ASP4058, a novel agonist for sphingosine 1-phosphate receptors 1 and 5, ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile

PLoS ONE

Volumn 9, Issue 10, 2014, Pages

  Yamamoto, Rie ^a   Okada, Youhei ^a   Hirose, Jun ^a   Koshika, Tadatsura ^a   Kawato, Yuka ^a   Maeda, Masashi ^a   Saito, Rika ^a   Hattori, Kazuyuki ^a   Harada, Hironori ^a   Nagasaka, Yasuhisa ^a   Morokata, Tatsuaki ^a  

^a ASTELLAS PHARMA INC   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

5 [ 5 [3 (TRIFLUOROMETHYL) 4 [(1,1,1 TRIFLUOROPROPAN 2 YL)OXY]PHENYL] 1,2,4 OXADIAZOL 3 YL] 1H BENZIMIDAZOLE; FINGOLIMOD; GUANINE NUCLEOTIDE BINDING PROTEIN GAMMA SUBUNIT; PROTEIN INHIBITOR; SPHINGOSINE 1 PHOSPHATE RECEPTOR; SPHINGOSINE 1 PHOSPHATE RECEPTOR 1; SPHINGOSINE 1 PHOSPHATE RECEPTOR 5; UNCLASSIFIED DRUG; ASP4058; BENZIMIDAZOLE DERIVATIVE; OXADIAZOLE DERIVATIVE; PROPANEDIOL DERIVATIVE; SPHINGOSINE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BINDING AFFINITY; CARDIOVASCULAR EFFECT; COMPARATIVE EFFECTIVENESS; CONTINUOUS INFUSION; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG DOSE COMPARISON; DRUG EFFICACY; DRUG PROTEIN BINDING; DRUG SAFETY; DRUG STRUCTURE; EXPERIMENTAL AUTOIMMUNE ENCEPHALOMYELITIS; FEMALE; HEART RATE; IMMUNOMODULATION; IN VITRO STUDY; IN VIVO STUDY; LEWIS RAT; LUNG FUNCTION; LYMPHOCYTE COUNT; MALE; NONHUMAN; PERIPHERAL LYMPHOCYTE; RAT; RECURRENT DISEASE; AGONISTS; ANALOGS AND DERIVATIVES; ANIMAL; BLOOD PRESSURE; BRONCHOCONSTRICTION; CELL LINE; DISEASE MODEL; DRUG EFFECTS; ENCEPHALOMYELITIS, AUTOIMMUNE, EXPERIMENTAL; LYMPHOCYTE; METABOLISM; MOUSE;

RODENTIA;

ANIMALS; BENZIMIDAZOLES; BLOOD PRESSURE; BRONCHOCONSTRICTION; CELL LINE; DISEASE MODELS, ANIMAL; ENCEPHALOMYELITIS, AUTOIMMUNE, EXPERIMENTAL; FEMALE; HEART RATE; LYMPHOCYTES; MALE; MICE; OXADIAZOLES; PROPYLENE GLYCOLS; RATS; RECEPTORS, LYSOSPHINGOLIPID; SPHINGOSINE;

EID: 84908568838     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0110819     Document Type: Article

References (34)

1. Compston A, Coles A (2002) Multiple sclerosis. The Lancet 359: 1221-1231.
2. Hemmer B, Nessler S, Zhou D, Kieseier B, Hartung H-P (2006) Immuno-pathogenesis and immunotherapy of multiple sclerosis. Nature Clinical Practice Neurology 2: 201-211.
3. Kennedy PC, Zhu R, Huang T, Tomsig JL, Mathews TP, et al. (2011) Characterization of a sphingosine 1-phosphate receptor antagonist prodrug. J Pharmacol Exp Ther 338: 879-889.
4. Maceyka M, Harikumar KB, Milstien S, Spiegel S (2012) Sphingosine-1-phosphate signaling and its role in disease. Trends in Cell Biology 22: 50-60.
5. Brinkmann V (2007) Sphingosine 1-phosphate receptors in health and disease: Mechanistic insights from gene deletion studies and reverse pharmacology. Pharmacology & Therapeutics 115: 84-105.
6. Schwab SR, Cyster JG (2007) Finding a way out: lymphocyte egress from lymphoid organs. Nat Immunol 8: 1295-1301.
7. Cyster JG, Schwab SR (2012) Sphingosine-1-phosphate and lymphocyte egress from lymphoid organs. Annu Rev Immunol 30: 69-94.
8. Chun J, Brinkmann V (2011) A mechanistically novel, first oral therapy for multiple sclerosis: the development of fingolimod (FTY720, Gilenya). Discov Med 12: 213-228.
9. Brinkmann V (2002) The Immune Modulator FTY720 Targets Sphingosine 1-Phosphate Receptors. Journal of Biological Chemistry 277: 21453-21457.
10. Mandala S (2002) Alteration of Lymphocyte Trafficking by Sphingosine-1-Phosphate Receptor Agonists. Science 296: 346-349.
11. Matloubian M, Lo CG, Cinamon G, Lesneski MJ, Xu Y, et al. (2004) Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor 1. Nature 427: 355-360.
12. Groves A, Kihara Y, Chun J (2013) Fingolimod: Direct CNS effects of sphingosine 1-phosphate (S1P) receptor modulation and implications in multiple sclerosis therapy. Journal of the Neurological Sciences 328: 9-18.
13. Cohen JA, Barkhof F, Comi G, Hartung HP, Khatri BO, et al. (2010) Oral fingolimod or intramuscular interferon for relapsing multiple sclerosis. N Engl J Med 362: 402-415.
14. Kappos L, Antel J, Comi G, Montalban X, O'Connor P, et al. (2006) Oral fingolimod (FTY720) for relapsing multiple sclerosis. N Engl J Med 355: 1124-1140.
15. Kappos L, Radue EW, O'Connor P, Polman C, Hohlfeld R, et al. (2010) A placebo-controlled trial of oral fingolimod in relapsing multiple sclerosis. N Engl J Med 362: 387-401.
16. DiMarco JP, O'Connor P, Cohen JA, Francis G, Collins W, et al. (2010) Firstdose effect of fingolimod: pooled safety data from two phase-3 studies (TRANSFORMS and FREEDOMS) (P830). Mult Scler 16: S290.
17. Forrest M (2004) Immune Cell Regulation and Cardiovascular Effects of Sphingosine 1-Phosphate Receptor Agonists in Rodents Are Mediated via Distinct Receptor Subtypes. Journal of Pharmacology and Experimental Therapeutics 309: 758-768.
18. Trifilieff A, Fozard JR (2012) Sphingosine-1-Phosphate-Induced Airway Hyper-Reactivity in Rodents Is Mediated by the Sphingosine-1-Phosphate Type 3 Receptor. Journal of Pharmacology and Experimental Therapeutics 342: 399-406.
19. Brinkmann V, Billich A, Baumruker T, Heining P, Schmouder R, et al. (2010) Fingolimod (FTY720): discovery and development of an oral drug to treat multiple sclerosis. Nature Reviews Drug Discovery 9: 883-897.
20. Walzer T, Chiossone L, Chaix J, Calver A, Carozzo C, et al. (2007) Natural killer cell trafficking in vivo requires a dedicated sphingosine 1-phosphate receptor. Nat Immunol 8: 1337-1344.
21. Jenne CN, Enders A, Rivera R, Watson SR, Bankovich AJ, et al. (2009) T-bet-dependent S1P5 expression in NK cells promotes egress from lymph nodes and bone marrow. J Exp Med 206: 2469-2481.
22. Zamvil SS, Steinman L (1990) The T lymphocyte in experimental allergic encephalomyelitis. Annu Rev Immunol 8: 579-621.
23. Choi JW, Gardell SE, Herr DR, Rivera R, Lee CW, et al. (2010) FTY720 (fingolimod) efficacy in an animal model of multiple sclerosis requires astrocyte sphingosine 1-phosphate receptor 1 (S1P1) modulation. Proceedings of the National Academy of Sciences 108: 751-756.
24. Miller RH, Mi S (2007) Dissecting demyelination. Nature Neuroscience 10: 1351-1354.
25. Miron VE, Jung CG, Kim HJ, Kennedy TE, Soliven B, et al. (2008) FTY720 modulates human oligodendrocyte progenitor process extension and survival. Annals of Neurology 63: 61-71.
26. Jaillard C (2005) Edg8/S1P5: An Oligodendroglial Receptor with Dual Function on Process Retraction and Cell Survival. Journal of Neuroscience 25: 1459-1469.
27. Miron VE, Hall JA, Kennedy TE, Soliven B, Antel JP (2008) Cyclical and Dose-Dependent Responses of Adult Human Mature Oligodendrocytes to Fingolimod. The American Journal of Pathology 173: 1143-1152.
28. Miron VE, Ludwin SK, Darlington PJ, Jarjour AA, Soliven B, et al. (2010) Fingolimod (FTY720) Enhances Remyelination Following Demyelination of Organotypic Cerebellar Slices. The American Journal of Pathology 176: 2682-2694.
29. Cohen JA, Chun J (2011) Mechanisms of fingolimod's efficacy and adverse effects in multiple sclerosis. Ann Neurol 69: 759-777.
30. Sanna MG (2004) Sphingosine 1-Phosphate (S1P) Receptor Subtypes S1P1 and S1P3, Respectively, Regulate Lymphocyte Recirculation and Heart Rate. Journal of Biological Chemistry 279: 13839-13848.
31. Gergely P, Nuesslein-Hildesheim B, Guerini D, Brinkmann V, Traebert M, et al. (2012) The selective sphingosine 1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate. British Journal of Pharmacology 167: 1035-1047.
32. Kume H, Takeda N, Oguma T, Ito S, Kondo M, et al. (2007) Sphingosine 1-phosphate causes airway hyper-reactivity by rho-mediated myosin phosphatase inactivation. J Pharmacol Exp Ther 320: 766-773.
33. Rosenfeldt HM (2003) Sphingosine-1-phosphate stimulates contraction of human airway smooth muscle cells. The FASEB Journal 17: 1789-1799.
34. Roviezzo F, D'Agostino B, Brancaleone V, De Gruttola L, Bucci M, et al. (2010) Systemic Administration of Sphingosine-1-Phosphate Increases Bronchial Hyperresponsiveness in the Mouse. American Journal of Respiratory Cell and Molecular Biology 42: 572-577.