Compatibility, physical stability, and characterization of an IgG4 monoclonal antibody after dilution into different intravenous administration bags

Journal of Pharmaceutical Sciences

Volumn 101, Issue 10, 2012, Pages 3636-3650

  Kumru, Ozan S ^a   Liu, Jun ^b   Ji, Junyan A ^b   Cheng, Wilson ^b   Wang, Y John ^b   Wang, Tingting ^a   Joshi, Sangeeta B ^a   Middaugh, C Russell ^a   Volkin, David B ^a  

^a UNIVERSITY OF KANSAS   (United States)

^b GENENTECH INC   (United States)

Author keywords

Formulation; I.v. administration; Monoclonal antibody; Parenteral; Protein aggregation; Stability

Indexed keywords

IMMUNOGLOBULIN G4; MONOCLONAL ANTIBODY; NANOPARTICLE; POLYOLEFIN; POLYSORBATE 20; POLYVINYLCHLORIDE; SODIUM CHLORIDE; THIOL;

ARTICLE; CONTROLLED STUDY; DENATURATION; DILUTION; DISULFIDE BOND; DRUG FORMULATION; DRUG STABILITY; FLUORESCENCE SPECTROSCOPY; GEL PERMEATION CHROMATOGRAPHY; HEAT; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; INFRARED SPECTROSCOPY; PARTICLE SIZE; PARTICULATE MATTER; TRANSMISSION ELECTRON MICROSCOPY; TURBIDITY;

EID: 84865393469     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23224     Document Type: Article

References (55)

1. Shire SJ, Shahrokh Z, Liu J. 2004. Challenges in the development of high protein concentration formulations. J Pharm Sci 93(6):1390-1402.
2. Shire SJ. 2009. Formulation and manufacturability of biologics. Curr Opin Biotechnol 20(6):708-714.
3. Yalkowsky SH, Krzyzaniak JF, Ward GH. 1998. Formulation-related problems associated with intravenous drug delivery. J Pharm Sci 87(7):787-796.
4. de Lemos ML, Hamata L. 2007. Stability issues of parenteral chemotherapy drugs. J Oncol Pharm Pract 13(1):27-31.
5. Waugh WN, Trissel LA, Stella VJ. 1991. Stability, compatibility, and plasticizer extraction of Taxol (NSC-125973) injection diluted in infusion solutions and stored in various containers. Am J Hosp Pharm 48(7):1520-1524.
6. Nuijen B, Bouma M, Manada C, Jimeno JM, Lazaro LL, Bult A, Beijnen JH. 2001. Compatibility and stability of the investigational polypeptide marine anticancer agent kahalalide F in infusion devices. Invest New Drugs 19(4):273-281.
7. DiMichele DM, Lasak ME, Miller CH. 1996. In vitro factor VIII recovery during the delivery of ultrapure factor VIII concentrate by continuous infusion. Am J Hematol 51(2):99-103.
8. McLeod AG, Walker IR, Zheng S, Hayward CP. 2000. Loss of factor VIII activity during storage in PVC containers due to adsorption. Haemophilia 6(2):89-92.
9. Chang JY, Xiao NJ, Zhu M, Zhang J, Hoff E, Russell SJ, Katta V, Shire SJ. 2010. Leachables from saline-containing IV bags can alter therapeutic protein properties. Pharm Res 27(11):2402-2413.
10. Parti R, Mankarious S. 1997. Stability assessment of lyophilized intravenous immunoglobulin after reconstitution in glass containers and poly(vinyl chloride) bags. Biotechnol Appl Biochem 25(Pt 1):13-18.
11. Knezevic-Maramica I, Kruskall MS. 2003. Intravenous immune globulins: An update for clinicians. Transfusion 43(10):1460-1480.
12. Bolli R, Woodtli K, Bärtschi M, Höfferer L, Lerch P. 2010. l-Proline reduces IgG dimer content and enhances the stability of intravenous immunoglobulin (IVIG) solutions. Biologicals 38(1):150-157.
13. Ikesue H, Vermeulen LC, Hoke R, Kolesar JM. 2010. Stability of cetuximab and panitumumab in glass vials and polyvinyl chloride bags. Am J Health Syst Pharm 67(3):223-226.
14. Fischer S, Hoernschemeyer J, Mahler HC. 2008. Glycation during storage and administration of monoclonal antibody formulations. Eur J Pharm Biopharm 70(1):42-50.
15. Demeule B, Palais C, Machaidze G, Gurny R, Arvinte T. 2009. New methods allowing the detection of protein aggregates: A case study on trastuzumab. MAbs 1(2):142-150.
16. Alavattam S, Glover ZK, Piros N, Xiao N, Patel A, Kabakoff B. 2012. Stability of IgG1 monoclonal antibodies in intravenous infusion bags under clinical in-use conditions. J Pharm Sci 101(1):21-30.
17. Wuchner K, Büchler J, Spycher R, Dalmonte P, Volkin DB. 2010. Development of a microflow digital imaging assay to characterize protein particulates during storage of a high concentration IgG1 monoclonal antibody formulation. J Pharm Sci 99(8):3343-3361.
18. Nayak A, Colandene J, Bradford V, Perkins M. 2011. Characterization of subvisible particle formation during the filling pump operation of a monoclonal antibody solution. J Pharm Sci 100(10):4198-4204.
19. Barnard JG, Singh S, Randolph TW, Carpenter JF. 2011. Subvisible particle counting provides a sensitive method of detecting and quantifying aggregation of monoclonal antibody caused by freeze-thawing: Insights into the roles of particles in the protein aggregation pathway. J Pharm Sci 100(2):492-503.
20. Demeule B, Messick S, Shire SJ, Liu J. 2010. Characterization of particles in protein solutions: Reaching the limits of current technologies. AAPS J 12(4):708-715.
21. Narhi LO, Jiang Y, Cao S, Benedek K, Shnek D. 2009. A critical review of analytical methods for subvisible and visible particles. Curr Pharm Biotechnol 10(4):373-381.
22. Singh SK. 2011. Impact of product-related factors on immunogenicity of biotherapeutics. J Pharm Sci 100(2):354-387.
23. Rosenberg AS. 2006. Effects of protein aggregates: An immunologic perspective. AAPS J 8(3):E501-E507.
24. Brinks V, Jiskoot W, Schellekens H. 2011. Immunogenicity of therapeutic proteins: The use of animal models. Pharm Res 28(10):2379-2385.
25. Kaliyaperumal A, Jing S. 2009. Immunogenicity assessment of therapeutic proteins and peptides. Curr Pharm Biotechnol 10(4):352-358.
26. Dillon TM, Ricci MS, Vezina C, Flynn GC, Liu YD, Rehder DS, Plant M, Henkle B, Li Y, Deechongkit S, Varnum B, Wypych J, Balland A, Bondarenko PV. 2008. Structural and functional characterization of disulfide isoforms of the human IgG2 subclass. J Biol Chem 283(23):16206-16215.
27. Wypych J, Li M, Guo A, Zhang Z, Martinez T, Allen MJ, Fodor S, Kelner DN, Flynn GC, Liu YD, Bondarenko PV, Ricci MS, Dillon TM, Balland A. 2008. Human IgG2 antibodies display disulfide-mediated structural isoforms. J Biol Chem 283(23):16194-16205.
28. Nirula A, Glaser SM, Kalled SL, Taylora FR. 2011. What is IgG4? A review of the biology of a unique immunoglobulin subtype. Curr Opin Rheumatol 23(1):119-124.
29. Rispens T, Ooijevaar-de Heer P, Bende O, Aalberse RC. 2011. Mechanism of immunoglobulin G4 Fab-arm exchange. J Am Chem Soc 133(26):10302-10311.
30. Brych SR, Gokarn YR, Hultgen H, Stevenson RJ, Rajan R, Matsumura M. 2010. Characterization of antibody aggregation: Role of buried, unpaired cysteines in particle formation. J Pharm Sci 99(2):764-781.
31. Bond MD, Panek ME, Zhang Z, Wang D, Mehndiratta P, Zhao H, Gunton K, Ni A, Nedved ML, Burman S, Volkin DB. 2010. Evaluation of a dual-wavelength size exclusion HPLC method with improved sensitivity to detect protein aggregates and its use to better characterize degradation pathways of an IgG1 monoclonal antibody. J Pharm Sci 99(6):2582-2597.
32. Joubert MK, Luo Q, Nashed-Samuel Y, Wypych J, Narhi LO. 2011. Classification and characterization of therapeutic antibody aggregates. J Biol Chem 286(28):25118-25133.
33. Filipe V, Hawe A, Jiskoot W. 2010. Critical evaluation of Nanoparticle Tracking Analysis (NTA) by NanoSight for the measurement of nanoparticles and protein aggregates. Pharm Res 27(5):796-810.
34. Boyd RD, Pichaimuthu SK, Cuenat A. 2011. New approach to inter-technique comparisons for nanoparticle size measurements; using atomic force microscopy, nanoparticle tracking analysis and dynamic light scattering. Colloid Surf A 387(1-3):35-42.
35. Zolls S, Tantipolphan R, Wiggenhorn M, Winter G, Jiskoot W, Friess W, Hawe A. 2012. Particles in therapeutic protein formulations, Part 1: Overview of analytical methods. J Pharm Sci 101(3):914-935.
36. Murphy BM, Zhang N, Payne RW, Davis JM, Abdul-Fattah AM, Matsuura JE, Herman AC, Manning MC. 2012. Structure, stability, and mobility of a lyophilized IgG1 monoclonal antibody as determined using second-derivative infrared spectroscopy. J Pharm Sci 101(1):81-91.
37. Narhi LO, Schmit J, Bechtold-Peters K, Sharma D. 2012. Classification of protein aggregates. J Pharm Sci 101(2):493-498.
38. Aalberse RC, Stapel SO, Schuurman J, Rispens T. 2009. Immunoglobulin G4: An odd antibody. Clin Exp Allergy 39(4):469-477.
39. Labrijn AF, Buijsse AO, van den Bremer ETJ, Verwilligen AYW, Bleeker WK, Thorpe SJ, Killestein J, Polman CH, Aalberse RC, Schuurman J, van de Winkel JGJ, Parren PWHI. 2009. Therapeutic IgG4 antibodies engage in Fab-arm exchange with endogenous human IgG4 in vivo. Nat Biotechnol 27(8):767-771.
40. Lewis KB, Meengs B, Bondensgaard K, Chin L, Hughes SD, Kjaer B, Lund S, Wang L. 2009. Comparison of the ability of wild type and stabilized human IgG(4) to undergo Fab arm exchange with endogenous IgG(4)in vitro and in vivo. Contemp Top Mol Immunol 46(16):3488-3494.
41. Gokarn YR, Fesinmeyer RM, Saluja A, Razinkov V, Chase SF, Laue TM, Brems DN. 2011. Effective charge measurements reveal selective and preferential accumulation of anions, but not cations, at the protein surface in dilute salt solutions. Protein Sci 20(3):580-587.
42. Fesinmeyer RM, Hogan S, Saluja A, Brych SR, Kras E, Narhi LO, Brems DN, Gokarn YR. 2009. Effect of ions on agitation- and temperature-induced aggregation reactions of antibodies. Pharm Res 26(4):903-913.
43. Trivedi MV, Laurence JS, Siahaan TJ. 2009. The role of thiols and disulfides on protein stability. Curr Protein Pept Sci 10(6):614-625.
44. Zhang W, Czupryn MJ. 2002. Free sulfhydryl in recombinant monoclonal antibodies. Biotechnol Prog 18(3):509-513.
45. Banks DD, Gadgil HS, Pipes GD, Bondarenko PV, Hobbs V, Scavezze JL, Kim J, Jiang X-R, Mukku V, Dillon TM. 2008. Removal of cysteinylation from an unpaired sulfhydryl in the variable region of a recombinant monoclonal IgG1 antibody improves homogeneity, stability, and biological activity. J Pharm Sci 97(2):775-790.
46. Franey H, Brych SR, Kolvenbach CG, Rajan RS. 2010. Increased aggregation propensity of IgG2 subclass over IgG1: Role of conformational changes and covalent character in isolated aggregates. Protein Sci 19(9):1601-1615.
47. Luo Q, Joubert MK, Stevenson R, Ketchem RR, Narhi LO, Wypych J. 2011. Chemical modifications in therapeutic protein aggregates generated under different stress conditions. J Biol Chem 286(28):25134-25144.
48. Dong A, Prestrelski SJ, Allison SD, Carpenter JF. 1995. Infrared spectroscopic studies of lyophilization- and temperature-induced protein aggregation. J Pharm Sci 84(4):415-424.
49. Jenke D 2007. Evaluation of the chemical compatibility of plastic contact materials and pharmaceutical products; safety considerations related to extractables and leachables. J Pharm Sci 96(10):2566-2581.
50. Pearson SD, Trissel LA 1993. Leaching of diethylhexyl phthalate from polyvinyl chloride containers by selected drugs and formulation components. Am J Hosp Pharm 50(7):1405-1409.
51. de Lemos ML, Hamata L, Vu T 2005. Leaching of diethylhexyl phthalate from polyvinyl chloride materials into etoposide intravenous solutions. J Oncol Pharm Pract 11(4):155-157.
52. Joel SP, Clark PI, Slevin ML. 1995. Stability of the i.v. and oral formulations of etoposide in solution. Cancer Chemother Pharmacol 37(1-2):117-124.
53. Faouzi Me-A, Dine T, Luyckx M, Brunet C, Mallevais ML, Goudaliez F, Gressier B, Cazin M, Kablan J, Cazin JC. 1995. Stability, compatibility and plasticizer extraction of miconazole injection added to infusion solutions and stored in PVC containers. J Pharm Biomed Anal 13(11):1363-1372.
54. Boyle DA, Goldspiel BR. 1998. A review of paclitaxel (Taxol) administration, stability, and compatibility issues. Clin J Oncol Nurs 2(4):141-145.
55. Lebitasy M, Hecq J-D, Athanassopoulos A, Vanbeckbergen D, Jamart J, Galanti L. 2009. Effect of freeze-thawing on the long-term stability of calcium levofolinate in 5% dextrose stored on polyolefin infusion bags. J Clin Pharm Ther 34(4):423-428.