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Drug delivery

Activation of sphingosine 1-phosphate receptor to improve drug delivery across the blood brain barrier (BBB)

Sphingosine 1-phosphate receptor agonists could help improve drug delivery across the BBB. In rat brains, sphingosine 1-phosphate receptor agonists increased BBB penetration of the opioid receptor agonist loperamide and the chemotherapeutic paclitaxel compared with delivering the two compounds without a sphingosine 1-phosphate receptor agonist. In the rat model, the sphingosine 1-phosphate receptor agonists decreased P glycoprotein (Mdr1; Abcb1; P-gp; Cd243)-mediated drug efflux compared with no agonist. Next steps include studies to elucidate the mechanism by which sphingosine 1-phosphate receptor agonists modulate P-gp-mediated drug efflux.
Mitsubishi Tanabe Pharma Corp. and Novartis AG market the sphingosine 1-phosphate receptor agonist Gilenya fingolimod to treat relapsing forms of multiple sclerosis (MS).
At least eight other companies have sphingosine 1-phosphate receptor-targeting compounds in Phase II testing or earlier to treat various diseases.
Loperamide is a generic drug for diarrhea.

SciBX 5(38); doi:10.1038/scibx.2012.1016
Published online Sept. 27, 2012

Unpatented; licensing status not applicable

Cannon, R.E. et al. Proc. Natl. Acad. Sci. USA; published online Sept. 4, 2012;
Contact: Ronald E. Cannon, National Institute of Environmental Health Sciences, National Institutes of Health, Research Triangle Park, N.C.