Peringatan Keamanan

Because of its cytotoxic actions that have a high potential to cause fetal harm, Radium Ra 223 Dichloride is contraindicated in women who are pregnant or are of child bearing age. Other side effects include several hematological lab abnormalities, peripheral edema, nausea, vomiting, and diarrhea.

Radium Ra 223 dichloride

DB08913

small molecule approved investigational

Deskripsi

Radium Ra 223 Dichloride is a radiopharmaceutical containing the radioisotope radium-223 that emits short range but high linear energy alpha particles. As a cation, radium mimics calicum and binds to hydroxyapatite, which is a bone mineral found in areas of high bone turnover as seen in bone metastases. It was first approved by the FDA in May 2013 and is currently marketed under the brand name Xofigo, which was formerly called Alpharadin. Xofigo is indicated in patients who have metastatic bone cancer that is symptomatic with no visceral metastases and patients who have prostate cancer that is castration resistant. The FDA label includes a warning that Radium Ra 223 Dichloride should not be used in women who are pregnant or may become pregnant due to the high risk of fetal harm.

Struktur Molekul 2D

Berat 293.924

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) The half-life is relatively long at 11.4 days for radium-223.

Volume Distribusi The volume of distribution was not quantified, but after 24 hours, there is only 1% radium-223 remaining in the blood. The rest of the radium-223 is distributed to bone (61% of the radioactive dose after 4 hours) and intestine (49% of the radioactive dose after 4 hours). No other organs were found to have significant uptake.

Klirens (Clearance) The clearance rate of radium-223 was not quantified.

Absorpsi

Since Radium Ra 223 Dichloride is administered I.V., the bioavailability should be 100%.

Metabolisme

Radium-223 does not undergo metabolism because it is a radioisotope that decays.

Rute Eliminasi

Radium-223 is mainly eliminated through the feces (13%) and to a lesser extent in the urine (2%). It is also noted that the elimination rate of radium-223 from the intestines is variable due to the high variability of intestinal transit rates among patients. Therefore there could be more intestinal radiation exposure in patients with slower intestinal transit rates, but the significance of this in relation to toxicity is not known.

Interaksi Makanan

1 Data

1. Drink plenty of fluids.

Interaksi Obat

38 Data

Darbepoetin alfa	The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Radium Ra 223 dichloride.
Erythropoietin	The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Radium Ra 223 dichloride.
Peginesatide	The risk or severity of Thrombosis can be increased when Peginesatide is combined with Radium Ra 223 dichloride.
Methoxy polyethylene glycol-epoetin beta	The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Radium Ra 223 dichloride.
Lidocaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Lidocaine.
Ropivacaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Ropivacaine.
Bupivacaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Bupivacaine.
Cinchocaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Cinchocaine.
Dyclonine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Dyclonine.
Procaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Procaine.
Prilocaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Prilocaine.
Proparacaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Proparacaine.
Meloxicam	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Meloxicam.
Oxybuprocaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Oxybuprocaine.
Cocaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Cocaine.
Mepivacaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Mepivacaine.
Levobupivacaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Levobupivacaine.
Diphenhydramine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Diphenhydramine.
Benzocaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Benzocaine.
Chloroprocaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Chloroprocaine.
Phenol	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Phenol.
Tetrodotoxin	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Tetrodotoxin.
Benzyl alcohol	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Benzyl alcohol.
Capsaicin	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Capsaicin.
Etidocaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Etidocaine.
Articaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Articaine.
Tetracaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Tetracaine.
Propoxycaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Propoxycaine.
Pramocaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Pramocaine.
Butamben	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Butamben.
Butacaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Butacaine.
Oxetacaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Oxetacaine.
Ethyl chloride	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Ethyl chloride.
Butanilicaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Butanilicaine.
Metabutethamine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Metabutethamine.
Quinisocaine	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Quinisocaine.
Ambroxol	The risk or severity of methemoglobinemia can be increased when Radium Ra 223 dichloride is combined with Ambroxol.
Etrasimod	The risk or severity of immunosuppression can be increased when Radium Ra 223 dichloride is combined with Etrasimod.

Referensi & Sumber

Artikel (PubMed)

PMID: 23682134
Suominen MI, Rissanen JP, Kakonen R, Fagerlund KM, Alhoniemi E, Mumberg D, Ziegelbauer K, Halleen JM, Kakonen SM, Scholz A: Survival benefit with radium-223 dichloride in a mouse model of breast cancer bone metastasis. J Natl Cancer Inst. 2013 Jun 19;105(12):908-16. doi: 10.1093/jnci/djt116. Epub 2013 May 16.
PMID: 17544845
Nilsson S, Franzen L, Parker C, Tyrrell C, Blom R, Tennvall J, Lennernas B, Petersson U, Johannessen DC, Sokal M, Pigott K, Yachnin J, Garkavij M, Strang P, Harmenberg J, Bolstad B, Bruland OS: Bone-targeted radium-223 in symptomatic, hormone-refractory prostate cancer: a randomised, multicentre, placebo-controlled phase II study. Lancet Oncol. 2007 Jul;8(7):587-94.
PMID: 17062709
Bruland OS, Nilsson S, Fisher DR, Larsen RH: High-linear energy transfer irradiation targeted to skeletal metastases by the alpha-emitter 223Ra: adjuvant or alternative to conventional modalities? Clin Cancer Res. 2006 Oct 15;12(20 Pt 2):6250s-6257s.

Contoh Produk & Brand

Produk: 3 • International brands: 1

Produk

Radium Ra 223 Dichloride

Injection • 90 uCi/1mL • Intravenous • US • Approved
Xofigo

Injection • 30 uCi/1mL • Intravenous • US • Approved
Xofigo

Injection, solution • 1100 kBq/mL • Intravenous • EU • Approved

International Brands

Alpharadin

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.