References
- Clemento A. New and integrated approaches to successful accelerated drug development. Drug Inf J 1999; 33: 699–710
- DiMasi J A. A new look at United States drug development and approval times. Am J Ther 1996; 3: 1–11
- Peck C C. Drug development: improving the process. Food Drug Law J 1997; 52: 163–167, [PUBMED], [INFOTRIEVE]
- Kleinberg M I, Wanke L A. New approaches and technologies in drug design and discovery. Am J Health‐Syst Pharm 1995; 52, pp. 1323–1336, 1341–1343
- Bugg C E, Carson W M, Montgomery J A. Drugs by design. Sci Am 1993; 269: 92–98, [PUBMED], [INFOTRIEVE]
- Zial M R, Beer B. Making business sense of science with rational drug design. Pharm Exec 1990; 10, pp. 40, 42, 44, 46
- DiMasi J A. Risks in new drug development: approval success rates for investigational drugs. Clin Pharmacol Ther 2001; 69: 297–307, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Sheiner L B. The intellectual health of clinical drug evaluation. Clin Pharmacol Ther 1991; 50: 4–9, [PUBMED], [INFOTRIEVE]
- Sheiner L B, Rubin D B. Intention‐to‐treat analysis and the goals of clinical trials. Clin Pharmacol Ther 1995; 57: 6–15, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Colburn W A. Early clinical development moves into the 21st century. Appl Clin Trials (Oct.), 1999; 54–56
- Caldwell G W. The importance of drug metabolism studies for efficient drug discovery and development. Yakubutsu Dotai 1996; 11(1)119–126
- Avdeef A. pH‐Metric solubitliy. 1. Solubility‐pH profiles from Bjerrum plots. Gibbs buffer and pKa in the solid state. Pharm Pharmacol Commun 1998; 4(3)165–178
- Daniel F V, Johnson S R, Cheng H‐Y, Smith B R, Ward K W, Kopple K D. Molecular properties that Influence the oral bioavailability of drug candidates. J Med Chem 2002; 45: 2615–2623, [CROSSREF]
- Veber D F, Marquis R W, Yamashita D S, Ru Y, Oh H J, Ward K, Smith B R. The role of conformational constraint in improved oral bioavailability of cathepsin K inhibitors. Peptides 2000: Proceedings of the Twenty‐Sixth European Peptide Symposium, J Martinex, J A Fehrentz. Editions EDK, Paris 2000; 113–114
- Avdeef A, Box K J, Comer J E, Gilges M, Hadley M, Hibbert C, Patterson W, Tam K Y. pH‐Metric log P 11, pKa determination of water‐insoluble drugs in organic solvent‐water mixtures. J Pharm Biomed Anal 1999; 20(4)631–641, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Takacs‐Novak K, Avdeef A. Interlaboratory study of log P determination by shake‐flask and potentiometric methods. J Pharm Biomed Anal 1996; 14(11)1405–1413, [CROSSREF]
- Avdeef A, Box J K, Comer J E, Hibber C, Tam K Y. pH‐Metric logP 10. Determination of liposomal membrane‐water partition coefficient of ionizable drugs. Pharm Res 1998; 15(2)209–215, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Yang C Y, Cal S J, Liu H, Pidgeon C. Immobolized artificial membranes‐screens for drug‐membrane interactions. Adv Drug Deliv Rev 1997; 23(1–3)229–258, [CROSSREF]
- Ducane A, Neuwels M, Goldstein S, Massingham R. IAM retention and blood brain barrier penetration. Eur J Med Chem 1998; 33: 215–223, [CROSSREF]
- Caldwell G W. Compound optimization in early‐and late‐phase drug discovery: acceptable pharmacokinetic properties utilizing combined physicochemical, in vitro and in vivo screens. Curr Opin Drug Discov Dev 2000; 3(1)30–41
- Anonymous. Guidance for Industry: Safety Pharmacology Studies for Human Pharmaceuticals, ICH. S7A, US FDA. 2001
- Redfern W S, Wakefield I D, Prior H, Pollard C E, Hammond T G, Valentin J‐P. Safety pharmacology—a progressive approach. Fund Clin Pharamcol 2002; 16: 161–173, [CROSSREF]
- Sheiner L B. Learning versus confirming in clinical drug development. Clin Pharmacol Ther 1997; 61: 275–291, [PUBMED], [INFOTRIEVE]
- Evans G O, Davis D T. General introduction and study design and regulatory requiremnets. Animal Clinical Chemistry, G O Evans. Taylor and Francis. 1996; 1–19
- Bandara L R, Kenedy S. Toxicoproteomics—new preclinical tool. Drug Disc Today 2002; 7: 411–418, [CROSSREF]
- Aicher L, Wahl D, Arce A, Grenet O, Steiner S. New insights into cyclosporine A nephrotoxicity by proteome analysis. Electrophoresis 1998; 19: 1998–2003, [PUBMED], [INFOTRIEVE]
- Aardema M J, MacGregor J T. Toxicology and genetic toxicology in the new era of “toxicogenomics”: impact of “‐omics” technologies. Mutat Res 2002; 499: 13–25, [PUBMED], [INFOTRIEVE]
- Corton J C, Anderson S P, Stauber A J, Janszen Db, Kimbell J S, Conolly R B. Entering the era of toxicogenomics with DNA microarrays. CIIT Activities 1999; 19: 1–9
- Nuwaysir E F, Bittner M, Trent J, Barrett J C, Afshari C A. Microarrays and toxicology: the advent of toxicogenomics. Mol Carcinog 1999; 24: 153–159, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Nicholson J K, Lindon J C, Holmes E. ‘Metabonomics’: understanding the metabolic responses of living systems to pathophysiological stimuli via multivariate statistical analysis of biological NMR spectroscopic data. Xenobiotica 1999; 29: 1181–1189, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Johnson D E, Wolfgang G HI. Assessing the potential toxicity of new pharmaceuticals. Curr Top Med Chem 2001; 1: 233–245, [PUBMED], [INFOTRIEVE]
- Derendorf H, Meibohm B. Modeling pharmacokinetic/pharmacodynamic (PK/PD) relationships: concepts and perspectives. Pharm Res 1999; 16: 176–185, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Derendorf H, Lesko L J, Chaikin P, Colburn W A, Lee P, Miller R, Powell R, Rhodes G, Stanski D, Venitz J. Pharmacokinetic/pharmacodynamic modeling in drug research and development. J Clin Pharmacol 2000; 40: 1399–1418, [PUBMED], [INFOTRIEVE]
- Curtis G, Colburn W, Heath G, Lenehan T, Kotschwar T. Faster drug development. Appl Clin Trials 2000; 9: 52–55
- Lee J W, Hulse J D, Colburn W A. Surrogate biochemical markers. Precise measurement for strategic drug and biologics development. J Clin Pharmacol 1995; 35: 362–464
- Colburn W A. Selecting and validating biomarkers for drug development. J Clin Pharmacol 1997; 37: 355–362, [PUBMED], [INFOTRIEVE]
- Rolan P E, Mercer A J, Wootton R, Posner J. Pharmacokinetics and pharmacodynamics of tucaresol, an anticsickling agent, in healthy volunteers. Br J Clin Pharmacol 1995; 39: 375–380, [PUBMED], [INFOTRIEVE]
- Rolan P. The contribution of clinical pharmacology surrogates and models to drug development—a critical appraisal. Br J Clin Pharmacol 1997; 44: 219–225, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Barrett J S, Yu J, Kapil R, Padovani P, Brown F, Ebling W F, Corjay M H, Reilly T M, Bozarth J M, Mousa S A, Pieniaszek H J, Jr. Disposition and exposure of the fibrinogen receptor antagonist XV459 on alphaIIBeta3 binding sites in the guinea pig. Biopharm Drug Dispos 1999; 20: 309–318, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Narjes H, Muller T H, Weisenberger H, Guth B, Brickl R. Inhibition of platelet aggregation as a surrogate marker. J Clin Pharmacol 1997; 37: 59S–64S, [PUBMED], [INFOTRIEVE]
- Van Der Graaf P H, Van Schaick E A, Math‐ot R A, Ijerman A P, Danhof M. Mechanism‐based pharmacokinetic‐pharmacodynamic modeling of the effects of N6‐cyclopentyladenosine analogs on heart rate: estimation of in vivo operational affinity and efficacy in adenosine A1 receptors. J Pharmacol Exp Ther 1997; 283: 809–816, [PUBMED], [INFOTRIEVE]
- Benincosa L J, Chow F S, Tobia L P, Kwok D C, Davis C B, Jusko W J. Pharmacokinetics and pharmacodynamics of a humanized monoclonal antibody of factor IX in cynomolgus monkeys. J Pharmacol Exp Ther 2000; 292: 810–816, [PUBMED], [INFOTRIEVE]
- Ekblom M, Hammarlund‐Udenaes M, Paalzow L. Modeling of tolerance development and rebound effect during different intravenous administrations of morphine of rats. J Pharmacol Exp Ther 1993; 266: 244–252, [PUBMED], [INFOTRIEVE]
- Ouellet D M, Pollack G M. Pharmacodynamics and tolerance development during multiple intravenous bolus morphine administration in rats. J Pharmacol Exp Ther 1997; 281: 713–720, [PUBMED], [INFOTRIEVE]
- Cox Eh, Kerbusch T, Van der Graaf P H, Danhof M. Pharmacokinetic‐pharmacodynamic modeling of the electroencephalogram effect of synthetic opoids in the rat. Correlation with the interaction at mu‐opoid receptor. J Pharmacol Exp Ther 1998; 284: 1095–1103, [PUBMED], [INFOTRIEVE]
- Cox E H, Langemeijer M W, Gubbens‐Stibbe J M, Muir K T, Danhof M. The comparative pharmacodynamics of ramifentanil and its metabolite, GR90291, in a rat electroencephalographic model. Anesthesiology 1999; 90: 535–544, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Danhof M, Mandema J W. Modeling of the pharmacodynamics and pharmacodynamic interactions of CNS active drugs. Int J Clin Pharmacol Ther Toxicol 1992; 30: 516–519, [PUBMED], [INFOTRIEVE]
- Bauer J A, Balthasar J P, Fung H L. Application of pharmacodynamic modeling for designing time‐variant dosing regimens to overcome nitroglycerin tolerance in experimental heart failure. Pharm Res 1997; 14: 1140–1145, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Sun Y N, Lee H J, Almon R R, Jusko W J. A pharmacokinetic/pharmacodynamic model for recombinant growth hormone effects on induction of insulin‐like growth factor I in monkeys. J Pharmacol Exp Ther 1999; 289: 1523–1532, [PUBMED], [INFOTRIEVE]
- Biomarkers Definitions Working Group. Biomarkers and surrogate endpoints: preferred definitions and conceptual framework. Clin Pharmacol Ther 2001; 69: 89–95, [CROSSREF]
- Blumer D D, Strong J M, Atkinson A J, Jr. The convulsant potency of lidocaine and its N‐dealkylated metabolites. J Pharmacol Exp Ther 1973; 186: 31–36, [PUBMED], [INFOTRIEVE]
- Breimer D D, Danhof M. Relevance of the application of pharmacokinetic‐pharmacodynamic modeling concepts in drug development. The ‘Wooden Shoe’ paradigm. Clin Pharmacokinet 1997; 32: 259–267, [PUBMED], [INFOTRIEVE]
- Smith L J, Glass M, Minkwitz M C. Inhibition of leukotrine D4‐induced bronchoconstriction in subjects with asthma: a concentration‐effect study of ICI 204,219. Clin Pharmacol Ther 1993; 54: 430–436, [PUBMED], [INFOTRIEVE]
- Mildvan D, Landay A, De Gruttola V, Machado S G, Kagan J. An approach to the validation of markers for use in AIDS clinical trials. Clin Inf Dis 1997; 24: 764–774
- Rolan P E, Parker J E, Gray S J, Weatherley B C, Ingram J, Ette E I, Garg V, Jayaraj A. The pharmacokinetics, tolerability and pharmacodynamics of tucaresol (589C80 4[2‐formyl‐3‐hydroxyphenoxymethyl] benzoic acid, a potential anti‐sickling agent, following oral administration to healthy subjects. Br J Clin Pharmacol 1993; 35: 419–425, [PUBMED], [INFOTRIEVE]
- Arya R, Rolan P E, Wootton R, Posner J, Bellingham A. Tucaresol increases oxygen affinity and reduces haemolysis in subjects with sickle cell anaemia. Br J Haematol 1996; 93: 817–821, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Liberman R, McMichael J. Role of pharmacokinetic‐pharmcodynamic principles in rational and cost‐effective drug development. Ther Drug Monit 1996; 18: 423–428, [CROSSREF]
- Mahmood I, Balian J D. Role of pharmacokinetic principles behind scaling from preclinical results to phase I protocols. Clin Pharmacokinet 1999; 36: 1–11, [PUBMED], [INFOTRIEVE]
- Cosson V F, Fuseau E, Ethymiopoulos C, Bye A. Mixed effect modeling of sumatriptan pharmacokinetics during drug development. I: interspecies allometric scaling. J Pharmacokinet Biopharm 1997; 25: 149–167, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Geomeni R, Falcoz C, D'Angeli C, Bye A. In‐silico prediction of drug properties in man using preclinical data and computer assisted drug development. Drug Inf J 2001; 35: 1047–1063
- Geomeni R, Bani M, D'Angeli C, Corsi M, Bye A. Computer assisted drug development (CADD): an emerging technology for designing first time‐in‐man and proof‐of‐concept studies from preclinical experiments. Eur J Pharm Sci 2001; 13: 261–270, [CROSSREF]
- Williams P J, Godfrey C J, Roy A, Chu H‐M, Ette E I. Pharmacokinetic/pharmacodynamic knowledge discovery during drug development. Pharmacokinetics in Drug Development: Regulatory and Development Paradigms, P Bonate, D Howard. AAPS Press, Arlington 2004; 163–202
- Schaefer H G, Heinig R, Ahr G, Adelmann H, Tetzloff W, Kulmann J. Pharmacokinetic‐pharmacodynamic modeling as a tool to evaluate the clinical relevance of a drug‐food interaction for nisoldipine controlled‐release dosage form. Eur J Clin Pharmacol 1997; 51: 473–480, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Guidance for Industry: Food‐Effect and Fed Bioequivalence Studies, http://www.fda.gov/cder/guidance/5194fnl.pdf. Accessed on March 17, 2004
- Parker C J, Hunter J M, Snowdon S L. Effect of age, gender and anesthetic technique on the pharmacodynamics of atracurium. Br J Anaesth 1993; 70: 38–41, [PUBMED], [INFOTRIEVE]
- Marino M T, Schuster B G, Brueckner RP, Lin E, Kaminskis A, Lasseter K C. Population pharmacokinetics and pharmacodynamics of pyridostigmine bromide for prophylaxis against nerve agents in humans. J Clin Pharmacol 1998; 38: 227–235, [PUBMED], [INFOTRIEVE]
- Belani C P, Kearns C M, Zuhowski E G, Erkmen K, Hiponia D, Zacharski D, Engstrom C, Ramathan R K, Capozzoli M J, Aisner J, Egorin M J. Phase I trial, ncluding pharmacokinetic and pharmacodynamic correlation, of combination paclitaxel and carboplatin in patients with metastatic non‐small‐cell lung cancer. J Clin Oncol 1999; 17: 676–684, [PUBMED], [INFOTRIEVE]
- FDA Guidance for Industry: Drug metabolism/Drug Interaction Studies in the Drug Development Process: Studies In Vitro, http://www.fda.gov/cder/guidance/clin3.pdf. Accessed on March 17, 2004.
- FDA Guidance for Industry: In Vivo Drug Metabolism/Drug Interaction Studies Study Design, Data Analysis, and Recommendations for Dosing and Labeling, http://www.fda.gov/cder/guidance/2635fnl.pdf. Accessed on March 17, 2004.
- Anderson B J, Holford N H, Woollard G A, Knagasundaram S, Mahadevan M. Perioperative pharmacodynamics of acetaminophen analgesia in children. Anesthesiology 1999; 90: 411–421, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Marshall J D, Wells T G, Letzig L, Kearns Gl. Pharmacokinetics and pharmacodynamics of bumetanide in critically ill pediatric patients. J Clin Pharmacol 1998; 38: 994–1002, [PUBMED], [INFOTRIEVE]
- Pihoker C, Kearns G L, French D, Bowers C Y. Pharmacokinetics and pharmacodnamics of growth hormone‐releasing peptide‐2: a phase I study in children. J Clin Endocrinol Metab 1998; 83: 1168–1172, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Sorooshian S S, Stafford M A, Eastwood N B, Boyd A H, Hull C J, Wright P M. Pharmacokinetics and pharmacodynamics of cisatracurium in young and elderly adult patients. Anesthesiology 1996; 84: 1083–1091, [PUBMED], [INFOTRIEVE], [CROSSREF]
- FDA Guidance for Industry: General Considerations for Pediatric Pharmacokinetic Studies for Drugs and Biological Products, http://www.fda.gov/cder/guidance/1970dft.pdf. Accessed on March 17, 2004.
- FDA Guideline for Industry‐Studies in Support of Special Populations: Geriatrics, http://www.fda.gov/cder/guidance/iche7.pdf. Accessed on March 17, 2004.
- FDA Guidance for Industry: Pharmacokinetics in Patients with Impaired Hepatic Function—Study Design, Data Analysis, and Impact on Dosing and Labeling, http://www.fda.gov/cder/guidance/3625fnl.pdf. Accessed on March 17, 2004.
- FDA Guidance for Industry: Pharmacokinetics in Patients with Impaired Renal Function—Study Design, Data Analysis, and Impact on Dosing and Labeling, http://www.fda.gov/cder/guidance/1449fnl.pdf. Accessed on March 17, 2004
- Ette E I, Lockwood P, Miller R, Mandema J W. Analysis of analgesic trials. Applied Statistics in the Pharmaceutical Industry Using S‐Plus, S Millard, A Krause. Springer‐Verlag, New York 2001; 237–266
- Lesko L J, Rowland M, Peck C C, Blaschke T F. Optimizing the science of drug development: opportunities for better candidate selection and accelerated evaluation in humans. Pharm Res 2000; 17: 1335–1344, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Mol M JTM, Erkelens D W, Gevers Leuven J A, Schouten J A, Stalenhoef A FH. Effects of synvinolin (MK‐733) on plasma lipids in familial hypercholesterolaemia. Lancet 1986; 2: 936–939, [PUBMED], [INFOTRIEVE], [CROSSREF]
- Scand. Simvastatin Surv. Study Group. Randomised trial of cholesterol lowering in 4444 patients with coronary heart disease: the Scandinavian Simvastatin Survival Study (4S). Lancet 1994; 344: 1383–1389
- US Gov. Print Off. Code of Federal Regulations. Title 21, US Gov. Print. Office, Washington, DC 1997; Vol. 5, Part 320, Subpart B