Metabolism and Disposition of Siponimod, a Novel Selective S1P1/S1P5 Agonist, in Healthy Volunteers and In Vitro Identification of Human Cytochrome P450 Enzymes Involved in Its Oxidative Metabolism.
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Cites background from "Metabolism and Disposition of Sipon..."
...The majority of the metabolites (M3, M5) are excreted through the feces [32]....
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...6 hours though unchanged siponimod was detected in plasma until 480 hours [32]....
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References
2,788 citations
"Metabolism and Disposition of Sipon..." refers background in this paper
...Enzymes of the CYP3A subfamily are the most abundant CYP enzymes in HLMs, although the levels vary enormously (.10-fold) among individuals, whereas CYP3A5 expression is relatively low in HLMs (10%–30% of human livers) (Shimada et al., 1994; Yeo et al., 2004)....
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...10-fold) among individuals, whereas CYP3A5 expression is relatively low in HLMs (10%–30% of human livers) (Shimada et al., 1994; Yeo et al., 2004)....
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2,400 citations
"Metabolism and Disposition of Sipon..." refers background in this paper
...The internalization of S1P1 receptors renders lymphocytes unresponsive to S1P, depriving them of an obligatory signal to egress from the lymph nodes and recirculate into the central nervous system (CNS), subsequently reducing neuroinflammation (Matloubian et al., 2004)....
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2,363 citations
"Metabolism and Disposition of Sipon..." refers methods in this paper
...…receptor modulation in multiple sclerosis treatment has been demonstrated using fingolimod (Gilenya), a functional antagonist of S1P1 receptors (Brinkmann et al., 2002; Baumruker et al., 2007; Cohen et al., 2010;Kappos et al., 2010), and siponimod (Selmaj et al., 2013; Kappos et al., 2016, 2018)....
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2,040 citations
"Metabolism and Disposition of Sipon..." refers methods in this paper
...…receptor modulation in multiple sclerosis treatment has been demonstrated using fingolimod (Gilenya), a functional antagonist of S1P1 receptors (Brinkmann et al., 2002; Baumruker et al., 2007; Cohen et al., 2010;Kappos et al., 2010), and siponimod (Selmaj et al., 2013; Kappos et al., 2016, 2018)....
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1,482 citations
"Metabolism and Disposition of Sipon..." refers background in this paper
...…S1P receptor modulation in multiple sclerosis treatment has been demonstrated using fingolimod (Gilenya), a functional antagonist of S1P1 receptors (Brinkmann et al., 2002; Baumruker et al., 2007; Cohen et al., 2010;Kappos et al., 2010), and siponimod (Selmaj et al., 2013; Kappos et al., 2016,…...
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...S1P signaling pathways play a role in multiple sclerosis pathophysiology, and the therapeutic potential of S1P receptor modulation in multiple sclerosis treatment has been demonstrated using fingolimod (Gilenya), a functional antagonist of S1P1 receptors (Brinkmann et al., 2002; Baumruker et al., 2007; Cohen et al., 2010;Kappos et al., 2010), and siponimod (Selmaj et al....
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