Liquid formulation for antibody drugs

Biochimica et Biophysica Acta - Proteins and Proteomics

Volumn 1844, Issue 11, 2014, Pages 2041-2052

  Uchiyama, Susumu ^a  

^a OSAKA UNIVERSITY   (Japan)

Author keywords

Aggregation; Antibody; Colloidal stability; Conformational stability; Formulation; Virial coefficient

Indexed keywords

DRUG ANTIBODY; INORGANIC SALT; POLYSORBATE;

ARTICLE; AUTOIMMUNE DISEASE; DEAMINATION; DENATURATION; DIFFERENTIAL SCANNING CALORIMETRY; DIPOLE; DRUG FORMULATION; DRUG MECHANISM; DRUG STABILITY; HUMAN; HYDROGEN BOND; IONIC STRENGTH; LIQUID; PHYSICAL CHEMISTRY; SEDIMENTATION RATE; TEMPERATURE; ULTRACENTRIFUGATION; VISCOSITY;

EID: 85028122676     PISSN: 15709639     EISSN: 18781454     Source Type: Journal    
DOI: 10.1016/j.bbapap.2014.07.016     Document Type: Review

References (71)

1. S.A. Abbas, V.K. Sharma, T.W. Patapoff, and D.S. Kalonia Opposite effects of polyols on antibody aggregation: thermal versus mechanical stresses Pharm. Res. 29 3 2012 683 694
2. M. Amano, J. Hasegawa, N. Kobayashi, N. Kishi, T. Nakazawa, S. Uchiyama, and K. Fukui Specific racemization of heavy-chain cysteine-220 in the hinge region of immunoglobulin gamma 1 as a possible cause of degradation during storage Anal. Chem. 15 2011 3857 3864
3. M. Amano, N. Kobayashi, M. Yabuta, S. Uchiyama, and K. Fukui Detection of histidine oxidation in a monoclonal immunoglobulin gamma (IgG) 1 antibody Anal. Chem. 86 2014 7536 7543
4. T. Arakawa, and S.N. Timasheff Stabilization of protein structure by sugars Biochemistry 21 1982 6536 6544
5. T. Arakawa, D. Ejima, Y. Kita, and K. Tsumoto Small molecule pharmacological chaperones: from thermodynamic stabilization to pharmaceutical drugs Biochim. Biophys. Acta 1764 2006 1677 1687
6. H. Bajaj, V.K. Sharma, A. Badkar, D. Zeng, S. Nema, and D.S. Kalonia Protein structural conformation and not second virial coefficient relates to long-term irreversible aggregation of a monoclonal antibody and ovalbumin in solution Pharm. Res. 23 6 Jun 2006 1382 1394
7. R.L. Baldwin How Hofmeister ion interactions affect protein stability Biophys. J. 71 4 Oct 1996 2056 2063 (ssv.)
8. A. Bertolotti-Ciarlet, W. Wang, R. Lownes, P. Pristatsky, Y. Fang, T. McKelvey, Y. Li, Y. Li, J. Drummond, T. Prueksaritanont, and J. Vlasak Impact of methionine oxidation on the binding of human IgG1 to Fc Rn and Fc gamma receptors Mol. Immunol. 46 2009 1878 1882
9. S.R. Brych, Y.R. Gokarn, H. Hultgen, R.J. Stevenson, R. Rajan, and M. Matsumura Characterization of antibody aggregation: role of buried, unpaired cysteines in particle formation J. Pharm. Sci. 99 2 Feb 2010 764 781
10. R.K. Brummitt, D.P. Nesta, and C.J. Roberts Predicting accelerated aggregation rates for monoclonal antibody formulations, and challenges for low-temperature predictions J. Pharm. Sci. 100 2011 4234 4243
11. R. Chaudhuri, Y. Cheng, C.R. Middaugh, and D.B. Volkin High-throughput biophysical analysis of protein therapeutics to examine interrelationships between aggregate formation and conformational stability AAPS J. 16 1 2014 48 64
12. E.Y. Chi, S. Krishnan, B.S. Kendrick, B.S. Chang, J.F. Carpenter, and T.W. Randolph Roles of conformational stability and colloidal stability in the aggregation of recombinant human granulocyte colony-stimulating factor Protein Sci. 12 2003 903 913
13. W. Cheng, S.B. Joshi, F. He, D.N. Brems, B. He, and B.A. Kerwin Comparison of high-throughput biophysical methods to identify stabilizing excipients for a model IgG2 monoclonal antibody: conformational stability and kinetic aggregation measurements J. Pharm. Sci. 101 2012 1701 1720
14. B.D. Connolly, C. Petry, S. Yadav, B. Demeule, N. Ciaccio, J.M. Moore, S.J. Shire, and Y.R. Gokarn Weak interactions govern the viscosity of concentrated antibody solutions: high-throughput analysis using the diffusion interaction parameter Biophys. J. 103 1 2012 69 78
15. R.A. Curtis, J.M. Prausnitz, and H.W. Blanch Protein-protein and protein-salt interactions in aqueous protein solutions containing concentrated electrolytes Biotech. Bioeng. 57 1998 11 21
16. D. Ejima, K. Tsumoto, H. Fukada, R. Yumioka, K. Nagase, T. Arakawa, and J.S. Philo Effects of acid exposure on the conformation, stability, and aggregation of monoclonal antibodies Proteins 66 4 Mar 1 2007 954 962
17. A.H. Elcock, and J.A. McCammon Calculation of weak protein-protein interactions: the pH dependence of the second virial coefficient Biophys. J. 80 2 2001 613 625
18. R.M. Fesinmeyer, S. Hogan, A. Saluja, S.R. Brych, E. Kras, L.O. Narhi, D.N. Brems, and Y.R. Gokarn Effect of ions on agitation- and temperature-induced aggregation reactions of antibodies Pharm. Res. 2009 903 913
19. S. Fischer, J. Hoernschemeyer, and H.C. Mahler Glycation during storage and administration of monoclonal antibody formulation Eur. J. Pharm. Biopharm. 70 2008 42 50
20. Y.R. Gokarn, R.M. Fesinmeyer, A. Saluja, S. Cao, J. Dankberg, A. Goetze, R.L. Rammele Jr., L.O. Narhi, and D.N. Brems Ion-specific modulation of protein interactions: anion-induced, reversible oligomerization of a fusion protein Protein Sci. 18 2009 169 179
21. A. Hawe, M. Sutter, and W. Jiskoot Extrinsic fluorescent dyes as tools for protein characterization Pharm. Res. 25 2008 1487 1499
22. F. He, C.E. Woods, G.W. Becker, L.O. Narhi, and V.I. Razinkov High-throughput assessment of thermal and colloidal stability parameters for monoclonal antibody formulations J. Pharm. Sci. 100 2011 5126 5141
23. J.G.S. Ho, A.P.J. Middelberg, P. Ramage, and H.P. Kocher The likelihood of aggregation during protein renaturation can be assessed using the second virial coefficient Protein Sci. 12 2003 708 716
24. C. Hoffmann, A. Blume, I. Miller, and P. Garidel Insights into protein-polysorbate interactions analysed by means of isothermal titration and differential scanning calorimetry Eur. Biophys. J. 38 5 2009 557 568
25. J.L. Jensen, C. Kolvenbach, S. Roy, and C. Schöneich Metal-catalyzed oxidation of brain-derived neurotrophic factor (BDNF): analytical challenges for the identification of modified sites Pharm. Res. 17 2 Feb 2000 190 196
26. M. Jiménez, G. Rivas, and A.P. Minton Quantitative characterization of weak self-association in concentrated solutions of immunoglobulin G via the measurement of sedimentation equilibrium and osmotic pressure Biochemistry 46 2007 8373 8378
27. S. Kanai, J. Liu, T.W. Patapoff, and S.J. Shire Reversible self-association of a concentrated monoclonal antibody solution mediated by Fab-Fab interaction that impacts solution viscosity J. Pharm. Sci. 97 10 Oct 2008 4219 4227
28. J.K. Kaushik, and R. Bhat Why is trehalose an exceptional protein stabilizer? An analysis of the thermal stability of proteins in the presence of the compatible osmolyte trehalose J. Biol. Chem. 278 29 Jul 18 2003 26458 26465
29. B.A. Kerwin Polysorbates 20 and 80 used in the formulation of protein biotherapeutics: structure and degradation pathways J. Pharm. Sci. 97 8 Aug 2008 2924 2935
30. R.S. Kishore, S. Kiese, S. Fischer, A. Pappenberger, U. Grauschopf, and H.C. Mahler The degradation of polysorbates 20 and 80 and its potential impact on the stability of biotherapeutics Pharm. Res. 28 5 2011 1194 1210
31. S. Krishnan, E.Y. Chi, J.N. Webb, B.S. Chang, D. Shan, M. Goldenberg, M.C. Manning, T.W. Randolph, and J.F. Carpenter Aggregation of granulocyte colony stimulating factor under physiological conditions: characterization and thermodynamic inhibition Biochemistry 41 2002 6422 6431
32. V. Kumar, N. Dixit, L. Zhou, and W. Fraunhofer Impact of short range hydrophobic interactions and long range electrostatic forces on the aggregation kinetics of a monoclonal antibody and a dual-variable domain immunoglobulin at low and high concentrations Int. J. Pharm. 421 2011 82 93
33. Tom Laue Proximity energies: a framework for understanding concentrated solutions J. Mol. Recognit. 25 2012 165 173
34. C. Lehermayr, H.C. Mahler, K. Mäder, and S.J. Fischer Assessment of net charge and protein-protein interactions of different monoclonal antibodies Pharm. Sci. 100 2011 2551 2562
35. J.L. Liu, K.V. Lu, T. Eris, V. Katta, K.R. Westcott, L.O. Narhi, and H.S. Lu In vitro methionine oxidation of recombinant human leptin Pharm. Res. 15 1998 632 640
36. D. Liu, D. Ren, H. Huang, J. Dankberg, R. Rosenfeld, M.J. Cocco, L. Li, D.N. Brems, and R.L. Remmele Jr. Biochemistry 47 2008 5088
37. H. Liu, G. Gaza-Bulseco, D. Faldu, C. Chumsae, and J. Sun Heterogeneity of monoclonal antibodies J. Pharm. Sci. 97 2008 2426 2447
38. H. Liu, G. Gaza-Bulseco, D. Faldu, C. Chumsae, and J. Sun Heterogeneity of monoclonal antibodies J. Pharm. Sci. 97 2008 2426 2447
39. R. Lumry, and H. Eyring Conformation changes of proteins J. Phys. Chem. 58 1954 110 120
40. N.R. Maddux, S.B. Joshi, D.B. Volkin, J.P. Ralston, and C.R. Middaugh Multidimensional methods for the formulation of biopharmaceuticals and vaccines J. Pharm. Sci. 100 2011 4171 4197
41. N.R. Maddux, I.T. Rosen, L. Hu, C.M. Olsen, D.B. Volkin, and C.R. Middaugh An improved methodology for multidimensional high-throughput preformulation characterization of protein conformational stability J. Pharm. Sci. 101 2012 2017 2024
42. H.C. Mahler, F. Senner, K. Maeder, and R. Mueller Surface activity of a monoclonal antibody J. Pharm. Sci. 98 12 2009 4525 4533
43. W.G. McMillan Jr., and J.E. Mayer The statistical thermodynamics of multicomponent systems J. Chem. Phys. 13 1945 276 305
44. B.L. Neal, D. Asthagiri, and A.M. Lenhoff Molecular origins of osmotic second virial coefficients of proteins Biophys. J. 75 5 Nov 1998 2469 2477
45. H. Nishi, M. Miyajima, H. Nakagami, M. Noda, S. Uchiyama, and K. Fukui Phase separation of an IgG1 antibody solution under a low ionic strength condition Pharm. Res. 27 7 2010 1348 1360
46. M. Printz, D.S. Kalonia, and W. Friess Individual second virial coefficient determination of monomer and oligomers in heat-stressed protein samples using size-exclusion chromatography-light scattering J. Pharm. Sci. 101 1 Jan 2012 363 372
47. C.H. Ramos, and R.L. Baldwin Sulfate anion stabilization of native ribonuclease A both by anion binding and by the Hofmeister effect Protein Sci. 11 7 Jul 2002 1771 1778
48. R.L. Remmele Jr., J. Zhang-van Enk, V. Dharmavaram, D. Balaban, M. Durst, A. Shoshitaishvili, and H. Rand Scan-rate-dependent melting transitions of interleukin-1 receptor (type II): elucidation of meaningful thermodynamic and kinetic parameters of aggregation acquired from DSC simulations J. Am. Chem. Soc. 127 23 Jun 15 2005 8328 8339
49. C.J. Roberts Non-native protein aggregation kinetics Biotechnol. Bioeng. 98 2007 927 938
50. C.J. Roberts, T.K. Das, and E. Sahin Predicting solution aggregation rates for therapeutic proteins: approaches and challenges Int. J. Pharm. 418 2011 318 333 (2011)
51. J. Rubin, A. San Miguel, A.S. Bommarius, and S.H. Behrens Correlating aggregation kinetics and stationary diffusion in protein-sodium salt systems observed with dynamic light scattering J. Phys. Chem. B 114 12 Apr 1 2010 4383 4387
52. A. Saluja, R.M. Fesinmeyer, S. Hogan, D.N. Brems, and Y.R. Gokarn Diffusion and sedimentation interaction parameters for measuring the second virial coefficient and their utility as predictors of protein aggregation Biophys. J. 99 8 Oct 20 2010 2657 2665
53. A. Saluja, and D.S. Kalonia Nature and consequences of protein-protein interactions in high protein concentration solutions Int. J. Pharm. 358 1-2 2008 1 15
54. S. Saito, J. Hasegawa, N. Kobayashi, N. Kishi, S. Uchiyama, and K. Fukui Behavior of monoclonal antibodies: relation between the second virial coefficient (B (2)) at low concentrations and aggregation propensity and viscosity at high concentrations Pharm. Res. 29 2012 397 410
55. S. Saito, J. Hasegawa, N. Kobayashi, T. Tomitsuka, S. Uchiyama, and K. Fukui Effects of ionic strength and sugars on the aggregation propensity of monoclonal antibodies: influence of colloidal and conformational stabilities Pharm. Res. 30 2013 1263 1280
56. S. Saito Development of a general strategy for formulation optimization of therapeutic monoclonal antibodies Ph.D thesis Prediction of Aggregation Propensity and Viscosity in Terms of Colloidal and Conformational Stabilities 2013 Osaka University
57. J.M. Sanchez-Ruiz Theoretical analysis of Lumry-Eyring models in differential scanning calorimetry Biophys. J. 61 1992 921 935
58. S.N. Telikepalli, O.S. Kumru, C. Kalonia, R. Esfandiary, S.B. Joshi, C.R. Middaugh, and D.B. Volkin Structural characterization of IgG1 mAb aggregates and particles generated under various stress conditions J. Pharm. Sci. 103 3 Mar 2014 796 809
59. P.M. Tessier, A.M. Lenhoff, and S.I. Sandler Rapid measurement of protein osmotic second virial coefficients by self-interaction chromatography Biophys. J. 82 3 Mar 2002 1620 1631
60. P.M. Tessier, J. Jinkoji, Y.C. Cheng, J.L. Prentice, and A.M. Lenhoff Self-interaction nanoparticle spectroscopy: a nanoparticle-based protein interaction assay J. Am. Chem. Soc. 130 10 Mar 12 2008 3106 3112
61. S. Uchiyama, J. Hasegawa, Y. Tanimoto, M. Mizutani, Y. Igarashi, Y. Sambongi, and Y. Kobayashi Thermodynamic characterization for variants of mesophilic cytochrome c and its thermophilic counterpart Protein Eng. 15 2002 455 461
62. S. Uchiyama, A. Ohshima, T. Yoshida, T. Ohkubo, and Y. Kobayashi Thermodynamic assessment of domain-domain interactions and in vitro activities of mesophilic and thermophilic ribosome recycling factors Biopolymers 100 4 Jul 2013 366 379
63. J.J. Valente, R.W. Payne, M.C. Manning, W.W. Wilson, and C.S. Henry Colloidal behavior of proteins: effects of the second virial coefficient on solubility, crystallization and aggregation of proteins in aqueous solution Curr. Pharm. Biotechnol. 6 2005 427 436
64. A.A. Wakankar, J. Liu, D. Vandervelde, Y.J. Wang, S.J. Shire, and R.T. Borchardt The effect of cosolutes on the isomerization of aspartic acid residues and conformational stability in a monoclonal antibody J. Pharm. Sci. 96 7 2007 1708 1718 (Jul)
65. W. Wang, S. Singh, D.L. Zeng, K. King, and S. Nema Antibody structure, instability, and formulation J. Pharm. Sci. 96 2007 1 26
66. W. Wang, and C.J. Roberts Non-Arrhenius protein aggregation AAPS J. 15 2013 840 851
67. S. Yadav, T.M. Laue, D.S. Kalonia, S.N. Singh, and S.J. Shire The influence of charge distribution on self-association and viscosity behavior of monoclonal antibody solutions Mol. Pharm. 9 4 2012 791 802
68. S. Yadav, J. Liu, S.J. Shire, and D.S. Kalonia Specific interactions in high concentration antibody solutions resulting in high viscosity J. Pharm. Sci. 99 3 2010 1152 1168
69. S. Yadav, S.J. Shire, and D.S. Kalonia Factors affecting the viscosity in high concentration solutions of different monoclonal antibodies J. Pharm. Sci. 99 12 2010 4812 4829
70. J. Zhang, and X.Y. Liu Effect of protein-protein interactions on protein aggregation kinetics J. Chem. Phys. 119 20 2003 10972 10976
71. J. Zhang-van Enk, B.D. Mason, L. Yu, L. Zhang, W. Hamouda, G. Huang, D. Liu, R.L. Remmele Jr., and J. Zhang Perturbation of thermal unfolding and aggregation of human IgG1 Fc fragment by Hofmeister anions Mol. Pharm. 10 2 Feb 4 2013 619 630