A PBPK workflow for first-in-human dose selection of a subcutaneously administered pegylated peptide

Journal of Pharmacokinetics and Pharmacodynamics

Volumn 42, Issue 2, 2015, Pages 135-150

  Offman, Elliot ^a   Edginton, Andrea N ^a  

^a UNIVERSITY OF WATERLOO   (Canada)

Author keywords

Human; Monkey; Physiologically based pharmacokinetic model; Protein; Subcutaneous

Indexed keywords

MACROGOL 400; PEPTIDE;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BIOLOGICAL MODEL; DOSE CALCULATION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; FEMALE; FIRST IN HUMAN STUDY; HUMAN; HUMAN EXPERIMENT; MACACA FASCICULARIS; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; NORMAL HUMAN; PHYSIOLOGICALLY BASED PHARMACOKINETIC MODEL; PRIORITY JOURNAL; PROCESS OPTIMIZATION; SCALE UP; SIMULATION; SINGLE DRUG DOSE; TIME TO MAXIMUM PLASMA CONCENTRATION; WORKFLOW; ANIMAL; PROCEDURES; SUBCUTANEOUS DRUG ADMINISTRATION;

ANIMALS; FEMALE; HUMANS; INJECTIONS, SUBCUTANEOUS; MACACA FASCICULARIS; MODELS, BIOLOGICAL; PEPTIDES; WORKFLOW;

EID: 84925508028     PISSN: 1567567X     EISSN: 15738744     Source Type: Journal    
DOI: 10.1007/s10928-015-9406-4     Document Type: Article

References (36)

1. Offman E, Edginton AN (2013) Contrasting toxicokinetic evaluations and interspecies pharmacokinetic scaling approaches for small molecules and biologics: applicability to biosimilar development. Xenobiotica 43:561–569
2. Ling J, Zhou H, Jiao Q, Davis HM (2009) Interspecies scaling of therapeutic monoclonal antibodies: initial look. J Clin Pharmacol 49:1382–1402
3. Deng R, Iyer S, Theil FP, Mortensen DL, Fielder PJ, Prabhu S (2011) Projecting human pharmacokinetics of therapeutic antibodies from nonclinical data: what have we learned? Ther Monoclon Antib 3:61–66
4. Supersaxo A, Hein W, Gallati H, Steffen H (1988) Recombinant human interferon alpha-2a: delivery to lymphoid tissue by selected modes of application. Pharm Res 5:472–476
5. Supersaxo A, Hein WR, Steffen H (1990) Effect of molecular weight on the lymphatic absorption of water-soluble compounds following subcutaneous administration. Pharm Res 7:167–169
6. Dahlberg AM, Kaminskas LM, Smith A, Nicolazzo JA, Porter CJ, Bulitta JB, McIntosh MP (2014) The lymphatic system plays a major role in the intravenous and subcutaneous pharmacokinetics of trastuzumab in rats. Mol Pharm 11:496–504
7. Wang W, Chen N, Shen X, Cunningham P, Fauty S, Michel K, Wang B, Hong X, Adreani C, Nunes CN, Johnson CV, Yin KC, Groff M, Zou Y, Liu L, Hamuro L, Prueksaritanont T (2012) Lymphatic transport and catabolism of therapeutic proteins after subcutaneous administration to rats and dogs. Drug Metab Dispos 40:952–962
8. Richter WF, Bhansali SG, Morris ME (2012) Mechanistic determinants of biotherapeutics absorption following SC administration. AAPS J 14:559–570
9. Rippe B, Haraldsson B (1994) Transport of macromolecules across microvascular walls: the two-pore theory. Physiol Rev 74:163–219
10. Rippe B, Haraldsson B (1987) Fluid and protein fluxes across small and large pores in the microvasculature. Application of two-pore equations. Acta Physiol Scand 131:411–428
11. Zhao L, Ji P, Li Z, Roy P, Sahajwalla CG (2013) The antibody drug absorption following subcutaneous or intramuscular administration and its mathematical description by coupling physiologically based absorption process with the conventional compartment pharmacokinetic model. J Clin Pharmacol 53:314–325
12. Kagan L, Mager DE (2013) Mechanisms of subcutaneous absorption of rituximab in rats. Drug Metab Dispos 41:248–255
13. Zheng Y, Tesar DB, Benincosa L, Birnbock H, Boswell CA, Bumbaca D, Cowan KJ, Danilenko DM, Daugherty AL, Fielder PJ, Grimm HP, Joshi A, Justies N, Kolaitis G, Lewin-Koh N, Li J, McVay S, O’Mahony J, Otteneder M, Pantze M, Putnam WS, Qiu ZJ, Ruppel J, Singer T, Stauch O, Theil FP, Visich J, Yang J, Ying Y, Khawli LA, Richter WF (2012) Minipig as a potential translatable model for monoclonal antibody pharmacokinetics after intravenous and subcutaneous administration. MAbs 4:243–255
14. Shah D, Betts A (2012) Towards a platform PBPK model to characterize the plasma and tissue disposition of monoclonal antibodies in preclinical species and human. J Pharmacokinet Pharmacodyn 39:67–86
15. 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
16. 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
17. Ferl GZ, Wu AM, DiStefano JJ III (2005) A predictive model of therapeutic monoclonal antibody dynamics and regulation by the neonatal Fc receptor (FcRn). Ann Biomed Eng 33:1640–1652
18. R Core Team (2013) R: A language and environment for statistical computing
19. Graf JF, Scholz BJ, Zavodszky MI (2012) BioDMET: a physiologically based pharmacokinetic simulation tool for assessing proposed solutions to complex biological problems. J Pharmacokinet Pharmacodyn 39:37–54
20. Kawai R, Mathew D, Tanaka C, Rowland M (1998) Physiologically based pharmacokinetics of cyclosporine A: extension to tissue distribution kinetics in rats and scale-up to human. J Pharmacol Exp Ther 287:457–468
21. Davies B, Morris T (1993) Physiological parameters in laboratory animals and humans. Pharm Res 10:1093–1095
22. Swartz MA (2001) The physiology of the lymphatic system. Adv Drug Deliv Rev 50:3–20
23. 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
24. Baumann A, Tuerck D, Prabhu S, Dickmann L, Sims J (2014) Pharmacokinetics, metabolism and distribution of PEGs and PEGylated proteins: quo vadis? Drug Discov Today 19:1623–1631
25. Woodburn KW, Fong KL, Wilson SD, Sloneker S, Strzemienski P, Solon E, Moriya Y, Tagawa Y (2013) Peginesatide clearance, distribution, metabolism, and excretion in monkeys following intravenous administration. Drug Metab Dispos 41:774–784
26. Iwama R, Sato T, Sakurai K, Takasuna K, Ichijo T, Furuhama K, Satoh H (2014) Estimation of glomerular filtration rate in cynomolgus monkeys (Macaca fascicularis). J Vet Med Sci 76:1423–1426
27. Gordon S (2003) Alternative activation of macrophages. Nat Rev Immunol 3:23–35
28. 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
29. Wang W, Prueksaritanont T (2010) Prediction of human clearance of therapeutic proteins: simple allometric scaling method revisited. Biopharm Drug Dispos 31:253–263
30. Li Z, Rana TM (2014) Therapeutic targeting of microRNAs: current status and future challenges. Nat Rev Drug Discov 13:622–638
31. Caliceti P, Veronese FM (2003) Pharmacokinetic and biodistribution properties of poly(ethylene glycol)-protein conjugates. Adv Drug Deliv Rev 55:1261–1277
32. 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
33. Kusterle M, Jevsevar S, Porekar VG (2008) Size of pegylated protein conjugates studied by various methods. Acta Chim Slov 55:594–601
34. Bacher G, Szymanski WW, Kaufman SL, Zollner P, Blaas D, Allmaier G (2001) Charge-reduced nano electrospray ionization combined with differential mobility analysis of peptides, proteins, glycoproteins, noncovalent protein complexes and viruses. J Mass Spectrom 36:1038–1052
35. 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
36. Woo S, Jusko WJ (2007) Interspecies comparisons of pharmacokinetics and pharmacodynamics of recombinant human erythropoietin. Drug Metab Dispos 35:1672–1678