Radiocaine

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. ↑ 1.0 1.1 1.2 "Imaging cardiac SCN5A using the novel F-18 radiotracer radiocaine". Scientific Reports 7. February 2017. doi:10.1038/srep42136. PMID 28205593. Bibcode: 2017NatSR...742136H.
2. ↑ 2.0 2.1 "Radiocaine: An Imaging Marker of Neuropathic Injury". ACS Chemical Neuroscience 13 (24): 3661–3667. December 2022. doi:10.1021/acschemneuro.2c00717. PMID 36472927.
3. ↑ "Radiotracers in the Diagnosis of Pain: A Mini Review". Seminars in Musculoskeletal Radiology 27 (6): 655–660. December 2023. 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". 1 July 2025. https://www.lutrooimaging.com/lutroo-imaging-begins-phase-1-clinical-trial-of-radiocaine.

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Diagnostic radiopharmaceuticals (ATC: V09)

Central nervous system|

* 99mTc (Exametazime)
* 123I (Ioflupane
* Iofetamine
* Iomazenil)
* 18F (Florbetapir, Flutemetamol)

Skeletal system|

* 99mTc (Medronic acid)

Renal|

* 123I (Sodium iodohippurate)
* 64Cu (Cu-ETS2)

Gastrointestinal/Hepatic|

* 75Se (SeHCAT)

Respiratory system|

* 133Xe
* 81mKr
* 99mTc (99mTc-MAA)

Cardiovascular system|

* 99mTc (Sestamibi
* Tetrofosmin)
* 111In (Imciromab)
* 82Rb (Rubidium chloride)

Inflammation/infection|

* 99mTc (Exametazime
* Sulesomab
* Tilmanocept)
* 111In
* 67Ga

Tumor|

* 99mTc (Arcitumomab
* Votumumab
* Hynic-octreotide)
* 111In (Capromab pendetide
* Satumomab pendetide)
* 125I (Minretumomab)
* 123I / 131I (Iobenguane)
* 18F (Fluciclovine
* Fludeoxyglucose
* Fluoroethyltyrosine
* Sodium fluoride)

Adrenal cortex|

* 123I
* 125I / 131I (Iodocholesterol)

Radionuclides
(including tracers)|

| positron (PET list)|

* 11C ([11C]ME@HAPTHI
* 25B-NBOMe (Cimbi-36)
* Acetate
* Choline
* Carfentanil
* DASB
* DTBZ
* Flumazenil
* Methionine
* N-Methylspiperone
* Pittsburgh compound B
* Raclopride
* Verapamil)
* 13N (Ammonia)
* 15O (Water)
* 18F (Altanserin
* Desmethoxyfallypride
* FMISO
* Fallypride
* Florbetaben
* Florbetapir
* Flubatine
* Fluciclovine
* Fludeoxyglucose (18F) (FDG)-glucose analogue
* Flumazenil
* Fluorocholine
* Fluorodeoxysorbitol (FDS)
* Fluorodopa
* Fluorothymidine F-18
* Fluspidine
* Flutemetamol
* MPPF
* Mefway
* Nifene
* N-Methylspiperone
* FET
* Setoperone)
* 64Cu
* 68Ga
* 82Rb (Rubidium chloride)

|

gamma ray/photon (SPECT/scintigraphy)|

* 51Cr
* 57Co
* 67Ga
* 75Se
* 81mKr
* 99mTc
* 111In
* 123I
* 125I
* 131I
* 133Xe
* 153Sm
* 201Tl

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