Galactosylation variations in marketed therapeutic antibodies

mAbs

Volumn 4, Issue 3, 2012, Pages 385-391

  Shantha Raju, T ^a   Jordan, Robert E ^a  

^a JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

Author keywords

Efficacy; Fucose; Galactose; Galactosylation; Glycans; Glycosylation; IgG; rIgG; Safety

Indexed keywords

ASPARAGINE; FC RECEPTOR; GALACTOSE; GLYCAN; IMMUNOGLOBULIN G; MONOCLONAL ANTIBODY; OLIGOSACCHARIDE; RITUXIMAB;

ANIMAL CELL; ARTICLE; BIOLOGICAL ACTIVITY; CHEMICAL MODIFICATION; CHEMICAL REACTION; CHO CELL; GALACTOSYLATION; GENE EXPRESSION SYSTEM; MATRIX ASSISTED LASER DESORPTION IONIZATION TIME OF FLIGHT MASS SPECTROMETRY; MOUSE; MYELOMA CELL; NONHUMAN;

ANIMALS; ANTIBODIES, MONOCLONAL; CELL CULTURE TECHNIQUES; CELL LINE, TUMOR; CHO CELLS; CRICETINAE; GALACTOSE; HUMANS; IMMUNOTHERAPY; MARKETING; MICE; POLYSACCHARIDES; PROTEIN PROCESSING, POST-TRANSLATIONAL;

EID: 84860914656     PISSN: 19420862     EISSN: 19420870     Source Type: Journal    
DOI: 10.4161/mabs.19868     Document Type: Article

References (29)

1. Raju TS. Terminal sugars of Fc glycans influence antibody effector functions of IgGs. Curr Opin Immunol 2008; 20:471-8; PMID:18606225; http://dx.doi.org/10.1016/j.coi.2008.06.007.
2. Reichert JM. Antibody-based therapeutics to watch in 2011. MAbs 2011; 3:76-99; PMID:21051951; http://dx.doi.org/10.4161/mabs.3.1.13895.
3. Reichert JM. Probabilities of success for antibody therapeutics. MAbs 2009; 1:387-9; PMID:20068390; http://dx.doi.org/10.4161/mabs.1.4.9031.
4. Strohl WR, Knight DM. Discovery and development of biopharmaceuticals: current issues. Curr Opin Biotechnol 2009; 20:668-72; PMID:19896824; http://dx.doi.org/10.1016/j.copbio.2009.10.012.
5. Jefferis R. Recombinant antibody therapeutics: the impact of glycosylation on mechanisms of action. Trends Pharmacol Sci 2009; 30:356-62; PMID:19552968; http://dx.doi.org/10.1016/j.tips.2009.04.007.
6. Jefferis R. Glycosylation as a strategy to improve antibody-based therapeutics. Nat Rev Drug Discov 2009; 8:226-34; PMID:19247305; http://dx.doi.org/10.1038/nrd2804.
7. Jefferis R. Aglycosylated antibodies and the methods of making and using them: WO2008030564. Expert Opin Ther Pat 2009; 19:101-5; PMID:19441902; http://dx.doi.org/10.1517/13543770802592408.
8. Hossler P, Khattak SF, Li ZJ. Optimal and consistent protein glycosylation in mammalian cell culture. Glycobiology 2009; 19:936-49; PMID:19494347; http://dx.doi.org/10.1093/glycob/cwp079.
9. Raju TS. Glycosylation variations with expression systems and their impact on biological Activity of therapeutic immunoglobulins. Bioprocess Int 2003; 1:44-54.
10. Raju TS, Briggs JB, Borge SM, Jones AJ. Speciesspecific variation in glycosylation of IgG: evidence for the species-specific sialylation and branch-specific galactosylation and importance for engineering recombinant glycoprotein therapeutics. Glycobiology 2000; 10:477-86; PMID:10764836; http://dx.doi.org/10.1093/glycob/10.5.477.
11. Gramer MJ, Eckblad JJ, Donahue R, Brown J, Shultz C, Vickerman K, et al. Modulation of antibody galactosylation through feeding of uridine, manganese chloride and galactose. Biotechnol Bioeng 2011; 108:1591-602; PMID:21328321; http://dx.doi.org/10.1002/bit.23075.
12. Hodoniczky J, Zheng YZ, James DC. Control of recombinant monoclonal antibody effector functions by Fc N-glycan remodeling in vitro. Biotechnol Prog 2005; 21:1644-52; PMID:16321047; http://dx.doi.org/10.1021/bp050228w.
13. Maloney DG, Grillo-López AJ, White CA, Bodkin D, Schilder RJ, Neidhart JA, et al. IDEC-C2B8 (Rituximab) anti-CD20 monoclonal antibody therapy in patients with relapsed low-grade non-Hodgkin's lymphoma. Blood 1997; 90:2188-95; PMID:9310469.
14. Schiestl M, Stangler T, Torella C, Cepeljnik T, Toll H, Grau R. Acceptable changes in quality attributes of glycosylated biopharmaceuticals. Nat Biotechnol 2011; 29:310-2; PMID:21478841; http://dx.doi.org/10.1038/nbt.1839.
15. Higgins E. Carbohydrate analysis throughout the development of a protein therapeutic. Glycoconj J 2010; 27:211-25; PMID:19888650; http://dx.doi.org/10. 1007/s10719-009-9261-x.
16. Strohl WR. Optimization of Fc-mediated effector functions of monoclonal antibodies. Curr Opin Biotechnol 2009; 20:685-91; PMID:19896358; http://dx.doi.org/10.1016/j.copbio.2009.10.011.
17. Papac DI, Wong A, Jones AJ. Analysis of acidic oligosaccharides and glycopeptides by matrix-assisted laser desorption/ionization time-of-flight mass spectrometry. Anal Chem 1996; 68:3215-23; PMID:8797382; http://dx.doi.org/10. 1021/ac960324z.
18. Anumula KR. Advances in fluorescence derivatization methods for high-performance liquid chromatographic analysis of glycoprotein carbohydrates. Anal Biochem 2006; 350:1-23; PMID:16271261; http://dx.doi.org/10.1016/j.ab.2005. 09.037.
19. Raju TS, Scallon BJ. Glycosylation in the Fc domain of IgG increases resistance to proteolytic cleavage by papain. Biochem Biophys Res Commun 2006; 341:797-803; PMID:16442075; http://dx.doi.org/10.1016/j. bbrc.2006.01.030.
20. Raju TS, Scallon B. Fc glycans terminated with N-acetylglucosamine residues increase antibody resistance to papain. Biotechnol Prog 2007; 23:964-71; PMID:17571902.
21. Shields RL, Lai J, Keck R, O'Connell LY, Hong K, Meng YG, et al. Lack of fucose on human IgG1 N-linked oligosaccharide improves binding to human Fcgamma RIII and antibody-dependent cellular toxicity. J Biol Chem 2002; 277:26733-40; PMID:11986321; http://dx.doi.org/10.1074/jbc.M202069200.
22. Read EK, Park JT, Brorson KA. Industry and regulatory experience of the glycosylation of monoclonal antibodies. Biotechnol Appl Biochem 2011; 58:213-9; PMID:21838794; http://dx.doi.org/10.1002/bab.35.
23. Wacker C, Berger CN, Girard P, Meier R. Glycosylation profiles of therapeutic antibody pharmaceuticals. Eur J Pharm Biopharm 2011; 79:503-7; PMID:21745568; http://dx.doi.org/10.1016/j.ejpb.2011.06.010.
24. Millward TA, Heitzmann M, Bill K, Längle U, Schumacher P, Forrer K. Effect of constant and variable domain glycosylation on pharmacokinetics of therapeutic antibodies in mice. Biologicals 2008; 36:41-7; PMID:17890101; http://dx.doi.org/10.1016/j.biologicals. 2007.05.003.
25. Scallon BJ, Tam SH, McCarthy SG, Cai AN, Raju TS. Higher levels of sialylated Fc glycans in immunoglobulin G molecules can adversely impact functionality. Mol Immunol 2007; 44:1524-34; PMID:17045339; http://dx.doi.org/ 10.1016/j.molimm.2006.09.005.
26. Scallon B, McCarthy S, Radewonuk J, Cai A, Naso M, Raju TS, et al. Quantitative in vivo comparisons of the Fc gamma receptor-dependent agonist activities of different fucosylation variants of an immunoglobulin G antibody. Int Immunopharmacol 2007; 7:761-72; PMID:17466910; http://dx.doi.org/10.1016/j. intimp.2007.01.014.
27. Brezski RJ, Vafa O, Petrone D, Tam SH, Powers G, Ryan MH, et al. Tumor-associated and microbial proteases compromise host IgG effector functions by a single cleavage proximal to the hinge. Proc Natl Acad Sci USA 2009; 106:17864-9; PMID:19815504; http://dx.doi.org/10.1073/pnas.0904174106.
28. Raju TS, Briggs JB, Chamow SM, Winkler ME, Jones AJ. Glycoengineering of therapeutic glycoproteins: in vitro galactosylation and sialylation of glycoproteins with terminal N-acetylglucosamine and galactose residues. Biochemistry 2001; 40:8868-76; PMID:11467948; http://dx.doi.org/10.1021/ bi010475i.
29. Son YD, Jeong YT, Park SY, Kim JH. Enhanced sialylation of recombinant human erythropoietin in Chinese hamster ovary cells by combinatorial engineering of selected genes. Glycobiology 2011; 21:1019-28; PMID:21436238; http://dx.doi.org/10.1093/glycob/cwr034.