Prediction of pharmacokinetic properties using experimental approaches during early drug discovery

Current Opinion in Chemical Biology

Volumn 5, Issue 4, 2001, Pages 452-463

  Chaturvedi, Pravin R ^a   Decker, Caroline J ^a   Odinecs, Aleksandrs ^a  

^a VERTEX PHARMACEUTICALS   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CAFFEINE; ENALAPRIL; GLUCOSE; METOPROLOL; TERBUTALINE; TESTOSTERONE;

DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG METABOLISM; DRUG PENETRATION; DRUG SCREENING; DRUG STABILITY; IN VITRO STUDY; INTESTINE MUCOSA PERMEABILITY; METHODOLOGY; NONHUMAN; PHYSICAL CHEMISTRY; REVIEW; SCIENTIFIC LITERATURE;

EID: 0035416240     PISSN: 13675931     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1367-5931(00)00228-3     Document Type: Review

References (71)

1. Ex vivo approaches to predicting oral phamacokinetics in humans
2. Prediction of hepatic metabolic clearance based on interspecies allometric scaling techniques and in vitro-in vivo correlations
3. Rational high throughput screening in preclinical drug metabolism
4. Pharmacokinetics and metabolism in early drug discovery
5. Intestinal permeability: Prediction from theory
6. The prediction of human pharmacokinetic parameters from preclinical and in vitro metabolism data
7. Applications and limitations of interspecies scaling and in vitro extrapolation in pharmacokinetics
8. Interspecies correlation of plasma concentration history of methotrexate (NSC 740)
9. Man vs. beast: Pharmacokinetic scaling in mammals
10. Interspecies scaling: Predicting pharmacokinetic parameters of antiepileptic drugs in humans from animals with special emphasis on clearance
11. Allometry as a tool for extrapolation of biological variables
12. Design principles for orally bioavailable drugs
13. Applications of the Caco-2 model in the design and development of orally active drugs: Elucidation of biochemical and physical barriers posed by the intestinal epithelium
14. Can we learn to distinguish between 'drug-like' and 'nondrug-like' molecules?
15. A saturable transport mechanism in the intestinal absorption of gabapentin is the underlying cause of the lack of proportionality between increasing dose and drug levels in plasma
16. Estimating human oral fraction dose absorbed: A correlation using rat intestinal membrane permeability for passive and carrier-mediated compounds
17. Comparison of intestinal permeabilities determined in multiple in vitro and in situ models: Relationship to absorption in humans
18. Sequential organ first pas effects: Simple methods for constructing compartmental pharmacokinetic models from physiological models of drug disposition by several organs
19. Utility of in vitro drug metabolism data in predicting in vivo metabolic clearance
20. Apparent volumes of distribution and drug binding to plasma proteins and tissues
21. Selection of development candidates based on in vitro permeability measurements
22. A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability
23. Drug-like properties and the causes of poor solubility and poor permeability
24. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
25. Estimation of Caco-2 permeability using calculated molecular descriptions
26. Prediction of membrane permeability to peptides from calculated dynamic molecular surface properties
27. Polar molecular surface properties predict the intestinal absorption of drugs in humans
28. Experimental and computational screening models for the prediction of intestinal drug absorption
29. The fundamental variable of the biopharmaceutics classification system (BCS) - A commentary
30. Absorption potential: Estimating the fraction absorbed for orally administered compounds
31. Influence of physicochemical properties on dissolution of drugs in the gastrointestinal tract
32. In vitro-in vivo correlations for lipophilic, poorly water-soluble drugs
33. Solubility as a limiting factor to drug absorption
34. Use of everted intestinal rings for in vitro examination of oral absorption potential
35. A correlation between the permeability characteristics of a series of peptides using an in vitro cell culture model (Caco-2) and those using an in situ perfused rat ileum model of the intestinal mucosa
36. Cultured intestinal epithelial cell models
37. Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells
38. In vitro permeability across Caco-2 cells (colonic) can predict in vivo (small intestinal) absorption in man - Fact or myth
39. Pharmacokinetic parameters of terbutaline in healthy man. An overview
40. Pharmacokinetics of the enantiomers of terbutaline after repeated oral dosing with racemic terbutaline
41. Pharmacokinetic evaluation in man of terbutaline given as separate enantiomers and as the racemate
42. Gastrointestinal absorption of drugs: Methods and studies
43. The Madin-Darby canine kidney (MDCK) epithelial monolayer as a model cellular transport barrier
44. Transepithelial transport of aliphatic carboxylic acids studied in Madin-Darby canine kidney (MDCK) cell monolayers
45. MDCK (Madin-Darby Canine Kidney) cells: A tool for membrane permeability screening
46. Cell cultures as tools in biopharmacy
47. Analysis of drug transport and metabolism in cell monolayer systems that have been modified by cytochrome P4503A4 cDNA-expression
48. Influence of D-glucose-induced water absorption on rat jejunal uptake of two passively absorbed drugs
49. Carrier-mediated transport of amino acids, small peptides and their drug analogs
50. Comparison between permeability coefficients in rat and human jejunum
51. IAM chromatography: An in vitro screen for predicting drug membrane permeability
52. Physiocochemical high throughput screening: Parallel artificial membrane permeation assay in the description of passive absorption processes
53. High throughput screening in drug metabolism and pharmacokinetic support of drug discovery
54. Animal scale-up
55. Interspecies scaling, allometry, physiological time and the ground plan of pharmacokinetics
56. Prediction of the disposition of B-lactam antibiotics in human from pharmacokinetic parameters in animals
57. Species similarities and differences in pharmacokinetics
58. Quantitative prediction of in vivo drug clearance and drug interactions from in vitro data on metabolism together with binding and transport
59. Prediction of hepatic extraction ratio from in vitro measurement of intrinsic clearance
60. The use of heterologously expressed drug metabolizing enzymes - State of the art and prospects for the future
61. Biliary excretion in primary rat hepatocytes cultured in a collagen-sandwich configuration
62. Scaling factors to relate drug metabolic clearance in hepatic microsomes, isolated hepatocytes and the intact liver: Studies with induced livers involving diazepam
63. Correlation between in vitro microsomal enzyme activity and whole organ hepatic elimination kinetics: Analysis with a dispersion model
64. A convenient in vitro screening method for predicting in vivo drug metabolic clearance using isolated hepatocytes suspended in serum
65. Disposition of enalapril in the perfused rat intestine-live preparation: Absorption, metabolism and first-pass effect
66. Absorption and metabolism of acetaminophen by the in situ perfused rat small intestine preparation
67. Tissue binding versus plasma binding of drugs: General principles and pharmacokinetic consequence
68. Comparative pharmacokinetics of benzodiazepines in dog and man
69. Comparison between active and passive drug transport in human intestinal epithelial Caco-2 cells in vitro and human jejunum in vivo
70. Prediction of invivo drug disposition from in vitro data based on physiological pharmacokinetics