poisons, 5th ed. Columbus, OH: McGraw-Hill, Inc. 1996; pp. 133-186.
-
Parkinson A. In: Klaassen CD, Ed. Biotransformation of xenobiotics. Casarett & Doull's Toxicology: The basic science of poisons, 5th ed. Columbus, OH: McGraw-Hill, Inc. 1996; pp. 133-186.
-
-
-
-
7
-
-
33644847684
-
Transporters as a determinant of drug clearance and tissue distribution
-
Shitara Y, Horie T, Sugiyama Y. Transporters as a determinant of drug clearance and tissue distribution. Eur J Pharm Sci 2006; 27: 425-46
-
(2006)
Eur J Pharm Sci
, vol.27
, pp. 425-446
-
-
Shitara, Y.1
Horie, T.2
Sugiyama, Y.3
-
8
-
-
1642294294
-
Organic chemistry in drug discovery
-
MacCoss M, Baillie TA. Organic chemistry in drug discovery. Science 2004; 303: 1810-3.
-
(2004)
Science
, vol.303
, pp. 1810-1813
-
-
MacCoss, M.1
Baillie, T.A.2
-
9
-
-
0034034259
-
High-throughput screening in drug metabolism and pharmacokinetic support of drug discovery
-
White RE. High-throughput screening in drug metabolism and pharmacokinetic support of drug discovery. Annu Rev Pharmacol Toxicol 2000; 40: 133-57.
-
(2000)
Annu Rev Pharmacol Toxicol
, vol.40
, pp. 133-157
-
-
White, R.E.1
-
10
-
-
4344645978
-
Can the pharmaceutical industry reduce attrition rates?
-
Kola I, Landis J. Can the pharmaceutical industry reduce attrition rates? Nat Rev 2004; 3: 711-5.
-
(2004)
Nat Rev
, vol.3
, pp. 711-715
-
-
Kola, I.1
Landis, J.2
-
11
-
-
24944492194
-
Utility of recombinant cytochrome P450 enzymes: A drug metabolism perspective
-
Tang W, Wang RW, Lu AYH. Utility of recombinant cytochrome P450 enzymes: A drug metabolism perspective. Curr Drug Metab 2005; 6: 503-17.
-
(2005)
Curr Drug Metab
, vol.6
, pp. 503-517
-
-
Tang, W.1
Wang, R.W.2
Lu, A.Y.H.3
-
12
-
-
3142514405
-
Influence of different recombinant systems on the cooperativity exhibited by cytochrome P4503A4
-
Zhang Z, Li Y, Shou M, Zhang Y, Ngui JS, Stearns RA, et al. Influence of different recombinant systems on the cooperativity exhibited by cytochrome P4503A4. Xenobiotica 2004; 34: 473-86.
-
(2004)
Xenobiotica
, vol.34
, pp. 473-486
-
-
Zhang, Z.1
Li, Y.2
Shou, M.3
Zhang, Y.4
Ngui, J.S.5
Stearns, R.A.6
-
13
-
-
33751085910
-
Enzyme source effects on CYP2C9 kinetics and inhibition
-
Kumar V, Rock DA, Warren CJ, Tracy TS, Wahistrom JL. Enzyme source effects on CYP2C9 kinetics and inhibition. Drug Metab Dispos 2006; 34: 1903-8.
-
(2006)
Drug Metab Dispos
, vol.34
, pp. 1903-1908
-
-
Kumar, V.1
Rock, D.A.2
Warren, C.J.3
Tracy, T.S.4
Wahistrom, J.L.5
-
14
-
-
0030763543
-
Drug metabolism in hepatocyte sandwich cultures of rats and humans
-
Kern A, Bader A, Pichlmary R, Sewing K-F. Drug metabolism in hepatocyte sandwich cultures of rats and humans. Biochem Pharmacol 1997; 54: 761-72.
-
(1997)
Biochem Pharmacol
, vol.54
, pp. 761-772
-
-
Kern, A.1
Bader, A.2
Pichlmary, R.3
Sewing, K.-F.4
-
15
-
-
4544373020
-
Substituted piperazines as novel dipeptidyl peptidase IV inhibitors
-
Brockunier LL, He J, Colwell LF, Habulihaz B, He H, Leiting B, et al. Substituted piperazines as novel dipeptidyl peptidase IV inhibitors. Bioorg Med Chem Lett 2004; 14: 4763-6.
-
(2004)
Bioorg Med Chem Lett
, vol.14
, pp. 4763-4766
-
-
Brockunier, L.L.1
He, J.2
Colwell, L.F.3
Habulihaz, B.4
He, H.5
Leiting, B.6
-
16
-
-
19944427998
-
-
Kim D, Wang L, Beconi M, Eiermann GJ, Fisher MH, He H, et al. (2R)-4-Oxo-4-3-(trifluoromethyl)- 5,6-dihydro1,2,4triazolo4,3- apyrazin-7(8H)-yl-1-(2,4,5- trifluorophenyl)butan-2-amine: A potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. J Med Chem 2005; 48: 141-51.
-
Kim D, Wang L, Beconi M, Eiermann GJ, Fisher MH, He H, et al. (2R)-4-Oxo-4-3-(trifluoromethyl)- 5,6-dihydro1,2,4triazolo4,3- apyrazin-7(8H)-yl-1-(2,4,5- trifluorophenyl)butan-2-amine: A potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. J Med Chem 2005; 48: 141-51.
-
-
-
-
17
-
-
32844473903
-
Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor: A double-blind, randomized, placebo-controlled study in healthy male volunteers
-
Bergman AJ, Stevens C, Zhou Y, Yi B, Laethem M, Smet MD, et al. Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor: A double-blind, randomized, placebo-controlled study in healthy male volunteers. Clin Ther 2006; 28: 55-72.
-
(2006)
Clin Ther
, vol.28
, pp. 55-72
-
-
Bergman, A.J.1
Stevens, C.2
Zhou, Y.3
Yi, B.4
Laethem, M.5
Smet, M.D.6
-
18
-
-
34047097841
-
Metabolism and excretion of the dipeptidyl peptidase 4 inhibitor 14Csitagliptin in humans
-
Vincent SH, Reed JR, Bergman AJ, Elmore CS, Zhu B, Xu S, et al. Metabolism and excretion of the dipeptidyl peptidase 4 inhibitor 14Csitagliptin in humans. Drug Metab Dispos 2007; 35: 533-8.
-
(2007)
Drug Metab Dispos
, vol.35
, pp. 533-538
-
-
Vincent, S.H.1
Reed, J.R.2
Bergman, A.J.3
Elmore, C.S.4
Zhu, B.5
Xu, S.6
-
19
-
-
38149111228
-
Importance of mechanistic drug metabolism studies in support of drug discovery: A case study with an N-sulfonylated dipeptide VLA-4 antagonist in rats
-
Tang W, Stearns RA, Chen Q, Bleasby K, Teffera Y, Colletti A, et al. Importance of mechanistic drug metabolism studies in support of drug discovery: A case study with an N-sulfonylated dipeptide VLA-4 antagonist in rats. Xenobiotica 2008; 38: 223-37.
-
(2008)
Xenobiotica
, vol.38
, pp. 223-237
-
-
Tang, W.1
Stearns, R.A.2
Chen, Q.3
Bleasby, K.4
Teffera, Y.5
Colletti, A.6
-
20
-
-
0035428023
-
The discovery of linezolid, the first oxazolidinone antibacterial agent
-
Ford CW, Zurenko GE, Barbachyn MR. The discovery of linezolid, the first oxazolidinone antibacterial agent. Curr Drug Targets 2001; 1: 181-99.
-
(2001)
Curr Drug Targets
, vol.1
, pp. 181-199
-
-
Ford, C.W.1
Zurenko, G.E.2
Barbachyn, M.R.3
-
21
-
-
0037115316
-
Linezolid: An oxazolidinone antimicrobial agent
-
Paladino JA. Linezolid: An oxazolidinone antimicrobial agent. Am J Health-Syst Pharm 2002; 59: 2413-25.
-
(2002)
Am J Health-Syst Pharm
, vol.59
, pp. 2413-2425
-
-
Paladino, J.A.1
-
23
-
-
39049090890
-
HPLC-MS/MS in drug metabolism and pharmacokinetic screening
-
Hsieh Y. HPLC-MS/MS in drug metabolism and pharmacokinetic screening. Expert Opin Drug Metab Toxicol 2008; 4: 93-101.
-
(2008)
Expert Opin Drug Metab Toxicol
, vol.4
, pp. 93-101
-
-
Hsieh, Y.1
-
24
-
-
48149111027
-
-
Ceccarelli SM, Schlotterbeck G, Boissin P, Binder M, Buettelmann B, Hanlon S, et al. Metabolite identification via LC-SPE-NMR-MS of the in vitro biooxidation products of a lead mGlu5 allosteric antagonist and impact on the improvement of metabolic stability in the series. ChemMedChem 2008; 3: 136-44.
-
Ceccarelli SM, Schlotterbeck G, Boissin P, Binder M, Buettelmann B, Hanlon S, et al. Metabolite identification via LC-SPE-NMR-MS of the in vitro biooxidation products of a lead mGlu5 allosteric antagonist and impact on the improvement of metabolic stability in the series. ChemMedChem 2008; 3: 136-44.
-
-
-
-
25
-
-
13444266910
-
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: Identification of 4-5-(4-methylphenyl)- 3-(trifluoromethyl)-1H- pyrazol-1-ylbenzenesulfonamide (SC-58635, celecoxib)
-
Penning TD, Talley JJ, Bertenshaw SR, Carter JS, Collins PW, Docter S, et al. Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: Identification of 4-5-(4-methylphenyl)- 3-(trifluoromethyl)-1H- pyrazol-1-ylbenzenesulfonamide (SC-58635, celecoxib). J Med Chem 1997; 40: 1347-65.
-
(1997)
J Med Chem
, vol.40
, pp. 1347-1365
-
-
Penning, T.D.1
Talley, J.J.2
Bertenshaw, S.R.3
Carter, J.S.4
Collins, P.W.5
Docter, S.6
-
26
-
-
0034052783
-
Pharmacokinetics, tissue distribution, metabolism, and excretion of celecoxib in rats
-
Paulson SK, Zhang JY, Breau AP, Hribar JD, Liu NWK, Jessen SM, et al. Pharmacokinetics, tissue distribution, metabolism, and excretion of celecoxib in rats. Drug Metab Dispos 2000; 28: 514-21.
-
(2000)
Drug Metab Dispos
, vol.28
, pp. 514-521
-
-
Paulson, S.K.1
Zhang, J.Y.2
Breau, A.P.3
Hribar, J.D.4
Liu, N.W.K.5
Jessen, S.M.6
-
27
-
-
0033621712
-
Metabolism and excretion of 14Ccelecoxib in healthy male volunteers
-
Paulson SK, Hribar JD, Liu NWK, Hajdu E, Bible Jr RH, Piergies A, et al. Metabolism and excretion of 14Ccelecoxib in healthy male volunteers. Drug Metab Dispos 2000; 28: 308-14.
-
(2000)
Drug Metab Dispos
, vol.28
, pp. 308-314
-
-
Paulson, S.K.1
Hribar, J.D.2
Liu, N.W.K.3
Hajdu, E.4
Bible Jr, R.H.5
Piergies, A.6
-
28
-
-
0000550245
-
A highly selective inhibitor of cyclooxygenase-2: Disposition kinetics in man and identification of its major CYP450 isozyme in its biotransformation
-
Karim A, Tolbert D, Burton E, Piergies A, Harper K, Paulson S, et al. A highly selective inhibitor of cyclooxygenase-2: Disposition kinetics in man and identification of its major CYP450 isozyme in its biotransformation. Pharm Res 1997; 14: S617.
-
(1997)
Pharm Res
, vol.14
-
-
Karim, A.1
Tolbert, D.2
Burton, E.3
Piergies, A.4
Harper, K.5
Paulson, S.6
-
29
-
-
1642281756
-
Drug-protein covalent adducts: An industry perspective on minimizing the potential for drug bioactivation in drug discovery and development
-
Evans DC, Watt AP, Nicoll-Griffith DA, Baillie TA. Drug-protein covalent adducts: An industry perspective on minimizing the potential for drug bioactivation in drug discovery and development. Chem Res Toxicol 2004; 17: 3-16.
-
(2004)
Chem Res Toxicol
, vol.17
, pp. 3-16
-
-
Evans, D.C.1
Watt, A.P.2
Nicoll-Griffith, D.A.3
Baillie, T.A.4
-
30
-
-
38949088196
-
Metabolism and toxicity of drugs. Two decades of progress in industrial drug metabolism
-
Baillie TA. Metabolism and toxicity of drugs. Two decades of progress in industrial drug metabolism. Chem Res Toxicol 2008; 21: 129-37.
-
(2008)
Chem Res Toxicol
, vol.21
, pp. 129-137
-
-
Baillie, T.A.1
-
31
-
-
0036163759
-
Mechanisms of hepatotoxicity
-
Jaeschke H, Gores GJ, Cederbaum AI, Hinson JA, Pessayre D, Lemasters JJ: Mechanisms of hepatotoxicity. Toxicol Sci 2002; 65: 166-76.
-
(2002)
Toxicol Sci
, vol.65
, pp. 166-176
-
-
Jaeschke, H.1
Gores, G.J.2
Cederbaum, A.I.3
Hinson, J.A.4
Pessayre, D.5
Lemasters, J.J.6
-
32
-
-
33747816149
-
Toxicophores: Investigations in drug safety
-
Williams DP: Toxicophores: Investigations in drug safety. Toxicology 2006; 226: 1-11.
-
(2006)
Toxicology
, vol.226
, pp. 1-11
-
-
Williams, D.P.1
-
33
-
-
24944499515
-
-
Yan Z, Caldwell GW, Eds, Totowa, NJ: Humana Press Inc
-
Tang W, Miller MR. In: Yan Z, Caldwell GW, Eds. Thiol conjugation in in vitro drug metabolism: Methods in pharmacology and toxicology, Optimization in drug discovery: In vitro Methods. Totowa, NJ: Humana Press Inc. 2004; pp. 369-383.
-
(2004)
Thiol conjugation in in vitro drug metabolism: Methods in pharmacology and toxicology, Optimization in drug discovery: In vitro Methods
, pp. 369-383
-
-
Tang, W.1
Miller, M.R.2
-
34
-
-
20244376331
-
In vitro bioactivation of dihydrobenzoxathiin selective estrogen receptor modulators by cytochrome P450 3A4 in human liver microsomes: Formation of reactive iminium and quinone type metabolites
-
Zhang Z, Chen Q, Li Y, Doss GA, Dean BJ, Ngui JS, et al. In vitro bioactivation of dihydrobenzoxathiin selective estrogen receptor modulators by cytochrome P450 3A4 in human liver microsomes: Formation of reactive iminium and quinone type metabolites. Chem Res Toxicol 2005; 18: 675-85.
-
(2005)
Chem Res Toxicol
, vol.18
, pp. 675-685
-
-
Zhang, Z.1
Chen, Q.2
Li, Y.3
Doss, G.A.4
Dean, B.J.5
Ngui, J.S.6
-
35
-
-
34548214599
-
Drug metabolite profiling and elucidation of drug-induced hepatotoxicity. Expert Opin Drug Metab
-
Tang W. Drug metabolite profiling and elucidation of drug-induced hepatotoxicity. Expert Opin Drug Metab Toxicol 2007; 3: 407-20.
-
(2007)
Toxicol
, vol.3
, pp. 407-420
-
-
Tang, W.1
-
36
-
-
37849042912
-
Minimizing metabolic activation during pharmaceutical lead optimization: Progress, knowledge gaps and future directions
-
Kumar S, Kassahun K, Tschirret-Guth RA, Mitra K, Baillie TA. Minimizing metabolic activation during pharmaceutical lead optimization: Progress, knowledge gaps and future directions. Curr Opin Drug Discov Dev 2008; 11: 43-52.
-
(2008)
Curr Opin Drug Discov Dev
, vol.11
, pp. 43-52
-
-
Kumar, S.1
Kassahun, K.2
Tschirret-Guth, R.A.3
Mitra, K.4
Baillie, T.A.5
-
37
-
-
0036890353
-
Complexities of glucuronidation affecting in vitro-in vivo extrapolation
-
Lin JH, Wong BK. Complexities of glucuronidation affecting in vitro-in vivo extrapolation. Curr Drug Metab 2002; 3: 623-46.
-
(2002)
Curr Drug Metab
, vol.3
, pp. 623-646
-
-
Lin, J.H.1
Wong, B.K.2
-
38
-
-
4844227887
-
The discovery and potential of N-sulfonylated dipeptide VLA-4 antagonists
-
Hagmann WK. The discovery and potential of N-sulfonylated dipeptide VLA-4 antagonists. Curr Topics Med Chem 2004; 4: 1461-71.
-
(2004)
Curr Topics Med Chem
, vol.4
, pp. 1461-1471
-
-
Hagmann, W.K.1
-
39
-
-
33847345910
-
-
2 receptor antagonist, (3R)-4-(4-chlorobenzyl -7-fluoro-5- (methylsulfonyl)-1,2,3,4- tetrahydrocyclopentabindol-3-yl-acetic acid. J Med Chem 2007; 50: 794-806.
-
2 receptor antagonist, (3R)-4-(4-chlorobenzyl -7-fluoro-5- (methylsulfonyl)-1,2,3,4- tetrahydrocyclopentabindol-3-yl-acetic acid. J Med Chem 2007; 50: 794-806.
-
-
-
-
40
-
-
34249301403
-
2 receptor 1 antagonist, in rats, dogs and monkeys
-
2 receptor 1 antagonist, in rats, dogs and monkeys. Xenobiotica 2007; 37: 514-33.
-
(2007)
Xenobiotica
, vol.37
, pp. 514-533
-
-
Chang, S.W.1
Reddy, V.2
Pereira, T.3
Dean, B.J.4
Xia, Y.-Q.5
Seto, C.6
-
41
-
-
34250713349
-
Absorption, metabolism, and excretion of 14CMK-0524, a prostaglandin D2 receptor antagonist, in humans
-
Karanam B, Maderia M, Bradley S, Wenning L, Desai R, Soli E, et al. Absorption, metabolism, and excretion of 14CMK-0524, a prostaglandin D2 receptor antagonist, in humans. Drug Metab Dispos 2007; 35: 1196-202.
-
(2007)
Drug Metab Dispos
, vol.35
, pp. 1196-1202
-
-
Karanam, B.1
Maderia, M.2
Bradley, S.3
Wenning, L.4
Desai, R.5
Soli, E.6
-
42
-
-
43949145969
-
Pharmacokinetics, pharmacodynamics, and safety of a prostaglandin D2 receptor antagonist
-
Lai E, Wenning LA, Crumley TM, De Lepeleire I, Liu F, De Hoon JN, et al. Pharmacokinetics, pharmacodynamics, and safety of a prostaglandin D2 receptor antagonist. Clin Pharmacol Ther 2008; 83: 840-7.
-
(2008)
Clin Pharmacol Ther
, vol.83
, pp. 840-847
-
-
Lai, E.1
Wenning, L.A.2
Crumley, T.M.3
De Lepeleire, I.4
Liu, F.5
De Hoon, J.N.6
-
43
-
-
0031794361
-
Inhibition and induction of cytochrome P450 and clinical implications
-
Lin JH, Lu AY. Inhibition and induction of cytochrome P450 and clinical implications. Clin Pharmacokinet 1998; 35: 361-90.
-
(1998)
Clin Pharmacokinet
, vol.35
, pp. 361-390
-
-
Lin, J.H.1
Lu, A.Y.2
-
44
-
-
0035069388
-
Use of in vitro drug metabolism data to evaluate metabolic drug-drug interactions in man: The need for quantitative databases
-
Rodrigues AD, Winchell GA, Dobrinska MR. Use of in vitro drug metabolism data to evaluate metabolic drug-drug interactions in man: The need for quantitative databases. J Clin Pharmacol 2001; 41: 368-73.
-
(2001)
J Clin Pharmacol
, vol.41
, pp. 368-373
-
-
Rodrigues, A.D.1
Winchell, G.A.2
Dobrinska, M.R.3
-
45
-
-
34247391128
-
Reduction of site-specific CYP3A-mediated metabolism for dual angiotensin and endothelin receptor antagonists in various in vitro systems and in cynomolgus monkeys
-
Zhang H, Zhang D, Li W, Yao M, D'Arienzo CD, Li Y-X, et al. Reduction of site-specific CYP3A-mediated metabolism for dual angiotensin and endothelin receptor antagonists in various in vitro systems and in cynomolgus monkeys. Drug Metab Dispos 2007; 35: 795-805.
-
(2007)
Drug Metab Dispos
, vol.35
, pp. 795-805
-
-
Zhang, H.1
Zhang, D.2
Li, W.3
Yao, M.4
D'Arienzo, C.D.5
Li, Y.-X.6
-
46
-
-
69249150914
-
-
FDA. Guidance for Industry: Drug interaction studies - Study design, data analysis, and implications for dosing and labeling. http://www.fda.gov/cder/guidance/index.htm 2006.
-
FDA. Guidance for Industry: Drug interaction studies - Study design, data analysis, and implications for dosing and labeling. http://www.fda.gov/cder/guidance/index.htm 2006.
-
-
-
-
47
-
-
14044254791
-
Selective inhibition of human cytochrome P4502C8 by montelukast
-
Walsky RL, Obach RS, Gaman EA, Gleeson J-PR, Proctor WR. Selective inhibition of human cytochrome P4502C8 by montelukast. Drug Metab Dispos 2005; 33: 413-8.
-
(2005)
Drug Metab Dispos
, vol.33
, pp. 413-418
-
-
Walsky, R.L.1
Obach, R.S.2
Gaman, E.A.3
Gleeson, J.-P.R.4
Proctor, W.R.5
-
48
-
-
69249149695
-
An open-label, randomized, 2-period, crossover study, to assess the effects of montelukast on the pharmacokinetics of rosiglitazone, a CYP2C8 substrate, in healthy adults
-
Friedman E, Ramakrishnan R, Larson P, Korzekwa K, Wagner JA, Migoya E. An open-label, randomized, 2-period, crossover study, to assess the effects of montelukast on the pharmacokinetics of rosiglitazone, a CYP2C8 substrate, in healthy adults. Clin Pharmacol Ther 2006; P72.
-
(2006)
Clin Pharmacol Ther
-
-
Friedman, E.1
Ramakrishnan, R.2
Larson, P.3
Korzekwa, K.4
Wagner, J.A.5
Migoya, E.6
-
49
-
-
0035996330
-
Cytochrome P450 3A4-mediated bioactivation of raloxifene: Irreversible enzyme inhibition and thiol adduct formation
-
Chen Q, Ngui JS, Doss GA, Wang RW, Cai X, DiNinno FP, et al. Cytochrome P450 3A4-mediated bioactivation of raloxifene: Irreversible enzyme inhibition and thiol adduct formation. Chem Res Toxicol 2002; 15: 907-14.
-
(2002)
Chem Res Toxicol
, vol.15
, pp. 907-914
-
-
Chen, Q.1
Ngui, J.S.2
Doss, G.A.3
Wang, R.W.4
Cai, X.5
DiNinno, F.P.6
-
51
-
-
0038311984
-
Prediction of the in vivo interaction between midazolam and macrolides based on in vitro studies using human liver microsomes
-
Ito K, Ogihara K, Kanamitsu S-I, Itoh T. Prediction of the in vivo interaction between midazolam and macrolides based on in vitro studies using human liver microsomes. Drug Metab Dispos 2003; 31: 945-54.
-
(2003)
Drug Metab Dispos
, vol.31
, pp. 945-954
-
-
Ito, K.1
Ogihara, K.2
Kanamitsu, S.-I.3
Itoh, T.4
-
52
-
-
33644827609
-
Quantitative prediction of macrolide drug-drug interaction potential from in vitro studies using testosterone as the human cytochrome P4503A substrate
-
Polasek TM, Miners JO. Quantitative prediction of macrolide drug-drug interaction potential from in vitro studies using testosterone as the human cytochrome P4503A substrate. Pharmacokinet Dispos 2006; 62: 203-8.
-
(2006)
Pharmacokinet Dispos
, vol.62
, pp. 203-208
-
-
Polasek, T.M.1
Miners, J.O.2
-
53
-
-
0027477751
-
A potentially hazardous interaction between erythromycin and midazolam
-
Oikkola K, Aranko K, Luurila H, Hiller A, Saarnivaara L, Himberg J-J, et al. A potentially hazardous interaction between erythromycin and midazolam. Clin Pharmacol Ther 1993; 53: 298-305.
-
(1993)
Clin Pharmacol Ther
, vol.53
, pp. 298-305
-
-
Oikkola, K.1
Aranko, K.2
Luurila, H.3
Hiller, A.4
Saarnivaara, L.5
Himberg, J.-J.6
-
54
-
-
0029813001
-
Interaction between midazolam and clarithromycin: Comparison with azithromycin
-
Yeates RA, Laufen H, Zimmerman T. Interaction between midazolam and clarithromycin: Comparison with azithromycin. Int J Clin Pharm Ther 1996; 34: 400-5.
-
(1996)
Int J Clin Pharm Ther
, vol.34
, pp. 400-405
-
-
Yeates, R.A.1
Laufen, H.2
Zimmerman, T.3
-
55
-
-
55549119262
-
Assessing and minimizing time-dependent inhibition of cytochrome P450 3A in drug discovery: A case study with melanocortin 4 receptor agonists
-
Tang W, Stearns RA, Wang RW, Miller RR, Chen Q, Ngui J, et al. Assessing and minimizing time-dependent inhibition of cytochrome P450 3A in drug discovery: A case study with melanocortin 4 receptor agonists. Xenobiotica 2008; 38: 1437-57.
-
(2008)
Xenobiotica
, vol.38
, pp. 1437-1457
-
-
Tang, W.1
Stearns, R.A.2
Wang, R.W.3
Miller, R.R.4
Chen, Q.5
Ngui, J.6
-
56
-
-
38549165867
-
Importance of drug transporters in pharmacokinetics and drug safety
-
Ward P. Importance of drug transporters in pharmacokinetics and drug safety. Toxicol Mech Method 2008; 18: 1-10.
-
(2008)
Toxicol Mech Method
, vol.18
, pp. 1-10
-
-
Ward, P.1
-
57
-
-
33644692006
-
Scientific perspectives on drug transporters and their role in drug interactions
-
Zhang L, Strong JM, Qiu W, Lesko LJ, Huang SM. Scientific perspectives on drug transporters and their role in drug interactions. Mol Pharmaceut 2006; 3: 62-9.
-
(2006)
Mol Pharmaceut
, vol.3
, pp. 62-69
-
-
Zhang, L.1
Strong, J.M.2
Qiu, W.3
Lesko, L.J.4
Huang, S.M.5
-
58
-
-
48749084803
-
-
Zhang L, Zhang Y(D), Strong JM, Reynolds KD, Huang S-M. A regulatory viewpoint on transporter-based drug interactions. Xenobiotica 2008; 38: 709-24.
-
Zhang L, Zhang Y(D), Strong JM, Reynolds KD, Huang S-M. A regulatory viewpoint on transporter-based drug interactions. Xenobiotica 2008; 38: 709-24.
-
-
-
-
59
-
-
20444480695
-
Imaging P-glycoprotein transport activity at the human blood-brain barrier with positron emission tomography
-
Sasongko L, Link JM, Muzi M, Mankoff DA, Yang X, Collier AC, et al. Imaging P-glycoprotein transport activity at the human blood-brain barrier with positron emission tomography. Clin Pharmacol Ther 2005; 77: 503-14.
-
(2005)
Clin Pharmacol Ther
, vol.77
, pp. 503-514
-
-
Sasongko, L.1
Link, J.M.2
Muzi, M.3
Mankoff, D.A.4
Yang, X.5
Collier, A.C.6
-
60
-
-
33847056693
-
Attenuating pregnane X receptor (PXR) activation: A molecular modeling approach
-
Gao Y-D, Olson SH, Balkovec JM, Zhu Y, ROYO I, Yabut J, et al. Attenuating pregnane X receptor (PXR) activation: A molecular modeling approach. Xenobiotica 2007; 37: 124-38.
-
(2007)
Xenobiotica
, vol.37
, pp. 124-138
-
-
Gao, Y.-D.1
Olson, S.H.2
Balkovec, J.M.3
Zhu, Y.4
ROYO, I.5
Yabut, J.6
-
61
-
-
0032906888
-
Disposition of ivermectin and cyclosporin A in CF-1 mice deficient in Mdr1a P-glycoprotein
-
Kwei GY, Alvaro RF, Chen Q, Jenkins HJ, Hop CEAC, Keohane CA, et al. Disposition of ivermectin and cyclosporin A in CF-1 mice deficient in Mdr1a P-glycoprotein. Drug Metab Dispos 1999; 27: 581-7.
-
(1999)
Drug Metab Dispos
, vol.27
, pp. 581-587
-
-
Kwei, G.Y.1
Alvaro, R.F.2
Chen, Q.3
Jenkins, H.J.4
Hop, C.E.A.C.5
Keohane, C.A.6
-
62
-
-
0033833430
-
Increased drug delivery to the brain by P-glycoprotein inhibition
-
Sadeque AJM, Wandel C, He H, Shah S, Wood AJJ. Increased drug delivery to the brain by P-glycoprotein inhibition. Clin Pharmacol Ther 2000; 68: 231-7.
-
(2000)
Clin Pharmacol Ther
, vol.68
, pp. 231-237
-
-
Sadeque, A.J.M.1
Wandel, C.2
He, H.3
Shah, S.4
Wood, A.J.J.5
-
63
-
-
0034888307
-
Affinity for the P-glycoprotein efflux pump at the blood-brain barrier may explain the lack of CNS-side-effects of modern antihistamines
-
Chrishty M, Reichel A, Siva J, Abbott NJ. Affinity for the P-glycoprotein efflux pump at the blood-brain barrier may explain the lack of CNS-side-effects of modern antihistamines. J Drug Target 2001; 9: 223-8.
-
(2001)
J Drug Target
, vol.9
, pp. 223-228
-
-
Chrishty, M.1
Reichel, A.2
Siva, J.3
Abbott, N.J.4
-
64
-
-
0036896304
-
Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs
-
Doan KMM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, et al. Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp ther 2002; 303: 1029-37.
-
(2002)
J Pharmacol Exp ther
, vol.303
, pp. 1029-1037
-
-
Doan, K.M.M.1
Humphreys, J.E.2
Webster, L.O.3
Wring, S.A.4
Shampine, L.J.5
Serabjit-Singh, C.J.6
-
65
-
-
1442301563
-
How significant is the role of P-glycoprotein in drug absorption and brain uptake?
-
Lin JH. How significant is the role of P-glycoprotein in drug absorption and brain uptake? Drug Today 2004; 40: 5-22.
-
(2004)
Drug Today
, vol.40
, pp. 5-22
-
-
Lin, J.H.1
-
66
-
-
42449100856
-
Progress in brain penetration evaluation in drug discovery and development
-
Liu X, Chen C, Smith BJ. Progress in brain penetration evaluation in drug discovery and development. J Pharmacol Exp Ther 2008; 325: 349-56.
-
(2008)
J Pharmacol Exp Ther
, vol.325
, pp. 349-356
-
-
Liu, X.1
Chen, C.2
Smith, B.J.3
-
67
-
-
33644692007
-
P-Glycoprotein recognition of substrates and circumvention through rational drug design
-
Raub TJ. P-Glycoprotein recognition of substrates and circumvention through rational drug design. Mol Pharmaceut 2005; 3: 3-25.
-
(2005)
Mol Pharmaceut
, vol.3
, pp. 3-25
-
-
Raub, T.J.1
-
68
-
-
0037091106
-
Preferential efflux by P-glycoprotein, but not MRP1, of compounds containing a free electron donor amine
-
Salerno M, Przewloka T, Fokt I, Priebe W, Garnier-Suillerot A. Preferential efflux by P-glycoprotein, but not MRP1, of compounds containing a free electron donor amine. Biochem Pharmacol 2002; 63: 1471-9.
-
(2002)
Biochem Pharmacol
, vol.63
, pp. 1471-1479
-
-
Salerno, M.1
Przewloka, T.2
Fokt, I.3
Priebe, W.4
Garnier-Suillerot, A.5
-
69
-
-
34247379910
-
Kinesin spindle protein (KSP) inhibitor. Part V: Discovery of 2-propyamino-2,4-diary-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by β-fluorination to overcome cellular efflux by P-glycoprotein
-
Cox CD, Breslin MJ, Whitman DB, Coleman PJ, Garbaccio RM, Fraley ME, et al. Kinesin spindle protein (KSP) inhibitor. Part V: Discovery of 2-propyamino-2,4-diary-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by β-fluorination to overcome cellular efflux by P-glycoprotein. Bioorg Med Chem Lett 2007; 17: 2697-702.
-
(2007)
Bioorg Med Chem Lett
, vol.17
, pp. 2697-2702
-
-
Cox, C.D.1
Breslin, M.J.2
Whitman, D.B.3
Coleman, P.J.4
Garbaccio, R.M.5
Fraley, M.E.6
-
70
-
-
4744353974
-
Principles and applicability of CSF sampling for the assessment of CNS drug delivery and pharmacokinetics
-
Shen DD, Artru AA, Adkison KK. Principles and applicability of CSF sampling for the assessment of CNS drug delivery and pharmacokinetics. Adv Drug Deliv Rev 2004; 56: 1825-57.
-
(2004)
Adv Drug Deliv Rev
, vol.56
, pp. 1825-1857
-
-
Shen, D.D.1
Artru, A.A.2
Adkison, K.K.3
-
71
-
-
38849136513
-
CSF as a surrogate for assessing CNS exposure: An industrial perspective
-
Lin JH. CSF as a surrogate for assessing CNS exposure: An industrial perspective. Curr Drug Metab 2008; 9: 46-59.
-
(2008)
Curr Drug Metab
, vol.9
, pp. 46-59
-
-
Lin, J.H.1
-
72
-
-
10744233020
-
Effect of P-glycoprotein-mediated efflux on cerebrospinal fluid/plasma concentration ratio
-
Ohe T, Sato M, Tanaka S, Fujino N, Hata M, Shibata Y, et al. Effect of P-glycoprotein-mediated efflux on cerebrospinal fluid/plasma concentration ratio. Drug Metab Dispos 2003; 31: 1251-4.
-
(2003)
Drug Metab Dispos
, vol.31
, pp. 1251-1254
-
-
Ohe, T.1
Sato, M.2
Tanaka, S.3
Fujino, N.4
Hata, M.5
Shibata, Y.6
-
73
-
-
0031663301
-
Rifampin concentrations in various compartments of the human brain: A novel method for determining drug levels in the cerebral extracellular space. Antimicrob
-
Mindermann T, Zimmerli W, Gratzl O. Rifampin concentrations in various compartments of the human brain: A novel method for determining drug levels in the cerebral extracellular space. Antimicrob Agents Chemother 1998; 42: 2626-9.
-
(1998)
Agents Chemother
, vol.42
, pp. 2626-2629
-
-
Mindermann, T.1
Zimmerli, W.2
Gratzl, O.3
-
74
-
-
0032563719
-
Changes in blood-brain barrier permeability associated with insertion of brain cannulas and microdialysis probes
-
Groothuis DR, Ward S, Schlageter KE, Itskovich AC, Schwerin SC, Allen CV, et al. Changes in blood-brain barrier permeability associated with insertion of brain cannulas and microdialysis probes. Brain Res 1998; 803: 218-30.
-
(1998)
Brain Res
, vol.803
, pp. 218-230
-
-
Groothuis, D.R.1
Ward, S.2
Schlageter, K.E.3
Itskovich, A.C.4
Schwerin, S.C.5
Allen, C.V.6
-
75
-
-
34648813134
-
High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery
-
Wan, H, Rehngren M, Giordanetto F, Bergstrom F, Tunek A. High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery. J Med Chem 2007; 50: 4606-15.
-
(2007)
J Med Chem
, vol.50
, pp. 4606-4615
-
-
Wan, H.1
Rehngren, M.2
Giordanetto, F.3
Bergstrom, F.4
Tunek, A.5
-
76
-
-
38749088304
-
Cytochrome P450 expression and regulation in CYP3A4/CYP2D6 double transgenic humanized mice
-
Felmlee MA, Lon H-K, Gonzalez FJ, Yu A-M. Cytochrome P450 expression and regulation in CYP3A4/CYP2D6 double transgenic humanized mice. Drug Metab Dispos 2008; 36: 435-41.
-
(2008)
Drug Metab Dispos
, vol.36
, pp. 435-441
-
-
Felmlee, M.A.1
Lon, H.-K.2
Gonzalez, F.J.3
Yu, A.-M.4
-
77
-
-
36048953756
-
CYP3A4 and pregnane X receptor humanized mice
-
Gonzalez FJ. CYP3A4 and pregnane X receptor humanized mice. J Biochem Mol Toxicol 2007; 27: 158-62.
-
(2007)
J Biochem Mol Toxicol
, vol.27
, pp. 158-162
-
-
Gonzalez, F.J.1
-
80
-
-
4344574035
-
Near completely humanized liver in mice shows human-type metabolic responses to drugs
-
Tateno C, Yoshizane Y, Saito N, Kataoka M, Utoh R, Yamasaki C, et al. Near completely humanized liver in mice shows human-type metabolic responses to drugs. Am J Pathol 2004; 165: 901-12.
-
(2004)
Am J Pathol
, vol.165
, pp. 901-912
-
-
Tateno, C.1
Yoshizane, Y.2
Saito, N.3
Kataoka, M.4
Utoh, R.5
Yamasaki, C.6
-
81
-
-
34447568362
-
Humanization of excretory pathway in chimeric mice with humanized liver
-
Okumura H, Katoh M, Sawada T, Nakajima M, Soene Y, Yabuuchi H, et al. Humanization of excretory pathway in chimeric mice with humanized liver. Toxicol Sci 2007; 97: 533-8.
-
(2007)
Toxicol Sci
, vol.97
, pp. 533-538
-
-
Okumura, H.1
Katoh, M.2
Sawada, T.3
Nakajima, M.4
Soene, Y.5
Yabuuchi, H.6
-
82
-
-
47749137002
-
Applications and limitations of genetically modified mouse models in drug discovery and development
-
Lin JH. Applications and limitations of genetically modified mouse models in drug discovery and development. Curr Drug Metab 2008; 9: 419-38.
-
(2008)
Curr Drug Metab
, vol.9
, pp. 419-438
-
-
Lin, J.H.1
-
83
-
-
34648834682
-
The third dimension bridges the gap between cell culture and live tissue
-
Pampaloni F, Reynaud EG, Stelzer EH. The third dimension bridges the gap between cell culture and live tissue. Nat Rev Mol Cell Biol 2007; 8: 839-45.
-
(2007)
Nat Rev Mol Cell Biol
, vol.8
, pp. 839-845
-
-
Pampaloni, F.1
Reynaud, E.G.2
Stelzer, E.H.3
-
84
-
-
38349143408
-
Evaluating drug efficacy and toxicology in three dimensions: Using synthetic extracellular matrices in drug discovery
-
Prestwich GD. Evaluating drug efficacy and toxicology in three dimensions: Using synthetic extracellular matrices in drug discovery. Accounts Chem Res 2008; 41: 139-48.
-
(2008)
Accounts Chem Res
, vol.41
, pp. 139-148
-
-
Prestwich, G.D.1
-
85
-
-
34547737909
-
3-D Culture in synthetic extracellular matrices: New tissue models for drug toxicology and cancer drug discovery
-
Prestwich GD, Liu Y, Yu B, Shu XZ, Scott A. 3-D Culture in synthetic extracellular matrices: New tissue models for drug toxicology and cancer drug discovery. Advan Enzyme Regul 2007; 47: 196-207.
-
(2007)
Advan Enzyme Regul
, vol.47
, pp. 196-207
-
-
Prestwich, G.D.1
Liu, Y.2
Yu, B.3
Shu, X.Z.4
Scott, A.5
-
86
-
-
30344448556
-
Knocking down transport: Applications of RNA interference in the study of drug transport proteins
-
Tian X, Zhang P, Zamek-Gliszczynski MJ, Brouwer KLR. Knocking down transport: Applications of RNA interference in the study of drug transport proteins. Drug Metab Rev 2005; 37: 705-23.
-
(2005)
Drug Metab Rev
, vol.37
, pp. 705-723
-
-
Tian, X.1
Zhang, P.2
Zamek-Gliszczynski, M.J.3
Brouwer, K.L.R.4
-
87
-
-
35348908290
-
Small interfering RNA in drug metabolism and transport
-
Yu A-M. Small interfering RNA in drug metabolism and transport. Curr Drug Metab 2007; 8: 700-8.
-
(2007)
Curr Drug Metab
, vol.8
, pp. 700-708
-
-
Yu, A.-M.1
-
88
-
-
34848828243
-
Broad but distinct role of pregnane X receptor on the expression of individual cytochrome P450s in human hepatocytes
-
Kojima K, Nagata K, Matsubara T, Yamazoe Y. Broad but distinct role of pregnane X receptor on the expression of individual cytochrome P450s in human hepatocytes. Drug Metab Pharmacokinet 2007; 22: 276-86.
-
(2007)
Drug Metab Pharmacokinet
, vol.22
, pp. 276-286
-
-
Kojima, K.1
Nagata, K.2
Matsubara, T.3
Yamazoe, Y.4
-
89
-
-
33746070441
-
Intravenously administered short interfering RNA accumulates in the kidney and selectively suppresses gene function in renal proximal tubules
-
van de Water FH, Boerman OC, Wouterse AC, Peters JGP, Russel FGM, Masereeuw R. Intravenously administered short interfering RNA accumulates in the kidney and selectively suppresses gene function in renal proximal tubules. Drug Metab Dispos 2006; 1393-7.
-
(2006)
Drug Metab Dispos
, pp. 1393-1397
-
-
van de Water, F.H.1
Boerman, O.C.2
Wouterse, A.C.3
Peters, J.G.P.4
Russel, F.G.M.5
Masereeuw, R.6
-
90
-
-
50249099700
-
The hERG potassium channel and hERG screening for drug-induced torsades de pointes
-
Hancox JC, McPate MJ, El Harchi A, Zhang YH. The hERG potassium channel and hERG screening for drug-induced torsades de pointes. Pharmacol Ther 2008; 119(2): 118-32.
-
(2008)
Pharmacol Ther
, vol.119
, Issue.2
, pp. 118-132
-
-
Hancox, J.C.1
McPate, M.J.2
El Harchi, A.3
Zhang, Y.H.4
-
91
-
-
60749092901
-
Current drug metabolism
-
Kerns EH. Current drug metabolism. Curr Drug Metab 2008; 9(9): 845-6
-
(2008)
Curr Drug Metab
, vol.9
, Issue.9
, pp. 845-846
-
-
Kerns, E.H.1
-
92
-
-
39749120717
-
Pharmacokinetics in drug discovery
-
Ruiz-Garcia A, Bermejo M, Moss A, Casabo VG. Pharmacokinetics in drug discovery. J Pharm Sci 2008; 97(2): 654-90.
-
(2008)
J Pharm Sci
, vol.97
, Issue.2
, pp. 654-690
-
-
Ruiz-Garcia, A.1
Bermejo, M.2
Moss, A.3
Casabo, V.G.4
|