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Items: 1 to 50 of 84

1.

Organic Anion Transporter 2-Mediated Hepatic Uptake Contributes to the Clearance of High-Permeability-Low-Molecular-Weight Acid and Zwitterion Drugs: Evaluation Using 25 Drugs.

Kimoto E, Mathialagan S, Tylaska L, Niosi M, Lin J, Carlo AA, Tess DA, Varma MVS.

J Pharmacol Exp Ther. 2018 Nov;367(2):322-334. doi: 10.1124/jpet.118.252049. Epub 2018 Aug 22.

PMID:
30135178
2.

Use of physiologically-based pharmacokinetic (PBPK) modeling to evaluate the effect of chronic kidney disease on the disposition of hepatic CYP2C8 and OATP1B drug substrates.

Tan ML, Zhao P, Zhang L, Ho YF, Varma MVS, Neuhoff S, Nolin TD, Galetin A, Huang SM.

Clin Pharmacol Ther. 2018 Aug 3. doi: 10.1002/cpt.1205. [Epub ahead of print]

PMID:
30074626
3.

Quantification of Hepatic Organic Anion Transport Proteins OAT2 and OAT7 in Human Liver Tissue and Primary Hepatocytes.

Vildhede A, Kimoto E, Rodrigues AD, Varma MVS.

Mol Pharm. 2018 Aug 6;15(8):3227-3235. doi: 10.1021/acs.molpharmaceut.8b00320. Epub 2018 Jun 25.

PMID:
29906129
4.

Simultaneous Assessment of Transporter-Mediated Drug-Drug Interactions Using a Probe Drug Cocktail in Cynomolgus Monkey.

Kosa RE, Lazzaro S, Bi YA, Tierney B, Gates D, Modi S, Costales C, Rodrigues AD, Tremaine LM, Varma MV.

Drug Metab Dispos. 2018 Aug;46(8):1179-1189. doi: 10.1124/dmd.118.081794. Epub 2018 Jun 7.

PMID:
29880631
5.

Application of Physiologically Based Pharmacokinetic Modeling in Understanding Bosutinib Drug-Drug Interactions: Importance of Intestinal P-Glycoprotein.

Yamazaki S, Loi CM, Kimoto E, Costales C, Varma MV.

Drug Metab Dispos. 2018 Aug;46(8):1200-1211. doi: 10.1124/dmd.118.080424. Epub 2018 May 8.

PMID:
29739809
6.

Predicting Human Clearance of Organic Anion Transporting Polypeptide Substrates Using Cynomolgus Monkey: In Vitro-In Vivo Scaling of Hepatic Uptake Clearance.

De Bruyn T, Ufuk A, Cantrill C, Kosa RE, Bi YA, Niosi M, Modi S, Rodrigues AD, Tremaine LM, Varma MVS, Galetin A, Houston JB.

Drug Metab Dispos. 2018 Jul;46(7):989-1000. doi: 10.1124/dmd.118.081315. Epub 2018 May 2.

PMID:
29720472
7.

In Vitro-In Vivo Extrapolation of OATP1B-Mediated Drug-Drug Interactions in Cynomolgus Monkey.

Ufuk A, Kosa RE, Gao H, Bi YA, Modi S, Gates D, Rodrigues AD, Tremaine LM, Varma MVS, Houston JB, Galetin A.

J Pharmacol Exp Ther. 2018 Jun;365(3):688-699. doi: 10.1124/jpet.118.247767. Epub 2018 Apr 11.

PMID:
29643253
8.

Navigating Transporter Sciences in Pharmacokinetics Characterization Using the Extended Clearance Classification System.

El-Kattan AF, Varma MVS.

Drug Metab Dispos. 2018 May;46(5):729-739. doi: 10.1124/dmd.117.080044. Epub 2018 Mar 1.

PMID:
29496721
9.

Comparison of Proteomic Quantification Approaches for Hepatic Drug Transporters: Multiplexed Global Quantitation Correlates with Targeted Proteomic Quantitation.

Vildhede A, Nguyen C, Erickson BK, Kunz RC, Jones R, Kimoto E, Bourbonais F, Rodrigues AD, Varma MVS.

Drug Metab Dispos. 2018 May;46(5):692-696. doi: 10.1124/dmd.117.079285. Epub 2018 Feb 8.

PMID:
29439128
10.

Role of Hepatic Organic Anion Transporter 2 in the Pharmacokinetics of R- and S-Warfarin: In Vitro Studies and Mechanistic Evaluation.

Bi YA, Lin J, Mathialagan S, Tylaska L, Callegari E, Rodrigues AD, Varma MVS.

Mol Pharm. 2018 Mar 5;15(3):1284-1295. doi: 10.1021/acs.molpharmaceut.7b01108. Epub 2018 Feb 20.

PMID:
29433307
11.

Organic Anion Transporter 2 Mediates Hepatic Uptake of Tolbutamide, a CYP2C9 Probe Drug.

Bi YA, Mathialagan S, Tylaska L, Fu M, Keefer J, Vildhede A, Costales C, Rodrigues AD, Varma MVS.

J Pharmacol Exp Ther. 2018 Mar;364(3):390-398. doi: 10.1124/jpet.117.245951. Epub 2018 Jan 11.

PMID:
29326367
12.

Molecular properties associated with transporter-mediated drug disposition.

Varma MV, Lai Y, El-Kattan AF.

Adv Drug Deliv Rev. 2017 Jul 1;116:92-99. doi: 10.1016/j.addr.2017.05.014. Epub 2017 May 26. Review.

PMID:
28554577
13.

Hepatobiliary Clearance Prediction: Species Scaling From Monkey, Dog, and Rat, and In Vitro-In Vivo Extrapolation of Sandwich-Cultured Human Hepatocytes Using 17 Drugs.

Kimoto E, Bi YA, Kosa RE, Tremaine LM, Varma MVS.

J Pharm Sci. 2017 Sep;106(9):2795-2804. doi: 10.1016/j.xphs.2017.04.043. Epub 2017 Apr 27.

PMID:
28456723
14.

Transporter-Mediated Disposition, Clinical Pharmacokinetics and Cholestatic Potential of Glyburide and Its Primary Active Metabolites.

Li R, Bi YA, Vildhede A, Scialis RJ, Mathialagan S, Yang X, Marroquin LD, Lin J, Varma MVS.

Drug Metab Dispos. 2017 Jul;45(7):737-747. doi: 10.1124/dmd.116.074815. Epub 2017 Apr 24.

15.

Leveraging of Rifampicin-Dosed Cynomolgus Monkeys to Identify Bile Acid 3-O-Sulfate Conjugates as Potential Novel Biomarkers for Organic Anion-Transporting Polypeptides.

Thakare R, Gao H, Kosa RE, Bi YA, Varma MVS, Cerny MA, Sharma R, Kuhn M, Huang B, Liu Y, Yu A, Walker GS, Niosi M, Tremaine L, Alnouti Y, Rodrigues AD.

Drug Metab Dispos. 2017 Jul;45(7):721-733. doi: 10.1124/dmd.117.075275. Epub 2017 Apr 10.

16.

Erratum to: Reliable Rate Measurements for Active and Passive Hepatic Uptake Using Plated Human Hepatocytes.

Bi YA, Scialis RJ, Lazzaro S, Mathialagan S, Kimoto E, Keefer J, Zhang H, Vildhede AM, Costales C, Rodrigues AD, Tremaine LM, Varma MVS.

AAPS J. 2017 May;19(3):882. doi: 10.1208/s12248-017-0061-0. No abstract available.

PMID:
28233243
17.

Response to "Quantitative Prediction of Drug-Drug Interactions Involving Inhibitory Metabolites by Physiologically Based Pharmacokinetic Models: Is It Worth?"

Templeton IE, Chen Y, Mao J, Lin J, Yu H, Peters S, Shebley M, Varma MV.

CPT Pharmacometrics Syst Pharmacol. 2017 Apr;6(4):227. doi: 10.1002/psp4.12183. No abstract available.

18.

Reliable Rate Measurements for Active and Passive Hepatic Uptake Using Plated Human Hepatocytes.

Bi YA, Scialis RJ, Lazzaro S, Mathialagan S, Kimoto E, Keefer J, Zhang H, Vildhede AM, Costales C, Rodrigues AD, Tremaine LM, Varma MVS.

AAPS J. 2017 May;19(3):787-796. doi: 10.1208/s12248-017-0051-2. Epub 2017 Feb 10. Erratum in: AAPS J. 2017 May;19(3):882.

PMID:
28188574
19.

Quantitative Prediction of Human Renal Clearance and Drug-Drug Interactions of Organic Anion Transporter Substrates Using In Vitro Transport Data: A Relative Activity Factor Approach.

Mathialagan S, Piotrowski MA, Tess DA, Feng B, Litchfield J, Varma MV.

Drug Metab Dispos. 2017 Apr;45(4):409-417. doi: 10.1124/dmd.116.074294. Epub 2017 Feb 8.

20.

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
21.

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
22.

Quantitative Prediction of Drug-Drug Interactions Involving Inhibitory Metabolites in Drug Development: How Can Physiologically Based Pharmacokinetic Modeling Help?

Templeton IE, Chen Y, Mao J, Lin J, Yu H, Peters S, Shebley M, Varma MV.

CPT Pharmacometrics Syst Pharmacol. 2016 Oct;5(10):505-515. doi: 10.1002/psp4.12110. Epub 2016 Sep 19.

23.

Transporter-Mediated Hepatic Uptake Plays an Important Role in the Pharmacokinetics and Drug-Drug Interactions of Montelukast.

Varma MV, Kimoto E, Scialis R, Bi Y, Lin J, Eng H, Kalgutkar AS, El-Kattan AF, Rodrigues AD, Tremaine LM.

Clin Pharmacol Ther. 2017 Mar;101(3):406-415. doi: 10.1002/cpt.520. Epub 2016 Nov 18.

PMID:
27648490
24.

Transporter-Enzyme Interplay: Deconvoluting Effects of Hepatic Transporters and Enzymes on Drug Disposition Using Static and Dynamic Mechanistic Models.

Varma MV, El-Kattan AF.

J Clin Pharmacol. 2016 Jul;56 Suppl 7:S99-S109. doi: 10.1002/jcph.695. Review.

PMID:
27385183
25.

Evaluation and Quantitative Prediction of Renal Transporter-Mediated Drug-Drug Interactions.

Feng B, Varma MV.

J Clin Pharmacol. 2016 Jul;56 Suppl 7:S110-21. doi: 10.1002/jcph.702. Review.

PMID:
27385169
26.

The Antimicrobial Agent Fusidic Acid Inhibits Organic Anion Transporting Polypeptide-Mediated Hepatic Clearance and May Potentiate Statin-Induced Myopathy.

Eng H, Scialis RJ, Rotter CJ, Lin J, Lazzaro S, Varma MV, Di L, Feng B, West M, Kalgutkar AS.

Drug Metab Dispos. 2016 May;44(5):692-9. doi: 10.1124/dmd.115.067447. Epub 2016 Feb 17.

27.

Pharmacokinetics and Disposition of the Thiouracil Derivative PF-06282999, an Orally Bioavailable, Irreversible Inactivator of Myeloperoxidase Enzyme, Across Animals and Humans.

Dong JQ, Varma MV, Wolford A, Ryder T, Di L, Feng B, Terra SG, Sagawa K, Kalgutkar AS.

Drug Metab Dispos. 2016 Feb;44(2):209-19. doi: 10.1124/dmd.115.067868. Epub 2015 Nov 25.

28.

Hepatic Disposition of Gemfibrozil and Its Major Metabolite Gemfibrozil 1-O-β-Glucuronide.

Kimoto E, Li R, Scialis RJ, Lai Y, Varma MV.

Mol Pharm. 2015 Nov 2;12(11):3943-52. doi: 10.1021/acs.molpharmaceut.5b00411. Epub 2015 Sep 30.

PMID:
26378985
29.

Predicting Clearance Mechanism in Drug Discovery: Extended Clearance Classification System (ECCS).

Varma MV, Steyn SJ, Allerton C, El-Kattan AF.

Pharm Res. 2015 Dec;32(12):3785-802. doi: 10.1007/s11095-015-1749-4. Epub 2015 Jul 9.

PMID:
26155985
30.

Quantitative Rationalization of Gemfibrozil Drug Interactions: Consideration of Transporters-Enzyme Interplay and the Role of Circulating Metabolite Gemfibrozil 1-O-β-Glucuronide.

Varma MV, Lin J, Bi YA, Kimoto E, Rodrigues AD.

Drug Metab Dispos. 2015 Jul;43(7):1108-18. doi: 10.1124/dmd.115.064303. Epub 2015 May 4.

31.

Dealing with the complex drug-drug interactions: towards mechanistic models.

Varma MV, Pang KS, Isoherranen N, Zhao P.

Biopharm Drug Dispos. 2015 Mar;36(2):71-92. doi: 10.1002/bdd.1934. Epub 2015 Feb 10. Review.

PMID:
25545151
32.
33.

Prediction of pharmacokinetics and drug-drug interactions when hepatic transporters are involved.

Li R, Barton HA, Varma MV.

Clin Pharmacokinet. 2014 Aug;53(8):659-78. doi: 10.1007/s40262-014-0156-z. Review.

PMID:
25056496
34.

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.

35.

In vitro and in vivo approaches to characterize transporter-mediated disposition in drug discovery.

Feng B, Varma MV, Costales C, Zhang H, Tremaine L.

Expert Opin Drug Discov. 2014 Aug;9(8):873-90. doi: 10.1517/17460441.2014.922540. Epub 2014 May 24. Review.

PMID:
24857286
36.

Mechanism-based pharmacokinetic modeling to evaluate transporter-enzyme interplay in drug interactions and pharmacogenetics of glyburide.

Varma MV, Scialis RJ, Lin J, Bi YA, Rotter CJ, Goosen TC, Yang X.

AAPS J. 2014 Jul;16(4):736-48. doi: 10.1208/s12248-014-9614-7. Epub 2014 May 17.

37.

Clearance mechanism assignment and total clearance prediction in human based upon in silico models.

Lombardo F, Obach RS, Varma MV, Stringer R, Berellini G.

J Med Chem. 2014 May 22;57(10):4397-405. doi: 10.1021/jm500436v. Epub 2014 May 6.

PMID:
24773013
38.

Quantitative prediction of renal transporter-mediated clinical drug-drug interactions.

Feng B, Hurst S, Lu Y, Varma MV, Rotter CJ, El-Kattan A, Lockwood P, Corrigan B.

Mol Pharm. 2013 Nov 4;10(11):4207-15. doi: 10.1021/mp400295c. Epub 2013 Oct 10.

PMID:
24066726
39.

A perspective on the prediction of drug pharmacokinetics and disposition in drug research and development.

Di L, Feng B, Goosen TC, Lai Y, Steyn SJ, Varma MV, Obach RS.

Drug Metab Dispos. 2013 Dec;41(12):1975-93. doi: 10.1124/dmd.113.054031. Epub 2013 Sep 24.

40.

Quantitative assessment of the contribution of sodium-dependent taurocholate co-transporting polypeptide (NTCP) to the hepatic uptake of rosuvastatin, pitavastatin and fluvastatin.

Bi YA, Qiu X, Rotter CJ, Kimoto E, Piotrowski M, Varma MV, Ei-Kattan AF, Lai Y.

Biopharm Drug Dispos. 2013 Nov;34(8):452-61. doi: 10.1002/bdd.1861. Epub 2013 Oct 3.

PMID:
23996477
41.

Elucidation of the biochemical basis for a clinical drug-drug interaction between atorvastatin and 5-(N-(4-((4-ethylbenzyl)thio)phenyl)sulfamoyl)-2-methyl benzoic acid (CP-778875), a subtype selective agonist of the peroxisome proliferator-activated receptor alpha.

Kalgutkar AS, Chen D, Varma MV, Feng B, Terra SG, Scialis RJ, Rotter CJ, Frederick KS, West MA, Goosen TC, Gosset JR, Walsky RL, Francone OL.

Xenobiotica. 2013 Nov;43(11):963-72. doi: 10.3109/00498254.2013.791004. Epub 2013 Apr 30.

PMID:
23631744
42.

High specificity in response of the sodium-dependent multivitamin transporter to derivatives of pantothenic acid.

Chirapu SR, Rotter CJ, Miller EL, Varma MV, Dow RL, Finn MG.

Curr Top Med Chem. 2013;13(7):837-42. Review.

PMID:
23578027
43.

Intestinal targeting of drugs: rational design approaches and challenges.

Filipski KJ, Varma MV, El-Kattan AF, Ambler CM, Ruggeri RB, Goosen TC, Cameron KO.

Curr Top Med Chem. 2013;13(7):776-802. Review.

PMID:
23578023
44.

Response to the comment on the article "physiologically based modeling of pravastatin transporter-mediated hepatobiliary disposition and drug-drug interactions".

Varma MV, Lai Y, Feng B, Litchfield J, Goosen TC, Bergman A.

Pharm Res. 2013 Jun;30(6):1469-70. doi: 10.1007/s11095-013-0987-6. Epub 2013 Mar 6. No abstract available.

PMID:
23462935
45.

Quantitative prediction of repaglinide-rifampicin complex drug interactions using dynamic and static mechanistic models: delineating differential CYP3A4 induction and OATP1B1 inhibition potential of rifampicin.

Varma MV, Lin J, Bi YA, Rotter CJ, Fahmi OA, Lam JL, El-Kattan AF, Goosen TC, Lai Y.

Drug Metab Dispos. 2013 May;41(5):966-74. doi: 10.1124/dmd.112.050583. Epub 2013 Feb 7.

46.

Model-based approaches to predict drug-drug interactions associated with hepatic uptake transporters: preclinical, clinical and beyond.

Barton HA, Lai Y, Goosen TC, Jones HM, El-Kattan AF, Gosset JR, Lin J, Varma MV.

Expert Opin Drug Metab Toxicol. 2013 Apr;9(4):459-72. doi: 10.1517/17425255.2013.759210. Epub 2013 Jan 21. Review.

PMID:
23331046
47.

Mechanistic modeling to predict the transporter- and enzyme-mediated drug-drug interactions of repaglinide.

Varma MV, Lai Y, Kimoto E, Goosen TC, El-Kattan AF, Kumar V.

Pharm Res. 2013 Apr;30(4):1188-99. doi: 10.1007/s11095-012-0956-5. Epub 2013 Jan 10.

PMID:
23307347
48.

Optimizing PK properties of cyclic peptides: the effect of side chain substitutions on permeability and clearance().

Rand AC, Leung SS, Eng H, Rotter CJ, Sharma R, Kalgutkar AS, Zhang Y, Varma MV, Farley KA, Khunte B, Limberakis C, Price DA, Liras S, Mathiowetz AM, Jacobson MP, Lokey RS.

Medchemcomm. 2012 Oct;3(10):1282-1289.

49.

Physiologically based modeling of pravastatin transporter-mediated hepatobiliary disposition and drug-drug interactions.

Varma MV, Lai Y, Feng B, Litchfield J, Goosen TC, Bergman A.

Pharm Res. 2012 Oct;29(10):2860-73. doi: 10.1007/s11095-012-0792-7. Epub 2012 May 26.

PMID:
22638872
50.

Physicochemical property space of hepatobiliary transport and computational models for predicting rat biliary excretion.

Varma MV, Chang G, Lai Y, Feng B, El-Kattan AF, Litchfield J, Goosen TC.

Drug Metab Dispos. 2012 Aug;40(8):1527-37. doi: 10.1124/dmd.112.044628. Epub 2012 May 11.

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