Peringatan Keamanan

There is no clinical experience with overdosage in humans.

Fulvestrant

DB00947

small molecule approved investigational

Deskripsi

Fulvestrant is a drug treatment of hormone receptor (HR)-positive metastatic breast cancer in post-menopausal women with disease progression following anti-estrogen therapy. It is an estrogen receptor antagonist with no agonist effects, which works both by down-regulating and by degrading the estrogen receptor. While it is used as monotherapy for the treatment of breast cancers, it is also used in combination with alpelisib for the treatment of HR-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated, advanced or metastatic breast cancer

Struktur Molekul 2D

Berat 606.78
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 40 days
Volume Distribusi * 3 to 5 L/kg
Klirens (Clearance) -

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Metabolism of fulvestrant appears to involve combinations of a number of possible biotransformation pathways analogous to those of endogenous steroids, including oxidation, aromatic hydroxylation, conjugation with glucuronic acid and/or sulphate at the 2, 3 and 17 positions of the steroid nucleus, and oxidation of the side chain sulphoxide. Identified metabolites are either less active or exhibit similar activity to fulvestrant in antiestrogen models. Studies using human liver preparations and recombinant human enzymes indicate that cytochrome P-450 3A4 (CYP 3A4) is the only P-450 isoenzyme involved in the oxidation of fulvestrant; however, the relative contribution of P-450 and non-P-450 routes in vivo is unknown.

Rute Eliminasi

Fulvestrant was rapidly cleared by the hepatobiliary route with excretion primarily via the feces (approximately 90%). Renal elimination was negligible (less than 1%).

Interaksi Obat

90 Data
Ospemifene The risk or severity of adverse effects can be increased when Fulvestrant is combined with Ospemifene.
Desogestrel The metabolism of Fulvestrant can be increased when combined with Desogestrel.
Zidovudine The metabolism of Fulvestrant can be increased when combined with Zidovudine.
Lamotrigine The metabolism of Fulvestrant can be increased when combined with Lamotrigine.
Ethinylestradiol The metabolism of Fulvestrant can be increased when combined with Ethinylestradiol.
Testosterone propionate The metabolism of Fulvestrant can be increased when combined with Testosterone propionate.
Nelfinavir The metabolism of Fulvestrant can be increased when combined with Nelfinavir.
Phenytoin The metabolism of Fulvestrant can be increased when combined with Phenytoin.
Ritonavir The metabolism of Fulvestrant can be increased when combined with Ritonavir.
Carbamazepine The metabolism of Fulvestrant can be increased when combined with Carbamazepine.
Efavirenz The metabolism of Fulvestrant can be increased when combined with Efavirenz.
Primidone The metabolism of Fulvestrant can be increased when combined with Primidone.
Tipranavir The metabolism of Fulvestrant can be increased when combined with Tipranavir.
Rifampin The metabolism of Fulvestrant can be increased when combined with Rifampicin.
Phenobarbital The metabolism of Fulvestrant can be increased when combined with Phenobarbital.
Adenine The metabolism of Fulvestrant can be decreased when combined with Adenine.
Valproic acid The metabolism of Fulvestrant can be decreased when combined with Valproic acid.
Indomethacin The metabolism of Fulvestrant can be decreased when combined with Indomethacin.
Sorafenib The metabolism of Fulvestrant can be decreased when combined with Sorafenib.
Erlotinib The metabolism of Fulvestrant can be decreased when combined with Erlotinib.
Flurbiprofen The metabolism of Fulvestrant can be decreased when combined with Flurbiprofen.
Propofol The metabolism of Fulvestrant can be decreased when combined with Propofol.
Probenecid The metabolism of Fulvestrant can be decreased when combined with Probenecid.
Gemfibrozil The metabolism of Fulvestrant can be decreased when combined with Gemfibrozil.
Flunitrazepam The metabolism of Fulvestrant can be decreased when combined with Flunitrazepam.
Deferasirox The metabolism of Fulvestrant can be decreased when combined with Deferasirox.
Eltrombopag The metabolism of Fulvestrant can be decreased when combined with Eltrombopag.
Pazopanib The metabolism of Fulvestrant can be decreased when combined with Pazopanib.
Regorafenib The metabolism of Fulvestrant can be decreased when combined with Regorafenib.
Dasabuvir The metabolism of Fulvestrant can be decreased when combined with Dasabuvir.
Sodium aurothiomalate The metabolism of Fulvestrant can be decreased when combined with Sodium aurothiomalate.
Ombitasvir The metabolism of Fulvestrant can be decreased when combined with Ombitasvir.
Paritaprevir The metabolism of Fulvestrant can be decreased when combined with Paritaprevir.
Silibinin The metabolism of Fulvestrant can be decreased when combined with Silibinin.
Dacomitinib The metabolism of Fulvestrant can be decreased when combined with Dacomitinib.
Fostamatinib The metabolism of Fulvestrant can be decreased when combined with Fostamatinib.
Enasidenib The metabolism of Fulvestrant can be decreased when combined with Enasidenib.
Pibrentasvir The metabolism of Fulvestrant can be decreased when combined with Pibrentasvir.
Glecaprevir The metabolism of Fulvestrant can be decreased when combined with Glecaprevir.
Pexidartinib The metabolism of Fulvestrant can be decreased when combined with Pexidartinib.
Indinavir The metabolism of Fulvestrant can be decreased when combined with Indinavir.
Amitriptyline The metabolism of Fulvestrant can be decreased when combined with Amitriptyline.
Ketoconazole The metabolism of Fulvestrant can be decreased when combined with Ketoconazole.
Atazanavir The metabolism of Fulvestrant can be decreased when combined with Atazanavir.
Nilotinib The metabolism of Fulvestrant can be decreased when combined with Nilotinib.
Fluoroestradiol F-18 Fulvestrant 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 Fulvestrant.
Erythropoietin The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Fulvestrant.
Peginesatide The risk or severity of Thrombosis can be increased when Peginesatide is combined with Fulvestrant.
Methoxy polyethylene glycol-epoetin beta The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Fulvestrant.
Asciminib The metabolism of Fulvestrant can be decreased when combined with Asciminib.
Mitapivat The metabolism of Fulvestrant can be increased when combined with Mitapivat.
Dabrafenib The metabolism of Fulvestrant can be decreased when combined with Dabrafenib.
Lidocaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Lidocaine.
Ropivacaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Ropivacaine.
Bupivacaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Bupivacaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Cinchocaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Dyclonine.
Procaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Procaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Prilocaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Proparacaine.
Meloxicam The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Meloxicam.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Oxybuprocaine.
Cocaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Cocaine.
Mepivacaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Mepivacaine.
Levobupivacaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Levobupivacaine.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Diphenhydramine.
Benzocaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Benzocaine.
Chloroprocaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Chloroprocaine.
Phenol The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Phenol.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Tetrodotoxin.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Benzyl alcohol.
Capsaicin The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Capsaicin.
Etidocaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Etidocaine.
Articaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Articaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Tetracaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Propoxycaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Pramocaine.
Butamben The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Butamben.
Butacaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Butacaine.
Oxetacaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Quinisocaine.
Ambroxol The risk or severity of methemoglobinemia can be increased when Fulvestrant is combined with Ambroxol.
Quizartinib The metabolism of Fulvestrant can be decreased when combined with Quizartinib.
Etrasimod The risk or severity of immunosuppression can be increased when Fulvestrant is combined with Etrasimod.
Repotrectinib The metabolism of Fulvestrant can be decreased when combined with Repotrectinib.
Encorafenib The metabolism of Fulvestrant can be decreased when combined with Encorafenib.

Target Protein

Estrogen receptor ESR1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 15950373
    Kansra S, Yamagata S, Sneade L, Foster L, Ben-Jonathan N: Differential effects of estrogen receptor antagonists on pituitary lactotroph proliferation and prolactin release. Mol Cell Endocrinol. 2005 Jul 15;239(1-2):27-36.
  • PMID: 20151846
    Kabos P, Borges VF: Fulvestrant: a unique antiendocrine agent for estrogen-sensitive breast cancer. Expert Opin Pharmacother. 2010 Apr;11(5):807-16. doi: 10.1517/14656561003641982.
  • PMID: 12490735
    Bross PF, Cohen MH, Williams GA, Pazdur R: FDA drug approval summaries: fulvestrant. Oncologist. 2002;7(6):477-80.

Contoh Produk & Brand

Produk: 52 • International brands: 0
Produk
  • Act Fulvestrant
    Solution • 50 mg / mL • Intramuscular • Canada • Approved
  • Apo-fulvestrant
    Solution • 50 mg / mL • Intramuscular • Canada • Generic • Approved
  • Faslodex
    Injection • 50 mg/1mL • Intramuscular • US • Approved
  • Faslodex
    Solution • 50 mg / mL • Intramuscular • Canada • Approved
  • Faslodex
    Injection, solution • 250 mg/5ml • Intramuscular • EU • Approved
  • Faslodex
    Injection, solution • 250 mg/5ml • Intramuscular • EU • Approved
  • Fulvestrant
    Injection, solution • 50 mg/1mL • Intramuscular • US • Approved
  • Fulvestrant
    Injection • 250 mg/5mL • Intramuscular • US • Approved
Menampilkan 8 dari 52 produk.

Sekuens Gen/Protein (FASTA)

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