Peringatan Keamanan

LD₅₀ in rats was 40 mg/kg following subcutaneous administration.^L43065

There have been no reports of overdosage with ganirelix in humans.^L43045 Clinical studies with subcutaneous administration of ganirelix at single doses up to 12 mg did not show systemic adverse reactions. In acute toxicity studies in rats and monkeys, non-specific toxic symptoms such as hypotension and bradycardia were only observed after intravenous administration of ganirelix over 1 and 3 mg/kg, respectively. As there is no known antidote for ganirelix, the drug should be discontinued in case of an overdose.^L43040

Ganirelix

DB06785

small molecule approved

Deskripsi

Ganirelix is a synthetic decapeptide and a competitive gonadotropin-releasing hormone (GnRH) antagonist. Derived from endogenous GnRH, ganirelix has amino acid substitutions. Ganirelix is indicated for controlled ovarian hyperstimulation in assisted reproduction techniques.^L43045 The first case of pregnancy achieved after the use of ganirelix in an assisted reproduction program was reported in 1998.^A252195 Ganirelix was first approved by the FDA on July 29, 1999.^L43070

Struktur Molekul 2D

Berat 1570.35

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 elimination half-life (t½) following subcutaneous administration of a single 250-mcg dose is approximately 13 hours.[L43040, L43045]

Volume Distribusi The mean (SD) volume of distribution of ganirelix in healthy females following subcutaneous administration of a single 250-mcg dose is 43.7 (11.4) L.[L43045]

Klirens (Clearance) Clearance following subcutaneous administration of a single 250-mcg dose is approximately 2.4 L/h.[L43040]

Absorpsi

Ganirelix is rapidly absorbed following subcutaneous administration with a mean absolute bioavailability of approximately 91%.^L43045 It has a T_max ranging from one to two hours.L43040, L43045 Ganirelix reaches steady-state serum concentrations after three days of administration.^L43045

Metabolisme

The metabolites are small peptide fragments formed by enzymatic hydrolysis of ganirelix at restricted sites.^L43040 The 1–4 peptide and 1–6 peptide of ganirelix are the primary metabolites observed in the feces.^L43045

Rute Eliminasi

Following single-dose intravenous administration of radiolabeled ganirelix to healthy female volunteers, Ganirelix is the major compound present in the plasma (50–70% of total radioactivity in the plasma) up to 4 hours and urine (17.1–18.4% of administered dose) up to 24 hours. Ganirelix is not found in the feces. On average, 97.2% of the total radiolabeled ganirelix dose is recovered in the feces and urine (75.1% and 22.1%, respectively) over 288 h following intravenous single dose administration of 1 mg ¹⁴C-ganirelix. Urinary excretion is virtually complete in 24 h, whereas fecal excretion starts to plateau 192 h after dosing.^L43045

Interaksi Obat

0 Data

Tidak ada data.

Target Protein

Gonadotropin-releasing hormone receptor GNRHR

Referensi & Sumber

Synthesis reference: "Patent Link":http://www.google.ca/patents/US5767082

Artikel (PubMed)

PMID: 10718102
Gillies PS, Faulds D, Balfour JA, Perry CM: Ganirelix. Drugs. 2000 Jan;59(1):107-11; discussion 112-3. doi: 10.2165/00003495-200059010-00007.
PMID: 11939160
Out HJ, Mannaerts BM: The gonadotrophin-releasing hormone antagonist ganirelix--history and introductory data. Hum Fertil (Camb). 2002 Feb;5(1):G5-10; discussion G10-2, G41-8. doi: 10.1080/1464727992000199771.
PMID: 27126581
Al-Inany HG, Youssef MA, Ayeleke RO, Brown J, Lam WS, Broekmans FJ: Gonadotrophin-releasing hormone antagonists for assisted reproductive technology. Cochrane Database Syst Rev. 2016 Apr 29;4:CD001750. doi: 10.1002/14651858.CD001750.pub4.

Link

Contoh Produk & Brand

Produk: 16 • International brands: 0

Produk

Fyremadel

Injection, solution • 250 ug/0.5mL • Subcutaneous • US • Generic • Approved
Ganirelix Acetate

Injection, solution • 250 ug/0.5mL • Subcutaneous • US • Approved
Ganirelix Acetate

Injection, solution • 250 ug/0.5mL • Subcutaneous • US • Generic • Approved
Ganirelix Acetate

Injection, solution • 250 ug/0.5mL • Subcutaneous • US • Generic • Approved
Ganirelix Acetate

Injection, solution • 250 ug/0.5mL • Subcutaneous • US • Approved
Ganirelix Acetate

Injection, solution • 250 ug/0.5mL • Subcutaneous • US • Generic • Approved
Ganirelix Acetate

Injection • 250 ug/0.5mL • Subcutaneous • US • Generic • Approved
Ganirelix Acetate

Injection, solution • 250 ug/0.5mL • Subcutaneous • US • Generic • Approved

Menampilkan 8 dari 16 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.