Drug intelligence / Profile preview

[11C]CS1P1

Development stage
Phase 2
Lead developer
Washington University School of Medicine
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

[11C]CS1P1 is a novel positron emission tomography (PET) radiotracer designed for the selective imaging of sphingosine-1-phosphate receptor 1 (S1PR1), a receptor implicated in neuroinflammatory and autoimmune diseases such as multiple sclerosis. Chemically, it is a fluorine-containing ligand labeled with carbon-11. [11C]CS1P1 binds S1PR1 with high specificity and selectivity, enabling visualization and quantification of S1PR1 expression in the central nervous system. Its favorable safety and biodistribution profiles have been demonstrated in Phase 1 healthy volunteer studies, where no significant adverse events were observed and brain uptake of the tracer correlated with known S1PR1 expression. The compound’s non-radioactive major plasma metabolite (N-oxide, TZ82121) does not cross the blood-brain barrier, ensuring PET imaging results are not confounded by radiolabeled metabolites. The tracer is intended for research and clinical investigation of neuroinflammation, particularly as a biomarker tool in multiple sclerosis and potentially other inflammatory disorders[1][2][3][4][5].

Other names
3-((2-fluoro-4-(5-(2'-methyl-2-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1,2,4-oxadiazol-3-yl)benzyl)(methyl-11C)amino)propanoic acid
02

Targets

EDG1 (Sphingosine-1-phosphate receptors)

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