Preclinical studies on insulin lispro

Drugs of Today

Volumn 34, Issue SUPPL. C, 1998, Pages 11-21

  Llewelyn, Julie ^a   Slieker, Lawrence J ^a   Zimmermann, John L ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

DNA; GLUCOSE; HUMAN INSULIN; INSULIN; INSULIN DERIVATIVE; INSULIN LISPRO; INSULIN RECEPTOR; SOMATOMEDIN C RECEPTOR;

BIOEQUIVALENCE; CARDIOVASCULAR EFFECT; CELL GROWTH; DISSOCIATION; DRUG MECHANISM; DRUG POTENCY; DRUG RECEPTOR BINDING; FERTILITY; HEART MUSCLE; HUMAN; HYPOGLYCEMIA; IMMUNOGENICITY; MUTAGENICITY; NONHUMAN; REVIEW; SMOOTH MUSCLE; SUBCUTANEOUS DRUG ADMINISTRATION; TOXICITY;

EID: 0031864008     PISSN: 16993993     EISSN: 16994019     Source Type: Journal    
DOI: None     Document Type: Review

References (50)

1. Chance, R.E., Frank, B.H., Radziuk, J.M., DiMarchi, R.D. Discovery and development of insulin lispro. Drugs Today 1998, 34 (Suppl. C): 1-9.
2. DiMarchi, R.D., Mayer, J.P., Fan, L. et al. Synthesis of a fast acting insulin based on structural homology with insulin-like growth factor I. In: Peptides: Chemistry and Biology. Proceedings of the 12th American Peptide Symposium. Smith, J.A., Rivier, J.E. (Eds.)- ESCOM: Leiden 1992, 26-8.
3. Long, H.B., Baker, J.C., Belagaje, R.M. et al. Human insulin analogues with rapid onset and short duration of action. In: Peptides: Chemistry and Biology. Proceedings of the 12th American Peptide Symposium. Smith, J.A., Rivier, J.E. (Eds.). ESCOM: Leiden 1992, 88-90.
4. Brems, D.N., Alter, L.A., Beckage, M.J. et al. Altering the association properties of insulin by amino acid replacement. Protein Eng 1992, 5: 527-33.
5. B29-human insulin. Structure 1995, 3: 615-22.
6. B29-insulin: Dissociation of a protein-ligand complex. Protein Sci 1996, 5: 2521-31.
7. B29-insulin hexamers: A comparison study. Pharm Res 1997, 14: 25-36.
8. Zimmermann, J. Subchronic and chronic toxicity, and mutagenicity studies con ducted with LysPro [Lys(B28), Pro(B29)] human insulin analog. LY275585. 15th Int Diabetes Fed Cong (Nov 6-11, Kobe) 1994, 123.
9. Buelke-Sam, J., Byrd, R.A., Hoyt, J.A., Zimmermann, J.L. A reproductive and developmental toxicity study in CD rats of LY275585, [Lys(B28), Pro(B29)]-human insulin. J Am Coll Toxicol 1994, 13: 247-60.
10. Zimmermann, J. A 12-month chronic toxicity study of LY275585 (human insulin analog) administered subcutaneously to Fischer 344 rats. Diabetes 1994, 43 (Suppl. 1): 166A.
11. Zimmermann, J.L., Truex, L.L. A 12-month chronic toxicity study of LY275585 (human insulin analog) administered subcutaneously to Fischer 344 rats. Int J Toxicol 1997, 16: 639-57.
12. Heath, W.F., Belagaje, R.M., Brooke, G.S. et al. (A-C-B) human proinsulin, a novel insulin agonist and intermediate in the synthesis of biosynthetic human insulin. J Biol Chem 1992, 267: 419-25.
13. Shaw, W., Su, K.S.E. Biological aspects of a new human insulin analog: [Lys(B28), Pro(B29)]-human insulin. Diabetes 1991, 40 (Suppl. 1): 464A.
14. Shaw, W.N. Hypoglycemic activity of [Lys(B28), Pro(B29)] human insulin (LY275585) in rats. Unpublished report on file at Lilly Research Laboratories, Preclinical Pharmacology Report No. 2, 1994.
15. British Pharmacopoeia 1980, Volume II. Appendix XIV, C10 & C11. Her Majesty's Stationery Office: London 1980.
16. Chance, R.E., Farid, N.A. Comparison of [Lys(B28), Pro(B29)]-human insulin analog (rDNA) (LY275585) with biosynthetic human insulin in rabbit hypoglycemia tests. Unpublished report on file at Lilly Research Laboratories, Preclinical Pharmacology Report No. 3, 1994.
17. Galloway, J.A., Chance, R.E., Su, K.S.E. Human insulin and its modifications. In: The Clinical Pharmacology of Biotechnology Products. Reidenberg, M.M. (Ed.). Elsevier: Amsterdam 1991, 23-34.
18. Su, K.S., Campanale, K.M., Chance. R.E., Hoffmann, J.A. Using dog model for comparing time action of insulins after subcutaneous (s.c.) injection: [Lys(B28). Pro(B29)]-human insulin. Pharm Res 1994, 11: S-357.
19. Radziuk, J., Davies, J., Pye, S., DiMarchi, R., Shields, J., Chance, R. Subcutaneous absorption of fast-acting insulin analogs: Kinetics and bioeffectiveness. Diabetologia 1992, 35 (Suppl. 1): A3.
20. B29-human insulin - assessed in a conscious pig model. Diabetes 1997, 46: 548-56.
21. Howey, D.C., Bowsher, R.R., Brunelle, R.L., Woodworth, J.R. [Lys(B28), Pro(B29)]-human insulin: A rapidly absorbed analogue of human insulin. Diabetes 1994, 43: 396-402.
22. Howey, D.C., Bowsher, R.R., Brunelle, R.L. et al. [Lys(B28), Pro(B29)]-human insulin: Effect of injection time on post-prandial glycemia. Clin Pharmacol Ther 1995, 58: 459-69.
23. Heinemann, L., Woodworth, J.R. Pharmacokinetics and glucodynamics of insulin lispro. Drugs Today 1998, 34 (Suppl. C): 23-36.
24. Slieker, L.J., Sundell, K. Modifications in the 28-29 position of the insulin B-chain alter binding to the IGF-I receptor with minimal effect on insulin receptor binding. Diabetes 1991, 40 (Suppl. 1): 168A.
25. Slieker, L.J., Brooke, G.S., Chance, R.E. et al. Insulin and IGF-I analogs: Novel approaches to improved insulin pharmacokinetics. In: Peptides - Biology and Chemistry. Proceedings of the 1992 Chinese Peptide Symposium. Du, Y.-C., Tam, J.P., Zhang, Y.-S. (Eds.). ESCOM: Leiden 1993, 7-10.
26. Slieker, L.J., Brooke, G.S., Chance, R.E. et al. Insulin and IGF-I analogs: Novel approaches to improved insulin pharma cokinetics. In: Current Directions in Insulin-Like Growth Factor Research. LeRoith, D., Raizada, M.K. (Eds.). Plenum Press: New York 1994, 25-32.
27. Sheker, L.J., Brooke, G.S., DiMarchi, R.D. et al. Modifications in the B10 and B26-30 regions of the B chain of human insulin alter affinity for the human IGF-I receptor more than for the insulin receptor. Diabetologia 1997, 40 (Suppl. 2): S54-61.
28. Brange, J., Owens, D.R., Kang, S., Vølund, A. Monomeric insulins and their experimental and clinical implications. Diabetes Care 1990, 13 : 923-54.
29. Schwartz, G.P., Burke, G.T., Katsoyannis, P.G. A superactive insulin: [B10-aspartic acid] insulin (human). Proc Natl Acad Sci USA 1987, 84: 6408-11.
30. Drejer, K. The bioactivity of insulin analogues from in vitro receptor binding to in vivo glucose uptake. Diabetes Metab Rev 1992, 8: 259-86.
31. Dideriksen, L.H., Jørgensen, L.N., Drejer, K. Carcinogenic effect on female rats after 12 months administration of insulin analogue 810 Asp. Diabetes 1992, 41 (Suppl. 1): 143A.
32. Jørgensen, L.N., Dideriksen, L.H., Drejer. K. Carcinogenic effect of the human insulin analogue B10 Asp in female rats. Diabetologia 1992, 35 (Suppl. 1): A3.
33. Jørgensen, L.N., Dideriksen, L.H. Preclinical studies of rapid-acting insulin analogues. In: Frontiers in Insulin Pharmacology. Berger, M., Gries, F.A. (Eds.). Thieme Medical Publishers: New York 1993, 110-17.
34. De Meyts, P., Christoffersen, C.T., Ish-Shalom, D. et al. Enhanced mitogenic potency of insulin analogues in a cell line devoid of IGF-I receptors correlates with slow dissociation from insulin receptors. Diabetes 1993, 42 (Suppl. 1): 163A.
35. De Meyts, P. The structural basis of insulin and insulin-like growth factor-1 receptor binding and negative co-operativity, and its relevance to mitogenic versus metabolic signalling. Diabetologia 1994, 37 (Suppl. 2): S135-48.
36. Danielsen, G., Lundemose, A., Hansen, B.F., Sorensen, A., Drejer, K. Early signalling events of insulin analogs. Eur J Endocrinol 1995, 132 (Suppl. 1): 8.
37. Lundemose, A.G., Hansen, B.F., Danielsen, G., Sørensen, A.R., Drejer, K. Molecular actions on insulin analogues. In: Diabetes 1994. Baba, S., Kaneko, T. (Eds.). Elsevier: Amsterdam 1995, 469-72.
38. Berti, L., Bossenmaier, B., Kellerer, M., Setter, E., Seipke, G., Häring, H. Comparison of the human insulin analogs HOE 901 and ASP(B10): Characteristics of receptor binding, activation and tyrosine phosphorylation of different substrate proteins. Diabetologia 1995, 38 (Suppl. 1): A191.
39. Hansen, B.F., Danielsen, G.M., Drejer, K. et al. Sustained signalling from the insulin receptor after stimulation with insulin analogues exhibiting increased mitogenic potency. Biochem J 1996, 315: 271-9.
40. Liu, L., Koenen, M., Seipke, G., Eckel, J. IGF-I receptor-mediated signalling of the human insulin analogue HOE 901. Diabetologia 1997, 40 (Suppl. 1): A355.
41. Drejer, K., Kruse, V., Larsen, U.D., Hougaard, P., Bjorn, S., Gammeltoft, S. Receptor binding and tyrosine kinase activation by insulin analogues with extreme affinities in human hepatoma HepG2 cells. Diabetes 1991, 40: 1488-95.
42. Hamel, F.G., Siford, G.L., Frank, B.H., Chance, R.E., Duckworth, W.C. B10-Asp insulin (B10) is resistant to metabolism by hepatocytes and insulin degrading enzyme (IDE). Diabetes 1997, 46 (Suppl. 1): 204A.
43. B29-human insulin. Submitted for publication.
44. Somwar, R., Ramlal, T., Klip, A. The cellular responses of L6 cells to insulin lispro are similar to those of regular human insulin. Celebrating the Discovery of Insulin: An International Research Symposium on Diabetes. (Oct 6-9, Toronto) 1996, 42.
45. Somwar, R., Sweeney, G., Ramlal, T., Klip, A. Stimulation of glucose and amino acid transport and activation of the insulin signalling pathways by insulin lispro in L6 skeletal muscle cells. Clin Ther 1998, 20: 125-40.
46. Slieker, L.J., Sundell, K.L. In vitro analysis of Lys(B28). Pro (B29) human insulin (LY275585): Comparison to human insulin in terms of insulin and IGF-I receptor binding, glucose uptake into adipocytes and thymidine incorporation into smooth muscle cells. Unpublished report on file at Lilly Research Laboratories, Preclinical Pharmacology Report No. 7, 1994.
47. Bornfeldt, K.E., Gidlof, R.A., Wasteson, A., Lake, M., Skottner, A., Arnqvist, H.J. Binding and biological effects of insulin, insulin analogues and insulin-like growth factors in rat aortic smooth muscle cells: Comparison of maximal growth promoting activities. Diabetologia 1991, 34: 307-13.
48. Helton, D.R., Zimmermann, J.L., Heim, A., Jones, T.W., Turk, J.A., Kallman, M.J. General pharmacology of insulin lispro in animals. Arzneim-Forsch/Drug Res 1996, 46: 91-7.
49. Data on file, Eli Lilly and Company. NDA No. 20-563. Application Summary 2.E. Nonclinical pharmacology and toxicology summary, 1995, 61-81.
50. Zwickl, C.M., Smith, H.W., Zimmermann. J.L., Wierda, D. Immunogenicity of biosynthetic human LysPro insulin compared to native-sequence human and purified porcine insulins in rhesus monkeys immunized over a 6-week period. Arzneim-Forsch/Drug Res 1995, 45: 524-8.