Bazedoxifene

DB06401

small molecule approved investigational

Deskripsi

Bazedoxifene is a third generation selective estrogen receptor modulator (SERM), developed by Pfizer following the completion of their takeover of Wyeth Pharmaceuticals. In late 2013, Pfizer received approval for bazedoxifene as part of the combination drug DUAVEE in the prevention (not treatment) of postmenopausal osteoporosis. It is approved in the European Union (marketed in Italy and Spain) and Japan as monotherapy. In 2013, the combination product containing conjugated estrogens and bazedoxifene was approved by the FDA for the treatment of moderate to severe vasomotor symptoms associated with menopause, as well as the prevention of postmenopausal osteoporosis in women.

Struktur Molekul 2D

Berat 470.613
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) ~30 hours.
Volume Distribusi Following intravenous administration of a 3 mg dose of bazedoxifene, the volume of distribution is 14.7 ± 3.9 l/kg.
Klirens (Clearance) The apparent oral clearance of bazedoxifene is approximately 4 to 5 l/h/kg.

Absorpsi

Bazedoxifene is rapidly absorbed with a tmax of approximately 2 hours and exhibits a linear increase in plasma concentrations for single doses from 0.5 mg up to 120 mg and multiple daily doses from 1 mg to 80 mg. The absolute bioavailability of bazedoxifene is approximately 6%.

Metabolisme

Glucuronidation is the major metabolic pathway. After peroral application, bazedoxifene is metabolized by UDP-glucuronosyltransferases (UGTs) to bazedoxifene-4'-glucuronide (M4) and bazedoxifene-5-glucuronide (M5).Little or no cytochrome P450-mediated metabolism is evident. The concentrations of this glucuronide are approximately 10-fold higher than those of unchanged active substance in plasma.

Rute Eliminasi

The major route of elimination of radio-labelled bazedoxifene is the faeces, and less than 1% of the dose is eliminated in urine.

Interaksi Makanan

4 Data
  • 1. Administer calcium supplement. If calcium intake from food is inadequate administer calcium supplements to prevent hypocalcemia.
  • 2. Administer vitamin supplements. If dietary intake of vitamin D is inadequate, then administer vitamin D supplements to avoid deficiency of vitamin D and calcium.
  • 3. Take at the same time every day.
  • 4. Take with or without food. Taking bazedoxifene with food may increase its AUC by 25% but does not impact the Cmax.

Interaksi Obat

55 Data
Phenytoin The serum concentration of Bazedoxifene can be decreased when it is combined with Phenytoin.
Fosphenytoin The serum concentration of Bazedoxifene can be decreased when it is combined with Fosphenytoin.
Ospemifene The risk or severity of adverse effects can be increased when Bazedoxifene is combined with Ospemifene.
Carbamazepine The serum concentration of Bazedoxifene can be decreased when it is combined with Carbamazepine.
Nelfinavir The metabolism of Bazedoxifene can be increased when combined with Nelfinavir.
Desogestrel The metabolism of Bazedoxifene can be increased when combined with Desogestrel.
Zidovudine The metabolism of Bazedoxifene can be increased when combined with Zidovudine.
Ritonavir The metabolism of Bazedoxifene can be increased when combined with Ritonavir.
Lamotrigine The metabolism of Bazedoxifene can be increased when combined with Lamotrigine.
Efavirenz The metabolism of Bazedoxifene can be increased when combined with Efavirenz.
Primidone The metabolism of Bazedoxifene can be increased when combined with Primidone.
Tipranavir The metabolism of Bazedoxifene can be increased when combined with Tipranavir.
Ethinylestradiol The metabolism of Bazedoxifene can be increased when combined with Ethinylestradiol.
Rifampin The metabolism of Bazedoxifene can be increased when combined with Rifampicin.
Phenobarbital The metabolism of Bazedoxifene can be increased when combined with Phenobarbital.
Testosterone propionate The metabolism of Bazedoxifene can be increased when combined with Testosterone propionate.
Adenine The metabolism of Bazedoxifene can be decreased when combined with Adenine.
Indinavir The metabolism of Bazedoxifene can be decreased when combined with Indinavir.
Valproic acid The metabolism of Bazedoxifene can be decreased when combined with Valproic acid.
Amitriptyline The metabolism of Bazedoxifene can be decreased when combined with Amitriptyline.
Indomethacin The metabolism of Bazedoxifene can be decreased when combined with Indomethacin.
Sorafenib The metabolism of Bazedoxifene can be decreased when combined with Sorafenib.
Erlotinib The metabolism of Bazedoxifene can be decreased when combined with Erlotinib.
Flurbiprofen The metabolism of Bazedoxifene can be decreased when combined with Flurbiprofen.
Propofol The metabolism of Bazedoxifene can be decreased when combined with Propofol.
Ketoconazole The metabolism of Bazedoxifene can be decreased when combined with Ketoconazole.
Probenecid The metabolism of Bazedoxifene can be decreased when combined with Probenecid.
Atazanavir The metabolism of Bazedoxifene can be decreased when combined with Atazanavir.
Gemfibrozil The metabolism of Bazedoxifene can be decreased when combined with Gemfibrozil.
Flunitrazepam The metabolism of Bazedoxifene can be decreased when combined with Flunitrazepam.
Deferasirox The metabolism of Bazedoxifene can be decreased when combined with Deferasirox.
Nilotinib The metabolism of Bazedoxifene can be decreased when combined with Nilotinib.
Eltrombopag The metabolism of Bazedoxifene can be decreased when combined with Eltrombopag.
Pazopanib The metabolism of Bazedoxifene can be decreased when combined with Pazopanib.
Regorafenib The metabolism of Bazedoxifene can be decreased when combined with Regorafenib.
Dasabuvir The metabolism of Bazedoxifene can be decreased when combined with Dasabuvir.
Sodium aurothiomalate The metabolism of Bazedoxifene can be decreased when combined with Sodium aurothiomalate.
Ombitasvir The metabolism of Bazedoxifene can be decreased when combined with Ombitasvir.
Paritaprevir The metabolism of Bazedoxifene can be decreased when combined with Paritaprevir.
Silibinin The metabolism of Bazedoxifene can be decreased when combined with Silibinin.
Dacomitinib The metabolism of Bazedoxifene can be decreased when combined with Dacomitinib.
Fostamatinib The metabolism of Bazedoxifene can be decreased when combined with Fostamatinib.
Enasidenib The metabolism of Bazedoxifene can be decreased when combined with Enasidenib.
Pibrentasvir The metabolism of Bazedoxifene can be decreased when combined with Pibrentasvir.
Glecaprevir The metabolism of Bazedoxifene can be decreased when combined with Glecaprevir.
Pexidartinib The metabolism of Bazedoxifene can be decreased when combined with Pexidartinib.
Idelalisib The metabolism of Bazedoxifene can be decreased when combined with Idelalisib.
Methylene blue The metabolism of Bazedoxifene can be decreased when combined with Methylene blue.
Fluoroestradiol F-18 Bazedoxifene may decrease effectiveness of Fluoroestradiol F-18 as a diagnostic agent.
Asciminib The metabolism of Bazedoxifene can be decreased when combined with Asciminib.
Mitapivat The metabolism of Bazedoxifene can be increased when combined with Mitapivat.
Dabrafenib The metabolism of Bazedoxifene can be decreased when combined with Dabrafenib.
Quizartinib The metabolism of Bazedoxifene can be decreased when combined with Quizartinib.
Repotrectinib The metabolism of Bazedoxifene can be decreased when combined with Repotrectinib.
Encorafenib The metabolism of Bazedoxifene can be decreased when combined with Encorafenib.

Target Protein

Estrogen receptor ESR1
Estrogen receptor beta ESR2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 15535430
    Gruber C, Gruber D: Bazedoxifene (Wyeth). Curr Opin Investig Drugs. 2004 Oct;5(10):1086-93.
  • PMID: 18072873
    Miller PD, Chines AA, Christiansen C, Hoeck HC, Kendler DL, Lewiecki EM, Woodson G, Levine AB, Constantine G, Delmas PD: Effects of bazedoxifene on BMD and bone turnover in postmenopausal women: 2-yr results of a randomized, double-blind, placebo-, and active-controlled study. J Bone Miner Res. 2008 Apr;23(4):525-35.

Contoh Produk & Brand

Produk: 10 • International brands: 1
Produk
  • Conbriza
    Tablet, film coated • 20 mg • Oral • EU • Approved
  • Conbriza
    Tablet, film coated • 20 mg • Oral • EU • Approved
  • Conbriza
    Tablet, film coated • 20 mg • Oral • EU • Approved
  • Conbriza
    Tablet, film coated • 20 mg • Oral • EU • Approved
  • Conbriza
    Tablet, film coated • 20 mg • Oral • EU • Approved
  • Duavee
    Tablet, film coated • - • Oral • US • Approved
  • Duavee
    Tablet, film coated • - • Oral • US • Approved
  • Duavee
    Tablet, film coated • - • Oral • US • Approved
Menampilkan 8 dari 10 produk.
International Brands
  • Viviant

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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