Fluoroestradiol F-18

DB15690

small molecule approved

Deskripsi

Fluoroestradiol F-18 is an imaging agent used with positron emission tomography (PET) to detect estrogen receptor-positive breast cancer lesions.^L14096 The ability to image ER-positive tumors in vivo is advantageous in that, while helping to visualize tumor progression/regression, it may also be used to assess for heterogeneity in ER expression across metastases (i.e. to identify sites that no longer express ER) without the need for multiple biopsies.^A203912

Fluoroestradiol F-18 was first granted FDA approval in May 2020, and will be developed by PETNET Solutions, Inc. and Zionexa USA under the brand name Cerianna.^L14117 It is expected to be available in late 2020/early 2021.^L14117

Struktur Molekul 2D

Berat 289.381

Wujud solid

Peta Jejaring Molekuler

Obat Target Gen Interaksi Enzim Transporter Carrier

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

1. Pendahuluan & Konsep

Fitur visualisasi ini dikembangkan menggunakan pendekatan Graph Theory untuk memetakan hubungan polifarmasi dan molekuler. Entitas (Obat, Target, Gen) direpresentasikan sebagai Simpul (Nodes), sedangkan hubungan biologisnya sebagai Sisi (Edges).

2. Sumber Data (Validasi)

Data Obat: Diekstraksi dari elemen drugbank-id dan name pada skema XML DrugBank.
Target Protein: Diambil dari elemen targets/target yang memuat polipeptida sasaran.
Genetik: Disinkronisasi dari sub-elemen gene-name dan varian snp-effects.
Genetik: Jumlah titik node dibatasi pada maksimal 10 (Slice=10) interaksi untuk menghindari tumpukan data.

3. Algoritma Visualisasi

Tata letak grafik menggunakan algoritma Force-Directed Graph (Barnes-Hut). Model fisika ini menerapkan gaya tolak-menolak antar simpul (Gravitasi: -3000) agar tidak tumpang tindih, serta gaya pegas (Spring: 0.04) pada garis penghubung untuk fleksibilitas interaksi.

4. Legenda Visual

Obat Utama (Pusat Analisis)

Target Protein (Mekanisme)

Gen (Faktor Genetik)

Metode ini mendukung analisis Precision Medicine dan evaluasi risiko Drug-Drug Interaction (DDI).

Profil Farmakokinetik

Waktu Paruh (Half-Life) -

Volume Distribusi As fluoroestradiol and its metabolites undergo enterohepatic circulation,[A203912] it is found primarily distributed within the hepatobiliary system.[L14096] It also distributes to the intestines, heart wall, blood, kidney, uterus, and bladder.[L14096]

Klirens (Clearance) Fluoroestradiol F-18 is rapidly cleared from the blood by the liver.[A203912]

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Fluoroestradiol F-18 is highly extracted and metabolized by the liver - at 2 hours post-administration, only 10% of the total activity is attributable to unmetabolized parent drug.^A203912 The majority of generated metabolites are products of glucuronide or sulfate conjugation.^A204023

Rute Eliminasi

Elimination is primarily via urinary and biliary excretion.^L14096 Unbound metabolites comprising mainly glucuronide and sulfate conjugates are secreted in the bile, reabsorbed via enterohepatic circulation, and then renally excreted.^A203912

Interaksi Obat

12 Data

Raloxifene	Raloxifene may decrease effectiveness of Fluoroestradiol F-18 as a diagnostic agent.
Toremifene	Toremifene may decrease effectiveness of Fluoroestradiol F-18 as a diagnostic agent.
Tamoxifen	Tamoxifen may decrease effectiveness of Fluoroestradiol F-18 as a diagnostic agent.
Clomifene	Clomifene may decrease effectiveness of Fluoroestradiol F-18 as a diagnostic agent.
Afimoxifene	Afimoxifene may decrease effectiveness of Fluoroestradiol F-18 as a diagnostic agent.
Ospemifene	Ospemifene may decrease effectiveness of Fluoroestradiol F-18 as a diagnostic agent.
Lasofoxifene	Lasofoxifene may decrease effectiveness of Fluoroestradiol F-18 as a diagnostic agent.
Bazedoxifene	Bazedoxifene may decrease effectiveness of Fluoroestradiol F-18 as a diagnostic agent.
Enclomiphene	Enclomiphene may decrease effectiveness of Fluoroestradiol F-18 as a diagnostic agent.
Ormeloxifene	Ormeloxifene may decrease effectiveness of Fluoroestradiol F-18 as a diagnostic agent.
Cyclofenil	Cyclofenil may decrease effectiveness of Fluoroestradiol F-18 as a diagnostic agent.
Fulvestrant	Fulvestrant may decrease effectiveness of Fluoroestradiol F-18 as a diagnostic agent.

Target Protein

Estrogen receptor ESR1

Estrogen receptor beta ESR2

Referensi & Sumber

Synthesis reference: Kiesewetter DO, Kilbourn MR, Landvatter SW, Heiman DF, Katzenellenbogen JA, Welch MJ: Preparation of four fluorine- 18-labeled estrogens and their selective uptakes in target tissues of immature rats. J Nucl Med. 1984 Nov;25(11):1212-21.

Artikel (PubMed)

PMID: 32210584
Liu Y, Ma H, Yao J: ERalpha, A Key Target for Cancer Therapy: A Review. Onco Targets Ther. 2020 Mar 11;13:2183-2191. doi: 10.2147/OTT.S236532. eCollection 2020.
PMID: 27307345
Liao GJ, Clark AS, Schubert EK, Mankoff DA: 18F-Fluoroestradiol PET: Current Status and Potential Future Clinical Applications. J Nucl Med. 2016 Aug;57(8):1269-75. doi: 10.2967/jnumed.116.175596. Epub 2016 Jun 15.
PMID: 9257333
Mankoff DA, Tewson TJ, Eary JF: Analysis of blood clearance and labeled metabolites for the estrogen receptor tracer F-18-16 alpha-fluoroestradiol (FES). Nucl Med Biol. 1997 May;24(4):341-8. doi: 10.1016/s0969-8051(97)00002-4.

Link

Contoh Produk & Brand

Produk: 1 • International brands: 0

Produk

Cerianna

Injection • 100 mCi/1mL • Intravenous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.