Lack of appreciable species differences in nonspecific microsomal binding

Journal of Pharmaceutical Sciences

Volumn 99, Issue 8, 2010, Pages 3620-3627

  Zhang, Ying ^a   Yao, Lili ^a   Lin, Jing ^a   Gao, Hua ^a   Wilson, Theresa C ^a   Giragossian, Craig ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

Clearance; Disposition; Enzyme kinetics; Microsomes; Protein binding

Indexed keywords

ASTEMIZOLE; CLOMIPRAMINE; MIDAZOLAM; TAMOXIFEN; DRUG; DYES, REAGENTS, INDICATORS, MARKERS AND BUFFERS; PHOSPHOLIPID; PROTEIN;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; CORRELATION ANALYSIS; EXPERIMENTAL DOG; EXPERIMENTAL MONKEY; HUMAN; HUMAN CELL; LIVER MICROSOME; MOLECULAR WEIGHT; NONHUMAN; PHYSICAL CHEMISTRY; RAT; SENSITIVITY ANALYSIS; SPECIES DIFFERENCE; ALGORITHM; ANIMAL; CHEMISTRY; COMPARATIVE STUDY; DOG; HAPLORHINI; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; IN VITRO STUDY; KINETICS; METABOLISM;

ALGORITHMS; ANIMALS; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DOGS; HAPLORHINI; HUMANS; IN VITRO TECHNIQUES; INDICATORS AND REAGENTS; KINETICS; MICROSOMES, LIVER; PHARMACEUTICAL PREPARATIONS; PHOSPHOLIPIDS; PROTEINS; RATS; SPECIES SPECIFICITY;

EID: 77951277569     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.22124     Document Type: Article

References (37)

1. Ito K, Houston JB. 2005. Prediction of human drug clearance from in vitro and preclinical data using physiologically based and empirical approaches. Pharm Res 22:103-112.
2. Riley RJ, McGinnity DF, Austin RP. 2005. A unified model for predicting human hepatic, metabolic clearance from in vitro intrinsic clearance data in hepatocytes and microsomes. Drug Metab Dispos 33:1304-1311.
3. Margolis JM, Obach RS. 2003. Impact of nonspecific binding to microsomes and phospholipid on the inhibition of cytochrome P4502D6: Implications for relating in vitro inhibition data to in vivo drug interactions. Drug Metab Dispos 31:606-611.
4. Kalvass JC, Tess DA, Giragossian C, Linhares MC, Maurer TS. 2001. Influence of microsomal concentration on apparent intrinsic clearance: Implications for scaling in vitro data. Drug Metab Dispos 29:1332-1336. (Pubitemid 32896583)
5. Austin RP, Barton P, Cockroft SL, Wenlock MC, Riley RJ. 2002. The influence of nonspecific microsomal binding on apparent intrinsic clearance, and its prediction from physicochemical properties. Drug Metab Dispos 30:1497-1503.
6. McLure JA, Miners JO, Birkett DJ. 2000. Nonspecific binding of drugs to human liver microsomes. Br J Clin Pharmacol 49:453-461.
7. Obach RS. 1997. Nonspecific binding to microsomes: Impact on scale-up of in vitro intrinsic clearance to hepatic clearance as assessed through examination of warfarin, imipramine, and propranolol. Drug Metab Dispos 25:1359-1369.
8. Pearce RE, McIntyre CJ, Madan A, Sanzgiri U, Draper AJ, Bullock PL, Cook DC, Burton LA, Latham J, Nevins C, Parkinson A. 1996. Effects of freezing, thawing, and storing human liver microsomes on cytochrome P450 activity. Arch Biochem Biophys 331:145-169.
9. Banker MJ, Clark TH, Williams JA. 2003. Development and validation of a 96-well equilibrium dialysis apparatus for measuring plasma protein binding. J Pharm Sci 92:967-974.
10. Gao H, Yao L, Mathieu HW, Zhang Y, Maurer TS, Troutman MD, Scott DO, Ruggeri RB, Lin J. 2008. In silico modeling of nonspecific binding to human liver microsomes. Drug Metab Dispos 36:2130-2135.
11. Kolarovic L, Fournier NC. 1986. A comparison of extraction methods for the isolation of phospholipids from biological sources. Anal Biochem 156:244-250. (Pubitemid 16044426)
12. Han X, Gross RW. 1995. Structural determination of picomole amounts of phospholipids via electrospray ionization tandem mass spectrometry. J Am Soc Mass Spectrom 6:1202-1210.
13. RamanadhamS, Hsu FF, Bohrer A, Nowatzke W, Ma Z, Turk J. 1998. Electrospray ionization mass spectrometric analyses of phospholipids from rat and human pancreatic islets and subcellular membranes: Comparison to other tissues and implications for membrane fusion in insulin exocytosis. Biochemistry 37:4553-4567.
14. Hsu FF, Turk J. 2000. Characterization of phosphatidylethanolamine as a lithiated adduct by triple quadrupole tandem mass spectrometry with electrospray ionization. J Mass Spectrom 35:595-606.
15. Hsu FF, Turk J. 2003. Electrospray ionization/tandem quadrupole mass spectrometric studies on phosphatidylcholines: The fragmentation processes. J Am Soc Mass Spectrom 14:352-363.
16. Hsu FF, Turk J. 2005. Studies on phosphatidylserine by tandem quadrupole and multiple stage quadrupole ion-trap mass spectrometry with electrospray ionization: Structural characterization and the fragmentation processes. J Am Soc Mass Spectrom 16:1510-1522. (Pubitemid 41169860)
17. Gertz M, Kilford PJ, Houston JB, Galetin A. 2008. Drug lipophilicity and microsomal protein concentration as determinants in the prediction of the fraction unbound in microsomal incubations. Drug Metab Dispos 36:535-542. (Pubitemid 351397979)
18. Hallifax D, Houston JB. 2006. Binding of drugs to hepatic microsomes: Comment and assessment of current prediction methodology with recommendation for improvement. Drug Metab Dispos 34:724-726.
19. Wilkinson GR, Shand DG. 1975. Commentary: A physiological approach to hepatic drug clearance. Clin Pharmacol Ther 18:377-390.
20. Austin RP, Barton P, Mohmed S, Riley RJ. 2005. The binding of drugs to hepatocytes and its relationship to physicochemical properties. Drug Metab Dispos 33:419-425.
21. Sykes MJ, Sorich MJ, Miners JO. 2006. Molecular modeling approaches for the prediction of the nonspecific binding of drugs to hepatic microsomes. J Chem Inf Model 46:2661-2673.
22. Evans GH, Nies AS, Shand DG. 1973. The disposition of propranolol. 3. Decreased half-life and volume of distribution as a result of plasma binding in man, monkey, dog and rat. J Pharmacol Exp Ther 186:114-122.
23. Loscher W. 1978. Serum protein binding and pharmacokinetics of valproate in man, dog, rat and mouse. J Pharmacol Exp Ther 204:255-261. (Pubitemid 8290127)
24. Beaumont KC, Causey AG, Coates PE, Smith DA. 1996. Pharmacokinetics and metabolism of zamifenacin in mouse, rat, dog and man. Xenobiotica 26:459-471.
25. Fichtl B, Nieciecki A, Walter K. 1991. Tissue binding versus plasma binding of drugs: General principles and pharmacokinetic consequences. Adv Drug Res 20:117-166.
26. Lin JH. 1995. Species similarities and differences in pharmacokinetics. Drug Metab Dispos 23:1008-1021.
27. McGinnity DF, Collington J, Austin RP, Riley RJ. 2007. Evaluation of human pharmacokinetics, therapeutic dose and exposure predictions using marketed oral drugs. Curr Drug Metab 8:463-479.
28. Francesco CD, Bickel MH. 1977. Membrane lipids as intracellular binders of chlorpromazine and related drugs. Chem Biol Interact 16:335-346.
29. Weihing RR, Manganiello VC, Chiu R, Phillips AH. 1972. Purification of hepatic microsomal membranes. Biochemistry 11:3128-3135.
30. Ernster L, Siekevitz P, Palade GE. 1962. Enzyme-structure relationship in the endoplasmic reticulum of rat liver. J Cell Biol 15:541-561.
31. Meftah NM, Skett P. 1989. The role of microsomal phospholipids and their fatty acid composition in the control of hepatic metabolism of lignocaine. Br J Pharmacol 98:1399-1405.
32. Waskell L, Koblin D, Canova-Davis E. 1982. The lipid composition of human liver microsomes. Lipids 17:317-320.
33. Dallner G, Ernster L. 1968. Subfractionation and composition of microsomal membranes: A review. J Histochem Cytochem 16:611-632.
34. Miller JE, Cornatzer WE. 1966. Phospholipid metabolism in mitochondria and microsomes of rabbit liver during development. Biochim Biophys Acta 125:534-541.
35. Moore L, Chen T, Knapp HR Jr, Landon EJ. 1975. Energy-dependent calcium sequestration activity in rat liver microsomes. J Biol Chem 250:4562-4568.
36. Goldberg MA, Todoroff T. 1976. Enhancement of diphenylhydantoin binding by lipid extraction. J Pharmacol Exp Ther 196:579-585.
37. Yata N, Toyoda T, Murakami T, Nishiura A, Higashi Y. 1990. Phosphatidylserine as a determinant for the tissue distribution of weakly basic drugs in rats. Pharm Res 7:1019-1025.