1. (18f)ge-148
2. (1r,3r)-1-amino-3(18f)fluorocyclobutane-1-carboxylic Acid
3. 1-amino-3-fluorocyclobutane-1-carboxylic Acid
4. Anti-(18f)facbc
5. Axumin
6. Cyclobutanecarboxylic Acid, 1-amino-3-(fluoro-18f)-, Trans-
7. F(18)-facbc
8. F(18)1-amino-3-fluorocyclobutane-1-carboxylic Acid
9. F-facbc
10. Fluciclovine F 18
11. Fluciclovine F-18
12. Ge-148 (18f)
13. Ge-148 F-18
14. Nmk 36
15. Nmk-36
16. Nmk36 Cpd
1. Fluciclovine F-18
2. Axumin
3. 222727-39-1
4. Fluciclovine F 18
5. Facbc
6. Fluciclovine F18
7. Nmk36
8. Ge-148
9. (18f)fluciclovine
10. Fluciclovine (18f) [inn]
11. Nmk-36
12. (18f)ge-148
13. Ge-148 F-18
14. Ge-148 (18f)
15. (18f)facbc
16. Facbc F-18
17. 38r1q0l1ze
18. Anti-1-amino-3-(18f)fluorocyclobutane-1-carboxylic Acid
19. (1r,3r)-1-amino-3(18f)fluorocyclobutane-1-carboxylic Acid
20. [18f]fluciclovine
21. [18f]facbc
22. Fluciclovine (18f) (inn)
23. 1-amino-3-(18f)fluoranylcyclobutane-1-carboxylic Acid
24. Cyclobutanecarboxylic Acid, 1-amino-3-(fluoro-18f)-, Trans-
25. Anti-(18f)fabc
26. Fluciclovine F18 [usan]
27. Anti-1-amino-3-[18f]fluorocyclobutane-1-carboxylic Acid
28. Unii-38r1q0l1ze
29. Fluciclovine ((sup 18)f)
30. Fluciclovine-f18
31. Moli001120
32. Fluciclovine ((sup 18)f) [inn]
33. Axumin (tn)
34. Nmk36 Cpd
35. Anti-[18f]facbc
36. Syn-3-[18f]facbc
37. Fluciclovine F-18 (usan)
38. Chembl254468
39. Chembl447701
40. Nmk 36
41. Schembl10017245
42. Schembl11939897
43. Schembl11939900
44. Chebi:134703
45. Dtxsid601027796
46. Fluciclovine (18f) [mi]
47. Fluciclovine F 18 [usan]
48. Bcp24384
49. Axumincn Facbccn Fluciclovine (18f)cn Ge 148cn Nmk 36
50. At31246
51. Db13146
52. Fluciclovine (18f) [who-dd]
53. Fluciclovine F-18 [orange Book]
54. D10860
55. F(18)1-amino-3-fluorocyclobutane-1-carboxylic Acid
56. Q25313613
57. Syn-1-amino-3-[18f]fluorocyclobutane-1-carboxylic Acid
58. Anti-3[18f] Facbc;f18; Anti-1-amino-3-18f-fluorocyclobutane-1-carboxylic Acid (facbc)
| Molecular Weight | 132.12 g/mol |
|---|---|
| Molecular Formula | C5H8FNO2 |
| XLogP3 | -2.6 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 4 |
| Rotatable Bond Count | 1 |
| Exact Mass | 132.056441 g/mol |
| Monoisotopic Mass | 132.056441 g/mol |
| Topological Polar Surface Area | 63.3 Ų |
| Heavy Atom Count | 9 |
| Formal Charge | 0 |
| Complexity | 142 |
| Isotope Atom Count | 1 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently Bonded Unit Count | 1 |
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.
FDA Label
This medicinal product is for diagnostic use only.
Axumin is indicated for Positron Emission Tomography (PET) imaging to detect recurrence of prostate cancer in adult men with a suspected recurrence based on elevated blood prostate specific antigen (PSA) levels after primary curative treatment.
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.
V09IX12
V - Various
V09 - Diagnostic radiopharmaceuticals
V09I - Tumour detection
V09IX - Other diagnostic radiopharmaceuticals for tumour detection
V09IX12 - 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.
Route of Elimination
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.
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.
Clearance
Fluciclovine renal clearance and excretion is minimal.
Fluciclovine is not metabolized and it is not incorporated into newly synthesized proteins.
Fluciclovine is a cyclotron produced radionuclide that decays by positron emission (+ decay, 96.7%) and orbital electron capture (3.3%) to stable oxygen 18 with a physical half-life of 109.7 minutes.
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.
