Pharmacokinetics and disposition of CS-0777, a sphingosine 1-phosphate receptor modulator, in rats and monkeys

References

• Akabane T, Gerst N, Masters JN, Tamura K. (2012). A quantitative approach to hepatic clearance prediction of metabolism by aldehyde oxidase using custom pooled hepatocytes. Xenobiotica 42:863–71
   PubMed Web of Science ®Google Scholar
• Brinkmann V, Pinschewer DD, Feng L, Chen S. (2001). FTY720: altered lymphocyte traffic results in allograft protection. Transplantation 72:764–9
   PubMed Web of Science ®Google Scholar
• Brinkmann V, Davis MD, Heise CE, et al. (2002). The immune modulator FTY720 targets sphingosine 1-phosphate receptors. J Biol Chem 277:21453–7
   PubMed Web of Science ®Google Scholar
• Cheng H, Jusko WJ. (1993). Pharmacokinetics of reversible metabolic systems. Biopharm Drug Dispos 14:721–66
   PubMed Web of Science ®Google Scholar
• Chiba K, Yanagawa Y, Masubuchi Y, et al. (1998). 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 160:5037–44
   PubMed Web of Science ®Google Scholar
• Cohen JA, Barkhof F, Comi G, et al. (2010). Oral fingolimod or intramuscular interferon for relapsing multiple sclerosis. N Engl J Med 362:402–15
   PubMed Web of Science ®Google Scholar
• Davis B, Morris T. (1993). Physiological parameters in laboratory animals and humans. Pharm Res 10:1093–5
   PubMed Web of Science ®Google Scholar
• Delplanque J, Delpierre G, Opperdoes FR, Schaftingen EV. (2004). Tissue distribution and evolution of fructosamine 3-kinase and fructosamine 3-kinase-related protein. J Biol Chem 279:46606–13
   PubMed Web of Science ®Google Scholar
• Fujino M, Funeshima N, Kitazawa Y, et al. (2003). Amelioration of experimental autoimmune encephalomyelitis in Lewis rats by FTY720 treatment. J Pharmacol Exp Ther 305:70–7
   PubMed Web of Science ®Google Scholar
• Hla T, Lee M-J, Ancellin N, et al. (2001). Lysophospholipids – receptor revelations. Science 294:1875–8
   PubMed Web of Science ®Google Scholar
• Kappos L, Radue E-W, O’Connor P, et al. (2010). A placebo-controlled trial of oral fingolimod in relapsing multiple sclerosis. N Engl J Med 362:382–401
   PubMedGoogle Scholar
• Kilford PJ, Stringer R, Sohal B, et al. (2009). Prediction of drug clearance by glucuronidation from in vitro data: use of combined cytochrome P450 and UDP-glucuronosyltransferase cofactors in alamethicin-activated human liver microsomes. Drug Metab Disops 37:82–9
   PubMed Web of Science ®Google Scholar
• Kovarik JM, Dole K, Riviere G-J, et al. (2009). Ketoconazole increases fingolimod blood levels in a drug interaction via CYP4F2 inhibition. J Clin Pharmacol 49:212–18
   PubMed Web of Science ®Google Scholar
• Liu X, Zhang QH, Yi GH. (2012). Regulation of metabolism and transport of sphingosine-1-phosphate in mammalian cells. Mol Cell Biochem 363:21–33
   PubMed Web of Science ®Google Scholar
• Mandala S, Hajdu R, Bergstorm J, et al. (2002). Alteration of lymphocyte trafficking by sphingosine-1-phosphate receptor agonists. Science 296:346–9
   PubMed Web of Science ®Google Scholar
• Matloubian M, Lo CG, Cinamon G, et al. (2004). Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor 1. Nature 427:355–60
   PubMed Web of Science ®Google Scholar
• Mechtcheriakova D, Wlachos A, Sobanov J, et al. (2007). FTY720-phosphate is dephosphorylated by lipid phosphate phosphatase 3. FEBS Lett 581:3063–8
   PubMed Web of Science ®Google Scholar
• Moberly JB, Rohatagi S, Zahir H, et al. (2012a). Pharmacological modulation of peripheral T and B lymphocytes by a selective sphingosine 1-phosphate receptor-1 modulator. J Clin Pharmacol 52:996–1006
   PubMed Web of Science ®Google Scholar
• Moberly JB, Ford DM, Zahir H, et al. (2012b). Pharmacological effects of CS-0777, a selective sphingosine 1-phosphate receptor-1 modulator: results from a 12-week, open-label pilot study in multiple sclerosis patients. J Neuroim 246:100–7
   PubMed Web of Science ®Google Scholar
• Nakai D, Kumamoto K, Sakikawa C, et al. (2004). Evaluation of the protein binding ratio of drugs by a micro-scale ultracentrifugation method. J Pharm Sci 93:847–54
   PubMed Web of Science ®Google Scholar
• Nishi T, Miyazaki S, Takemoto T, et al. (2011). Discovery of CS-0777: a potent, selective, and orally active S1P1 agent. ACS Med Chem Lett 2:368–72
   PubMed Web of Science ®Google Scholar
• O’Connor P, Comi G, Montalban X, et al. (2009). Oral fingolimod (FTY720) in multiple sclerosis: two-year results of a phase II extension study. Neurology 72:73–9
   PubMed Web of Science ®Google Scholar
• Paugh SW, Payne SG, Barbour SE, et al. (2003). The immunosuppressant FTY720 is phosphorylated by sphingosine kinase type 2. FEBS Lett 554:189–93
   PubMed Web of Science ®Google Scholar
• Poulin P, Hop CECA, Ho Q, et al. (2012). Comparative assessment of in vitro-in vivo extrapolation methods used for predicting hepatic metabolic clearance of drugs. J Pharm Sci 101:4308–26
   PubMed Web of Science ®Google Scholar
• Rohatagi S, Zahir H, Moberly JB, et al. (2009). Use of an exposure-response model to aid early drug development of an oral sphingosine 1-phosphate receptor modulator. J Clin Pharm 49:50–62
   PubMed Web of Science ®Google Scholar
• Sakurai H, Kubota K, Inaba S, et al. (2013). Identification of a metabolizing enzyme in human kidney by proteomic correlation profiling. Mol Cell Proteomics 12:2313–23
   PubMed Web of Science ®Google Scholar
• Van Hoof VO, De Broe ME. (1994). Interpretation and clinical significance of alkaline phosphatase isoenzyme patterns. Clin Rev Clin Lab Sci 31:197–293
   PubMed Web of Science ®Google Scholar
• Yamanaka M, Anada Y, Igarashi Y, Kihara A. (2008). A splicing isoform of LPP1, LPP1a, exhibits high phosphatase activity toward FTY720 phosphate. Biochem Biophys Res Commun 375:675–9
   PubMed Web of Science ®Google Scholar
• Yonesu K, Kubota K, Tamura M, et al. (2011). Purification and identification of activating enzymes of CS-0777, a selective sphingosine 1-phosphate receptor 1 modulator, in erythrocytes. J Biol Chem 286:24765–75
   PubMed Web of Science ®Google Scholar
• Zollinger M, Gschwind HP, Jin Y, et al. (2011). Absorption and disposition of the sphingosine 1-phosphate receptor modulator fingolimod (FTY720) in healthy volunteers: a case of xenobiotic biotransformation following endogenous metabolic pathways. Drug Metab Dispos 39:199–207
   PubMed Web of Science ®Google Scholar