Peringatan Keamanan

The most common adverse reactions (? 5% higher patient incidence in Nplate versus placebo) are arthralgia, dizziness, insomnia, myalgia, pain in extremity, abdominal pain, shoulder pain, dyspepsia, and paresthesia. Headache was the most commonly reported adverse reaction that did not occur at ? 5% higher patient incidence in Nplate versus placebo.
LD50 = 980 mg/kg.

Romiplostim

DB05332

biotech approved

Deskripsi

Romiplostim is a thrombopoiesis stimulating dimer Fc-peptide fusion protein (peptibody) to increase platelet production through activation of the thrombopoietin receptor. The peptibody molecule has two identical single-chain subunits, each one is made up of 269 amino acid residues. Each subunit consists of an IgG1 Fc carrier domain that is covalently attached to a polypeptide sequence that contains two binding domains to interact with thrombopoietin receptor c-Mpl. Each domain consists of 14 amino acids. Interestingly, romiplostim's amino acid sequence is not similar to that of endogenous thrombopoietin. Romiplostim is produced by recombinant DNA technology in Escherichia coli. FDA approved on August 22, 2008.

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) Immune thrombocytopenia patients, subQ = 3.5 days (median) (range 1-34 days)

Volume Distribusi In healthy volunteers, non-linear decrease in Vd with increase IV dose of romiplostim which indicates saturation of c-Mpl receptors. Vd, 0.3 ?g/kg = 122 mL/kg Vd, 10 ?g/kg = 48.2 mL/kg

Klirens (Clearance) -

Absorpsi

Cmax, healthy volunteers, subQ = 24-36 hours; Cmax, immune thrombocytopenia patients, subQ = 7-50 hours (median = 14 hours). Not affected by age, weight, or gender. Accumulation does not occur after six weekly doses of 3 mcg/kg romiplostim.

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

Renal clearance (more dominant mode of clearance as dose increases) and binding to c-Mpl receptors (dominant mode of clearance at low doses)

Interaksi Obat

8 Data

Cyclophosphamide	The risk or severity of pulmonary toxicity can be increased when Romiplostim is combined with Cyclophosphamide.
Vindesine	The risk or severity of peripheral neuropathy can be increased when Romiplostim is combined with Vindesine.
Vinorelbine	The risk or severity of peripheral neuropathy can be increased when Romiplostim is combined with Vinorelbine.
Vincristine	The risk or severity of peripheral neuropathy can be increased when Romiplostim is combined with Vincristine.
Vinblastine	The risk or severity of peripheral neuropathy can be increased when Romiplostim is combined with Vinblastine.
Vintafolide	The risk or severity of peripheral neuropathy can be increased when Romiplostim is combined with Vintafolide.
Vinflunine	The risk or severity of peripheral neuropathy can be increased when Romiplostim is combined with Vinflunine.
Vincamine	The risk or severity of peripheral neuropathy can be increased when Romiplostim is combined with Vincamine.

Target Protein

Thrombopoietin receptor MPL

Referensi & Sumber

Artikel (PubMed)

PMID: 17925591
Kumagai Y, Fujita T, Ozaki M, Sahashi K, Ohkura M, Ohtsu T, Arai Y, Sonehara Y, Nichol JL: Pharmacodynamics and pharmacokinetics of AMG 531, a thrombopoiesis-stimulating peptibody, in healthy Japanese subjects: a randomized, placebo-controlled study. J Clin Pharmacol. 2007 Dec;47(12):1489-97. Epub 2007 Oct 9.
PMID: 17002262
Rice L: Drug evaluation: AMG-531 for the treatment of thrombocytopenias. Curr Opin Investig Drugs. 2006 Sep;7(9):834-41.
PMID: 22316355
Keating GM: Romiplostim: a review of its use in immune thrombocytopenia. Drugs. 2012 Feb 12;72(3):415-35. doi: 10.2165/11208260-000000000-00000.

Link

Link

Contoh Produk & Brand

Produk: 15 • International brands: 0

Produk

Nplate

Injection, powder, for solution • 250 mcg • Subcutaneous • EU • Approved
Nplate

Powder, for solution • 250 mcg / vial • Subcutaneous • Canada • Approved
Nplate

Injection, powder, for solution • 500 mcg • Subcutaneous • EU • Approved
Nplate

Powder, for solution • 500 mcg / vial • Subcutaneous • Canada • Approved
Nplate

Injection, powder, for solution • 250 mcg • Subcutaneous • EU • Approved
Nplate

Injection, powder, for solution • 500 mcg • Subcutaneous • EU • Approved
Nplate

Injection, powder, for solution • 250 mcg • Subcutaneous • EU • Approved
Nplate

Injection, powder, for solution • 250 mcg • Subcutaneous • EU • Approved

Menampilkan 8 dari 15 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.