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Items: 15


Clearance Prediction of Targeted Covalent Inhibitors by In Vitro-In Vivo Extrapolation of Hepatic and Extrahepatic Clearance Mechanisms.

Leung L, Yang X, Strelevitz TJ, Montgomery J, Brown MF, Zientek MA, Banfield C, Gilbert AM, Thorarensen A, Dowty ME.

Drug Metab Dispos. 2017 Jan;45(1):1-7. Epub 2016 Oct 26.


Undesired versus designed enzymatic cleavage of linkers for liver targeting.

Chirapu SR, Bauman JN, Eng H, Goosen TC, Strelevitz TJ, Sinha SC, Dow RL, Finn MG.

Bioorg Med Chem Lett. 2014 Feb 15;24(4):1144-7. doi: 10.1016/j.bmcl.2013.12.126. Epub 2014 Jan 8.


Mechanistic insights from comparing intrinsic clearance values between human liver microsomes and hepatocytes to guide drug design.

Di L, Keefer C, Scott DO, Strelevitz TJ, Chang G, Bi YA, Lai Y, Duckworth J, Fenner K, Troutman MD, Obach RS.

Eur J Med Chem. 2012 Nov;57:441-8. doi: 10.1016/j.ejmech.2012.06.043. Epub 2012 Jul 16.


Hydralazine as a selective probe inactivator of aldehyde oxidase in human hepatocytes: estimation of the contribution of aldehyde oxidase to metabolic clearance.

Strelevitz TJ, Orozco CC, Obach RS.

Drug Metab Dispos. 2012 Jul;40(7):1441-8. doi: 10.1124/dmd.112.045195. Epub 2012 Apr 20.


Deuterium isotope effects on drug pharmacokinetics. I. System-dependent effects of specific deuteration with aldehyde oxidase cleared drugs.

Sharma R, Strelevitz TJ, Gao H, Clark AJ, Schildknegt K, Obach RS, Ripp SL, Spracklin DK, Tremaine LM, Vaz AD.

Drug Metab Dispos. 2012 Mar;40(3):625-34. doi: 10.1124/dmd.111.042770. Epub 2011 Dec 21.


Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection.

Flanagan ME, Blumenkopf TA, Brissette WH, Brown MF, Casavant JM, Shang-Poa C, Doty JL, Elliott EA, Fisher MB, Hines M, Kent C, Kudlacz EM, Lillie BM, Magnuson KS, McCurdy SP, Munchhof MJ, Perry BD, Sawyer PS, Strelevitz TJ, Subramanyam C, Sun J, Whipple DA, Changelian PS.

J Med Chem. 2010 Dec 23;53(24):8468-84. doi: 10.1021/jm1004286. Epub 2010 Nov 24.


Discovery of azetidinyl ketolides for the treatment of susceptible and multidrug resistant community-acquired respiratory tract infections.

Magee TV, Ripp SL, Li B, Buzon RA, Chupak L, Dougherty TJ, Finegan SM, Girard D, Hagen AE, Falcone MJ, Farley KA, Granskog K, Hardink JR, Huband MD, Kamicker BJ, Kaneko T, Knickerbocker MJ, Liras JL, Marra A, Medina I, Nguyen TT, Noe MC, Obach RS, O'Donnell JP, Penzien JB, Reilly UD, Schafer JR, Shen Y, Stone GG, Strelevitz TJ, Sun J, Tait-Kamradt A, Vaz AD, Whipple DA, Widlicka DW, Wishka DG, Wolkowski JP, Flanagan ME.

J Med Chem. 2009 Dec 10;52(23):7446-57. doi: 10.1021/jm900729s.


Novel CCR1 antagonists with improved metabolic stability.

Brown MF, Avery M, Brissette WH, Chang JH, Colizza K, Conklyn M, DiRico AP, Gladue RP, Kath JC, Krueger SS, Lira PD, Lillie BM, Lundquist GD, Mairs EN, McElroy EB, McGlynn MA, Paradis TJ, Poss CS, Rossulek MI, Shepard RM, Sims J, Strelevitz TJ, Truesdell S, Tylaska LA, Yoon K, Zheng D.

Bioorg Med Chem Lett. 2004 May 3;14(9):2175-9.


Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.

Changelian PS, Flanagan ME, Ball DJ, Kent CR, Magnuson KS, Martin WH, Rizzuti BJ, Sawyer PS, Perry BD, Brissette WH, McCurdy SP, Kudlacz EM, Conklyn MJ, Elliott EA, Koslov ER, Fisher MB, Strelevitz TJ, Yoon K, Whipple DA, Sun J, Munchhof MJ, Doty JL, Casavant JM, Blumenkopf TA, Hines M, Brown MF, Lillie BM, Subramanyam C, Shang-Poa C, Milici AJ, Beckius GE, Moyer JD, Su C, Woodworth TG, Gaweco AS, Beals CR, Littman BH, Fisher DA, Smith JF, Zagouras P, Magna HA, Saltarelli MJ, Johnson KS, Nelms LF, Des Etages SG, Hayes LS, Kawabata TT, Finco-Kent D, Baker DL, Larson M, Si MS, Paniagua R, Higgins J, Holm B, Reitz B, Zhou YJ, Morris RE, O'Shea JJ, Borie DC.

Science. 2003 Oct 31;302(5646):875-8.


Flavin-containing monooxygenase activity in hepatocytes and microsomes: in vitro characterization and in vivo scaling of benzydamine clearance.

Fisher MB, Yoon K, Vaughn ML, Strelevitz TJ, Foti RS.

Drug Metab Dispos. 2002 Oct;30(10):1087-93.


The role of hepatic and extrahepatic UDP-glucuronosyltransferases in human drug metabolism.

Fisher MB, Paine MF, Strelevitz TJ, Wrighton SA.

Drug Metab Rev. 2001 Aug-Nov;33(3-4):273-97. Review.


Disposition and metabolism of the novel macrolide antibiotic CP-163505 in cattle.

Linhares MC, Harran LP, Strelevitz TJ, Gauthier JW, Cole MJ, Hassfurther RL, Risk JE.

J Vet Pharmacol Ther. 1998 Apr;21(2):99-106.


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