Peringatan Keamanan

The most common reported adverse reaction was headache, occurring in 2% of patients, followed by musculoskeletal pain, blood pressure increased, fatigue, nausea, and injection site reaction, all occurring in <1% of patients.

Florbetapir F-18

DB09149

small molecule approved investigational

Deskripsi

Florbetapir (18F) is a radiopharmaceutical compound containing the radionuclide fluorine-18 bound to the compound florbetapir, a molecule that binds with high affinity to beta amyloid plaque, a peptide that plays a key role in Alzheimer's Disease pathogenesis. Marketed as the product Amyvid, florbetapir 18F is indicated for positron emission tomography (PET) imaging of the brain to estimate ?-amyloid neuritic plaque density in adult patients with cognitive impairment who are being evaluated for Alzheimer's Disease (AD) and other causes of cognitive decline.

The radionucleide fluorine-18 was chosen as it has a half life of 110 minutes allowing it to accumulate sufficiently in the brain before undergoing positon emission decay.

Struktur Molekul 2D

Berat 359.432
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

The time-activity curves for florbetapir F 18 in the brain of subjects with positive scans show continual signal increases from time zero through 30 minutes post-administration, with stable values thereafter up to at least 90 minutes post-injection. Following the intravenous administration of 370 MBq (10 mCi) of florbetapir F 18 to healthy volunteers, the drug was distributed throughout the body with less than 5% of the injected F 18 radioactivity present in the blood by 20 minutes following administration, and less than 2% present by 45 minutes after administration.

Metabolisme

The residual F 18 in circulation during the 30-90 minute imaging window was principally in the form of polar F 18 metabolites. Essentially all radioactivity collected in the urine was present as polar metabolites of florbetapir F 18. Three metabolites have been discovered and identified as 18FAV-160 (desmethyl-18FAV-45), 18FAV-267 (N-acetyl–18FAV-160), and an 18F-Polar species, the identity of which has not been confirmed. Additionally, although metabolites may make some contribution to signal detection, particularly to the nontarget activity, it is concluded that there will be minimal interference from these radiolabeled metabolites to the amyloid target binding in the 18FAV-45 brain PET image (Wong et al, 2010).

Rute Eliminasi

Whole body scanning following the intravenous injection showed accumulation of radioactivity in the liver within four minutes post-injection, followed by elimination of the radioactivity predominantly through the biliary/gastrointestinal tract with much lower radioactivity detected in the bladder. Essentially all radioactivity collected in the urine was present as polar metabolites of florbetapir F 18.

Interaksi Obat

727 Data
Cyclosporine Cyclosporine may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Meloxicam Meloxicam may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Tacrolimus Tacrolimus may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Atazanavir Atazanavir may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cefpodoxime Cefpodoxime may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Aminophenazone Aminophenazone may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Antipyrine Antipyrine may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Tiaprofenic acid Tiaprofenic acid may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Lopinavir Lopinavir may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Etoricoxib Etoricoxib may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Hydrolyzed Cephalothin Hydrolyzed Cephalothin may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cephalothin Group Cephalothin Group may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Oxyphenbutazone Oxyphenbutazone may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Latamoxef Latamoxef may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Nimesulide Nimesulide may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Benoxaprofen Benoxaprofen may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Metamizole Metamizole may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Zomepirac Zomepirac may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Ceftobiprole Ceftobiprole may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Cimicoxib Cimicoxib may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Ceftaroline fosamil Ceftaroline fosamil may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Lornoxicam Lornoxicam may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.
Aceclofenac Aceclofenac may decrease the excretion rate of Florbetapir (18F) which could result in a higher serum level.

Target Protein

Amyloid-beta precursor protein APP
Beta amyloid plaque

Referensi & Sumber

Synthesis reference: - Wong DF, Rosenberg PB, Zhou Y, Kumar A, Raymont V, Ravert HT, Dannals RF, Nandi A, Brasic JR, Ye W, Hilton J, Lyketsos C, Kung HF, Joshi AD, Skovronsky DM, Pontecorvo MJ: In vivo imaging of amyloid deposition in Alzheimer disease using the radioligand 18F-AV-45 (florbetapir corrected F 18). J Nucl Med. 2010 Jun;51(6):913-20. doi: 10.2967/jnumed.109.069088. - Fowler J. S. and Wolf A. P. (1982) The synthesis of carbon-11, fluorine-18 and nitrogen-13 labeled radiotracers for biomedical applications. Nucl. Sci. Ser. Natl Acad. Sci. Natl Res. Council Monogr. 1982.
Artikel (PubMed)
  • PMID: 20501908
    Wong DF, Rosenberg PB, Zhou Y, Kumar A, Raymont V, Ravert HT, Dannals RF, Nandi A, Brasic JR, Ye W, Hilton J, Lyketsos C, Kung HF, Joshi AD, Skovronsky DM, Pontecorvo MJ: In vivo imaging of amyloid deposition in Alzheimer disease using the radioligand 18F-AV-45 (florbetapir corrected F 18). J Nucl Med. 2010 Jun;51(6):913-20. doi: 10.2967/jnumed.109.069088.
  • PMID: 19837759
    Choi SR, Golding G, Zhuang Z, Zhang W, Lim N, Hefti F, Benedum TE, Kilbourn MR, Skovronsky D, Kung HF: Preclinical properties of 18F-AV-45: a PET agent for Abeta plaques in the brain. J Nucl Med. 2009 Nov;50(11):1887-94. doi: 10.2967/jnumed.109.065284. Epub 2009 Oct 16.

Contoh Produk & Brand

Produk: 5 • International brands: 0
Produk
  • Amyvid
    Injection, solution • 51 mCi/1mL • Intravenous • US • Approved
  • Amyvid
    Injection, solution • 800 MBq/ml • Intravenous • EU • Approved
  • Amyvid
    Injection, solution • 800 MBq/ml • Intravenous • EU • Approved
  • Amyvid
    Injection, solution • 1900 MBq/ml • Intravenous • EU • Approved
  • Amyvid
    Injection, solution • 1900 MBq/ml • Intravenous • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul