Translational pharmacokinetic-pharmacodynamic analysis in the pharmaceutical industry: an IQ Consortium PK-PD Discussion Group perspective

Lessons learned from the fate of AstraZeneca's drug pipeline: a five-dimensional framework

Cook, D., Brown, D., Alexander, R., March, R., Morgan, P., Satterthwaite, G., & Pangalos, M. N. (2014) · Nature Reviews Drug Discovery · doi:10.1038/nrd4309 · Cited by 1,344 · see citing works

Simultaneous modeling of pharmacokinetics and pharmacodynamics: Application to d‐tubocurarine

Sheiner, L. B., Stanski, D. R., Vožeh, S., Miller, R. D., & Ham, J. (1979) · Clinical Pharmacology & Therapeutics · doi:10.1002/cpt1979253358 · Cited by 1,133 · see citing works

Comparison of four basic models of indirect pharmacodynamic responses

Dayneka, N., Garg, V., & Jusko, W. J. (1993) · Journal of Pharmacokinetics and Biopharmaceutics · doi:10.1007/bf01061691 · Cited by 821 · see citing works

Antimicrobial Resistance: Pharmacokinetics‐Pharmacodynamics of Antimicrobial Therapy: It’s Not Just for Mice Anymore

Ambrose, P. G., Bhavnani, S. M., Rubino, C. M., Louie, A., Gumbo, T., Forrest, A., & Drusano, G. L. (2007) · Clinical Infectious Diseases · doi:10.1086/510079 · Cited by 697 · see citing works

Can the flow of medicines be improved? Fundamental pharmacokinetic and pharmacological principles toward improving Phase II survival

Morgan, P., Van Der Graaf, P. H., Arrowsmith, J., Feltner, D. E., Drummond, K. S., Wegner, C. D., & Street, S. D. A. (2012) · Drug Discovery Today · doi:10.1016/j.drudis.2011.12.020 · Cited by 692 · see citing works

Rational Intravenous Doses of Theophylline

Mitenko, P. A., & OGILVIE, R. I. (1973) · New England Journal of Medicine · doi:10.1056/nejm197309202891202 · Cited by 648 · see citing works

Phase II failures: 2008–2010

Arrowsmith, J. (2011) · Nature Reviews Drug Discovery · doi:10.1038/nrd3439 · Cited by 622 · see citing works

Basic Concepts in Population Modeling, Simulation, and Model‐Based Drug Development

Mould, D., & Upton, R. N. (2012) · CPT Pharmacometrics & Systems Pharmacology · doi:10.1038/psp.2012.4 · Cited by 552 · see citing works

Predictive Pharmacokinetic-Pharmacodynamic Modeling of Tumor Growth Kinetics in Xenograft Models after Administration of Anticancer Agents

Simeoni, M., Magni, P., Cammia, C., Nicolao, G. D., Croci, V., Pesenti, E. A., Germani, M., Poggesi, I., & Rocchetti, M. (2004) · Cancer Research · doi:10.1158/0008-5472.can-03-2524 · Cited by 509 · see citing works

Phase III and submission failures: 2007–2010

Arrowsmith, J. E. (2011) · Nature Reviews Drug Discovery · doi:10.1038/nrd3375 · Cited by 480 · see citing works

Model-based Drug Development

Lalonde, R. L., Kowalski, K., Hutmacher, M. M., Ewy, W., Nichols, D., Milligan, P. A., Corrigan, B., Lockwood, P. A., Marshall, S. A., Benincosa, L. J., et al. (2007) · Clinical Pharmacology & Therapeutics · doi:10.1038/sj.clpt.6100235 · Cited by 452 · see citing works

Physiologic indirect response models characterize diverse types of pharmacodynamic effects

Jusko, W. J., & Ko, H. C. (1994) · Clinical Pharmacology & Therapeutics · doi:10.1038/clpt.1994.155 · Cited by 360 · see citing works

Mechanism-based pharmacokinetic-pharmacodynamic (PK-PD) modeling in translational drug research

Danhof, M., DELANGE, E., Pasqua, O. E. D., Ploeger, B. A., & Voskuyl, R. A. (2008) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2008.01.007 · Cited by 287 · see citing works

Mechanism-Based Pharmacokinetic-Pharmacodynamic Modeling: Biophase Distribution, Receptor Theory, and Dynamical Systems Analysis

Danhof, M., DeJongh, J., de Lange, E. C. M., Pasqua, O. E. D., Ploeger, B. A., & Voskuyl, R. A. (2006) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev.pharmtox.47.120505.105154 · Cited by 258 · see citing works

Use of Preclinical Data for Selection of a Phase II/III Dose for Evernimicin and Identification of a Preclinical MIC Breakpoint

Drusano, G. L., Preston, S. L., Hardalo, C. J., Hare, R. S., Banfield, C. R., Andes, D. R., Vesga, Ó., & Craig, W. A. (2001) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.45.1.13-22.2001 · Cited by 243 · see citing works

Implementation of pharmacokinetic and pharmacodynamic strategies in early research phases of drug discovery and development at Novartis Institute of Biomedical Research

Tuntland, T., Ethell, B., Kosaka, T., Blasco, F., Zang, R. X., Jain, M., Gould, T., & Hoffmaster, K. (2014) · Frontiers in Pharmacology · doi:10.3389/fphar.2014.00174 · Cited by 239 · see citing works

Characteristics of indirect pharmacodynamic models and applications to clinical drug responses

Sharma, A., & Jusko, W. J. (1998) · British Journal of Clinical Pharmacology · doi:10.1046/j.1365-2125.1998.00676.x · Cited by 197 · see citing works

Pharmacodynamics of Chemotherapeutic Effects: Dose-Time-Response Relationships for Phase-Nonspecific Agents

Jusko, W. J. (1971) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.2600600618 · Cited by 164 · see citing works

Bench to bedside translation of antibody drug conjugates using a multiscale mechanistic PK/PD model: a case study with brentuximab-vedotin

Shah, D. K., Haddish‐Berhane, N., & Betts, A. M. (2012) · Journal of Pharmacokinetics and Pharmacodynamics · doi:10.1007/s10928-012-9276-y · Cited by 160 · see citing works

Simultaneous Modeling of Pharmacokinetics and Pharmacodynamics with a Nonparametric Pharmacodynamic Model

Fuseau, E., & Sheiner, L. B. (1984) · Clinical Pharmacology & Therapeutics · doi:10.1038/clpt.1984.104 · Cited by 143 · see citing works

Systems Pharmacology of Adverse Event Mitigation by Drug Combinations

Zhao, S., Nishimura, T., Chen, Y., Azeloglu, E. U., Gottesman, O., Giannarelli, C., Zafar, M. U., Bénard, L., Badimón, J. J., Hajjar, R. J., et al. (2013) · Science Translational Medicine · doi:10.1126/scitranslmed.3006548 · Cited by 135 · see citing works

Antitumor activity of targeted and cytotoxic agents in murine subcutaneous tumor models correlates with clinical response

Wong, H., Choo, E. F., Alicke, B., Ding, X., La, H., McNamara, E., Theil, F.-P., Tibbitts, J., Friedman, L. S., Hop, C. E. C. A., et al. (2012) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-12-0738 · Cited by 133 · see citing works

Mechanism-based pharmacokinetic–pharmacodynamic modeling of antimicrobial drug effects

Czock, D., & Keller, F. (2007) · Journal of Pharmacokinetics and Pharmacodynamics · doi:10.1007/s10928-007-9069-x · Cited by 118 · see citing works

Simultaneous modeling of pharmacokinetics and pharmacodynamics with nonparametric kinetic and dynamic models

Unadkat, J. D., Bartha, F. A., & Sheiner, L. B. (1986) · Clinical Pharmacology & Therapeutics · doi:10.1038/clpt.1986.143 · Cited by 116 · see citing works

Pharmacokinetic–Pharmacodynamic Analysis of Vismodegib in Preclinical Models of Mutational and Ligand-Dependent Hedgehog Pathway Activation

Wong, H., Alicke, B., West, K. A., Pacheco, P., La, H., Januario, T., Yauch, R. L., de Sauvage, F. J., & Gould, S. E. (2011) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-11-0975 · Cited by 113 · see citing works

The Application of Target Information and Preclinical Pharmacokinetic/Pharmacodynamic Modeling in Predicting Clinical Doses of a Dickkopf-1 Antibody for Osteoporosis

Betts, A. M., Clark, T. H., Yang, J., Treadway, J. L., Li, M., Giovanelli, M. A., Abdiche, Y. N., Stone, D. M., & Paralkar, V. M. (2010) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.109.164129 · Cited by 104 · see citing works

A whole-body mathematical model of cholesterol metabolism and its age-associated dysregulation

Auley, M. T. M., Wilkinson, D. J., Jones, J. J., & Kirkwood, T. B. L. (2012) · BMC Systems Biology · doi:10.1186/1752-0509-6-130 · Cited by 102 · see citing works

Predicting the active doses in humans from animal studies: A novel approach in oncology

Rocchetti, M., Simeoni, M., Pesenti, E. A., Nicolao, G. D., & Poggesi, I. (2007) · European Journal of Cancer · doi:10.1016/j.ejca.2007.05.011 · Cited by 101 · see citing works

Optimizing Oncology Therapeutics Through Quantitative Translational and Clinical Pharmacology: Challenges and Opportunities

Venkatakrishnan, K., Friberg, L. E., Ouellet, D., Mettetal, J. T., Stein, A. M., Trocóniz, I. F., Bruno, R., Mehrotra, N., Gobburu, J. V. S., & Mould, D. (2014) · Clinical Pharmacology & Therapeutics · doi:10.1002/cpt.7 · Cited by 96 · see citing works

Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor

He, K., Luettgen, J. M., Zhang, D., He, B., Grace, J. E., Xin, B., Pinto, D. J. P., Wong, P. C., Knabb, R. M., Lam, P. Y. S., et al. (2011) · European Journal of Drug Metabolism and Pharmacokinetics · doi:10.1007/s13318-011-0037-x · Cited by 96 · see citing works

Disease System Analysis: Basic Disease Progression Models in Degenerative Disease

Post, T. M., Freijer, J. I., DeJongh, J., & Danhof, M. (2005) · Pharmaceutical Research · doi:10.1007/s11095-005-5641-5 · Cited by 96 · see citing works

Pharmacokinetic-Pharmacodynamic Modeling of Biomarker Response and Tumor Growth Inhibition to an Orally Available cMet Kinase Inhibitor in Human Tumor Xenograft Mouse Models

Yamazaki, S., Skaptason, J., Romero, D., Lee, J. H., Zou, H. Y., Christensen, J. G., Koup, J. R., Smith, B. J., & Koudriakova, T. B. (2008) · Drug Metabolism and Disposition · doi:10.1124/dmd.107.019711 · Cited by 94 · see citing works

Antiarthritis Effect of a Novel Bruton’s Tyrosine Kinase (BTK) Inhibitor in Rat Collagen-Induced Arthritis and Mechanism-Based Pharmacokinetic/Pharmacodynamic Modeling: Relationships between Inhibition of BTK Phosphorylation and Efficacy

Liu, L., Paolo, J. A. D., Barbosa, J., Rong, H., Reif, K., & Wong, H. (2011) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.111.181545 · Cited by 89 · see citing works

Bridging the Gap between Preclinical and Clinical Studies Using Pharmacokinetic–Pharmacodynamic Modeling: An Analysis of GDC-0973, a MEK Inhibitor

Wong, H., Vernillet, L., Peterson, A., Ware, J. A., Lee, L., Martini, J., Yu, P., Li, C., Rosario, G. D., Choo, E. F., et al. (2012) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-12-0445 · Cited by 80 · see citing works

A Generic Integrated Physiologically based Whole-body Model of the Glucose-Insulin-Glucagon Regulatory System

Schaller, S., Willmann, S., Lippert, J., Schaupp, L., Pieber, T., Schuppert, A., & Eissing, T. (2013) · CPT: Pharmacometrics & Systems Pharmacology · doi:10.1038/psp.2013.40 · Cited by 79 · see citing works

Pharmacokinetic/Pharmacodynamic Modeling of Crizotinib for Anaplastic Lymphoma Kinase Inhibition and Antitumor Efficacy in Human Tumor Xenograft Mouse Models

Yamazaki, S., Vicini, P., Shen, Z., Zou, H. Y., Lee, J. J., Li, Q., Christensen, J. G., Smith, B. J., & Shetty, B. V. (2011) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.111.188870 · Cited by 68 · see citing works

Multiscale Kinetic Modeling of Liposomal Doxorubicin Delivery Quantifies the Role of Tumor and Drug‐Specific Parameters in Local Delivery to Tumors

Hendriks, B. S., Reynolds, J. G., Klinz, S., Geretti, E., Lee, H. H., Leonard, S., Gaddy, D. F., Espelin, C. W., Nielsen, U., & Wickham, T. (2012) · CPT Pharmacometrics & Systems Pharmacology · doi:10.1038/psp.2012.16 · Cited by 63 · see citing works

Pharmacokinetic-pharmacodynamic modelling of antibacterial activity of cefpodoxime and cefixime in in vitro kinetic models

Liu, P., Rand, K. H., Obermann, B., & Derendorf, H. (2005) · International Journal of Antimicrobial Agents · doi:10.1016/j.ijantimicag.2004.09.012 · Cited by 59 · see citing works

Enhancing ketamine translational pharmacology via receptor occupancy normalization

Shaffer, C. L., Osgood, S. M., Smith, D. L., Liu, J., & Trapa, P. E. (2014) · Neuropharmacology · doi:10.1016/j.neuropharm.2014.07.008 · Cited by 55 · see citing works

Learning and Confirming with Preclinical Studies: Modeling and Simulation in the Discovery of GDC-0917, an Inhibitor of Apoptosis Proteins Antagonist

Wong, H., Gould, S. E., Budha, N. R., Darbonne, W. C., Kadel, E. E., La, H., Alicke, B., Halladay, J. S., Erickson, R., Portera, C. C., et al. (2013) · Drug Metabolism and Disposition · doi:10.1124/dmd.113.053926 · Cited by 54 · see citing works

Preclinical Pharmacokinetic/Pharmacodynamic Modeling and Simulation in the Pharmaceutical Industry: An IQ Consortium Survey Examining the Current Landscape

Schuck, E. L., Bohnert, T., Chakravarty, A., Damian‐Iordache, V., Gibson, C. R., Hsu, C., Heimbach, T., Krishnatry, A. S., Liederer, B. M., Jing, L., et al. (2015) · The AAPS Journal · doi:10.1208/s12248-014-9716-2 · Cited by 52 · see citing works

Prediction of clinical response based on pharmacokinetic/pharmacodynamic models of 5‐hydroxytryptamine reuptake inhibitors in mice

Kreilgaard, M., Smith, D. G., Brennum, L. T., & Sánchez, C. (2008) · British Journal of Pharmacology · doi:10.1038/bjp.2008.243 · Cited by 50 · see citing works

Modeling and Validating Chronic Pharmacological Manipulation of Circadian Rhythms

Kim, J. K., Forger, D. B., Marconi, M., Wood, D., Doran, A. C., Wager, T. T., Chang, C., & Walton, K. (2013) · CPT Pharmacometrics & Systems Pharmacology · doi:10.1038/psp.2013.34 · Cited by 49 · see citing works

Quantitative Relationship Between Myocardial Concentration of Tacrolimus and QT Prolongation in Guinea Pigs: Pharmacokinetic/Pharmacodynamic Model Incorporating a Site of Adverse Effect

Minematsu, T., Ohtani, H., Yamada, Y., Sawada, Y., Sato, H., & Iga, T. (2001) · Journal of Pharmacokinetics and Pharmacodynamics · doi:10.1023/a:1014460404352 · Cited by 48 · see citing works

Scaling the time-course of myelosuppression from rats to patients with a semi-physiological model

Friberg, L. E., Sandström, M., & Karlsson, M. O. (2009) · Investigational New Drugs · doi:10.1007/s10637-009-9308-7 · Cited by 44 · see citing works

Pharmacokinetic–Pharmacodynamic Modeling and Simulation for in Vivo Bactericidal Effect in Murine Infection Model

Katsube, T., Yamano, Y., & Yano, Y. (2007) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.21062 · Cited by 43 · see citing works

Translational pharmacokinetic-pharmacodynamic modeling of QTc effects in dog and human.

Parkinson, J., Visser, S., Jarvis, P., Pollard, C., Valentin, J., Yates, J., & Ewart, L. (2013) · Journal of pharmacological and toxicological methods · doi:10.1016/j.vascn.2013.03.007 · Cited by 42 · see citing works

Quantitative PK–PD Model-Based Translational Pharmacology of a Novel Kappa Opioid Receptor Antagonist Between Rats and Humans

Chang, C., Byon, W., Lu, Y.-F., Jacobsen, L., Badura, L., Sawant-Basak, A., Miller, E., Liu, J., Grimwood, S., Wang, E., et al. (2011) · AAPS Journal · doi:10.1208/s12248-011-9296-3 · Cited by 41 · see citing works

Pharmacokinetic–Pharmacodynamic Reasoning in Drug Discovery and Early Development

van der Graaf, P. H., & Gabrielsson, J. (2009) · Future Medicinal Chemistry · doi:10.4155/fmc.09.124 · Cited by 39 · see citing works

THU0127 Pharmacodynamics of A Novel JAK1 Selective Inhibitor in Rat Arthritis and Anemia Models and in Healthy Human Subjects

Voss, J. W., Graff, C. L., Schwartz, A., Hyland, D., Argiriadi, M. A., Camp, H. S., Dowding, L., Friedman, M., Frank, K., George, J., et al. (2014) · Annals of the Rheumatic Diseases · doi:10.1136/annrheumdis-2014-eular.3823 · Cited by 39 · see citing works

Pharmacodynamic Model of Sodium–Glucose Transporter 2 (SGLT2) Inhibition: Implications for Quantitative Translational Pharmacology

Maurer, T. S., Ghosh, A., Haddish‐Berhane, N., Sawant‐Basak, A., Boustany, C., She, L., Leininger, M. T., Zhu, T., Tugnait, M., Yang, X., et al. (2011) · The AAPS Journal · doi:10.1208/s12248-011-9297-2 · Cited by 37 · see citing works

Preclinical Assessment of the Absorption and Disposition of the Phosphatidylinositol 3-Kinase/Mammalian Target of Rapamycin Inhibitor GDC-0980 and Prediction of Its Pharmacokinetics and Efficacy in Human

Salphati, L., Pang, J., Plise, E. G., Lee, L. B., Olivero, A. G., Prior, W. W., Sampath, D., Wong, S., & Zhang, X. (2012) · Drug Metabolism and Disposition · doi:10.1124/dmd.112.046052 · Cited by 37 · see citing works

Pharmacokinetics of New Calcium Channel Antagonist Clevidipine in the Rat, Rabbit, and Dog and Pharmacokinetic/Pharmacodynamic Relationship in Anesthetized Dogs

Ericsson, H., Tholander, B., Björkman, J., Nordlander, M., & Regårdh, C. G. (1999) · Drug Metabolism and Disposition · doi:10.1016/s0090-9556(24)15249-x · Cited by 36 · see citing works

Drug effects on the CVS in conscious rats: separating cardiac output into heart rate and stroke volume using PKPD modelling

Snelder, N., Ploeger, B. A., Luttringer, O., Rigel, D. F., Fu, F., Beil, M. E., Stanski, D. R., & Danhof, M. (2014) · British Journal of Pharmacology · doi:10.1111/bph.12824 · Cited by 34 · see citing works

A Viral Dynamic Model for Treatment Regimens with Direct-acting Antivirals for Chronic Hepatitis C Infection

Adiwijaya, B. S., Kieffer, T. L., Henshaw, J., Eisenhauer, K. M., Kimko, H. H. C., Alam, J. J., Kauffman, R. S., & Garg, V. (2012) · PLoS Computational Biology · doi:10.1371/journal.pcbi.1002339 · Cited by 33 · see citing works

Translational PK/PD modeling for cardiovascular safety assessment of drug candidates: Methods and examples in drug development

Caruso, A., Frances, N., Meille, C., Greiter‐Wilke, A., Hillebrecht, A., & Lavé, T. (2014) · Journal of Pharmacological and Toxicological Methods · doi:10.1016/j.vascn.2014.05.004 · Cited by 32 · see citing works

Predictive pharmacokinetic–pharmacodynamic modeling of tumor growth after administration of an anti-angiogenic agent, bevacizumab, as single-agent and combination therapy in tumor xenografts

Rocchetti, M., Germani, M., Bene, F. D., Poggesi, I., Magni, P., Pesenti, E. A., & Nicolao, G. D. (2013) · Cancer Chemotherapy and Pharmacology · doi:10.1007/s00280-013-2107-z · Cited by 32 · see citing works

Identifying the translational gap in the evaluation of drug‐induced QTc interval prolongation

Chain, A. S. Y., Dubois, V. F. S., Danhof, M., Sturkenboom, M., Pasqua, O. E. D., & Cardiovascular Safety Project Team, T. P. P. P. (2013) · British Journal of Clinical Pharmacology · doi:10.1111/bcp.12082 · Cited by 31 · see citing works

From Target Selection to the Minimum Acceptable Biological Effect Level for Human Study: Use of Mechanism-based PK/PD Modeling to Design Safe and Efficacious Biologics

Yu, J., Karcher, H., Feire, A. L., & Lowe, P. J. (2011) · The AAPS Journal · doi:10.1208/s12248-011-9256-y · Cited by 29 · see citing works

A System Approach to Pharmacodynamics. Ill: An Algorithm and Computer Program, COLAPS, for Pharmacodynamic Modeling

Veng‐Pedersen, P., Mandema, J. W., & Danhof, M. (1991) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.2600800518 · Cited by 29 · see citing works

Modeling and Simulation Approaches for Cardiovascular Function and Their Role in Safety Assessment

Collins, T., Bergenholm, L., Abdulla, T., Yates, J. W. T., Evans, N. D., Chappell, M., & Mettetal, J. T. (2015) · CPT Pharmacometrics & Systems Pharmacology · doi:10.1002/psp4.18 · Cited by 28 · see citing works

Clockwise hysteresis or proteresis

Girard, P., & Boissel, J. (1989) · Journal of Pharmacokinetics and Biopharmaceutics · doi:10.1007/bf01061905 · Cited by 28 · see citing works

PKPD modelling of the interrelationship between mean arterial BP , cardiac output and total peripheral resistance in conscious rats

Snelder, N., Ploeger, B. A., Luttringer, O., Rigel, D. F., Webb, R. L., Feldman, D., Fu, F., Beil, M. E., Jin, L., Stanski, D. R., et al. (2013) · British Journal of Pharmacology · doi:10.1111/bph.12190 · Cited by 27 · see citing works

Pharmacokinetic–Pharmacodynamic Modeling and Simulation for Bactericidal Effect in an In Vitro Dynamic Model

Katsube, T., Yano, Y., Yamano, Y., Munekage, T., Kuroda, N., & Takano, M. (2008) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.21265 · Cited by 27 · see citing works

Optimization of Human Dose Prediction by Using Quantitative and Translational Pharmacology in Drug Discovery

Bueters, T., Gibson, C. R., & Visser, S. A. G. (2015) · Future Medicinal Chemistry · doi:10.4155/fmc.15.143 · Cited by 27 · see citing works

A Systems Pharmacology Perspective on the Clinical Development of Fatty Acid Amide Hydrolase Inhibitors for Pain

Benson, N., Metelkin, E., Demin, O. O., Li, G., Nichols, D., & van der Graaf, P. (2014) · CPT Pharmacometrics & Systems Pharmacology · doi:10.1038/psp.2013.72 · Cited by 26 · see citing works

Interaction Between Domperidone and Ketoconazole: Toward Prediction of Consequent QTc Prolongation Using Purely <i>In Vitro</i> Information

Mishra, H., Polak, S., Jamei, M., & Rostami‐Hodjegan, A. (2014) · CPT: Pharmacometrics &amp; Systems Pharmacology · doi:10.1038/psp.2014.26 · Cited by 24 · see citing works

A Quantitative Systems Pharmacology Computer Model for Schizophrenia Efficacy and Extrapyramidal Side Effects

Spiros, Ä., Roberts, P., & Geerts, H. (2012) · Drug Development Research · doi:10.1002/ddr.21008 · Cited by 22 · see citing works

Agonistic TAM-163 antibody targeting tyrosine kinase receptor-B

Vugmeyster, Y., Rohde, C. M., Perreault, M., Gimeno, R. E., & Singh, P. (2013) · mAbs · doi:10.4161/mabs.23826 · Cited by 22 · see citing works

Prediction of Neutropenia-Related Effects of a New Combination Therapy With the Anticancer Drugs BI 2536 (a Plk1 Inhibitor) and Pemetrexed

Soto, E., Staab, A., Freiwald, M., Munzert, G. M., Fritsch, H., Döge, C., & Trocóniz, I. F. (2010) · Clinical Pharmacology & Therapeutics · doi:10.1038/clpt.2010.148 · Cited by 19 · see citing works

A modeling approach for compounds affecting body composition

Gennemark, P., Jansson‐Löfmark, R., Hyberg, G., Wigstrand, M., Kakol‐Palm, D., Håkansson, P., Hovdal, D., Brodin, P., Fredin, M. F., Antonsson, M., et al. (2013) · Journal of Pharmacokinetics and Pharmacodynamics · doi:10.1007/s10928-013-9337-x · Cited by 18 · see citing works

Dogs Are More Sensitive to Antagonists of Inhibitor of Apoptosis Proteins Than Rats and Humans: A Translational Toxicokinetic/Toxicodynamic Analysis

Wong, H., Budha, N. R., West, K. A., Blackwood, E. R., Ware, J. A., Yu, R., Darbonne, W. C., Gould, S. E., Steigerwalt, R. W., Erickson, R., et al. (2012) · Toxicological Sciences · doi:10.1093/toxsci/kfs235 · Cited by 18 · see citing works

A rat pharmacokinetic/pharmacodynamic model for assessment of lipopolysaccharide-induced tumor necrosis factor-alpha production

Wang, Q., Zhang, Y., Hall, J. P., Lin, L., Raut, U., Mollova, N. N., Green, N., Cuozzo, J. W., Chesley, S., Xu, X., et al. (2007) · Journal of Pharmacological and Toxicological Methods · doi:10.1016/j.vascn.2007.02.001 · Cited by 18 · see citing works

Plasma timolol levels and systolic time intervals

Singh, B. N., Williams, F. M., Whitlock, R. M. L., Collett, J., & Chew, C. (1980) · Clinical Pharmacology & Therapeutics · doi:10.1038/clpt.1980.145 · Cited by 18 · see citing works

Translational pharmacokinetic–pharmacodynamic modelling; application to cardiovascular safety data for PF‐00821385, a novel HIV agent

Langdon, G., Davis, J. D., McFadyen, L., Dewhurst, M., Brunton, N. S., Rawal, J. K., van der Graaf, P. H., & Benson, N. (2009) · British Journal of Clinical Pharmacology · doi:10.1111/j.1365-2125.2009.03594.x · Cited by 16 · see citing works

Development of a Preclinical PK/PD Model to Assess Antitumor Response of a Sequential Aflibercept and Doxorubicin-Dosing Strategy in Acute Myeloid Leukemia

Fetterly, G. J., Aras, U., Lal, D., Murphy, M., Meholick, P. D., & Wang, E. S. (2013) · The AAPS Journal · doi:10.1208/s12248-013-9480-8 · Cited by 13 · see citing works

Integrating Experimentation and Quantitative Modeling to Enhance Discovery of Beta Amyloid Lowering Therapeutics for Alzheimer’s Disease

Lu, Y. (2012) · Frontiers in Pharmacology · doi:10.3389/fphar.2012.00177 · Cited by 8 · see citing works

Preclinical PK/PD modeling and human efficacious dose projection for a glucokinase activator in the treatment of diabetes

Zager, M. G., Kozminski, K. D., Pascual, B., Ogilvie, K. M., & Sun, S. (2014) · Journal of Pharmacokinetics and Pharmacodynamics · doi:10.1007/s10928-014-9351-7 · Cited by 6 · see citing works

Translational pharmacokinetic/pharmacodynamic analysis in cancer pharmacology: a tool to maximize the value of antitumor efficacy from tumor bearing mice

Wong, H., & Gould, S. E. (2016) · Drug Discovery Today Technologies · doi:10.1016/j.ddtec.2016.08.003 · Cited by 5 · see citing works

Steady-State Pharmacokinetics and Pharmacodynamics of Benazeprilat in Spontaneously Hypertensive Rats (SHR) and Wistar–Kyoto (WKY) Rats

LeRoy, S., & Berner, B. (1991) · Pharmaceutical Research · doi:10.1023/a:1015803529013 · Cited by 4 · see citing works

Applications of Quantitative Systems Pharmacology in Model‐Informed Drug Discovery: Perspective on Impact and Opportunities

Bradshaw‐Pierce, E. L., Spilker, M. E., Zang, R., Bansal, L., He, H., Jones, R. D. O., Le, K. N., Penney, M., Schuck, E. L., Topp, B. G., et al. (2019) · CPT Pharmacometrics & Systems Pharmacology · doi:10.1002/psp4.12463 · Cited by 93 · see citing works

Model-based Target Pharmacology Assessment (mTPA): An Approach Using PBPK/PD Modeling and Machine Learning to Design Medicinal Chemistry and DMPK Strategies in Early Drug Discovery

Chen, E. P., Bondi, R. W., & Michalski, P. J. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c02033 · Cited by 44 · see citing works

Design and Measurement of Drug Tissue Concentration Asymmetry and Tissue Exposure-Effect (Tissue PK-PD) Evaluation

Zang, R., Barth, A., Wong, H., Mařı́k, J., Shen, J., Lade, J. M., Grove, K. J., Durk, M. R., Parrott, N. J., Rudewicz, P. J., et al. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c00502 · Cited by 37 · see citing works

Translational and pharmacokinetic‐pharmacodynamic application for the clinical development of GDC‐0334, a novel TRPA1 inhibitor

Chan, P., Ding, H. T., Liederer, B. M., Mao, J., Belloni, P., Chen, L., Gao, S. S., Joseph, V. T., Yang, X., Lin, J. S., et al. (2021) · Clinical and Translational Science · doi:10.1111/cts.13049 · Cited by 23 · see citing works

Translating pharmacology models effectively to predict therapeutic benefit

Dudal, S., Bissantz, C., Caruso, A., David‐Pierson, P., Driessen, W. H. P., Koller, E., Krippendorff, B., Lechmann, M., Olivares‐Morales, A., Paehler, A., et al. (2022) · Drug Discovery Today · doi:10.1016/j.drudis.2022.03.009 · Cited by 16 · see citing works

Exposure-Effect Relationships in Established Rat Adjuvant-Induced and Collagen-Induced Arthritis: A Translational Pharmacokinetic-Pharmacodynamic Analysis

Wong, H., Liu, L., Ouyang, W., Deng, Y., Wright, M. R., & Hop, C. E. C. A. (2019) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.118.255562 · Cited by 16 · see citing works

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Gibbs, J. P., Yuraszeck, T. M., Biesdorf, C., Xu, Y., & Kasichayanula, S. (2020) · The Journal of Clinical Pharmacology · doi:10.1002/jcph.1706 · Cited by 15 · see citing works

Pharmacokinetics/pharmacometabolomics-pharmacodynamics reveals the synergistic mechanism of a multicomponent herbal formula, Baoyuan decoction against cardiac hypertrophy

Du, Z., Lu, Y., Sun, J., Chang, K., Lu, M., Fang, M., Zeng, X., Zhang, W., Song, J., Guo, X., et al. (2021) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2021.111665 · Cited by 15 · see citing works

Preclinical Animal Models to Investigate the Role of Nav1.7 Ion Channels in Pain

Yogi, Á., Banderali, U., Moreno, M., & Martina, M. (2025) · Life · doi:10.3390/life15040640 · Cited by 12 · see citing works

Predictive Platforms of Bond Cleavage and Drug Release Kinetics for Macromolecule–Drug Conjugates

Ghosal, S., Walker, J. E., & Alabi, C. A. (2021) · Annual Review of Chemical and Biomolecular Engineering · doi:10.1146/annurev-chembioeng-091720-030636 · Cited by 11 · see citing works

A quantitative systems pharmacology approach to predict the safe‐equivalent dose of doxorubicin in patients with cardiovascular comorbidity

Sang, L., Yuan, Y. H., Zhou, Y. F., Zhou, Z., Jiang, M., Liu, X., Hao, K., & He, H. (2021) · CPT Pharmacometrics & Systems Pharmacology · doi:10.1002/psp4.12719 · Cited by 11 · see citing works

Translational PK/PD: a retrospective analysis of performance and impact from a drug portfolio

Jansson‐Löfmark, R., Fridén, M., Badolo, L., Ahlström, C., Gurrell, I. K., Pangalos, M. N., & Jones, R. D. O. (2025) · Drug Discovery Today · doi:10.1016/j.drudis.2025.104417 · Cited by 10 · see citing works

Application of Pharmacokinetic-Pharmacodynamic Modeling to Inform Translation of In Vitro NaV1.7 Inhibition to In Vivo Pharmacological Response in Non-human Primate

Ballard, J. E., Pall, P. S., Vardigan, J. D., Zhao, F., Holahan, M. A., Kraus, R. L., Li, Y., Henze, D. A., Houghton, A. K., Burgey, C. S., et al. (2020) · Pharmaceutical Research · doi:10.1007/s11095-020-02914-9 · Cited by 8 · see citing works

Translational Pharmacokinetic–Pharmacodynamic Modeling of NaV1.7 Inhibitor MK-2075 to Inform Human Efficacious Dose

Ballard, J. E., Pall, P. S., Vardigan, J. D., Zhao, F., Holahan, M. A., Zhou, X., Jochnowitz, N., Kraus, R. L., Klein, R. M., Henze, D. A., et al. (2021) · Frontiers in Pharmacology · doi:10.3389/fphar.2021.786078 · Cited by 8 · see citing works

Mechanistic Multilayer Quantitative Model for Nonlinear Pharmacokinetics, Target Occupancy and Pharmacodynamics (PK/TO/PD) Relationship of D-Amino Acid Oxidase Inhibitor, TAK-831 in Mice

Yoneyama, T., Sato, S., Sykes, A. P., Fradley, R. L., Stafford, S., Bechar, S., Howley, E., Patel, T. R., Tagawa, Y., Moriwaki, T., et al. (2020) · Pharmaceutical Research · doi:10.1007/s11095-020-02893-x · Cited by 8 · see citing works

Drug discovery

Bateman, T. J. (2021) · Elsevier eBooks · doi:10.1016/b978-0-12-819869-8.00019-7 · Cited by 6 · see citing works

Physiologically‐based pharmacokinetic/pharmacodynamic modeling to predict tumor growth inhibition and the efficacious dose of selective estrogen receptor degraders in humans

Ganti, A., Yu, S., Sharpnack, D., Ingalla, E., & Bruyn, T. D. (2023) · Biopharmaceutics & Drug Disposition · doi:10.1002/bdd.2358 · Cited by 6 · see citing works

Translational PBPK/PD modeling in drug discovery: A CRO perspective

Esposito, S., & Cebrián, D. Á. (2025) · Drug Discovery Today · doi:10.1016/j.drudis.2025.104427 · Cited by 5 · see citing works

Zebrafish as a multimodal platforms for anti-inflammatory phytomedicine discovery and translation

Tan, X., Liu, H., Liang, F., & Chen, G. (2026) · Frontiers in Pharmacology · doi:10.3389/fphar.2026.1775366 · Cited by 4 · see citing works

Translational Model‐Informed Dose Selection for a Human Positron Emission Tomography Imaging Study of JNJ‐54175446, a P2X7 Receptor Antagonist

Xu, Y. C., Miao, X., Ravenstijn, P. G. M., Hijzen, A., Schmidt, M. E., Nandy, P., & Zhou, H. (2019) · Clinical and Translational Science · doi:10.1111/cts.12711 · Cited by 4 · see citing works

Preclinical Modeling of Navtemadlin Pharmacokinetics, Pharmacodynamics, and Efficacy in IDH–Wild-type Glioblastoma

Vaubel, R. A., Zhang, W., Oh, J.-H., Mladek, A. C., Pasa, T. I., Gantchev, J. K., Waller, K. L., Baquer, G., Stopka, S. A., Regan, M. S., et al. (2025) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-25-0244 · Cited by 2 · see citing works

Application value of quantitative system pharmacology in drug discovery for traditional Chinese medicine

Meng, F., & Tao, X. (2020) · Journal of Medical Care Research and Review · doi:10.15520/mcrr.v3i9.113 · Cited by 1 · see citing works

Pharmacokinetic Models of Tafenoquine: Insights for Optimal Malaria Treatment Strategies

Santos, L. O., Alves, I. A., & Azeredo, F. J. (2024) · Pharmaceutics · doi:10.3390/pharmaceutics16091124 · Cited by 2 · see citing works

Pharmacokinetic-Pharmacodynamic-Efficacy Modeling of ONO-7579, a Novel Pan–Tropomyosin Receptor Kinase Inhibitor, in a Murine Xenograft Tumor Model

Iida, H., Fujikawa, R., Kozaki, R., Harada, R., Hosokawa, Y., Ogawara, K., & Ohno, T. (2020) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.119.264499 · Cited by 2 · see citing works

Oral hyoscine butylbromide exerts spasmolytic effects in both gastrointestinal and urogenital tissues in rats

Traserra, S., Appelqvist, T., Lange, R., Corsetti, M., & Jiménez, M. (2025) · British Journal of Pharmacology · doi:10.1111/bph.17474 · Cited by 1 · see citing works

Integrated pharmacokinetic/pharmacodynamic/efficacy analysis in oncology: importance of pharmacodynamic/efficacy relationships

Wong, H. (2023) · Elsevier eBooks · doi:10.1016/b978-0-12-817134-9.00015-5

Pharmacodynamics‐informed Drug Discovery

Chen, E. P. (2025) · Wiley eBooks · doi:10.1002/9781119650263.ch13

The role of mechanism-based pharmacokinetic–pharmacodynamic (PK–PD) modelling in translational research of biologics

Agoram, B. M., Martin, S. W., & van der Graaf, P. H. (2007) · Drug Discovery Today · doi:10.1016/j.drudis.2007.10.002 · Cited by 143 · see citing works

Translational PK/PD modeling to increase probability of success in drug discovery and early development

Lavé, T., Caruso, A., Parrott, N. J., & Walz, A. (2016) · Drug Discovery Today Technologies · doi:10.1016/j.ddtec.2016.11.005 · Cited by 36 · see citing works

The virtue of translational PKPD modeling in drug discovery: selecting the right clinical candidate while sparing animal lives

Bueters, T., Ploeger, B. A., & Visser, S. A. G. (2013) · Drug Discovery Today · doi:10.1016/j.drudis.2013.05.001 · Cited by 43 · see citing works

Development of Translational Pharmacokinetic–Pharmacodynamic Models

Mager, D. E., & Jusko, W. J. (2008) · Clinical pharmacology and therapy · doi:10.1038/clpt.2008.52 · Cited by 122 · see citing works

Translational PK/PD: a retrospective analysis of performance and impact from a drug portfolio

Jansson‐Löfmark, R., Fridén, M., Badolo, L., Ahlström, C., Gurrell, I. K., Pangalos, M. N., & Jones, R. D. O. (2025) · Drug Discovery Today · doi:10.1016/j.drudis.2025.104417 · Cited by 10 · see citing works