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| rdf:type
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| http://linked.open...gbank/description
| - 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. (en)
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| http://linked.open...y/drugbank/dosage
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| http://linked.open...generalReferences
| - # 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. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11457665 # 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. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12443837 # 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. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/14501605 # 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. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/14501606 # 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 May 14:1-9. doi: 10.1515/dmdi-2013-0016. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23729558 # 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. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20429673 (en)
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| http://linked.open...gy/drugbank/group
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| http://linked.open...drugbank/halfLife
| - Terminal half-life = 26 hours . (en)
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| http://linked.open...ugbank/indication
| - Ospemifene is used for the treatment of moderate to dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause. (en)
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| sameAs
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| Title
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| adms:identifier
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| http://linked.open...mechanismOfAction
| - Ospemifene is a next generation SERM (selective estrogen receptor modulator) that selectively binds to estrogen receptors and either stimulates or blocks estrogen's activity in different tissue types. It has an agonistic effect on the endometrium. (en)
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| http://linked.open...y/drugbank/patent
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| http://linked.open...outeOfElimination
| - 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. (en)
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| http://linked.open.../drugbank/synonym
| - Deamino-hydroxytoremifene (en)
- FC-1271 (en)
- FC-1271a (en)
- Osphena (en)
- 2-(P-((Z)-4-Chloro-1,2-diphenyl-1-butenyl)phenoxy)ethanol (en)
- 2-(4-(4-Chloro-1,2-diphenyl-but-1-enyl)phenoxy)ethanol (en)
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| http://linked.open...drugbank/toxicity
| - Adverse reactions (≥1 percent) include: hot flush, vaginal discharge, muscle spasms, genital discharge, hyperhidrosis. (en)
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| http://linked.open...umeOfDistribution
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| http://linked.open.../drug/hasAHFSCode
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| http://linked.open...k/foodInteraction
| - In general, food increased the bioavailability of ospemifene by approximately 2-3 fold. (en)
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| http://linked.open...nk/proteinBinding
| - >99% bound to serum proteins (en)
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| http://linked.open...ynthesisReference
| - 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. (en)
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| foaf:page
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| http://linked.open...ugbank/IUPAC-Name
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| http://linked.open...gy/drugbank/InChI
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| http://linked.open...Molecular-Formula
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| http://linked.open.../Molecular-Weight
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| http://linked.open...noisotopic-Weight
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| http://linked.open...y/drugbank/SMILES
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| http://linked.open.../Water-Solubility
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| http://linked.open...ogy/drugbank/logP
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| http://linked.open...ogy/drugbank/logS
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| http://linked.open...l/drug/hasATCCode
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| http://linked.open...nd-Acceptor-Count
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| http://linked.open...-Bond-Donor-Count
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| http://linked.open...drugbank/InChIKey
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| http://linked.open...urface-Area--PSA-
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| http://linked.open...nk/Polarizability
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| http://linked.open...bank/Refractivity
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| http://linked.open...atable-Bond-Count
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| http://linked.open...ugbank/absorption
| - 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. (en)
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| http://linked.open.../affectedOrganism
| - Humans and other mammals (en)
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| http://linked.open...casRegistryNumber
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| http://linked.open...drugbank/category
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| http://linked.open...rugbank/clearance
| - Total body clearance = 9.16 L/hr. (en)
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| http://linked.open...k/Bioavailability
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| http://linked.open...bank/Ghose-Filter
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| http://linked.open...nk/MDDR-Like-Rule
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| http://linked.open...k/Number-of-Rings
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| http://linked.open...siological-Charge
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| http://linked.open...bank/Rule-of-Five
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| http://linked.open...tional-IUPAC-Name
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| http://linked.open...strongest-acidic-
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| http://linked.open...-strongest-basic-
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