Peringatan Keamanan

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.L1052

Fluciclovine (18F)

DB13146

small molecule approved

Deskripsi

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.A31384 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.A31385 Fluciclovine was developed by Blue Earth Diagnostics, Ltd. and FDA approved in May 27, 2016.L1049

Struktur Molekul 2D

Berat 132.125
Wujud liquid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (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.[A31383]
Volume Distribusi 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.[A31390]
Klirens (Clearance) Fluciclovine renal clearance and excretion is minimal.[A31390]

Absorpsi

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.L1051

Metabolisme

Fluciclovine is not metabolized and it is not incorporated into newly synthesized proteins.L1051

Rute Eliminasi

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.L1051

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Neutral amino acid transporter B(0) SLC1A5
Y+L amino acid transporter 1 SLC7A7
Cationic amino acid transporter 3 SLC7A3
Glutamate (NMDA) receptor GRIN1
Glutamate receptor 1 GRIA1
Glutamate receptor 2 GRIA2
Glutamate receptor 3 GRIA3
Glutamate receptor 4 GRIA4

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17504867
    Nye JA, Schuster DM, Yu W, Camp VM, Goodman MM, Votaw JR: Biodistribution and radiation dosimetry of the synthetic nonmetabolized amino acid analogue anti-18F-FACBC in humans. J Nucl Med. 2007 Jun;48(6):1017-20. doi: 10.2967/jnumed.107.040097. Epub 2007 May 15.
  • PMID: 17204699
    Schuster DM, Votaw JR, Nieh PT, Yu W, Nye JA, Master V, Bowman FD, Issa MM, Goodman MM: Initial experience with the radiotracer anti-1-amino-3-18F-fluorocyclobutane-1-carboxylic acid with PET/CT in prostate carcinoma. J Nucl Med. 2007 Jan;48(1):56-63.
  • PMID: 24094575
    Schiavina R, Brunocilla E, Martorana G: The new promise of FACBC position emission tomography/computed tomography in the localization of disease relapse after radical treatment for prostate cancer: are we turning to the right radiotracer? Eur Urol. 2014 Jan;65(1):255-6. doi: 10.1016/j.eururo.2013.08.053. Epub 2013 Aug 30.
  • PMID: 27825431
    Schuster DM, Nanni C, Fanti S: PET Tracers Beyond FDG in Prostate Cancer. Semin Nucl Med. 2016 Nov;46(6):507-521. doi: 10.1053/j.semnuclmed.2016.07.005. Epub 2016 Sep 7.
  • PMID: 22007000
    Wang Q, Bailey CG, Ng C, Tiffen J, Thoeng A, Minhas V, Lehman ML, Hendy SC, Buchanan G, Nelson CC, Rasko JE, Holst J: Androgen receptor and nutrient signaling pathways coordinate the demand for increased amino acid transport during prostate cancer progression. Cancer Res. 2011 Dec 15;71(24):7525-36. doi: 10.1158/0008-5472.CAN-11-1821. Epub 2011 Oct 17.
  • PMID: 23208700
    Sorensen J, Owenius R, Lax M, Johansson S: Regional distribution and kinetics of 18Ffluciclovine (anti-18FFACBC), a tracer of amino acid transport, in subjects with primary prostate cancer. Eur J Nucl Med Mol Imaging. 2013 Feb;40(3):394-402. doi: 10.1007/s00259-012-2291-9. Epub 2012 Dec 4.

Contoh Produk & Brand

Produk: 5 • International brands: 0
Produk
  • Axumin
    Injection, solution • 1600 MBq/ml • Intravenous • EU • Approved
  • Axumin
    Injection, solution • 3200 MBq/ml • Intravenous • EU • Approved
  • Axumin
    Injection, solution • 1600 MBq/ml • Intravenous • EU • Approved
  • Axumin
    Injection, solution • 3200 MBq/ml • Intravenous • EU • Approved
  • Axumin
    Injection, solution • 221 mCi/1mL • Intravenous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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