The evolution of thalidomide and its IMiD derivatives as anticancer agents

Nature Reviews Cancer

Volumn 4, Issue 4, 2004, Pages 314-322

  Bartlett, J Blake ^b   Dredge, Keith ^a   Dalgleish, Angus G ^a  

^a ST GEORGE'S UNIVERSITY OF LONDON   (United Kingdom)

^b CELGENE CORPORATION   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 (4 AMINO 1,3 DIHYDRO 1,3 DIOXO 2H ISOINDOL 2 YL)GLUTARIMIDE; CYCLOPHOSPHAMIDE; DEXAMETHASONE; IMMUNOMODULATING AGENT; LENALIDOMIDE; THALIDOMIDE; THALIDOMIDE DERIVATIVE; TUMOR NECROSIS FACTOR ALPHA;

ANTIANGIOGENIC ACTIVITY; ANTIINFLAMMATORY ACTIVITY; ANTINEOPLASTIC ACTIVITY; AUTOIMMUNE DISEASE; BIRTH DEFECT; CLINICAL TRIAL; DISEASE SEVERITY; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; DRUG SCREENING; HUMAN; IMMUNOMODULATION; INHIBITION KINETICS; LYMPHOCYTE ACTIVATION; MONOCYTE; MULTIPLE MYELOMA; NEUROPATHY; NONHUMAN; PRIORITY JOURNAL; REVIEW; T LYMPHOCYTE; TERATOGENICITY;

EID: 1942534043     PISSN: 1474175X     EISSN: None     Source Type: Journal    
DOI: 10.1038/nrc1323     Document Type: Review

References (57)

1. McBride, W. G. Thalidomide and congenital abnormalities. Lancet 2, 1358 (1961).
2. Lenz, W. Thalidomide and congenital abnormalities. Lancet 1, 45 (1961).
3. Fullerton, P. M. & Kremer, M. Neuropathy after intake of thalidomide. Br. Med. J. 2, 855-858 (1961).
4. Sheskin, J. Thalidomide in the treatment of lepra reactions. Clin. Pharmacol. Ther. 6, 303-306 (1965).
5. Iyer, G. C. et al. WHO co-ordinated short-term double-blind trial with thalidomide in the treatment of acute lepra reactions in male lepromatous patients. Bull. World Health Organ. 45, 719-732 (1971).
6. Marriott, J. B., Muller, G. & Dalgleish, A. G. Thalidomide as an emerging immunotherapeutic agent. Immunol. Today 583, 538-540 (1999).
7. Raje, N. & Anderson, K. Thalidomide - a revival story. N. Engl. J. Med. 341, 1606-1609 (1999).
8. Hales, B. Thalidomide on the comeback trail. Nature Med. 5, 489-490 (1999).
9. Sampaio, E. P. et al. The influence of thalidomide on the clinical and immunologic manifestation of erythema nodosum leprosum. J. Infect. Dis. 168, 408-414 (1993).
10. Gutierrez-Roddguez, O. Thalidomide. A promising new treatment for rheumatoid arthritis. Arthritis Rheum. 27, 1118-1121 (1984).
11. Atra, E. & Sato, E. I. Treatment of the cutaneous lesions of systemic lupus erythematosus with thalidomide. Clin. Exp. Rheumatol. 11, 487-493 (1993).
12. Hamza, M. H. Treatment of Behcet's disease with thalidomide. Clin. Rheumatol. 5, 365-371 (1986).
13. McCarthy, D. M., Kanfer, E. J. & Barrett, A. J. Thalidomide for the therapy of graft-versus-host disease following allogeneic bone marrow transplantation. Biomed. Pharmacother. 43, 693-697 (1989).
14. Heney, D. et al. Thalidomide treatment for chronic graft-versus-host disease. Br. J. Hematol. 78, 23-27 (1991).
15. Vogelsang, G. B. et al. Thalidomide for the treatment of chronic graft-versus-host disease. N. Engl. J. Med. 326, 1055-1058 (1992).
16. Sampaio, E. P., Sarno, E. N., Galilly, R., Cohn, Z. A. & Kaplan, G. Thalidomide selectively inhibits tumour necrosis factor α production by stimulated human monocytes. J. Exp. Med. 173, 699-703 (1991).
17. Lokensgard, J. R. et al. Effect of thalidomide on chemokine production by human microglia. J. Infect. Dis. 182, 983-987 (2000).
18. Deng, L., Ding, W. & Granstein, R. D. Thalidomide inhibits tumour necrosis factor-α production and antigen presentation by langerhans cells. J. Invest. Dermatol. 121, 1060-1065 (2003).
19. Szlosarek, P. W. & Balkwill, F. R. Tumour necrosis factor α: a potential target for the therapy of solid tumours. Lancet Oncol. 4, 565-573 (2003).
20. Wettstein, A. R. & Meagher, A. P. Thalidomide in Crohn's disease. Lancet 350, 1445-1446 (1997).
21. D'Amato, R. J., Loughnan, M. S., Flynn, E. & Folkman, J. Thalidomide is an inhibitor of angiogenesis. Proc. Natl Acad. Sci. 91, 4082-4085 (1994).
22. Tabin, C. J. A developmental model for thalidomide defects. Nature 396, 322-323 (1998).
23. Parman, T., Wiley, M. J. & Wells, P. G. Free radical-mediated oxidative DNA damage in the mechanism of thalidomide teratogenicity. Nature Med. 5, 582-585 (1999).
24. + subset. J. Exp. Med. 187, 1885-1892 (1998).
25. Moller, D. R. et al. Inhibition of IL-12 production by thalidomide. J. Immunol. 159, 5157-5161 (1997).
26. Wolkenstein, P. et al. Randomised comparison of thalidomide versus placebo in toxic epidermal necrolysis. Lancet 352, 1586-1589 (1998).
27. 3 in the disruption of the tumour vasculature induced by TNF and IFN-γ. Nature Med. 4, 408-414 (1998).
28. Singhal, S. et al. Antitumour activity of thalidomide in refractory multiple myeloma. N. Engl. J. Med. 341, 1565-1571 (1999).
29. Kumar, S. et al. Effect of thalidomide therapy on bone marrow angiogenesis in multiple myeloma. Leukemia 18, 624-627 (2004).
30. Juliusson, G. et al. Frequent good partial remissions from thalidomide including best response ever in patients with advanced refractory and relapsed myeloma. Br. J. Hematol. 109, 89-96 (2000).
31. Weber, D. Thalidomide and its derivatives: new promise for multiple myeloma. Cancer Control 10, 375-382 (2003).
32. Garcia-Sanz, R. et al. The oral combination of thalidomide, cyclophosphamide and dexamethasone (ThaCyDex) is effective in relapsed/refractory multiple myeloma. Leukemia 19 Feb 2004 (doi: 10.1038/sj.leu.2403322).
33. Stebbing, J. et al. The treatment of advanced renal cell cancer patients with high dose oral thalidomide. Brit. J. Cancer 85, 953-958 (2001).
34. Gordon, R. et al. Current status of thalidomide and its role in the treatment of metastatic prostate cancer. Crit. Rev. Oncol. Hematol. 46, S49-S57 (2003).
35. Fine, H. A. et al. Phase II trial of the antiangiogenic agent thalidomide in patients with recurrent high grade gliomas. J. Clin. Oncol. 18, 708-715 (2000).
36. Eisen, T. et al. Continuous low dose thalidomide: a phase II study in advanced melanoma, renal cell, ovarian and breast cancer. Br. J. Cancer 82, 812-817 (2000).
37. Fanelli, M. et al. Thalidomide: a new anticancer drug? Exp. Opin. Investig. Drugs 12, 1211-1225 (2003).
38. Kumar, S., Witzig, T. E. & Rajkumar, S. V. Thalidomide as an anti-cancer agent. J. Cell. Mol. Med. 6, 160-174 (2002).
39. Marriott, J. B., Muller, G. W., Stirling, D. & Dalgleish, A. G. Immunotherapeutic and anti-tumour potential of thalidomide analogues. Exp. Opin. Biol. Ther. 1, 675-682 (2001).
40. Muller, G. W. et al. Structural modifications of thalidomide produce analogs with enhanced tumour necrosis factor inhibitory activity. J. Med. Chem. 39, 3238-3240 (1996).
41. Marriott, J. B. et al. CC-3052: a water soluble analog of thalidomide and potent inhibitor of activation-induced TNF-α production. J. Immunol. 161, 4236-4243 (1998).
42. Muller, G. W. et al. Amino-substituted thalidomide analogs: potent inhibitors of TNF-α production. Bioorg. Med. Chem. Lett. 9, 1625-1630 (1999).
43. Lentzsch, S. et al. S-3-Amino-phthalimido-glutarimide inhibits angiogenesis and growth of B-cell neoplasias in mice. Cancer Res. 62, 2300-2305 (2002).
44. Dredge, K. et al. Potent anti-angiogenic activity across distinct classes of thalidomide analogues is independent of immunomodulatory activity. Br. J. Cancer 87, 1166-1172 (2002).
45. + T cells. Clin. Exp. Immunol. 130, 75-84 (2002).
46. LeBlanc, R. et al. Immunomodulatory drug costimulates T cells via the B7-CD28 pathway. Blood 103, 1787-1790 (2004).
47. Schafer, P. H. et al. Enhancement of cytokine production and AP-1 transcriptional activity in T Cells by thalidomide-related immunomodulatory drugs. J. Pharmacol. Exp. Ther. 305, 1222-1232 (2003).
48. Dredge, K. et al. Protective anti-tumour immunity induced by a costimulatory thalidomide analogue in an autologous vaccination model of colorectal cancer is mediated by increased Th1-type immunity. J. Immunol. 168, 4914-4919 (2002).
49. Davies, F. E. et al. Thalidomide and immunomodulatory derivatives augment natural killer cell cytotoxicity in multiple myeloma. Blood 98, 210-216 (2001).
50. Hideshima, T. et al. Thalidomide and its analogs overcome drug resistance of human multiple myeloma cells to conventional therapy. Blood 96, 2943-2950 (2000).
51. Hideshima, T. & Anderson, K. C. Molecular mechanisms of novel therapeutic approaches for multiple myeloma. Nature Rev. Cancer 2, 927-937 (2002).
52. Mitsiades, N. et al. Apoptotic signalling induced by immunomodulatory thalidomide analogues in human multiple myeloma cells: therapeutic implications. Blood 99, 4525-4530 (2002).
53. Gupta, D. et al. Adherence of multiple myeloma cells to bone marrow stromal cells upregulates vascular endothelial growth factor secretion: therapeutic applications. Leukemia 15, 1950-1961 (2001).
54. Richardson, P. G. et al. Immunomodulatory drug CC-5013 overcomes drug resistance and is well tolerated in patients with relapsed multiple myeloma. Blood 100, 3063-3067 (2002).
55. Bartlett, J. B. et al. A phase 1 study to determine the safety, tolerability and immunostimulatory activity of thalidomide analogue CC-5013 in patients with metastatic malignant melanoma and other advanced cancers. Br. J. Cancer 90, 955-961 (2004).
56. Schey, S. A., Jones, R. W., Raj, K. & Streetley M. A phase I study of an immunomodulatory drug (CC-4047), a structural analogue of thalidomide, in relapsed/refractory multiple myeloma. Exp. Hematol. 30, 280 (2002).
57. Eigler, A., Sinha, B., Hartmann, G. & Endres S. Taming TNF: strategies to restrain this proinflammatory cytokine. Immunol. Today 18, 487-492 (1997).