Peringatan Keamanan

The LD₅₀ of lutetium Lu 177 vipivotide tetraxetan is unknown. The oral and intraperitoneal LD₅₀ lutetium Lu-177 chloride in mice was 315 mg/kg and 7100 mg/kg, respectively.^L41295

There is limited clinical experience of overdose from lutetium Lu 177 vipivotide tetraxetan. In the event of administration of a radiation overdosage with lutetium Lu 177 vipivotide tetraxetan, reduce the radiation absorbed dose to the patient by increasing the elimination of the radionuclide from the body by frequent micturition or by forced diuresis and frequent bladder voiding. Estimate the effective radiation dose that was applied and treat with additional supportive care measures as clinically indicated.^L41280

Lutetium Lu-177 vipivotide tetraxetan

DB16778

biotech approved

Deskripsi

Lutetium Lu-177 vipivotide tetraxetan is a radioligand therapeutic agent. It consists of a radionuclide, lutetium Lu-177, linked to a moiety that binds to PSMA, a transmembrane protein that is expressed in prostate cancer.^L41280

Lutetium Lu-177 vipivotide tetraxetan was first approved by the FDA on March 23, 2022 as a treatment for prostate-specific membrane antigen–positive metastatic castration-resistant prostate cancer.^L41290 In October 2022, the EMA's Committee for Medicinal Products for Human Use (CHMP) recommended lutetium Lu-177 vipivotide tetraxetan be granted marketing authorization for the treatment of prostate cancer.^L43787 In December 2022, lutetium Lu-177 vipivotide tetraxetan was approved by the EMA.L43787,L45533

Struktur Molekul 2D

Struktur tidak tersedia

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 terminal elimination half-life (%CV) of lutetium Lu 177 vipivotide tetraxetan is 41.6 hours (68.8%)[L41280]

Volume Distribusi The mean volume of distribution (%CV) is 123 L (78.1%). Within 2.5 hours of administration, lutetium Lu 177 vipivotide tetraxetan distributes to gastrointestinal tract, liver, lungs, kidneys, heart wall, bone marrow, and salivary glands.[L41280]

Klirens (Clearance) The mean clearance (CL) (%CV) is 2.04 L/h (31.5%).[L41280]

Absorpsi

The blood area under the curve (AUC) (geometric mean coefficient of variation or %CV) of lutetium Lu 177 vipivotide tetraxetan is 52.3 ng x h/mL (31.4%) and the maximum blood concentration (%CV) is 6.58 ng/mL (43.5%) at the recommended dosage.^L41280

Metabolisme

Once dissociated from the parent compound, lutetium-177 decays to a stable hafnium-177.^L41280

Rute Eliminasi

Lutetium Lu 177 vipivotide tetraxetan is primarily eliminated renally.^L41280 It is renally-excreted in the first 48 h following injection.^A246145

Interaksi Obat

0 Data

Tidak ada data.

Target Protein

Prostate-specific antigen KLK3

Referensi & Sumber

Artikel (PubMed)

PMID: 28303694
Emmett L, Willowson K, Violet J, Shin J, Blanksby A, Lee J: Lutetium (177) PSMA radionuclide therapy for men with prostate cancer: a review of the current literature and discussion of practical aspects of therapy. J Med Radiat Sci. 2017 Mar;64(1):52-60. doi: 10.1002/jmrs.227.
PMID: 32147685
Tateishi U: Prostate-specific membrane antigen (PSMA)-ligand positron emission tomography and radioligand therapy (RLT) of prostate cancer. Jpn J Clin Oncol. 2020 Apr 7;50(4):349-356. doi: 10.1093/jjco/hyaa004.

Link

Contoh Produk & Brand

Produk: 2 • International brands: 0

Produk

1 Pluvicto

Injection, solution • 1000 MBq/mL • Intravenous • EU • Approved
Pluvicto

Injection, solution • 27 mCi/1mL • Intravenous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.