Radiocaine

Radiocaine

Structural formula of Radiocaine
Identifiers
IUPAC name N-(2,6-dimethylphenyl)-2-[ethyl(2-(18F)fluoranylethyl)amino]acetamide
CAS Number	2235413-00-8
PubChem CID	153316836
UNII	KJ6WA6AYC5
Chemical and physical data
Formula	C14H2118FN2O
Molar mass	251.34
3D model (JSmol)	Interactive image
SMILES CCN(CC[18F])CC(=O)NC1=C(C=CC=C1C)C
InChI InChI=InChI=1S/C14H21FN2O/c1-4-17(9-8-15)10-13(18)16-14-11(2)6-5-7-12(14)3/h5-7H,4,8-10H2,1-3H3,(H,16,18)/i15-1 Key:NLNDMDUJSHQLQA-HUYCHCPVSA-N

Radiocaine ([18F]-fluorolidocaine) is a fluorine-18 (¹⁸F) labeled radiotracer designed for positron emission tomography (PET) imaging of voltage-gated sodium channels (NaVs), particularly the SCN5A isoform, which is predominant in cardiac tissue. It is being explored for its potential in diagnosing and monitoring cardiac and neurological diseases through quantification of NaVs. ^{[1] [2]}

Radiocaine is a structural analog of lidocaine, a class Ib antiarrhythmic agent. The only difference is the presence of a fluorine-18 isotope at the terminus of one ethyl chain. ^[1]

Development

Radiocaine was developed to enable non-invasive imaging of NaVs, which play an important role in generating and propagating action potentials in excitable tissues such as the heart and nervous system. It is valuable for studying the SCN5A isoform, the primary voltage-gated sodium channel in the heart, ^[1] and NaVs expressed in peripheral nerves. ^{[2] [3]}

A Phase 1 clinical trial began in June 2025 to evaluate Radiocaine's safety, biodistribution, and radiation dosimetry in healthy volunteers. ^[4]

References

1. Hooker JM, Strebl MG, Schroeder FA, Wey HY, Ambardekar AV, McKinsey TA, et al. (February 2017). "Imaging cardiac SCN5A using the novel F-18 radiotracer radiocaine". Scientific Reports. 7: 42136. Bibcode:2017NatSR...742136H. doi:10.1038/srep42136. PMC   5311962 . PMID   28205593.
2. Bartolo ND, Reid SE, Krishnan HS, Haseki A, Renganathan M, Largent-Milnes TM, et al. (December 2022). "Radiocaine: An Imaging Marker of Neuropathic Injury". ACS Chemical Neuroscience. 13 (24): 3661–3667. doi:10.1021/acschemneuro.2c00717. PMID   36472927.
3. Hascalovici J, Babb A, Norwood BA (December 2023). "Radiotracers in the Diagnosis of Pain: A Mini Review". Seminars in Musculoskeletal Radiology. 27 (6): 655–660. doi:10.1055/s-0043-1775743. PMID   37935212.
4. "Lutroo Imaging Begins Phase 1 Clinical Trial of Radiocaine™, a First-in-Class PET Radiotracer for Pain Imaging and Diagnosis". Lutroo Imaging. 1 July 2025. Retrieved 11 July 2025.