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Items: 1 to 50 of 55

1.

In vitro-In vivo extrapolation of key transporter activity at the blood-brain barrier.

Trapa PE, Troutman MD, Lau TY, Wager TT, Maurer TS, Patel NC, West MA, Umland JP, Carlo AA, Feng B, Liras JL.

Drug Metab Dispos. 2019 Jan 25. pii: dmd.118.083279. doi: 10.1124/dmd.118.083279. [Epub ahead of print]

2.

Clearance in Drug Design.

Smith D, Beaumont K, Maurer TS, Di L.

J Med Chem. 2018 Oct 3. doi: 10.1021/acs.jmedchem.8b01263. [Epub ahead of print]

PMID:
30281973
3.

Quantitative Translational Analysis of Brain Kynurenic Acid Modulation via Irreversible Kynurenine Aminotransferase II Inhibition.

Chang C, Fonseca KR, Li C, Horner W, Zawadzke LE, Salafia MA, Welch KA, Strick CA, Campbell BM, Gernhardt SS, Rong H, Sawant-Basak A, Liras J, Dounay A, Tuttle JB, Verhoest P, Maurer TS.

Mol Pharmacol. 2018 Aug;94(2):823-833. doi: 10.1124/mol.118.111625. Epub 2018 May 31.

PMID:
29853495
4.

A Study on Pharmacokinetics of Bosentan with Systems Modeling, Part 1: Translating Systemic Plasma Concentration to Liver Exposure in Healthy Subjects.

Li R, Niosi M, Johnson N, Tess DA, Kimoto E, Lin J, Yang X, Riccardi KA, Ryu S, El-Kattan AF, Maurer TS, Tremaine LM, Di L.

Drug Metab Dispos. 2018 Apr;46(4):346-356. doi: 10.1124/dmd.117.078790. Epub 2018 Jan 12. Erratum in: Drug Metab Dispos. 2018 Apr;46(4):483. Drug Metab Dispos. 2019 Mar;47(3):269.

PMID:
29330218
5.

Relevance of Half-Life in Drug Design.

Smith DA, Beaumont K, Maurer TS, Di L.

J Med Chem. 2018 May 24;61(10):4273-4282. doi: 10.1021/acs.jmedchem.7b00969. Epub 2017 Nov 17.

PMID:
29112446
6.

In Vitro-In Vivo Extrapolation of Intestinal Availability for Carboxylesterase Substrates Using Portal Vein-Cannulated Monkey.

Trapa PE, Beaumont K, Atkinson K, Eng H, King-Ahmad A, Scott DO, Maurer TS, Di L.

J Pharm Sci. 2017 Mar;106(3):898-905. doi: 10.1016/j.xphs.2016.12.001. Epub 2016 Dec 18.

PMID:
27998705
7.

Extended Clearance Classification System (ECCS) informed approach for evaluating investigational drugs as substrates of drug transporters.

Varma MV, El-Kattan AF, Feng B, Steyn SJ, Maurer TS, Scott DO, Rodrigues AD, Tremaine LM.

Clin Pharmacol Ther. 2017 Jul;102(1):33-36. doi: 10.1002/cpt.595. Epub 2017 Feb 3. No abstract available.

PMID:
27984654
8.

Passive drug permeation through membranes and cellular distribution.

Scott DO, Ghosh A, Di L, Maurer TS.

Pharmacol Res. 2017 Mar;117:94-102. doi: 10.1016/j.phrs.2016.11.028. Epub 2016 Nov 24. Review.

PMID:
27890815
9.

Projecting ADME Behavior and Drug-Drug Interactions in Early Discovery and Development: Application of the Extended Clearance Classification System.

El-Kattan AF, Varma MV, Steyn SJ, Scott DO, Maurer TS, Bergman A.

Pharm Res. 2016 Dec;33(12):3021-3030. Epub 2016 Sep 12.

PMID:
27620173
10.

Evaluation of a Mathematical Model of Rat Body Weight Regulation in Application to Caloric Restriction and Drug Treatment Studies.

Selimkhanov J, Thompson WC, Patterson TA, Hadcock JR, Scott DO, Maurer TS, Musante CJ.

PLoS One. 2016 May 26;11(5):e0155674. doi: 10.1371/journal.pone.0155674. eCollection 2016.

11.

Model-Based Assessment of Plasma Citrate Flux Into the Liver: Implications for NaCT as a Therapeutic Target.

Li Z, Erion DM, Maurer TS.

CPT Pharmacometrics Syst Pharmacol. 2016 Mar;5(3):132-9. doi: 10.1002/psp4.12062. Epub 2016 Mar 4.

12.

Does the Systemic Plasma Profile Inform the Liver Profile? Analysis Using a Physiologically Based Pharmacokinetic Model and Individual Compounds.

Li R, Maurer TS, Sweeney K, Barton HA.

AAPS J. 2016 May;18(3):746-56. doi: 10.1208/s12248-016-9895-0. Epub 2016 Mar 7.

13.

Rapid Method To Determine Intracellular Drug Concentrations in Cellular Uptake Assays: Application to Metformin in Organic Cation Transporter 1-Transfected Human Embryonic Kidney 293 Cells.

Chien HC, Zur AA, Maurer TS, Yee SW, Tolsma J, Jasper P, Scott DO, Giacomini KM.

Drug Metab Dispos. 2016 Mar;44(3):356-64. doi: 10.1124/dmd.115.066647. Epub 2015 Dec 23.

14.

Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.

Ruggeri RB, Buckbinder L, Bagley SW, Carpino PA, Conn EL, Dowling MS, Fernando DP, Jiao W, Kung DW, Orr ST, Qi Y, Rocke BN, Smith A, Warmus JS, Zhang Y, Bowles D, Widlicka DW, Eng H, Ryder T, Sharma R, Wolford A, Okerberg C, Walters K, Maurer TS, Zhang Y, Bonin PD, Spath SN, Xing G, Hepworth D, Ahn K, Kalgutkar AS.

J Med Chem. 2015 Nov 12;58(21):8513-28. doi: 10.1021/acs.jmedchem.5b00963. Epub 2015 Oct 28.

PMID:
26509551
15.

A Mechanistic Pharmacokinetic Model for Liver Transporter Substrates Under Liver Cirrhosis Conditions.

Li R, Barton HA, Maurer TS.

CPT Pharmacometrics Syst Pharmacol. 2015 Jun;4(6):338-49. doi: 10.1002/psp4.39. Epub 2015 Jun 1.

16.

Volume of Distribution in Drug Design.

Smith DA, Beaumont K, Maurer TS, Di L.

J Med Chem. 2015 Aug 13;58(15):5691-8. doi: 10.1021/acs.jmedchem.5b00201. Epub 2015 Apr 1.

PMID:
25799158
17.

PF-1355, a mechanism-based myeloperoxidase inhibitor, prevents immune complex vasculitis and anti-glomerular basement membrane glomerulonephritis.

Zheng W, Warner R, Ruggeri R, Su C, Cortes C, Skoura A, Ward J, Ahn K, Kalgutkar A, Sun D, Maurer TS, Bonin PD, Okerberg C, Bobrowski W, Kawabe T, Zhang Y, Coskran T, Bell S, Kapoor B, Johnson K, Buckbinder L.

J Pharmacol Exp Ther. 2015 May;353(2):288-98. doi: 10.1124/jpet.114.221788. Epub 2015 Feb 19.

PMID:
25698787
18.

Toward Prospective Prediction of Pharmacokinetics in OATP1B1 Genetic Variant Populations.

Li R, Barton HA, Maurer TS.

CPT Pharmacometrics Syst Pharmacol. 2014 Dec 10;3:e151. doi: 10.1038/psp.2014.50.

19.

Physiologically based pharmacokinetic prediction of telmisartan in human.

Li R, Ghosh A, Maurer TS, Kimoto E, Barton HA.

Drug Metab Dispos. 2014 Oct;42(10):1646-55. doi: 10.1124/dmd.114.058461. Epub 2014 Aug 4.

PMID:
25092714
20.

Toward a unified model of passive drug permeation II: the physiochemical determinants of unbound tissue distribution with applications to the design of hepatoselective glucokinase activators.

Ghosh A, Maurer TS, Litchfield J, Varma MV, Rotter C, Scialis R, Feng B, Tu M, Guimaraes CR, Scott DO.

Drug Metab Dispos. 2014 Oct;42(10):1599-610. doi: 10.1124/dmd.114.058032. Epub 2014 Jul 14.

PMID:
25024402
21.

A "middle-out" approach to human pharmacokinetic predictions for OATP substrates using physiologically-based pharmacokinetic modeling.

Li R, Barton HA, Yates PD, Ghosh A, Wolford AC, Riccardi KA, Maurer TS.

J Pharmacokinet Pharmacodyn. 2014 Jun;41(3):197-209. doi: 10.1007/s10928-014-9357-1. Epub 2014 Apr 10.

PMID:
24718648
22.

Towards a unified model of passive drug permeation I: origins of the unstirred water layer with applications to ionic permeation.

Ghosh A, Scott DO, Maurer TS.

Eur J Pharm Sci. 2014 Feb 14;52:109-24. doi: 10.1016/j.ejps.2013.10.004. Epub 2013 Nov 7.

PMID:
24211511
23.

PF-03882845, a non-steroidal mineralocorticoid receptor antagonist, prevents renal injury with reduced risk of hyperkalemia in an animal model of nephropathy.

Orena S, Maurer TS, She L, Eudy R, Bernardo V, Dash D, Loria P, Banker ME, Tugnait M, Okerberg CV, Qian J, Boustany-Kari CM.

Front Pharmacol. 2013 Oct 14;4:115. doi: 10.3389/fphar.2013.00115. eCollection 2013.

24.

Impact of recovery on fraction unbound using equilibrium dialysis.

Di L, Umland JP, Trapa PE, Maurer TS.

J Pharm Sci. 2012 Mar;101(3):1327-35. doi: 10.1002/jps.23013. Epub 2011 Dec 9.

PMID:
22161810
25.

Pharmacodynamic model of sodium-glucose transporter 2 (SGLT2) inhibition: implications for quantitative translational pharmacology.

Maurer TS, Ghosh A, Haddish-Berhane N, Sawant-Basak A, Boustany-Kari CM, She L, Leininger MT, Zhu T, Tugnait M, Yang X, Kimoto E, Mascitti V, Robinson RP.

AAPS J. 2011 Dec;13(4):576-84. doi: 10.1208/s12248-011-9297-2. Epub 2011 Aug 26.

26.

Quantitative PK-PD model-based translational pharmacology of a novel kappa opioid receptor antagonist between rats and humans.

Chang C, Byon W, Lu Y, Jacobsen LK, Badura LL, Sawant-Basak A, Miller E, Liu J, Grimwood S, Wang EQ, Maurer TS.

AAPS J. 2011 Dec;13(4):565-75. doi: 10.1208/s12248-011-9296-3. Epub 2011 Aug 17.

27.

Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.

Mascitti V, Maurer TS, Robinson RP, Bian J, Boustany-Kari CM, Brandt T, Collman BM, Kalgutkar AS, Klenotic MK, Leininger MT, Lowe A, Maguire RJ, Masterson VM, Miao Z, Mukaiyama E, Patel JD, Pettersen JC, Préville C, Samas B, She L, Sobol Z, Steppan CM, Stevens BD, Thuma BA, Tugnait M, Zeng D, Zhu T.

J Med Chem. 2011 Apr 28;54(8):2952-60. doi: 10.1021/jm200049r. Epub 2011 Mar 30.

PMID:
21449606
28.

Pharmacodynamic model of parathyroid hormone modulation by a negative allosteric modulator of the calcium-sensing receptor.

Abraham AK, Maurer TS, Kalgutkar AS, Gao X, Li M, Healy DR, Petersen DN, Griffith DA, Mager DE.

AAPS J. 2011 Jun;13(2):265-73. doi: 10.1208/s12248-011-9266-9. Epub 2011 Mar 25.

29.

Discovery and evaluation of pyrazolo[1,5-a]pyrimidines as neuropeptide Y1 receptor antagonists.

Griffith DA, Hargrove DM, Maurer TS, Blum CA, De Lombaert S, Inthavongsay JK, Klade LE, Mack CM, Rose CR, Sanders MJ, Carpino PA.

Bioorg Med Chem Lett. 2011 May 1;21(9):2641-5. doi: 10.1016/j.bmcl.2010.12.116. Epub 2011 Jan 7.

PMID:
21295475
30.

Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of obesity.

Elliott RL, Cameron KO, Chin JE, Bartlett JA, Beretta EE, Chen Y, Jardine Pda S, Dubins JS, Gillaspy ML, Hargrove DM, Kalgutkar AS, LaFlamme JA, Lame ME, Martin KA, Maurer TS, Nardone NA, Oliver RM, Scott DO, Sun D, Swick AG, Trebino CE, Zhang Y.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6797-801. doi: 10.1016/j.bmcl.2010.08.115. Epub 2010 Sep 28.

PMID:
20851601
31.

Metabolism-guided design of short-acting calcium-sensing receptor antagonists.

Southers JA, Bauman JN, Price DA, Humphries PS, Balan G, Sagal JF, Maurer TS, Zhang Y, Oliver R, Herr M, Healy DR, Li M, Kapinos B, Fate GD, Riccardi KA, Paralkar VM, Brown TA, Kalgutkar AS.

ACS Med Chem Lett. 2010 May 13;1(5):219-23. doi: 10.1021/ml100058w. eCollection 2010 Aug 12.

32.

C-Aryl glycoside inhibitors of SGLT2: Exploration of sugar modifications including C-5 spirocyclization.

Robinson RP, Mascitti V, Boustany-Kari CM, Carr CL, Foley PM, Kimoto E, Leininger MT, Lowe A, Klenotic MK, Macdonald JI, Maguire RJ, Masterson VM, Maurer TS, Miao Z, Patel JD, Préville C, Reese MR, She L, Steppan CM, Thuma BA, Zhu T.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1569-72. doi: 10.1016/j.bmcl.2010.01.075. Epub 2010 Jan 21.

PMID:
20149653
33.

Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity.

Liu KK, Cornelius P, Patterson TA, Zeng Y, Santucci S, Tomlinson E, Gibbons C, Maurer TS, Marala R, Brown J, Kong JX, Lee E, Werner W, Wenzel Z, Vage C.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):266-71. doi: 10.1016/j.bmcl.2009.10.112. Epub 2009 Oct 30.

PMID:
19914063
34.

Short-acting 5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3H)-one derivatives as orally-active calcium-sensing receptor antagonists.

Didiuk MT, Griffith DA, Benbow JW, Liu KK, Walker DP, Bi FC, Morris J, Guzman-Perez A, Gao H, Bechle BM, Kelley RM, Yang X, Dirico K, Ahmed S, Hungerford W, DiBrinno J, Zawistoski MP, Bagley SW, Li J, Zeng Y, Santucci S, Oliver R, Corbett M, Olson T, Chen C, Li M, Paralkar VM, Riccardi KA, Healy DR, Kalgutkar AS, Maurer TS, Nguyen HT, Frederick KS.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4555-9. doi: 10.1016/j.bmcl.2009.07.004. Epub 2009 Jul 8.

PMID:
19625189
35.
36.

Mechanism-based pharmacokinetic/pharmacodynamic model of parathyroid hormone-calcium homeostasis in rats and humans.

Abraham AK, Mager DE, Gao X, Li M, Healy DR, Maurer TS.

J Pharmacol Exp Ther. 2009 Jul;330(1):169-78. doi: 10.1124/jpet.109.152033. Epub 2009 Apr 22.

PMID:
19386792
37.

Prediction of human pharmacokinetics from preclinical information: comparative accuracy of quantitative prediction approaches.

Hosea NA, Collard WT, Cole S, Maurer TS, Fang RX, Jones H, Kakar SM, Nakai Y, Smith BJ, Webster R, Beaumont K.

J Clin Pharmacol. 2009 May;49(5):513-33. doi: 10.1177/0091270009333209. Epub 2009 Mar 19.

PMID:
19299532
38.

In silico modeling of nonspecific binding to human liver microsomes.

Gao H, Yao L, Mathieu HW, Zhang Y, Maurer TS, Troutman MD, Scott DO, Ruggeri RB, Lin J.

Drug Metab Dispos. 2008 Oct;36(10):2130-5. doi: 10.1124/dmd.107.020131. Epub 2008 Jul 7.

PMID:
18606744
39.

A combined model for predicting CYP3A4 clinical net drug-drug interaction based on CYP3A4 inhibition, inactivation, and induction determined in vitro.

Fahmi OA, Maurer TS, Kish M, Cardenas E, Boldt S, Nettleton D.

Drug Metab Dispos. 2008 Aug;36(8):1698-708. doi: 10.1124/dmd.107.018663. Epub 2008 May 19. Erratum in: Drug Metab Dispos. 2008 Sep;36(9):1975.

PMID:
18490437
40.

Discovery of potent and orally bioavailable heterocycle-based beta3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity.

Lafontaine JA, Day RF, Dibrino J, Hadcock JR, Hargrove DM, Linhares M, Martin KA, Maurer TS, Nardone NA, Tess DA, Dasilva-Jardine P.

Bioorg Med Chem Lett. 2007 Sep 15;17(18):5245-50. Epub 2007 Jun 30.

PMID:
17632003
42.

Genotoxicity of 2-(3-chlorobenzyloxy)-6-(piperazinyl)pyrazine, a novel 5-hydroxytryptamine2c receptor agonist for the treatment of obesity: role of metabolic activation.

Kalgutkar AS, Dalvie DK, Aubrecht J, Smith EB, Coffing SL, Cheung JR, Vage C, Lame ME, Chiang P, McClure KF, Maurer TS, Coelho RV Jr, Soliman VF, Schildknegt K.

Drug Metab Dispos. 2007 Jun;35(6):848-58. Epub 2007 Mar 7.

PMID:
17344339
44.

Use of immortalized human hepatocytes to predict the magnitude of clinical drug-drug interactions caused by CYP3A4 induction.

Ripp SL, Mills JB, Fahmi OA, Trevena KA, Liras JL, Maurer TS, de Morais SM.

Drug Metab Dispos. 2006 Oct;34(10):1742-8. Epub 2006 Jul 12.

PMID:
16837568
45.

Relationship between exposure and nonspecific binding of thirty-three central nervous system drugs in mice.

Maurer TS, Debartolo DB, Tess DA, Scott DO.

Drug Metab Dispos. 2005 Jan;33(1):175-81. Epub 2004 Oct 22.

PMID:
15502010
46.

Potent and selective, sulfamide-based human beta 3-adrenergic receptor agonists.

Dow RL, Paight ES, Schneider SR, Hadcock JR, Hargrove DM, Martin KA, Maurer TS, Nardone NA, Tess DA, DaSilva-Jardine P.

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3235-40.

PMID:
15149682
47.

Structure-activity relationship studies on 2-heteroaryl-4-arylimidazoles NPY5 receptor antagonists.

Elliott RL, Oliver RM, LaFlamme JA, Gillaspy ML, Hammond M, Hank RF, Maurer TS, Baker DL, DaSilva-Jardine PA, Stevenson RW, Mack CM, Cassella JV.

Bioorg Med Chem Lett. 2003 Oct 20;13(20):3593-6.

PMID:
14505677
48.

In vitro and in vivo characterization of 3-[2-[6-(2-tert-butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl]benzonitrile hydrochloride salt, a potent and selective NPY5 receptor antagonist.

Elliott RL, Oliver RM, Hammond M, Patterson TA, She L, Hargrove DM, Martin KA, Maurer TS, Kalvass JC, Morgan BP, DaSilva-Jardine PA, Stevenson RW, Mack CM, Cassella JV.

J Med Chem. 2003 Feb 27;46(5):670-3.

PMID:
12593645
49.
50.

Influence of microsomal concentration on apparent intrinsic clearance: implications for scaling in vitro data.

Kalvass JC, Tess DA, Giragossian C, Linhares MC, Maurer TS.

Drug Metab Dispos. 2001 Oct;29(10):1332-6.

PMID:
11560877

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