Foundation review: Progressing preclinical drug candidates: Strategies on preclinical safety studies and the quest for adequate exposure

Drug Discovery Today

Volumn 17, Issue 15-16, 2012, Pages 828-836

  Higgins, John ^a   Cartwright, Mark E ^a   Templeton, Allen C ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALKYLATING AGENT; CELLULOSE; EXCIPIENT; NUCLEOSIDE ANALOG; QUINOLONE DERIVATIVE;

CARDIOTOXICITY; CLINICAL TRIAL (TOPIC); DRUG ABSORPTION; DRUG DELIVERY SYSTEM; DRUG DEVELOPMENT; DRUG FORMULATION; DRUG SAFETY; DRUG TOXICITY; GENETIC TOXICOLOGY; GOOD LABORATORY PRACTICE; HEART VENTRICLE TACHYCARDIA; HUMAN; IC 50; MAXIMUM TOLERATED DOSE; MUSTARD; MUTAGENICITY; NEUROTOXICITY; NONHUMAN; PHARMACEUTICS; PHASE 1 CLINICAL TRIAL; PHASE 1 CLINICAL TRIAL (TOPIC); REVIEW; RISK ASSESSMENT; ANIMAL; DRUG SCREENING;

ANIMALS; DRUG EVALUATION, PRECLINICAL; DRUG TOXICITY; HUMANS;

EID: 84864626280     PISSN: 13596446     EISSN: 18785832     Source Type: Journal    
DOI: 10.1016/j.drudis.2012.03.016     Document Type: Review

References (38)

1. M. MacCoss, and T.A. Baillie Organic chemistry in drug discovery Science 303 2004 1810 1813 (Pubitemid 38374865)
2. A.S. Bass Exploratory drug safety: a discovery strategy to reduce attrition in development J. Phamacol. Toxicol. Methods 60 2009 69 78
3. A. Bass Origins, practices and future of safety pharmacology J. Pharmacol. Toxicol. Methods 49 2004 145 151 (Pubitemid 38686652)
4. S. Lindgren Benchmarking safety pharmacology regulatory packages and best practice J. Pharmacol. Toxicol. Methods 58 2008 99 109
5. A.S. Bass International life sciences institute (health and environmental sciences institute, HESI) initiative on moving towards better predictors of drug-induced torsades de pointes Br. J. Pharmacol. 154 2008 1491 1501
6. R.A. Boyd, and R.L. Lalonde Nontraditional approaches to first-in-human studies to increase efficiency of drug development, will microdose studies make a significant impact? Clin. Pharmacol. Ther. 81 2007 24 26 (Pubitemid 46050861)
7. G.A. Gintant Preclinical Torsades-de-Pointes screens: advantages and limitations of surrogate and direct approaches in evaluating proarrhythmic risk Pharmacol. Ther. 119 2008 199 209
8. R.L. Hamlin Animal models of ventricular arrhythmias Pharmacol. Ther. 113 2007 276 295 (Pubitemid 46151721)
9. R.S. Wymore Tissue and species distribution of mRNA for the Ikr-like K Channel, erg Circ. Res. 80 1997 261 268 (Pubitemid 27056989)
10. W.S. Redfern Relationship between preclinical cardiac electrophysiology, clinical QT interval prolongation and torsades de pointes for a broad range of drugs: evidence for a provisional safety margin in drug development Cardiovasc. Res. 58 2003 32 45 (Pubitemid 36351620)
11. S. Irwin Comprehensive observational assessment: Ia. A systematic, quantitative procedure for assessing the behavioral and physiologic state of the mouse Psychopharmacologia 13 1968 222 257
12. J.L. Mattson A performance standard for clinical and functional observational battery examination of rats J. Am. Coll. Toxicol. 15 1996 239 250
13. L.B. Kinter Safety pharmacology of the renal and gastro-intestinal systems P.D. Williams, A.S. Bass, Safety Pharmacology: A Practical Guide 2003 TherImmune Research Gaithersburg, MD 99 116
14. M.S. Diehl Comparison of the results of a modified miniscreen and the standard bacterial reverse mutation assays Environ. Mol. Mutagen 36 2000 72 77 (Pubitemid 30620746)
15. M.H. Chen Mechanisms of cardiac dysfunction associated with tyrosine kinase inhibitor cancer therapeutics Circulation 118 2008 84 95
16. N.Z. Lu International Union of Pharmacology. LXV. The pharmacology and classification of the nuclear receptor superfamily: glucocorticoid, mineralocorticoid, progesterone, and androgen receptors Pharmacol. Rev. 58 2006 782 797 (Pubitemid 44833746)
17. S.M. Foord International Union of Pharmacology. XLVI. G protein-coupled receptor list Pharmacol. Rev. 57 2011 279 288
18. D.E. Clapham International Union of Pharmacology. XLIII. Compendium of voltage-gated ion channels: transient receptor potential channels Pharmacol. Rev. 55 2003 591 596 (Pubitemid 37500520)
19. F. Hofmann International Union of Pharmacology. XLII. Compendium of voltage-gated ion channels: cyclic nucleotide-modulated channels Pharmacol. Rev. 55 2003 587 589 (Pubitemid 37500519)
20. M.R. Fielden, and K.L. Kolaja The role of early in vivo toxicity testing in drug discovery toxicology Expert Opin. Drug Saf. 7 2008 107 110 (Pubitemid 351447694)
21. B.D. Car, and R.T. Robertson Commentary: discovery toxicology - a nascent science Toxicol. Pathol. 27 1999 481 483 (Pubitemid 29357633)
22. I. Kola, and D. Hazuda Innovation and greater probability of success in drug discovery and development - from target to biomarkers Curr. Opin. Biotechnol. 16 2005 644 646 (Pubitemid 41654643)
23. M. Palucki Strategies at the interface of drug discovery and development: early optimization of the solid state: phase and preclinical toxicology formulation for potential drug candidates J. Med. Chem. 53 2010 5897 5905
24. ICH Topic M3 (R2) (2009) Non-Clinical Safety Studies for the Conduct of Human Clinical Trials and Marketing Authorization of Pharmaceuticals
25. M3 R2 Implementation Working Group on the M# R2 Guideline (2011) Guidance on Non-clinical Safety Studies for the Conduct of Human Clinical Trials and Marketing Authorizationfor Pharmaceuticals; Questions and Answers
26. H. Rosen, and T. Abrigat The rise and rise of drug delivery Nat. Rev. Drug Discov. 4 2005 381 385 (Pubitemid 40704121)
27. M.V. Chaubal Application of formulation technologies in lead candidate selection and optimization Drug Discov. Today 9 2004 603 609 (Pubitemid 38900510)
28. J. Mass An Integrated early formulation strategy - from Hit evaluation to preclinical candidate profiling Eur. J. Pharm. Biopham. 66 2007 1 10
29. W. Curatolo Physical chemical properties of oral drug candidates in the discovery and exploratory development settings Pharm. Sci. Technol. Today 1 1998 387 393 (Pubitemid 28559133)
30. D. Sun In vitro testing of drug absorption for drug 'developability' assessment: forming an interface between in vitro preclinical data and clinical outcomes Curr. Opin. Drug Discov. Dev. 7 2004 75 85 (Pubitemid 44111916)
31. E. Merisko-Liversidge Nanosizing: a formulation approach for poorly-water-soluble compounds Eur. J. Pharm. Sci. 18 2003 113 120 (Pubitemid 36184748)
32. C.J. Porter Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs Nat. Rev. Drug Discov. 6 2007 231 248 (Pubitemid 46344627)
33. T.R. Kommuru Self-emulsifying drug delivery systems (SEDDS) of coenzyme Q10: formulation development and bioavailability assessment Int. J. Pharm. 212 2001 233 246 (Pubitemid 32119449)
34. J. Dressman, and C. Reppas In vitro-in vivo correlations for lipophilic, poorly water soluble drugs Eur. J. Pharm. Sci. 11 2000 S73 S80
35. B. Hancock, and G. Zografi Characteristics and significance of the amorphous state in pharmaceutical systems J. Pharm. Sci. 86 1997 1 12
36. S. Neervannan Preclinical formulations for discovery and toxicology: physicochemical challenges Expert Opin. Drug Metab. Toxicol. 2 2006 715 731 (Pubitemid 46118317)
37. S.C. Gad Nonclinical vehicle use in studies by multiple routes in multiple species Int. J. Toxicol. 25 2006 449 521
38. H. Stahl, and C. Wermuth Handbook of Pharmaceutical Salts 2002 Wiley