Afimoxifene

DB04468

small molecule investigational

Deskripsi

Afimoxifene (4-Hydroxytamoxifen, trade name TamoGel) is a new estrogen inhibitor under investigation for a variety of estrogen-dependent conditions, including cyclic breast pain and gynecomastia. TamoGel is formulated using Enhanced Hydroalcoholic Gel (EHG) Technology. This technology enables percutaneous delivery of drugs that cannot be delivered orally. It is being developed by Ascent Therapeutics.

Struktur Molekul 2D

Berat 387.514
Wujud solid

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

Profil Farmakokinetik

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

Absorpsi

Absorbed following topical application.

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

41 Data
Ospemifene The risk or severity of adverse effects can be increased when Afimoxifene is combined with Ospemifene.
Fluoroestradiol F-18 Afimoxifene may decrease effectiveness of Fluoroestradiol F-18 as a diagnostic agent.
Darbepoetin alfa The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Afimoxifene.
Erythropoietin The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Afimoxifene.
Peginesatide The risk or severity of Thrombosis can be increased when Peginesatide is combined with Afimoxifene.
Methoxy polyethylene glycol-epoetin beta The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Afimoxifene.
Lidocaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Lidocaine.
Ropivacaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Ropivacaine.
Bupivacaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Bupivacaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Cinchocaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Dyclonine.
Procaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Procaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Prilocaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Proparacaine.
Meloxicam The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Meloxicam.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Oxybuprocaine.
Cocaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Cocaine.
Mepivacaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Mepivacaine.
Levobupivacaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Levobupivacaine.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Diphenhydramine.
Benzocaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Benzocaine.
Chloroprocaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Chloroprocaine.
Phenol The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Phenol.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Tetrodotoxin.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Benzyl alcohol.
Capsaicin The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Capsaicin.
Etidocaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Etidocaine.
Articaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Articaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Tetracaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Propoxycaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Pramocaine.
Butamben The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Butamben.
Butacaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Butacaine.
Oxetacaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Quinisocaine.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Afimoxifene.
Ambroxol The risk or severity of methemoglobinemia can be increased when Afimoxifene is combined with Ambroxol.
Etrasimod The risk or severity of immunosuppression can be increased when Afimoxifene is combined with Etrasimod.

Target Protein

Estrogen receptor ESR1
Trefoil factor 1 TFF1
Steroid hormone receptor ERR1 ESRRA
Nuclear receptor subfamily 1 group I member 2 NR1I2
Sex hormone-binding globulin SHBG
Estrogen receptor beta ESR2
Estrogen-related receptor gamma ESRRG

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17646931
    Bollig A, Xu L, Thakur A, Wu J, Kuo TH, Liao JD: Regulation of intracellular calcium release and PP1alpha in a mechanism for 4-hydroxytamoxifen-induced cytotoxicity. Mol Cell Biochem. 2007 Nov;305(1-2):45-54. Epub 2007 Jul 24.
  • PMID: 17351746
    Mansel R, Goyal A, Nestour EL, Masini-Eteve V, O'Connell K: A phase II trial of Afimoxifene (4-hydroxytamoxifen gel) for cyclical mastalgia in premenopausal women. Breast Cancer Res Treat. 2007 Dec;106(3):389-97. Epub 2007 Mar 10.
  • PMID: 17203231
    Leblanc K, Sexton E, Parent S, Belanger G, Dery MC, Boucher V, Asselin E: Effects of 4-hydroxytamoxifen, raloxifene and ICI 182 780 on survival of uterine cancer cell lines in the presence and absence of exogenous estrogens. Int J Oncol. 2007 Feb;30(2):477-87.
  • PMID: 16120301
    Cardoso CM, Almeida LM, Custodio JB: 4-Hydroxytamoxifen is a potent inhibitor of the mitochondrial permeability transition. Mitochondrion. 2002 Oct;1(6):485-95.

Contoh Produk & Brand

Produk: 0 • International brands: 1
International Brands
  • Tamogel

Sekuens Gen/Protein (FASTA)

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