Peringatan Keamanan

Toxicity information regarding Flortaucipir F-18 is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as headaches and increased blood pressure. Symptomatic and supportive measures are recommended.

Flortaucipir F-18

DB14914

small molecule approved investigational

Deskripsi

Flortaucipir F-18, also known as 18F-T807 and 18F-AV-1451, is a small indole molecule synthesized with a radioactive fluorine isotope.A203933 It is used as a marker in positron emission tomography (PET) imaging of patients suspected of having Alzheimer's disease. After crossing the blood-brain barrier, flortaucipir F-18 binds to aggregated tau protein, a hallmark of Alzheimer's disease whose incidence correlates well with disease progression.A203933, A203936, A203939

Although flortaucipir F-18 displays low levels of background binding throughout the brain,A203936 it does display off-target binding to monoamine oxidase MAO-A and MAO-B, as well as to regions containing high levels of melanin, neuromelanin, and iron.A203942, A203945. It was approved by the FDA on May 28, 2020, for sale by Avid Radiopharmaceuticals under the name TAUVID™ and is the first FDA-approved molecule for imaging aggregated tau protein in the brain.L14114

Struktur Molekul 2D

Berat 262.278
Wujud -

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Flortaucipir F-18 plasma half-life was calculated at 17.0 ± 4.2 minutes; correction for metabolite half-life yielded a biexponential distribution with half-lives of 18.1 ± 5.8 and 2.4 ± 0.5 minutes.[A203939]
Volume Distribusi Flortaucipir F-18 injected into mice accumulates primarily in the kidneys (14.99 ± 0.39 %ID/g at five minutes and 5.52 ± 0.91 %ID/g at 30 minutes post-injection) and liver (4.44 ± 0.16/5.99 ± 0.42 %ID/g at five/30 minutes, respectively). It is able to cross the blood-brain barrier, with relatively high penetration early (4.43 ± 0.91 %ID/g at five minutes) and low residual penetration later (0.62 ± 0.06 %ID/g at 30 minutes). Detectable amounts of Flortaucipir F-18 are found in the systemic circulation, as well as in muscle and bone.[A203936]
Klirens (Clearance) -

Absorpsi

Flortaucipir F-18 is administered as an intravenous bolus injection, L14114 and peak brain uptake in mice of 4.16% ID/g is achieved by 2 minutes.A203936 Fast transfer from the peripheral circulation to the brain was corroborated by human studies that demonstrated peak SUV in gray matter >2 across subjects approximately 5 minutes after administration.A203939 Pharmacokinetic studies in humans suggest that equilibrium is achieved by 55 minutes (Logan DVR) and by 80 - 100 minutes (SUVR),A203939 and current guidelines recommend initiating imaging approximately 80 minutes after initial administration.L14114

Metabolisme

Initial studies in mice described the parent compound and four uncharacterized metabolites, one of which, termed metabolite 1, is presumed to be 18Ffluoride. Plasma radioactivity corresponded only to the parent compound and metabolite 1. All metabolites were detected in the liver while all metabolites except metabolite 2 were found in the kidneys.A203936

Rute Eliminasi

The major route of elimination for Flortaucipir F-18 is via the kidneys.A203936

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Microtubule-associated protein tau MAPT
Amine oxidase [flavin-containing] A MAOA
Amine oxidase [flavin-containing] B MAOB

Referensi & Sumber

Synthesis reference: Neil Vasdev, Timothy M. Shoup. "Radiosynthesis of tau radiopharmaceuticals." US patent US9546167B2, issued January 17, 2017.
Artikel (PubMed)
  • PMID: 31172290
    Wang YT, Edison P: Tau Imaging in Neurodegenerative Diseases Using Positron Emission Tomography. Curr Neurol Neurosci Rep. 2019 Jun 6;19(7):45. doi: 10.1007/s11910-019-0962-7.
  • PMID: 23411393
    Xia CF, Arteaga J, Chen G, Gangadharmath U, Gomez LF, Kasi D, Lam C, Liang Q, Liu C, Mocharla VP, Mu F, Sinha A, Su H, Szardenings AK, Walsh JC, Wang E, Yu C, Zhang W, Zhao T, Kolb HC: (18)FT807, a novel tau positron emission tomography imaging agent for Alzheimer's disease. Alzheimers Dement. 2013 Nov;9(6):666-76. doi: 10.1016/j.jalz.2012.11.008. Epub 2013 Feb 12.
  • PMID: 27660144
    Wooten DW, Guehl NJ, Verwer EE, Shoup TM, Yokell DL, Zubcevik N, Vasdev N, Zafonte RD, Johnson KA, El Fakhri G, Normandin MD: Pharmacokinetic Evaluation of the Tau PET Radiotracer (18)F-T807 ((18)F-AV-1451) in Human Subjects. J Nucl Med. 2017 Mar;58(3):484-491. doi: 10.2967/jnumed.115.170910. Epub 2016 Sep 22.
  • PMID: 29278274
    Vermeiren C, Motte P, Viot D, Mairet-Coello G, Courade JP, Citron M, Mercier J, Hannestad J, Gillard M: The tau positron-emission tomography tracer AV-1451 binds with similar affinities to tau fibrils and monoamine oxidases. Mov Disord. 2018 Feb;33(2):273-281. doi: 10.1002/mds.27271. Epub 2017 Dec 26.
  • PMID: 28775201
    Choi JY, Cho H, Ahn SJ, Lee JH, Ryu YH, Lee MS, Lyoo CH: Off-Target (18)F-AV-1451 Binding in the Basal Ganglia Correlates with Age-Related Iron Accumulation. J Nucl Med. 2018 Jan;59(1):117-120. doi: 10.2967/jnumed.117.195248. Epub 2017 Aug 3.

Contoh Produk & Brand

Produk: 4 • International brands: 0
Produk
  • Tauvid
    Injection, solution • 800 MBq/ml • Intravenous • EU • Approved
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  • Tauvid
    Injection, solution • 51 mCi/1mL • Intravenous • US • Approved
  • Tauvid
    Injection, solution • 100 mCi/1mL • Intravenous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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