Peringatan Keamanan

The LD₅₀ of this medication is not readily available.^L8597

In the event of an overdose, give patients plenty of fluids and diuretics if necessary to encourage frequent urination.^L8597 If possible, an estimation of radioactive dose should be performed.^L8597

Edotreotide gallium Ga-68

DB15494

small molecule approved

Deskripsi

Edotreotide gallium Ga-68 is an 8 amino acid peptide bound to the chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA).^L8603 Edotreotide gallium Ga-68 is indicated for localizing somatostatin receptor positive neuroendocrine tumors by positron emission tomography.^L8597 Dotatate gallium Ga-68 is used for a similar indication.^A185852 Dotatate gallium Ga-68 has lower tumor uptake but this data is highly variable between patients.^A185852

Edotreotide gallium Ga-68 was granted FDA approval on 21 August 2019.^L8597

Struktur Molekul 2D

Berat 1486.55

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) Edotreotide gallium Ga-68 has a radioactive half life of 68 minutes.[A185867,L8603] Edotreotide gallium Ga-68 has two half lives, 2.0±0.3min and 48±7min for its removal from blood.[A185867,L8603]

Volume Distribusi Data regarding the volume of distribution of this medication is not readily available.[L8597]

Klirens (Clearance) Data regarding the clearance of this medication is not readily available.[L8597]

Absorpsi

Edotreotide gallium Ga-68 reaches 80% activity in tumors within 30 minutes,^A185867 and reaches its highest activity in tumors 70±20min post injection.^L8603 Edotreotide is mostly taken up into the spleen, followed by kidneys, liver, pituitary, thyroid, and adrenal gland.A185861,A185867,L8603 Accumulation in non-tumor tissue reaches a maximum within 40 minutes.^A185867

Metabolisme

Edotreotide gallium Ga-68 is largely unmetabolized.^L8603 4 hours post injection there are no metabolites or degradation products detectable in serum.^A185867

Rute Eliminasi

16% of a Edotreotide gallium Ga-68 dose is eliminated in the urine within 2h.A185849,L8597 It is expected that Edotreotide gallium Ga-68 is exclusively eliminated in the urine.A185849,L8597 In animal studies, edotreotide Y-90 was >80% eliminated in the urine within 24h, with 95.6±3.4% being unmetabolized.A185861,L8603 <1% of a dose is detected in the feces.^A185870

Interaksi Obat

5 Data

Octreotide	Octreotide may decrease effectiveness of Edotreotide gallium Ga-68 as a diagnostic agent.
Vapreotide	Vapreotide may decrease effectiveness of Edotreotide gallium Ga-68 as a diagnostic agent.
Pasireotide	Pasireotide may decrease effectiveness of Edotreotide gallium Ga-68 as a diagnostic agent.
Lanreotide	Lanreotide may decrease effectiveness of Edotreotide gallium Ga-68 as a diagnostic agent.
Somatostatin	Somatostatin may decrease effectiveness of Edotreotide gallium Ga-68 as a diagnostic agent.

Target Protein

Somatostatin receptor type 2 SSTR2

Somatostatin receptor type 5 SSTR5

Somatostatin receptor type 3 SSTR3

Somatostatin receptor type 1 SSTR1

Referensi & Sumber

Artikel (PubMed)

PMID: 19639164
Hartmann H, Zophel K, Freudenberg R, Oehme L, Andreeff M, Wunderlich G, Eisenhofer G, Kotzerke J: Radiation exposure of patients during 68Ga-DOTATOC PET/CT examinations. Nuklearmedizin. 2009;48(5):201-7. doi: 10.3413/nukmed-0214. Epub 2009 Jul 28.
PMID: 22072704
Poeppel TD, Binse I, Petersenn S, Lahner H, Schott M, Antoch G, Brandau W, Bockisch A, Boy C: 68Ga-DOTATOC versus 68Ga-DOTATATE PET/CT in functional imaging of neuroendocrine tumors. J Nucl Med. 2011 Dec;52(12):1864-70. doi: 10.2967/jnumed.111.091165. Epub 2011 Nov 9.
PMID: 9096086
de Jong M, Bakker WH, Krenning EP, Breeman WA, van der Pluijm ME, Bernard BF, Visser TJ, Jermann E, Behe M, Powell P, Macke HR: Yttrium-90 and indium-111 labelling, receptor binding and biodistribution of DOTA0,d-Phe1,Tyr3octreotide, a promising somatostatin analogue for radionuclide therapy. Eur J Nucl Med. 1997 Apr;24(4):368-71. doi: 10.1007/bf00881807.
PMID: 11734911
Hofmann M, Maecke H, Borner R, Weckesser E, Schoffski P, Oei L, Schumacher J, Henze M, Heppeler A, Meyer J, Knapp H: Biokinetics and imaging with the somatostatin receptor PET radioligand (68)Ga-DOTATOC: preliminary data. Eur J Nucl Med. 2001 Dec;28(12):1751-7. doi: 10.1007/s002590100639. Epub 2001 Oct 31.
PMID: 10319747
Kwekkeboom DJ, Kooij PP, Bakker WH, Macke HR, Krenning EP: Comparison of 111In-DOTA-Tyr3-octreotide and 111In-DTPA-octreotide in the same patients: biodistribution, kinetics, organ and tumor uptake. J Nucl Med. 1999 May;40(5):762-7.
PMID: 10901448
Bangard M, Behe M, Guhlke S, Otte R, Bender H, Maecke HR, Biersack HJ: Detection of somatostatin receptor-positive tumours using the new 99mTc-tricine-HYNIC-D-Phe1-Tyr3-octreotide: first results in patients and comparison with 111In-DTPA-D-Phe1-octreotide. Eur J Nucl Med. 2000 Jun;27(6):628-37. doi: 10.1007/s002590050556.

Link

Contoh Produk & Brand

Produk: 2 • International brands: 0

Produk

Ga-68-DOTATOC

Injection, solution • 4 mCi/1mL • Intravenous • US • Approved
Somakit Toc

Kit • 40 mcg • Intravenous • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.