Peringatan Keamanan

In case of an overdose of flotufolastat F-18, maintain patients hydrated and promote frequent voiding to reduce the effects of radiation exposure. Diuretics can also be used in case of overdose. The product label also recommends estimating the radiation-effective dose administered to the patient, if possible.L46731 The carcinogenic or mutagenic potential of flotufolastat F-18 in animals has not been evaluated. However, this compound can potentially be mutagenic due to the F-18 radionuclide. Animal studies evaluating the potential impairment of fertility have not been conducted.L46731

Flotufolastat F-18

DB17851

small molecule approved investigational

Deskripsi

Flotufolastat F-18 (18F-rhPSMA-7.3) is an 18F-labeled ligand that targets the prostate-specific membrane antigen (PSMA).A259846,L46731 In patients with recurrent prostate cancer that require localized treatment, the use of 18F-labeled ligands for positron emission tomography (PET) offers accurate diagnostic imaging. Unlike 68Ga-labeled PSMA-targeting ligands, 18F-labeled compounds targeting this protein have a longer half-life and can be produced in larger batches. Flotufolastat F-18 is a diastereoisomer of 18F-rhPSMA-7, and compared to the other diastereoisomers of this compound, flotufolastat F-18 has a faster clearance from blood pool, liver, and kidney, and a high level of accumulation in tumors.A259846

In May 2023, the FDA approved the use of flotufolastat F-18 for PET of PSMA-positive lesions in men with prostate cancer with suspected metastasis who are candidates for initial definitive therapy or suspected recurrence based on elevated serum prostate-specific antigen (PSA) level.L46731,L46737 This is the first FDA-approved, PSMA-targeted imaging agent developed with proprietary radiohybrid (rh) technology.L46737 Additional studies have shown that in patients with primary prostate cancer, the use of flotufolastat F-18 shows led to low interreader variation and a good distinction between primary-tumor activity and bladder background activity.A259851

Struktur Molekul 2D

Berat 1470.63
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Not available.
Volume Distribusi Not available.
Klirens (Clearance) Not available.

Absorpsi

After flotufolastat F-18 is administered intravenously, it distributes to the liver, heart blood pool and kidneys, with 15.8%, 7.4% and 3.2% of the administered activity, respectively. Flotufolastat F-18 is cleared from the blood.L46731

Metabolisme

After it is injected, flotufolastat F-18 is not metabolized for up to 50 minutes.L46731

Rute Eliminasi

Flotufolastat F-18 is eliminated by urinary excretion. In the first 2 hours after flotufolastat F-18 is injected, approximately 7% of the administered activity is excreted in the urine. Approximately 15% is excreted 4.5 hours after flotufolastat F-18 is injected.L46731

Interaksi Obat

11 Data
Flutamide Flutamide may decrease effectiveness of Flotufolastat F-18 as a diagnostic agent.
Nilutamide Nilutamide may decrease effectiveness of Flotufolastat F-18 as a diagnostic agent.
Bicalutamide Bicalutamide may decrease effectiveness of Flotufolastat F-18 as a diagnostic agent.
Cyproterone acetate Cyproterone acetate may decrease effectiveness of Flotufolastat F-18 as a diagnostic agent.
Enzalutamide Enzalutamide may decrease effectiveness of Flotufolastat F-18 as a diagnostic agent.
Relugolix Relugolix may decrease effectiveness of Flotufolastat F-18 as a diagnostic agent.
Apalutamide Apalutamide may decrease effectiveness of Flotufolastat F-18 as a diagnostic agent.
Clascoterone Clascoterone may decrease effectiveness of Flotufolastat F-18 as a diagnostic agent.
Darolutamide Darolutamide may decrease effectiveness of Flotufolastat F-18 as a diagnostic agent.
Chlormadinone Chlormadinone may decrease effectiveness of Flotufolastat F-18 as a diagnostic agent.
Chlormadinone acetate Chlormadinone acetate may decrease effectiveness of Flotufolastat F-18 as a diagnostic agent.

Target Protein

Glutamate carboxypeptidase 2 FOLH1

Referensi & Sumber

Synthesis reference: Bejot, R., et al. (2022). Methods of preparation of 18F labelled silyl-fluoride compounds (WO 2023047138 A1). World Intellectual Property Organization. https://patents.google.com/patent/WO2023047138A1/en?oq=WO2023047138A1
Artikel (PubMed)
  • PMID: 35393348
    Kroenke M, Schweiger L, Horn T, Haller B, Schwamborn K, Wurzer A, Maurer T, Wester HJ, Eiber M, Rauscher I: Validation of (18)F-rhPSMA-7 and (18)F-rhPSMA-7.3 PET Imaging Results with Histopathology from Salvage Surgery in Patients with Biochemical Recurrence of Prostate Cancer. J Nucl Med. 2022 Dec;63(12):1809-1814. doi: 10.2967/jnumed.121.263707. Epub 2022 Apr 7.
  • PMID: 34992154
    Langbein T, Wang H, Rauscher I, Kroenke M, Knorr K, Wurzer A, Schwamborn K, Maurer T, Horn T, Haller B, Wester HJ, Eiber M: Utility of (18)F-rhPSMA-7.3 PET for Imaging of Primary Prostate Cancer and Preoperative Efficacy in N-Staging of Unfavorable Intermediate- to Very High-Risk Patients Validated by Histopathology. J Nucl Med. 2022 Sep;63(9):1334-1342. doi: 10.2967/jnumed.121.263440. Epub 2022 Jan 6.

Contoh Produk & Brand

Produk: 1 • International brands: 1
Produk
  • Posluma
    Injection • 158 mCi/1mL • Intravenous • US • Approved
International Brands
  • Posluma — Blue Earth Diagnostics Ltd.

Sekuens Gen/Protein (FASTA)

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