The DOI matches its Crossref record; 55 of the 55 references it cites were found in a registry or an index.
Ozanimod (RPC1063) is a potent sphingosine‐1‐phosphate receptor‐1 (S1P 1 ) and receptor‐5 (S1P 5 ) agonist with autoimmune disease‐modifying activity
Open accessAbstract
Background and Purpose: Sphingosine1‐phosphate (S1P) receptors mediate multiple events including lymphocyte trafficking, cardiac function, and endothelial barrier integrity. Stimulation of S1P 1 receptors sequesters lymphocyte subsets in peripheral lymphoid organs, preventing their trafficking to inflamed tissue sites, modulating immunity. Targeting S1P receptors for treating autoimmune disease has been established in clinical studies with the non‐selective S1P modulator, FTY720 (fingolimod, Gilenya™). The purpose of this study was to assess RPC1063 for its therapeutic utility in autoimmune diseases. Experimental Approach: The specificity and potency of RPC1063 (ozanimod) was evaluated for all five S1P receptors, and its effect on cell surface S1P 1 receptor expression, was characterized in vitro . The oral pharmacokinetic (PK) parameters and pharmacodynamic effects were established in rodents, and its activity in three models of autoimmune disease (experimental autoimmune encephalitis, 2,4,6‐trinitrobenzenesulfonic acid colitis and CD4 + CD45RB hi T cell adoptive transfer colitis) was assessed. Key Results: RPC1063 was specific for S1P 1 and S1P 5 receptors, induced S1P 1 receptor internalization and induced a reversible reduction in circulating B and CCR7 + T lymphocytes in vivo . RPC1063 showed high oral bioavailability and volume of distribution, and a circulatory half‐life that supports once daily dosing. Oral RPC1063 reduced inflammation and disease parameters in all three autoimmune disease models. Conclusions and Implications: S1P receptor selectivity, favourable PK properties and efficacy in three distinct disease models supports the clinical development of RPC1063 for the treatment of relapsing multiple sclerosis and inflammatory bowel disease, differentiates RPC1063 from other S1P receptor agonists, and could result in improved safety outcomes in the clinic.
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Cites
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Cited by
Targeting sphingosine-1-phosphate signaling in immune-mediated diseases: beyond multiple sclerosis
Pérez-Jeldres, T., Alvarez-Lobos, M., & Rivera-Nieves, J. (2021) · Drugs · doi:10.1007/s40265-021-01528-8 · Cited by 197
Next generation of small molecules in inflammatory bowel disease
Olivera, P., Danese, S., & Peyrin-Biroulet, L. (2017) · Gut · doi:10.1136/gutjnl-2016-312912 · Cited by 154
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Structural basis for receptor selectivity and inverse agonism in S1P5 receptors
Lyapina, E., Marin, E., Gusach, A., Orekhov, P., Gerasimov, A., Luginina, A., Vakhrameev, D., Ergasheva, M., Kovaleva, M., Khusainov, G., et al. (2022) · Nature Communications · doi:10.1038/s41467-022-32447-1 · Cited by 26
Metadata
- Authors
- Scott, F. L., Clemons, B., Brooks, J., Brahmachary, E., Powell, R., Dedman, H., Desale, H. G., Timony, G. A., Martinborough, E., Rosen, H., Roberts, E., Boehm, M. F., & Peach, R. J.
- Venue
- British Journal of Pharmacology
- Publisher
- Wiley
- Published
- 2016-04-28
- Volume
- 173
- Issue
- 11
- Pages
- 1778-1792
- ISSN
- 0007-1188 (ISSN-L)
- 1476-5381
- OpenAlex
- W2299774205
- Cited by
- 308
- References
- 55
- FWCI
- 9.48
- Type
- journal article
- Language
- en
- Open access
- bronze
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- CoChat. (2026). Citation check: Ozanimod (RPC1063) is a potent sphingosine‐1‐phosphate receptor‐1 (S1P 1 ) and receptor‐5 (S1P 5 ) agonist with autoimmune disease‐modifying activity. https://app.cochat.ai/papers/10.1111/bph.13476
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- Scott, F. L., Clemons, B., Brooks, J., Brahmachary, E., Powell, R., Dedman, H., Desale, H. G., Timony, G. A., Martinborough, E., Rosen, H., Roberts, E., Boehm, M. F., & Peach, R. J. (2016). Ozanimod (RPC1063) is a potent sphingosine‐1‐phosphate receptor‐1 (S1P 1 ) and receptor‐5 (S1P 5 ) agonist with autoimmune disease‐modifying activity. British Journal of Pharmacology. https://doi.org/10.1111/bph.13476
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