Tirapazamine

DB04858

small molecule investigational

Deskripsi

Tirapazamine, also known as SR-4233, is an experimental anticancer drug that is activated in hypoxic conditions. This activation is very useful as this hypoxic state is found in human solid tumors in a common phenomenon known as tumor hypoxia. Hence, tirapazamine is solely activated in those hypoxic areas of solid tumors. It is important to take into consideration that normally, the cells in these hypoxic regions are resistant to radiotherapy and most anticancer drugs. For all these reasons, the combination of tirapazamine with other anticancer treatments is highly recommended.

Tirapazamine entered phase III testing in 2006 for patients with head and neck cancer and gynecological cancer, as well as for other solid tumor cancer types.

Struktur Molekul 2D

Berat 178.151

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) -

Volume Distribusi -

Klirens (Clearance) -

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

39 Data

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

Target Protein

DNA topoisomerase 2-alpha TOP2A

DNA topoisomerase 2-beta TOP2B

DNA

Referensi & Sumber

Artikel (PubMed)

PMID: 15379691
Denny WA: Prospects for hypoxia-activated anticancer drugs. Curr Med Chem Anticancer Agents. 2004 Sep;4(5):395-9.
PMID: 11894020
Gandara DR, Lara PN Jr, Goldberg Z, Le QT, Mack PC, Lau DH, Gumerlock PH: Tirapazamine: prototype for a novel class of therapeutic agents targeting tumor hypoxia. Semin Oncol. 2002 Feb;29(1 Suppl 4):102-9.
PMID: 3744945
Zeman EM, Brown JM, Lemmon MJ, Hirst VK, Lee WW: SR-4233: a new bioreductive agent with high selective toxicity for hypoxic mammalian cells. Int J Radiat Oncol Biol Phys. 1986 Jul;12(7):1239-42.

Contoh Produk & Brand

Produk: 0 • International brands: 1

International Brands

Tirazone — Sanofi-aventis

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.