Towards a platform PBPK model to characterize the plasma and tissue disposition of monoclonal antibodies in preclinical species and human

Journal of Pharmacokinetics and Pharmacodynamics

Volumn 39, Issue 1, 2012, Pages 67-86

  Shah, Dhaval K ^a   Betts, Alison M ^a  

^a PFIZER INC   (United States)

Author keywords

FcRn; Interspecies scaling; Monoclonal antibody; Physiologically based pharmacokinetic; Tissue disposition

Indexed keywords

FC RECEPTOR; MONOCLONAL ANTIBODY;

ALGORITHM; ANIMAL TISSUE; ANTIBODY BLOOD LEVEL; ANTIGEN SPECIFICITY; ARTICLE; BLOOD ANALYSIS; CELL COMPARTMENTALIZATION; CONTROLLED STUDY; EVALUATION RESEARCH; HAPLORHINI; HUMAN; HUMAN TISSUE; HUMAN VERSUS ANIMAL COMPARISON; MALE; MATHEMATICAL COMPUTING; MATHEMATICAL MODEL; MOLECULAR INTERACTION; MOUSE; NONHUMAN; PINOCYTOSIS; POROSITY; PREDICTION; PRIORITY JOURNAL; PROCESS DEVELOPMENT; RAT; SYSTEMIC CIRCULATION; TISSUE BLOOD FLOW; TISSUE DISTRIBUTION; WILD TYPE;

ALGORITHMS; ANIMAL STRUCTURES; ANIMALS; ANTIBODIES, MONOCLONAL; ANTIBODIES, MONOCLONAL, HUMANIZED; ANTIGENS, NEOPLASM; AREA UNDER CURVE; BLOOD; DRUG EVALUATION, PRECLINICAL; ENDOSOMES; EXTRACELLULAR SPACE; HAPLORHINI; HISTOCOMPATIBILITY ANTIGENS CLASS I; HUMANS; IMMUNOGLOBULINS, INTRAVENOUS; LYMPH; MALE; MICE; MICE, KNOCKOUT; MODELS, BIOLOGICAL; NEOPLASMS; PINOCYTOSIS; RATS; RECEPTORS, FC; TISSUE DISTRIBUTION; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84861480783     PISSN: 1567567X     EISSN: 15738744     Source Type: Journal    
DOI: 10.1007/s10928-011-9232-2     Document Type: Article

References (70)

1. Levy G (1966) Kinetics of pharmacologic effects. Clin Pharmacol Ther 7:362-372
2. Lobo ED, Hansen RJ, Balthasar JP (2004) Antibody pharmacokinetics and pharmacodynamics. J Pharm Sci 93:2645-2668 (Pubitemid 39506617)
3. Wang W, Wang EQ, Balthasar JP (2008) Monoclonal antibody pharmacokinetics and pharmacodynamics. Clin Pharmacol Ther 84:548-558
4. Mould DR, Sweeney KR (2007) The pharmacokinetics and pharmacodynamics of monoclonal antibodies-mechanistic modeling applied to drug development. Curr Opin Drug Discov Devel 10:84-96 (Pubitemid 46438261)
5. Mager DE, Jusko WJ (2001) General pharmacokinetic model for drugs exhibiting target-mediated drug disposition. J Pharmacokinet Pharmacodyn 28:507-532 (Pubitemid 34289541)
6. Mahmood I (2009) Pharmacokinetic allometric scaling of antibodies: application to the first-in-human dose estimation. J Pharm Sci 98:3850-3861
7. Dong JQ, Salinger DH, Endres CJ, Gibbs JP, Hsu CP, Stouch BJ, Hurh E, Gibbs MA (2011) Quantitative prediction of human pharmacokinetics for monoclonal antibodies: retrospective analysis of monkey as a single species for first-in-human prediction. Clin Pharmacokinet 50:131-142
8. De Buck SS, Sinha VK, Fenu LA, Nijsen MJ, Mackie CE, Gilissen RA (2007) Prediction of human pharmacokinetics using physiologically based modeling: a retrospective analysis of 26 clinically tested drugs. Drug Metab Dispos 35:1766-1780 (Pubitemid 47481568)
9. Grime KH, Bird J, Ferguson D, Riley RJ (2009) Mechanismbased inhibition of cytochrome P450 enzymes: an evaluation of early decision making in vitro approaches and drug-drug interaction prediction methods. Eur J Pharm Sci 36:175-191
10. Thygesen P, Macheras P, Van Peer A (2009) Physiologicallybased PK/PD modelling of therapeutic macromolecules. Pharm Res 26:2543-2550
11. Dedrick RL (1973) Animal scale-up. J Pharmacokinet Biopharm 1:435-461
12. Bischoff KB, Dedrick RL, Zaharko DS, Longstreth JA (1971) Methotrexate pharmacokinetics. J Pharm Sci 60:1128-1133
13. Baxter LT, Zhu H, Mackensen DG, Jain RK (1994) Physiologically based pharmacokinetic model for specific and nonspecific monoclonal antibodies and fragments in normal tissues and human tumor xenografts in nude mice. Cancer Res 54:1517-1528 (Pubitemid 24106416)
14. Baxter LT, Zhu H, Mackensen DG, Butler WF, Jain RK (1995) Biodistribution of monoclonal antibodies: scale-up from mouse to human using a physiologically based pharmacokinetic model. Cancer Res 55:4611-4622
15. Garg A, Balthasar JP (2007) Physiologically-based pharmacokinetic (PBPK) model to predict IgG tissue kinetics in wild-type and FcRn-knockout mice. J Pharmacokinet Pharmacodyn 34:687-709 (Pubitemid 47477039)
16. Urva SR, Yang VC, Balthasar JP (2010) Physiologically based pharmacokinetic model for T84.66: a monoclonal anti-CEA antibody. J Pharm Sci 99:1582-1600
17. Covell DG, Barbet J, Holton OD, Black CD, Parker RJ, Weinstein JN (1986) Pharmacokinetics of monoclonal immunoglobulin G1, F(ab')2, and Fab' in mice. Cancer Res 46:3969-3978 (Pubitemid 16075893)
18. Ferl GZ, Wu AM, DiStefano JJ 3rd (2005) A predictive model of therapeutic monoclonal antibody dynamics and regulation by the neonatal Fc receptor (FcRn). Ann Biomed Eng 33:1640-1652 (Pubitemid 41801648)
19. Davda JP, Jain M, Batra SK, Gwilt PR, Robinson DH (2008) A physiologically based pharmacokinetic (PBPK) model to characterize and predict the disposition of monoclonal antibody CC49 and its single chain Fv constructs. Int Immunopharmacol 8:401-413 (Pubitemid 351221431)
20. Garg A (2007). Investigation of the role of FcRn in the absorption, distribution, and elimination ofmonoclonal antibodies,Chap. 3.PhD Thesis, Department of Pharmaceutical Sciences. 71-111
21. Williams LE, Wu AM, Yazaki PJ, Liu A, Raubitschek AA, Shively JE, Wong JY (2001) Numerical selection of optimal tumor imaging agents with application to engineered antibodies. Cancer Biother Radiopharm 16:25-35 (Pubitemid 32231714)
22. Bazin-Redureau MI, Renard CB, Scherrmann JM (1997) Pharmacokinetics of heterologous and homologous immunoglobulin G, F(ab')2 and Fab after intravenous administration in the rat. J Pharm Pharmacol 49:277-281 (Pubitemid 27197013)
23. Hinton PR, Johlfs MG, Xiong JM, Hanestad K, Ong KC, Bullock C, Keller S, Tang MT, Tso JY, Vasquez M, Tsurushita N (2004) Engineered human IgG antibodies with longer serum half-lives in primates. J Biol Chem 279:6213-6216 (Pubitemid 38248752)
24. Weisman MH, Moreland LW, Furst DE, Weinblatt ME, Keystone EC, Paulus HE, Teoh LS, Velagapudi RB, Noertersheuser PA, Granneman GR, Fischkoff SA, Chartash EK (2003) Efficacy, pharmacokinetic, and safety assessment of adalimumab, a fully human anti-tumor necrosis factor-alpha monoclonal antibody, in adults with rheumatoid arthritis receiving concomitant methotrexate: a pilot study. Clin Ther 25:1700-1721 (Pubitemid 36801943)
25. Brown RP, Delp MD, Lindstedt SL, Rhomberg LR, Beliles RP (1997) Physiological parameter values for physiologically based pharmacokinetic models. Toxicol Ind Health 13:407-484 (Pubitemid 27314117)
26. Davies B, Morris T (1993) Physiological parameters in laboratory animals and humans. Pharm Res 10:1093-1095 (Pubitemid 23211439)
27. Swartz MA (2001) The physiology of the lymphatic system. Adv Drug Deliv Rev 50:3-20 (Pubitemid 32727274)
28. Sarin H (2010) Physiologic upper limits of pore size of different blood capillary types and another perspective on the dual pore theory of microvascular permeability. J Angiogenes Res 2:14
29. Vaughn DE, Bjorkman PJ (1997) High-affinity binding of the neonatal Fc receptor to its IgG ligand requires receptor immobilization. Biochemistry 36:9374-9380 (Pubitemid 27346975)
30. Hinton PR, Xiong JM, Johlfs MG, Tang MT, Keller S, Tsurushita N (2006) An engineered human IgG1 antibody with longer serum half-life. J Immunol 176:346-356 (Pubitemid 43023280)
31. Datta-Mannan A, Witcher DR, Tang Y, Watkins J, Jiang W, Wroblewski VJ (2007) Humanized IgG1 variants with differential binding properties to the neonatal Fc receptor: relationship to pharmacokinetics in mice and primates. Drug Metab Dispos 35:86-94 (Pubitemid 46036480)
32. Datta-Mannan A, Witcher DR, Tang Y, Watkins J, Wroblewski VJ (2007) Monoclonal antibody clearance. Impact of modulating the interaction of IgG with the neonatal Fc receptor. J Biol Chem 282:1709-1717 (Pubitemid 47076691)
33. Chen Y, Balthasar JP (2010) A physiologically-based pharmacokinetic (PBPK) model for disposition of IgG with altered FcRn binding kinetics, AAPS Annual Meeting, New Orleans, p R6397
34. Emond C, Birnbaum LS, DeVito MJ (2006) Use of a physiologically based pharmacokinetic model for rats to study the influence of body fat mass and induction of CYP1A2 on the pharmacokinetics of TCDD. Environ Health Perspect 114:1394-1400 (Pubitemid 44314763)
35. Dedrick RL, Bischoff KB (1980) Species similarities in pharmacokinetics. Fed Proc. 39:54-59 (Pubitemid 10146117)
36. Johnson TN (2005) Modelling approaches to dose estimation in children. Br J Clin Pharmacol 59:663-669
37. Parrott N, Lave T (2002) Prediction of intestinal absorption: comparative assessment of GASTROPLUS and IDEA. Eur J Pharm Sci 17:51-61 (Pubitemid 35287171)
38. Bischoff KB, Dedrick RL (1968) Thiopental pharmacokinetics. J Pharm Sci 57:1346-1351
39. Roopenian DC, Akilesh S (2007) FcRn: the neonatal Fc receptor comes of age. Nat Rev Immunol 7:715-725 (Pubitemid 47327396)
40. Ghetie V, Hubbard JG, Kim JK, Tsen MF, Lee Y, Ward ES (1996) Abnormally short serum half-lives of IgG in beta 2-microglobulin-deficient mice. Eur J Immunol 26:690-696 (Pubitemid 26091401)
41. Junghans RP, Anderson CL (1996) The protection receptor for IgG catabolism is the beta2-microglobulin-containing neonatal intestinal transport receptor. Proc Natl Acad Sci USA 93:5512-5516
42. Brambell FW (1969) The transmission of immune globulins from the mother to the foetal and newborn young. Proc Nutr Soc 28:35-41
43. Ober RJ, Martinez C, Vaccaro C, Zhou J, Ward ES (2004) Visualizing the site and dynamics of IgG salvage by the MHC class I-related receptor, FcRn. J Immunol 172:2021-2029 (Pubitemid 38182347)
44. Montoyo HP, Vaccaro C, Hafner M, Ober RJ, Mueller W, Ward ES (2009) Conditional deletion of the MHC class I-related receptor FcRn reveals the sites of IgG homeostasis in mice. Proc Natl Acad Sci USA 106:2788-2793
45. Zhou J, Johnson JE, Ghetie V, Ober RJ, Ward ES (2003) Generation of mutated variants of the human form of the MHC class I-related receptor, FcRn, with increased affinity for mouse immunoglobulin G. J Mol Biol 332:901-913 (Pubitemid 37101376)
46. Haymann JP, Levraud JP, Bouet S, Kappes V, Hagege J, Nguyen G, Xu Y, Rondeau E, Sraer JD (2000) Characterization and localization of the neonatal Fc receptor in adult human kidney. J Am Soc Nephrol 11:632-639 (Pubitemid 30171872)
47. Kobayashi N, Suzuki Y, Tsuge T, Okumura K, Ra C, Tomino Y (2002) FcRn-mediated transcytosis of immunoglobulin G in human renal proximal tubular epithelial cells. Am J Physiol Renal Physiol 282:F358-F365 (Pubitemid 34654568)
48. Borvak J, Richardson J, Medesan C, Antohe F, Radu C, Simionescu M, Ghetie V, Ward ES (1998) Functional expression of the MHC class I-related receptor, FcRn, in endothelial cells of mice. Int Immunol 10:1289-1298 (Pubitemid 28414334)
49. Cauza K, Hinterhuber G, Dingelmaier-Hovorka R, Brugger K, Klosner G, Horvat R, Wolff K, Foedinger D (2005) Expression of FcRn, the MHC class I-related receptor for IgG, in human keratinocytes. J Invest Dermatol 124:132-139 (Pubitemid 40100961)
50. Blumberg RS, Koss T, Story CM, Barisani D, Polischuk J, Lipin A, Pablo L, Green R, Simister NE (1995) A major histocompatibility complex class I-related Fc receptor for IgG on rat hepatocytes. J Clin Invest 95:2397-2402
51. Cianga P, Cianga C, Cozma L, Ward ES, Carasevici E (2003) The MHC class I related Fc receptor, FcRn, is expressed in the epithelial cells of the human mammary gland. Hum Immunol 64:1152-1159 (Pubitemid 37475276)
52. Zhu X, Meng G, Dickinson BL, Li X, Mizoguchi E, Miao L, Wang Y, Robert C, Wu B, Smith PD, Lencer WI, Blumberg RS (2001) MHC class I-related neonatal Fc receptor for IgG is functionally expressed in monocytes, intestinal macrophages, and dendritic cells. J Immunol 166:3266-3276 (Pubitemid 33117326)
53. Akilesh S, Christianson GJ, Roopenian DC, Shaw AS (2007) Neonatal FcR expression in bone marrow-derived cells functions to protect serum IgG from catabolism. J Immunol 179:4580-4588
54. Kandil E, Egashira M, Miyoshi O, Niikawa N, Ishibashi T, Kasahara M (1996) The human gene encoding the heavy chain of the major histocompatibility complex class I-like Fc receptor (FCGRT) maps to 19q13.3. Cytogenet Cell Genet 73:97-98
55. Su AI, Wiltshire T, Batalov S, Lapp H, Ching KA, Block D, Zhang J, Soden R, Hayakawa M, Kreiman G, Cooke MP, Walker JR, Hogenesch JB (2004) A gene atlas of the mouse and human protein-encoding transcriptomes. Proc Natl Acad Sci USA 101:6062-6067 (Pubitemid 38520528)
56. Israel EJ, Taylor S, Wu Z, Mizoguchi E, Blumberg RS, Bhan A, Simister NE (1997) Expression of the neonatal Fc receptor, FcRn, on human intestinal epithelial cells. Immunology 92:69-74 (Pubitemid 27380883)
57. Haigler HT, McKanna JA, Cohen S (1979) Rapid stimulation of pinocytosis in human carcinoma cells A-431 by epidermal growth factor. J Cell Biol 83:82-90 (Pubitemid 10197035)
58. Pease LF III, Elliott JT, Tsai DH, Zachariah MR, Tarlov MJ (2008) Determination of protein aggregation with differential mobility analysis: application to IgG antibody. Biotechnol Bioeng 101:1214-1222
59. Vugmeyster Y, DeFranco D, Szklut P, Wang Q, Xu X (2010) Biodistribution of [125I]-labeled therapeutic proteins: application in protein drug development beyond oncology. J Pharm Sci 99:1028-1045
60. Alley SC, Okeley NM, Senter PD (2010) Antibody-drug conjugates: targeted drug delivery for cancer. Curr Opin Chem Biol 14:529-537
61. Doppalapudi VR, Tryder N, Li L, Aja T, Griffith D, Liao FF, Roxas G, Ramprasad MP, Bradshaw C, Barbas CF 3rd (2007) Chemically programmed antibodies: endothelin receptor targeting CovX-Bodies. Bioorg Med Chem Lett 17:501-506 (Pubitemid 46073729)
62. Stanfield RL, Dooley H, Verdino P, Flajnik MF, Wilson IA (2007) Maturation of shark single-domain (IgNAR) antibodies: evidence for induced-fit binding. J Mol Biol 367:358-372 (Pubitemid 46295421)
63. Igawa T, Tsunoda H, Tachibana T, Maeda A, Mimoto F, Moriyama C, Nanami M, Sekimori Y, Nabuchi Y, Aso Y, Hattori K (2010) Reduced elimination of IgG antibodies by engineering the variable region. Protein Eng Des Sel 23:385-392
64. Boswell CA, Tesar DB, Mukhyala K, Theil FP, Fielder PJ, Khawli LA (2010) Effects of charge on antibody tissue distribution and pharmacokinetics. Bioconjug Chem 21:2153-2163
65. Ghetie V, Popov S, Borvak J, Radu C, Matesoi D, Medesan C, Ober RJ, Ward ES (1997) Increasing the serum persistence of an IgG fragment by random mutagenesis. Nat Biotechnol 15:637-640 (Pubitemid 27291163)
66. Gurbaxani B, Dela Cruz LL, Chintalacharuvu K, Morrison SL (2006) Analysis of a family of antibodies with different half-lives in mice fails to find a correlation between affinity for FcRn and serum half-life. Mol Immunol 43:1462-1473 (Pubitemid 43356386)
67. Yeung YA, Leabman MK, Marvin JS, Qiu J, Adams CW, Lien S, Starovasnik MA, Lowman HB (2009) Engineering human IgG1 affinity to human neonatal Fc receptor: impact of affinity improvement on pharmacokinetics in primates. J Immunol 182:7663-7671
68. Deng R, Loyet KM, Lien S, Iyer S, DeForge LE, Theil FP, Lowman HB, Fielder PJ, Prabhu S (2010) Pharmacokinetics of humanized monoclonal anti-tumor necrosis factor-{alpha} antibody and its neonatal Fc receptor variants in mice and cynomolgus monkeys. Drug Metab Dispos 38:600-605
69. Wang W, Lu P, Fang P, Hamuro L, Pittman T, Carr B, Hochman J, Prueksaritanont T (2011) Monoclonal antibodies with identical Fc sequences can bind to FcRn differentially with pharmacokinetic consequences. Drug Metab Dispos 39(9):1469-1477
70. Qiao SW, Kobayashi K, Johansen FE, Sollid LM, Andersen JT, Milford E, Roopenian DC, Lencer WI, Blumberg RS (2008) Dependence of antibody-mediated presentation of antigen on FcRn. Proc Natl Acad Sci USA 105:9337-9342