Search Results - "CALLEGARI, Ernesto"

Mini‐Review: Comprehensive Drug Disposition Knowledge Generated in the Modern Human Radiolabeled ADME Study by Spracklin, Douglas K., Chen, Danny, Bergman, Arthur J., Callegari, Ernesto, Obach, R. Scott

“…The human radiolabeled absorption, distribution, metabolism, and excretion (ADME) study offers a quantitative and comprehensive overall picture of the…”
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A comprehensive non‐clinical evaluation of the CNS penetration potential of antimuscarinic agents for the treatment of overactive bladder by Callegari, Ernesto, Malhotra, Bimal, Bungay, Peter J., Webster, Rob, Fenner, Katherine S., Kempshall, Sarah, LaPerle, Jennifer L., Michel, Martin C., Kay, Gary G.

“…WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT • This study provides antimuscarinic agents for overactive bladder (OAB) display variable association with side…”
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Physiologically‐Based Pharmacokinetic Modeling of the Drug–Drug Interaction of the UGT Substrate Ertugliflozin Following Co‐Administration with the UGT Inhibitor Mefenamic Acid by Callegari, Ernesto, Lin, Jian, Tse, Susanna, Goosen, Theunis C., Sahasrabudhe, Vaishali

“…The sodium‐glucose cotransporter 2 inhibitor ertugliflozin is metabolized by the uridine 5'‐diphospho‐glucuronosyltransferase (UGT) isozymes UGT1A9 and…”
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Prediction of Metabolite‐to‐Parent Drug Exposure: Derivation and Application of a Mechanistic Static Model by Callegari, Ernesto, Varma, Manthena V.S., Obach, R. Scott

“…In the development of new drugs, the prediction of metabolite‐to‐parent plasma exposure ratio in humans prior to administration in a clinical study has emerged…”
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Recommendations for the Design of Clinical Drug–Drug Interaction Studies With Itraconazole Using a Mechanistic Physiologically‐Based Pharmacokinetic Model by Chen, Yuan, Cabalu, Tamara D., Callegari, Ernesto, Einolf, Heidi, Liu, Lichuan, Parrott, Neil, Peters, Sheila Annie, Schuck, Edgar, Sharma, Pradeep, Tracey, Helen, Upreti, Vijay V., Zheng, Ming, Zhu, Andy Z.X., Hall, Stephen D.

“…Regulatory agencies currently recommend itraconazole (ITZ) as a strong cytochrome P450 3A (CYP3A) inhibitor for clinical drug–drug interaction (DDI) studies…”
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In vitro characterization of ertugliflozin glucuronidation by Lapham, Kimberly, Callegari, Ernesto, Lin, Jian, Niosi, Mark, Orozco, Christine, Sharma, Raman, Goosen, Theunis

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THE IMPACT OF P-GLYCOPROTEIN ON THE DISPOSITION OF DRUGS TARGETED FOR INDICATIONS OF THE CENTRAL NERVOUS SYSTEM: EVALUATION USING THE MDR1A/1B KNOCKOUT MOUSE MODEL by Doran, Angela, Obach, R Scott, Smith, Bill J, Hosea, Natilie A, Becker, Stacey, Callegari, Ernesto, Chen, Cuiping, Chen, Xi, Choo, Edna, Cianfrogna, Julie, Cox, Loretta M, Gibbs, John P, Gibbs, Megan A, Hatch, Heather, Hop, Cornelis E C A, Kasman, Ilana N, Laperle, Jennifer, Liu, Jianhua, Liu, Xingrong, Logman, Michael, Maclin, Debra, Nedza, Frank M, Nelson, Frederick, Olson, Emily, Rahematpura, Sandhya, Raunig, David, Rogers, Sabrinia, Schmidt, Kari, Spracklin, Douglas K, Szewc, Mark, Troutman, Matthew, Tseng, Elaine, Tu, Meihua, Van Deusen, Jeffrey W, Venkatakrishnan, Karthik, Walens, Gary, Wang, Ellen Q, Wong, Diane, Yasgar, Adam S, Zhang, Chenghong

“…Thirty-two structurally diverse drugs used for the treatment of various conditions of the central nervous system (CNS), along with two active metabolites, and…”
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A comprehensive listing of bioactivation pathways of organic functional groups by Kalgutkar, Amit S, Gardner, Iain, Obach, R Scott, Shaffer, Christopher L, Callegari, Ernesto, Henne, Kirk R, Mutlib, Abdul E, Dalvie, Deepak K, Lee, Jae S, Nakai, Yasuhiro, O'Donnell, John P, Boer, Jason, Harriman, Shawn P

“…The occurrence of idiosyncratic adverse drug reactions during late clinical trials or after a drug has been released can lead to a severe restriction in its…”
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End‐to‐end application of model‐informed drug development for ertugliflozin, a novel sodium‐glucose cotransporter 2 inhibitor by Fediuk, Daryl J., Nucci, Gianluca, Dawra, Vikas K., Callegari, Ernesto, Zhou, Susan, Musante, Cynthia J., Liang, Yali, Sweeney, Kevin, Sahasrabudhe, Vaishali

“…Model‐informed drug development (MIDD) is critical in all stages of the drug‐development process and almost all regulatory submissions for new agents…”
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Physiologically based pharmacokinetic modeling of the drug drug interaction between rifampin and SGLT2 inhibitors: The contribution of CYP induction to the observed interaction by Callegari, Ernesto, Lin, Jian, Tse, Susanna, Goosen, Theunis C., Sahasrabudhe, Vaishali, Kumar, Vikas

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Evaluation of Cerebrospinal Fluid Concentration and Plasma Free Concentration As a Surrogate Measurement for Brain Free Concentration by XINGRONG LIU, SMITH, Bill J, HOSEA, Natilie, JIANHUA LIU, NELSON, Frederick R, SZEWC, Mark A, VAN DEUSEN, Jeffrey, CUIPING CHEN, CALLEGARI, Ernesto, BECKER, Stacey L, XI CHEN, CIANFROGNA, Julie, DORAN, Angela C, DORAN, Shawn D, GIBBS, John P

“…This study was designed to evaluate the use of cerebrospinal fluid (CSF) drug concentration and plasma unbound concentration ( C u,plasma ) to predict brain…”
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Use of a physiologically based pharmacokinetic model to study the time to reach brain equilibrium: an experimental analysis of the role of blood-brain barrier permeability, plasma protein binding, and brain tissue binding by Liu, Xingrong, Smith, Bill J, Chen, Cuiping, Callegari, Ernesto, Becker, Stacey L, Chen, Xi, Cianfrogna, Julie, Doran, Angela C, Doran, Shawn D, Gibbs, John P, Hosea, Natilie, Liu, Jianhua, Nelson, Frederick R, Szewc, Mark A, Van Deusen, Jeffery

“…This study was designed 1) to examine the effects of blood-brain barrier (BBB) permeability [quantified as permeability-surface area product (PS)], unbound…”
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Physiologically-based Pharmacokinetic Modeling for Assessment of the Drug-drug Interaction Potential of Zavegepant (P9-12.006) by Ke, Alice, Callegari, Ernesto, Bhardwaj, Rajinder, Varma, Manthena, Muto, Chieko, Bertz, Richard, Sahasrabudhe, Vaishali, Liu, Jing

“…Abstract only…”
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Physiologically Based Pharmacokinetic Modeling of the Drug-Drug Interaction Between CYP3A4 Substrate Glasdegib and Moderate CYP3A4 Inducers in Lieu of a Clinical Study by Callegari, Ernesto, Tse, Susanna, Doran, Angela C, Goosen, Theunis C, Shaik, Naveed

“…Glasdegib (DAURISMO) is a hedgehog pathway inhibitor approved for the treatment of acute myeloid leukemia (AML). Cytochrome P450 3A4 (CYP3A4) has been…”
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In Vitro Characterization of Ertugliflozin Metabolism by UDP-Glucuronosyltransferase and Cytochrome P450 Enzymes by Lapham, Kimberly, Callegari, Ernesto, Cianfrogna, Julie, Lin, Jian, Niosi, Mark, Orozco, Christine C, Sharma, Raman, Goosen, Theunis C

“…Ertugliflozin is primarily cleared through UDP-glucurosyltransferase (UGT)-mediated metabolism (86%) with minor oxidative clearance (12%). In vitro phenotyping…”
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Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects by Miao, Zhuang, Nucci, Gianluca, Amin, Neeta, Sharma, Raman, Mascitti, Vincent, Tugnait, Meera, Vaz, Alfin D, Callegari, Ernesto, Kalgutkar, Amit S

“…The disposition of ertugliflozin (PF-04971729), an orally active selective inhibitor of the sodium-dependent glucose cotransporter 2, was studied after a…”
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Enzalutamide and Apalutamide: In Vitro Chemical Reactivity Studies and Activity in a Mouse Drug Allergy Model by Ji, Changhua, Guha, Mausumee, Zhu, Xu, Whritenour, Jessica, Hemkens, Michelle, Tse, Susanna, Walker, Gregory S, Evans, Ellen, Khan, Nasir K, Finkelstein, Martin B, Callegari, Ernesto, Obach, R. Scott

“…Enzalutamide and apalutamide are two androgen receptor inhibitors approved for the treatment of castration-resistant prostate cancer (CRPC) and nonmetastatic…”
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Role of Hepatic Organic Anion Transporter 2 in the Pharmacokinetics of R- and S‑Warfarin: In Vitro Studies and Mechanistic Evaluation by Bi, Yi-an, Lin, Jian, Mathialagan, Sumathy, Tylaska, Laurie, Callegari, Ernesto, Rodrigues, A. David, Varma, Manthena V. S

“…Interindividual variability in warfarin dose requirement demands personalized medicine approaches to balance its therapeutic benefits (anticoagulation) and…”
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Mechanistic Modeling to Predict Midazolam Metabolite Exposure from In Vitro Data by Nguyen, Hoa Q, Kimoto, Emi, Callegari, Ernesto, Obach, R Scott

“…Methods to predict the pharmacokinetics of drugs in humans from in vitro data have been established, but corresponding methods to predict exposure to…”
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Prediction of Losartan-Active Carboxylic Acid Metabolite Exposure Following Losartan Administration Using Static and Physiologically Based Pharmacokinetic Models by Nguyen, Hoa Q, Lin, Jian, Kimoto, Emi, Callegari, Ernesto, Tse, Susanna, Obach, R Scott

“…The aim of this study was to evaluate a strategy based on static and dynamic physiologically based pharmacokinetic (PBPK) modeling for the prediction of…”
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