1. FDA, T., FDA final rule, October 15, 1996, published through REGO (under the President's reinventing government) initiative. 1996.

2. Elimination of ELA and PLA requirement, May 14,1996 and replaced by BLA. Federal Register, 1996. 63(147): 40858-71.

3. Daggett, V., Validation of protein-unfolding transition states identified in molecular dynamics simulations. Biochem Soc Symp, 2001(68): 83-93.

4. Galluppi, G.R., M.C. Rogge, L.K. Roskos, L.J. Lesko, M.D. Green, D.W. Feigal, Jr., and C.C. Peck, Integration of pharmacokinetic and pharmacodynamic studies in the discovery, development, and review of protein therapeutic agents: a conference report. Clin Pharmacol Ther, 2001. 69(6): 387-99.

5. Tsutsumi, Y., M. Onda, S. Nagata, B. Lee, R.J. Kreitman, and I. Pastan, Site-specific chemical modification with polyethylene glycol of recombinant immunotoxin anti-Tac(Fv)-PE38 (LMB-2) improves antitumor activity and reduces animal toxicity and immunogenicity. Proc Natl Acad Sci USA,

6. Rosenberg, J.J., S.W. Martin, J.E. Seely, et al., Development of a novel, nonimmunogenic, soluble human TNF receptor type I (sTNFR-I) construct in the baboon. J Appl Physiol,

7. Taylor, P.C., Anti-tumor necrosis factor therapies. Curr Op in Rheumatol, 2001. 13(3): 164-9.

8 Yap, I., and S.H. Chan, A new pre-S containing recombinant hepatitis B vaccine and its effect on non-responders: a preliminary observation. Ann Acad Med Singapore, 1996. 25(1): 120-2.

9. Ho, R.J., B.T. Rouse, and L. Huang, Targetsensitive immunoliposomes as an efficient drug carrier for antiviral activity. J Biol Chem, 1987. 262(29): 13973-8.

10. Cheng, Y.C., E.S. Huang, J.C. Lin, E.C. Mar, J.S. Pagano, G.E. Dutschman, and S.P. Grill, Unique spectrum of activity of 9-[(1,3-dihydroxy-2-propoxy)methyl]-guanine against herpesviruses in vitro and its mode of action against herpes simplex virus type 1. Proc Natl Acad Sci USA, 1983. 80(9): 2767-70.

11. Lotze, M.T., M.C. Custer, and S.A. Rosenberg, Intraperitoneal administration of interleukin-2 in patients with cancer. Arch Surg, 1986. 121(12): 1373-9.

12. Arakawa, T., Y. Kita, and J.F. Carpenter, Protein-solvent interactions in pharmaceutical formulations. Pharm Res, 1991. 8(3): 285-91.

13. Hora, M.S., R.K. Rana, C.L. Wilcox, N.V. Katre, P. Hirtzer, S.N. Wolfe, and J.W. Thomson, Development of a lyophilized formulation of interleukin-2. Dev Biol Stand, 1992. 74: 295-303; discussion 303-6.

14. Arakawa, T., Prestrelski, S.J., Kenny, W.C., Carpenter, J.F., Factors affecting short-term and long term stabilities of proteins. Adv Drug Deliv Rev, 1993.10:1-28.

15. Cleland, J.L., M.F. Powell, and S.J. Shire, The development of stable protein formulations:

a close look at protein aggregation, deami-dation, and oxidation. Crit Rev Ther Drug Carrier Syst, 1993.10(4): 307-77.

16. Wang, W., Lyophilization and development of solid protein pharmaceuticals. International Journal of Pharmaceutics, 2000. 203(1-2): 1-60.

17. Donahue, R.E., E.A. Wang, R.J. Kaufman, L. Foutch, A.C. Leary, J.S. Witek-Giannetti, M. Metzger, R.M. Hewick, D.R. Steinbrink, G. Shaw, and et al., Effects of N-linked carbohydrate on the in vivo properties of human GM-CSF. Cold Spring Harb Symp Quant Biol, 1986. 51 Pt 1: 685-92.

18. Manning, M.C., K. Patel, and R.T. Bor-chardt, Stability of protein pharmaceuticals. Pharm Res, 1989. 6(11): 903-18.

19. Son, K., and C. Kwon, Stabilization of human epidermal growth factor (hEGF) in aqueous formulation. Pharm Res, 1995. 12(3): 451-4.

20. Wang, P.L., and T.P. Johnston, Enhanced stability of two model proteins in an agitated solution environment using poloxamer 407. J Parenter Sci Technol, 1993. 47(4): 183-9.

21. Chen, B.L., T. Arakawa, E. Hsu, L.O. Narhi, T.J. Tressel, and S.L. Chien, Strategies to suppress aggregation of recombinant keratinocyte growth factor during liquid formulation development. J Pharm Sci, 1994. 83(12): 1657-61.

22. Costantino, H.R., K.G. Carrasquillo, R.A. Cordero, M. Mumenthaler, C.C. Hsu, and K. Griebenow, Effect of excipients on the sta bility and structure of lyophilized recombinant human growth hormone. J Pharm Sci, 1998. 87(11): 1412-20.

23. Chang, B.S., R.M. Beauvais, T. Arakawa, L.O. Narhi, A. Dong, D.I. Aparisio, and J.F. Carpenter, Formation of an active dimer during storage of interleukin-1 receptor antagonist in aqueous solution. Biophys J, 1996. 71(6): 3399-406.

24. Prestrelski, S.J., K.A. Pikal, and T. Arakawa, Optimization of lyophilization conditions for recombinant human interleukin-2 by dried-state conformational analysis using Fourier-transform infrared spectroscopy. Pharm Res, 1995.12(9): 1250-9.

25. Strickley, R.G., and B.D. Anderson, Solidstate stability of human insulin. II. Effect of water on reactive intermediate partitioning in lyophiles from pH 2-5 solutions: stabilization against covalent dimer formation. J Pharm Sci, 1997. 86(6): 645-53.

26. Costantino, H.R., J.D. Andya, P.A. Nguyen, N. Dasovich, T.D. Sweeney, S.J. Shire, C.C. Hsu, and Y.F. Maa, Effect of mannitol crystallization on the stability and aerosol performance of a spray-dried pharmaceutical protein, recombinant humanized anti-IgE monoclonal antibody. J Pharm Sci, 1998. 87(11): 1406-11.

27. Unanue, E.R., and B. Benacerrat, Textbook of Immunology, 2nd ed. Williams and Wilkins, Baltimore. 1986.

28. Stein, K.E., Division of Monoclonal Antibodies, CDER/FDA, presented 2122/01.

Part II

0 0

Post a comment