Peringatan Keamanan

Adverse reactions (?1 percent) include: hot flush, vaginal discharge, muscle spasms, genital discharge, hyperhidrosis.

Ospemifene

DB04938

small molecule approved investigational

Deskripsi

Ospemifene is a new selective non-hormonal estrogen receptor modulator (SERM) that is used for the treatment of moderate to severe dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause. FDA approved on February 26, 2013.

Struktur Molekul 2D

Berat 378.891
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Terminal half-life = 26 hours .
Volume Distribusi 448 L
Klirens (Clearance) Total body clearance = 9.16 L/hr.

Absorpsi

When a single oral dose of ospemifene 60 mg is given to postmenopausal women under fasted conditions, the pharmacokinetic parameters are as follows: Tmax = 2 hours (range of 1 - 8 hours); Cmax = 533 ng/mL; AUC (0-inf) = 4165 ng•hr/mL. When the same aforementioned dose is given to postmenopausal women under fed conditions, the pharmacokinetic parameters are as follows: Tmax = 2.5 hours (1 - 6 hours); Cmax = 1198 ng/mL; AUC (0-inf) = 7521 ng•hr/mL. Accumulation occurs following repeated doses. Time to steady state = 9 days. Although the bioavailability of ospemifene has not been formally evaluated, it is expected to have a low bioavailability because of its lipophilic nature.

Metabolisme

Ospemifene is hepatically metabolized via CYP3A4, CYP2C9, CYP2C19, and CYP2B6. The major metabolite was 4-hydroxyospemifene, 25% of the parent compound will undergo this biotransformation. Other metabolites include 4'-hydroxy-ospemifene, <7% of the parent compound will undergo this biotransformation. In order of decreasing potency, ospemifene was suggested to be a weak inhibitor for CYP2B6, CYP2C9, CYP2C19, CYP2C8, CYP2D6 and CYP3A4.

Rute Eliminasi

Following an oral administration of ospemifene, approximately 75% and 7% of the dose was excreted in feces and urine, respectively. Less than 0.2% of the ospemifene dose was excreted unchanged in urine.

Interaksi Makanan

1 Data
  • 1. Take with food.

Interaksi Obat

631 Data
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Ospemifene.
Raloxifene The risk or severity of adverse effects can be increased when Raloxifene is combined with Ospemifene.
Toremifene The risk or severity of adverse effects can be increased when Toremifene is combined with Ospemifene.
Tamoxifen The risk or severity of adverse effects can be increased when Tamoxifen is combined with Ospemifene.
Clomifene The risk or severity of adverse effects can be increased when Clomifene is combined with Ospemifene.
Fulvestrant The risk or severity of adverse effects can be increased when Fulvestrant is combined with Ospemifene.
Afimoxifene The risk or severity of adverse effects can be increased when Afimoxifene is combined with Ospemifene.
Lasofoxifene The risk or severity of adverse effects can be increased when Lasofoxifene is combined with Ospemifene.
Bazedoxifene The risk or severity of adverse effects can be increased when Bazedoxifene is combined with Ospemifene.
Enclomiphene The risk or severity of adverse effects can be increased when Enclomiphene is combined with Ospemifene.
Ormeloxifene The risk or severity of adverse effects can be increased when Ormeloxifene is combined with Ospemifene.
Cyclofenil The risk or severity of adverse effects can be increased when Cyclofenil is combined with Ospemifene.
Diethylstilbestrol The risk or severity of adverse effects can be increased when Diethylstilbestrol is combined with Ospemifene.
Chlorotrianisene The risk or severity of adverse effects can be increased when Chlorotrianisene is combined with Ospemifene.
Conjugated estrogens The risk or severity of adverse effects can be increased when Conjugated estrogens is combined with Ospemifene.
Estrone The risk or severity of adverse effects can be increased when Estrone is combined with Ospemifene.
Estradiol The risk or severity of adverse effects can be increased when Estradiol is combined with Ospemifene.
Dienestrol The risk or severity of adverse effects can be increased when Dienestrol is combined with Ospemifene.
Ethinylestradiol The risk or severity of adverse effects can be increased when Ethinylestradiol is combined with Ospemifene.
Mestranol The risk or severity of adverse effects can be increased when Mestranol is combined with Ospemifene.
Estriol The risk or severity of adverse effects can be increased when Estriol is combined with Ospemifene.
Estrone sulfate The risk or severity of adverse effects can be increased when Estrone sulfate is combined with Ospemifene.
Quinestrol The risk or severity of adverse effects can be increased when Quinestrol is combined with Ospemifene.
Hexestrol The risk or severity of adverse effects can be increased when Hexestrol is combined with Ospemifene.
Tibolone The risk or severity of adverse effects can be increased when Tibolone is combined with Ospemifene.
Synthetic Conjugated Estrogens, A The risk or severity of adverse effects can be increased when Synthetic Conjugated Estrogens, A is combined with Ospemifene.
Synthetic Conjugated Estrogens, B The risk or severity of adverse effects can be increased when Synthetic Conjugated Estrogens, B is combined with Ospemifene.
Polyestradiol phosphate The risk or severity of adverse effects can be increased when Polyestradiol phosphate is combined with Ospemifene.
Esterified estrogens The risk or severity of adverse effects can be increased when Esterified estrogens is combined with Ospemifene.
Zeranol The risk or severity of adverse effects can be increased when Zeranol is combined with Ospemifene.
Equol The risk or severity of adverse effects can be increased when Equol is combined with Ospemifene.
Promestriene The risk or severity of adverse effects can be increased when Promestriene is combined with Ospemifene.
Methallenestril The risk or severity of adverse effects can be increased when Methallenestril is combined with Ospemifene.
Epimestrol The risk or severity of adverse effects can be increased when Epimestrol is combined with Ospemifene.
Moxestrol The risk or severity of adverse effects can be increased when Moxestrol is combined with Ospemifene.
Estradiol acetate The risk or severity of adverse effects can be increased when Estradiol acetate is combined with Ospemifene.
Estradiol benzoate The risk or severity of adverse effects can be increased when Estradiol benzoate is combined with Ospemifene.
Estradiol cypionate The risk or severity of adverse effects can be increased when Estradiol cypionate is combined with Ospemifene.
Estradiol valerate The risk or severity of adverse effects can be increased when Estradiol valerate is combined with Ospemifene.
Biochanin A The risk or severity of adverse effects can be increased when Biochanin A is combined with Ospemifene.
Formononetin The risk or severity of adverse effects can be increased when Formononetin is combined with Ospemifene.
Estetrol The risk or severity of adverse effects can be increased when Estetrol is combined with Ospemifene.
Fluvoxamine The metabolism of Ospemifene can be decreased when combined with Fluvoxamine.
Troglitazone The metabolism of Ospemifene can be decreased when combined with Troglitazone.
Fluoxetine The metabolism of Ospemifene can be decreased when combined with Fluoxetine.
Nabilone The metabolism of Ospemifene can be decreased when combined with Nabilone.
Imatinib The metabolism of Ospemifene can be decreased when combined with Imatinib.
Mifepristone The metabolism of Ospemifene can be decreased when combined with Mifepristone.
Felbamate The metabolism of Ospemifene can be decreased when combined with Felbamate.
Sulfinpyrazone The metabolism of Ospemifene can be decreased when combined with Sulfinpyrazone.
Iproniazid The metabolism of Ospemifene can be decreased when combined with Iproniazid.
Medical Cannabis The metabolism of Ospemifene can be decreased when combined with Medical Cannabis.
Valproic acid The metabolism of Ospemifene can be decreased when combined with Valproic acid.
Quinidine The metabolism of Ospemifene can be decreased when combined with Quinidine.
Dabrafenib The serum concentration of Ospemifene can be decreased when it is combined with Dabrafenib.
Fluconazole The metabolism of Ospemifene can be decreased when combined with Fluconazole.
Floxuridine The metabolism of Ospemifene can be decreased when combined with Floxuridine.
Nicardipine The metabolism of Ospemifene can be decreased when combined with Nicardipine.
Miconazole The metabolism of Ospemifene can be decreased when combined with Miconazole.
Gemfibrozil The metabolism of Ospemifene can be decreased when combined with Gemfibrozil.
Sulfaphenazole The metabolism of Ospemifene can be decreased when combined with Sulfaphenazole.
Pitolisant The serum concentration of Ospemifene can be decreased when it is combined with Pitolisant.
Aripiprazole The metabolism of Aripiprazole can be decreased when combined with Ospemifene.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be decreased when combined with Ospemifene.
Metreleptin The metabolism of Ospemifene can be increased when combined with Metreleptin.
Ticlopidine The metabolism of Ospemifene can be decreased when combined with Ticlopidine.
Memantine The metabolism of Ospemifene can be decreased when combined with Memantine.
Orphenadrine The metabolism of Ospemifene can be decreased when combined with Orphenadrine.
Rilpivirine The metabolism of Ospemifene can be decreased when combined with Rilpivirine.
Clopidogrel The metabolism of Ospemifene can be decreased when combined with Clopidogrel.
Thiotepa The metabolism of Ospemifene can be decreased when combined with Thiotepa.
Piperaquine The metabolism of Ospemifene can be decreased when combined with Piperaquine.
Nevirapine The metabolism of Ospemifene can be increased when combined with Nevirapine.
Rifabutin The metabolism of Ospemifene can be increased when combined with Rifabutin.
Nicotine The metabolism of Ospemifene can be decreased when combined with Nicotine.
Methadone The metabolism of Ospemifene can be decreased when combined with Methadone.
Clobazam The metabolism of Ospemifene can be decreased when combined with Clobazam.
Mexiletine The metabolism of Ospemifene can be decreased when combined with Mexiletine.
Cinnarizine The metabolism of Ospemifene can be decreased when combined with Cinnarizine.
Diclofenac The metabolism of Ospemifene can be decreased when combined with Diclofenac.
Verapamil The metabolism of Ospemifene can be decreased when combined with Verapamil.
Isoflurane The metabolism of Ospemifene can be decreased when combined with Isoflurane.
Irinotecan The metabolism of Ospemifene can be decreased when combined with Irinotecan.
Propofol The metabolism of Ospemifene can be decreased when combined with Propofol.
Brompheniramine The metabolism of Ospemifene can be decreased when combined with Brompheniramine.
Methylphenobarbital The metabolism of Ospemifene can be decreased when combined with Methylphenobarbital.
Benzphetamine The metabolism of Ospemifene can be decreased when combined with Benzphetamine.
Methoxyflurane The metabolism of Ospemifene can be decreased when combined with Methoxyflurane.
Selegiline The metabolism of Ospemifene can be decreased when combined with Selegiline.
Promethazine The metabolism of Ospemifene can be decreased when combined with Promethazine.
Perhexiline The metabolism of Ospemifene can be decreased when combined with Perhexiline.
Bupropion The metabolism of Ospemifene can be decreased when combined with Bupropion.
Halothane The metabolism of Ospemifene can be decreased when combined with Halothane.
Domperidone The metabolism of Ospemifene can be decreased when combined with Domperidone.
Sevoflurane The metabolism of Ospemifene can be decreased when combined with Sevoflurane.
Antipyrine The metabolism of Ospemifene can be decreased when combined with Antipyrine.
Ethylmorphine The metabolism of Ospemifene can be decreased when combined with Ethylmorphine.
Flunitrazepam The metabolism of Ospemifene can be decreased when combined with Flunitrazepam.
Clotiazepam The metabolism of Ospemifene can be decreased when combined with Clotiazepam.
Lorcaserin The metabolism of Ospemifene can be decreased when combined with Lorcaserin.

Target Protein

Estrogen receptor ESR1

Referensi & Sumber

Synthesis reference: Marja Sodervall, Maire Eloranta, Arja Kalapudas, Brian Kearton, Michael McKenzie, "METHODS FOR THE PREPARATION OF FISPEMIFENE FROM OSPEMIFENE." U.S. Patent US20080214860, issued September 04, 2008.
Artikel (PubMed)
  • PMID: 11457665
    Taras TL, Wurz GT, DeGregorio MW: In vitro and in vivo biologic effects of Ospemifene (FC-1271a) in breast cancer. J Steroid Biochem Mol Biol. 2001 Jun;77(4-5):271-9.
  • PMID: 12443837
    Voipio SK, Komi J, Kangas L, Halonen K, DeGregorio MW, Erkkola RU: Effects of ospemifene (FC-1271a) on uterine endometrium, vaginal maturation index, and hormonal status in healthy postmenopausal women. Maturitas. 2002 Nov 20;43(3):207-14.
  • PMID: 14501605
    Rutanen EM, Heikkinen J, Halonen K, Komi J, Lammintausta R, Ylikorkala O: Effects of ospemifene, a novel SERM, on hormones, genital tract, climacteric symptoms, and quality of life in postmenopausal women: a double-blind, randomized trial. Menopause. 2003 Sep-Oct;10(5):433-9.
  • PMID: 14501606
    Ylikorkala O, Cacciatore B, Halonen K, Lassila R, Lammintausta R, Rutanen EM, Heikkinen J, Komi J: Effects of ospemifene, a novel SERM, on vascular markers and function in healthy, postmenopausal women. Menopause. 2003 Sep-Oct;10(5):440-7.
  • PMID: 23729558
    Tolonen A, Koskimies P, Turpeinen M, Uusitalo J, Lammintausta R, Pelkonen O: Ospemifene metabolism in humans in vitro and in vivo: metabolite identification, quantitation, and CYP assignment of major hydroxylations. Drug Metabol Drug Interact. 2013;28(3):153-61. doi: 10.1515/dmdi-2013-0016.
  • PMID: 20429673
    McCall JL, DeGregorio MW: Pharmacologic evaluation of ospemifene. Expert Opin Drug Metab Toxicol. 2010 Jun;6(6):773-9. doi: 10.1517/17425255.2010.487483.

Contoh Produk & Brand

Produk: 7 • International brands: 0
Produk
  • Osphena
    Tablet, film coated • 60 mg/1 • Oral • US • Approved
  • Osphena
    Tablet, film coated • 60 mg/1 • Oral • US • Approved
  • Osphena
    Tablet, film coated • 60 mg/1 • Oral • US • Approved
  • Osphena
    Tablet • 60 mg • Oral • Canada • Approved
  • Senshio
    Tablet • 60 mg • Oral • EU • Approved
  • Senshio
    Tablet • 60 mg • Oral • EU • Approved
  • Senshio
    Tablet • 60 mg • Oral • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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