Peringatan Keamanan

The oral, subcutaneous, and intravenous LD₅₀ in mice are 4360 mg/kg, 600 mg/kg, and 55 mg/kg, respectively.^L47716

Rapid intravenous infusion of gallium nitrate or use of doses higher than recommended (200 mg/m²) may cause nausea and vomiting and a substantially increased risk of renal insufficiency. In the event of overdosage, further drug administration should be discontinued, serum calcium should be monitored, and the patient should receive vigorous intravenous hydration, with or without diuretics, for two to three days. During this time period, renal function and urinary output should be carefully monitored so that fluid intake and output are balanced.^L47721

Gallium nitrate

DB05260

small molecule approved investigational

Deskripsi

Gallium nitrate is a nitrate salt of DB14524, a heavy metal that has been used as a diagnostic agent.^A260816 Gallium nitrate is reported to possess antiresorptive and hypocalcemic effects on bone.^A17097 GANITE, a product of gallium nitrate previously used to treat cancer-related hypercalcemia, was discontinued from marketing in the US for reasons other than safety or effectiveness.^L47726

Apart from cancer-related hypercalcemia, gallium nitrate has been studied in arthritis, autoimmune disorders, and tumours.^A260830

Struktur Molekul 2D

Berat 255.738

Wujud liquid

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) In phase I studies involving cancer patients who received a short-term intravenous infusion of single doses ranging from 300 to 900 mg/m2, a biphasic curve was observed. Gallium nitrate exhibited a mean initial (distribution phase) half-life of 1 to 1.5 hours and a terminal (elimination phase) half-lives of 25 to 30 hours.[A260816]

Volume Distribusi In phase I studies involving cancer patients who received a short-term intravenous infusion of single doses ranging from 300 to 900 mg/m2, the mean volume of distribution of gallium was 1.27 L/kg.[A260816]

Klirens (Clearance) In cancer patients who received a daily infusion of gallium nitrate at a dose of 200 mg/m2 for five to seven consecutive days, the average plasma clearance of gallium was 0.15 L/hr/kg (range: 0.12 to 0.20 L/hr/kg).[L47721]

Absorpsi

Gallium nitrate was infused at a daily dose of 200 mg/m² for 5 (n=2) or 7 (n=10) consecutive days to 12 cancer patients. In most patients, mean steady-state plasma concentrations were reached after 18 to 24 hours of infusion. The average steady-state plasma levels of gallium observed among seven fully evaluable patients was between 1134 and 2399 ng/mL. In one patient who received daily infusion doses of 100, 150 and 200 mg/m², the apparent steady-state levels of gallium did not increase proportionally with an increase in dose.^L47721

Metabolisme

Gallium nitrate is not metabolized either by the liver or the kidney.^L47721

Rute Eliminasi

Gallium nitrate appears to be significantly excreted via the kidney.A260820, L47721 In phase I studies involving cancer patients who received a short-term intravenous infusion of single doses ranging from 300 to 900 mg/m², about two-thirds of the administered dose was recovered in the urine in the first 24 hours post-dose.^A260816

Interaksi Obat

1 Data

Magnesium

The serum concentration of Magnesium can be decreased when it is combined with Gallium nitrate.

Target Protein

Interleukin-1 beta IL1B

Ribonucleoside-diphosphate reductase subunit M2 RRM2

V-type proton ATPase subunit B, brain isoform ATP6V1B2

Referensi & Sumber

Artikel (PubMed)

PMID: 16122880
Eby G: Elimination of arthritis pain and inflammation for over 2 years with a single 90 min, topical 14% gallium nitrate treatment: case reports and review of actions of gallium III. Med Hypotheses. 2005;65(6):1136-41. Epub 2005 Aug 24.
PMID: 10727770
Panagakos FS, Kumar E, Venescar C, Guidon P: The effect of gallium nitrate on synoviocyte MMP activity. Biochimie. 2000 Feb;82(2):147-51. doi: 10.1016/s0300-9084(00)00384-9.
PMID: 7427907
Kelsen DP, Alcock N, Yeh S, Brown J, Young C: Pharmacokinetics of gallium nitrate in man. Cancer. 1980 Nov 1;46(9):2009-13. doi: 10.1002/1097-0142(19801101)46:9<2009::aid-cncr2820460919>3.0.co;2-a.
PMID: 1717224
Todd PA, Fitton A: Gallium nitrate. A review of its pharmacological properties and therapeutic potential in cancer related hypercalcaemia. Drugs. 1991 Aug;42(2):261-73. doi: 10.2165/00003495-199142020-00007.
PMID: 12776254
Bockman R: The effects of gallium nitrate on bone resorption. Semin Oncol. 2003 Apr;30(2 Suppl 5):5-12.
PMID: 8227174
Bockman RS, Guidon PT Jr, Pan LC, Salvatori R, Kawaguchi A: Gallium nitrate increases type I collagen and fibronectin mRNA and collagen protein levels in bone and fibroblast cells. J Cell Biochem. 1993 Aug;52(4):396-403. doi: 10.1002/jcb.240520404.
PMID: 11329118
Apseloff G: Therapeutic uses of gallium nitrate: past, present, and future. Am J Ther. 1999 Nov;6(6):327-39. doi: 10.1097/00045391-199911000-00008.

Link

Contoh Produk & Brand

Produk: 1 • International brands: 0

Produk

Ganite

Injection, solution, concentrate • 25 mg/1mL • Intravenous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.