Establishing in vitro to clinical correlations in the evaluation of cardiovascular safety pharmacology

Drug Discovery Today: Technologies

Volumn 10, Issue 3, 2013, Pages

  Chain, A S Y ^a   Sturkenboom, M C J M ^b   Danhof, M ^a   Pasqua, O E Della ^a,c  

^a LEIDEN UNIVERSITY   (Netherlands)

^b ERASMUS MEDICAL CENTER   (Netherlands)

^c GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

CIPROFLOXACIN; CISAPRIDE; DOFETILIDE; FLECAINIDE; GREPAFLOXACIN; LEVOFLOXACIN; MOXIFLOXACIN; OFLOXACIN; POTASSIUM CHANNEL HERG; QUINIDINE; SOTALOL; TERFENADINE;

ANESTHESIA; CALCIUM CURRENT; CARDIOVASCULAR RISK; CONSCIOUSNESS; DECISION TREE; DRUG EFFECT; DRUG SAFETY; ELECTROCARDIOGRAPHY MONITORING; HEART ARRHYTHMIA; HEART CONDUCTION; HEART MUSCLE POTENTIAL; HEART RATE; HEART REPOLARIZATION; HEART RHYTHM; HUMAN; IC 50; IN VITRO STUDY; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; POTASSIUM CURRENT; QT INTERVAL; QT PROLONGATION; REVIEW; RISK ASSESSMENT; SODIUM CURRENT; TORSADE DES POINTES;

ANIMALS; CARDIOVASCULAR SYSTEM; DRUG EVALUATION, PRECLINICAL; DRUGS, INVESTIGATIONAL; HUMANS; PHARMACOLOGY, CLINICAL; TRANSLATIONAL MEDICAL RESEARCH;

EID: 84879243310     PISSN: None     EISSN: 17406749     Source Type: Journal    
DOI: 10.1016/j.ddtec.2012.07.001     Document Type: Review

References (69)

1. K.E. Lasser Timing of new black box warnings and withdrawals for prescription medications JAMA 287 2002 2215 2220
2. B. Munos Lessons from 60 years of pharmaceutical innovation Nat. Rev. Drug Discov. 8 2009 959 968
3. J.P. Valentin, and T. Hammond Safety and secondary pharmacology: successes, threats, challenges and opportunities J. Pharmacol. Toxicol. Methods 58 2008 77 87
4. H.G. Laverty How can we improve our understanding of cardiovascular safety liabilities to develop safer medicines Br. J. Pharmacol. 163 2011 675 693
5. C.M. Krejsa Predicting ADME properties and side effects: the BioPrint approach Curr. Opin. Drug Discov. Dev. 6 2003 470 480
6. D.S. Budnitz National surveillance of emergency department visits for outpatient adverse drug events JAMA 296 2006 1858 1866
7. X. Yao Predicting QT prolongation in humans during early drug development using hERG inhibition and an anaesthetized guinea-pig model Br. J. Pharmacol. 154 2008 1446 1456
8. N. Guler The effects of volatile anesthetics on the Q-Tc interval J. Cardiothorac. Vasc. Anesth. 15 2001 188 191
9. Nolvadex (Tamoxifen) Package Insert 1999 LP. AZP
10. C.E. Pollard An introduction to QT interval prolongation and non-clinical approaches to assessing and reducing risk Br. J. Pharmacol. 159 2010 12 21
11. J. Ducroq Action potential experiments complete hERG assay and QT-interval measurements in cardiac preclinical studies J. Pharmacol. Toxicol. Methods 56 2007 159 170
12. H.M. Vargas Scientific review and recommendations on preclinical cardiovascular safety evaluation of biologics J. Pharmacol. Toxicol. Methods 58 2008 72 76
13. P. Milberg Comparison of the in vitro electrophysiologic and proarrhythmic effects of amiodarone and sotalol in a rabbit model of acute atrioventricular block J. Cardiovasc. Pharmacol. 44 2004 278 286
14. W.S. Redfern Relationships between preclinical cardiac electrophysiology, clinical QT interval prolongation and torsade de pointes for a broad range of drugs: evidence for a provisional safety margin in drug development Cardiovasc. Res. 58 2003 32 45
15. R.R. Shah Drugs, QT interval prolongation and ICH E14: the need to get it right Drug Saf. 28 2005 115 125
16. T. Omata QT PRODACT: comparison of non-clinical studies for drug-induced delay in ventricular repolarization and their role in safety evaluation in humans J. Pharmacol. Sci. 99 2005 531 541
17. R. Webster Towards a drug concentration effect relationship for QT prolongation and torsades de pointes Curr. Opin. Drug Discov. Dev. 5 2002 116 126
18. C.L. Lawrence Nonclinical proarrhythmia models: predicting Torsades de Pointes J. Pharmacol. Toxicol. Methods 52 2005 46 59
19. N. Lee The continuing evolution of torsades de pointes liability testing methods: is there an end in sight? Toxicol. Appl. Pharmacol. 243 2010 146 153
20. ICH Topic S7B The Nonclinical Evaluation of the Potential for Delayed Ventricular Repolarization (QT Interval Prolongation) by Human Pharmaceuticals 2005
21. M. Holbrook Drug induced shortening of the QT/QTc interval: an emerging safety issue warranting further modelling and evaluation in drug research and development? J. Pharmacol. Toxicol. Methods 59 2009 21 28
22. G.A. Gintant The canine Purkinje fiber: an in vitro model system for acquired long QT syndrome and drug-induced arrhythmogenesis J. Cardiovasc. Pharmacol. 37 2001 607 618
23. D.P. Zipes Mechanisms of clinical arrhythmias J. Cardiovasc. Electrophysiol. 14 2003 902 912
24. L. Eckardt Experimental models of torsade de pointes Cardiovasc. Res. 39 1998 178 193
25. T.G. Hammond Methods of collecting and evaluating non-clinical cardiac electrophysiology data in the pharmaceutical industry: results of an international survey Cardiovasc. Res. 49 2001 741 750
26. B.D. Guth Developing a strategy for the nonclinical assessment of proarrhythmic risk of pharmaceuticals due to prolonged ventricular repolarization J. Pharmacol. Toxicol. Methods 49 2004 159 169
27. H.R. Lu Predicting drug-induced changes in QT interval and arrhythmias: QT-shortening drugs point to gaps in the ICHS7B guidelines Br. J. Pharmacol. 154 2008 1427 1438
28. R.L. Martin The utility of hERG and repolarization assays in evaluating delayed cardiac repolarization: influence of multi-channel block J. Cardiovasc. Pharmacol. 43 2004 369 379
29. D.A. Terrar Comparison of guinea-pig ventricular myocytes and dog Purkinje fibres for in vitro assessment of drug-induced delayed repolarization J. Pharmacol. Toxicol. Methods 56 2007 171 185
30. P. Milberg Proarrhythmia as a class effect of quinolones: increased dispersion of repolarization and triangulation of action potential predict torsades de pointes J. Cardiovasc. Electrophysiol. 18 2007 647 654
31. M.B. Thomsen Increased short-term variability of repolarization predicts d-sotalol-induced torsades de pointes in dogs Circulation 110 2004 2453 2459
32. C. Antzelevitch, and W. Shimizu Cellular mechanisms underlying the long QT syndrome Curr. Opin. Cardiol. 17 2002 43 51
33. L.M. Hondeghem Instability and triangulation of the action potential predict serious proarrhythmia, but action potential duration prolongation is antiarrhythmic Circulation 103 2001 2004 2013
34. L.M. Hondeghem Phase 2 prolongation, in the absence of instability and triangulation, antagonizes class III proarrhythmia Cardiovasc. Res. 50 2001 345 353
35. W. Suter Predictive value of in vitro safety studies Curr. Opin. Chem. Biol. 10 2006 362 366
36. S.P. Pinney Terfenadine increases the QT interval in isolated guinea pig heart J. Cardiovasc. Pharmacol. 25 1995 30 34
37. S. Szilagyi The effects of levosimendan and OR-1896 on isolated hearts, myocyte-sized preparations and phosphodiesterase enzymes of the guinea pig Eur. J. Pharmacol. 486 2004 67 74
38. L. Wu Antiarrhythmic effects of ranolazine in a guinea pig in vitro model of long-QT syndrome J. Pharmacol. Exp. Ther. 310 2004 599 605
39. X. Chen Use of arterially perfused rabbit ventricular wedge in predicting arrhythmogenic potentials of drugs J. Pharmacol. Toxicol. Methods 54 2006 261 272
40. B.M. Heath Translation of flecainide- and mexiletine-induced cardiac sodium channel inhibition and ventricular conduction slowing from nonclinical models to clinical J. Pharmacol. Toxicol. Methods 63 2011 258 268
41. ICH Topic S7A Safety Pharmacology Studies for Human Pharmaceuticals 2000
42. F. De Clerck In vivo measurement of QT prolongation, dispersion and arrhythmogenesis: application to the preclinical cardiovascular safety pharmacology of a new chemical entity Fundam. Clin. Pharmacol. 16 2002 125 140
43. D.S. Hauser Cardiovascular parameters in anaesthetized guinea pigs: a safety pharmacology screening model J. Pharmacol. Toxicol. Methods 52 2005 106 114
44. L.A. Hanson ILSI-HESI cardiovascular safety subcommittee initiative: evaluation of three non-clinical models of QT prolongation J. Pharmacol. Toxicol. Methods 54 2006 116 129
45. S.D. Pettit A call for more integrated cardiovascular safety assessment J. Pharmacol. Toxicol. Methods 61 2010 1 2
46. S. Authier Conscious and anesthetized non-human primate safety pharmacology models: hemodynamic sensitivity comparison J. Pharmacol. Toxicol. Methods 58 2008 94 98
47. K. Ando QT PRODACT: in vivo QT assay with a conscious monkey for assessment of the potential for drug-induced QT interval prolongation J. Pharmacol. Sci. 99 2005 487 500
48. K.J. Watson Pharmacokinetic-pharmacodynamic modelling of the effect of Moxifloxacin on QTc prolongation in telemetered cynomolgus monkeys J. Pharmacol. Toxicol. Methods 63 2011 304 313
49. G. Bode The utility of the minipig as an animal model in regulatory toxicology J. Pharmacol. Toxicol. Methods 62 2010 196 220
50. M. Markert Validation of the normal, freely moving Gottingen minipig for pharmacological safety testing J. Pharmacol. Toxicol. Methods 60 2009 79 87
51. A.A. Fossa Differential effect of HERG blocking agents on cardiac electrical alternans in the guinea pig Eur. J. Pharmacol. 486 2004 209 221
52. R.L. Hamlin QT and RR intervals in conscious and anesthetized guinea pigs with highly varying RR intervals and given QTc-lengthening test articles Toxicol. Sci. 76 2003 437 442
53. L. Testai QT prolongation in anaesthetized guinea-pigs: an experimental approach for preliminary screening of torsadogenicity of drugs and drug candidates J. Appl. Toxicol. 24 2004 217 222
54. K.J. Sampson A computational model of Purkinje fibre single cell electrophysiology: implications for the long QT syndrome J. Physiol. 588 Pt 14 2010 2643 2655
55. D. Bottino Preclinical cardiac safety assessment of pharmaceutical compounds using an integrated systems-based computer model of the heart Prog. Biophys. Mol. Biol. 90 2006 414 443
56. G.R. Mirams Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk Cardiovasc. Res. 91 2011 53 61
57. A. Sivarajah Cardiovascular safety assessments in the conscious telemetered dog: utilisation of super-intervals to enhance statistical power J. Pharmacol. Toxicol. Methods 62 2010 12 19
58. A. Ollerstam Comparison of the QT interval response during sinus and paced rhythm in conscious and anesthetized beagle dogs J. Pharmacol. Toxicol. Methods 56 2007 131 144
59. S.W. Mittelstadt, and S.M. Hart Effects of moxifloxacin on QT interval in conscious dogs J. Vet. Pharmacol. Ther. 28 2005 253 256
60. R.L. Lalonde Model-based drug development Clin. Pharmacol. Ther. 82 2007 21 32
61. I. Cavero Using pharmacokinetic/pharmacodynamic modelling in safety pharmacology to better define safety margins: a regional workshop of the Safety Pharmacology Society Expert Opin. Drug Saf. 6 2007 465 471
62. G. Langdon Translational pharmacokinetic-pharmacodynamic modelling; application to cardiovascular safety data for PF-00821385, a novel HIV agent Br. J. Clin. Pharmacol. 69 2010 336 345
63. A. Fleury A pharmacokinetic-pharmacodynamic model for cardiovascular safety assessment of R1551 J. Pharmacol. Toxicol. Methods 63 2010 123 133
64. A. Ollerstam Pharmacokinetic-pharmacodynamic modeling of drug-induced effect on the QT interval in conscious telemetered dogs J. Pharmacol. Toxicol. Methods 53 2006 174 183
65. M. Danhof Mechanism-based pharmacokinetic-pharmacodynamic (PK-PD) modeling in translational drug research Trends Pharmacol. Sci. 29 2008 186 191
66. K.P. Zuideveld Allometric scaling of pharmacodynamic responses: application to 5-Ht1A receptor mediated responses from rat to man Pharm. Res. 24 2007 2031 2039
67. D.M. Jonker A pharmacokinetic-pharmacodynamic model for the quantitative prediction of dofetilide clinical QT prolongation from human ether-a-go-go-related gene current inhibition data Clin. Pharmacol. Ther. 77 2005 572 582
68. A.S. Chain Assessing the probability of drug-induced QTc-interval prolongation during clinical drug development Clin. Pharmacol. Ther. 90 2011 867 875
69. R. Krishna Model-based evaluation of QTc interval risk: an increasing emphasis on early decision making J. Clin. Pharmacol. 49 2009 1010 1011