Fluciclovine (18F)
Chemical compound
From Wikipedia, the free encyclopedia
Fluciclovine (18F), also known as anti-1-amino-3-18F-fluorocyclobutane-1-carboxylic acid (anti-3[18F] FACBC),[3][4] and sold under the brand name Axumin, is a diagnostic agent used for positron emission tomography (PET) imaging in men with suspected prostate cancer recurrence based on elevated prostate specific antigen (PSA) levels.[5][6]
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| Trade names | Axumin |
| AHFS/Drugs.com | Micromedex Detailed Consumer Information |
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| Formula | C5H818FNO2 |
| Molar mass | 132.12 g·mol−1 |
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Background
Most imaging tests have not been able to localize recurrent prostate cancer when the PSA is mildly increased.[3][5] Axumin scans were compared to [11C]-tagged choline PET scans, another FDA approved PET scan that can assist in this situation, and to biopsy results.[5][7] Fluciclovine tagged PET scans appear to more sensitive than CT scans[8] and to [11C]-tagged choline PET scans.[9][10]
Mechanism
Fluciclovine is a [18F]-tagged synthetic analog of the amino acid L-leucine.[11][12] FACBC uptake by the tumor is related to functional activity of two amino acid transporters,[13] specifically sodium-dependent system ASC, with a lesser contribution by sodium-independent system L.[12] Although it is handled by the amino acid transporter system, it does not undergo terminally incorporative metabolism within the body.[12] The distribution of the tracer in the body differs from choline and FDG, as kidney uptake of FACBC is negligible, and no activity is found in the urinary tract.[12][13] There is low native brain uptake compared to FDG, which may enhance detection of brain metastases[4][12] or primary brain tumors.[12] The more intense native liver and pancreatic uptake seen with this agent would be expected to limit disease detection in those organs.[12] FACBC has a short synthesis time and a long half-life, which eliminate the need for an onsite cyclotron.[13]
Marketing
Axumin is marketed by Blue Earth Diagnostics, Ltd., United Kingdom.[6]