Search Results - "Mudra, Daniel R."

In silico, in vitro and in situ models to assess interplay between CYP3A and P-gp by Mudra, Daniel R, Desino, Kelly E, Desai, Prashant V

“…The bioavailability, fraction of dose that reaches systemic circulation, of orally administered drugs is often limited by both physical barriers of the…”
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Preclinical Pharmacokinetic/Pharmacodynamic Modeling and Simulation in the Pharmaceutical Industry: An IQ Consortium Survey Examining the Current Landscape by Schuck, Edgar, Bohnert, Tonika, Chakravarty, Arijit, Damian-Iordache, Valeriu, Gibson, Christopher, Hsu, Cheng-Pang, Heimbach, Tycho, Krishnatry, Anu Shilpa, Liederer, Bianca M, Lin, Jing, Maurer, Tristan, Mettetal, Jerome T, Mudra, Daniel R, Nijsen, Marjoleen JMA, Raybon, Joseph, Schroeder, Patricia, Schuck, Virna, Suryawanshi, Satyendra, Su, Yaming, Trapa, Patrick, Tsai, Alice, Vakilynejad, Majid, Wang, Shining, Wong, Harvey

“…The application of modeling and simulation techniques is increasingly common in preclinical stages of the drug discovery and development process. A survey…”
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Novel Autotaxin Inhibitors for the Treatment of Osteoarthritis Pain: Lead Optimization via Structure-Based Drug Design by Jones, Spencer B, Pfeifer, Lance A, Bleisch, Thomas J, Beauchamp, Thomas J, Durbin, Jim D, Klimkowski, V. Joseph, Hughes, Norman E, Rito, Christopher J, Dao, Yen, Gruber, Joseph M, Bui, Hai, Chambers, Mark G, Chandrasekhar, Srinivasan, Lin, Chaohua, McCann, Denis J, Mudra, Daniel R, Oskins, Jennifer L, Swearingen, Craig A, Thirunavukkarasu, Kannan, Norman, Bryan H

“…In an effort to develop a novel therapeutic agent aimed at addressing the unmet need of patients with osteoarthritis pain, we set out to develop an inhibitor…”
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Development of LC-MS/MS-Based Receptor Occupancy Tracers and Positron Emission Tomography Radioligands for the Nociceptin/Orphanin FQ (NOP) Receptor by Pedregal, Concepción, Joshi, Elizabeth M, Toledo, Miguel A, Lafuente, Celia, Diaz, Nuria, Martinez-Grau, Maria A, Jiménez, Alma, Benito, Ana, Navarro, Antonio, Chen, Zhaogen, Mudra, Daniel R, Kahl, Steven D, Rash, Karen S, Statnick, Michael A, Barth, Vanessa N

“…Currently, a lack of sufficient tools has limited the understanding of the relationship between neuropsychiatric disorders and the nociceptin/orphanin FQ…”
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Absorption barriers in the rat intestinal mucosa: 1. Application of an in situ perfusion model to simultaneously assess drug permeation and metabolism by Mudra, Daniel R, Borchardt, Ronald T

“…Modulation of intestinal drug absorption barriers can have a profound impact on the bioavailability of orally administered compounds. With its commonality of…”
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The effects of gender, age, ethnicity, and liver cirrhosis on cytochrome P450 enzyme activity in human liver microsomes and inducibility in cultured human hepatocytes by Parkinson, Andrew, Mudra, Daniel R., Johnson, Cory, Dwyer, Anne, Carroll, Kathleen M.

“…We have measured cytochrome P450 (CYP) activity in nearly 150 samples of human liver microsomes and 64 samples of cryopreserved human hepatocytes, and we have…”
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Absorption barriers in the rat intestinal mucosa. 3: Effects of polyethoxylated solubilizing agents on drug permeation and metabolism by Mudra, Daniel R, Borchardt, Ronald T

“…Modern drug discovery chemical libraries contain a large number of molecular entities exhibiting low aqueous solubility, often necessitating the inclusion of…”
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Translational pharmacokinetic-pharmacodynamic analysis in the pharmaceutical industry: an IQ Consortium PK-PD Discussion Group perspective by Wong, Harvey, Bohnert, Tonika, Damian-Iordache, Valeriu, Gibson, Christopher, Hsu, Cheng-Pang, Krishnatry, Anu Shilpa, Liederer, Bianca M., Lin, Jing, Lu, Qiang, Mettetal, Jerome T., Mudra, Daniel R., Nijsen, Marjoleen J.M.A., Schroeder, Patricia, Schuck, Edgar, Suryawanshi, Satyendra, Trapa, Patrick, Tsai, Alice, Wang, Haiqing, Wu, Fan

“…[Display omitted] •Preclinical pharmacokinetic-pharmacodynamic modeling (PK-PD) is an important translational tool to understand drug efficacy in the…”
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A Highly Selective Hydantoin Inhibitor of Aggrecanase‑1 and Aggrecanase‑2 with a Low Projected Human Dose by Durham, Timothy B, Marimuthu, Jothirajah, Toth, James L, Liu, Chin, Adams, Lisa, Mudra, Daniel R, Swearingen, Craig, Lin, Chaohua, Chambers, Mark G, Thirunavukkarasu, Kannan, Wiley, Michael R

“…Aggrecanase-1 and -2 (ADAMTS-4 and ADAMTS-5) are zinc metalloproteases involved in the degradation of aggrecan in cartilage. Inhibitors could provide a means…”
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Discovery of a Novel Series of Orally Active Nociceptin/Orphanin FQ (NOP) Receptor Antagonists Based on a Dihydrospiro(piperidine-4,7′-thieno[2,3‑c]pyran) Scaffold by Toledo, Miguel A, Pedregal, Concepción, Lafuente, Celia, Diaz, Nuria, Martinez-Grau, Maria Angeles, Jiménez, Alma, Benito, Ana, Torrado, Alicia, Mateos, Carlos, Joshi, Elizabeth M, Kahl, Steven D, Rash, Karen S, Mudra, Daniel R, Barth, Vanessa N, Shaw, David B, McKinzie, David, Witkin, Jeffrey M, Statnick, Michael A

“…Nociceptin/OFQ (N/OFQ) is a 17 amino acid peptide that is the endogenous ligand for the ORL1/NOP receptor. Nociceptin appears to regulate a host of…”
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Discovery and characterization of [(cyclopentyl)ethyl]benzoic acid inhibitors of microsomal prostaglandin E synthase-1 by Partridge, Katherine M., Antonysamy, Stephen, Bhattachar, Shobha N., Chandrasekhar, Srinivasan, Fisher, Matthew J., Fretland, Adrian, Gooding, Karen, Harvey, Anita, Hughes, Norman E., Kuklish, Steven L., Luz, John G., Manninen, Peter R., McGee, James E., Mudra, Daniel R., Navarro, Antonio, Norman, Bryan H., Quimby, Steven J., Schiffler, Matthew A., Sloan, Ashley V., Warshawsky, Alan M., Weller, Jennifer M., York, Jeremy S., Yu, Xiao-Peng

“…[Display omitted] We describe a novel class of acidic mPGES-1 inhibitors with nanomolar enzymatic and human whole blood (HWB) potency. Rational design in…”
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Use of Osmotic Pumps to Establish the Pharmacokinetic–Pharmacodynamic Relationship and Define Desirable Human Performance Characteristics for Aggrecanase Inhibitors by Wiley, Michael R, Durham, Timothy B, Adams, Lisa A, Chambers, Mark G, Lin, Chaohua, Liu, Chin, Marimuthu, Jothirajah, Mitchell, Peter G, Mudra, Daniel R, Swearingen, Craig A, Toth, James L, Weller, Jennifer M, Thirunavukkarasu, Kannan

“…The development of reliable relationships between in vivo target engagement, pharmacodynamic activity, and efficacy in chronic disease models is beneficial for…”
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Effects of Prototypical Microsomal Enzyme Inducers on Cytochrome P450 Expression in Cultured Human Hepatocytes by Ajay Madan, Richard A. Graham, Kathleen M. Carroll, Daniel R. Mudra, L. Alayne Burton, Linda A. Krueger, April D. Downey, Maciej Czerwinski, Jameson Forster, Maria D. Ribadeneira, Liang-Shang Gan, Edward L. LeCluyse, Karl Zech, Philmore Robertson, Jr, Patrick Koch, Lida Antonian, Greg Wagner, Li Yu, Andrew Parkinson

“…Cultured human hepatocytes are a valuable in vitro system for evaluating new molecular entities as inducers of cytochrome P450 (P450) enzymes. The present…”
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Absorption barriers in the rat intestinal mucosa: 2. Application of physiologically based mathematical models to quantify mechanisms of drug permeation and metabolism by Mudra, Daniel R, Jin, Jin Y, Borchardt, Ronald T

“…The absorption of drug molecules is often investigated using in vitro or in situ models of the intestinal mucosa; however, few studies have quantified the…”
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The effect of fenbuconazole on cell proliferation and enzyme induction in the liver of female CD1 mice by Juberg, Daland R., Mudra, Daniel R., Hazelton, George A., Parkinson, Andrew

“…Fenbuconazole, a triazole fungicide, has been associated with an increase in the incidence of liver adenomas in female mice following long-term dietary…”
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Analysis of CYP mRNA expression by branched DNA technology by Czerwinski, Maciej, Opdam, Peter, Madan, Ajay, Carroll, Kathy, Mudra, Daniel R, Gan, Lawrence L, Luo, Gang, Parkinson, Andrew

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Discovery and characterization of [(cyclopentyl)ethyl]benzoic acid inhibitors of microsomal prostaglandin E synthase-1 by Partridge, Katherine M., Antonysamy, Stephen, Bhattachar, Shobha N., Chandrasekhar, Srinivasan, Fisher, Matthew J., Fretland, Adrian, Gooding, Karen, Harvey, Anita, Hughes, Norman E., Kuklish, Steven L., Luz, John G., Manninen, Peter R., McGee, James E., Mudra, Daniel R., Navarro, Antonio, Norman, Bryan H., Quimby, Steven J., Schiffler, Matthew A., Sloan, Ashley V., Warshawsky, Alan M., Weller, Jennifer M., York, Jeremy S., Yu, Xiao-Peng

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Function and modulation of physical and biological barriers to drug absorption in the rat intestinal mucosa by Mudra, Daniel R

“…Preclinical drug development is dependent upon human and laboratory-animal derived experimental models of absorption, metabolism and elimination requiring a…”
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