Drug intelligence / Profile preview

fluciclovine F-18 + methionine C-11

Development stage
Unknown
Lead developer
Blue Earth Diagnostics
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

fluciclovine F-18 + methionine C-11 refers to a combination of positron emission tomography (PET) radiopharmaceuticals utilized in clinical research at Memorial Sloan Kettering Cancer Center for the diagnostic imaging of brain tumors. Fluciclovine F-18 (also known as FACBC) is a synthetic, non-metabolized amino acid analogue that is transported into cells primarily via the ASCT2 and LAT1 amino acid transporters, which are frequently overexpressed in malignant glioma cells. Methionine C-11 is a radiolabeled version of the essential amino acid methionine, which serves as a marker for amino acid transport and protein synthesis. In the context of brain cancer, these tracers are used to differentiate recurrent tumor tissue from post-treatment effects (such as radiation necrosis) by exploiting the increased metabolic demand and transporter activity of cancer cells. Clinical studies have compared these two agents to evaluate their relative sensitivity and tumor-to-background contrast, with fluciclovine F-18 often demonstrating superior contrast due to minimal uptake in healthy brain tissue.

Other names
18F-fluciclovine11C-METL-[methyl-11C]methionine1-amino-3-[18F]fluorocyclobutane-1-carboxylic acid
02

Targets

SLC1A5 (Alanine/serine/cysteine transporter 2)SLC7A5 (Large neutral amino acid transporter small subunit 1)SLC6A19 (Na+-dependent system B0 transporter)

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