2-Methoxyestradiol

DB02342

small molecule investigational

Deskripsi

2-Methoxyestradiol (2ME2) is a drug that prevents the formation of new blood vessels that tumors need in order to grow (angiogenesis). It has undergone Phase 1 clinical trials against breast cancers and preclinical studies suggest that 2ME2 could also be effective against inflammatory diseases such as rheumatoid arthritis.

Struktur Molekul 2D

Berat 302.4079
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

In vivo metabolism, assessed using 24-h collections of urine from cancer patients treated with 2ME2 revealed that <0.01% of the total administered dose of 2ME2 is excreted unchanged in urine and about 1% excreted as glucuronides. Collectively, this suggests that glucuronidation and subsequent urinary excretion are elimination pathways for 2ME2.

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 2-Methoxyestradiol.
Erythropoietin The risk or severity of Thrombosis can be increased when Erythropoietin is combined with 2-Methoxyestradiol.
Peginesatide The risk or severity of Thrombosis can be increased when Peginesatide is combined with 2-Methoxyestradiol.
Methoxy polyethylene glycol-epoetin beta The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with 2-Methoxyestradiol.
Lidocaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Lidocaine.
Ropivacaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Ropivacaine.
Bupivacaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Bupivacaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Cinchocaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Dyclonine.
Procaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Procaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Prilocaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Proparacaine.
Meloxicam The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Meloxicam.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Oxybuprocaine.
Cocaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Cocaine.
Mepivacaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Mepivacaine.
Levobupivacaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Levobupivacaine.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Diphenhydramine.
Benzocaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Benzocaine.
Chloroprocaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Chloroprocaine.
Phenol The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Phenol.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Tetrodotoxin.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Benzyl alcohol.
Capsaicin The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Capsaicin.
Etidocaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Etidocaine.
Articaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Articaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Tetracaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Propoxycaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Pramocaine.
Butamben The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Butamben.
Butacaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Butacaine.
Oxetacaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Quinisocaine.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with 2-Methoxyestradiol.
Ambroxol The risk or severity of methemoglobinemia can be increased when 2-Methoxyestradiol is combined with Ambroxol.
Etrasimod The risk or severity of immunosuppression can be increased when 2-Methoxyestradiol is combined with Etrasimod.

Target Protein

Hypoxia-inducible factor 1-alpha HIF1A
Catechol O-methyltransferase COMT
Cytochrome P450 1A1 CYP1A1
Cytochrome P450 1B1 CYP1B1
Aromatase CYP19A1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17645459
    Schumacher G, Hoffmann J, Cramer T, Spinelli A, Jacob D, Bahra M, Pratschke J, Pfitzmann R, Schmidt S, Lage H: Antineoplastic activity of 2-methoxyestradiol in human pancreatic and gastric cancer cells with different multidrug-resistant phenotypes. J Gastroenterol Hepatol. 2007 Sep;22(9):1469-73. Epub 2007 Jul 20.
  • PMID: 17631253
    Sutherland TE, Anderson RL, Hughes RA, Altmann E, Schuliga M, Ziogas J, Stewart AG: 2-Methoxyestradiol--a unique blend of activities generating a new class of anti-tumour/anti-inflammatory agents. Drug Discov Today. 2007 Jul;12(13-14):577-84. Epub 2007 Jun 26.
  • PMID: 17415781
    Fong YC, Yang WH, Hsu SF, Hsu HC, Tseng KF, Hsu CJ, Lee CY, Scully SP: 2-methoxyestradiol induces apoptosis and cell cycle arrest in human chondrosarcoma cells. J Orthop Res. 2007 Aug;25(8):1106-14.
  • PMID: 17229934
    Eichenlaub-Ritter U, Winterscheidt U, Vogt E, Shen Y, Tinneberg HR, Sorensen R: 2-methoxyestradiol induces spindle aberrations, chromosome congression failure, and nondisjunction in mouse oocytes. Biol Reprod. 2007 May;76(5):784-93. Epub 2007 Jan 17.
  • PMID: 17252610
    Lakhani NJ, Sparreboom A, Xu X, Veenstra TD, Venitz J, Dahut WL, Figg WD: Characterization of in vitro and in vivo metabolic pathways of the investigational anticancer agent, 2-methoxyestradiol. J Pharm Sci. 2007 Jul;96(7):1821-31.
  • PMID: 16940808
    Lakhani N, Sparreboom A, Venitz J, Dahut WL, Figg WD: Plasma protein binding of the investigational anticancer agent 2-methoxyestradiol. Anticancer Drugs. 2006 Sep;17(8):977-83.
  • PMID: 12587805
    Lakhani NJ, Sarkar MA, Venitz J, Figg WD: 2-Methoxyestradiol, a promising anticancer agent. Pharmacotherapy. 2003 Feb;23(2):165-72.

Contoh Produk & Brand

Produk: 0 • International brands: 3
International Brands
  • Panzem
  • Panzem NCD
  • Pulmolar

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