Ospemifene: structure in first source
ospemifene : An organochlorine compound that is a selective estrogen receptor modulator; used for treatment of dyspareunia.
ID Source | ID |
---|---|
PubMed CID | 3036505 |
CHEMBL ID | 2105395 |
CHEBI ID | 73275 |
SCHEMBL ID | 948118 |
MeSH ID | M0305127 |
Synonym |
---|
ospemifene |
ophena |
fc-1271a |
senshio |
osphena |
z-2-(4-(4-chloro-1,2-diphenyl-but-1-enyl)phenoxy)ethanol |
osphena (tn) |
ospemifene (inn/usan/ban) |
128607-22-7 |
D08958 |
b0p231ilbk , |
fc-1271 |
unii-b0p231ilbk |
ccris 9205 |
2-(p-((z)-4-chloro-1,2-diphenyl-1-butenyl)phenoxy)ethanol |
2-(4-(4-chloro-1,2-diphenyl-but-1-enyl)phenoxy)ethanol |
hsdb 8281 |
deamino-hydroxytoremifene |
ospemifene [usan:inn:ban] |
chebi:73275 , |
(deaminohydroxy) toremifene |
tore iii |
CHEMBL2105395 |
S4285 |
2-{4-[(1z)-4-chloro-1,2-diphenylbut-1-en-1-yl]phenoxy}ethanol |
ospemifene [who-dd] |
ospemifene [mart.] |
ethanol, 2-(4-((1z)-4-chloro-1,2-diphenyl-1-butenyl)phenoxy)- |
ospemifene [vandf] |
ospemifene [inn] |
ospemifene [mi] |
ospemifene [usan] |
ospemifene [orange book] |
2-[4-[(z)-4-chloro-1,2-di(phenyl)but-1-enyl]phenoxy]ethanol |
gtpl7349 |
DB04938 |
LUMKNAVTFCDUIE-VHXPQNKSSA-N |
z-2-[4-(4-chloro-1,2-diphenyl-but-1-enyl)-phenoxy]-ethanol |
SCHEMBL948118 |
ethanol, 2-[4-[(1z)-4-chloro-1,2-diphenyl-1-butenyl]phenoxy]- |
AC-27645 |
O0441 |
AKOS025401964 |
J-005613 |
HY-B0723 |
ethanol, 2-[4-[(1z)-4-chloro-1,2-diphenyl-1-buten-1-yl]phenoxy]- |
CS-5961 |
SW219657-1 |
BCP20981 |
mfcd00871890 |
Q7107372 |
A14261 |
ospemifene, fc-1271a |
CCG-268392 |
NCGC00386347-01 |
DTXSID101025426 |
ospemifeno |
ospemifene (mart.) |
g03xc05 |
2-(4-((1z)-4-chloro-1,2-diphenylbut-1-en-1-yl)phenoxy)ethanol |
ospemifenum |
2-{4-[(1z)-4-chloro-1,2-diphenylbut-1-en-1-yl]phenoxy}ethan-1-ol |
EN300-21702760 |
Ospemifene is a novel selective estrogen receptor modulator developed for the treatment of moderate to severe postmenopausal vulvovaginal atrophy (VVA) The drug has been shown to be effective in women with VVA and dyspareunia, vaginal dryness and vulvar vestibular symptoms.
Excerpt | Reference | Relevance |
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"Ospemifene is a selective estrogen receptor modulator licensed for the treatment of VVA." | ( Effects of ospemifene on overactive bladder in postmenopausal women with vulvovaginal atrophy. Giannini, A; Misasi, G; Montt-Guevara, MM; Russo, E; Simoncini, T, 2023) | 2.02 |
"Ospemifene is a novel selective estrogen receptor modulator developed for the treatment of moderate to severe postmenopausal vulvovaginal atrophy (VVA)." | ( Efficacy, tolerability, and endometrial safety of ospemifene compared with current therapies for the treatment of vulvovaginal atrophy: a systematic literature review and network meta-analysis. Beauchemin, C; Black, D; Castonguay, A; Ferenczy, A; Marouf, R; Royer, C; Simon, JA, 2023) | 2.61 |
"Ospemifene is an efficacious, well-tolerated, and safe therapeutic option for postmenopausal women with moderate to severe symptoms of VVA. " | ( Efficacy, tolerability, and endometrial safety of ospemifene compared with current therapies for the treatment of vulvovaginal atrophy: a systematic literature review and network meta-analysis. Beauchemin, C; Black, D; Castonguay, A; Ferenczy, A; Marouf, R; Royer, C; Simon, JA, 2023) | 2.61 |
"Ospemifene is a third-generation Selective Estrogen Receptor Modulator (SERM) that has been shown to be effective in women with VVA and dyspareunia, vaginal dryness and vulvar vestibular symptoms." | ( Ospemifene efficacy and safety data in women with vulvovaginal atrophy. Pup, LD; Sánchez-Borrego, R, 2020) | 2.72 |
"Ospemifene is a cost-effective intervention that has recently been accepted by the SMC for the treatment of postmenopausal women with moderate to severe VVA who are not candidates for local oestrogen." | ( Economic Evaluation of Senshio Craig, J; Davies, H; Dymond, A; Holmes, H; McMaster, J; Mealing, S; Perard, R, 2021) | 2.06 |
"Ospemifene is a nonsteroidal selective estrogen receptor modulator (SERM) for the treatment of moderate symptomatic vulvar and vaginal atrophy (VVA) due to menopause. " | ( Incidence of venous thromboembolism among postmenopausal women prescribed ospemifene, selective estrogen receptor modulators for noncancer indications, or untreated vulvar and vaginal atrophy. Cai, B; De Gregorio, F; Dhalwani, N; Fraeman, KH; Gibbs, T; Nordstrom, BL; Yoshida, Y, 2020) | 2.23 |
"Ospemifene is an oral daily drug, which has proven to treat vaginal dryness and dyspareunia effectively." | ( Clinical profile of women with vulvar and vaginal atrophy who are not candidates for local vaginal estrogen therapy. Biglia, N; Murina, F; Nappi, RE; Perrone, G; Villa, P, 2017) | 1.18 |
"Ospemifene is an effective potential therapy for postmenopausal women with VVA improving OAB symptoms and quality of life." | ( Retrospective analysis in 46 women with vulvovaginal atrophy treated with ospemifene for 12 weeks: improvement in overactive bladder symptoms. Benedetti Panici, P; Colagiovanni, V; D'Oria, O; Di Donato, V; Di Tucci, C; Faiano, P; Giannini, A; Monti, M; Muzii, L; Perniola, G; Prata, G; Schiavi, MC; Zullo, MA, 2017) | 2.13 |
"Ospemifene is a valid alternative with excellent tolerability for the UTI" | ( Prevention of recurrent lower urinary tract infections in postmenopausal women with genitourinary syndrome: outcome after 6 months of treatment with ospemifene. Benedetti Panici, P; Carraro, C; D'oria, O; Di Pinto, A; Di Tucci, C; Faiano, P; Martoccia, A; Muzii, L; Ostuni, R; Prata, G; Schiavi, MC; Sciuga, V; Zullo, MA, 2018) | 1.4 |
"Ospemifene is an effective potential therapy for postmenopausal women with VVA affected by OAB or UUI improving sexual function and quality of life." | ( Overactive bladder syndrome treatment with ospemifene in menopausal patients with vulvovaginal atrophy: improvement of sexuality? Aleksa, N; Benedetti Panici, P; Capone, C; D'oria, O; Di Mascio, D; Di Tucci, C; Giannini, A; Meggiorini, ML; Monti, M; Muzii, L; Prata, G; Savone, D; Schiavi, MC; Sciuga, V; Vena, F; Zullo, MA, 2018) | 1.46 |
"Ospemifene is a selective estrogen-receptor modulator approved for treating menopause-related moderate to severe dyspareunia and vaginal dryness, symptoms of vulvovaginal atrophy (VVA), in the United States, and for treating menopause-related, symptomatic VVA in women not appropriate for local estrogen therapy in Europe. " | ( Effects of ospemifene on bone in postmenopausal women. Altomare, C; de Villiers, TJ; Gambacciani, M; Particco, M, 2019) | 2.35 |
"Ospemifene (Osphena™) is an oral selective estrogen receptor modulator (SERM), with tissue-specific estrogenic agonist/antagonist effects. " | ( Ospemifene: first global approval. Elkinson, S; Yang, LP, 2013) | 3.28 |
"Ospemifene is a unique tissue-selective estrogen agonist/antagonist (also known as a selective estrogen receptor modulator [SERM]) with demonstrated efficacy in Phase 3 studies of postmenopausal women with vulvar and vaginal atrophy (VVA). " | ( Vaginal effects of ospemifene in the ovariectomized rat preclinical model of menopause. Kari, S; Lammintausta, R; Unkila, M; Yatkin, E, 2013) | 2.16 |
"Ospemifene is a tissue-selective estrogen agonist/antagonist (a selective estrogen receptor modulator) recently approved by the US Food and Drug Administration for treatment of dyspareunia, a symptom of VVA, due to menopause." | ( Profile of ospemifene in the breast. Berga, SL, 2013) | 1.5 |
"Ospemifene is a non-estrogen agent that exerts tissue-specific estrogen agonistic and weak antagonistic effects (i. e., is a selective estrogen receptor modulator [SERM]). " | ( Effects of the selective estrogen receptor modulator ospemifene on bone in rats. Härkönen, P; Kangas, L; Peng, Z; Väänänen, K, 2014) | 2.09 |
"Ospemifene is a nonestrogen tissue-selective estrogen agonist/antagonist approved to treat moderate to severe dyspareunia due to vulvar and vaginal atrophy in postmenopausal women. " | ( The effect of renal and hepatic impairment on the pharmacokinetics of ospemifene, a tissue-selective estrogen agonist/antagonist. Graham, S; Marbury, TC; Preston, RA; Wajima, T, ) | 1.81 |
"Ospemifene is a new oral estrogen receptor agonist/antagonist with tissue-selective effects approved for the treatment of moderate to severe dyspareunia, a symptom of postmenopausal vulvar and vaginal atrophy (VVA)." | ( Assessment of ospemifene or lubricants on clinical signs of VVA. Constantine, G; Graham, S; Kingsberg, SA; Koltun, WD, 2014) | 2.21 |
"Ospemifene is a tissue-selective estrogen agonist/antagonist that was recently approved for the treatment of dyspareunia associated with vulvar and vaginal atrophy, which occurs in up to approximately 50% of postmenopausal women. " | ( Effects of ospemifene on breast tissue morphology and proliferation: a comparative study versus other selective estrogen receptor modulators in ovariectomized rats. Eigéliené, N; Härkönen, P; Kangas, L; Keskitalo, J; Väänänen, K, 2014) | 2.23 |
"Ospemifene is a new oral estrogen receptor agonist/antagonist indicated for moderate to severe dyspareunia. " | ( Ospemifene in the treatment of vulvovaginal atrophy. Barnes, KN; Forinash, AB; Pearce, EF; Yancey, AM, 2014) | 3.29 |
"Ospemifene is a third-generation selective estrogen receptor modulator (SERM), structurally closely related to toremifene. " | ( Ospemifene for the treatment of dyspareunia in postmenopausal women. Paton, DM, 2014) | 3.29 |
"Ospemifene is a selective estrogen receptor modulator (SERM) approved for the treatment of dyspareunia associated with vulvar and vaginal atrophy (VVA) due to menopause. " | ( Ospemifene: a first-in-class, non-hormonal selective estrogen receptor modulator approved for the treatment of dyspareunia associated with vulvar and vaginal atrophy. DeGregorio, MW; Wurz, GT; Zerbe, RL, 2014) | 3.29 |
"Ospemifene is a non-estrogen, tissue selective estrogen receptor agonist/antagonist, or selective estrogen receptor modulator, recently approved for the treatment of dyspareunia, a symptom of vulvar and vaginal atrophy (VVA), due to menopause. " | ( Female sexual function improved with ospemifene in postmenopausal women with vulvar and vaginal atrophy: results of a randomized, placebo-controlled trial. Constantine, G; Graham, S; Kingsberg, SA; Portman, DJ; Rosen, RC, 2015) | 2.13 |
"Ospemifene is a novel, oral selective estrogen receptor modulator that has been approved in the USA for treatment of dyspareunia. " | ( Ospemifene: a novel selective estrogen receptor modulator for treatment of dyspareunia. Eder, SE, 2014) | 3.29 |
"Ospemifene is a non-steroidal estrogen receptor agonist/antagonist, also known as a selective estrogen receptor modulator (SERM), from the same chemical class as the breast cancer drugs tamoxifen and toremifene." | ( Safety and efficacy of ospemifene for the treatment of dyspareunia associated with vulvar and vaginal atrophy due to menopause. DeGregorio, MW; Kao, CJ; Wurz, GT, 2014) | 1.43 |
"Ospemifene is a nonhormonal, estrogen receptor agonist/antagonist (ERAA) FDA-approved for the treatment of moderate to severe dyspareunia, a symptom of VVA, due to menopause." | ( Ospemifene for the treatment of postmenopausal vulvar and vaginal atrophy: recommendations for clinical use. Kagan, R; Pinkerton, JV, 2015) | 2.58 |
"Ospemifene is an approved oral option for postmenopausal women seeking treatment for VVA with bothersome dyspareunia, particularly for those who have tried and failed over-the-counter options or do not want vaginal therapies. " | ( Ospemifene for the treatment of postmenopausal vulvar and vaginal atrophy: recommendations for clinical use. Kagan, R; Pinkerton, JV, 2015) | 3.3 |
"Ospemifene is an estrogen-receptor agonist/antagonist (also known as a selective estrogen-receptor modulator) that is FDA approved for the treatment of moderate-to-severe dyspareunia, a symptom of vulvovaginal atrophy, due to menopause. " | ( Effects of ospemifene on bone parameters including clinical biomarkers in postmenopausal women. Constantine, GD; Kagan, R; Miller, PD, 2016) | 2.27 |
"Ospemifene (Osp) is a novel selective estrogen-receptor modulator (SERM) accepted for the treatment of dyspareunia, a symptom of postmenopausal vulvovaginal atrophy. " | ( Effects of ospemifene, a novel selective estrogen-receptor modulator, on human breast tissue ex vivo. Eigeliene, N; Erkkola, R; Härkönen, P; Hellmer, C; Kangas, L; Kauko, T, 2016) | 2.27 |
"Ospemifene is a selective estrogen receptor modulator recently approved by the FDA for the treatment postmenopausal women experiencing moderate-to-severe dyspareunia and by the EMA for the treatment of moderate-to-severe symptomatic genitourinary syndrome of menopause (GSM) in women who are not suitable candidates for local vaginal estrogen therapy." | ( Pharmacokinetics, pharmacodynamics and clinical efficacy of ospemifene for the treatment of dyspareunia and genitourinary syndrome of menopause. Bondi, C; Ferrero, S; Leone Roberti Maggiore, U; Racca, A; Scala, C; Tafi, E; Venturini, PL, 2016) | 2.12 |
"Ospemifene is a non-hormonal estrogen receptor agonist/antagonist effective in the treatment of VVA." | ( Pharmacologic evaluation of ospemifene. DeGregorio, MW; McCall, JL, 2010) | 1.38 |
"Ospemifene is a new, non-hormonal selective estrogen receptor modulator (SERM) triphenylethylene derivative that is effective in treating VVA in postmenopausal women." | ( Ospemifene, vulvovaginal atrophy, and breast cancer. DeGregorio, MW; Soe, LH; Wurz, GT, 2013) | 2.55 |
"Ospemifene (FC-1271a) is a novel SERM compound, which has been shown in animal models to have estrogen-like effects on bone and the cardiovascular system, while having antiestrogen-like effects in uterus and breast." | ( Effects of ospemifene (FC-1271a) on uterine endometrium, vaginal maturation index, and hormonal status in healthy postmenopausal women. DeGregorio, MW; Erkkola, RU; Halonen, K; Kangas, L; Komi, J; Voipio, SK, 2002) | 1.43 |
"Ospemifene is a novel selective estrogen receptor modulator (SERM). " | ( Effects of ospemifene, a novel SERM, on biochemical markers of bone turnover in healthy postmenopausal women. Halonen, K; Heikkinen, J; Komi, J; Lammintausta, R; Rutanen, EM; Ylikorkala, O, 2004) | 2.16 |
"Ospemifene is a new selective estrogen receptor modulator (SERM) that is being developed for the treatment of urogenital atrophy and osteoporosis. " | ( Ospemifene inhibits the growth of dimethylbenzanthracene-induced mammary tumors in Sencar mice. Beckett, LA; Degregorio, MW; Gregg, JP; Marchisano-Karpman, C; Read, KC; Wurz, GT; Yu, Q, 2005) | 3.21 |
"Ospemifene is a novel selective estrogen receptor modulator (SERM) that is initially being developed for the treatment of vaginal atrophy in postmenopausal women. " | ( Effects of ospemifene and raloxifene on biochemical markers of bone turnover in postmenopausal women. DeGregorio, M; Erkkola, R; Halonen, K; Heikkinen, J; Komi, J; Lammintausta, R; Lankinen, KS; Saarikoski, S; Tuppurainen, M; Väänänen, K; Ylikorkala, O, 2006) | 2.17 |
"Ospemifene (Ophena) is a new selective oestrogen receptor modulator currently in phase III clinical development for treatment of post-menopausal vulvar and vaginal atrophy. " | ( Pharmacologic effects of ospemifene in rhesus macaques: a pilot study. DeGregorio, MW; Hellmann-Blumberg, U; Wurz, GT, 2008) | 2.09 |
"Ospemifene (FC-1271a) is a novel selective estrogen receptor modulator under development for osteoporosis prevention. " | ( In vitro and in vivo biologic effects of Ospemifene (FC-1271a) in breast cancer. DeGregorio, MW; Taras, TL; Wurz, GT, 2001) | 2.02 |
Ospemifene has been shown to reverse changes associated with vulvovaginal atrophy and relieve symptoms of dyspareunia. No studies comparing ospem ifene with estrogen products exist.
Excerpt | Reference | Relevance |
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"Ospemifene has been authorized for the treatment of vulvovaginal atrophy (VVA). " | ( A real-world disproportionality analysis of ospemifene: data mining of the public version of FDA adverse event reporting system. Lu, C; Qi, X; Wen, H; Zhang, M, ) | 1.84 |
"Ospemifene has been effective in improving symptoms of vulvovaginal atrophy when compared with placebo; however, no studies comparing ospemifene with estrogen products exist. " | ( Ospemifene in the treatment of vulvovaginal atrophy. Barnes, KN; Forinash, AB; Pearce, EF; Yancey, AM, 2014) | 3.29 |
"Ospemifene has been shown to reverse changes associated with vulvovaginal atrophy and relieve symptoms of dyspareunia." | ( Ospemifene: a novel selective estrogen receptor modulator for treatment of dyspareunia. Eder, SE, 2014) | 2.57 |
Excerpt | Reference | Relevance |
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"Ospemifene does not increase the incidence of endometrial cancer or hyperplasia." | ( Ospemifene efficacy and safety data in women with vulvovaginal atrophy. Pup, LD; Sánchez-Borrego, R, 2020) | 2.72 |
Ospemifene treatment was statistically associated with a greater endometrial thickness in women with an intact uterus. Treatment with ospemfene was associated with an additional cost of £847 per patient and an increase in quality-adjusted life-years (QALY) of 0.06.
Excerpt | Reference | Relevance |
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"Ospemifene treatment was statistically associated with a greater endometrial thickness in women with an intact uterus both at 12 weeks (SMD: 0.40, (95% CI 0.17 to 0.63, p < 0.0005) and at 52 weeks (SMD: 0.62, 95% CI 0.23-1.01, p = 0.002); however, this increase was not clinically relevant." | ( Ospemifene for the treatment of vulvar and vaginal atrophy: A meta-analysis of randomized trials. Part II: Evaluation of tolerability and safety. Benedetti Panici, P; D'oria, O; Di Donato, V; Iacobelli, V; Kontopantelis, E; Muzii, L; Schiavi, MC; Simoncini, T, 2019) | 2.68 |
"Ospemifene treatment reduced the loss of bone mineral content and density observed in untreated OVX rats, significantly increased distal femur bone mineral content at 51 weeks at 25 mg/kg dose compared with untreated OVX rats (p<0.01), and significantly increased trabecular bone mineral density of the distal femur and proximal tibia with 1, 5, or 25 mg/kg doses after 52 weeks." | ( Effects of the selective estrogen receptor modulator ospemifene on bone in rats. Härkönen, P; Kangas, L; Peng, Z; Väänänen, K, 2014) | 1.37 |
"Ospemifene prevents and treats estrogen receptor-positive MTag.Tg mammary tumors in this immune-intact mouse model in a dose-dependent fashion. " | ( Ospemifene and 4-hydroxyospemifene effectively prevent and treat breast cancer in the MTag.Tg transgenic mouse model. Bell, KE; Burich, RA; DeGregorio, MW; Greenberg, BE; Griffey, SM; McCall, JL; Mehta, NR; Wurz, GT, 2012) | 3.26 |
"Treatment with ospemifene was associated with an additional cost of £847 per patient and an increase in quality-adjusted life-years (QALY) of 0.06 per patient. " | ( Economic Evaluation of Senshio Craig, J; Davies, H; Dymond, A; Holmes, H; McMaster, J; Mealing, S; Perard, R, 2021) | 0.97 |
"Treatment with ospemifene was consistently associated with greater improvement, substantial improvement or relief in the severity of the most bothersome symptoms of vaginal dryness or dyspareunia compared with placebo." | ( The clinical relevance of the effect of ospemifene on symptoms of vulvar and vaginal atrophy. Bruyniks, N; Castelo-Branco, C; De Villiers, TJ; Nappi, RE; Panay, N; Simon, JA, 2015) | 1.04 |
Ospemifene is not only well tolerated and safe but also reduces bone turnover in postmenopausal women. Available data indicate no safety concerns for breast tissue. Up to 52 weeks of treatment with oral ospem ifene 60 mg/day was safe for the endometrium.
Excerpt | Reference | Relevance |
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" Phase 3 clinical data have shown that bazedoxifene is effective in preventing and treating postmenopausal osteoporosis, without adverse effects on the endometrium or breast." | ( Endometrial safety: a key hurdle for selective estrogen receptor modulators in development. Goldstein, SR; Pinkerton, JV, ) | 0.13 |
" Safety assessments included adverse events, cervical Papanicolaou tests, endometrial histology, endometrial thickness, gynecological examination, breast palpation, mammography, physical examination, and clinical safety laboratory assessments." | ( One-year long-term safety extension study of ospemifene for the treatment of vulvar and vaginal atrophy in postmenopausal women with a uterus. Bachmann, GA; Lin, VH; Radovich, C; Simon, JA, 2013) | 0.65 |
"No clinically significant adverse changes in safety assessments were observed in any treatment group." | ( One-year long-term safety extension study of ospemifene for the treatment of vulvar and vaginal atrophy in postmenopausal women with a uterus. Bachmann, GA; Lin, VH; Radovich, C; Simon, JA, 2013) | 0.65 |
"Daily doses of ospemifene 30 mg and ospemifene 60 mg yielded few treatment-emergent adverse events and demonstrated no significant endometrial changes during the 1-year treatment of vulvar and vaginal atrophy in postmenopausal women with a uterus." | ( One-year long-term safety extension study of ospemifene for the treatment of vulvar and vaginal atrophy in postmenopausal women with a uterus. Bachmann, GA; Lin, VH; Radovich, C; Simon, JA, 2013) | 1 |
"00001), treatment emergent adverse event, discontinuations due to adverse event, and serious adverse event indicated that ospemifene was generally safe." | ( The efficacy and safety of ospemifene in treating dyspareunia associated with postmenopausal vulvar and vaginal atrophy: a systematic review and meta-analysis. Cui, Y; Li, N; Yan, H; Zhang, Y; Zong, H, 2014) | 0.91 |
"This meta-analysis indicates that ospemifene to be an effective and safe treatment for dyspareunia associated with postmenopausal vulvar and vaginal atrophy." | ( The efficacy and safety of ospemifene in treating dyspareunia associated with postmenopausal vulvar and vaginal atrophy: a systematic review and meta-analysis. Cui, Y; Li, N; Yan, H; Zhang, Y; Zong, H, 2014) | 0.98 |
"Safety assessments included adverse events, laboratory studies, physical and gynecologic examination, vital signs, breast palpation, and mammography." | ( Long-term safety of ospemifene (52-week extension) in the treatment of vulvar and vaginal atrophy in hysterectomized postmenopausal women. Mabey, RG; Portman, D; Simon, J, 2014) | 0.73 |
"Most treatment-emergent adverse events (TEAEs) during the extension study were mild or moderate in severity." | ( Long-term safety of ospemifene (52-week extension) in the treatment of vulvar and vaginal atrophy in hysterectomized postmenopausal women. Mabey, RG; Portman, D; Simon, J, 2014) | 0.73 |
"Ospemifene is clinically safe and generally well tolerated in postmenopausal patients with dyspareunia, a symptom of VVA." | ( Long-term safety of ospemifene (52-week extension) in the treatment of vulvar and vaginal atrophy in hysterectomized postmenopausal women. Mabey, RG; Portman, D; Simon, J, 2014) | 2.17 |
"These clinical trial data indicate that up to 52 weeks of treatment with oral ospemifene 60 mg/day was safe for the endometrium." | ( Endometrial safety of ospemifene: results of the phase 2/3 clinical development program. Archer, DF; Constantine, GD; Goldstein, SR, 2015) | 0.96 |
" Safety information in a long-term safety trial was used to assess the potential changes in risk of adverse events with ospemifene-exposure increase." | ( Population pharmacokinetics of ospemifene and safety evaluation of pharmacokinetic alterations caused by intrinsic and extrinsic factors
. Kubota, R; Matsumoto, S; Wajima, T, 2017) | 0.95 |
" The drug appears safe to use in renal impairment, moderate hepatic impairment, and when coadministered with ketoconazole." | ( Population pharmacokinetics of ospemifene and safety evaluation of pharmacokinetic alterations caused by intrinsic and extrinsic factors
. Kubota, R; Matsumoto, S; Wajima, T, 2017) | 0.74 |
"Post hoc analysis of safety data (treatment-emergent adverse events [TEAEs]) pooled from six phase 2 and 3 randomized, double-blind, multicenter placebo-controlled studies, evaluating the effects of ospemifene 60 mg on the breast, cardiovascular system, and bone in postmenopausal women." | ( Overall Safety of Ospemifene in Postmenopausal Women from Placebo-Controlled Phase 2 and 3 Trials. Altomare, C; Cort, S; Jiang, W; Pinkerton, JV; Simon, JA, 2018) | 1 |
" Most women discontinued treatment due to adverse events (AEs): hot flushes, muscle spasms, headache, and vaginal discharge." | ( Overall Safety of Ospemifene in Postmenopausal Women from Placebo-Controlled Phase 2 and 3 Trials. Altomare, C; Cort, S; Jiang, W; Pinkerton, JV; Simon, JA, 2018) | 0.81 |
" Two groups of outcomes were selected: 1) side-effects, including hot flushes, urinary tract infection (UTI), headache, deep venous thrombosis (DVT), coronary heart disease (CHD), cardiovascular event (CVE), discontinuation due to side-effects, serious adverse event (SAE); 2) Safety, in relation to endometrial thickness, vaginal bleeding, breast tenderness, breast and endometrial cancer." | ( Ospemifene for the treatment of vulvar and vaginal atrophy: A meta-analysis of randomized trials. Part II: Evaluation of tolerability and safety. Benedetti Panici, P; D'oria, O; Di Donato, V; Iacobelli, V; Kontopantelis, E; Muzii, L; Schiavi, MC; Simoncini, T, 2019) | 1.96 |
" Safety was assessed by treatment-emergent adverse events (TEAEs) and endometrial biopsies." | ( Efficacy and safety of ospemifene in postmenopausal women with moderate-to-severe vaginal dryness: a phase 3, randomized, double-blind, placebo-controlled, multicenter trial. Altomare, C; Archer, DF; Goldstein, SR; Schaffer, S; Simon, JA; Soulban, G; Sussman, SA; Waldbaum, AS; Yoshida, Y; Zhu, J, 2019) | 0.82 |
" While the efficacy is comparable with that of estrogenic treatments, ospemifene is not only well tolerated and safe but also reduces bone turnover in postmenopausal women, and available data indicate no safety concerns for breast tissue." | ( Ospemifene efficacy and safety data in women with vulvovaginal atrophy. Pup, LD; Sánchez-Borrego, R, 2020) | 2.23 |
" Ospemifene therapy was however superior to laser and vaginal estrogen therapies in ameliorating sexual function, however, it presents a high risk of developing adverse events and endometrial hyperplasia." | ( Efficacy and safety of current therapies for genitourinary syndrome of menopause: A Bayesian network analysis of 29 randomized trials and 8311 patients. Chang, Y; Duan, H; Li, B; Wang, S, 2021) | 1.53 |
"Ospemifene is an efficacious, well-tolerated, and safe therapeutic option for postmenopausal women with moderate to severe symptoms of VVA." | ( Efficacy, tolerability, and endometrial safety of ospemifene compared with current therapies for the treatment of vulvovaginal atrophy: a systematic literature review and network meta-analysis. Beauchemin, C; Black, D; Castonguay, A; Ferenczy, A; Marouf, R; Royer, C; Simon, JA, 2023) | 2.61 |
" This study wasto evaluate adverse events (AEs) associated with ospemifene by data mining the US Food and Drug Administration Adverse Event Reporting System (FAERS)." | ( A real-world disproportionality analysis of ospemifene: data mining of the public version of FDA adverse event reporting system. Lu, C; Qi, X; Wen, H; Zhang, M, ) | 0.63 |
" The investigation turned up a number of anticipated adverse drug reactions (ADRs), and significant unanticipated ADRs linked to eye and renal problems were found, indicating potential side effects not yet included in the prescription instructions." | ( A real-world disproportionality analysis of ospemifene: data mining of the public version of FDA adverse event reporting system. Lu, C; Qi, X; Wen, H; Zhang, M, ) | 0.39 |
Ospemifene was rapidly absorbed, with a median tmax of 1. CYP3A4 is important for ospem ifene metabolism, but other CYP isoforms and metabolic pathways also contribute.
Excerpt | Reference | Relevance |
---|---|---|
" Standard pharmacokinetic parameters were assessed." | ( Pharmacokinetics of (deaminohydroxy)toremifene in humans: a new, selective estrogen-receptor modulator. DeGregorio, MW; Erkkola, RU; Halonen, KH; Huupponen, RK; Taras, TL; Wurz, GT, 2000) | 0.31 |
"The clinical pharmacokinetic findings and in vitro data suggest that CYP3A4 is important for ospemifene metabolism, but other CYP isoforms and metabolic pathways also contribute." | ( Effects of cytochrome P450 inhibitors and inducers on the metabolism and pharmacokinetics of ospemifene. Lammintausta, R; Lehtinen, T; Pelkonen, O; Scheinin, M; Tolonen, A; Turpeinen, M; Uusitalo, J; Vuorinen, J, 2013) | 0.83 |
" Three single-dose, open-label, parallel-group pharmacokinetic studies examined the pharmacokinetics of ospemifene in postmenopausal women with (1) mild hepatic impairment (n = 7), (2) moderate hepatic impairment (n = 8), and (3) severe renal impairment (n = 8) compared with a similar number of matched healthy controls." | ( The effect of renal and hepatic impairment on the pharmacokinetics of ospemifene, a tissue-selective estrogen agonist/antagonist. Graham, S; Marbury, TC; Preston, RA; Wajima, T, ) | 0.58 |
"To develop a population pharmacokinetic (PPK) model to assess factors influencing ospemifene pharmacokinetics and to assess safety for pharmacokinetic alteration observed in drug development." | ( Population pharmacokinetics of ospemifene and safety evaluation of pharmacokinetic alterations caused by intrinsic and extrinsic factors
. Kubota, R; Matsumoto, S; Wajima, T, 2017) | 0.97 |
Excerpt | Reference | Relevance |
---|---|---|
"To assess the effect of concomitant food intake on the relative bioavailability of ospemifene and its main metabolite, 4-hydroxyospemifene, after single oral dosing." | ( Oral bioavailability of ospemifene improves with food intake. Aaltonen, AM; Katila, K; Koskimies, P; Lammintausta, R; Saarni, O; Scheinin, M; Vuorinen, J, 2013) | 0.92 |
" The increase in bioavailability was not linearly related with the fat content of the meal." | ( Oral bioavailability of ospemifene improves with food intake. Aaltonen, AM; Katila, K; Koskimies, P; Lammintausta, R; Saarni, O; Scheinin, M; Vuorinen, J, 2013) | 0.7 |
In healthy postmenopausal women, ospemifene 60 mg/day reached steady state concentrations by Day 7 and showed minimal accumulation of parent drug or its two main metabolites. Overall, there was no clinically important effect of hepatic or renal impairment on the pharmacokinetics of ospamifene.
Excerpt | Relevance | Reference |
---|---|---|
" The prophylactic use of this agent in women susceptible to development of osteoporosis, cardiovascular disease and breast cancer could, therefore, be tested using a once-daily dosing schedule similar to those of other hormone-replacement therapy regimens." | ( Pharmacokinetics of (deaminohydroxy)toremifene in humans: a new, selective estrogen-receptor modulator. DeGregorio, MW; Erkkola, RU; Halonen, KH; Huupponen, RK; Taras, TL; Wurz, GT, 2000) | 0.31 |
" Ospemifene (N = 18), tamoxifen (N = 20) and raloxifene (N = 17), each dosed at 50 mg/kg, were administered daily by oral gavage, in combination with 20 microg DMBA for the first 6 weeks." | ( Ospemifene inhibits the growth of dimethylbenzanthracene-induced mammary tumors in Sencar mice. Beckett, LA; Degregorio, MW; Gregg, JP; Marchisano-Karpman, C; Read, KC; Wurz, GT; Yu, Q, 2005) | 2.68 |
" In the present study, we examined the pharmacokinetics, toxicity, and DNA adduct forming potential of ospemifene in the liver and endometrium of rhesus macaques following single and subchronic dosing schedules to better understand the potential toxicologic effects of ospemifene." | ( Pharmacologic effects of ospemifene in rhesus macaques: a pilot study. DeGregorio, MW; Hellmann-Blumberg, U; Wurz, GT, 2008) | 0.86 |
" Factors that may contribute to poor compliance and persistence with current osteoporosis therapies include drug intolerance, complexity of dosing regimens, and poor understanding of the relative benefit and risk with treatment." | ( Current and emerging pharmacologic therapies for the management of postmenopausal osteoporosis. Lewiecki, EM, 2009) | 0.35 |
" In this study, we test the effects of three dosing levels of ospemifene in both the prevention and treatment of breast cancer in the MTag." | ( Ospemifene and 4-hydroxyospemifene effectively prevent and treat breast cancer in the MTag.Tg transgenic mouse model. Bell, KE; Burich, RA; DeGregorio, MW; Greenberg, BE; Griffey, SM; McCall, JL; Mehta, NR; Wurz, GT, 2012) | 2.06 |
"In healthy postmenopausal women, ospemifene 60 mg/day reached steady state concentrations by Day 7 and showed minimal accumulation of parent drug or its two main metabolites, indicating that once daily dosing is appropriate." | ( Single-dose and steady-state pharmacokinetics of ospemifene, a selective estrogen receptor modulator, in postmenopausal women. Koskimies, P; Lammintausta, R; Scheinin, M; Turunen, J, 2013) | 0.93 |
" Overall, there was no clinically important effect of hepatic or renal impairment on the pharmacokinetics of ospemifene, indicating that dosing does not need to be adjusted in postmenopausal women with mild or moderate hepatic impairment or in subjects with severe renal impairment." | ( The effect of renal and hepatic impairment on the pharmacokinetics of ospemifene, a tissue-selective estrogen agonist/antagonist. Graham, S; Marbury, TC; Preston, RA; Wajima, T, ) | 0.58 |
" The effects of ospemifene (OSP) on the immune response to a peptide cancer vaccine (PV) were evaluated after chronic [control (n = 22); OSP 50 mg/kg (n = 16); PV (n = 6); OSP+PV (n = 11)], intermittent [control (n = 10); OSP 10 and 50 mg/kg (n = 11); PV (n = 11); combination treatment (n = 11 each dose)] and pretreatment [control; OSP 100 mg/kg; PV 100 μg; combination treatment (n = 8 all groups)] ospemifene oral dosing schedules in a total of 317 mixed-sex tumor-bearing and nontumor-bearing mice." | ( Repurposing ospemifene for potentiating an antigen-specific immune response. DeGregorio, MW; Kao, CJ; Lin, YC; Phong, B; Vang, DP; Wurz, GT, 2017) | 1.18 |
" The pretreatment, intermittent, and chronic dosing schedules of ospemifene activate naive T-cells, modulate antigen-induced tolerance and reduce tumor-associated, pro-inflammatory cytokines, respectively." | ( Repurposing ospemifene for potentiating an antigen-specific immune response. DeGregorio, MW; Kao, CJ; Lin, YC; Phong, B; Vang, DP; Wurz, GT, 2017) | 1.07 |
" Therefore, in women with a uterus, it is recommended that physicians prescribe combination therapy only to treat menopausal symptoms such as vasomotor symptoms (hot flashes) and vaginal atrophy, using the smallest effective dosage for the shortest possible duration." | ( Hormone Therapy and Other Treatments for Symptoms of Menopause. Crider, M; Hill, DA; Hill, SR, 2016) | 0.43 |
Role | Description |
---|---|
estrogen receptor modulator | A substance that possess antiestrogenic actions but can also produce estrogenic effects as well. It acts as complete or partial agonist or as antagonist. It can be either steroidal or nonsteroidal in structure. |
antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
anti-inflammatory agent | Any compound that has anti-inflammatory effects. |
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Class | Description |
---|---|
organochlorine compound | An organochlorine compound is a compound containing at least one carbon-chlorine bond. |
aromatic ether | Any ether in which the oxygen is attached to at least one aryl substituent. |
primary alcohol | A primary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has either three hydrogen atoms attached to it or only one other carbon atom and two hydrogen atoms attached to it. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Process | via Protein(s) | Taxonomy |
---|---|---|
virion membrane | Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus |
[Information is prepared from geneontology information from the June-17-2024 release] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1161697 | Cytotoxicity against MEFs assessed as reduction in cell viability up to 100 uM after 48 to 96 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents. |
AID1161698 | Cytotoxicity against human MDA-MB-231 cells assessed as induction of cell death at 25 uM after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents. |
AID1161705 | Induction of cell death in human MCF7 cells at 50 uM after 24 hrs using calcein AM and ethidium homodimer-1 by live/dead assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents. |
AID1161693 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents. |
AID1161694 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents. |
AID1676127 | Antiviral activity against pseudotyped Marburgvirus-Musoke infected in human A549 cells assessed as reduction in viral infection incubated for 48 hrs by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. |
AID1161699 | Cytotoxicity against human MCF7 cells assessed as induction of cell death at 25 uM after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents. |
AID1676125 | Selectivity index, ratio of CC50 for human A549 cells to IC50 for antiviral activity against pseudotyped Ebola virus - Mayinga, Zaire infected in human A549 cells | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. |
AID1161695 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 96 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents. |
AID1161696 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 96 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents. |
AID1676126 | Antiviral activity against pseudotyped Ebola virus - Mayinga, Zaire infected in human A549 cells assessed as reduction in viral infection incubated for 48 hrs by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. |
AID1291365 | Antimigratory activity in human ER-negative MDA-MB-231 cells assessed as cell migration level at 1 uM after 24 hrs by scratch assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Design, synthesis, and anti-breast cancer evaluation of new triarylethylene analogs bearing short alkyl- and polar amino-/amido-ethyl chains. |
AID1291379 | Cytotoxicity against human ER-negative MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Design, synthesis, and anti-breast cancer evaluation of new triarylethylene analogs bearing short alkyl- and polar amino-/amido-ethyl chains. |
AID1676124 | Selectivity index, ratio of CC50 for human A549 cells to IC50 for antiviral activity against pseudotyped Marburgvirus-Musoke infected in human A549 cells | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. |
AID1291378 | Cytotoxicity against human ER-positive MCF7 cells assessed as cell viability after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Design, synthesis, and anti-breast cancer evaluation of new triarylethylene analogs bearing short alkyl- and polar amino-/amido-ethyl chains. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 1 (0.72) | 18.2507 |
2000's | 21 (15.22) | 29.6817 |
2010's | 87 (63.04) | 24.3611 |
2020's | 29 (21.01) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (52.92) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 30 (20.41%) | 5.53% |
Reviews | 50 (34.01%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 4 (2.72%) | 0.25% |
Other | 63 (42.86%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |