The use of preclinical pharmacokinetic and pharmacodynamic data to predict clinical doses: Current and future perspectives

International Congress Series

Volumn 1220, Issue C, 2001, Pages 1-12

  Morgan, Paul ^a  

^a PFIZER INC   (United States)

Author keywords

Clearance; Extrapolation of pharmacokinetics; Free drug theory; Pharmacological potency; Receptor occupancy

Indexed keywords

EID: 84859730935     PISSN: 05315131     EISSN: None     Source Type: Book Series    
DOI: 10.1016/S0531-5131(01)00282-5     Document Type: Article

References (40)

1. DiMasi, J., Success rates for new drugs entering clinical testing in the United States. Clin. Pharm. Ther. 58 (1995), 1–14.
2. Kennedy, T., Managing the drug discovery/development interface. Drug Discovery Today 2 (1997), 436–444.
3. Prentis, R.A., Lis, Y., Walker, S.R., Pharmaceutical innovation by the seven UK-owned pharmaceutical companies (1964–1985). Br. J. Clin. Pharmacol. 25 (1988), 387–396.
4. Smith, D.A., Jones, B.C., Walker, D.K., Design of drugs involving the concepts and theories of drug metabolism and pharmacokinetics. Med. Res. Rev. 16 (1996), 243–266.
5. Lin, J.H., Applications and limitations of interspecies scaling and in vitro extrapolation in pharmacokinetics. Drug Metab. Dispos. 26 (1998), 1202–1212.
6. Wilkinson, G.R., Shand, D.G., A physiological approach to hepatic drug clearance. Clin. Pharmacol. Ther. 18 (1975), 377–390.
7. Yamada, Y., Ito, K., Nakamura, K., Sawada, Y., Iga, T., Prediction of therapeutic doses of beta-adrenergic receptor blocking agents based on quantitative structure—pharmacokinetic/pharmacodynamic relationship. Biol. Pharm. Bull. 16 (1993), 1251–1259.
8. Smith, D.A., Physicochemical properties in drug metabolism and pharmacokinetics. van de Waterbeemd, H., Testa, B., Folkers, G., (eds.) Computer-Assisted Lead Finding and Optimisation, 1997, Verlag, Basel, 267–276.
9. Lin, J., Species similarities and differences in pharmacokinetics. Drug Metab. Dispos. 23 (1995), 1021–1088.
10. Lin, J., Lu, A.Y.H., Role of pharmacokinetics and metabolism in drug discovery and development. Pharmacol. Rev. 49 (1997), 403–449.
11. Boxenbaum, H., Interspecies scaling, allometry, physiological time, and the ground plan of pharmacokinetics. J. Pharmacokinet. Biopharm. 10 (1982), 201–227.
12. Ritschel, W.A., Vachharajani, N.N., Johson, R.D., Hussain, A.S., The allometric approach for interspecies scaling of pharmacokinetic parameters. Comp. Biochem. Physiol. 103 (1992), 249–253.
13. Mahmood, I., Balian, J.D., Interspecies scaling: predicting clearance of drugs in humans. Three different approaches. Xenobiotica 26 (1996), 887–895.
14. Swabb, E.A., Bonner, D.P., Prediction of aztreonam pharmacokinetics in humans based upon data in animals. J. Pharmacokinet. Biopharm. 11 (1983), 215–223.
15. Smith, D.A., Rasmussen, H.S., Stopher, D.A., Walker, D.K., Pharmacokinetics of and metabolism of dofetilide in mouse, rat, dog and man. Xenobiotica 22 (1992), 709–719.
16. Lavé, T., Saner, A., Cassolo, P., Brandt, R., Schmitt-Hoffmann, A.H., Chou, R.C., Animal pharmacokinetics and interspecies scaling from animals to man of lamifiban, a new platelet aggregation inhibitor. J. Pharm. Pharmacol. 48 (1996), 573–577.
17. Jezequel, S., Fluconazole: interspecies scaling and allometric relationships of pharmacokinetic properties. J. Pharm. Pharmacol. 46 (1994), 196–199.
18. Tett, S.E., Moore, S., Ray, J., Pharmacokinetics and bioavailability of fluconazole in two groups of males with human immunodeficiency virus (HIV) infection compared with those in a group of males without HIV infection. Antimicrob. Agents Chemother. 39 (1995), 1835–1841.
19. McLachlan, A.J., Tett, S.E., Pharmacokinetics of fluconazole in people with HIV infection: a population analysis. J. Clin. Pharmacol. 41 (1996), 291–298.
20. Blychert, E., Edgar, B., Elmfeldt, D., Hedner, T., A population study of the pharmacokinetics of felodipine. Br. J. Clin. Pharmacol. 31 (1991), 15–24.
21. Friedman, H., Greenblatt, D.J., Burstein, E.S., Harmatz, J.S., Shader, R.I., Population study of triazolam pharmacokinetics. Br. J. Clin. Pharmacol. 22 (1986), 639–642.
22. Brynne, N., Dalen, P., Alvan, G., Bertilsson, L., Gabrielsson, J., Influence of CYP2D6 polymorphism on the pharmacokinetics and pharmacodynamics of tolterodine. Clin. Pharmacol. Ther. 63 (1998), 529–539.
23. Smith, D.A., Can we design drugs with low variability?. Tucker, G.T., (eds.) Variability in human drug response, Proceedings of the Esteve Foundation Symposium VIII, 1999, Elsevier, Amsterdam, 251–261.
24. Mordenti, J., Man versus beast: pharmacokinetic scaling in mammals. J. Pharm. Sci. 11 (1986), 1028–1040.
25. Boxenbaum, H., DiLea, C., First-time-in-human dose selection: allometric thoughts and perspectives. J. Clin. Pharmacol. 35 (1995), 957–966.
26. Lavé, T., Dupin, S., Schmitt, C., Chou, R.C., Jaeck, D., Coassolo, P., Integration of in vitro data into allometric scaling to predict hepatic metabolic clearance in man: application to 10 extensively metabolised drugs. J. Pharm. Sci. 86 (1997), 584–590.
27. Ward, K.W., Azzarano, L.M., Bondinell, W.E., Cousins, R.D., Huffman, W.F., Jakas, D.R., Keenan, R.M., Preclinical pharmacokinetics and interspecies scaling of a novel vitronectin receptor antagonist. Drug Metab. Dispos. 27 (1999), 1232–1241.
28. Mahmood, I., Balian, J.D., Interspecies scaling: predicting pharmacokinetic parameters of antiepileptic drugs in humans from animals with special emphasis on clearance. J. Pharm. Sci. 85 (1996), 411–414.
29. Gerlowski, L.E., Jain, R.K., Physiologically based pharmacokinetic modeling: principles and applications. J. Pharm. Sci. 72 (1983), 1103–1127.
30. Kawai, R., Lemaire, M., Steimer, J.-L., Bruelisauer, A., Niederberger, W., Rowland, M., Physiologically based pharmacokinetic study on a cyclosporin derivative SDZ IMM 125. J. Pharmacokinet. Biopharm. 22 (1994), 327–365.
31. Houston, J.B., Utility of in vitro drug metabolism data in predicting in vivo metabolic clearance. Biochem. Pharmacol. 47 (1994), 1469–1479.
32. Obach, R.S., Baxter, J.G., Liston, T.E., Silber, B.M., Jones, B.C., MacIntyre, F., Rance, D.J., Wastall, P., The prediction of human pharmacokinetic parameters from preclinical and in vitro metabolism data. J. Pharmacol. Exp. Ther. 283 (1997), 46–58.
33. Ito, K., Iwatsubo, T., Kanamitsu, S., Nakajima, Y., Sugiyama, Y., Quantitative prediction of in vivo drug clearance and drug interactions from in vitro data on metabolism together with binding and transport. Annu. Rev. Pharmacol. Toxicol. 38 (1998), 461–499.
34. Obach, R.S., Prediction of human clearance of twenty-nine drugs from hepatic microsomal intrinsic clearance data: an examination of in vitro half-life approach and non-specific binding to microsomes. Drug Metab. Dispos. 27 (1999), 1350–1359.
35. Lave, T., Dupin, S., Schmitt, C., Valles, B., Ubeaud, G., Chou, R.C., Jaeck, D., Coassolo, P., The use of human hepatocytes to select compounds based on their expected hepatic extraction ratios in humans. Pharm. Res. 14 (1997), 152–155.
36. +-independent multispecific anion transporter mediates active transport of pravastatin into rat liver. Am. J. Physiol. 264 (1993), G36–G44.
37. Yamazaki, M., Suzuki, H., Sugiyama, Y., Recent advances in carrier-mediated uptake and biliary excretion of xenobiotics. Pharm. Res. 13 (1996), 497–513.
38. Yamazaki, M., Akiyama, S., Nishigaki, R., Sugiyama, Y., Uptake is the rate-limiting step in the overall hepatic elimination of pravastatin at steady-state in rats. Pharm. Res. 13 (1996), 1559–1564.
39. Zhao, J.I., Rogers, J.D., Holland, S.D., Larson, P., Amin, R.D., Haesen, R., Freeman, A., Seiberling, M., Merz, M., Cheng, H., Pharmacokinetics and bioavailability of montelukast sodium (MK-0476) in healthy young and elderly volunteers. Biopharm. Drug Dispos. 18 (1997), 769–777.
40. 4receptor antagonist. Can. J. Physiol. Pharmacol. 73 (1995), 191–201.