PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 28509812-7 2017 Ospemifene significantly improved fibrinogen and protein C antigen levels relative to placebo at months 3 (-8.7% vs -0.8% and -2.7% vs 0.5%, respectively), 6 (-6.0% vs 6.7% and -3.6 vs 8.0%), and 12 (-8.7% vs 7.3% and -4.5% vs 6.6%; P < 0.01, for all). Ospemifene 0-10 fibrinogen beta chain Homo sapiens 34-44 24055829-5 2013 Ospemifene binds ERalpha and ERbeta with approximately equal affinities. Ospemifene 0-10 estrogen receptor 1 Homo sapiens 17-24 27922937-5 2017 RESULTS: The results showed that ospemifene induced expression of the key TH1 cytokines interferon gamma and interleukin-2 in vitro, which may be mediated by stimulating T-cells through phosphoinositide 3-kinase and calmodulin signaling pathways. Ospemifene 33-43 negative elongation factor complex member C/D, Th1l Mus musculus 74-77 27922937-5 2017 RESULTS: The results showed that ospemifene induced expression of the key TH1 cytokines interferon gamma and interleukin-2 in vitro, which may be mediated by stimulating T-cells through phosphoinositide 3-kinase and calmodulin signaling pathways. Ospemifene 33-43 interferon gamma Mus musculus 88-104 27922937-5 2017 RESULTS: The results showed that ospemifene induced expression of the key TH1 cytokines interferon gamma and interleukin-2 in vitro, which may be mediated by stimulating T-cells through phosphoinositide 3-kinase and calmodulin signaling pathways. Ospemifene 33-43 interleukin 2 Mus musculus 109-122 25936229-3 2015 AREAS COVERED: This review describes the safety profile of SERMs (tamoxifen, raloxifene, toremifene, bazedoxifene, lasofoxifene, and ospemifene) and fulvestrant (a pure ER antagonist) from Phase III trials, long-term extension studies, and active comparator studies. Ospemifene 133-143 estrogen receptor 1 Homo sapiens 9-11 26634778-2 2015 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 0-10 estrogen receptor 1 Homo sapiens 29-46 24918836-4 2014 Preclinical and clinical studies showed that ospemifene has an agonist action on bone and reduced the growth of all breast cancer models in animal studies, providing they expressed estrogen receptor-alpha. Ospemifene 45-55 estrogen receptor 1 Homo sapiens 181-204 24055829-5 2013 Ospemifene binds ERalpha and ERbeta with approximately equal affinities. Ospemifene 0-10 estrogen receptor 2 Homo sapiens 29-35 23665515-9 2013 Ospemifene showed similar affinity for estrogen receptor (ER)-alpha and ER-beta, but an overall lower affinity than estradiol. Ospemifene 0-10 estrogen receptor 1 Rattus norvegicus 39-67 23665515-9 2013 Ospemifene showed similar affinity for estrogen receptor (ER)-alpha and ER-beta, but an overall lower affinity than estradiol. Ospemifene 0-10 estrogen receptor 2 Rattus norvegicus 72-79 23985562-8 2013 These include vaginal lubricants and moisturizers, vaginal estrogen, hormone therapy, and the selective estrogen-receptor modulator ospemifene (indicated for dyspareunia). Ospemifene 132-142 estrogen receptor 1 Homo sapiens 104-121 23852652-0 2013 Effects of cytochrome P450 inhibitors and inducers on the metabolism and pharmacokinetics of ospemifene. Ospemifene 93-103 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 11-26 23852652-1 2013 PURPOSE: The objectives were to determine the cytochrome P450 (CYP) enzymes involved in the metabolism of ospemifene and its main hydroxylated metabolites and to examine the effects of CYP inhibitors and inducers on ospemifene pharmacokinetics. Ospemifene 106-116 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 46-61 23852652-1 2013 PURPOSE: The objectives were to determine the cytochrome P450 (CYP) enzymes involved in the metabolism of ospemifene and its main hydroxylated metabolites and to examine the effects of CYP inhibitors and inducers on ospemifene pharmacokinetics. Ospemifene 106-116 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 63-66 23852652-1 2013 PURPOSE: The objectives were to determine the cytochrome P450 (CYP) enzymes involved in the metabolism of ospemifene and its main hydroxylated metabolites and to examine the effects of CYP inhibitors and inducers on ospemifene pharmacokinetics. Ospemifene 216-226 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 63-66 23852652-4 2013 RESULTS: Although several CYP inhibitors decreased the in vitro formation of ospemifene metabolites, none of them completely blocked metabolism. Ospemifene 77-87 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 26-29 23852652-5 2013 Roles for CYP3A4, CYP2C9, CYP2C19 and CYP2B6 in the metabolism of ospemifene and its two main metabolites, 4--hydroxyospemifene and 4"-hydroxyospemifene, were confirmed. Ospemifene 66-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 10-16 23852652-5 2013 Roles for CYP3A4, CYP2C9, CYP2C19 and CYP2B6 in the metabolism of ospemifene and its two main metabolites, 4--hydroxyospemifene and 4"-hydroxyospemifene, were confirmed. Ospemifene 66-76 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 18-24 23852652-5 2013 Roles for CYP3A4, CYP2C9, CYP2C19 and CYP2B6 in the metabolism of ospemifene and its two main metabolites, 4--hydroxyospemifene and 4"-hydroxyospemifene, were confirmed. Ospemifene 66-76 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 26-33 23852652-5 2013 Roles for CYP3A4, CYP2C9, CYP2C19 and CYP2B6 in the metabolism of ospemifene and its two main metabolites, 4--hydroxyospemifene and 4"-hydroxyospemifene, were confirmed. Ospemifene 66-76 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 38-44 23852652-7 2013 CONCLUSIONS: 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. Ospemifene 106-116 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 82-88 23852652-7 2013 CONCLUSIONS: 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. Ospemifene 106-116 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 82-85 23852652-8 2013 Strong CYP3A or CYP2C9 inducers (e.g. rifampicin) would be expected to decrease the exposure to ospemifene. Ospemifene 96-106 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 7-12 23852652-8 2013 Strong CYP3A or CYP2C9 inducers (e.g. rifampicin) would be expected to decrease the exposure to ospemifene. Ospemifene 96-106 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 16-22 23852652-9 2013 Ospemifene should be used with caution when coadministered with the modest CYP3A inhibitor ketoconazole and should not be coadministered with the potent CYP3A/CYP2C9/CYP2C19 inhibitor fluconazole. Ospemifene 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-80 18455292-6 2008 Osp also opposed apoptosis at least in U2OS/ERalpha cells. Ospemifene 0-3 estrogen receptor 1 Homo sapiens 44-51 23880855-0 2013 Effects of ospemifene on drug metabolism mediated by cytochrome P450 enzymes in humans in vitro and in vivo. Ospemifene 11-21 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 53-68 23880855-1 2013 The objective of these investigations was to determine the possible effects of the novel selective estrogen receptor modulator, ospemifene, on cytochrome P450 (CYP)-mediated drug metabolism. Ospemifene 128-138 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 143-158 23880855-1 2013 The objective of these investigations was to determine the possible effects of the novel selective estrogen receptor modulator, ospemifene, on cytochrome P450 (CYP)-mediated drug metabolism. Ospemifene 128-138 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 160-163 23880855-2 2013 Ospemifene underwent testing for possible effects on CYP enzyme activity in human liver microsomes and in isolated human hepatocytes. Ospemifene 0-10 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 53-56 23880855-3 2013 Based on the results obtained in vitro, three Phase 1 crossover pharmacokinetic studies were conducted in healthy postmenopausal women to assess the in vivo effects of ospemifene on CYP-mediated drug metabolism. Ospemifene 168-178 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 182-185 23880855-4 2013 Ospemifene and its main metabolites 4-hydroxyospemifene and 4"-hydroxyospemifene weakly inhibited a number of CYPs (CYP2B6, CYP2C9, CYP2C19, CYP2C8, and CYP2D6) in vitro. Ospemifene 0-10 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 116-122 23880855-4 2013 Ospemifene and its main metabolites 4-hydroxyospemifene and 4"-hydroxyospemifene weakly inhibited a number of CYPs (CYP2B6, CYP2C9, CYP2C19, CYP2C8, and CYP2D6) in vitro. Ospemifene 0-10 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 124-130 23880855-4 2013 Ospemifene and its main metabolites 4-hydroxyospemifene and 4"-hydroxyospemifene weakly inhibited a number of CYPs (CYP2B6, CYP2C9, CYP2C19, CYP2C8, and CYP2D6) in vitro. Ospemifene 0-10 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 132-139 23880855-4 2013 Ospemifene and its main metabolites 4-hydroxyospemifene and 4"-hydroxyospemifene weakly inhibited a number of CYPs (CYP2B6, CYP2C9, CYP2C19, CYP2C8, and CYP2D6) in vitro. Ospemifene 0-10 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 141-147 23880855-4 2013 Ospemifene and its main metabolites 4-hydroxyospemifene and 4"-hydroxyospemifene weakly inhibited a number of CYPs (CYP2B6, CYP2C9, CYP2C19, CYP2C8, and CYP2D6) in vitro. Ospemifene 0-10 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 153-159 23880855-8 2013 Therefore, the risk that ospemifene will affect the pharmacokinetics of drugs that are substrates for CYP enzymes is low. Ospemifene 25-35 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 102-105 23729558-0 2013 Ospemifene metabolism in humans in vitro and in vivo: metabolite identification, quantitation, and CYP assignment of major hydroxylations. Ospemifene 0-10 peptidylprolyl isomerase G Homo sapiens 99-102 21564348-11 2012 Ospemifene and bazedoxifene exert anti-inflammatory effects in astrocytes by a mechanism involving classical oestrogen receptors and the inhibition of nuclear factor-kappa B p65 transactivation. Ospemifene 0-10 synaptotagmin 1 Rattus norvegicus 174-177 21926925-11 2012 Ospemifene increased survival time and exerted an antitumor effect on the development and growth of estrogen receptor-positive mammary tumors in the MTag.Tg mouse model at the 50-mg/kg dose. Ospemifene 0-10 estrogen receptor 1 (alpha) Mus musculus 100-117 21926925-14 2012 CONCLUSIONS: Ospemifene prevents and treats estrogen receptor-positive MTag.Tg mammary tumors in this immune-intact mouse model in a dose-dependent fashion. Ospemifene 13-23 estrogen receptor 1 (alpha) Mus musculus 44-61 19533603-9 2010 Finally, we report that news SERMs, ospemifene and bazedoxifene, exert anti-inflammatory actions by a mechanism involving classical estrogen receptors and by the inhibition of LPS-induced NFkappaB p65 transactivation. Ospemifene 36-46 v-rel reticuloendotheliosis viral oncogene homolog A (avian) Mus musculus 197-200 18455292-11 2008 Osp opposed the effect of etoposide on OPG primarily in U2OS/ERbeta cells but interestingly, it had little effect on IL-6 expression. Ospemifene 0-3 basic transcription factor 3 pseudogene 11 Homo sapiens 39-42 18455292-11 2008 Osp opposed the effect of etoposide on OPG primarily in U2OS/ERbeta cells but interestingly, it had little effect on IL-6 expression. Ospemifene 0-3 estrogen receptor 2 Homo sapiens 61-67 18455292-12 2008 E2, PPT, DNP and Osp also inhibited etoposide-induced death and cytokine changes in SAOS-2 osteosarcoma cells expressing endogenous ERalpha and ERbeta. Ospemifene 17-20 estrogen receptor 1 Homo sapiens 132-139 18455292-12 2008 E2, PPT, DNP and Osp also inhibited etoposide-induced death and cytokine changes in SAOS-2 osteosarcoma cells expressing endogenous ERalpha and ERbeta. Ospemifene 17-20 estrogen receptor 2 Homo sapiens 144-150 15084346-4 2004 The maximum level of VEGF mRNA was observed at 1 h after raloxifene and 6 h after tamoxifen or ospemifene treatment. Ospemifene 95-105 vascular endothelial growth factor A Rattus norvegicus 21-25 17420779-12 2007 The effects of ospemifene and raloxifene were mediated by oestrogen receptors by a mechanism involving paracrine induction of osteoprotegerin in cultures with osteoblast derived osteosarcoma cells. Ospemifene 15-25 TNF receptor superfamily member 11b Homo sapiens 126-141 15255284-10 2004 Bone ALP decreased in 60 and 90 mg ospemifene groups by 1.9 and 2.6%, respectively (p < 0.05 for both dose levels when compared to placebo). Ospemifene 35-45 alkaline phosphatase, placental Homo sapiens 5-8 16280035-13 2005 In contrast, the ospemifene treatment significantly increased ER levels while tamoxifen significantly decreased them. Ospemifene 17-27 estrogen receptor 1 (alpha) Mus musculus 62-64 31953613-0 2020 Long non-coding RNA MALAT1 facilitates the tumorigenesis, invasion and glycolysis of multiple myeloma via miR-1271-5p/SOX13 axis. Ospemifene 110-117 metastasis associated lung adenocarcinoma transcript 1 Homo sapiens 20-26 14501606-6 2003 Of the markers reflecting coagulation and fibrinolysis, plasma fibrinogen was significantly reduced in the 60- and 90-mg groups of ospemifene (8.7% and 8.5%, respectively) when compared with the placebo group. Ospemifene 131-141 fibrinogen beta chain Homo sapiens 63-73 34463164-10 2022 CONCLUSIONS: Up to date, this is the only prospective and observational study with ospemifene in routine clinical practice conditions and confirms the results previously reported from randomized controlled clinical trials, improving VVA, not increasing endometrial thickness, and decreasing CTx levels by exerting an anti-resorptive function. Ospemifene 83-93 cytochrome P450 family 27 subfamily A member 1 Homo sapiens 291-294 34464022-5 2021 US Food and Drug Administration (FDA)-approved treatment options include vaginally administered estrogen products as well as dehydroepiandrosterone (prasterone) and the selective estrogen receptor modulator ospemifene. Ospemifene 207-217 estrogen receptor 1 Homo sapiens 179-196 34169794-8 2021 Oral ospemifene is an effective selective estrogen receptor modulator to treat VVA. Ospemifene 5-15 estrogen receptor 1 Homo sapiens 42-59 32631589-1 2020 OBJECTIVES: To report the effects on the urinary function of ospemifene prescribed for vulvovaginal atrophy (VVA) in patients with overactive bladder (OAB) symptoms refractory to the first line of pharmacologic treatment with antimuscarinic or beta3-agonists drugs. Ospemifene 61-71 T cell immune regulator 1, ATPase H+ transporting V0 subunit a3 Homo sapiens 244-249 32631589-10 2020 CONCLUSIONS: Ospemifene might be a useful option for postmenopausal women with VVA and OAB symptoms, refractory to the first line of treatment with beta3-agonists or antimuscarinic drugs, before considering invasive options. Ospemifene 13-23 T cell immune regulator 1, ATPase H+ transporting V0 subunit a3 Homo sapiens 148-153 31953613-0 2020 Long non-coding RNA MALAT1 facilitates the tumorigenesis, invasion and glycolysis of multiple myeloma via miR-1271-5p/SOX13 axis. Ospemifene 110-117 SRY-box transcription factor 13 Homo sapiens 118-123 31953613-11 2020 MALAT1 directly targeted miR-1271-5p and miR-1271-5p depression reverted the effects of MALAT1 knockdown on MM cells. Ospemifene 29-36 metastasis associated lung adenocarcinoma transcript 1 Homo sapiens 0-6 31953613-11 2020 MALAT1 directly targeted miR-1271-5p and miR-1271-5p depression reverted the effects of MALAT1 knockdown on MM cells. Ospemifene 45-52 metastasis associated lung adenocarcinoma transcript 1 Homo sapiens 0-6 31953613-11 2020 MALAT1 directly targeted miR-1271-5p and miR-1271-5p depression reverted the effects of MALAT1 knockdown on MM cells. Ospemifene 45-52 metastasis associated lung adenocarcinoma transcript 1 Homo sapiens 88-94 31953613-12 2020 SOX13 was a target of miR-1271-5p and SOX13 overexpression weakened the effects of miR-1271-5p on MM. Ospemifene 26-33 SRY-box transcription factor 13 Homo sapiens 0-5 31953613-12 2020 SOX13 was a target of miR-1271-5p and SOX13 overexpression weakened the effects of miR-1271-5p on MM. Ospemifene 87-94 SRY-box transcription factor 13 Homo sapiens 0-5 31953613-12 2020 SOX13 was a target of miR-1271-5p and SOX13 overexpression weakened the effects of miR-1271-5p on MM. Ospemifene 87-94 SRY-box transcription factor 13 Homo sapiens 38-43 31953613-13 2020 MALAT1 indirectly modulated SOX13 expression through targeting miR-1271-5p. Ospemifene 67-74 metastasis associated lung adenocarcinoma transcript 1 Homo sapiens 0-6 31953613-13 2020 MALAT1 indirectly modulated SOX13 expression through targeting miR-1271-5p. Ospemifene 67-74 SRY-box transcription factor 13 Homo sapiens 28-33 31953613-14 2020 MALAT1 down-regulation inhibited MM growth by miR-1271-5p/SOX13 axis in vivo. Ospemifene 50-57 metastasis associated lung adenocarcinoma transcript 1 Homo sapiens 0-6 31953613-14 2020 MALAT1 down-regulation inhibited MM growth by miR-1271-5p/SOX13 axis in vivo. Ospemifene 50-57 SRY-box transcription factor 13 Homo sapiens 58-63 31953613-15 2020 CONCLUSION: LncRNA MALAT1 expedited MM tumorigenesis, invasion, and glycolysis via miR-1271-5p/SOX13 axis. Ospemifene 87-94 metastasis associated lung adenocarcinoma transcript 1 Homo sapiens 19-25 31953613-15 2020 CONCLUSION: LncRNA MALAT1 expedited MM tumorigenesis, invasion, and glycolysis via miR-1271-5p/SOX13 axis. Ospemifene 87-94 SRY-box transcription factor 13 Homo sapiens 95-100 31915515-8 2019 RPS27A, UBC, and RAC1 were the top three proteins in our study; their corresponding RNAs were miR-1271-5p, miR-130a-3p, miR-130b-3p, and miR-574-3p. Ospemifene 98-105 ribosomal protein S27a Homo sapiens 0-6 31915515-8 2019 RPS27A, UBC, and RAC1 were the top three proteins in our study; their corresponding RNAs were miR-1271-5p, miR-130a-3p, miR-130b-3p, and miR-574-3p. Ospemifene 98-105 Rac family small GTPase 1 Homo sapiens 17-21