Assessment of QT liabilities in drug development

Cell Biology and Toxicology

Volumn 23, Issue 1, 2007, Pages 1-13

  Arrigoni, C ^a   Crivori, P ^a  

^a NERVIANO MEDICAL SCIENCES   (Italy)

Author keywords

ICH; In vitro; In vivo; QT prolongation; Safety pharmacology; Telemetry

Indexed keywords

AMIODARONE; DOFETILIDE; SOTALOL; TERFENADINE;

COMPUTER MODEL; CONFERENCE PAPER; DRUG FATALITY; DRUG SAFETY; HUMAN; IN VITRO STUDY; IN VIVO STUDY; NONHUMAN; PRACTICE GUIDELINE; PRIORITY JOURNAL; QT PROLONGATION; RISK ASSESSMENT; TORSADE DES POINTES;

ANIMALS; CARDIOVASCULAR SYSTEM; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; HUMANS; LONG QT SYNDROME; MODELS, ANIMAL; TORSADES DE POINTES;

RODENTIA;

EID: 33845680784     PISSN: 07422091     EISSN: None     Source Type: Journal    
DOI: 10.1007/s10565-006-0141-x     Document Type: Conference Paper

References (47)

1. Kr potassium channels with HERG and is associated with cardiac arrhythmia. Cell. 1999;97:175-87.
2. Albengres E, Le Louet H, Tillement JP. Systemic antifungal agents. Drug interactions of clinical significance. Drug Safety. 1998;18(2):83-97.
3. Anonymous Committee for Proprietary Medicinal Products (CPMP) Points to Consider: The assessment of the potential for QT interval prolongation by non-cardiovascular medicinal products. CPMP/986/96. 1997. [http://www.emea.eu. int/home.htm].
4. Anonymous. ICH S7A: Safety pharmacology studies for human pharmaceuticals (ICH step 5). CPMP/ICH/539/00. 2000. [http://www.emea.eu.int/pdfs/human/ich/ 053900en.pdf].
5. Anonymous. ICH S7B: The non-clinical evaluation of the potential for delayed ventricular repolarization (QT interval prolongation) by human pharmaceuticals (ICH step 4). CHMP/ICH/432/02. 2005a. [http://www.emea.eu.int/ pdfs/human/ich/042302en.pdf].
6. Anonymous. ICH E14: The clinical evaluation of Qt/Qtc interval prolongation and proarrhythmic potential for non-antiarrhythmic drugs. CHMP/ICH/2/04. 2005b. [http://www.emea.eu.int/pdfs/human/ich/000204en.pdf].
7. Bass AS, Tomaselli G, Bullingham R, Kinter LB. Drugs effects on ventricular repolarization: a critical evaluation of the strengths and weaknesses of current methodologies and regulatory practices. J Pharmacol Toxicol Methods. 2005;52:12-21.
8. Bazett HC. An analysis of the time-relations of electrocardiograms. Heart. 1918;7:353-370.
9. Cavalli A, Poluzzi E, De Ponti F, Recanatini M. Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers. J Med Chem. 2002;45:3844-53.
10. Chiang CE, Roden DM. The long QT syndromes: genetic basis and clinical implications. J Am Coll Cardiol. 2000; 36:1-12.
11. Cooper M, Branch C, Bastianse R, et al. Mathematical corrections for the inverse relationship between QT interval and heart rate in conscious beagle dogs and cynomolgus monkeys. Toxicol Sci. 2001;60:A1251.
12. Curran ME, Splawski I, Timothy KW, Vincent GM, Green ED, Keating MT. A molecular basis for cardiac arrhythmia: HERG mutations cause long QT syndrome. Cell. 1995;180:795-803.
13. Davies AJ, Harinda V, McEwan E, Ghose RR. Cardiotoxic effect with convulsions in terfenadine overdose. Br Med J. 1989;298:325.
14. Detweiler DK. Appropriateness of various laboratory species as models. Electrocardiography in toxicological studies. 1997;6:104-15.
15. +]o. J Pharmacol Toxicol Methods. 2004;50:187-99.
16. Ekins S. Predicting undesirable drug interactions with promiscuous proteins in silico. Drug Discov Today. 2004; 9(6):276-85.
17. Ekins S, Crumb WJ, Sarazan RD, Wikel JH, Wrighton SA. Three-dimensional quantitative structure-activity relationship for inhibition of human ether-a-go-go-related gene. J Pharmacol Exp Ther. 2002;301:427-34.
18. Fermini B, Fossa AA. The impact of drug-induced QT interval prolongation on drug discovery and development. Nat Rev Drug Discov. 2003;2:439-47.
19. Fredericia LS. Die systolendauer im elektrokardiogramm bei normalen menschen und bei herzkranken. Acta Med Scand. 1920;53:469-86.
20. Friedrichs GS, Patmore L, Bass AS. Non-clinical evaluation of ventricular repolarization (ICH S7B): results of an interim survey of international pharmaceutical companies. J. Pharmacol Toxicol Methods. 2005;52:6-11.
21. Granberry MC, Gardner SF. Erythromycin monotherapy associated with torsade de pointes. Ann Pharmacother. 1996;30(1):77-8.
22. Hammond TG, Carlsson L, Davis AS, et al. Methods of collecting and evaluating non-clinical cardiac electrophysiology data in the pharmaceutical industry: results of an international survey. Cardiovasc Res. 2001;49:741-50.
23. Katapady K, Kostandy G, Katapadi M, Hussain KM, Schifter D. A review of erythomycin-induced malignant tachyarrhythmia - torsade de pointes. A case report. Angiology. 1997;48(9): 821-6.
24. Kemp JP. Antihistamines - is there anything safe to prescribe? Ann Allergy. 1992;69:276-80.
25. Keseru GM. Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods. Bioorg Med Chem Lett. 2003;13:2773-5.
26. Koh KK, Rim MS, Yoon J, Kim SS. Torsade de pointes induced by terfenadine in a patient with long QT syndrome. J Electrocardiol. 1994;27(4):343-6.
27. Matsunaga T, Mitsui T, Harada T, et al. QT corrected for heart rate and relation between QT and RR intervals in bearle dogs. J Pharmacol Toxicol Methods. 1997;38:201-9.
28. Minkel JR. Open and shut: the case for ion channel screening. Drug Discov Dev. 2003;6(9):75-80.
29. Mitcheson JS, Chen J, Lin M, Culberson C, Sanguinetti MC. A structural basis for drug-induced long QT syndrome. Proc Natl Acad Sci USA. 2000;97:12329-33.
30. Mohler PJ, Gramolini AO, Bennet V. The Ankyrin-B C-terminal domain determines activity of Ankyrin-B/G chimeras in rescue of abnormal inositol 1,4,5-triphosphate and ryanodine receptor distribution in Ankyrin (-/-) neonatal cardiomyocytes. J Biol Chem. 2002;277:10599-607.
31. Monahan BP, Ferguson CL, Killeavy ES, Lloyd BK, Troy J, Cantilena LR Jr. Torsades de pointes occurring in association with terfenadine use. JAMA. 1990;264:2788-90.
32. O'Brien JM, Rockwood RP, Suh KI. Haloperidol-induced torsade de pointes. Ann Pharmacother. 1999;33(10):1046-50.
33. Osborne BE, Leach GDH. The beagle electrocardiogram. Food Cosmet Toxicol. 1971;9:857-64.
34. Pearlstein RA, Vaz RJ, Kang J, et al. Characterization of HERG potassium channel inhibition using CoMSiA 3D QSAR and homology modeling approaches. Bioorg Med Chem Lett. 2003;13:1829-35.
35. Piquette RK. Torsade de pointes induced by cisapride/clarythromycin interaction. Ann Pharmacother. 1999;33(1):22-6.
36. Redfern WS, Carlsson L, Davis S, et al. 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. 2003;58(1):32-45.
37. Roche O, Trube G, Zuegge J, Pflimlin P, Alanine A, Schneider G. A virtual screening method for prediction of the hERG potassium channel liability of compound libraries. Chem Biochem. 2002;3:455-9.
38. Roy ML, Dumaine R, Brown AM. HERG, a primary human ventricular target of the non-sedating antihistamine terfenadine. Circulation. 1996;94:817-23.
39. Sakemi H, Van Natta B. Torsade de pointes induced by astemizole in a patient with prolongation of the QT interval. Am Heart J. 1993;125(5 Pt 1):1436-8.
40. Sanguinetti MS, Mitcheson JS. Predicting drug-hERG channel interactions that cause acquired long QT syndrome. Trends Pharmacol Sci. 2005;26:119-24.
41. Sarma JSA, Sarma RJ, Bilitch M, Katz D, Song SL. An exponential formula for heart rate dependence of QT interval during exercise and cardiac pacing in humans: reevaluation of Bazett's formula. Am Heart J. 1984;54:103-8.
42. Spence S, Soper K, Hoe CM, Coleman J. The heart rate corrected QT interval of conscious beagle dogs: a formula based on analysis of covariance. Toxicol Sci. 1998;45(2):247-58.
43. Vitola J, Vukanovic J, Roden DM. Cisapride-induced torsade de pointes. J Cardiovasc Electrophysiol. 1998;9(10):1109-13.
44. Wang Q, Shen J, Splawski I, et al. SCN5A mutations associated with an inherited cardiac arrhythmia, long QT syndrome. Cell. 1995;80:805-11.
45. + ions. J Mol Struct. 2001;562:63-78.
46. Wilson WH, Weiler SJ. Case report of phenothiazine-induced torsade de pointes. Am J Psychiatry. 1984;141(10):1265-6.
47. Wood C, Williams C, Waldron GJ. Patch clamping by numbers. Drug Discov Today. 2004;9(10):434-41.