Manthena VARMA (Pfizer)  SITE

  • Eur J Drug Metab Pharmacokinet. 2021;In press. Cytochrome P450 enzyme inhibition and Herb-Drug Interaction potential of medicinal plant extracts used for management of diabetes in Nigeria. Amaeze O, Eng H, Horlbogen L, Varma MVS, Slitt A. PubMed 
  • Drug Metab Dispos. 2021;In press. IVIVE of transporter-mediated renal clearance: Relative Expression Factor (REF) vs Relative Activity Factor (RAF) approach. Kumar AR, Prasad B, Bhatt DK, Mathialagan S, Varma MVS, Unadkat JD. PubMed
  • J Pharmacol Exp Ther. 2021;377:169-180. Organic Anion-Transporting Polypeptide 1B1/1B3-mediated hepatic uptake determines the pharmacokinetics of large lipophilic acids: In vitro-in vivo evaluation in Cynomolgus monkey. Eng H, Bi YA, West MA, Ryu S, Yamaguchi E, Kosa RE, Tess DA, Griffith DA, Litchfield J, Kalgutkar AS, Varma MVS. PubMed
  • Clin Pharmacol Ther. 2020;In press. Drug-Drug Interactions involving renal OCT2/MATE transporters: Clinical risk assessment may require endogenous biomarker-informed approach. Mathialagan S, Feng B, Rodrigues AD, Varma MVS. PubMed
  • Drug Metab Dispos. 2021;49:72-83. Effect of human plasma on hepatic uptake of Organic Anion-Transporting Polypeptide 1B substrates: Studies using transfected cells and primary human hepatocytes. Bi YA, Ryu S, Tess DA, Rodrigues AD, Varma MVS. PubMed
  • J Pharm Sci. 2021;110:376-387. Evaluation of hepatic uptake of OATP1B substrates by short term-cultured plated human hepatocytes: Comparison with isolated suspended hepatocytes. Yoshikado T, Lee W, Toshimoto K, Morita K, Kiriake A, Chu X, Lee N, Kimoto E, Varma MVS, Kikuchi R, Scialis RJ, Shen H, Ishiguro N, Lotz R, Li AP, Maeda K, Kusuhara H, Sugiyama Y.  PubMed
  • J Med Chem. 2020;63:11831-11844. Predicting the human hepatic clearance of acidic and zwitterionic drugs. Tess DA, Eng H, Kalgutkar AS, Litchfield J, Edmonds DJ, Griffith DA, Varma MVS. PubMed
  • J Med Chem. 2020;63:10879-10896. Optimizing the Benefit/Risk of Acetyl-CoA Carboxylase Inhibitors through Liver Targeting. Huard K, Smith AC, Cappon G, Dow RL, Edmonds DJ, El-Kattan A, Esler WP, Fernando DP, Griffith DA, Kalgutkar AS, Ross TT, Bagley SW, Beebe D, Bi YA, Cabral S, Crowley C, Doran SD, Dowling MS, Liras S, Mascitti V, Niosi M, Pfefferkorn JA, Polivkova J, Préville C, Price DA, Shavnya A, Shirai N, Smith AH, Southers JR, Tess DA, Thuma BA, Varma MV, Yang X. PubMed
  • Mol Pharm. 2020;17:3024-3032. Cytochrome-P450-mediated Drug-Drug Interactions of substrate drugs: Assessing clinical risk based on molecular properties and an Extended Clearance Classification System. Steyn SJ, Varma MVS. PubMed
  • Eur J Pharm Biopharm. 2020;156:50-63. IMI - Oral biopharmaceutics tools project - Evaluation of bottom-up PBPK prediction success part 4: Prediction accuracy and software comparisons with improved data and modelling strategies. Ahmad A, Pepin X, Aarons L, Wang Y, Darwich AS, Wood JM, Tannergren C, Karlsson E, Patterson C, Thörn H, Ruston L, Mattinson A, Carlert S, Berg S, Murphy D, Engman H, Laru J, Barker R, Flanagan T, Abrahamsson B, Budhdeo S, Franek F, Moir A, Hanisch G, Pathak SM, Turner D, Jamei M, Brown J, Good D, Vaidhyanathan S, Jackson C, Nicolas O, Beilles S, Nguefack JF, Louit G, Henrion L, Ollier C, Boulu L, Xu C, Heimbach T, Ren X, Lin W, Nguyen-Trung AT, Zhang J, He H, Wu F, Bolger MB, Mullin JM, van Osdol B, Szeto K, Korjamo T, Pappinen S, Tuunainen J, Zhu W, Xia B, Daublain P, Wong S, Varma MVS, Modi S, Schäfer KJ, Schmid K, Lloyd R, Patel A, Tistaert C, Bevernage J, Nguyen MA, Lindley D, Carr R, Rostami-Hodjegan A. PubMed
  • Expert Opin Drug Metab Toxicol. 2020;16:387-401. Transporter-enzyme interplay and the hepatic drug clearance: what have we learned so far? Alluri RV, Li R, Varma MVS. PubMed
  • Biochem Pharmacol. 2020;174:113829. Nicotinic acid transport into human liver involves organic anion transporter 2 (SLC22A7). Mathialagan S, Bi YA, Costales C, Kalgutkar AS, Rodrigues AD, Varma MVS. PubMed
  • Drug Metab Pharmacokinet. 2020;35:18-29. Identification and quantitation of enzyme and transporter contributions to hepatic clearance for the assessment of potential drug-drug interactions. Kimoto E, Obach RS, Varma MVS. PubMed
  • Clin Transl Sci. 2019; In press. Prediction of metabolite-to-parent drug exposure: Derivation and application of a mechanistic static model. Callegari E, Varma MVS, Obach RS. PubMed
  • Drug Metab Dispos. 2020;48:205-216. Induction of human intestinal and hepatic Organic Anion Transporting Polypeptides: Where is the evidence for its relevance in drug-drug interactions? Rodrigues AD, Lai Y, Shen H, Varma MVS, Rowland A, Oswald S. PubMed
  • Clin Pharmacol Ther. 2019;In press. Quantitative proteomics and mechanistic modeling of transporter-mediated disposition in Nonalcoholic Fatty Liver Disease. Vildhede A, Kimoto E, Pelis RM, Rodrigues AD, Varma MVS. PubMed
  • CPT Pharmacometrics Syst Pharmacol. 2019;8:634-642. Physiologically-Based Pharmacokinetic Modeling Approach to Predict Rifampin-Mediated Intestinal P-Glycoprotein Induction. Yamazaki S1, Costales C2, Lazzaro S2, Eatemadpour S2, Kimoto E2, Varma MV2. PubMed
  • J Pharmacol Exp Ther. 2019;370:72-83. Quantitative contribution of six major transporters to the hepatic uptake of drugs: "SLC-phenotyping" using primary human hepatocytes. Bi YA, Costales C, Mathialagan S, West M, Eatemadpour S, Lazzaro S, Tylaska L, Scialis R, Zhang H, Umland J, Kimoto E, Tess DA, Feng B, Tremaine LM, Varma MVS, Rodrigues AD. PubMed
  • Clin Pharmacol Ther. 2019;105:1295-1299. Clopidogrel as a perpetrator of drug-drug interactions: A challenge for quantitative predictions? Varma MVS, Bi YA, Lazzaro S, West M. PubMed
  • Clin Pharmacol Ther. 2019;106:792-802. Effect of hepatic Organic Anion-Transporting Polypeptide 1B inhibition and chronic kidney disease on the pharmacokinetics of a liver-targeted glucokinase activator: A model-based evaluation. Bergman A, Bi YA, Mathialagan S, Litchfield J, Kazierad DJ, Pfefferkorn JA, Varma MVS. PubMed
  • Drug Metab Dispos. 2019;47:493-503. Mechanistic evaluation of the complex Drug-Drug Interactions of Maraviroc: Contribution of Cytochrome P450 3A, P-Glycoprotein and Organic Anion Transporting Polypeptide 1B1. Kimoto E, Vourvahis M, Scialis RJ, Eng H, Rodrigues AD, Varma MVS. PubMed
  • Drug Metab Dispos. 2019;47:493-503. Mechanistic evaluation of the complex Drug-Drug Interactions of Maraviroc: Contribution of Cytochrome P450 3A, P-Glycoprotein and Organic Anion Transporting Polypeptide 1B1. Kimoto E, Vourvahis M, Scialis RJ, Eng H, Rodrigues AD, Varma MVS. PubMed
  • J Pharmacol Exp Ther. 2018;367:322-334. 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. PubMed
  • Clin Pharmacol Ther. 2019;105:719-729. Use of Physiologically Based Pharmacokinetic 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. PubMed
  • Mol Pharm. 2018;15:3227-3235. 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. PubMed
  • Drug Metab Dispos. 2018;46:1179-1189. 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. PubMed
  • Drug Metab Dispos. 2018;46:1200-1211. 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. PubMed
  • Drug Metab Dispos. 2018;46:989-1000. 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. PubMed
  • J Pharmacol Exp Ther. 2018;365:688-699. 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. PubMed
  • Drug Metab Dispos. 2018;46:729-739. Navigating transporter sciences in pharmacokinetics characterization using the Extended Clearance Classification System. El-Kattan AF, Varma MVS. PubMed
  • Drug Metab Dispos. 2018;46:692-696. 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. PubMed
  • Mol Pharm. 2018;15:1284-1295. 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. PubMed
  • J Pharmacol Exp Ther. 2018;364:390-398. 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. PubMed
  • Adv Drug Deliv Rev. 2017;116:92-99. Molecular properties associated with transporter-mediated drug disposition. Varma MV, Lai Y, El-Kattan AF. PubMed
  • J Pharm Sci. 2017;106:2795-2804. 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. PubMed
  • Drug Metab Dispos. 2017;45:737-747. 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. PubMed
  • Drug Metab Dispos. 2017;45:721-733. Leveraging of Rifampicin-dosed Cynomolgus monkeys to identify bile Acid 3-O-Sulfate conjugates as potential vovel 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. PubMed
  • AAPS J. 2017;19:787-796. 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. PubMed
  • Drug Metab Dispos. 2017;45:409-417. 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. PubMed
  • Clin Pharmacol Ther. 2017;102:33-36. 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. PubMed
  • Pharm Res. 2016;33:3021-3030. 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. PubMed
  • CPT Pharmacometrics Syst Pharmacol. 2016;5:505-515. 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. PubMed
  • Clin Pharmacol Ther. 2017;101:406-415. 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. PubMed
  • J Clin Pharmacol. 2016;56 Suppl 7:S99-S109. Transporter-enzyme interplay: Deconvoluting effects of hepatic transporters and enzymes on drug disposition using static and dynamic mechanistic models. Varma MV, El-Kattan AF. PubMed
  • J Clin Pharmacol. 2016;56:S110-21. Evaluation and quantitative prediction of renal transporter-mediated Drug-Drug Interactions. Feng B, Varma MV. PubMed
  • Drug Metab Dispos. 2016;44:692-9. 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. PubMed
  • Mol Pharm. 2015;12:3943-52. Hepatic disposition of Gemfibrozil and its major metabolite Gemfibrozil 1-O-β-Glucuronide. Kimoto E, Li R, Scialis RJ, Lai Y, Varma MV. PubMed
  • Pharm Res. 2015 Dec;32(12):3785-802. Predicting clearance mechanism in drug discovery: Extended Clearance Classification System (ECCS). Varma MV, Steyn SJ, Allerton C, El-Kattan AF. PubMed
  • Drug Metab Dispos. 2015;43:1108-18. 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. PubMed
  • Biopharm Drug Dispos. 2015;36:71-92. Dealing with the complex drug-drug interactions: towards mechanistic models. Varma MV, Pang KS, Isoherranen N, Zhao P. PubMed
  • J Pharmacol Exp Ther. 2014;351:214-23. Quantitative prediction of transporter- and enzyme-mediated clinical drug-drug interactions of organic anion-transporting polypeptide 1B1 substrates using a mechanistic net-effect model. Varma MV, Bi YA, Kimoto E, Lin J. PubMed
  • Clin Pharmacokinet. 2014;53:659-78. Prediction of pharmacokinetics and drug-drug interactions when hepatic transporters are involved. Li R, Barton HA, Varma MV. PubMed
  • Drug Metab Dispos. 2014;42:1599-610. 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. PubMed
  • Expert Opin Drug Discov. 2014;9:873-90. In vitro and in vivo approaches to characterize transporter-mediated disposition in drug discovery. Feng B, Varma MV, Costales C, Zhang H, Tremaine L. PubMed
  • AAPS J. 2014;16:736-48. 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. PubMed
  • J Med Chem. 2014;57:4397-405. Clearance mechanism assignment and total clearance prediction in human based upon in silico models. Lombardo F, Obach RS, Varma MV, Stringer R, Berellini G. PubMed
  • Mol Pharm. 2013;10:4207-15. 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. PubMed
  • Drug Metab Dispos. 2013;41:1975-93. 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. PubMed
  • Biopharm Drug Dispos. 2013;34:452-61. 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. PubMed
  • Drug Metab Dispos. 2013;41:966-74. 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. PubMed
  • Expert Opin Drug Metab Toxicol. 2013;9:459-72. 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. PubMed
  • Pharm Res. 2013;30:1188-99. 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. PubMed
  • Pharm Res. 2012;29:2860-73. 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. PubMed
  • Drug Metab Dispos. 2012;40:1527-37. 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. PubMed
  • Mol Pharm. 2011;8:1303-13. pH-sensitive interaction of HMG-CoA reductase inhibitors (statins) with organic anion transporting polypeptide 2B1. Varma MV, Rotter CJ, Chupka J, Whalen KM, Duignan DB, Feng B, Litchfield J, Goosen TC, El-Kattan AF. PubMed

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Last update: April 2021