All Stories

  1. Bundling arrows: improving translational CNS drug development by integrated PK/PD-metabolomics

    Article • Expert Opinion on Drug Discovery, March 2018, Taylor & Francis

    Professor Piet H. van der Graaf

  2. A SYSTEMS PHARMACOLOGY MODEL TO EXPLAIN DEVELOPMENTAL DIFFERENCES IN SENSITIVITY TO DRUG-INDUCED QT PROLONGATION

    Article • Archives of Disease in Childhood, December 2015, BMJ

    Professor Piet H. van der Graaf

  3. Structure-Based Prediction of Anti-infective Drug Concentrations in the Human Lung Epithelial Lining Fluid

    Article • Pharmaceutical Research, December 2015, Springer Science + Business Media

    Professor Piet H. van der Graaf

  4. Mechanistic models enable the rational use ofin vitrodrug-target binding kinetics for better drug effects in patients

    Article • Expert Opinion on Drug Discovery, October 2015, Informa Healthcare

    Professor Piet H. van der Graaf

  5. Prediction of long-term treatment outcome in HCV following 24 day PEG-IFN alpha-2b therapy using population pharmacokinetic-pharmacodynamic mixture modeling and classification analysis

    Article • Journal of Theoretical Biology, October 2015, Elsevier

    Professor Piet H. van der Graaf

  6. Towards integrative systems pharmacology models in oncology drug development

    Article • Drug Discovery Today Technologies, August 2015, Elsevier

    Professor Piet H. van der Graaf

  7. Topics in Mathematical Pharmacology

    Article • Journal of Dynamics and Differential Equations, July 2015, Springer Science + Business Media

    Professor Piet H. van der Graaf

  8. Sensitivity of pharmacokinetic–pharmacodynamic analysis for detecting small magnitudes of QTc prolongation in preclinical safety testing

    Article • Journal of Pharmacological and Toxicological Methods, March 2015, Elsevier

    Professor Piet H. van der Graaf

  9. Drug Disposition in Obesity: Toward Evidence-Based Dosing

    Article • The Annual Review of Pharmacology and Toxicology, January 2015, Annual Reviews

    Professor Piet H. van der Graaf

  10. Translating the gap in the evaluation of drug-induced QTc-interval prolongation from in vivo to the clinic

    Article • Journal of Pharmacological and Toxicological Methods, November 2014, Elsevier

    Professor Piet H. van der Graaf

  11. The rise of systems pharmacology in drug discovery and development

    Article • Future Medicinal Chemistry, October 2014, Future Science

    Professor Piet H. van der Graaf

  12. Pharmacometrics in Cardiovascular Safety

    Article • January 2014, Springer Science + Business Media

    Professor Piet H. van der Graaf

  13. Pharmacodynamic modeling of cough responses to capsaicin inhalation calls into question the utility of the C5 end point

    Article • Journal of Allergy and Clinical Immunology, October 2013, Elsevier

    Professor Piet H. van der Graaf

  14. A4S: A user-friendly graphical tool for pharmacokinetic and pharmacodynamic (PK/PD) simulation

    Article • Computer Methods and Programs in Biomedicine, May 2013, Elsevier

    Professor Piet H. van der Graaf

  15. A mathematical model of the human menstrual cycle for the administration of GnRH analogues

    Article • Journal of Theoretical Biology, March 2013, Elsevier

    Professor Piet H. van der Graaf

  16. Cross-membrane signal transduction of receptor tyrosine kinases (RTKs): from systems biology to systems pharmacology

    Article • Journal of Mathematical Biology, December 2012, Springer Science + Business Media

    Professor Piet H. van der Graaf

  17. CPT: Pharmacometrics and Systems Pharmacology

    Article • CPT Pharmacometrics & Systems Pharmacology, September 2012, Wiley

    Professor Piet H. van der Graaf

  18. Mechanism-based PK–PD model for the prolactin biological system response following an acute dopamine inhibition challenge: quantitative extrapolation to humans

    Article • Journal of Pharmacokinetics and Pharmacodynamics, July 2012, Springer Science + Business Media

    Professor Piet H. van der Graaf

  19. Biomarkers and biomeasures: key enablers for pharmacokinetic–pharmacodynamic modeling in drug discovery and development

    Article • Bioanalysis, June 2012, Future Science

    Professor Piet H. van der Graaf

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

    Article • Drug Discovery Today, May 2012, Elsevier

    Professor Piet H. van der Graaf

  21. Use of modelling and simulation techniques to support decision making on the progression of PF-04878691, a TLR7 agonist being developed for hepatitis C

    Article • British Journal of Clinical Pharmacology, December 2011, Wiley

    Professor Piet H. van der Graaf

  22. Quantitative pharmacological analysis of antagonist binding kinetics at CRF1 receptors in vitro and in vivo

    Article • British Journal of Pharmacology, September 2011, Wiley

    Professor Piet H. van der Graaf

  23. Translation of drug-induced QTc prolongation in early drug development

    Article • Journal of Pharmacological and Toxicological Methods, July 2011, Elsevier

    Oscar Della Pasqua, Professor Piet H. van der Graaf

  24. Mathematical analysis of the pharmacokinetic–pharmacodynamic (PKPD) behaviour of monoclonal antibodies: Predicting in vivo potency

    Article • Journal of Theoretical Biology, July 2011, Elsevier

    Professor Piet H. van der Graaf

  25. Systems Pharmacology: Bridging Systems Biology and Pharmacokinetics-Pharmacodynamics (PKPD) in Drug Discovery and Development

    Article • Pharmaceutical Research, May 2011, Springer Science + Business Media

    Professor Piet H. van der Graaf

  26. Pharmacokinetic–pharmacodynamic modelling of the effect of Moxifloxacin on QTc prolongation in telemetered cynomolgus monkeys

    Article • Journal of Pharmacological and Toxicological Methods, May 2011, Elsevier

    Professor Piet H. van der Graaf

  27. Pharmacodynamic-Pharmacokinetic Integration as a Guide to Medicinal Chemistry

    Article • Current Topics in Medicinal Chemistry, February 2011, Bentham Science Publishers

    Professor Piet H. van der Graaf

  28. Cardiovascular profiles of beta3 agonists

    Article • Journal of Pharmacological and Toxicological Methods, September 2010, Elsevier

    Professor Piet H. van der Graaf

  29. PK/PD Modelling: Validation and use of iterative development of experimental designs

    Article • Journal of Pharmacological and Toxicological Methods, September 2010, Elsevier

    Professor Piet H. van der Graaf

  30. Impact of protein binding on receptor occupancy: A two-compartment model

    Article • Journal of Theoretical Biology, August 2010, Elsevier

    Professor Piet H. van der Graaf

  31. ChemInform Abstract: Synthesis and Use of FSCPX, an Irreversible Adenosine A1 Antagonist, as a “Receptor Knock-Down” Tool.

    Article • ChemInform, May 2010, Wiley

    Professor Piet H. van der Graaf

  32. Online solid phase extraction with liquid chromatography–tandem mass spectrometry to analyze remoxipride in small plasma-, brain homogenate-, and brain microdialysate samples

    Article • Journal of Chromatography B, April 2010, Elsevier

    Professor Piet H. van der Graaf

  33. Translational pharmacokinetic-pharmacodynamic modelling; application to cardiovascular safety data for PF-00821385, a novel HIV agent

    Article • British Journal of Clinical Pharmacology, April 2010, Wiley

    Professor Piet H. van der Graaf

  34. Estimation of binding rate constants using a simultaneous mixed-effects method: application to monoamine transporter reuptake inhibitor reboxetine

    Article • British Journal of Pharmacology, March 2010, Wiley

    Professor Piet H. van der Graaf

  35. Optimising in vivo pharmacology studies—Practical PKPD considerations

    Article • Journal of Pharmacological and Toxicological Methods, March 2010, Elsevier

    Professor Piet H. van der Graaf

  36. Pharmacokinetic–pharmacodynamic reasoning in drug discovery and early development

    Article • Future Medicinal Chemistry, November 2009, Future Science

    Professor Piet H. van der Graaf

  37. Incorporating Receptor Theory in Mechanism-Based Pharmacokinetic-Pharmacodynamic (PK-PD) Modeling

    Article • Drug Metabolism and Pharmacokinetics, January 2009, Japanese Society for the Study of Xenobiotics

    Professor Piet H. van der Graaf

  38. Impact of plasma-protein binding on receptor occupancy: An analytical description

    Article • Journal of Theoretical Biology, January 2009, Elsevier

    Professor Piet H. van der Graaf

  39. A non-parametric method to analyse time-course of effect in the absence of pharmacokinetic data: Application to inhaled bronchodilators

    Article • European Journal of Pharmaceutical Sciences, August 2008, Elsevier

    Professor Piet H. van der Graaf

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

    Article • Drug Discovery Today, December 2007, Elsevier

    Professor Piet H. van der Graaf

  41. IMPACT OF EXPERIMENTAL DESIGN AND PK/PD MODELING ON SAFETY MARGIN ESTIMATION: A CASE STUDY

    Article • Journal of Pharmacological and Toxicological Methods, September 2007, Elsevier

    Professor Piet H. van der Graaf

  42. Allometric Scaling of Pharmacodynamic Responses: Application to 5-Ht1A Receptor Mediated Responses from Rat to Man

    Article • Pharmaceutical Research, May 2007, Springer Science + Business Media

    Professor Piet H. van der Graaf

  43. Current methods used to investigate G protein coupled receptor oligomerisation

    Article • Journal of Pharmacological and Toxicological Methods, July 2006, Elsevier

    Professor Piet H. van der Graaf

  44. Novel Selective Inhibitors of Neutral Endopeptidase for the Treatment of Female Sexual Arousal Disorder. Synthesis and Activity of Functionalized Glutaramides

    Article • Journal of Medicinal Chemistry, July 2006, American Chemical Society (ACS)

    Professor Piet H. van der Graaf

  45. Correlation between affinity and efficacy

    Article • Trends in Pharmacological Sciences, January 2003, Elsevier

    Professor Piet H. van der Graaf

  46. Modulation of agonist responses at the A1 adenosine receptor by an irreversible antagonist, receptor–G protein uncoupling and by the G protein activation state

    Article • Biochemical Pharmacology, October 2002, Elsevier

    Professor Piet H. van der Graaf

  47. Pharmacokinetic–pharmacodynamic modelling of the hypothermic and corticosterone effects of the 5-HT1A receptor agonist flesinoxan

    Article • European Journal of Pharmacology, June 2002, Elsevier

    Professor Piet H. van der Graaf

  48. Synthesis and use of FSCPX, an irreversible adenosine A1 antagonist, as a ‘Receptor Knock-Down’ tool

    Article • Bioorganic & Medicinal Chemistry Letters, March 2001, Elsevier

    Professor Piet H. van der Graaf

  49. High-performance liquid chromatography of the neuroactive steroids alphaxalone and pregnanolone in plasma using dansyl hydrazine as fluorescent label: application to a pharmacokinetic-pharmacodynamic study in rats

    Article • Journal of Chromatography B Biomedical Sciences and Applications, August 2000, Elsevier

    Professor Piet H. van der Graaf

  50. Enantioselective high-performance liquid chromatographic analysis of the 5-HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino)tetralin

    Article • Journal of Chromatography B Biomedical Sciences and Applications, January 2000, Elsevier

    Professor Piet H. van der Graaf

  51. Estimation of agonist affinity, using the slope of the concentration-effect curve: comment on the method of Calderone and Martinotti

    Article • Journal of Pharmacological and Toxicological Methods, November 1998, Elsevier

    Professor Piet H. van der Graaf