Fluciclovine (18F)

Absorption

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.

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.

Background

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.

Indications

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.

Definition

ChEBI: Fluciclovine ((18)F) is a member of the class of cyclobutanes that is cyclobutane which carries a carboxy, amino and ((18)F)fluoro groups at positions 1, 1 and 3, respectively (the 1r,3r-stereoisomer). It is a positron emission tomography (PET) radiotracer for visualizing prostate cancer. It has a role as a radioactive imaging agent. It is a (18)F radiopharmaceutical, an alpha-amino acid, a member of cyclobutanes, a fluoroamino acid, a monocarboxylic acid and a primary amino compound.

Pharmacokinetics

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.

Metabolism

Fluciclovine is not metabolized and it is not incorporated into newly synthesized proteins.