Drug intelligence / Profile preview

[18F]RoSMA-18-d6

Development stage
Phase 1
Lead developer
Roche
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

[18F]-RoSMA-18-d6 is a trisubstituted pyridine-based positron emission tomography (PET) radioligand specifically designed for imaging cannabinoid type 2 (CB2) receptors in living organisms. This radiotracer has demonstrated high binding affinity and selectivity for CB2 receptors, making it valuable for visualizing CB2 receptor expression in various inflammatory conditions. The compound has been successfully tested in rodents and nonhuman primates (NHPs), showing promising results for clinical translation to humans. In vitro and in vivo studies have confirmed its ability to bind specifically to CB2-rich tissues such as the spleen, while showing no specific binding in healthy brain tissue (consistent with the known low expression of CB2 in healthy mammalian brains). Notably, [18F]-RoSMA-18-d6 has shown potential utility in detecting CB2 receptor upregulation in experimental multiple sclerosis (MS) models and may serve as a valuable marker for hematopoietic activity in various pathologies. The deuterated version of this compound (d6) demonstrates improved stability against microsomal degradation compared to its non-deuterated counterpart.

Other names
[18F]RoSMALS4-[18F]Fluorobutyl-2-ethyl-2-[[6-[[(1S,2S)-2-]
02

Targets

CB (Cannabinoid receptors)

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