Allometric issues in drug development.

The concept of correlating pharmacokinetic parameters with body weight from different animal species has become a useful tool in drug development. The allometric approach is based on the power function, where the body weight of the species is plotted against the pharmacokinetic parameter(s) of interest. Clearance, volume of distribution, and elimination half-life are the three most frequently extrapolated pharmacokinetic parameters. Over the years, many approaches have been suggested to improve the prediction of these pharmacokinetic parameters in humans from animal data. A literature review indicates that there are different degrees of success with different methods for different drugs. Overall, though interspecies scaling requires refinement and better understanding, the approach has lot of potential during the drug development process.

[1]  Bischoff Kb,et al.  Some fundamental considerations of the applications of pharmacokinetics to cancer chemotherapy. , 1975 .

[2]  S. Higuchi,et al.  Disposition of the selective alpha1A-adrenoceptor antagonist tamsulosin in humans: comparison with data from interspecies scaling. , 1997, Journal of pharmaceutical sciences.

[3]  I Mahmood,et al.  Interspecies scaling: predicting pharmacokinetic parameters of antiepileptic drugs in humans from animals with special emphasis on clearance. , 1996, Journal of pharmaceutical sciences.

[4]  J B Houston,et al.  Utility of in vitro drug metabolism data in predicting in vivo metabolic clearance. , 1994, Biochemical pharmacology.

[5]  W. Löscher Serum protein binding and pharmacokinetics of valproate in man, dog, rat and mouse. , 1978, The Journal of pharmacology and experimental therapeutics.

[6]  K. Bischoff,et al.  Interspecies correlation of plasma concentration history of methotrexate (NSC-740). , 1970, Cancer chemotherapy reports.

[7]  I. Mahmood Prediction of Clearance, Volume of Distribution and Half‐life by Allometric Scaling and by use of Plasma Concentrations Predicted from Pharmacokinetic Constants: a Comparative Study , 1999, The Journal of pharmacy and pharmacology.

[8]  H Boxenbaum,et al.  Interspecies pharmacokinetic scaling and the evolutionary-comparative paradigm. , 1984, Drug metabolism reviews.

[9]  M. Mayersohn,et al.  Comparative Pharmacokinetics and Interspecies Scaling of Amphotericin B in Several Mammalian Species , 1997, The Journal of pharmacy and pharmacology.

[10]  T. Lavé,et al.  Animal Pharmacokinetics and Interspecies Scaling from Animals to Man of Lamifiban, a New Platelet Aggregation Inhibitor , 1996, The Journal of pharmacy and pharmacology.

[11]  T. Guentert,et al.  Disposition of quinidine in the rabbit. , 1982, Journal of pharmaceutical sciences.

[12]  J. Mordenti,et al.  Man versus beast: pharmacokinetic scaling in mammals. , 1986, Journal of pharmaceutical sciences.

[13]  K. Bachmann Predicting toxicokinetic parameters in humans from toxicokinetic data acquired from three small mammalian species , 1989, Journal of applied toxicology : JAT.

[14]  S. Brody Relativity of physiologic time and physiologic weight. , 1937 .

[15]  I Mahmood,et al.  Interspecies Scaling: Predicting Volumes, Mean Residence Time and Elimination Half‐life. * Some Suggestions , 1998, The Journal of pharmacy and pharmacology.

[16]  D J Rance,et al.  The prediction of human pharmacokinetic parameters from preclinical and in vitro metabolism data. , 1997, The Journal of pharmacology and experimental therapeutics.

[17]  D. Campbell Can Allometric Interspecies Scaling be Used to Predict Human Kinetics? , 1994 .

[18]  J. Balian,et al.  Interspecies scaling: predicting clearance of drugs in humans. Three different approaches. , 1996, Xenobiotica; the fate of foreign compounds in biological systems.

[19]  C. T. Ueda,et al.  Concentration-time effects of quinidine disposition kinetics in rhesus monkeys. , 1977, The Journal of pharmacology and experimental therapeutics.

[20]  M Bonati,et al.  Cyclosporine pharmacokinetics in rats and interspecies comparison in dogs, rabbits, rats, and humans. , 1988, Drug metabolism and disposition: the biological fate of chemicals.

[21]  I. Mahmood Integration of in vitro data and brain weight in allometric scaling to predict clearance in humans: some suggestions. , 1998, Journal of pharmaceutical sciences.

[22]  J. Mordenti,et al.  Pharmacokinetic scale-up: accurate prediction of human pharmacokinetic profiles from animal data. , 1985, Journal of pharmaceutical sciences.

[23]  J. Balian,et al.  Interspecies scaling: a comparative study for the prediction of clearance and volume using two or more than two species. , 1996, Life sciences.

[24]  R C Chou,et al.  Integration of in vitro data into allometric scaling to predict hepatic metabolic clearance in man: application to 10 extensively metabolized drugs. , 1997, Journal of pharmaceutical sciences.

[25]  John F. Young,et al.  Interspecies comparison of in vivo caffeine pharmacokinetics in man, monkey, rabbit, rat, and mouse. , 1984, Drug metabolism reviews.

[26]  R. Yuan,et al.  A comparative study of allometric scaling with plasma concentrations predicted by species‐invariant time methods , 1999, Biopharmaceutics & drug disposition.

[27]  D. Lu,et al.  Interspecies pharmacokinetic scaling of BSH in mice, rats, rabbits, and humans , 1995, Biopharmaceutics & drug disposition.

[28]  H. Boxenbaum,et al.  Interspecies pharmacokinetic scaling and the Dedrick plots. , 1983, The American journal of physiology.

[29]  G. Preston,et al.  First Time in Human for GV196771: Interspecies Scaling Applied on Dose Selection , 1999, Journal of clinical pharmacology.

[30]  K H Antonin,et al.  Pharmacokinetics and plasma binding of diazepam in man, dog, rabbit, guinea pig and rat. , 1976, The Journal of pharmacology and experimental therapeutics.

[31]  I Mahmood,et al.  Interspecies scaling of renally secreted drugs. , 1998, Life sciences.