| ID Source | ID |
|---|---|
| PubMed CID | 154257 |
| CHEMBL ID | 46740 |
| CHEBI ID | 135947 |
| SCHEMBL ID | 41935 |
| MeSH ID | M0535317 |
| Synonym |
|---|
| bazedoxifene |
| CHEBI:135947 |
| CHEMBL46740 , |
| 1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methylindol-5-ol |
| bdbm50099585 |
| 1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxy-phenyl)-3-methyl-1h-indol-5-ol |
| 1-(4-(2-(azepan-1-yl)ethoxy)benzyl)-2-(4-hydroxyphenyl)-3-methyl-1h-indol-5-ol |
| us8815934, no. 98 |
| bazedoxifeno [inn-spanish] |
| 198481-32-2 |
| 1h-indol-5-ol, 1-((4-(2-(hexahydro-1h-azepin-1-yl)ethoxy)phenyl)methyl)-2-(4-hydroxyphenyl)-3-methyl- |
| bazedoxifene [inn] |
| 1-((4-(2-hexahydro-1h-azepin-1-yl)ethoxy)phenyl)methyl)-2-(4-hydroxyphenyl)-3-methyl-1h-indol-5-ol |
| way 140424 |
| bazedoxifeno |
| unii-q16tt9c5bk |
| q16tt9c5bk , |
| HY-A0031 |
| bazedoxifene [vandf] |
| bazedoxifene [who-dd] |
| ak-r215 component bazedoxifene |
| bazedoxifene [mi] |
| bazedoxifene [ema epar] |
| 1-(p-(2-(hexahydro-1h-azepin-1-yl)ethoxy)benzyl)-2-(p-hydroxyphenyl)-3-methylindol-5-ol |
| ak r215 component bazedoxifene |
| CS-0932 |
| gtpl7355 |
| SCHEMBL41935 |
| UCJGJABZCDBEDK-UHFFFAOYSA-N |
| 1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-indol-5-ol |
| AB01566901_01 |
| DTXSID70173593 |
| DB06401 |
| AKOS030255808 |
| 1h-indol-5-ol, 1-[[4-[2-(hexahydro-1h-azepin-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl- |
| J-012822 |
| A15019 |
| 1-{4-[2-(azepan-1-yl)ethoxy]benzyl}-2-(4-hydroxyphenyl)-3-methyl-1h-indol-5-ol |
| Q4875166 |
| 198481-32-2 (free base) |
| bazedoxifene free base |
| SB19326 |
| D94589 |
| EX-A5409 |
| A879977 |
| AS-78494 |
| nsc823462 |
| nsc-823462 |
| 1-({4-[2-(azepan-1-yl)ethoxy]phenyl}methyl)-2-(4-hydroxyphenyl)-3-methyl-1h-indol-5-ol |
| EN300-20600169 |
Bazedoxifene (BZA) is a third-generation selective estrogen receptor (ER) modulator and selective ER degrader with activity in preclinical models of endocrine-resistant breast cancer, including models harboring ESR1 mutations. It is an effective drug for the treatment of postmenopausal osteoporosis.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Bazedoxifene is a third-generation selective estrogen receptor (ER) modulator and selective ER degrader with activity in preclinical models of endocrine-resistant breast cancer, including models harboring ESR1 mutations." | ( Clinical Efficacy and Whole-Exome Sequencing of Liquid Biopsies in a Phase IB/II Study of Bazedoxifene and Palbociclib in Advanced Hormone Receptor-Positive Breast Cancer. Anderson, L; Cibulskis, C; Coorens, T; Getz, G; Grinshpun, A; Jeselsohn, R; Krop, IE; Lennon, NJ; Leshchiner, I; Li, T; McDonnell, DP; Nardone, A; Patterson, C; Rees, R; Russo, D; Stewart, C; Tayob, N; Tolaney, SM; Tsuji, J; Tung, N; Winer, EP, 2022) | 1.66 |
| "Bazedoxifene (BZA) is a selective estrogen receptor modulator identified in a novel high-throughput unbiased screen for its remyelinating potential, and its remyelinating effects were demonstrated in pre-clinical models." | ( Re-WRAP (Remyelination for women at risk of axonal loss and progression): A phase II randomized placebo-controlled delayed-start trial of bazedoxifene for myelin repair in multiple sclerosis. Anderson, A; Bove, R; Green, A; Hsu, S; Lazar, AA; Mayoral, SR; Nylander, A; Pease-Raissi, SE; Rowles, W, 2023) | 1.83 |
| "Bazedoxifene is an effective drug for the treatment of postmenopausal osteoporosis. " | ( Bazedoxifene effects on osteoprotegerin, insulin-like growth factor, tumor necrosis factor and bone mineral density. Chai, Z; Hu, Q; Ma, Y; Ren, L, 2020) | 3.44 |
| "Bazedoxifene is an attractive novel therapeutic reagent for atherosclerosis diseases." | ( Bazedoxifene exhibits anti-inflammation and anti-atherosclerotic effects via inhibition of IL-6/IL-6R/STAT3 signaling. Guo, J; Huo, S; Li, C; Li, S; Lin, J; Lin, L; Liu, T; Luo, P; Lv, J; Ma, H; Shi, W; Wang, M; Wang, Y; Yan, D; Zhang, C; Zhao, C, 2021) | 2.79 |
| "Bazedoxifene is a new IL6/GP130 inhibitor recommended by the FDA for clinical use as a selective estrogen receptor modulator." | ( Bazedoxifene Plays a Protective Role against Inflammatory Injury of Endothelial Cells by Targeting CD40. Guo, R; Huang, P; Lv, Y; Nie, F; Pei, Q; Song, W; Tang, Z, 2020) | 2.72 |
| "Bazedoxifene (BZA) is a synthetic selective estrogen receptor modulator, approved by the United States Food and Drug Administration for the treatment of osteoporosis in postmenopausal women." | ( A comprehensive review on anticancer mechanism of bazedoxifene. Iqbal, A; Irfan, M; Khan, M; Li, Y; Ma, T; Maqbool, MF; Maryam, A; Shakir, HA; Zafar, E, 2022) | 1.7 |
| "Bazedoxifene is a selective estrogen receptor modulator that has estrogen agonist effects on bone and lipid metabolism while having neutral or estrogen antagonist effects on the breast and endometrium. " | ( Pharmacokinetics, Dose Proportionality, and Bioavailability of Bazedoxifene in Healthy Postmenopausal Women. McKeand, W, 2017) | 2.14 |
| "Bazedoxifene is an estrogen receptor agonist in bone but an antagonist/degrader in the endometrium, which has contributed to its success as a TSEC component." | ( Tissue selective estrogen complex (TSEC): a review. Boucher, M; Morgenstern, D; Pickar, JH, 2018) | 1.2 |
| "Bazedoxifene (BZA) is a third-generation selective estrogen receptor modulator (SERM) and has been investigated as a treatment for postmenopausal osteoporosis." | ( Bazedoxifene protects cerebral autoregulation after traumatic brain injury and attenuates impairments in blood-brain barrier damage: involvement of anti-inflammatory pathways by blocking MAPK signaling. Ding, Y; Lan, YL; Lou, JC; Ma, BB; Wang, X; Xing, JS; Zhang, B; Zou, S; Zou, YJ, 2019) | 2.68 |
| "Bazedoxifene acetate (BZA) is a selective estrogen receptor modulator that is approved in a number of countries for the prevention and/or treatment of osteoporosis in postmenopausal women. " | ( Renal tumors in male rats following long-term administration of bazedoxifene, a tissue-selective estrogen receptor modulator. Bailey, S; Cukierski, MA; Earnhardt, JN; Komm, B; Perry, R; Thompson, CA; Wright, DJ, 2013) | 2.07 |
| "Bazedoxifene is a third-generation Selective Estrogen Receptor Modulator, developed on raloxifene's model, and investigated as treatment for postmenopausal osteoporosis and menopause management. " | ( Pharmacokinetic evaluation of bazedoxifene for the treatment of osteoporosis. Gatti, D; Lello, S; Rossini, M; Sblendorio, I, 2013) | 2.12 |
| "Bazedoxifene appears to be a cost-effective strategy compared to raloxifene for the treatment of postmenopausal osteoporotic women in Europe, particularly in patients at high fracture risk." | ( Comparative cost-effectiveness of bazedoxifene and raloxifene in the treatment of postmenopausal osteoporosis in Europe, using the FRAX algorithm. Kanis, JA; Kim, K; Luo, X; Sutradhar, S; Svedbom, A, 2014) | 2.12 |
| "Bazedoxifene (BZA) is a novel selective estrogen receptor modulator in clinical development for the prevention and treatment of postmenopausal osteoporosis. " | ( The effects of bazedoxifene in the ovariectomized aged cynomolgus monkey. Chouinard, L; Jolette, J; Komm, BS; Smith, SY, 2015) | 2.21 |
| "Bazedoxifene is a third-generation selective estrogen receptor modulator (SERM) used for osteoporosis management in postmenopausal women at fracture risk that has demonstrated a powerful antiestrogenic effect on the endometrium." | ( Bazedoxifene/conjugated estrogens combination for the treatment of the vasomotor symptoms associated with menopause and for prevention of osteoporosis in postmenopausal women. Mejía Ríos, A; Palacios, S, 2015) | 2.58 |
| "Bazedoxifene (BZA) is a selective estrogen receptor modulator that has been shown to prevent and treat postmenopausal osteoporosis. " | ( The effects of bazedoxifene on bone structural strength evaluated by hip structure analysis. Beck, TJ; Chines, AA; Fuerst, T; Gaither, KW; Hines, T; Levine, AB; Mirkin, S; Sutradhar, S; Williams, R; Yu, CR, 2015) | 2.21 |
| "Bazedoxifene (BZA) is a selective estrogen receptor modulator that reduces fracture risk and bone turnover in postmenopausal women with osteoporosis. " | ( Efficacy and tolerability of bazedoxifene in Mexican women with osteoporosis: a subgroup analysis of a randomized phase 3 trial. Arias, L; Komm, BS; Mirkin, S; Palacios, S; Pan, K; Williams, R, 2016) | 2.17 |
| "Bazedoxifene is a novel selective estrogen receptor modulator in clinical development for the prevention and treatment of postmenopausal osteoporosis. " | ( A double-blind, randomized, ascending, multiple-dose study of bazedoxifene in healthy postmenopausal women. Chines, AA; Ermer, JC; McKeand, WE; Orczyk, GP, 2014) | 2.09 |
| "Bazedoxifene is a SERM that is being clinically evaluated both as a monotherapy for the prevention and treatment of osteoporosis and in combination with conjugated estrogens (CEs) for the treatment of menopausal symptoms and prevention of osteoporosis." | ( Effects of various selective estrogen receptor modulators with or without conjugated estrogens on mouse mammary gland. Crabtree, JS; Harris, HA; Komm, BS; Peano, BJ; Winneker, RC, 2009) | 1.07 |
| "Bazedoxifene is a third-generation selective estrogen-receptor modulator being developed for use alone or in combination with estrogen for prevention and treatment of osteoporosis in postmenopausal women. " | ( Bazedoxifene: a selective estrogen-receptor modulator. Mitwally, MF, 2008) | 3.23 |
| "Bazedoxifene is a selective estrogen receptor modulator under development for the prevention and treatment of osteoporosis. " | ( Metabolic disposition of [14C]bazedoxifene in healthy postmenopausal women. Chandrasekaran, A; DeMaio, W; McKeand, WE; Scatina, J; Stoltz, R; Sullivan, P, 2009) | 2.08 |
| "Bazedoxifene is a novel SERM under clinical investigation for the prevention and treatment of postmenopausal osteoporosis." | ( Bazedoxifene: a novel selective estrogen receptor modulator for postmenopausal osteoporosis. de Villiers, TJ, 2010) | 2.52 |
| "Bazedoxifene is a novel SERM that was recently approved in the European Union and is undergoing regulatory review in the United States for the prevention and treatment of postmenopausal osteoporosis." | ( Efficacy and safety of bazedoxifene, a novel selective estrogen receptor modulator for the prevention and treatment of postmenopausal osteoporosis. Palacios, S, 2010) | 1.39 |
| "Bazedoxifene is a new-generation SERM with a novel chemical structure, which has been developed to provide improved efficacy on the bone and the lipid profile, as well as improved safety for breast and endometrial tissues. " | ( [Bazedoxifene as a new-generation SERM]. Ohta, H, 2011) | 2.72 |
| "Bazedoxifene acetate is a new, third-generation, selective estrogen receptor modulator." | ( Bazedoxifene acetate for the management of postmenopausal osteoporosis. Palacios, S, 2011) | 2.53 |
| "Bazedoxifene Acetate (BZA) is a third-generation SERM that showed to protect bone mass in postmenopausal women with osteopenia, and to reduce vertebral fracture risk in osteoporotic postmenopausal women; moreover, BZA decreased the non-vertebral fracture risk in a subgroup of patients at high-risk for fracture in comparison to placebo." | ( [Selective estrogen receptor modulators: focus on bazedoxifene]. Lello, S, 2011) | 1.34 |
| "Bazedoxifene is a novel selective estrogen receptor modulator with a unique tissue-selectivity profile." | ( Bazedoxifene: a new selective estrogen receptor modulator for postmenopausal osteoporosis. Genant, HK, 2011) | 2.53 |
| "Bazedoxifene (BZA) is a third-generation selective estrogen receptor modulator (SERM) that has been approved for the prevention and treatment of postmenopausal osteoporosis. " | ( The selective estrogen receptor modulator bazedoxifene inhibits hormone-independent breast cancer cell growth and down-regulates estrogen receptor α and cyclin D1. Curpan, R; Grigg, R; Jordan, VC; Kim, H; Lewis-Wambi, JS; Sarker, MA, 2011) | 2.08 |
| "Bazedoxifene is a selective estrogen receptor modulator (SERM) that has been developed for use in post-menopausal osteoporosis. " | ( In vitro bioactivation of bazedoxifene and 2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol in human liver microsomes. Lušin, TT; Mrhar, A; Peterlin-Mašič, L; Tomašić, T; Trontelj, J, 2012) | 2.12 |
| "Bazedoxifene Acetate (BZA) is a selective estrogen receptor modulator (SERM) that is approved for the prevention and/or treatment of osteoporosis in postmenopausal women. " | ( Carcinogenicity and hormone studies with the tissue-selective estrogen receptor modulator bazadoxifene. Bailey, S; Cukierski, MA; Earnhardt, JN; Komm, B; Minck, DR; Perry, R; Wright, DJ, 2013) | 1.83 |
| "Bazedoxifene is a novel selective estrogen receptor modulator (SERM) for the prevention and treatment of osteoporosis. " | ( Cost-effectiveness of bazedoxifene compared with raloxifene in the treatment of postmenopausal osteoporotic women. Ben Sedrine, W; Hiligsmann, M; Reginster, JY, 2013) | 2.15 |
| "Bazedoxifene is a tissue-specific selective estrogen receptor modulator being developed by Wyeth Pharmaceuticals (formerly Wyeth-Ayerst Laboratories) to be used alone for the prevention and treatment of osteoporosis in postmenopausal women and in combination with Premarin for menopausal symptoms. " | ( Bazedoxifene (Wyeth). Gruber, C; Gruber, D, 2004) | 3.21 |
| "Bazedoxifene is a third-generation SERM currently in Phase III clinical trials. " | ( Bazedoxifene: a third-generation selective estrogen receptor modulator for treatment of postmenopausal osteoporosis. Kelley, KW; Stump, AL; Wensel, TM, 2007) | 3.23 |
| "Bazedoxifene is a selective estrogen receptor modulator (SERM) currently in development for osteoporosis prevention and treatment." | ( Update on bazedoxifene: a novel selective estrogen receptor modulator. Biskobing, DM, 2007) | 1.46 |
| "Bazedoxifene is a third-generation selective estrogen receptor modulator (SERM) that is being developed by Ligand Pharmaceuticals in collaboration with Wyeth. " | ( Bazedoxifene: bazedoxifene acetate, TSE 424, TSE-424, WAY 140424. , 2008) | 3.23 |
Bazedoxifene (BAZ) has been proven to have anti-inflammatory effects. In combination with oral conjugated equine estrogens, improves the signs and symptoms of VVA. BazedOxifene has been shown to significantly decrease the risk of vertebral fractures in postmenopausal women.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Bazedoxifene has recently been reported to inhibit inflammation and alleviate blood-brain barrier disruption caused by traumatic brain injury." | ( Biodegradable bilayer hydrogel membranes loaded with bazedoxifene attenuate blood-spinal cord barrier disruption via the NF-κB pathway after acute spinal cord injury. Baokun, Z; Erzhu, Y; Jianguang, X; Qiang, S; Xiaofeng, L; Xin, W; Zhiheng, C, 2023) | 1.88 |
| "Bazedoxifene (BAZ) has been proven to have anti-inflammatory effects." | ( Bazedoxifene attenuates intestinal injury in sepsis by suppressing the NF-κB/NLRP3 signaling pathways. Duan, XB; Gao, G; Guo, R; Li, D; Li, X; Ning, W; Zhang, X; Zhou, Y, 2023) | 3.07 |
| "Bazedoxifene has no demonstrated efficacy for VVA but, in combination with oral conjugated equine estrogens, improves the signs and symptoms of VVA." | ( Clinical effects of selective estrogen receptor modulators on vulvar and vaginal atrophy. Pinkerton, JV; Stanczyk, FZ, 2014) | 1.12 |
| "Bazedoxifene has been found to be efficacious in reducing bone turnover without adverse effects of breast pain." | ( Bazedoxifene: a selective estrogen-receptor modulator. Mitwally, MF, 2008) | 2.51 |
| "Bazedoxifene has been shown to significantly decrease the risk of vertebral fractures in postmenopausal women. " | ( Bazedoxifene reduces vertebral and clinical fractures in postmenopausal women at high risk assessed with FRAX. Johansson, H; Kanis, JA; McCloskey, EV; Oden, A, 2009) | 3.24 |
| "Bazedoxifene has demonstrated a favorable safety and tolerability profile with no significant differences observed among the treatment groups in coronary artery events, cerebrovascular events, and overall death rates." | ( [Bazedoxifene as a new-generation SERM]. Ohta, H, 2011) | 2 |
| "Bazedoxifene has been shown to be safe and well tolerated, with no evidence of endometrial or breast stimulation." | ( Bazedoxifene: a new selective estrogen receptor modulator for postmenopausal osteoporosis. Genant, HK, 2011) | 2.53 |
| "Bazedoxifene has shown significant reductions in vertebral and non-vertebral (in higher-risk women) fracture risk, with no evidence of breast or endometrial stimulation." | ( An update on selective estrogen receptor modulators for the prevention and treatment of osteoporosis. Chines, AA; Komm, BS, 2012) | 1.1 |
| "Bazedoxifene 20 mg has been associated with a significant reduction in the risk of non-vertebral fracture versus placebo and raloxifene 60 mg in women at higher baseline fracture risk." | ( The evolution of selective estrogen receptor modulators in osteoporosis therapy. Hadji, P, 2012) | 1.1 |
Bazedoxifene may inhibit the proliferation and migration of VSMCs through up-regulate the autophagy level after PDGF-BB stimulation. It did not inhibit the growth of HUVECs while suppressing the proliferation of VS MCs.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Bazedoxifene may inhibit the proliferation and migration of VSMCs through up-regulate the autophagy level after PDGF-BB stimulation." | ( Bazedoxifene inhibits PDGF-BB induced VSMC phenotypic switch via regulating the autophagy level. Gao, K; Guo, R; Huang, P; Jia, S; Nie, F; Song, W; Tang, Z, 2020) | 2.72 |
| "Bazedoxifene did not inhibit the growth of HUVECs while suppressing the proliferation of VSMCs." | ( Bazedoxifene exhibits anti-inflammation and anti-atherosclerotic effects via inhibition of IL-6/IL-6R/STAT3 signaling. Guo, J; Huo, S; Li, C; Li, S; Lin, J; Lin, L; Liu, T; Luo, P; Lv, J; Ma, H; Shi, W; Wang, M; Wang, Y; Yan, D; Zhang, C; Zhao, C, 2021) | 2.79 |
Bazedoxifene treatment effectively prevents the Hcy-induced detrimental reactions of osteoblasts. Treatment with bazedox ifene for 2 years did not affect age-related changes in breast density in this population of postmenopausal women with osteoporosis.
Two global, double-blind, placebo- and active-controlled, phase-3 studies. Bazedoxifene significantly increased bone mineral density and reduced bone turnover versus placebo. Although there were no severe adverse events in this study, bazedox ifene use in patients with hepatic impairment is not recommended.
Bazedoxifene displayed linear pharmacokinetics with doses ranging from 5 to 40 mg, with no unexpected accumulation. In subjects with severe (Child-Pugh C) liver impairment, bazedox ifene mean half-life was 50% longer than that of healthy subjects.
Bazedoxifene combined with conjugated estrogens is an investigational tissue-selective estrogen complex. First in a new class of therapeutic agents that pairs a selective estrogen receptor modulator with estrogens.
| Excerpt | Reference | Relevance |
|---|---|---|
| " Bazedoxifene combined with conjugated estrogens is an investigational tissue-selective estrogen complex, the first in a new class of therapeutic agents that pairs a selective estrogen receptor modulator with estrogens." | ( Bazedoxifene and bazedoxifene combined with conjugated estrogens for the management of postmenopausal osteoporosis. Lewiecki, EM, 2007) | 2.69 |
| " The primary aim of this study was to evaluate the endometrial profile of bazedoxifene acetate (BZA), a third-generation SERM, alone and in combination with conjugated equine estrogens (CEE) in a postmenopausal primate model." | ( Endometrial profile of bazedoxifene acetate alone and in combination with conjugated equine estrogens in a primate model. Appt, SE; Clarkson, TB; Cline, JM; Ethun, KF; Register, TC; Wood, CE, 2013) | 0.93 |
Bazedoxifene is a novel selective estrogen receptor modulator. It has complex pharmacokinetics with rapid absorption, high metabolic clearance, and low oral bioavailability (6%)
| Excerpt | Reference | Relevance |
|---|---|---|
| " The bioavailability was low (16%) after a 1 mg/kg oral dose of BZA." | ( Disposition of bazedoxifene in rats. Ahmad, S; Chandrasekaran, A; DeMaio, W; Hultin, T; Scatina, J; Shen, L, 2010) | 0.71 |
| "Bazedoxifene, a novel selective estrogen receptor modulator, has complex pharmacokinetics with rapid absorption, high metabolic clearance, low oral bioavailability (6." | ( Efflux and uptake transporters involved in the disposition of bazedoxifene. Berginc, K; Kristl, A; Lušin, TT; Mrhar, A; Stieger, B; Trontelj, J, 2016) | 2.12 |
| " The present report describes findings from 3 Phase I clinical studies that evaluated the single-dose pharmacokinetics (study 1; n = 84), multiple-dose pharmacokinetics (study 2; n = 23), and absolute bioavailability (study 3; n = 18) of bazedoxifene." | ( Pharmacokinetics, Dose Proportionality, and Bioavailability of Bazedoxifene in Healthy Postmenopausal Women. McKeand, W, 2017) | 0.88 |
| " In study 3, tablet and capsule formulations of bazedoxifene formulations had an estimated oral bioavailability of ~6%." | ( Pharmacokinetics, Dose Proportionality, and Bioavailability of Bazedoxifene in Healthy Postmenopausal Women. McKeand, W, 2017) | 0.95 |
| " Bazedoxifene had an estimated oral bioavailability of ~6% and was safe and well tolerated in the range of doses evaluated." | ( Pharmacokinetics, Dose Proportionality, and Bioavailability of Bazedoxifene in Healthy Postmenopausal Women. McKeand, W, 2017) | 1.6 |
The study evaluated the efficacy and safety of bazedoxifene in postmenopausal Japanese women 85 years of age or younger with osteoporosis.
| Excerpt | Relevance | Reference |
|---|---|---|
| " 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 |
| "This randomized, double-blind, placebo-controlled, dose-response late phase 2 study evaluated the efficacy and safety of bazedoxifene in postmenopausal Japanese women 85 years of age or younger with osteoporosis." | ( Effects of bazedoxifene on bone mineral density, bone turnover, and safety in postmenopausal Japanese women with osteoporosis. Chines, AA; Constantine, GD; Gorai, I; Itabashi, A; Miki, T; Mizunuma, H; Ochi, H; Ohta, H; Sato, H; Sugimoto, T; Takada, M; Yoh, K, 2011) | 0.97 |
| "72) was observed with the higher dosage for all populations, and with the lower dosage in the VVA (-0." | ( Menopause-specific quality of life across varying menopausal populations with conjugated estrogens/bazedoxifene. Abraham, L; Komm, BS; Messig, M; Mirkin, S; Pinkerton, JV; Ryan, KA, 2014) | 0.62 |
| " 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 |
| "4 years) who received a single oral dose of atorvastatin 20 mg on day 1 (period 1), multiple daily dosing of bazedoxifene 40 mg on days 4-11 (period 2), and coadministration of atorvastatin 20 mg + bazedoxifene 40 mg on day 12 (period 3)." | ( A Study of the Potential Interaction Between Bazedoxifene and Atorvastatin in Healthy Postmenopausal Women. Baird-Bellaire, S; Ermer, J; McKeand, W; Patat, A, 2018) | 0.95 |
| "Primary cultures from human umbilical artery endothelial cells were used in dose-response experiments (0." | ( Bazedoxifene increases the proliferation of human arterial endothelial cells but does not affect the expression of cyclins A, B, and D1 and of p27 Cano, A; Dudenko, D; García-Pérez, MÁ; Gómez, R; Tarín, JJ, 2021) | 2.06 |
| Class | Description |
|---|---|
| phenylindole | |
| [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) |
|---|---|---|---|---|---|---|---|
| PPM1D protein | Homo sapiens (human) | Potency | 32.9993 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| Interferon beta | Homo sapiens (human) | Potency | 32.9993 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Estrogen receptor | Homo sapiens (human) | IC50 (µMol) | 7.9343 | 0.0000 | 0.7237 | 32.7000 | AID102611; AID1372349; AID256998; AID70008 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 (µMol) | 3.4400 | 0.0002 | 2.4585 | 9.9600 | AID1804171 |
| Estrogen receptor beta | Homo sapiens (human) | IC50 (µMol) | 0.0444 | 0.0001 | 0.5294 | 32.7000 | AID256999; AID70176 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| AID1220256 | Total clearance in human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1372347 | Antiproliferative activity against human T47D cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 | Design, synthesis and biological evaluation of novel indole-xanthendione hybrids as selective estrogen receptor modulators. |
| AID1075144 | Cytotoxicity against human MIAPaCa2 cells assessed as cell viability | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Drug design targeting protein-protein interactions (PPIs) using multiple ligand simultaneous docking (MLSD) and drug repositioning: discovery of raloxifene and bazedoxifene as novel inhibitors of IL-6/GP130 interface. |
| AID1075153 | Inhibition of IL-6Ralpha/GP130 interaction in human PANC-1 cells assessed as inhibition of IL-6-induced STAT3 phosphorylation at Y705 at 25 uM preincubated for 30 mins followed by IL-6 induction measured after 24 hrs by Western blot analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Drug design targeting protein-protein interactions (PPIs) using multiple ligand simultaneous docking (MLSD) and drug repositioning: discovery of raloxifene and bazedoxifene as novel inhibitors of IL-6/GP130 interface. |
| AID1220257 | Ratio of drug level in blood to plasma in human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID256999 | Inhibition of binding to recombinant human ERbeta by scintillation proximity assay | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms. |
| AID1283264 | Inhibition of delta 8-7 isomerase in human SLOS fibroblasts assessed as decrease in 7-DHC levels at 10 nM after 5 days by LC-MS/GC-MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3 | The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts. |
| AID1808020 | Inhibition of porcine heart malate dehydrogenase preincubated for 5 min followed by nicotinamide adenine dinucleotide addition and monitered for 90 sec by spectrophotometric method | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | Colloidal Aggregators in Biochemical SARS-CoV-2 Repurposing Screens. |
| AID1220240 | Unbound fraction during CYP4500-mediated metabolism in human intestinal microsomes | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1808021 | Inhibition of porcine heart malate dehydrogenase assessed as reduction in enzyme inhibition at 3 times IC50 preincubated for 5 min followed by nicotinamide adenine dinucleotide addition and monitered for 90 sec in presence of 0.01% Triton-X100 by spectrop | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | Colloidal Aggregators in Biochemical SARS-CoV-2 Repurposing Screens. |
| AID1075147 | Inhibition of IL-6Ralpha/GP130 interaction in ER-negative human SUM159 cells overexpressing IL-6 assessed as inhibition of constitutive STAT3 phosphorylation at Y705 at 10 to 30 uM after 24 hrs by Western blot analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Drug design targeting protein-protein interactions (PPIs) using multiple ligand simultaneous docking (MLSD) and drug repositioning: discovery of raloxifene and bazedoxifene as novel inhibitors of IL-6/GP130 interface. |
| AID1283244 | Inhibition of DR24 in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 200 nM after 24 hrs by LC-MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3 | The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts. |
| AID1220242 | Unbound intrinsic clearance in human intestinal microsomes assessed CYP450-mediated glucuronidation clearance | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1220245 | Activity of human UGT1A8 expressed in insect cells assessed as reduction in compound level after 30 mins | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1283268 | Inhibition of delta 8-7 isomerase in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3 | The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts. |
| AID1220237 | Unbound fraction during UGT-mediated glucuronidation in human intestinal microsomes | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| 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. |
| AID1372349 | Displacement of Fluormone-tagged ES2 from human recombinant ERalpha after 2 hrs by fluorescence polarization assay | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 | Design, synthesis and biological evaluation of novel indole-xanthendione hybrids as selective estrogen receptor modulators. |
| AID70008 | In vitro inhibition of [3H]17-beta-estradiol binding to human estrogen receptor alpha | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. |
| AID1220236 | Oral clearance in human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1075146 | Cytotoxicity against ER-negative human SUM159 cells assessed as cell viability after 72 hrs by MTT assay in presence of IL-6 | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Drug design targeting protein-protein interactions (PPIs) using multiple ligand simultaneous docking (MLSD) and drug repositioning: discovery of raloxifene and bazedoxifene as novel inhibitors of IL-6/GP130 interface. |
| 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. |
| AID257000 | Selectivity for human ERbeta over ERalpha | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms. |
| AID1220260 | Oral bioavailability in human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1220259 | Oral absorption in human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1283275 | Inhibition of DR24 in mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3 | The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts. |
| AID1559014 | Induction of uterotrophic activity in Sprague-Dawley rat assessed as increase in uterine weight at 10 mg/kg, po administered for 3 days and measured after 24 hrs of last dosing by hematoxylin eosin staining based imaging analysis | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Design and Synthesis of Basic Selective Estrogen Receptor Degraders for Endocrine Therapy Resistant Breast Cancer. |
| AID1220253 | Drug metabolism human intestinal microsomes assessed as bazedoxifene-6'-glucuronide formation | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID257001 | Antiproliferative activity against human breast cancer MCF7 cell line in presence of 0.003 nM estradiol | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms. |
| AID1220255 | Apparent permeability by PAMPA method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1352589 | Downregulation of ERalpha mRNA levels in human T47D cells at 15 uM after 48 hrs by semi-quantitative RT-PCR analysis | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of novel indole-benzimidazole hybrids targeting estrogen receptor alpha (ER-α). |
| AID1075148 | Inhibition of IFN-gamma receptor/GP130 interaction in human PANC-1 cells assessed as inhibition of IFN-gamma-induced STAT1 phosphorylation at Y701 at 25 uM preincubated for 30 mins followed by IFN-gamma induction measured after 24 hrs by Western blot anal | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Drug design targeting protein-protein interactions (PPIs) using multiple ligand simultaneous docking (MLSD) and drug repositioning: discovery of raloxifene and bazedoxifene as novel inhibitors of IL-6/GP130 interface. |
| AID1220239 | Unbound intrinsic clearance in human intestinal microsomes assessed UGT-mediated glucuronidation clearance | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1283277 | Inhibition of delta 8-7 isomerase in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 200 nM after 24 hrs by LC-MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3 | The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts. |
| AID1283273 | Decrease in cholesterol levels in human SLOS fibroblasts at 10 nM after 5 days by LC-MS/GC-MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3 | The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts. |
| AID70176 | In vitro inhibitory concentration against [3H]17-beta-estradiol binding to human estrogen receptor 2 | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. |
| AID1220244 | Activity of human UGT1A1 expressed in insect cells assessed as reduction in compound level after 30 mins | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1220258 | Renal clearance in human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1220251 | Drug metabolism human intestinal microsomes assessed as bazedoxifene-4'-glucuronide formation | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1075149 | Inhibition of LIFR/GP130 interaction in human PANC-1 cells assessed as inhibition of LIF-induced STAT3 phosphorylation at Y705 at 25 uM after 24 hrs by Western blot analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Drug design targeting protein-protein interactions (PPIs) using multiple ligand simultaneous docking (MLSD) and drug repositioning: discovery of raloxifene and bazedoxifene as novel inhibitors of IL-6/GP130 interface. |
| AID1283267 | Cytotoxicity against human SLOS fibroblasts at 5 uM after 5 days by Cell Titer assay | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3 | The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts. |
| AID256998 | Inhibition of binding to recombinant human ERalpha by scintillation proximity assay | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms. |
| AID1283262 | Inhibition of DR24 in human SLOS fibroblasts assessed as decrease in 7-DHC levels at 10 nM after 5 days by LC-MS/GC-MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3 | The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts. |
| AID1220241 | Intrinsic clearance in human intestinal microsomes assessed CYP450-mediated glucuronidation clearance | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1480298 | Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8 | Computer-Aided Discovery and Characterization of Novel Ebola Virus Inhibitors. |
| 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. |
| AID257003 | In vivo agonism of estradiol in rat uterine tissue after 1 mg/kg, po by uterine weight assay | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms. |
| AID1808022 | Inhibition of porcine heart malate dehydrogenase assessed as critical aggregation concentration preincubated for 5 min followed by nicotinamide adenine dinucleotide addition and monitered for 90 sec by spectrophotometric method | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | Colloidal Aggregators in Biochemical SARS-CoV-2 Repurposing Screens. |
| AID1220246 | Activity of human UGT1A10 expressed in insect cells assessed as reduction in compound level after 30 mins | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1220238 | Intrinsic clearance in human intestinal microsomes assessed UGT-mediated glucuronidation clearance | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1283269 | Inhibition of DR24 in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3 | The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts. |
| AID257002 | In vivo antagonism of estradiol in rat uterine tissue after 1 mg/kg, po by uterine weight assay | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23 | Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms. |
| AID1075152 | Binding affinity to GP130 in human RH30 cells assessed as protection against pronase-induced cleavage at 100 to 1000 uM preincubated for 1 hr followed by pronase induction measured after 30 mins by DARTS assay | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Drug design targeting protein-protein interactions (PPIs) using multiple ligand simultaneous docking (MLSD) and drug repositioning: discovery of raloxifene and bazedoxifene as novel inhibitors of IL-6/GP130 interface. |
| AID1283247 | Inhibition of delta 8-7 isomerase in mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3 | The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts. |
| AID102611 | In vitro antagonist effect on estrogen receptor alpha transcriptional activation in MCF-7 cells against 10 pM 17-beta-estradiol | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. |
| 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. |
| AID1804171 | DRC analysis by immunofluorescence from Article 10.1128/AAC.00819-20: \\Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs.\\ | 2020 | Antimicrobial agents and chemotherapy, 06-23, Volume: 64, Issue:7 | Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs. |
| AID1346880 | Human Estrogen receptor-beta (3A. Estrogen receptors) | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. |
| AID1346845 | Human Estrogen receptor-alpha (3A. Estrogen receptors) | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. |
| [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 | 0 (0.00) | 18.2507 |
| 2000's | 33 (11.04) | 29.6817 |
| 2010's | 219 (73.24) | 24.3611 |
| 2020's | 47 (15.72) | 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 (52.59) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 69 (22.48%) | 5.53% |
| Reviews | 82 (26.71%) | 6.00% |
| Case Studies | 2 (0.65%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 154 (50.16%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| A Randomized, Open-label, Single-dose Study to Evaluate the Safety and the Pharmacokinetics After Oral Concurrent Administration of HDDO-16141 and HDDO-16142 in Healthy Adult Subjects [NCT03234244] | Phase 1 | 37 participants (Actual) | Interventional | 2017-04-12 | Completed | ||
| Bazedoxifene - A New Selective Estrogen Receptor Modulator Treatment for Women With Schizophrenia: a Double-blind, Randomized, Placebo Controlled Trial [NCT04113993] | Phase 4 | 160 participants (Anticipated) | Interventional | 2019-10-07 | Recruiting | ||
| Pilot Study of Effects of Bazedoxifene Plus Conjugated Estrogen on Imaging and Blood Biomarkers In Women With Menopausal Symptoms at Increased Risk for Breast Cancer [NCT04821375] | Early Phase 1 | 20 participants (Anticipated) | Interventional | 2021-12-02 | Recruiting | ||
| Effects of a Tissue Selective Estrogen Complex (TESC) on Depression and the Neural Reward System in the Perimenopause [NCT03740009] | Phase 4 | 20 participants (Actual) | Interventional | 2019-01-02 | Completed | ||
| Bazedoxifene as a Concomitant Treatment of Patients With Metastatic Pancreatic Adenocarcinoma [NCT04812808] | 10 participants (Anticipated) | Interventional | 2022-02-01 | Recruiting | |||
| Multi-centre, Randomized, Open Label Trial to Evaluate the Effects of Switching to Bazedoxifene in Comparison With Switching to Calcium and Vitamin D in Postmenopausal Women Previously Treated With Bisphosphonates [NCT02090400] | Phase 4 | 110 participants (Actual) | Interventional | 2013-05-31 | Completed | ||
| Pilot Study of Effects of Duavee® on Imaging and Blood Biomarkers In Women With Menopausal Symptoms at Increased Risk for Breast Cancer [NCT04379024] | Early Phase 1 | 11 participants (Actual) | Interventional | 2020-06-01 | Terminated(stopped due to Study agent no longer available) | ||
| Mechanisms and Interventions Addressing Accelerated Cardiovascular Disease Risk in Women With Endometriosis [NCT05059626] | Phase 4 | 28 participants (Anticipated) | Interventional | 2023-12-01 | Recruiting | ||
| Randomized IIB Study of the Effect of Bazedoxifene Plus Conjugated Estrogens on Breast Imaging and Tissue Biomarkers in Peri or Post-Menopausal Women at Increased Risk for Development of Breast Cancer [NCT04821141] | Phase 2 | 120 participants (Anticipated) | Interventional | 2021-12-14 | Recruiting | ||
| Bazedoxifene/Conjugated Estrogens (BZA/CE) Improvement of Metabolism (BIM) [NCT02237079] | Phase 4 | 17 participants (Actual) | Interventional | 2014-12-31 | Completed | ||
| A Multicenter, Double Blind, Randomized, Placebo and Raloxifene Controlled Study to Assess Safety and Efficacy of TSE-424 (Bazedoxifene Acetate) in the Prevention of Postmenopausal Osteoporosis [NCT00481169] | Phase 3 | 1,742 participants (Actual) | Interventional | 2001-07-31 | Completed | ||
| RNA Expression Analysis Of Endometrial Biopsies Comparing Placebo, Bazedoxifene/ Conjugated Estrogens And Raloxifene [NCT00847821] | 185 participants (Actual) | Observational | 2009-05-31 | Terminated(stopped due to See termination reason in detailed description.) | |||
| Atherosclerosis Intervention With Novel Tissue Selective Estrogen Complex Therapy [NCT04103476] | Phase 2 | 400 participants (Anticipated) | Interventional | 2021-04-13 | Recruiting | ||
| Pilot Study of the Effect of Duavee® on Benign Breast Tissue Proliferation in Peri or Post-menopausal Women at Moderate Risk for Development of Breast Cancer [NCT02729701] | Phase 2 | 28 participants (Actual) | Interventional | 2016-05-31 | Completed | ||
| Fracture Incidence Reduction And Safety Of TSE-424 (Bazedoxifene Acetate) Compared To Placebo And Raloxifene In Osteoporotic Postmenopausal Women [NCT00205777] | Phase 3 | 7,609 participants (Actual) | Interventional | 2001-12-31 | Completed | ||
| Hand Osteoarthritis: Investigating Pain Effects in a Randomised Placebo-controlled Feasibility Study of an Estrogen-containing Therapy [NCT04036929] | 28 participants (Actual) | Interventional | 2019-05-09 | Completed | |||
| A Double-Blind, Randomized, Placebo And Active- Controlled Efficacy And Safety Study Of The Effects Of Bazedoxifene/Conjugated Estrogens Combinations On Endometrial Hyperplasia And Prevention Of Osteoporosis In Postmenopausal Women [NCT00808132] | Phase 3 | 1,886 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
| A Double-Blind, Randomized, Placebo- And Active-Controlled Efficacy And Safety Study Of Bazedoxifene/Conjugated Estrogens Combinations For Prevention Of Endometrial Hyperplasia And Prevention Of Osteoporosis In Postmenopausal Women [NCT00242710] | Phase 3 | 1,083 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
| A Double-Blind, Randomized, Placebo-Controlled, Efficacy and Safety Study of Bazedoxifene/Conjugated Estrogen Combinations for Treatment of Vasomotor Symptoms Associated With Menopause [NCT00234819] | Phase 3 | 325 participants | Interventional | 2005-10-31 | Completed | ||
| Effectiveness of Bazedoxifene for Prevention of Glucocorticoid-induced Bone Loss in RA Patients [NCT02602704] | Phase 4 | 114 participants (Actual) | Interventional | 2015-12-29 | Completed | ||
| An Open-Label, Single/Multiple Dose, Non-Randomized, 3-Period, Crossover Study To Determine The Potential Drug Interaction Of Bazedoxifene On Conjugated Estrogens (CE) In Healthy Postmenopausal Women [NCT00706225] | Phase 1 | 30 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
| An Open-Label, Single-Dose, Randomized, 4-Period, Crossover, Bioequivalence Study of Clinical and Commercial Formulations of Bazedoxifene/Conjugated Estrogens in Healthy Postmenopausal Women [NCT00550433] | Phase 1 | 0 participants | Interventional | 2007-09-30 | Completed | ||
| An Open-Label, Single-Dose, Non-Randomized, 4-Period Crossover Bioavailability Study of Bazedoxifene Contained in Bazedoxifene/Conjugated Estrogen Tablets Administered to Healthy Postmenopausal Women [NCT00550303] | Phase 1 | 28 participants (Anticipated) | Interventional | 2007-10-31 | Completed | ||
| A Double-Blind, Randomized, Placebo- and Active-Controlled Safety and Efficacy Study of Bazedoxifene/Conjugated Estrogens Combinations in Postmenopausal Women [NCT00675688] | Phase 3 | 3,544 participants (Actual) | Interventional | 2002-04-30 | Completed | ||
| An Open-Label, Single-Dose, 3-Period, Crossover Study To Determine The Effect Of A High-Fat Meal On The Relative Bioavailability And Pharmacokinetics Of A Single Dose Of Bazedoxifene Acetate/Conjugated Estrogens (Premarin© New Process) Administered Orally [NCT00465075] | Phase 1 | 24 participants (Anticipated) | Interventional | 2007-03-31 | Completed | ||
| An Open Label, Randomized, Multicenter Study To Compare Bazedoxifene Steady-State Exposures Obtained With 2 Bazedoxifene Acetate/Conjugated Estrogen Formulations In Postmenopausal Women [NCT00479778] | Phase 1 | 72 participants | Interventional | 2007-04-30 | Completed | ||
| Effects of Novel Estrogens on Glucose and Lipids in Postmenopausal Prediabetic Women Veterans [NCT05073237] | Phase 2 | 40 participants (Anticipated) | Interventional | 2023-12-29 | Not yet recruiting | ||
| Impact of Estrogen + Estradiol Receptor Alpha Modulator Therapy on Oxidative Stress in Post-menopausal Women With and Without Sleep Apnea [NCT03981341] | Phase 3 | 36 participants (Anticipated) | Interventional | 2019-11-01 | Recruiting | ||
| An Open-label, Single-dose, Randomized-to-sequence, 4-period Crossover Bioavailability Study of Bazedoxifene Contained in Bazedoxifene/Conjugated Estrogen Tablets Administered to Healthy Postmenopausal Women. [NCT00367536] | Phase 1 | 24 participants | Interventional | 2006-08-31 | Completed | ||
| A Multicenter, Double Blind, Randomized, Placebo Controlled Study to Assess the Safety and Efficacy of Bazedoxifene in Postmenopausal Asian Women [NCT00384072] | Phase 3 | 500 participants (Anticipated) | Interventional | 2006-05-31 | Completed | ||
| Viviant®20mg Special Investigation (Regulatory Post Marketing Commitment Plan) [NCT01470326] | 3,187 participants (Actual) | Observational | 2011-11-30 | Completed | |||
| A Double-Blind, Randomized, Placebo-and Active-Controlled Efficacy and Safety Study of Bazedoxifene/Conjugated Estrogens Combinations for Treatment of Moderate to Severe Vulvar/Vaginal Atrophy in Postmenopausal Women [NCT00238732] | Phase 3 | 650 participants | Interventional | 2005-10-31 | Completed | ||
| A Phase 1 Clinical Trial to Evaluate the Safety and Pharmacokinetic Characteristics After Coadministration of C1-R215 and C2-R215 Compared to the Administration of C1-R215 and C2-R215 Independently in Healthy Male Volunteers [NCT03005340] | Phase 1 | 24 participants (Actual) | Interventional | 2016-12-31 | Enrolling by invitation | ||
| An Open-Label, Single-Dose, Randomized, 3-Period, Crossover, Bioequivalence Study Between Bazedoxifene/Conjugated Estrogens (Premarin Current Process) And Bazedoxifene/Conjugated Estrogens (Premarin New Process) In Healthy Postmenopausal Women [NCT00464789] | Phase 1 | 0 participants | Interventional | 2007-03-31 | Completed | ||
| An Open-Label, Single-Dose, Randomized-to-Sequence, 2-Period, Crossover, Pivotal Bioequivalence Study Between Bazedoxifene Acetate/Conjugated Estrogens (Premarin Current Process) and Bazedoxifene Acetate/Conjugated Estrogens (Premarin New Process) Tablets [NCT00396799] | Phase 1 | 0 participants | Interventional | 2006-11-30 | Completed | ||
| Bone Mineral Density Increase and Safety of TSE-424 Compared to Placebo in Osteoporotic Postmenopausal Women [NCT00238745] | Phase 2 | 375 participants | Interventional | 2003-08-31 | Completed | ||
| A Phase 1, Open-label, Single-dose, Randomized, 4-treatment, 4- Period, Crossover, Pilot Bioavailability Study of 3 Test Tablet Formulations of Bazedoxifene (Bza) Compared With A Reference Tablet Formulation of Bza/Conjugated Estrogens (ce) in Healthy Pos [NCT01634789] | Phase 1 | 2 participants (Actual) | Interventional | 2012-08-31 | Terminated(stopped due to This study was terminated on 10 December 2012 due to low enrollment. The decision to terminate the study was not based on safety or efficacy issues.) | ||
| COHORT STUDY OF VENOUS THROMBOEMBOLISM AND OTHER CLINICAL ENDPOINTS AMONG OSTEOPOROTIC WOMEN PRESCRIBED BAZEDOXIFENE, BISPHOSPHONATES OR RALOXIFENE IN EUROPE [NCT01416194] | 10,497 participants (Actual) | Observational | 2011-07-25 | Completed | |||
| A Phase II Randomized, Double-Blind, Parallel-Group, Placebo Controlled Delayed-Start Trial to Assess the Efficacy, Safety, and Tolerability of Bazedoxifene Acetate (BZA) as a Remyelinating Agent in Patients With Multiple Sclerosis [NCT04002934] | Phase 2 | 50 participants (Anticipated) | Interventional | 2019-09-10 | Recruiting | ||
| A Large-scale Multicenter Phase II Study Evaluating the Protective Effect of a Tissue Selective Estrogen Complex (TSEC) in Women With Newly Diagnosed Ductal Carcinoma in Situ [NCT02694809] | Phase 2 | 160 participants (Anticipated) | Interventional | 2017-01-31 | Recruiting | ||
| A Phase Ib/II Study of Palbociclib in Combination With Bazedoxifene in Hormone Receptor Positive Breast Cancer [NCT02448771] | Phase 1/Phase 2 | 36 participants (Actual) | Interventional | 2015-07-09 | Completed | ||
| A Randomized, Open-label, Single-dose, Crossover Study to Evaluate the Pharmacokinetic Characteristics After Co-administration of HDDO-16141 and HDDO-16143 and Administration of HDDO-1614 in Healthy Adult Male Subjects [NCT03382314] | Phase 1 | 38 participants (Actual) | Interventional | 2017-10-16 | Completed | ||
| AK-R215 Pharmacokinetic Study Pharmacokinetic Characteristics of AK-R215 in Comparison to Each Component Coadministered in Healthy Adult Male or Menopausal Female Valunteers. [NCT03321318] | Phase 1 | 52 participants (Anticipated) | Interventional | 2017-07-13 | Active, not recruiting | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||