Fluciclovine (18F)
Fluciclovine (18F) Uses, Dosage, Side Effects, Food Interaction and all others data.
Fluciclovine is a [18F]-tagged synthetic analog of the amino acid L-leucine. It presents excellent diagnostic properties to be used in positron emission tomography (PET) imaging. The structure of fluciclovine allows it to be uptaken by the tumoral cells by its amino acid transporter without incorporating in the metabolism within the body. Fluciclovine was developed by Blue Earth Diagnostics, Ltd. and FDA approved in May 27, 2016.
Following intravenous administration, the tumor-to-normal tissue contrast is highest between 2 and 10 minutes after injection, with a 63% reduction in mean tumor uptake at 90 minutes after injection. The scanning time point should be evaluated carefully as an early scanning can present an increased blood pool and a late scanning will translate into an increased muscle uptake. These variations should always be considered in the image interpretation.
| Trade Name | Fluciclovine (18F) |
| Generic | Fluciclovine (18F) |
| Fluciclovine (18F) Other Names | (18F)FACBC, FACBC F-18, Fluciclovine (18F), Fluciclovine F 18, Fluciclovine F-18 |
| Type | |
| Formula | C5H8FNO2 |
| Weight | Average: 132.125 Monoisotopic: 132.056441169 |
| Protein binding | Pre clinical studies showed that fluciclovine does not bind to plasma proteins. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Fluciclovine (18F) is a radiolabelled L-leucine derivative used to image tumors, especially in the prostate.
Fluciclovine is indicated as a detection agent for positron emission tomography (PET) in men with suspected prostate cancer recurrence based on elevated blood prostate specific antigen (PSA) levels following prior treatment. The overexpression of L-type amino acid transporters such as LAT1 and LAT3 that mediate the uptake of essential amino acids has been extensively reported as a tumoral mechanism of cell growth.
Fluciclovine (18F) is also used to associated treatment for these conditions: Prostate Cancer
How Fluciclovine (18F) works
Fluciclovine is transported into the prostate cancer cells via ASCT2 and LAT1 transporters. The activity of LAT1 gets increased in acidic pH, condition that is developed intra-tumorally at certain size. The uptake of fluciclovine presents an androgen-dependent dynamic in hormone sensitive cells.
Toxicity
The hasn't been long-term carcinogenity or fertility studies in animals. Even though all reports have shown no mutagenicity, fluciclovine has the potential to be mutagenic.
Food Interaction
No interactions found.Volume of Distribution
The compartmental volume of distribution of fluciclovine is in prostate 0.97 L, vesicle 0.79 L, red bone marrow 0.98 L, gluteus muscle 2.13 L and obturator muscle 2.23 L.
Elimination Route
After intravenous administration of fluciclovine, the major distribution happens in liver (14%), red bone marrow (12%), lung (7%), myocardium (4%) and pancreas (3%). With increasing time, the dose gets distributed into skeletal muscle.
Half Life
Fluciclovine is a cyclotron produced radionuclide that decays by positron emission (ß+ decay, 96.7%) and orbital electron capture (3.3%) to stable oxygen 18 with a physical half-life of 109.7 minutes.
Clearance
Fluciclovine renal clearance and excretion is minimal.
Elimination Route
In the first four hours post-injection, 3% of administered dose is excreted in the urine which increases to 5% after 24 hours post-injection.
Innovators Monograph
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