FTY720, a new class of immunomodulator, inhibits lymphocyte egress from secondary lymphoid tissues and thymus by agonistic activity at sphingosine 1-phosphate receptors

Pharmacology and Therapeutics

Volumn 108, Issue 3, 2005, Pages 308-319

  Chiba, Kenji ^a,b  

^a MITSUBISHI TANABE PHARMA CORPORATION   (Japan)

^b NONE   (Japan)

Author keywords

FTY720; Immunosuppression; Lymphocyte egress; S1P1; Sphingosine 1 phosphate

Indexed keywords

2 AMINO 2 [2 (4 OCTYLPHENYL)ETHYL] 1,3 PROPANEDIOL HYDROCHLORIDE PHOSPHATE; AZATHIOPRINE; CALCINEURIN INHIBITOR; CD4 ANTIGEN; CYCLOSPORIN A; FINGOLIMOD; IMMUNOMODULATING AGENT; MYCOPHENOLIC ACID 2 MORPHOLINOETHYL ESTER; PREDNISOLONE; RECOMBINANT BETA INTERFERON; SPHINGOSINE 1 PHOSPHATE RECEPTOR; TACROLIMUS; THERMOZYMOCIDIN; UNCLASSIFIED DRUG;

ALLERGIC ENCEPHALOMYELITIS; ALLOGRAFT; AUTOIMMUNE DISEASE; B LYMPHOCYTE; CELL INFILTRATION; CELL MIGRATION; CLINICAL TRIAL; DOSE RESPONSE; DOWN REGULATION; DRUG EFFICACY; DRUG POTENCY; DRUG SAFETY; GRAFT REJECTION; GRAFT SURVIVAL; GRAFT VERSUS HOST REACTION; HUMAN; KIDNEY ALLOGRAFT; KIDNEY FUNCTION; KIDNEY GRAFT; LYMPH NODE; LYMPHOCYTE; LYMPHOID TISSUE; MULTIPLE SCLEROSIS; NONHUMAN; PRIORITY JOURNAL; REVIEW; RHEUMATOID ARTHRITIS; SYSTEMIC LUPUS ERYTHEMATOSUS; T LYMPHOCYTE; THYMOCYTE; THYMUS;

ANIMALS; AUTOIMMUNE DISEASES; CALCINEURIN; CLINICAL TRIALS; DISEASE MODELS, ANIMAL; DRUG SYNERGISM; GRAFT VS HOST DISEASE; HUMANS; IMMUNOSUPPRESSIVE AGENTS; LYMPH NODES; LYMPHOCYTES; PEYER'S PATCHES; PROPYLENE GLYCOLS; RECEPTORS, LYSOSPHINGOLIPID; SPHINGOSINE; SPLEEN; T-LYMPHOCYTES; THYMUS GLAND;

EID: 28044462458     PISSN: 01637258     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.pharmthera.2005.05.002     Document Type: Review

References (52)

1. K. Adachi, T. Kohara, N. Nakao, M. Arita, K. Chiba, and T. Mishina Design, synthesis and structure-activity relationships of 2-substituted-2-amino- 1.3-propanediols: discovery of a novel immunosuppressant, FTY720 Biomed Chem Lett 5 1995 853 856
2. V. Brinkmann, and K.R. Lynch FTY720: target G-protein-coupled receptors for sphingosine 1-phosphate in transplantation and autoimmunity Curr Opin Immunol 14 2002 569 575
3. V. Brinkmann, D. Pinschewer, K. Chiba, and L. Feng FTY720: a novel transplantation drug that modulates lymphocyte traffic rather than activation Trends Pharmacol Sci 21 2000 49 52
4. V. Brinkmann, M.D. Davis, C.E. Heise, R. Albert, S. Cottens, and R. Hof The immune modulator FTY720 targets sphingosine 1-phosphate receptors J Biol Chem 277 2002 21453 21457
5. V. Brinkmann, J.G. Cyster, and T. Hla FTY720: sphingosine 1-phosphate receptor-1 in the control of lymphocyte egress and endotherial barrier function Am J Transplant 4 2004 1019 1025
6. K. Budde, R.L. Schmouder, R. Brunkhorst, B. Nashan, P.W. Luker, and T. Mayer Fuman first trail of FTY720, a novel immunomodulator, in stable renal transplant patients J Am Soc Nephrol 13 2002 1073 1083
7. K. Budde, R.L. Schmouder, B. Nashan, R. Brunkhorst, P.W. Luker, and T. Mayer Pharmacodynamics of single doses of the novel immunosuppressant FTY720 in stable renal transplant patients Am J Transplant 3 2003 846 854
8. K. Chiba, and K. Adachi FTY720, immunosuppressant Drugs Future 22 1997 18 22
9. K. Chiba, Y. Hoshino, C. Suzuki, Y. Masubuchi, Y. Yanagawa, and M. Ohtsuki FTY720, a novel immunosuppressant possessing unique mechanisms: I. Prolongation of skin allograft survival and synergistic effect in combination with cyclosporin A in rats Transplant Proc 28 1996 1056 1059
10. K. Chiba, Y. Yanagawa, Y. Masubuchi, H. Kataoka, T. Kawaguchi, and M. Ohtsuki FTY720, a novel immunosuppressant, induces sequestration of circulating mature-lymphocytes by acceleration of lymphocyte homing in rats: I. FTY720 selectively decreases the number of circulating mature lymphocytes by acceleration of lymphocyte homing J Immunol 160 1998 5037 5044
11. K. Chiba, Y. Yanagawa, H. Kataoka, T. Kawaguchi, M. Ohtsuki, and Y. Hoshino FTY720, a novel immunosuppressant, induces sequestration of circulating lymphocytes by acceleration of lymphocyte homing Transplant Proc 31 1999 1230 1233
12. K. Chiba, Y. Hoshino, M. Ohtsuki, H. Kataoka, Y. Maeda, and K. Matsuyuki Immunosuppressive activity of FTY720, sphingosine 1-phosphate receptor agonist: I. Prevention of allograft rejection in rats and dogs by FTY720 and FTY720-phosphate Transplant Proc 37 2005 102 106
13. M. Fujino, N. Funeshima, Y. Kitazawa, H. Kimura, H. Amemiya, and S. Suzuki Amelioration of experimental autoimmune encephalomyelitis in Lewis rats by FTY720 treatment J Pharmacol Exp Ther 305 2003 70 77
14. T. Fujita, K. Inoue, S. Yamamoto, T. Ikumoto, S. Sasaki, and R. Toyama Fungal metabolites: Part 11. A potent immunosuppressive activity found in Isaria sinclairii metabolite J Antibiotics 47 1994 208 215
15. T. Fujita, K. Inoue, S. Yamamoto, T. Ikumoto, S. Sasaki, and R. Toyama Fungal metabolites: Part 12. Potent immunosuppressant, 14-deoxomyruiocin, (2S,3R,4R)-(E)-2-amino-3,4-dihydroxy-2-hydroxymethyleicos-6-enoic acid and structure-activity relationships of myriocin derivatives J Antibiotics 47 1994 216 224
16. T. Fujita, M. Yoneta, R. Hirose, S. Sasaki, K. Inoue, and M. Kiuchi Simple compounds, 2-alkyl-2-amino-1,3-propane-diols have potent immunosuppressive activity Biomed Chem Lett 5 1995 847 852
17. T. Fujita, R. Hirose, M. Yoneta, S. Sasaki, K. Inoue, and M. Kiuchi Potent immunosuppressants, 2-alkyl-2-aminopropane-1, 3-diols J Med Chem 39 1996 4451 4459
18. M.H. Graler, and E.J. Goetzl The immunosuppressant FTY720 down-regulates sphingosine 1-phosphate G-protein-coupled receptors FASEB J 18 2004 551 553
19. R. Hirose, N. Hamamichi, Y. Kitao, T. Matsuzaki, K. Chiba, and T. Fujita 2-Aminoalcohol immunosuppressants: structure-activity relationships Biomed Chem Lett 6 1996 2647 2650
20. T. Hla, M.J. Lee, N. Ancellin, J.H. Paik, and M.J. Kluk Lysophospholipids-receptor revelations Science 294 2001 1875 1878
21. Y. Hoshino, C. Suzuki, M. Ohtsuki, Y. Masubuchi, Y. Amano, and K. Chiba FTY720, a novel immunosuppressant possessing unique mechanisms: II. Long-term graft survival induction in rat hetrotopic cardiac allograft and synergistic effect in combination with cyclosporin A Transplant Proc 28 1996 1060 1061
22. Y. Hoshino, Y. Yanagawa, M. Ohtsuki, S. Nakayama, T. Hashimoto, and K. Chiba FTY720, a novel immunosuppressant, shows a synergistic effect in combination with FK506 in rat allograft models Transplant Proc 31 1999 1224 1226
23. B.D. Kahan, J.L. Karlix, R.M. Ferguson, A.B. Leichtman, S. Mulgaonkar, and T.A. Gonwa Pharmacodynamics, pharmacokinetics, and safety of multiple doses of FTY720 in stable renal transplant patients: a multicenter, randomized, placebo-controlled, phase I study Transplantation 76 2003 1079 1084
24. H. Kataoka, K. Sugahara, H. Tanaka, M. Ohtsuki, Y. Maeda, and M. Murata The therapeutic effect of FTY720 on experimental autoimmune encephalomyelitis in mice Immunology 2004 2004 87 89
25. H. Kataoka, M. Ohtsuki, K. Shimano, S. Mochizuki, K. Oshita, and M. Murata Immunosuppressive activity of FTY720, sphingosine 1-phosphate receptor agonist: II. Effect of FTY720 and FTY720-phosphate on host-versus-graft and graft-versus-host reaction in mice Transplant Proc 37 2005 107 109
26. T. Kawaguchi, Y. Hoshino, F. Rahman, Y. Amano, H. Higashi, and H. Kataoka FTY720, a novel immunosuppressant possessing unique mechanisms: III. Synergistic prolongation of canine renal allograft survival in combination with cyclosporin A Transplant Proc 28 1996 1062 1063
27. Y. Kimura, K. Sato, A. Kuwabara, H. Tomura, M. Ishikawa, and I. Kobayashi Sphingosine 1-phosphate may be a major component of plasma lipoproteins responsible for the cytoprotective actions in human umbilical vein endotherial cells J Biol Chem 276 2001 31780 31785
28. M. Kiuchi, K. Adachi, T. Kohara, M. Minoguchi, T. Hanano, and Y. Aoki Synthesis and immunosuppressive activity of 2-substituted 2-aminopropane-1,3- diols and 2-aminoethanols J Med Chem 43 2000 2946 2961
29. M. Kiuchi, K. Adachi, A. Tomatsu, M. Chino, S. Takeda, and Y. Tanaka Asymmetric synthesis and biological evaluation of the enantiomeric isomer of immunosuppressive FTY720-phosphate Bioorg Med Chem 13 2005 425 432
30. H. Li, G.L. Meno-Tetang, K. Chiba, N. Arima, P. Heinig, and W.L. Jusko Pharmacokinetics and cell trafficking dynamics of 2-amino-2-[2-(4-octylphenyl) ethyl]propane-1,3-diol hydrochloride (FTY720) in cynomolgus monkeys after single oral and intravenous doses J Pharmacol Exp Ther 301 2002 519 526
31. C.G. Lo, Y. Xu, R. Proia, and J.G. Cyster Cyclical modulation of sphingosine-1-phosphate receptor 1 surface expression during lymphocyte recirculation and relationship to lymphoid organ transit J Exp Med 201 2005 291 301
32. S. Mandala, R. Hajdu, J. Bergstrom, E. Quackenbush, J. Xie, and J. Milligan Alteration of lymphocyte trafficking by sphingosine-1-phosphate receptor agonists Science 296 2002 346 349
33. Y. Masubuchi, T. Kawaguchi, M. Ohtsuki, C. Suzuki, Y. Amano, and Y. Hoshino FTY720, a novel immunosuppressant possessing unique mechanisms: IV. Prevention of graft versus host reactions in rats Transplant Proc 28 1996 1064 1065
34. M. Matloubian, C.G. Lo, G. Cinamon, M.J. Lesneski, Y. Xu, and V. Brinkmann Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor 1 Nature 427 2004 355 360
35. M. Matsuura, T. Imayoshi, K. Chiba, and T. Okumoto Effect of FTY720, a novel immunosuppressant, on adjuvant-induced arthritis in rats Inflamm Res 49 2000 404 410
36. M. Matsuura, T. Imayoshi, and T. Okumoto Effect of FTY720, a novel imunosuppressant, on adjuvant- and collagen-induced arthritis in rats Int J Immunopharmacol 22 2000 323 331
37. H. Okazaki, D. Hirata, T. Kamimura, H. Sato, M. Iwamoto, and T. Yoshio Effect of FTY720 in MRL-lpr/lpr mice: therapeutic potential in systemic lupus erythematosus J Rheumatol 29 2002 707 716
38. S.W. Paugh, S.G. Payne, S.E. Barbour, S. Milstien, and S. Spiegel The immunosuppressant FTY720 is phosphorylated by sphingosine kinase type 2 FEBS Lett 554 2003 189 193
39. S. Pyne, and N. Pyne Sphingosine 1 phosphate signaling via the endotherial differentiation gene family of G-protein-coupled receptors Pharmacol Ther 88 2000 115 131
40. S. Sasaki, R. Hashimoto, M. Kiuchi, K. Inoue, T. Ikumoto, and R. Hirose Fungal metabolites: Part 14. Novel potent immunosuppressants, mycestericins, produced by Mycelia sterilia J Antibiot 47 1994 420 433
41. K. Sugahara, H. Kataoka, M. Ohtsuki, Y. Hoshino, and K. Chiba The therapeutic effect of FTY720 on lupus nephritis in aoutoimmune MRL/lpr mice Immunology 2004 2004 271 274
42. S. Suzuki, S. Enosawa, T. Kakefuda, T. Shinomiya, M. Amari, and S. Naoe A novel immunosuppressant, FTY720, having an unique mechanism of action induces long-term graft acceptance in rat and dog allotransplantation Transplantation 61 1996 200 205
43. S. Suzuki, X.-K. Li, S. Enosawa, and T. Shinomiya A new immunosuppressant, FTY720 induces bcl-2-associated apoptotic cell death in human lymphocytes Immunology 89 1996 518
44. S. Suzuki, T. Kakefuda, H. Amemiya, K. Chiba, Y. Hoshino, and T. Kawaguchi An immunosuppressive regime using FTY720 combined with cyclosporin in canine kidney transplantation Transpl Int 11 1998 95 101
45. H. Tedesco-Silva, G. Mourad, B.D. Kahan, J.G. Boira, W. Weimar, and S. Mulgaonkar FTY720, a novel immunomodulator: efficacy and safety results from the first phase 2a study in de novo renal transplantation Transplantation 77 2004 1826 1833
46. K. Teshima, T. Imayoshi, M. Matsuura, S. Yamaguchi, K. Chiba, and M. Terasawa FTY720, a novel immunosuppressant, possessing unique mechanisms: III. Pharmacological activities in several autoimmune and inflammatory models Int Congr Immunol 9 1995 864 (No.5126)
47. P. Troncoso, S.M. Stepkowski, M.-E. Wang, X. Qu, S.-C. Chueh, and J. Clark Prophylaxis of acute renal allograft rejection using FTY720 in combination with subtherapeutic doses of cyclosporine Transplantation 67 1999 145 151
48. H. Yagi, R. Kamba, K. Chiba, H. Soga, K. Yaguchi, and M. Nakamura Immunosuppressant FTY720 inhibits thymocyte emigration Eur J Immunol 30 2000 1435 1444
49. Y. Yanagawa, K. Sugahara, H. Kataoka, T. Kawaguchi, Y. Masubuchi, and K. Chiba FTY720, a novel immunosuppressant, induces sequestration of circulating mature lymphocytes by acceleration of lymphocyte homing in rats: II. FTY720 prolongs skin allograft survival by preventing infiltration of T cells into the grafts, but not production of cytokines in vivo J Immunol 160 1998 5493 5499
50. Y. Yanagawa, Y. Masubuchi, and K. Chiba FTY720, a novel immunosuppressant, induces sequestration of circulating mature lymphocytes by acceleration of lymphocyte homing in rats: III. Increase in frequency of CD62L-positive T cells in Peyer's patches by FTY720-induced lymphocyte homing Immunology 95 1998 591 594
51. Y. Yanagawa, Y. Hoshino, H. Kataoka, T. Kawaguchi, M. Ohtsuki, and K. Sugahara FTY720, a novel immunosuppressant, prolongs rat skin allograft survival by decreasing T cell infiltration into grafts Transplant Proc 31 1999 1227 1229
52. Y. Yanagawa, Y. Hoshino, and K. Chiba The significance of timing of FTY720 administration on the immunosuppressive effect to prolong rat skin allograft survival Int J Immunopharmacol 22 2000 597 602