Peringatan Keamanan

Studies on dotatate gallium 68 have not been studied but the comparative studies to other non-radioactivity compounds showed no mutation.^{FDA label}

Dotatate gallium Ga-68

DB13925

small molecule approved investigational

Deskripsi

Dotatate gallium (Ga-68) is a somatostatin-2 receptor analog which is radiolabeled with gallium 68 as a positron-emitting radioisotope. Ga-68 dotatate has a high affinity for somatostatin-2 receptor and it is rapidly excreted from the nontarget sites which gives it an ideal candidate for imaging neuroendocrine tumors. Dotatate gallium (Ga-68) explotes its ability to detect somatostatin receptor scintigraphy and this characteristic tends to change with tumor grade which gives Ga-68 dotate a high diagnostic value.^A31358 Dotatate gallium 68 was developed by Advanced Accelerator Applications USA, Inc. and FDA approved in June 1, 2016.

Struktur Molekul 2D

Berat 1500.54

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) The half-life of gallium 68 is estimated to be of 68 min.[A31362]

Volume Distribusi The volume of distribution is registered in a range from 0.25-0.65 ml/cm3.[A31369]

Klirens (Clearance) The pharmacokinetics of dotatate gallium 68 is matched to the short half-life of the isotope gallium 68 thus, this pharmaceutical presents a very fast blood clearance.[A31362]

Absorpsi

Dotatate gallium 68 presents a higher affinity for the somatostatin receptor subtype 2 when compared with the other gallium 68 analogues. Intravenous administration of dotatate gallium 68 is absorbed and distributed to all the somatostatin subtype 2 receptor-containing organs like pituitary, thyroid, spleen, adrenals, kidney, pancreas, prostate, liver and salivary glands. There is no uptake in cerebral cortex or in the heart and the uptake presented in thymus and lung are very low.^A31365

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

In the first four hours after the intravenous administration of dotatate gallium 68 there is an elimination of about 12% of the injected dose by the urine.^A31365

Interaksi Obat

5 Data

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

Target Protein

Somatostatin receptor type 2 SSTR2

Referensi & Sumber

Artikel (PubMed)

PMID: 18383518
Kayani I, Bomanji JB, Groves A, Conway G, Gacinovic S, Win T, Dickson J, Caplin M, Ell PJ: Functional imaging of neuroendocrine tumors with combined PET/CT using 68Ga-DOTATATE (DOTA-DPhe1,Tyr3-octreotate) and 18F-FDG. Cancer. 2008 Jun;112(11):2447-55. doi: 10.1002/cncr.23469.
PMID: 23522791
Banerjee SR, Pomper MG: Clinical applications of Gallium-68. Appl Radiat Isot. 2013 Jun;76:2-13. doi: 10.1016/j.apradiso.2013.01.039. Epub 2013 Feb 20.
PMID: 25143861
Mojtahedi A, Thamake S, Tworowska I, Ranganathan D, Delpassand ES: The value of (68)Ga-DOTATATE PET/CT in diagnosis and management of neuroendocrine tumors compared to current FDA approved imaging modalities: a review of literature. Am J Nucl Med Mol Imaging. 2014 Aug 15;4(5):426-34. eCollection 2014.
PMID: 20926978
Shastry M, Kayani I, Wild D, Caplin M, Visvikis D, Gacinovic S, Reubi JC, Bomanji JB: Distribution pattern of 68Ga-DOTATATE in disease-free patients. Nucl Med Commun. 2010 Dec;31(12):1025-32. doi: 10.1097/MNM.0b013e32833f635e.
PMID: 25918675
Schottelius M, Simecek J, Hoffmann F, Willibald M, Schwaiger M, Wester HJ: Twins in spirit - episode I: comparative preclinical evaluation of (68)GaDOTATATE and (68)GaHA-DOTATATE. EJNMMI Res. 2015 Apr 10;5:22. doi: 10.1186/s13550-015-0099-x. eCollection 2015.
PMID: 25369268
Soto-Montenegro ML, Pena-Zalbidea S, Mateos-Perez JM, Oteo M, Romero E, Morcillo MA, Desco M: Meningiomas: a comparative study of 68Ga-DOTATOC, 68Ga-DOTANOC and 68Ga-DOTATATE for molecular imaging in mice. PLoS One. 2014 Nov 4;9(11):e111624. doi: 10.1371/journal.pone.0111624. eCollection 2014.

Link

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Contoh Produk & Brand

Produk: 0 • International brands: 0

Belum ada data produk/brand untuk obat ini pada database. Jalankan import DrugBank untuk mengisi field produk/brand.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.