ID Source | ID |
---|---|
PubMed CID | 2733526 |
CHEMBL ID | 83 |
CHEBI ID | 41774 |
SCHEMBL ID | 4084 |
MeSH ID | M0021024 |
Synonym |
---|
BIDD:GT0009 |
BIDD:PXR0003 |
BIDD:ER0008 |
AB00053547-18 |
AB00053547-16 |
BRD-K93754473-048-05-3 |
BRD-K93754473-001-02-9 |
2-[4-[(z)-1,2-di(phenyl)but-1-enyl]phenoxy]-n,n-dimethylethanamine |
gtpl1016 |
BSPBIO_001150 |
BSPBIO_001982 |
c26h29no |
NCGC00024928-01 |
tocris-0999 |
IDI1_002170 |
SPECTRUM5_001417 |
BPBIO1_000278 |
(z)-2-[p-(1,2-diphenyl-1-butenyl)phenoxy]-n,n-dimethylethylamine |
,citrate |
2-[4-[(z)-1,2-diphenylbut-1-enyl]phenoxy]-n,n-dimethyl-ethanamine |
1-p-.beta.-dimethylamino-ethoxyphenyl-trans-1,2-diphenylbut-1-ene |
(z)-2-(4-(1,2-diphenylbut-1-enyl)phenoxy)-n,n-dimethylethanamine |
QTL1_000079 |
PRESTWICK2_000146 |
PRESTWICK3_000146 |
LOPAC0_001203 |
smr000059172 |
MLS001332535 |
MLS001332536 |
bdbm20607 |
tamoxifen, 7 |
chembl83 , |
cid_2733526 |
(2-{4-[(1z)-1,2-diphenylbut-1-en-1-yl]phenoxy}ethyl)dimethylamine |
ici-47699 |
istubol |
einecs 234-118-0 |
hsdb 6782 |
tamoplex |
tamoxifen [inn:ban] |
tamoxifenum [inn-latin] |
tamoxen |
valodex |
ethylamine, n,n-dimethyl-2-(p-(1,2-diphenyl-1-butenyl)phenoxy)-, (z)- |
novaldex |
tamizam |
retaxim |
tamoxifen (z) |
ethanamine, 2-(4-(1,2-diphenyl-1-butenyl)phenoxy)-n,n-dimethyl-, (z)- |
tamoxifeno [inn-spanish] |
(z)-2-(para-(1,2-diphenyl-1-butenyl)phenoxy)-n,n-dimethylamine (iupac) |
ccris 3275 |
citofen |
oncomox |
ici 47699 |
tamoxifene [inn-french] |
10540-29-1 |
TAMOXIFEN , |
C07108 |
tamoxifen, >=99% |
tamoxifeno |
1-para-beta-dimethylaminoethoxyphenyl-trans-1,2-diphenylbut-1-ene |
CHEBI:41774 , |
1-p-beta-dimethylaminoethoxyphenyl-trans-1,2-diphenylbut-1-ene |
2-{4-[(1z)-1,2-diphenylbut-1-en-1-yl]phenoxy}-n,n-dimethylethanamine |
diemon |
tamoxifenum |
crisafeno |
(z)-2-(para-(1,2-diphenyl-1-butenyl)phenoxy)-n,n-dimethylamine |
trans-tamoxifen |
(z)-2-(4-(1,2-diphenyl-1-butenyl)phenoxy)-n,n-dimethylethanamine |
tamoxifene |
DB00675 |
UPCMLD-DP027 |
1YA4 |
trans form of tamoxifen |
(z)-2-[4-(1,2)-diphenyl-1-butenyl)-phenoxy]-n,n-dimethylethanamine |
BSPBIO_000252 |
IDI1_000258 |
CMAP_000044 |
NCGC00024928-04 |
NCGC00024928-05 |
SPECTRUM5_002043 |
nsc727681 |
nsc-727681 |
NCGC00024928-07 |
NCGC00024928-09 |
NCGC00024928-08 |
NCGC00024928-03 |
ici47699 |
L024126 |
HMS1990J11 |
HMS2090N08 |
NCGC00024928-12 |
mammaton |
tamoplex (tn) |
D08559 |
tamoxifen (inn) |
tamoxifen (tn) |
HMS1362J11 |
HMS1792J11 |
2-[4-[(z)-1,2-diphenylbut-1-enyl]phenoxy]-n,n-dimethylethanamine |
A801229 |
NCGC00024928-11 |
NCGC00024928-16 |
NCGC00024928-18 |
NCGC00024928-19 |
NCGC00024928-15 |
NCGC00024928-13 |
NCGC00024928-14 |
NCGC00024928-17 |
NCGC00024928-10 |
HMS3261D09 |
unii-094zi81y45 |
ec 234-118-0 |
ethanamine, 2-(4-((1z)-1,2-diphenyl-1-butenyl)phenoxy)-n,n-dimethyl- |
094zi81y45 , |
tox21_201243 |
cas-10540-29-1 |
dtxcid9014187 |
tox21_300539 |
dtxsid1034187 , |
NCGC00254455-01 |
NCGC00258795-01 |
CCG-205277 |
HMS2232C12 |
7728-73-6 |
LP00494 |
tamoxifen [vandf] |
ethanamine, 2-(4-((1z)-1,2-diphenyl-1-buten-1-yl)phenoxy)-n,n-dimethyl- |
tamoxifen [mi] |
tamoxifen [who-dd] |
tamoxifen [iarc] |
tamoxifen [inn] |
tamoxifen [hsdb] |
[3h]-tamoxifen |
gtpl5384 |
[3h]tamoxifen |
AM84324 |
HY-13757A |
trans-2-[4-(1,2-diphenyl-1-butenyl)phenoxy]-n,n-dimethylethylamine |
AKOS022143035 |
SCHEMBL4084 |
AB00053547-17 |
NCGC00261179-01 |
tox21_500494 |
ethanamine, 2-[4-[(1z)-1,2-diphenyl-1-buten-1-yl]phenoxy]-n,n-dimethyl- |
FD12063 |
W-108788 |
(z)-2-[4-(1,2-diphenyl-1-butenyl)phenoxy]-n,n-dimethylethanamine |
HB0601 |
HMS3403J11 |
AB00053547_19 |
AB00053547_20 |
2-[4-[(1z)-1,2-diphenyl-1-buten-1-yl]phenoxy]-n,n-dimethylethanamine |
(z)-2-(4-(1,2-diphenylbut-1-en-1-yl)phenoxy)-n,n-dimethylethanamine |
tamoxifen, analytical standard |
tamoxifen, certified reference material, tracecert(r) |
EN300-1273241 |
ethanamine, 2-[4-[(1z)-1,2-diphenyl-1-butenyl]phenoxy]-n,n-dimethyl- |
SBI-0051170.P004 |
(z)-2-(4-(1,2-diphenylbut-1-en-1-yl)phenoxy)-n,n-dimethylethan-1-amine |
(e/z)-tamoxifen |
ici47699;z-tamoxifen;trans-tamoxifen |
Q412178 |
KS-1472 |
z-tamoxifen |
HMS3411P04 |
BRD-K93754473-048-04-6 |
BRD-K93754473-048-10-3 |
SDCCGSBI-0051170.P007 |
NCGC00024928-40 |
NCGC00024928-39 |
ethyl3-(4-hydroxy-3-methoxyphenyl)propionate |
BT164438 |
CS-0694848 |
tamoxifen (standard) |
HY-13757AR |
tamoxifene (inn-french) |
tamoxifenum (inn-latin) |
tamoxifen (iarc) |
l02ba01 |
tamoxifeno (inn-spanish) |
2-(4-((1z)-1,2-diphenylbut-1-en-1-yl)phenoxy)-n,n-dimethylethanamine |
1-p-beta-dimethylamino-ethoxyphenyl-trans-1,2-diphenylbut-1-ene |
(z)-2-(4-(1,2-diphenyl-1-butenyl)phenoxy)phenoxy)-n,n-dimethylethanamine |
AC-35768 |
Z2527624834 |
Tamoxifen (TAM) is a widely used drug in the prophylaxis and treatment of breast cancer. It is a selective estrogen receptor modulator (SERM) used in estrogen receptor-alpha (ERα)-dependent breast cancers and off-target indications such as infections. The immune activity of TAM and its active metabolite, 4-OH tamox ifen (4HT), is poorly characterized.
Tamoxifen has a good tolerability profile and has demonstrated benefits for breast cancer patients. It prolongs overall and disease-free survival and reduces the incidence of contralateral breast cancer. TamoxifEN has a beneficial effect on bone density presumably through its estrogen agonistic effects.
Tamoxifen has been used for a long time as an adjuvant hormonal treatment in breast cancer patients. It has been shown to be a potent liver carcinogen in rats. Concerns about its long-term safety and efficacy are being raised.
Tamoxifen (TAM) has a lower affinity to ER compared with one of its main metabolites, 4-OH-TAM. Tamox ifen did not enhance vorinostat-induced HIV transcription (between-arm ratio, 0.8; 95% confidence interval [CI], .2-2.4). Tamoxifens may cause proliferative effects in the endometrium.
Tamoxifen/trastuzumab treatment had a significant effect on pathways essential for the control of energy-production, which have previously been linked to cancer progression, and aggressiveness. Tamox ifen may induce dysregulation of estrogen homeostasis, leading to the occurrence of related adverse reactions.
Tamoxifen and fenretinide is safe but not synergistic in lowering IGF-I levels in premenopausal women. CYP2D6 genotypes and phenotypes were related to the occurrence of hot flashes as adverse event during the first year of use.
Pharmacokinetic parameters of tamoxifen and 4-hydroxytamox ifen were determined in rats after an oral administration of 10 mg/kg. The presence of kaempferol did not alter the pharmacokinetic parameters of a metabolite of tam Oxifen. A pharmacokinetics interaction has been established between letrozole and tamoxIfen.
Tamoxifen (TMX) combined with coenzyme Q10 (CoQ10) can significantly improve sperm concentration, motility and morphology in patients with idiopathic oligoasthenospermia.
Tamoxifen (TAM) is frequently prescribed for the management breast cancer, but is associated with the challenges like compromised aqueous solubility and poor bioavailability. The present study aimed to develop a surface-modified biocompatible nanostructured lipid carrier (NLCs) system using polyoxyethylene (40) stearate.
Excerpt | Reference | Relevance |
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" The data suggest that estrone sulfate can play an important role on the bioavailability of E2 in hormone-dependent breast cancer, and that understanding the control of estrone sulfatase activity can open new knowledge of the estrogen responses and new possibilities of therapeutic application in breast cancer." | ( Estrone sulfatase activity and effect of antiestrogens on transformation of estrone sulfate in hormone-dependent vs. independent human breast cancer cell lines. Nguyen, BL; Pasqualini, JR, 1991) | 0.28 |
" The enhancement was not due to increased bioavailability because cellular uptake of [3H]tamoxifen was not increased and the lipoprotein fraction of serum had negligible [3H]tamoxifen-binding capacity." | ( Cytostatic effect of antiestrogens in lymphoid cells: relationship to high affinity antiestrogen-binding sites and cholesterol. Kon, OL; Ng, ML; Sim, KY; Tang, BL; Teo, CC, 1989) | 0.5 |
"The bioavailability of tamoxifen from 40 mg suppositories was tested in six male volunteers and compared with that of tamoxifen (Nolvadex) tablets." | ( Comparison of bioavailability in man of tamoxifen after oral and rectal administration. Blankenstein, MA; Nortier, JW; Tukker, JJ, 1986) | 0.85 |
"The bioavailability of two tamoxifen preparations (Tamoplex and Nolvadex) was compared in a multiple dose two-way cross-over design in twelve breast cancer patients." | ( The bioavailability of Tamoplex (tamoxifen). Part 3. A steady-state study in breast cancer patients. Chapman, D; De Vos, D; Slee, PH; Stevenson, D, 1988) | 0.85 |
" Finally, new perspectives are opened on combined anti-estrogen + progestogen treatment of all gynaecological malignancies, with special regard to the cytosol steroid receptor concentrations and to the bioavailability of progestogens and anti-estrogens." | ( The endometrial adenocarcinoma as a model for hormone-dependency and hormone-responsiveness of gynaecological cancers. Bonte, J, 1984) | 0.27 |
" The bioavailability was 8% in mice, 18% in rats and 11% in monkeys due to extensive first-pass metabolism." | ( Pharmacokinetics of droloxifene in mice, rats, monkeys, premenopausal and postmenopausal patients. Esumi, Y; Hata, T; Ninomiya, S; Sawamoto, T; Sekiguchi, M; Sugai, S; Tanaka, Y, ) | 0.13 |
" The present data suggest that estrogen sulfates can play an important biological role in the target tissues of the fetus, and that the enzymatic mechanisms of the bioavailability of E2 for the biological responses of the hormone can be operated in the target tissue itself." | ( Transformation of estrone, estradiol, and estrone sulfate in uterine and vaginal isolated cells of fetal guinea pig. Effect of various antiestrogens in the conversion of estrone sulfate to estradiol. Chetrite, G; Pasqualini, JR; Urabe, M, 1993) | 0.29 |
" Our findings suggest that the intestine is neither a metabolic nor an absorptive barrier to the bioavailability of droloxifene in the female Sprague-Dawley rat and that first-pass hepatic extraction is approximately 70-80% following an oral dose of 1 mg/kg." | ( First-pass metabolism and biliary recirculation of droloxifene in the female Sprague-Dawley rat. Nickerson, DF; Tess, DA; Toler, SM, 1997) | 0.3 |
" Our findings suggest that hepatic first-pass metabolism may have been saturated following intraperitoneal drug administration due to the rapid rate of absorption and the corresponding high drug concentrations achieved." | ( Intraperitoneal and intraportal administration of droloxifene to the Sprague-Dawley rat: assessing the first-pass effect. Nickerson, DF; Toler, SM, 1997) | 0.3 |
" A fall in FT4 and FT3 combined with increase in TSH suggests a reduced bioavailability of T4 and T3 during tamoxifen treatment." | ( Thyroid function in postmenopausal breast cancer patients treated with tamoxifen. Aakvaag, A; Anker, GB; Lien, EA; Lønning, PE, 1998) | 0.75 |
"The extrapolated area under the concentration-time curve (AUC0-infinity) for any drug is considered by operating guidelines as the primary parameter related to the extent of absorption in single-dose bioavailability and bioequivalence trials." | ( Experimental, extrapolated and truncated areas under the concentration-time curve in bioequivalence trials. Marzo, A; Monti, NC; Vuksic, D, 1999) | 0.3 |
" This occurs with most extended-release formulations, endogenous substances, and poorly absorbed drugs." | ( Experimental, extrapolated and truncated areas under the concentration-time curve in bioequivalence trials. Marzo, A; Monti, NC; Vuksic, D, 1999) | 0.3 |
"It has been suggested that estrogen receptor-independent high-affinity binding sites for antiestrogens could limit their local bioavailability and response." | ( Microsomal epoxide hydrolase expression as a predictor of tamoxifen response in primary breast cancer: a retrospective exploratory study with long-term follow-up. Eichelbaum, M; Fritz, P; Mürdter, TE; Siegle, I; Weissert, M; Zanger, UM, 2001) | 0.55 |
" Products from assorted makers bioavailability problems has been associated to the incomplete dissolution of the tablets." | ( In vitro dissolution test of tamoxifen citrate preparations. Braga, RM; Carvalho, RD; De Albuquerque, MM; De Santana, DP; Fonseca, SG; Strattmann, R, ) | 0.42 |
" Single oral doses of a solution formulation of (14)C-droloxifene citrate (141 mg) appeared to be rapidly and well absorbed in four post-menopausal female subjects." | ( Pharmacokinetics and metabolism of the anti-oestrogen droloxifene in female human subjects. Baldock, GA; Brodie, RR; Chasseaud, LF; Jank, P; John, BA; McBurney, A; Von Nieciecki, A, 2002) | 0.31 |
"Sulfation of 4-OH TAM provides a previously unanticipated benefit, possibly due to alterations in the bioavailability of the active metabolite or to undefined estrogen receptor-mediated events." | ( Association between sulfotransferase 1A1 genotype and survival of breast cancer patients receiving tamoxifen therapy. Ambrosone, CB; Hutchins, LF; Kadlubar, FF; Lang, NP; Nowell, S; Stone, A; Sweeney, C; Winters, M, 2002) | 0.53 |
" The plasma concentration-time profiles were primarily controlled by the rate of absorption from the injection site; post-peak plasma concentrations declined over time and were measurable up to 84 days after administration of fulvestrant 125 and 250 mg." | ( Pharmacokinetics of a single dose of fulvestrant prolonged-release intramuscular injection in postmenopausal women awaiting surgery for primary breast cancer. Harrison, MP; Holcombe, C; Kohlhardt, SR; Odling-Smee, W; Robertson, JF, 2003) | 0.32 |
"Arzoxifene (ARZ) is a selective estrogen receptor (ER) modulator with greater bioavailability than raloxifene which is being developed as treatment for breast cancer." | ( Comparison of the selective estrogen receptor modulator arzoxifene (LY353381) with tamoxifen on tumor growth and biomarker expression in an MCF-7 human breast cancer xenograft model. A'Hern, R; Detre, S; Dowsett, M; Johnston, SR; Riddler, S; Salter, J, 2003) | 0.54 |
"To reduce the frequency of administration of tamoxifen citrate so as to improve its bioavailability and patients' compliance." | ( [Development of sustained release tablet of tamoxifen citrate and its in vitro release profile]. Wu, K; Zhang, Q; Zhang, S; Zhao, G, 2003) | 0.84 |
" To increase the bioavailability of tamoxifen, we incorporated tamoxifen into polyethylene glycol (PEG)-coated nanoparticles (NP-PEG-TAM)." | ( Intraocular injection of tamoxifen-loaded nanoparticles: a new treatment of experimental autoimmune uveoretinitis. Andrieux, K; Couvreur, P; de Kozak, Y; Garcia, E; Klein, C; Naud, MC; Thillaye-Goldenberg, B; Villarroya, H, 2004) | 0.9 |
" It is assumed that the enhanced and accelerated uptake of liposomal HT in the cell line with relative drug resistance can increase the intracellular bioavailability of HT." | ( Liposomal 4-hydroxy-tamoxifen: effect on cellular uptake and resulting cytotoxicity in drug resistant breast cancer cells in vitro. Behrens, D; Fichtner, I; Teppke, AD; Zeisig, R, 2004) | 0.65 |
" In a pharmacokinetic experiment carried out in rats, 29 displayed an interesting profile, with a bioavailability of 49%." | ( Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands. Bischoff, SF; Buhl, T; Floersheim, P; Fournier, B; Geiser, M; Halleux, C; Kallen, J; Keller, H; Ramage, P; Renaud, J, 2005) | 0.33 |
" This study investigated the effect of quercetin, a dual inhibitor of CYP3A4 and P-gp, on the bioavailability and pharmacokinetics of tamoxifen and one of its metabolites, 4-hydroxytamoxifen, in rats." | ( Enhanced bioavailability of tamoxifen after oral administration of tamoxifen with quercetin in rats. Choi, JS; Li, X; Shin, SC, 2006) | 0.83 |
" The antiproliferative activity of tamoxifen, relying primarily on its ability to compete with estrogen for the ER alpha ligand binding site in breast tumor tissue, hypotheses forwarded to explain treatment failure include: (1) the existence of a second estrogen receptor (ER beta), (2) an imbalance in estrogen biosynthesis and catabolism, (3) altered bioavailability of tamoxifen, (4) altered cellular trafficking of ER alpha, (5) non genomic effects of ER alpha, directly interacting with several signal transduction pathways, and (6) transcriptional dysregulation of ER alpha target genes, which may involve both genomic (ERE alteration) and non genomic alterations." | ( Role of estrogen receptor alpha transcriptional coregulators in tamoxifen resistance in breast cancer. Bièche, I; Girault, I; Lidereau, R, 2006) | 0.85 |
"The concurrent administration of tamoxifen and bicalutamide reduces the synthesis and bioavailability of IGF-1." | ( Influence of bicalutamide with or without tamoxifen or anastrozole on insulin-like growth factor 1 and binding proteins in prostate cancer patients. Battaglia, M; Bertaccini, A; Boccardo, F; Conti, G; Romagnoli, A; Rubagotti, A; Zattoni, F, ) | 0.68 |
" Co-administration of letrozole and TAM orally increased the absorption half-life of letrozole threefold although the absolute bioavailability remained unchanged." | ( The effect of tamoxifen on the pharmacokinetics of letrozole in female rats. Brodie, AM; Nnane, IP; Tao, X, 2006) | 0.69 |
" MMPs degrade extracellular matrix components enabling tumor cell invasion and metastasis, but may also regulate the bioavailability of a variety of biologically active molecules such as anti-angiogenic fragments, which may be beneficial for the host." | ( MMP-2 and MMP-9 activity is regulated by estradiol and tamoxifen in cultured human breast cancer cells. Dabrosin, C; Garvin, S; Nilsson, UW, 2007) | 0.59 |
"Oral and intravenous administration of tamoxifen base and tamoxifen citrate formulated with hydroxybutenyl-beta-cyclodextrin (HBenBCD) to Sprague-Dawley rats significantly increased the oral bioavailability of tamoxifen relative to that of parent drug (no HBenBCD)." | ( Pharmacokinetics of tamoxifen after intravenous and oral dosing of tamoxifen-hydroxybutenyl-beta-cyclodextrin formulations. Buchanan, CM; Buchanan, NL; Edgar, KJ; Little, JL; Malcolm, MO; Ruble, KM; Wacher, VJ; Wempe, MF, 2007) | 0.93 |
"Lonafarnib is an orally bioavailable farnesyltransferase inhibitor." | ( Enhancement of the antitumor activity of tamoxifen and anastrozole by the farnesyltransferase inhibitor lonafarnib (SCH66336). Basso, AD; Black, S; Kirschmeier, P; Liu, G; Liu, M; Long, BJ; Marrinan, CH; Robert Bishop, W; Taylor, SA, 2007) | 0.61 |
" The method has been validated for use in a clinical bioavailability research of tamoxifen." | ( Optimizing high-performance liquid chromatography method with fluorescence detection for quantification of tamoxifen and two metabolites in human plasma: application to a clinical study. Xiao, DW; Yu, CX; Zhang, Q; Zhu, YB; Zou, JJ, 2008) | 0.79 |
" The enhanced bioavailability of oral tamoxifen by oral kaempferol could have been due to an inhibition of CYP3A and P-gp by kaempferol." | ( Effects of oral kaempferol on the pharmacokinetics of tamoxifen and one of its metabolites, 4-hydroxytamoxifen, after oral administration of tamoxifen to rats. Choi, JS; Piao, Y; Shin, SC, 2008) | 0.87 |
"This study examined the effect of morin on the bioavailability and pharmacokinetics of tamoxifen and its metabolite, 4-hydroxytamoxifen, in rats." | ( Effects of morin on the bioavailability of tamoxifen and its main metabolite, 4-hydroxytamoxifen, in rats. Choi, JS; Piao, YJ; Shin, SC, ) | 0.62 |
" With the aim to improve TMX oral bioavailability and decrease its side effects, crosslinked alginate microparticles for the targeting to the lymphatic system by Peyer's patch (PP) uptake were developed and in vitro characterized." | ( Alginate/chitosan microparticles for tamoxifen delivery to the lymphatic system. Coppi, G; Iannuccelli, V, 2009) | 0.63 |
"The aim of this study was to investigate the effect of naringin on the bioavailability and pharmacokinetics of tamoxifen and of its metabolite, 4-hydroxytamoxifen in rats." | ( Enhanced tamoxifen bioavailability after oral administration of tamoxifen in rats pretreated with naringin. Choi, JS; Kang, KW, 2008) | 0.97 |
"The effects of epigallocatechin gallate (EGCG) on the oral bioavailability and pharmacokinetics of tamoxifen and its metabolite, 4-hydroxytamoxifen, were investigated in rats." | ( Effects of epigallocatechin gallate on the oral bioavailability and pharmacokinetics of tamoxifen and its main metabolite, 4-hydroxytamoxifen, in rats. Choi, JS; Shin, SC, 2009) | 0.79 |
" We assessed whether the addition of a lower dose of tamoxifen influenced anastrozole bioavailability and favorably modulated biomarkers of bone fracture, breast cancer, cardiovascular disease, and endometrial cancer risk." | ( Randomized biomarker trial of anastrozole or low-dose tamoxifen or their combination in subjects with breast intraepithelial neoplasia. Bonanni, B; Cassano, E; Cazzaniga, M; Decensi, A; Gandini, S; Guerrieri-Gonzaga, A; Johansson, H; Lien, EA; Luini, A; Macis, D; Oldani, S; Pelosi, G; Serrano, D, 2009) | 0.85 |
"The addition of a weekly tamoxifen administration did not impair anastrozole bioavailability and modulated favorably its safety profile, providing the rationale for further studies." | ( Randomized biomarker trial of anastrozole or low-dose tamoxifen or their combination in subjects with breast intraepithelial neoplasia. Bonanni, B; Cassano, E; Cazzaniga, M; Decensi, A; Gandini, S; Guerrieri-Gonzaga, A; Johansson, H; Lien, EA; Luini, A; Macis, D; Oldani, S; Pelosi, G; Serrano, D, 2009) | 0.9 |
" Furthermore, current water quality monitoring does not differentiate between soluble and colloidal phases in water samples, hindering our understanding of the bioavailability and bioaccumulation of pharmaceuticals in aquatic organisms." | ( Colloids as a sink for certain pharmaceuticals in the aquatic environment. Maskaoui, K; Zhou, JL, 2010) | 0.36 |
" Such strong pharmaceutical/colloid interactions may provide a long-term storage of pharmaceuticals, hence, increasing their persistence while reducing their bioavailability in the environment." | ( Colloids as a sink for certain pharmaceuticals in the aquatic environment. Maskaoui, K; Zhou, JL, 2010) | 0.36 |
" As aquatic colloids are abundant, ubiquitous, and highly powerful sorbents, they are expected to influence the bioavailability and bioaccumulation of such chemicals by aquatic organisms." | ( Colloids as a sink for certain pharmaceuticals in the aquatic environment. Maskaoui, K; Zhou, JL, 2010) | 0.36 |
" With the aim of improving both bioavailability and tamoxifen selective toxicity, the activity of tamoxifen embedded in calcium alginate/chitosan microparticles was studied." | ( Role of the pharmaceutical excipients in the tamoxifen activity on MCF-7 and vero cell cultures. Baggio, G; Bruni, E; Coppi, G; Iannuccelli, V; Rossi, T, 2009) | 0.86 |
" Consequently, the absolute bioavailability (AB) of tamoxifen in the presence of silybinin (2." | ( Effects of silybinin on the pharmacokinetics of tamoxifen and its active metabolite, 4-hydroxytamoxifen in rats. Choi, JS; Choi, SJ; Kim, CS; Li, C; Park, CY, 2010) | 0.87 |
" This is the first study demonstrating that single oral doses of endoxifen are safe and well tolerated and have sufficient bioavailability to reach systemically effective levels in human subjects." | ( Endoxifen, a new cornerstone of breast cancer therapy: demonstration of safety, tolerability, and systemic bioavailability in healthy human subjects. Ahmad, A; Ahmad, I; Kale, P; Krishnappa, M; Rane, RC; Shahabuddin, S; Sheikh, S, 2010) | 0.36 |
"This study examined the effect of myricetin, an anticancer compound, on the bioavailability and pharmacokinetics of tamoxifen and its metabolite, 4-hydroxytamoxifen, in rats." | ( Effects of myricetin, an anticancer compound, on the bioavailability and pharmacokinetics of tamoxifen and its main metabolite, 4-hydroxytamoxifen, in rats. Choi, JS; Kim, J; Li, C; Lim, SC, 2011) | 0.8 |
" As BCA is an inhibitor of CYP 3A and P-gp it was expected to increase the bioavailability of tamoxifen, a known substrate of CYP3A4/Pgp." | ( Reduced bioavailability of tamoxifen and its metabolite 4-hydroxytamoxifen after oral administration with biochanin A (an isoflavone) in rats. Ali, MM; Jain, GK; Kohli, K; Raju, KS; Singh, SP, 2012) | 0.89 |
" Consequently, the absolute bioavailability of tamoxifen in the presence of baicalein (3 and 10 mg/kg) was significantly increased by 47." | ( Effects of baicalein on the pharmacokinetics of tamoxifen and its main metabolite, 4-hydroxytamoxifen, in rats: possible role of cytochrome P450 3A4 and P-glycoprotein inhibition by baicalein. Choi, H; Choi, J; Kim, M; Li, C, 2011) | 0.88 |
" Biodistribution studies of (99m)Tc labeled TMX SNP in rats revealed no significant absorption however oral pharmacokinetics revealed enhanced oral bioavailability of TMX (165%) compared to TMX suspension." | ( Self nanoprecipitating preconcentrate of tamoxifen citrate for enhanced bioavailability. Devarajan, PV; Gaikwad, RV; Kapse, SV; Samad, A, 2012) | 0.64 |
"The effects of curcumin, a natural anti-cancer compound, on the bioavailability and pharmacokinetics of tamoxifen and its metabolite, 4-hydroxytamoxifen, were investigated in rats." | ( Effects of curcumin on the pharmacokinetics of tamoxifen and its active metabolite, 4-hydroxytamoxifen, in rats: possible role of CYP3A4 and P-glycoprotein inhibition by curcumin. Cho, YA; Choi, JS; Lee, W, 2012) | 0.85 |
"Tamoxifen citrate (Tmx) was formulated in nanostructured lipid carrier system (NLC) using long chain solid lipids (LCSL) and oils (LCO) with the aim to target lymphatic system to improve its bioavailability in plasma and lymphnode (initial sites for metastasis) and reduce its drug associated toxicity." | ( Long chain lipid based tamoxifen NLC. Part I: preformulation studies, formulation development and physicochemical characterization. Patravale, V; Shete, H, 2013) | 2.14 |
" At the same time, higher Caco-2 cell uptake revealed its potential for oral delivery, which was well corroborated with in vivo pharmacokinetics, which suggested ∼ 5-fold and ∼ 3-fold increase in oral bioavailability as compared to the free Tmx citrate and free QT, respectively." | ( Co-encapsulation of tamoxifen and quercetin in polymeric nanoparticles: implications on oral bioavailability, antitumor efficacy, and drug-induced toxicity. Jain, AK; Jain, S; Thanki, K, 2013) | 0.71 |
"The objective of this study was to evaluate the influence of solid lipid nanoparticles (SLN) loaded with the poorly water-soluble drug tamoxifen citrate (TC) on the in vitro antitumor activity and bioavailability of the drug." | ( In vitro cytotoxicity and bioavailability of solid lipid nanoparticles containing tamoxifen citrate. Hashem, FM; Khairy, A; Nasr, M, 2014) | 0.83 |
"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) | 0.39 |
" 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) | 0.39 |
"In vivo pharmacokinetics revealed ~8-fold and ~4-fold increase in oral bioavailability of tamoxifen and quercetin, respectively as compared to free counterparts." | ( Solidified self-nanoemulsifying formulation for oral delivery of combinatorial therapeutic regimen: part II in vivo pharmacokinetics, antitumor efficacy and hepatotoxicity. Jain, AK; Jain, S; Thanki, K, 2014) | 0.62 |
" Docking experiments raveled that 10 and 19 occupied the same binding pocket of paclitaxel with some difference in active site amino acids and good bioavailability of both the compounds." | ( Synthesis of neolignans as microtubule stabilisers. Chanda, D; Hasanain, M; Khan, F; Konwar, R; Kumar, A; Luqman, S; Masood, N; Mitra, K; Negi, AS; Pal, A; Sarkar, J; Sathish Kumar, B; Singh, A; Singh, J; Yadav, DK, 2014) | 0.4 |
" The aim was to achieve improved systemic bioavailability of Tamoxifen, prevent systemic and hepatotoxicity and enhance antitumor efficacy." | ( Tamoxifen nanostructured lipid carriers: enhanced in vivo antitumor efficacy with reduced adverse drug effects. Patravale, VB; Selkar, N; Shete, HK; Vanage, GR, 2014) | 2.09 |
"In the present study, tamoxifen-phospholipid complex (TMX-PLC) was developed and evaluated for its impact on solubility and bioavailability of tamoxifen." | ( Development of tamoxifen-phospholipid complex: novel approach for improving solubility and bioavailability. Dora, CP; Jena, SK; Singh, C; Suresh, S, 2014) | 1.07 |
"An early prediction of solubility in physiological media (PBS, SGF and SIF) is useful to predict qualitatively bioavailability and absorption of lead candidates." | ( Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. Bharate, SS; Vishwakarma, RA, 2015) | 0.42 |
" We describe the identification and characterization of a series of small-molecule, orally bioavailable SERDs which are potent antagonists and degraders of ER-α and in which the ER-α degrading properties were prospectively optimized." | ( Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. Aparicio, A; Bonnefous, C; Brigham, D; Darimont, B; Douglas, K; Govek, S; Grillot, K; Hager, JH; Heyman, R; Joseph, JD; Julien, J; Kahraman, M; Kaufman, J; Lai, A; Lee, KJ; Lu, N; Moon, MJ; Nagasawa, J; Prudente, R; Qian, J; Rix, PJ; Sensintaffar, J; Shao, G; Smith, ND, 2015) | 0.62 |
" The discovery and development of orally bioavailable SERDs provide the opportunity to evaluate the utility of eliminating ERα expression in advanced metastatic breast cancers." | ( Oral Selective Estrogen Receptor Downregulators (SERDs), a Breakthrough Endocrine Therapy for Breast Cancer. McDonnell, DP; Norris, JD; Wardell, SE, 2015) | 0.42 |
" However, direct administration of endoxifen may present the problem of low bioavailability due to its rapid first-pass metabolism via O-glucuronidation." | ( Boronic prodrug of endoxifen as an effective hormone therapy for breast cancer. Miele, L; Wang, G; Zhang, C; Zhang, Q; Zheng, S; Zhong, Q, 2015) | 0.42 |
" While the drug-drug interaction potential between flavonoids and co-ingested drugs still remain an issue, opportunities exist for the combination of flavonoids with suitable anti-cancer drugs to enhance the bioavailability of anti-cancer drugs and thereby reduce the dose size of the anti-cancer drugs and improve its therapeutic index." | ( Recent trends in preclinical drug-drug interaction studies of flavonoids--Review of case studies, issues and perspectives. Srinivas, NR, 2015) | 0.42 |
" The implications for improved bioavailability of the NP formulations were supported by cytotoxicity results that showed a similar efficacy to free dual drug formulations and even enhanced anti-cancer effects in the recovery condition." | ( Dual drug delivery of tamoxifen and quercetin: Regulated metabolism for anticancer treatment with nanosponges. Beezer, DB; Harth, E; Kravitz, A; Lockhart, JN; Stevens, DM, 2015) | 0.73 |
" Pharmacokinetic studies were conducted to evaluate the metabolism and bioavailability of the drug in mice." | ( Boronic prodrug of 4-hydroxytamoxifen is more efficacious than tamoxifen with enhanced bioavailability independent of CYP2D6 status. Miele, L; Wang, G; Zhang, C; Zhang, Q; Zheng, S; Zhong, Q, 2015) | 0.71 |
" The boronic prodrug was shown to have far superior bioavailability of 4-OHT compared to tamoxifen or 4-OHT administration as measured by the area under the plasma concentration time curve (AUC), plasma peak concentrations, and drug accumulation in tumor tissues." | ( Boronic prodrug of 4-hydroxytamoxifen is more efficacious than tamoxifen with enhanced bioavailability independent of CYP2D6 status. Miele, L; Wang, G; Zhang, C; Zhang, Q; Zheng, S; Zhong, Q, 2015) | 0.93 |
"The discovery of an orally bioavailable selective estrogen receptor downregulator (SERD) with equivalent potency and preclinical pharmacology to the intramuscular SERD fulvestrant is described." | ( Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregu Andrews, DM; Ballard, P; Bradbury, RH; Buttar, D; Callis, RJ; Currie, GS; Curwen, JO; Davies, CD; de Almeida, C; De Savi, C; Donald, CS; Feron, LJ; Gingell, H; Glossop, SC; Hayter, BR; Hussain, S; Karoutchi, G; Lamont, SG; MacFaul, P; Moss, TA; Norman, RA; Pearson, SE; Rabow, AA; Tonge, M; Walker, GE; Weir, HM; Wilson, Z, 2015) | 0.42 |
" Enhanced DNA cleavage potential, nuclear fragmentation and condensation in apoptotic cells confirm greater bioavailability of PLGA-Tmx as compared to pure Tmx in terms of receptor mediated endocytosis." | ( Controlled release of drug and better bioavailability using poly(lactic acid-co-glycolic acid) nanoparticles. Haldar, C; Maiti, P; Maurya, AK; Mishra, DP; Pandey, SK; Patel, DK; Thakur, R; Vinayak, M, 2016) | 0.43 |
"This study was undertaken to develop and investigate the effect of tamoxifen polymer-lipid hybrid nanoparticles (Tmx-PLN) on its oral bioavailability and efficacy in the 7,12-dimethylbenzanthracene (DMBA)-induced breast cancer model." | ( Development of Novel Polymer-Lipid Hybrid Nanoparticles of Tamoxifen: In Vitro and In Vivo Evaluation. Dora, CP; Jena, SK; Pawar, H; Singh, C; Suresh, S; Varthya, M, 2016) | 0.91 |
" Furthermore, It has superior oral bioavailability (AUC = 2547." | ( Fulvestrant-3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD). Akerstrom, VL; Bratton, MR; Guo, S; Liu, J; Ma, P; Ma, Y; Miele, L; Pannuti, A; Skripnikova, EV; Wang, G; Wiese, TE; Yuan, C; Zhang, C; Zhang, Q; Zheng, S; Zhong, Q, 2016) | 0.43 |
" Despite many promises, tamoxifen is associated with various challenges like low hydrophilicity, poor bioavailability and dose-dependent toxicity." | ( Chitosan-modified PLGA polymeric nanocarriers with better delivery potential for tamoxifen. Chitkara, D; Kumar, P; Kumar, R; Raza, K; Singh, B; Thakur, CK; Thotakura, N, 2016) | 0.97 |
" This drug has low oral bioavailability due to its low aqueous solubility." | ( Preparation, characterization and in-vivo evaluation of microemulsions containing tamoxifen citrate anti-cancer drug. Biriaee, A; Dehghani, F; Ebrahimi, M; Farhadian, N; Golmohammadzadeh, S; Karimi, M, 2017) | 0.68 |
"59-fold increase in relative bioavailability as compared to TMX suspension." | ( Alpha-lipoic acid-stearylamine conjugate-based solid lipid nanoparticles for tamoxifen delivery: formulation, optimization, in-vivo pharmacokinetic and hepatotoxicity study. Chand, M; Dhaundiyal, A; Jena, SK; Samal, SK; Sangamwar, AT; Sonvane, B, 2016) | 0.66 |
"α-lipoic acid-stearylamine conjugate-based SLNs have a great potential in enhancing the oral bioavailability of poorly soluble drugs like TMX." | ( Alpha-lipoic acid-stearylamine conjugate-based solid lipid nanoparticles for tamoxifen delivery: formulation, optimization, in-vivo pharmacokinetic and hepatotoxicity study. Chand, M; Dhaundiyal, A; Jena, SK; Samal, SK; Sangamwar, AT; Sonvane, B, 2016) | 0.66 |
" An alternative approach, particularly considering agents with relatively low toxicity, such as orally bioavailable fluoropyrimidines, is to continue chemotherapy until disease progression." | ( Use of maintenance endocrine therapy after chemotherapy in metastatic breast cancer. Makris, A; Miles, D; Sutherland, S, 2016) | 0.43 |
"Tamoxifen (TAM) is frequently prescribed for the management breast cancer, but is associated with the challenges like compromised aqueous solubility and poor bioavailability to the target site." | ( Biocompatible Phospholipid-Based Mixed Micelles for Tamoxifen Delivery: Promising Evidences from In - Vitro Anticancer Activity and Dermatokinetic Studies. Chitkara, D; Katare, OP; Kumar, P; Kumar, R; Malik, R; Raza, K; Sharma, G; Singh, B, 2017) | 2.15 |
"Recent studies showed an enhanced oral bioavailability of tamoxifen (TMX) by hydrophobically modified α-tocopherol succinate-g-carboxymethyl chitosan (Cmc-TS) micelles." | ( Potential of amphiphilic graft copolymer α-tocopherol succinate-g-carboxymethyl chitosan in modulating the permeability and anticancer efficacy of tamoxifen. Chand, M; Jena, SK; Kaur, S; Samal, SK; Sangamwar, AT, 2017) | 0.9 |
"Present investigation deals with formulation and evaluation of tamoxifen (TMX)-loaded liquid crystalline nanoparticles (TMX-LCNPs) for improving oral bioavailability and safety of the existing treatment." | ( Improved Oral Bioavailability, Therapeutic Efficacy, and Reduced Toxicity of Tamoxifen-Loaded Liquid Crystalline Nanoparticles. Heeralal, B; Jain, S; Kushwah, V; Swami, R; Swarnakar, NK, 2018) | 0.95 |
" We describe the design and synthesis of a series of potent benzothiophene-containing compounds that exhibit oral bioavailability and preclinical activity as SERDs." | ( Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer. Abrams, T; Baird, J; Burks, HE; Firestone, B; Gaither, LA; Hamann, LG; He, G; Kim, S; Kirby, CA; Lombardo, F; Macchi, KJ; McDonnell, DP; Mishina, Y; Norris, JD; Nunez, J; Peukert, S; Springer, C; Sun, Y; Thomsen, NM; Tiong-Yip, CL; Tria, GS; Wang, C; Wang, J; Yu, B, 2018) | 0.48 |
" Results demonstrated that extrusion significantly increased the tamoxifen oral bioavailability (p < 0." | ( Development of Hot Melt Extruded Solid Dispersion of Tamoxifen Citrate and Resveratrol for Synergistic Effects on Breast Cancer Cells. Bagde, A; Chowdhury, N; Kutlehria, S; Patel, K; Singh, M; Vhora, I, 2018) | 0.97 |
" The selective ER degrader (SERD), fulvestrant, is effective in patients with metastatic breast cancer, but its intramuscular route of administration and low bioavailability are major clinical limitations." | ( The oral selective oestrogen receptor degrader (SERD) AZD9496 is comparable to fulvestrant in antagonising ER and circumventing endocrine resistance. Brown, H; Cataldo, ML; Chamness, GC; De Angelis, C; Delpuech, O; Fu, X; Hilsenbeck, SG; Jeselsohn, R; Mitchell, T; Nagi, C; Nardone, A; Osborne, CK; Pilling, M; Rimawi, MF; Schiff, R; Shea, MJ; Trivedi, M; Veeraraghavan, J; Weir, H, 2019) | 0.51 |
"The present study aimed to develop a surface-modified biocompatible nanostructured lipid carrier (NLCs) system using polyoxyethylene (40) stearate (POE-40-S) to improve the oral bioavailability of poorly water-soluble Biopharmaceutics Classification System class-II drug like tamoxifen (TMX)." | ( Development of tamoxifen-loaded surface-modified nanostructured lipid carrier using experimental design: Damodharan, N; Poovi, G, 2020) | 1.09 |
" Tamoxifen citrate (TMX) (BCS Class II drug) with low water solubility has poor oral bioavailability in the range of 20%-30%, therefore, high doses are required for treatment with TMX." | ( Development and evaluation of polymeric micelle containing tablet formulation for poorly water-soluble drug: tamoxifen citrate. Çalış, S; Kaplan, M; Öztürk-Atar, K, 2020) | 1.68 |
" In phase 1/2 clinical studies, the efficacy of Z-endoxifen, the active isomer of endoxifen, was evaluated in patients with endocrine-refractory metastatic breast cancer as well as in patients with gynecologic, desmoid, and hormone-receptor positive solid tumors, and demonstrated substantial oral bioavailability and promising antitumor activity." | ( Endoxifen, an Estrogen Receptor Targeted Therapy: From Bench to Bedside. Goetz, MP; Hawse, JR; Jayaraman, S; Reid, JM, 2021) | 0.62 |
" Weight, race on clearance, and aspartate aminotransferase on the absorption rate constant were identified as significant covariates in the final model." | ( Population Pharmacokinetics of Z-Endoxifen in Patients With Advanced Solid Tumors. Adjei, AA; Ames, MM; Buhrow, SA; Covey, JM; Goetz, MP; Koubek, EJ; Larson, TR; McGovern, RM; Ralya, AT; Reid, JM; Takebe, N, 2022) | 0.72 |
" Lung and liver tissues from EC Arg1 KO mice showed respectively increase or decrease in nitrosyl-heme species, indicating that the lack of endothelial Arg1 affects NO bioavailability in these organs." | ( Downregulation of eNOS and preserved endothelial function in endothelial-specific arginase 1-deficient mice. Carlström, M; Cortese-Krott, MM; Grandoch, M; Guimaraes Braga, DD; Heuser, SK; Kelm, M; Leo, F; Li, J; LoBue, A; Lundberg, JO; Montero, L; Olsson, A; Pernow, J; Schmitt, JP; Schmitz, OJ; Schneckmann, R; Srivrastava, T; Suvorava, T; Weitzberg, E; Zhuge, Z, 2022) | 0.72 |
" Re-engagement of the pharmaceutical and biotechnology industries with ERα as a drug target has been further underpinned by the impressive advances made in medicinal chemistry, enabling desirable mechanistic features - high potency full ERα antagonism - to be combined with improved drug-like properties - oral bioavailability and optimized pharmacokinetics." | ( Clinical Translation: Targeting the Estrogen Receptor. Lauchle, JO; Metcalfe, C, 2022) | 0.72 |
" Here, we characterized the pharmacokinetics and oral bioavailability of ENDX in female rats and dogs." | ( Bioavailability and Pharmacokinetics of Endoxifen in Female Rats and Dogs: Evidence to Support the Use of Endoxifen to Overcome the Limitations of CYP2D6-Mediated Tamoxifen Metabolism. Ames, MM; Buhrow, SA; Goetz, MP; Jia, L; Koubek, EJ; Reid, JM; Safgren, SL, 2023) | 1.11 |
" A higher bioavailability of tamoxifen in older patients may explain the observed differences." | ( Tamoxifen pharmacokinetics and pharmacodynamics in older patients with non-metastatic breast cancer. Gelderblom, H; Guchelaar, HJ; Moes, DJAR; Portielje, JEA; Sanchez-Spitman, A; Souwer, ETD; Swen, JJ; van Gelder, T, 2023) | 2.64 |
Adenomyosis was induced in 28 female ICR mice neonatally dosed with tamoxifen. Endogenous sex steroid levels were altered in mice via gonadectomy, via physiological or supraphysiological doses of testosterone and/or estradiol.
Excerpt | Relevance | Reference |
---|---|---|
"High dosage MAP (medroxyprogesterone acetate) was used in the treatment of very advanced breast cancer." | ( High dose medroxyprogesterone-acetate treatment in advanced mammary carcinoma. A phase II investigation. Mattsson, W, 1978) | 0.26 |
"6 Since the administration of anti-oestrogenic doses of non-steroidal anti-oestrogens during a 3-day uterine weight test did not inhibit the total binding of oestradiol in the uterus, or affect the translocation of the steroid to the nucleus, the mechanism of action of non-steroidal anti-oestrogens over the range of the partial agonist dose-response curve must involve an interaction, or competition of oestradiol-17beta- and anti-oestrogen-oestrogen receptor complexes for sites within the nucleus." | ( The binding of [3H]-oestradiol-17 beta in the immature rat uterus during the sequential administration of non-steroidal anti-oestrogens. Jordan, VC; Naylor, KE, 1979) | 0.26 |
" In the 10-mg bid dosage group, 30 of the 31 patients were considered evaluable for efficacy." | ( Phase II study of tamoxifen: report of 74 patients with stage IV breast cancer. Band, PR; Israel, L; Lerner, HJ; Leung, BS, 1976) | 0.59 |
" Two dosage schedules were compared." | ( Suppression of lactation by an antiestrogen, tamoxifen. Shaaban, MM, 1975) | 0.51 |
" Furthermore, a dose-response relationship has been reported with anthracyclines used as adjuvant therapy or in metastatic disease." | ( [Cancer of the breast]. Maugard-Louboutin, C, 1992) | 0.28 |
" Meanwhile, Provera exerted dose-response inhibition on both AE7 and ECC-1 cell lines." | ( Determination of hormonal response in uterine cancer cell lines by the ATP bioluminescence assay and flow cytometry. Angioli, R; Averette, HE; Donato, D; Nguyen, HN; Penalver, M; Perras, J; Ramos, R; Sevin, BU; Voigt, W, 1992) | 0.28 |
" Our results show that a dose-response relationship exists between cell growth inhibition and cell cycle measurements for human plasma with added toremifene or tamoxifen, and also for human plasma specimens containing drug and its metabolites after treatment." | ( A bioassay for antiestrogenic activity--potential utility in drug development and monitoring effective in vivo dosing. DeGregorio, M; Emshoff, V; Koester, S; Minor, P; Wiebe, V; Wurz, G, 1992) | 0.48 |
" On cessation of dosing there was a loss of adducts from the liver DNA." | ( Genotoxic potential of tamoxifen and analogues in female Fischer F344/n rats, DBA/2 and C57BL/6 mice and in human MCL-5 cells. Crofton-Sleigh, C; Davies, A; de Matteis, F; Hewer, A; Phillips, DH; Smith, LL; Venitt, S; White, IN, 1992) | 0.59 |
" Although systemic therapy has improved the prognosis for breast cancer, numerous issues, such as the optimal combination and dosage of drugs, the worth of chemohormonotherapy and the appropriate sequencing of treatment, remain the subjects of continuing investigation." | ( Recent trends in the management of breast cancer. 3. Controversies in the use of adjuvant chemotherapy, hormonotherapy and radiotherapy for breast cancer. Donegan, WL, 1992) | 0.28 |
" A significant dose-response relationship was observed for the potentiating effect of tamoxifen on TCDD lethality." | ( The potentiation of 2,3,7,8-tetrachlorodibenzo-p-dioxin toxicity by tamoxifen in female CD1 mice. Gallo, MA; MacKenzie, SA; Thomas, T; Umbreit, TH, 1992) | 0.74 |
" In the first approach medroxyprogesterone dosage increased up to 400 mg a day, achieved better results in curative as well as adjuvant treatment of advanced or early gynecologic cancers." | ( New trends in the use of medroxyprogesterone acetate as a chemotherapeutic agent in gynecologic malignancies. Bonte, J; Vanderstappen, D, 1992) | 0.28 |
" To determine whether the inabilities of TAM to stimulate cell proliferation and induce PR were a function of TAM concentration, dose-response experiments were performed." | ( The estrogenic and antiestrogenic properties of tamoxifen in GH4C1 pituitary tumor cells are gene specific. Baldwin, TM; Beams, FE; Gilchrist, CA; Hrbek, MJ; Shull, JD, 1992) | 0.54 |
"Twenty-nine Nigerian women with advanced breast carcinoma treated with Tamoxifen (Nolvadex ICI) at a dosage of 20 mg twice daily have been reviewed." | ( Tamoxifen in the management of advanced breast carcinoma in Nigerian women. Ajayi, OO; Ihekwaba, FN; Senbanjo, RO, ) | 1.81 |
" Serum tamoxifen levels were elevated to nearly 400 ng ml-1 by injecting 1 mg day-1 tamoxifen (IP 3 x weekly); this dosage was more effective at inhibiting oestradiol stimulated tumour growth than subcutaneous tamoxifen capsules alone." | ( Reversible control of oestradiol-stimulated growth of MCF-7 tumours by tamoxifen in the athymic mouse. Iino, Y; Johnson, DA; Jordan, VC; Langan-Fahey, SM; Ricchio, M; Thompson, ME; Wolf, DM, 1991) | 0.97 |
" Animals were dosed daily, a day after implantation, for 14 days with either 17 beta-estradiol or tamoxifen at different doses." | ( The effects of estrogens on cartilage degradation using in vivo and in vitro models. Chander, CL; Desa, FM, 1991) | 0.5 |
" Tamoxifen was administered in a daily dosage of 30 mg (3 x 1 tablet)." | ( [Results of treatment of breast cancer with tamoxifen]. Freisleben, G; Pietrzak, J; Pniewska, I; Polubiec, A, 1991) | 1.45 |
" One hundred and seven women were treated at one of six dosage levels (10, 20, 40, 60, 200, or 400 mg/d orally) for at least 8 weeks." | ( Phase I study of toremifene in patients with advanced cancer. Green, M; Haller, D; Hamm, JT; Kohler, PC; Shemano, I; Tormey, DC, 1991) | 0.28 |
" Endogenous sex steroid levels were altered in mice via gonadectomy, via physiological or supraphysiological doses of testosterone and/or estradiol, and via tamoxifen dosing to antagonize estrogens." | ( Effect of sex steroids on cocaine lethality in male and female mice. Davis, WM; Dickerson, GA; Waters, IW; Wilson, MC, 1991) | 0.48 |
" With this method, we determined the drug and metabolite concentrations during one dosing interval in various tissues (brain, fat, liver, heart, lung, kidney, uterus, and testes) of rats given tamoxifen once daily for 3 or 14 days, and in various normal and malignant tissues obtained during surgery or at autopsy from patients with breast cancer treated with tamoxifen." | ( Distribution of tamoxifen and its metabolites in rat and human tissues during steady-state treatment. Lien, EA; Solheim, E; Ueland, PM, 1991) | 0.82 |
" 82 patients in 2 groups who were diagnosed with metastatic mammary carcinoma received Tamoxifen (ICI) and Tamoxifen (Ebewe) orally in a dosage of 20 to 40 mg/day." | ( [The treatment of metastasizing breast carcinoma using antiestrogens]. Palucka-Bartoszewicz, A; Pienkowska, F; Pienkowski, T; Schneider, J; Zborzil, J, 1991) | 0.5 |
" Dose-response curves of GCDFP-15 mRNA contents and GCDFP-15 levels in culture media and cells versus hormone or antihormone concentration have been established." | ( Stimulatory effect of oestradiol-17 beta and tamoxifen on gross cystic disease fluid protein 15,000 production and mRNA levels in T47D human breast cancer cells. Carlisi, I; Collette, J; Dejardin, L; Delvenne, C; Franchimont, P; Gol-Winkler, R; Haagensen, DE, 1991) | 0.54 |
" We investigated melatonin's effect on the anchorage-independent growth of MCF-7 cells as well as the dose-response characteristics of this indoleamine under clonogenic culture conditions." | ( Effects of the pineal hormone melatonin on the anchorage-independent growth of human breast cancer cells (MCF-7) in a clonogenic culture system. Blask, DE; Cos, S, 1990) | 0.28 |
" There is apparently a dose-response between megestrol acetate and breast cancer, along with a response dependent on the number and type of estrogen and progestin receptors." | ( Megestrol acetate: clinical experience. Canetta, R; Kelley, S; Nicaise, C; Rozencweig, M; Schacter, L; Smaldone, L, 1989) | 0.28 |
" The often discussed intrinsic estrogen activity of the antiestrogens was present only in the highest dosage tested of tamoxifen." | ( Antiestrogen and antiandrogen administration reduce bone mass in the rat. Bauss, F; Feldmann, S; Lempert, UG; Minne, HW; Parvizi, S; Pfeifer, M; Ziegler, R, 1989) | 0.49 |
" The estrogen agonist and antagonist effects of tamoxifen (TAM, a triphenylethylene antiestrogen) and chlorotrianisene (TACE, a triphenylethylene estrogen) on anterior pituitary glandular kallikrein and PRL were examined to see if TAM and TACE differentially affect these estrogen response of lactotrophs after in vivo dosing of rats." | ( Differential responses of pituitary kallikrein and prolactin to tamoxifen and chlorotrianisene. Hatala, MA; Pagano, PJ; Powers, CA, 1989) | 0.77 |
" Tamoxifen in high dosage and in some reports at conventional dosage is associated with ocular toxicity." | ( A controlled study of the ocular effects of tamoxifen in conventional dosage in the treatment of breast carcinoma. Longstaff, S; O'Keeffe, M; Ogston, S; Preece, P; Sigurdsson, H, 1989) | 1.45 |
" 4) Among nine patients, one PR and three NC case were observed with subsequent increase of the dosage to 40 mg/day after 20 mg/day." | ( [A comparison of two doses of tamoxifen in patients with advanced breast cancer: 20 mg/day versus 40 mg/day]. Aikawa, T; Inaji, H; Takatsuka, Y; Yayoi, E, 1989) | 0.57 |
" For both compounds the interaction with insulin was complex and characterized by a bell-shaped dose-response curve." | ( Effects of antioestrogens on the proliferation of MCF-7 human breast cancer cells. Newboult, E; Peters, SW; Wakeling, AE, 1989) | 0.28 |
" Thirty-four received treatment B: tamoxifen 30 mg per day and after relapse, high dosage of MPA alone." | ( [Hormonotherapy of metastatic breast cancer with tamoxifen and medroxyprogesterone acetate. Randomized trial comparing alternating sequences with successive applications]. Bonichon, F; Chauvergne, J; Durand, M; Mauriac, L, 1986) | 0.8 |
"A controlled trial has been conducted in which 60 women with mastalgia were randomly allocated to receive tamoxifen at a dosage of either 10 mg or 20 mg daily for either 3 or 6 months." | ( Dosage and duration of tamoxifen treatment for mastalgia: a controlled trial. Caleffi, M; Chaudary, MA; Fentiman, IS; Hamed, H, 1988) | 0.8 |
" The data fitted log dose-response curves." | ( The effect of oestriol and tamoxifen on oestradiol induced prolactin secretion in anaesthetised rats. Gilna, P; Martin, F, 1986) | 0.57 |
" The sperm density increased significantly, but we could not ascertain whether a dosage of 2 X 20 mg/die will provide better therapeutic results." | ( [Therapeutic results with tamoxifen in oligospermia. II. Hormonal analysis and semen parameters]. Adam, W; Armann, J; Bantel, E; Cörlin, R; Egenrieder, H; Fierlbeck, G; Hook, B; Schieferstein, G; Schiek, A; Schubring, G, ) | 0.43 |
" One of each cycle was given preoperatively at half dosage and five of each were repeated postoperatively at full dosage." | ( Six-year results of a multimodality treatment strategy for locally advanced breast cancer. Arrigo, C; Balikdjian, D; Cantraine, F; de Valeriola, D; Heuson, JC; Loriaux, C; Mattheiem, WH; Paridaens, R; Piccart, MJ, 1988) | 0.27 |
" It is concluded that, while the priming action exerted by E2B on PgRs might explain the potentiating effect shown by E2B on MPA activity, the synergism observed between TMX and MPA should be explained on an extrareceptorial basis, an induction on PgR synthesis by TMX not being evident at the dosage and priming time employed in this study." | ( Effects of tamoxifen, estradiol benzoate and medroxyprogesterone acetate on the growth of DMBA-induced rat mammary carcinoma. Barbi, GP; Boccardo, F; Dandolo, G; De Menech, R; Guarneri, D; Moro, MG; Paganuzzi, M; Pino, G; Sanguineti, M; Zanardi, S, 1985) | 0.66 |
" By contrast, the timing of the ODC activity peak induced by tamoxifen and monohydroxytamoxifen was highly dependent upon the dosing conditions and was delayed to 18 h at lower tamoxifen doses." | ( Estrogen- and antiestrogen-induced ornithine decarboxylase activity and uterine growth in the rat. Branham, WS; Leamons, ML; Sheehan, DM, 1988) | 0.52 |
" At higher E2- or AE-concentrations this positive effect was lost, resulting in bell shaped dose-response curves." | ( Effects of estradiol and some antiestrogens (clomiphene, tamoxifen, and hydroxytamoxifen) on luteinizing hormone secretion by rat pituitary cells in culture. Emons, G; Knuppen, R; Ortmann, O; Thiessen, S, 1986) | 0.52 |
" When added to the oviduct cell cultures 3 days after they were plated out, estradiol increased the steady-state concentration (relative to total RNA) of 7F and 6G mRNAs by 3- to 7-fold after 60-80 h, but with different time-course and dose-response kinetics for the two messages." | ( Hormonal regulation of RNA synthesis and specific gene expression in Xenopus oviduct cells in primary culture. Marsh, J; Tata, JR, 1987) | 0.27 |
" This became more clearly apparent when cells were treated with the 4-hydroxylated derivatives of these compounds where, because of enhanced affinity for the oestrogen receptor (ER), the dose-response curves for the two components could be separated." | ( Mechanisms of growth inhibition by nonsteroidal antioestrogens in human breast cancer cells. Hall, RE; Ruenitz, PC; Sutherland, RL; Watts, CK, 1987) | 0.27 |
"A 57-year-old woman developed bilateral optic neuritis after being treated for 6 months with tamoxifen in the dosage of 30 to 40 mg orally a day." | ( Bilateral optic neuritis evolved during tamoxifen treatment. Pugesgaard, T; Von Eyben, FE, 1986) | 0.76 |
" Estrogens are approximately 10-fold more potent in stimulating cell number than in stimulating prolactin production, but the antiestrogens showed the same dose-response for both effects." | ( Characterization of antiestrogen stimulation of cell number and prolactin production. Amara, JF; Dannies, PS, 1986) | 0.27 |
" The dose-response relationship was biphasic; 10(-10) M Ly-117018 and 10(-7) M tamoxifen caused maximal stimulation, but higher concentrations caused no stimulation and completely antagonized the 5-fold stimulation caused by estrogen." | ( Antiestrogens are partial estrogen agonists for prolactin production in primary pituitary cultures. Amara, JF; Dannies, PS; Martinez-Campos, A, 1986) | 0.5 |
" As systemic cancer chemotherapy was not so effective, targeted cancer chemotherapy for lymph node metastasis and carcinomatous peritonitis was carried out by modification of drug dosage form as fat emulsion and activated carbon incorporating anticancer agent." | ( [Combined therapy of gastric cancer]. Takahashi, T, 1985) | 0.27 |
" In one variant tamoxifen dosage was 20 mg (2 tablets) daily taken orally from day 5 to day 25 of the menstrual cycle, associated with 10 mg (2 tablets) of lynestrenol daily, only during the last 15 days." | ( Combined tamoxifen-lynestrenol treatment in benign breast disease. Cupceancu, B, ) | 0.89 |
" Cyclic treatment with a combination of chlorambucil, methotrexate and 5-fluorouracil was more myelotoxic and required more extensive dose reductions than treatment with cyclophosphamide, methotrexate and 5-fluorouracil with the dosage used." | ( Influence of adjuvant chemotherapy on the blood lymphocyte population in operable breast carcinoma. Comparison between two types of treatments. Baral, E; Blomgren, H; Petrini, B; Strender, LE; Wallgren, A; Wasserman, J, 1982) | 0.26 |
" Menopausal status did not seem to influence response, and no dose-response relationship has been documented." | ( Antiestrogen therapy of breast cancer. Lippman, ME, 1983) | 0.27 |
" Provided the dosage is the same for both groups, there is no evidence of any clear difference between pre-menopausal and post-menopausal patients." | ( [Adjuvant chemotherapy in breast cancer: present status]. Eidtmann, H; Jonat, W; Kaufmann, M; Kubli, F; Maass, H, 1984) | 0.27 |
" Thus far, we have defined dose-response curves for tamoxifen, adriamycin, thiotepa, and methotrexate." | ( In vitro drug screening and individualized treatment planning for cancer patients. Safa, AR; Tseng, MT, 1983) | 0.52 |
" The partial uterotrophic effect of monohydroxytamoxifen and full uterotrophic effects of estradiol were both inhibited by high doses of LY117018 at an approximate dosage ratio of 1:24, w/w." | ( Differential antiestrogen action in the immature rat uterus: a comparison of hydroxylated antiestrogens with high affinity for the estrogen receptor. Gosden, B; Jordan, VC, 1983) | 0.52 |
" Dose-response analysis showed that, in the R27 variant, TAM and OH-TAM acquired the ability to induce the Mr 52,000 protein at concentrations compatible with their relative affinities for the estrogen receptor, while these antiestrogens were inefficient in the wild MCF7 cells." | ( Induction of two estrogen-responsive proteins by antiestrogens in R27, a tamoxifen-resistant clone of MCF7 cells. Derocq, D; Lippman, ME; Nawata, H; Rochefort, H; Vignon, F, 1984) | 0.5 |
" Analysis of the dose-response curves shows induction by Oe2 to be 10 times and 50 times greater than Oe3 and Oe4, respectively." | ( Different effects of oestradiol, oestriol, oestetrol and of oestrone on human breast cancer cells (MCF-7) in long term tissue culture. Bayard, F; Jozan, S; Kreitmann, B, 1981) | 0.26 |
" No significant dose-response relationships emerged." | ( Evaluation of tamoxifen doses with and without fluoxymesterone in advanced breast cancer. Cassidy, JG; Edwards, BK; Lippman, ME; Tormey, DC, 1983) | 0.63 |
"In 17 patients treated with tamoxifen in a low dosage (30 mg daily) ophthalmological examination was performed." | ( Retinopathy caused by treatment with tamoxifen in low dosage. Nielsen, NV; Vinding, T, 1983) | 0.83 |
" However, in the rat, LY117018 was more effective against the less potent compound tamoxifen, at a 6:1 dosage ratio compared with a 24:1 dosage ratio required for the potent compound monohydroxytamoxifen." | ( Inhibition of the uterotropic activity of estrogens and antiestrogens by the short acting antiestrogen LY117018. Gosden, B; Jordan, VC, 1983) | 0.49 |
" This hormonal therapy should be suggested, where is possible, by the results of hormonal dosage on plasma and urine." | ( [Treatment of breast cancer in aged women]. Beani, G; Berta, V; Perelli-Ercolini, M, 1980) | 0.26 |
"The data on adjuvant chemotherapy for mammary carcinoma obtained from animal models suggest that (a) systemic chemotherapy combined with tumour excision provides more long-term cures than either method alone, (b) systemic treatment may be effective in eradicating occult micrometastases and (c) the effect of systemic chemotherapy decreases with advancing tumour stage preoperatively, with increasing time lag between operation and chemotherapy, and as the drug dosage decreases." | ( Symposium on the management of early breast cancer (stages I and II). Part II: Clinical experience with treatment methods. 4. Adjuvant chemoimmunotherapy. Bowman, DM, 1981) | 0.26 |
" At the time of progression, increasing the dosage to 20 mg twice daily resulted in an objective remission now lasting 8+ months." | ( Tamoxifen-induced remission in breast cancer by escalating the dose to 40 mg daily after progression on 20 mg daily: a case report and review of the literature. Arafah, BM; Manni, A, 1981) | 1.71 |
"Blood tamoxifen levels were determined for patients with metastatic breast cancer following initial and chronic dosing at twice daily 10 mg/m2 or a 20 mg/m2 single dose." | ( Clinical pharmacology of tamoxifen in patients with breast cancer: correlation with clinical data. Cain, L; El-Serafi, M; Fabian, C; Hearne, E; Sternson, L, 1981) | 1.05 |
" over the range of the partial agonist dose-response curve, the biological activity of tamoxifen is the net result of the activities of the parent compound and its metabolites." | ( Evidence for the metabolic activation of non-steroidal antioestrogens: a study of structure-activity relationships. Allen, KE; Clark, ER; Jordan, VC, 1980) | 0.48 |
" We detected no clear evidence of a dose-response effect for TOR." | ( Randomized comparison of tamoxifen and two separate doses of toremifene in postmenopausal patients with metastatic breast cancer. Berris, RF; Bezwoda, WR; Goedhals, L; Hacking, A; Hayes, DF; Jones, SE; Mailliard, JA; Shemano, I; Van Zyl, JA; Vogel, CL, 1995) | 0.59 |
" The pattern of 32P-postlabelled adducts was not the same as those seen in rats dosed with this drug." | ( 32P-postlabelled DNA adducts in liver obtained from women treated with tamoxifen. Martin, EA; Powles, TJ; Rich, KJ; Smith, LL; White, IN; Woods, KL, 1995) | 0.52 |
" Dose-response studies show the S554fs mutant to be the most potent of the three ER mutants as a repressor of estrogen action in these cells." | ( Repression of endogenous estrogen receptor activity in MCF-7 human breast cancer cells by dominant negative estrogen receptors. Ince, BA; Katzenellenbogen, BS; Schodin, DJ; Shapiro, DJ, 1995) | 0.29 |
" Antineoplastic efficacy of tamoxifen at this dosage in this cohort of patients was at best marginal and well in the range associated with the occurrence of spontaneous remissions." | ( Lack of therapeutic efficacy of tamoxifen in advanced renal cell carcinoma. Atzpodien, J; Fenner, M; Kirchner, H; Menzel, T; Poliwoda, H; Schomburg, A, 1993) | 0.86 |
" There may be a trend toward a dose-response effect, which represents a suitable topic for a future prospective trial." | ( Hormonal palliation of chemoresistant ovarian cancer: three consecutive phase II trials of the Mid-Atlantic Oncology Program. Ahlgren, JD; Alt, D; Ellison, NM; Gottlieb, RJ; Laluna, F; Lokich, JJ; Sinclair, PR; Ueno, W; Wampler, GL; Yeung, KY, 1993) | 0.29 |
" The major adducts formed following incubation of DNA with tamoxifen had similar Rf values to two of the 32P-postlabelled adducts seen following dosing of rats with tamoxifen." | ( Peroxidase activation of tamoxifen and toremifene resulting in DNA damage and covalently bound protein adducts. Davies, AM; Jones, RM; Lim, CK; Martin, EA; Smith, LL; White, IN, 1995) | 0.84 |
" The greater potential of mouse liver microsomes to activate tamoxifen, relative to rats, does not reflect DNA damage or hepatocarcinogenicity seen following dosing with tamoxifen in vivo." | ( Species differences in the covalent binding of [14C]tamoxifen to liver microsomes and the forms of cytochrome P450 involved. De Matteis, F; Gibbs, AH; Henderson, C; Lim, CK; Smith, LL; White, IN; Wolf, CR, 1995) | 0.78 |
" Some of the primary response genes in this network may exhibit dose-response and induction kinetics similar to pS2, which is constitutively upregulated in the MCF7/MIII, MCF7/LCC1 and MCF7/LCC2 cells." | ( Hormonal carcinogenesis in breast cancer: cellular and molecular studies of malignant progression. Baumann, K; Brunner, N; Clarke, R; Freter, C; James, M; Leonessa, F; Lippman, J; Skaar, T; Thompson, EW, 1994) | 0.29 |
" A dose-response effect was observed at ICI 182,780 concentrations of up to 5 microM." | ( Differential effects of estrogen, tamoxifen and the pure antiestrogen ICI 182,780 in human drug-resistant leukemia cell lines. Ching, M; de Luise, M; Hu, XF; Marschner, IC; Wakeling, A; Wall, DM; Zalcberg, JR, 1993) | 0.57 |
"After previous treatment failure using tamoxifen either alone or in combination with kallikrein, 25 patients with idiopathic oligoasthenoteratozoospermia (OAT syndrome) were subjected to 3 months of treatment with pentoxifylline at a dosage of 1200 mg/day." | ( Oral pentoxifylline in therapy-resistant idiopathic OAT syndrome. Ludvik, G; Maier, U; Szabo, N, ) | 0.4 |
" The issues under investigation include best chemotherapy dosage and duration, identification of risk factors and the role of preoperative chemotherapy." | ( ["State of the art" of adjuvant chemo-endocrine therapy for breast cancer in Japan]. Ikeda, T, 1994) | 0.29 |
" pretreatment with pentachlorophenol (20 mg/kg) 1 h before dosing with tamoxifen." | ( Strong intensification of mouse hepatic tamoxifen DNA adduct formation by pretreatment with the sulfotransferase inhibitor and ubiquitous environmental pollutant pentachlorophenol. Bi, J; Mabon, N; Moorthy, B; Randerath, K; Sriram, P, 1994) | 0.79 |
" Female Sprague-Dawley rats were dosed with equimolar doses of tamoxifen (11." | ( Alterations of drug metabolizing and antioxidant enzyme activities during tamoxifen-induced hepatocarcinogenesis in the rat. Ahotupa, M; Hirsimäki, P; Mäntylä, E; Pärssinen, R, 1994) | 0.76 |
" Thus, tamoxifen dosage may be a critical factor in the subsequent occurrence of endometrial cancer." | ( Descriptive clinicopathologic study of 17 patients with endometrial cancer during or after adjuvant tamoxifen in early breast cancer. Fornander, T; Hellström, AC; Moberger, B, 1993) | 0.96 |
" There were 102 male and 104 female controls dosed with vehicle alone." | ( Two-year carcinogenicity study of tamoxifen in Alderley Park Wistar-derived rats. Goonetilleke, R; Greaves, P; Nunn, G; Orton, T; Topham, J, 1993) | 0.57 |
" The dosage administered was estimated to be that necessary to achieve tissue concentrations within the low micromolar range, shown necessary to inhibit PKC in these tumors in vitro, and is approximately 5 times that used for standard antiestrogen therapy." | ( Clinical and radiographic response in a minority of patients with recurrent malignant gliomas treated with high-dose tamoxifen. Apuzzo, ML; Conti, PS; Couldwell, WT; DeGiorgio, CM; Ehresmann, GR; Hinton, DR; Weiner, LP; Weiss, MH, 1993) | 0.5 |
"In this nonblinded, controlled multicenter trial, postmenopausal women were randomly assigned to receive graded doses of toremifene and tamoxifen or no antiestrogen to assess dose-response levels and evaluation methodology." | ( Antiestrogenic potency of toremifene and tamoxifen in postmenopausal women. Bump, RC; Gams, RA; Harry, DS; Hickox, PG; Homesley, HD; Mullin, TJ; O'Toole, RV; Rebar, RW; Shemano, I; Wentz, AC, 1993) | 0.75 |
" No tumor was observed in the toremifene-treated rats (48 mg/kg per day) either after 52 weeks of dosing or after the recovery period." | ( Tamoxifen induces hepatocellular carcinoma in rat liver: a 1-year study with two antiestrogens. Hirsimäki, P; Hirsimäki, Y; Nieminen, L; Payne, BJ, 1993) | 1.73 |
" A dose-response curve was always consistently obtained using estradiol-17 beta (E2), with a mid point at around 100 nM E2 and a maximum response at around 1000 nM." | ( Vitellogenin synthesis in cultured hepatocytes; an in vitro test for the estrogenic potency of chemicals. Bennetau, B; Dunoguès, J; Flouriot, G; Foucher, JL; Le Gac, F; Pelissero, C; Sumpter, JP, 1993) | 0.29 |
" Three dosage schedules were used: single oral dose of 40 mg tamoxifen alone and in combination with 200 mg RU 486, and 40 mg tamoxifen for three consecutive days starting on the first day after the luteinizing hormone (LH) surge." | ( Effect of tamoxifen alone and in combination with RU 486 on the endometrium in the mid-luteal phase. Bygdeman, M; Cekan, S; Johannisson, E; Seppälä, M; Swahn, ML, 1993) | 0.93 |
"0001; SR all dosing errors v MEMS all dosing errors, P < ." | ( Adherence to oral tamoxifen: a comparison of patient self-report, pill counts, and microelectronic monitoring. Brenner, DE; Calzone, KA; Mele, C; Waterhouse, DM, 1993) | 0.62 |
" Thus, under dosing conditions commonly used to assess uterotrophic activity, these "antiestrogens" are complete, albeit less potent, estrogen agonists in the luminal epithelium and, unlike estrogens, induce hypertrophy in the glandular epithelium." | ( Differential sensitivity of rat uterine growth and epithelium hypertrophy to estrogens and antiestrogens. Branham, WS; Sheehan, DM; Zehr, DR, 1993) | 0.29 |
"The authors describe three cases of tamoxifen-associated steatohepatitis, which resulted from a daily dosage of 20 mg used as the adjuvant treatment of breast carcinoma." | ( Tamoxifen-associated steatohepatitis--report of three cases. Baptista, A; Camilo, ME; de Costa, EB; de Moura, MC; Pinto, HC; Valente, A, 1995) | 2.01 |
", approximately 35% [CR+PR] in unselected patients), although dosage regimens of the new antiestrogens are higher than the 20 mg tamoxifen required daily." | ( Alternate antiestrogens and approaches to the prevention of breast cancer. Jordan, VC, 1995) | 0.5 |
" Significant increases in the production of females were detected, but only in the groups receiving the highest dosage of estradiol-17 beta (1." | ( Steroid-induced sex determination at incubation temperatures producing mixed sex ratios in a turtle with TSD. Crews, D; Wibbels, T, 1995) | 0.29 |
" In OVX rats treated with DRO, body weight decreased significantly in a dose-response manner, and total serum cholesterol was significantly reduced by 65% to 70% compared to both sham and OVX controls." | ( Effects of droloxifene on prevention of cancellous bone loss and bone turnover in the axial skeleton of aged, ovariectomized rats. Chen, HK; Jee, WS; Ke, HZ; Ma, YF; Pirie, CM; Qi, H; Simmons, HA; Thompson, DD, 1995) | 0.29 |
" The log-rank test showed no statistical difference between the dosage groups." | ( Therapeutic effects of the aromatase inhibitor fadrozole hydrochloride in advanced breast cancer. Bonnefoi, HR; Coombes, RC; da Luz, RJ; Dowsett, M; Houston, SJ; Powles, TJ; Rubens, RD; Smith, IE; Trunet, PF, 1996) | 0.29 |
" In rats, long-term dosing leads to the development of hepatocellular tumours." | ( Chemoprevention of breast cancer by tamoxifen: risks and opportunities. Smith, LL; White, IN, 1995) | 0.57 |
" Five weeks of oral dosing confirmed that ethynyl estradiol, tamoxifen, and raloxifene are potent inhibitors of the loss in volumetric bone mineral density (BMD, mg/cc) induced by ovariectomy, as measured by computed tomography." | ( Raloxifene, tamoxifen, nafoxidine, or estrogen effects on reproductive and nonreproductive tissues in ovariectomized rats. Bryant, HU; Rippy, MK; Sato, M, 1996) | 0.91 |
" These include novel dosing and scheduling strategies, newer active agents, fresh biochemical targets, and different combinations of chemotherapy with hormonal therapy." | ( Adjuvant drug therapy for operable breast cancer. Hudis, CA; Norton, L, 1996) | 0.29 |
" The factors involved in the genesis of these lesions remain poorly understood but a combination of inherited factors and cumulative tamoxifen dosage may be important." | ( The effects of tamoxifen on the uterus. Ismail, SM, 1996) | 0.85 |
" We conclude that the dosage and schedule of vinblastine and tamoxifen used in this study is inactive in the treatment of metastatic hormone refractory prostate cancer." | ( A phase II evaluation of oral tamoxifen and intermittent intravenous vinblastine in hormone-refractory adenocarcinoma of the prostate. Esper, PS; Flaherty, LE; Pienta, KJ; Redman, BG, 1996) | 0.82 |
" Tamoxifen did not induce malignancies in mice when administered according to dosing protocols that are effective in inducing hepatocellular carcinomas in rat liver." | ( Review of the toxicology of tamoxifen. Wogan, GN, 1997) | 1.5 |
" The higher dosage tamoxifen given group animals show significantly favourable results from therapy stand point when compared to diseased group." | ( Effect of tamoxifen on lipids and lipid metabolising marker enzymes in experimental atherosclerosis in Wistar rats. Sachdanandam, P; Thangaraju, M; Vinitha, R, 1997) | 1.03 |
" However, biochanin A, flavone, or chrysin could inhibit the activity of estradiol in a dose-response manner with IC50 values of 500 nM, 2 microM, and 10 microM, respectively." | ( The estrogenic and antiestrogenic activities of phytochemicals with the human estrogen receptor expressed in yeast. Arnold, SF; Collins, BM; McLachlan, JA, 1997) | 0.3 |
" Liver DNA from animals dosed with tamoxifen at 10 mg/kg also showed a similar increase in MF." | ( Tamoxifen causes gene mutations in the livers of lambda/lacI transgenic rats. Davies, R; Festing, MF; Martin, EA; Oreffo, VI; Smith, LL; Styles, JA; White, IN, 1997) | 2.02 |
" For the future, clinical trials and laboratory advances indicate that novel dosing and scheduling of chemotherapy agents combined with newer modalities may provide even greater impact against occult disseminated disease." | ( Systemic treatment for stage I and stage II breast cancer. Borgen, P; Hudis, CA, 1997) | 0.3 |
" Dose-response experiments showed no significant difference in the rate of LDL uptake when arteries were perfused with estradiol at physiological concentrations (0." | ( Nitric oxide mediates LDL uptake in the artery wall in response to high concentrations of 17 beta-estradiol. Roberts, KA; Rutledge, JC; Woo, MM, 1997) | 0.3 |
" We found no retinopathy in patients receiving tamoxifen within the first 3 years of treatment or in patients receiving a total tamoxifen dosage of less than 23." | ( Retinal changes associated with tamoxifen treatment for breast cancer. Hampton, J; Li, H; Locher, D; Pardo, G; Prager, T; Schiffman, J; Shields, J; Tang, R, 1997) | 0.84 |
" The animals in group A were administered heparin (Liquemine) intraperitoneally at the dosage of 1000 IU/kg/day." | ( Effect of medication on biomechanical properties of rabbit bones: heparin induced osteoporosis. Akkas, N; Delilbasi, E; Gunel, U; Turan, B; Yeni, YN, 1997) | 0.3 |
" Using our dosage regimen, 'chemical oophorectomy' with leuprolide was not as effective as surgical oophorectomy in the prevention of chemical carcinogenesis by DMBA but was comparable to the results obtained with tamoxifen." | ( Prevention of DMBA-induced rat mammary carcinomas comparing leuprolide, oophorectomy, and tamoxifen. Brackett, DJ; Hanas, JS; Hollingsworth, AB; Lerner, MR; Lightfoot, SA; McCay, PB; Wilkerson, KB, 1998) | 0.71 |
" Estrogenic effects of TAM were not detected with either dosage on the endometrium." | ( Side effects of tamoxifen in oophorectomized rats. Akbaşak, B; Aksoy, T; Biotec, FT; Biotech, MG; Birincioglu, M; Burak, F; Erdem, F; Kafkasli, A; Müezzinoglu, B, 1998) | 0.65 |
"The data suggests that TAM may not act as an estrogen receptor agonist with the given dosage on the endometrium in OX rats." | ( Side effects of tamoxifen in oophorectomized rats. Akbaşak, B; Aksoy, T; Biotec, FT; Biotech, MG; Birincioglu, M; Burak, F; Erdem, F; Kafkasli, A; Müezzinoglu, B, 1998) | 0.65 |
" No correlation was found between the duration of TAM therapy, the TAM dosage level or the ER or PR content in the adenomyotic or endometrial tissues." | ( Estrogen and progesterone receptors of adenomyosis in postmenopausal breast cancer patients treated with tamoxifen. Altaras, MM; Bernheim, J; Beyth, Y; Cohen, I; Cordoba, M; Shapira, J; Tepper, R, 1998) | 0.51 |
" Anastrozole is administered in a convenient, once-daily oral dosing regimen and does not require steroid replacement therapy." | ( Anastrozole: a new addition to the armamentarium against advanced breast cancer. Buzdar, AU, 1998) | 0.3 |
" The patients were randomly divided into two groups of 44: one group received tamoxifen at a dose of 10 mg by mouth from day 5 to day 24 of the menstrual cycle, whilst a placebo was administered to the other group using the same dosage scheme." | ( [Clinical efficacy of tamoxifen in the treatment of premenstrual mastodynia]. Cellura, A; Geranio, R; Grio, R; Piacentino, R; Porpiglia, M, 1998) | 0.84 |
" The frequent adverse reactions observed in all dosing groups included hot flashes, anorexia, nausea and vomiting, sweating, and abnormal values in liver function tests." | ( [Early phase II study of TAT-59 in patients with advanced or recurrent breast cancer--a multicenter dose finding study]. Abe, O; Aoyama, H; Tominaga, T, 1998) | 0.3 |
" The results support the previously proposed concept of a relationship between the amphiphilic cationic character of a compound and its ability to cause intralysosomal storage of polar lipids after a high dosage treatment of these drugs in animals." | ( Lipidosis induced in rat uteri by high doses of tamoxifen. Ioannidis, N, 1998) | 0.56 |
" The dosage of tamoxifen administered was 200 mg/day to males and 160 mg/day to females given in a twice daily schedule." | ( Treatment of recurrent malignant gliomas with chronic oral high-dose tamoxifen. Apuzzo, ML; Couldwell, WT; DeGiorgio, CM; Hinton, DR; Law, RE; Masri, L; Surnock, AA; Weiner, LP; Weiss, MH, 1996) | 0.88 |
" Tamoxifen dosing was adjusted based on serum levels." | ( Tamoxifen in liver disease: potential exacerbation of hepatic dysfunction. Cisneros, A; Floren, LC; Hebert, MF; Jordan, VC; Somberg, KA; Venook, AP, 1998) | 2.65 |
"Prediction of the drug level in the volume of distribution was made using a numerical model taking into account the following facts: the kinetics of drug release out of the dosage form along the gastrointestinal tract, the kinetics of absorption in the blood compartment and the kinetics of elimination." | ( Assessment of blood level with controlled-release dosage forms: effect of the rate constant of elimination of the drug. Aïnaoui, A; Vergnaud, JM, ) | 0.13 |
" This fact permits the use of high Drol Z dosage in order to achieve a relevant modulating effect in vivo and to use this drug in combination with a further modulator so as to reach maximum efficacy with tolerable side effects." | ( In vitro efficacy of known P-glycoprotein modulators compared to droloxifene E and Z: studies on a human T-cell leukemia cell line and their resistant variants. Gieseler, F; Gullis, E; Hasmann, M; Löser, R; Nüssler, V; Pelka-Fleisc, R; Stötzer, O; Wilmanns, W; Zwierzina, H, 1998) | 0.3 |
" Tamoxifen was administered orally in very high dosage to one child as monotherapy and to two children in combination with oral etoposide and dexamethasone." | ( Clinical and radiographic response in three children with recurrent malignant cerebral tumors with high-dose tamoxifen. Ben Arush, MW; Constantini, S; el Hasid, R; Goldsher, D; Postovsky, S, ) | 1.25 |
" Tamoxifen citrate was administered orally at a fixed dosage of 80 mg/m2 as a single or a twice-daily dosage." | ( Salvage chemotherapy with tamoxifen for recurrent anaplastic astrocytomas. Chamberlain, MC; Kormanik, PA, 1999) | 1.51 |
" Following dosing with N-desmethyltamoxifen, the major product co-eluted with one of the main peaks seen following treatment of rats with tamoxifen." | ( Further characterization of the DNA adducts formed in rat liver after the administration of tamoxifen, N-desmethyltamoxifen or N, N-didesmethyltamoxifen. Brown, K; Heydon, RT; Jukes, R; Martin, EA; White, IN, 1999) | 0.8 |
" Tamoxifen dose-response effects were more pronounced among women with both previous ERT exposure and higher body mass index than among women in other risk groups." | ( Tamoxifen therapy for breast cancer and endometrial cancer risk. Bernstein, L; Cerhan, JR; Deapen, D; Ford, L; Liff, J; McGann-Maloney, E; Perlman, JA; Schwartz, SM, 1999) | 2.66 |
" Hence, using a range of dosing protocols, sub-cutaneous administration of genistein for periods of up to 1 week did not alter intestinal epithelial homeostasis." | ( In vivo administration of genistein has no effect on small intestinal epithelial proliferation and apoptosis, but a modest effect on clonogen survival. Booth, C; Hargreaves, DF; O'Shea, JA; Potten, CS, 1999) | 0.3 |
" Interestingly, a dose-response study showed that Cre-ER(T2) was approximately 10-fold more sensitive to OHT induction than Cre-ER(T)." | ( Temporally-controlled site-specific mutagenesis in the basal layer of the epidermis: comparison of the recombinase activity of the tamoxifen-inducible Cre-ER(T) and Cre-ER(T2) recombinases. Bornert, JM; Brocard, J; Chambon, P; Indra, AK; Metzger, D; Warot, X; Xiao, JH, 1999) | 0.51 |
" We attempted to improve its efficacy and decrease its toxicity by using decrescendo dosing of interleukin-2 (IL-2), posttreatment granulocyte colony-stimulating factor (G-CSF), and low-dose tamoxifen." | ( Advantages of concurrent biochemotherapy modified by decrescendo interleukin-2, granulocyte colony-stimulating factor, and tamoxifen for patients with metastatic melanoma. Boasberg, PD; Cannon, M; Edwards, S; Essner, R; Fawzy, NW; Foshag, LJ; Fournier, P; Gammon, G; Guo, M; Johnson, TD; Kristedja, TS; Martin, MA; Morton, DL; O'Day, SJ; Stern, S; Weisberg, M, 1999) | 0.7 |
" Decrescendo IL-2 dosing and administration of G-CSF seemed to reduce toxicity, length of hospital stay, and readmission rates." | ( Advantages of concurrent biochemotherapy modified by decrescendo interleukin-2, granulocyte colony-stimulating factor, and tamoxifen for patients with metastatic melanoma. Boasberg, PD; Cannon, M; Edwards, S; Essner, R; Fawzy, NW; Foshag, LJ; Fournier, P; Gammon, G; Guo, M; Johnson, TD; Kristedja, TS; Martin, MA; Morton, DL; O'Day, SJ; Stern, S; Weisberg, M, 1999) | 0.51 |
" Therapeutic treatment with either idoxifene or estrogen (starting on day 10 of disease) of male and female Lewis rats also was effective in reducing paw inflammation in these animals, although the effect was much less than that observed with the prophylactic dosing protocol." | ( Idoxifene, a novel selective estrogen receptor modulator, is effective in a rat model of adjuvant-induced arthritis. Badger, AM; Blake, SM; Dodds, RA; Gowen, M; Griswold, DE; Hoffman, SJ; Rieman, DJ; Stroup, GB; Swift, BA, 1999) | 0.3 |
" Bicalutamide is also a nonsteroidal anti-androgen that offers the advantages of reduced dosage amounts and reduction in side effects." | ( Anti-androgens and other hormonal therapies for prostate cancer. Richie, JP, 1999) | 0.3 |
" Dose-response experiments indicated that the lowest stimulatory concentration of 17 beta-estradiol, DHT, and norgestrel is 10(-11) M, 10(-10) M, and 10(-10) M, respectively." | ( The normal epithelial cell-specific 1 (NES1) gene is up-regulated by steroid hormones in the breast carcinoma cell line BT-474. Diamandis, EP; Grass, L; Luo, LY, ) | 0.13 |
" Efficiencies and potencies of several isomers were calculated by fitting experimental data with a logistic dose-response function." | ( Agonistic and synergistic activity of tamoxifen in a yeast model system. Graumann, K; Jungbauer, A, 2000) | 0.58 |
" Dosage with tamoxifen must be tailored to individual patient requirement and symptom control balanced against troublesome side-effects." | ( Management of breast pain. Faiz, O; Fentiman, IS, 2000) | 0.68 |
" Using these standard markers, we analyzed the hepatic DNA adducts of female DBA/2 mice treated with tamoxifen at a dosage of 120 mg/kg/day for 7 days by (32)P-post-labeling coupled with an HPLC/radioactive detector." | ( Identification of hepatic tamoxifen-DNA adducts in mice: alpha-(N(2)-deoxyguanosinyl)tamoxifen and alpha-(N(2)-deoxyguanosinyl)tamoxifen N-oxide. Kanno, Y; Komaki, K; Lin, CX; Momen, MA; Monden, Y; Ravindernath, A; Shibutani, S; Suwa, M; Suzuki, M; Ueyama, Y; Umemoto, A, 2000) | 0.82 |
" The dose-response effects of phenol red were compared directly to those of E2." | ( Estrogen mitogenic action. III. is phenol red a "red herring"? Moreno-Cuevas, JE; Sirbasku, DA, ) | 0.13 |
" 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 |
"The combination of GM-CSF with biochemotherapy is feasible and there appears to be a dose-response relationship with GM-CSF in terms of host immunological response, and possibly clinical efficacy." | ( GM-CSF with biochemotherapy (cisplatin, DTIC, tamoxifen, IL-2 and interferon-alpha): a phase I trial in melanoma. A'Hern, RP; Ayliffe, MJ; Eisen, T; Gore, ME; Hill, ME; Johnston, SR; Moore, J; Riches, PG; Thomas, JM; Vaughan, MM, 2000) | 0.57 |
") for 6 weeks to female lambda/lacI transgenic rats caused a 4-fold increase in mutation frequency (MF) at the lacI gene locus in the livers of dosed animals compared with controls." | ( Tamoxifen mutagenesis and carcinogenesis in livers of lambda/lacI transgenic rats: selective influence of phenobarbital promotion. Davies, R; Fenwick, S; Smith, LL; Styles, JA; Walker, J; White, IN, 2001) | 1.75 |
" I33' may have accounted for Vg increases observed in trout fed I3C as it is present in liver after oral dosing at concentrations (70 microM) expected to maximally induce Vg." | ( 3,3'-diindolylmethane, a major condensation product of indole-3-carbinol, is a potent estrogen in the rainbow trout. Carlson, DB; Katchamart, S; Shilling, AD; Williams, DE, 2001) | 0.31 |
"Retrospective dose-response data suggest that a boost of about 15 Gy to the tumor bed following whole-breast radiotherapy reduces the risk of local recurrence (IBTR) by as much as 2-fold." | ( Which patients don't need a tumor-bed boost after whole-breast radiotherapy? Kurtz, JM, 2001) | 0.31 |
" Toxicity management consisted of dosage reduction or treatment delay; treatment often was discontinued." | ( Pegylated liposomal doxorubicin: tolerability and toxicity. Goram, AL; Richmond, PL, 2001) | 0.31 |
" In rats dosed intraperitoneally, the relative order of binding was alpha-hydroxytamoxifen > tamoxifen > 3-hydroxytamoxifen approximately 4-hydroxytamoxifen." | ( DNA adduct formation and mutant induction in Sprague-Dawley rats treated with tamoxifen and its derivatives. Beland, FA; Gamboa da Costa, G; Heflich, RH; Marques, MM; McDaniel-Hamilton, LP, 2001) | 0.77 |
" The reason is that the appropriate dosage is not identical to that of Western countries." | ( [Developments of hormonal agents for breast cancer]. Tominaga, T, 2001) | 0.31 |
" Tamoxifen induced increased cell cycle activity in the livers of rats following gavage dosing at all sampling times (1-12 weeks), whereas toremifene had no effect on the incidence of cycling in hepatic cells, demonstrating that the hepatic cell proliferation is not a general response to anti-oestrogen treatment." | ( Delayed effects of tamoxifen in hepatocarcinogenesis-resistant Fischer 344 rats as compared with susceptible strains. Carthew, P; Davies, R; Higginson, F; Martin, E; Stanley, LA; Styles, JA, 2001) | 1.55 |
" Uterine adenomyosis was found in all (14 of 14) mice dosed with tamoxifen and most mice (12 of 14) treated with toremifene, but in none of the vehicle-dosed controls, in only one animal treated with raloxifene at 42 and 90 days after dosing and in none of the mice treated with estradiol at 42 days." | ( Adenomyosis--a result of disordered stromal differentiation. Butterworth, M; Greaves, P; Green, A; Parrott, E; White, IN, 2001) | 0.55 |
" We have examined the dose-response relationship of tamoxifen-induced DNA adducts in the liver and the subsequent increase in the development of liver cancer, with and without phenobarbital promotion." | ( Cumulative exposure to tamoxifen: DNA adducts and liver cancer in the rat. Carthew, P; Edwards, RE; Heydon, RT; Lee, PN; Martin, EA; Nolan, BM, 2001) | 0.87 |
" Even if the single and total dosage of antiestrogens given to the patient is sufficient to cause tamoxifen retinopathy, this diagnosis can be excluded because, in tamoxifen retinopathy unlike in the case presented here, the deposits are not distributed in all retinal layers." | ( Tamoxifen side effects, age-related macular degeneration (AMD) or cancer associated retinopathy (CAR)? Apfelstedt-Sylla, E; Kriegbaum, C; Sadowski, B, ) | 1.79 |
" It has not yet been demonstrated conclusively that HER2 positivity increases resistance to adjuvant cyclophosphamide, methotrexate, 5-FU (CMF), but there are indications that HER2-positive patients benefit more from adequately dosed anthracyclines than from CMF." | ( The predictive value of HER2 in breast cancer. Di Leo, A; Larsimont, D; Lohrisch, C; Piccart, M, 2001) | 0.31 |
" A study evaluating time-dependent alterations in the PK profile of TAM showed no change in apparent oral clearance (Cl(app)) during two weeks of chronic dosing with TAM." | ( Molecular and pharmacokinetic evaluation of rat hepatic and gastrointestinal cytochrome p450 induction by tamoxifen. Cotreau, MM; Greenblatt, DJ; Harmatz, JS; von Moltke, LL, 2001) | 0.52 |
" Estradiol induced stimulation of proliferation was inhibited by a dosage >1 microg/ml of extract concentration, gene expression was suppressed by doses of 100-1000 microg/ml of Cimicifuga racemosa extracts." | ( Antiestrogenic activities of Cimicifuga racemosa extracts. Bodinet, C; Kolba, S; Vollmer, G; Wulf, M; Zierau, O, 2002) | 0.31 |
"The cytotoxicity of the selected systemic and intravitreally dosed drugs tamoxifen, toremifene, chloroquine, 5-fluorouracil, gentamicin and ganciclovir was studied in retinal pigment epithelium (RPE) in vitro." | ( Evaluation of the cytotoxicity of selected systemic and intravitreally dosed drugs in the cultures of human retinal pigment epithelial cell line and of pig primary retinal pigment epithelial cells. Diehl, H; Engelke, M; Huhtala, A; Mäenpää, H; Mannerström, M; Mäntylä, E; Mäntylä, M; Marselos, M; Pappas, P; Salminen, L; Tähti, H; Toimela, T; Uusitalo, H; Zorn-Kruppa, M, 2002) | 0.55 |
" Immature Sprague-Dawley female rats (21 days of age) were dosed daily for 20 days by oral gavage (DES, tamoxifen, and flutamide) or sc injection (testosterone)." | ( Evaluation of the 20-day pubertal female assay in Sprague-Dawley rats treated with DES, tamoxifen, testosterone, and flutamide. Han, SY; Kang, IH; Kim, HS; Kim, IY; Kim, TS; Moon, HJ; Park, KL; Seok, JH; Shin, JH, 2002) | 0.75 |
" Cumulative dose-response vasorelaxation to idoxifene (0." | ( Idoxifene causes endothelium-dependent, nitric oxide-mediated vasorelaxation in male rats. Christopher, TA; Gao, E; Gao, F; Lopez, BL; Ma, XL; Ohlstein, EH; Stillwagon, JC; Yue, TL, 2002) | 0.31 |
" Preclinical research has demonstrated that the estrogen dose-response curve for breast cancer cells can be shifted by modification of the estrogen environment." | ( Estrogen as therapy for breast cancer. Ingle, JN, 2002) | 0.31 |
" Tamoxifen forms liver DNA adducts in both short- and long-term dosing of rodents, and DNA adducts have also been reported in tissues of women undergoing tamoxifen therapy." | ( DNA adducts formed from 4-hydroxytamoxifen are more mutagenic than those formed by alpha-acetoxytamoxifen in a shuttle vector target gene replicated in human Ad293 cells. Brown, K; Farmer, PB; Gaskell, M; Martin, EA; McLuckie, KI; Roberts, GC; Routledge, MN, 2002) | 1.51 |
" Ovary weight, uterus weight, peak plasma GH concentration, and hepatic CYP2A1 content were decreased 37 days after treatment with tamoxifen at a dosage of 20 mg/kg, but expression of other P450 enzymes was not affected." | ( Persistent suppression of hepatic CYP2A1 expression and serum triiodothyronine levels by tamoxifen in intact female rats: dose-response analysis and comparison with 4-hydroxytamoxifen, fulvestrant (ICI 182,780), and 17beta-estradiol-3-benzoate. Bandiera, SM; Ickenstein, LM, 2002) | 0.74 |
" Dosing with 25 microM genistein at 0 and 12 hours after inoculation of BHV-1 was optimal for decreasing BHV-1 replication." | ( Effect of genistein on replication of bovine herpesvirus type 1. Akula, SM; Chase, CC; Hurley, DJ; Wang, C; Wixon, RL, 2002) | 0.31 |
" The potent estrogen suppressive action and simple dosage regimen of anastrozole suggest it may be advantageous compared to other aromatase inhibitors such as testolactone or anti-estrogens." | ( Effective aromatase inhibition by anastrozole in a patient with gonadotropin-independent precocious puberty in McCune-Albright syndrome. Albers, N; Freiberg, C; Roth, C; Zappel, H, 2002) | 0.31 |
" A total of 329 patients from 10 centers in 9 countries in the Asia-Pacific region enrolled in a double-blind randomized controlled trial of TMX 120 mg/d (TMX120) against P as a control arm with an intermediate dosage of TMX 60 mg/d (TMX60) to assess possible dose response." | ( High-dose tamoxifen in the treatment of inoperable hepatocellular carcinoma: A multicenter randomized controlled trial. Chow, PK; Johnson, PJ; Machin, D; Soo, KC; Tai, BC; Tan, CK; Win, KM, 2002) | 0.72 |
"Oral dosing of CD-1 mice on days 2-5 after birth with tamoxifen but not raloxifene disrupts the development of the myometrium, resulting in adult uterine adenomyosis." | ( Comparison of the effect of oestradiol, tamoxifen and raloxifene on nerve growth factor-alpha expression in specific neonatal mouse uterine cell types using laser capture microdissection. Edwards, RE; Greaves, P; Green, AR; White, IN, 2003) | 0.83 |
" Dose-response experiments with six selected compounds were carried out using two different human breast cancer cell lines, MCF-7 and the tamoxifen resistant cell line MCF-/TAM(R)-1." | ( N-Alkoxypyrazoles as biomimetics for the alkoxyphenyl group in tamoxifen. Barfoed, M; Begtrup, M; Gissel, B; Huusfeldt, PO; Jakobsen, P; Lundin Brockdorff, B; Lykkesfeldt, AE; Vedsø, P; Wenckens, M, 2003) | 0.76 |
" After oral dosing in mice, tam and the potent metabolite 4-hydroxytamoxifen (4-hydroxytam), were detectable in liver and lung tissue, but not in serum." | ( Tamoxifen administration and metabolism in nude mice and nude rats. Gjerde, J; Kisanga, ER; Lien, EA; Mellgren, G; Schjøtt, J, 2003) | 2 |
" Several blood biomarkers showed dose-response relationships with tamoxifen, including decreased insulin-like growth factor-I, increased sex hormone-binding globulin, and decreased low-density lipoprotein-cholesterol, ultrasensitive C-reactive protein, fibrinogen, and antithrombin-III levels." | ( A randomized trial of low-dose tamoxifen on breast cancer proliferation and blood estrogenic biomarkers. Cazzaniga, M; Decensi, A; Goldhirsch, A; Johansson, H; Kisanga, ER; Lien, EA; Luini, A; Mora, S; Pelosi, G; Pigatto, F; Robertson, C; Sandri, MT; Torrisi, R; Veronesi, P; Veronesi, U; Viale, G, 2003) | 0.84 |
"3-fold after dosing TAT-59 and 500 microM fosphenytoin, respectively." | ( Absorption rate limit considerations for oral phosphate prodrugs. Fleisher, D; Flynn, G; Forsberg, M; Heimbach, T; Leppänen, J; Li, LY; Matsunaga, Y; Oh, DM; Savolainen, J, 2003) | 0.32 |
" The prolonged-release properties of this formulation suggested that it may be well suited for the once-monthly dosing schedule intended for clinical use." | ( Pharmacokinetics of a single dose of fulvestrant prolonged-release intramuscular injection in postmenopausal women awaiting surgery for primary breast cancer. Harrison, MP; Holcombe, C; Kohlhardt, SR; Odling-Smee, W; Robertson, JF, 2003) | 0.32 |
"291 for the linear dose-response trend)." | ( Effect of tamoxifen at low doses on ultrasensitive C-reactive protein in healthy women. Bonanni, B; Decensi, A; Gandini, S; Guerrieri-Gonzaga, A; Johansson, H; Lien, EA; Mariette, F; Sandri, MT, 2003) | 0.72 |
" Studies reviewed evaluate the role of aromatase inhibitors, incorporation of taxanes into chemotherapy regimens, novel dosage schedules, and supportive care with epoetin alfa." | ( Recent advances in adjuvant therapy for breast cancer. Palmieri, FM; Perez, EA, 2003) | 0.32 |
" We investigated concentrations of tamoxifen, 4-hydroxytamoxifen, N-desmethyltamoxifen, and N-didesmethyltamoxifen in serum, normal breast, and breast cancer tissues during conventional dosage and two low-dose regimens." | ( Tamoxifen and metabolite concentrations in serum and breast cancer tissue during three dose regimens in a randomized preoperative trial. Decensi, A; Gjerde, J; Guerrieri-Gonzaga, A; Kisanga, ER; Lien, EA; Pelosi, G; Pesci-Feltri, A; Pigatto, F; Robertson, C; Serrano, D, 2004) | 2.04 |
"33 mM in the ST cross only and without a clear dose-response effect." | ( Genotoxicity of tamoxifen citrate and 4-nitroquinoline-1-oxide in the wing spot test of Drosophila melanogaster. Castañeda-Partida, L; Contreras-Sousa, M; Dueñas-García, I; Durán-Díaz, A; Graf, U; Heres-Pulido, ME; Sánchez-García, A, 2004) | 0.67 |
" Full thickness human skin was dosed with 500 microl saturated solution of tamoxifen in borage oil (25% GLA) and the simultaneous permeation of the two actives determined." | ( Simultaneous permeation of tamoxifen and gamma linolenic acid across excised human skin. Further evidence of the permeation of solvated complexes. Harwood, JL; Heard, CM; Karia, C; Morris, AP, 2004) | 0.85 |
"In the present experiment we evaluated the dose-response effects of estrogen (estradiol benzoate; EB) and tamoxifen (TMX) in modulating the acute behavioral and chronic effects of methamphetamine (MA) upon the nigrostriatal dopaminergic (NSDA) system in ovariectomized (OVX) mice." | ( Dose-response effects of estrogen and tamoxifen upon methamphetamine-induced behavioral responses and neurotoxicity of the nigrostriatal dopaminergic system in female mice. Dluzen, DE; Mickley, KR, 2004) | 0.81 |
" This was prevented by ormeloxifene and the effect, though apparently more in females supplemented with higher dose of ormeloxifene, was not always significantly different and clear dose-response was not evident until BMD data was evaluated on T-/Z-score basis." | ( In vitro anti-resorptive activity and prevention of ovariectomy-induced osteoporosis in female Sprague-Dawley rats by ormeloxifene, a selective estrogen receptor modulator. Arshad, M; Ghosh, R; Sawlani, V; Sengupta, S; Sharma, S; Singh, MM, 2004) | 0.32 |
" DES alone affected mammary growth (an inverted-U-shaped dose-response curve) both in male and female mice." | ( Mouse bioassay to assess oestrogenic and anti-oestrogenic compounds: hydroxytamoxifen, diethylstilbestrol and genistein. Köhlerová, E; Skarda, J, 2004) | 0.55 |
"Rats were injected subcutaneously with peanut oil (vehicle) or tamoxifen at a dosage of 20 or 200 mg/kg for 2 consecutive days." | ( Tamoxifen alters hepatic cytochrome P450 enzyme expression and circulating growth hormone levels in intact male rats. Bandiera, SM; Holsmer, SL; Ickenstein, LM, 2004) | 2.01 |
" The dosage of tamoxifen was extrapolated from the human dosage." | ( Plasma leptin concentration in tamoxifen-treated ovariectomized rats. Hakamata, Y; Hozumi, Y; Nagai, H, 2005) | 0.97 |
" Also, TAS-108 strongly inhibited tumor growth in dimethylbenzanthracene-induced mammary carcinomain the rat, the endogenous E2 model, at a dosage of 1 to 3 mg/kg/day." | ( TAS-108, a novel oral steroidal antiestrogenic agent, is a pure antagonist on estrogen receptor alpha and a partial agonist on estrogen receptor beta with low uterotrophic effect. Aoyagi, Y; Asao, T; Buzdar, AU; Hashimoto, A; Sato, K; Shibata, J; Terada, T; Wierzba, K; Yamamoto, Y; Yano, S; Yonekura, K, 2005) | 0.33 |
"Consistent with previous reports, the dose-response of the E2 effect on the PR expression indicated an ED(50) value of approximately 60 pM and the maximum induction of PR mRNA was nearly ten-fold." | ( Endoxifen (4-hydroxy-N-desmethyl-tamoxifen) has anti-estrogenic effects in breast cancer cells with potency similar to 4-hydroxy-tamoxifen. Desta, Z; Flockhart, DA; Lim, YC; Skaar, TC, 2005) | 0.61 |
" However, critical requirements of this system are that the nuclear localization of the transgene product be tightly regulated, that the dosage of the inducing agent remains consistent among experimental animals and that the transgene cassette cannot express in the absence of the inducing agent." | ( Cross-contamination with tamoxifen induces transgene expression in non-exposed inducible transgenic mice. Begley, CG; Brake, RL; Simmons, PJ, 2004) | 0.63 |
" The neonatal mouse, exquisitely sensitive to xenobiotic estrogens, has been used to investigate the effects of short-term oral dosing with tamoxifen (1 mg/kg on days 2-5 after birth) on long-term changes in uterine pathology and gene expression." | ( Neonatal tamoxifen treatment of mice leads to adenomyosis but not uterine cancer. Al-Azzawi, F; Edwards, RE; Gant, TW; Gray, D; Greaves, P; Green, AR; Parrott, EL; Smith, AG; Styles, JA; White, IN, 2005) | 0.95 |
" drug dosage and selection." | ( Role of cytochrome P450 activity in the fate of anticancer agents and in drug resistance: focus on tamoxifen, paclitaxel and imatinib metabolism. Rochat, B, 2005) | 0.55 |
" The significance of treatment dosage and duration was obvious when 5-DFUR and Tam cotreatment was observed to be antagonistic in 3-day cultures of a second MCF-7 subline and T47D cells." | ( Combination of 5-deoxy-5-fluorouridine and tamoxifen show cell-type specific antagonistic and cooperative effects on cytotoxicity in human mammary carcinoma cells. Bollig, A; Du, QQ; Fan, ST; Liao, J; Sarkar, FH; Yu, B, 2005) | 0.59 |
" Treatment with tamoxifen, in a dosage of 20 mg twice a day for more than 1(1/2) years, completely resolved the neck mass (substantiated by follow-up magnetic resonance imaging) and relieved the signs and symptoms of compression of the neck." | ( A case of Riedel's thyroiditis treated with tamoxifen: another successful outcome. Jung, YJ; Muehlenbein, SJ; Rhodes, R; Rich, FA; Schaub, CR, ) | 0.74 |
" A dose-response significant inhibition of the capillary-like formation was detected when increasing concentrations of tamoxifen, ilomastat, or echistatin were added for 1 week to the culture medium of the ERCT." | ( In vitro evaluation of the angiostatic potential of drugs using an endothelialized tissue-engineered connective tissue. Auger, FA; Berthod, F; Germain, L; Tremblay, PL, 2005) | 0.54 |
" Dose-response curves of different ligands could be obtained for each receptor interaction." | ( Diffusion-time distribution analysis reveals characteristic ligand-dependent interaction patterns of nuclear receptors in living cells. Izewska, P; Jankevics, H; Leufgen, K; Pick, H; Prummer, M; Vogel, H, 2005) | 0.33 |
" 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) | 0.64 |
" Two different clones of the breast cancer cell line MCF-7 were exposed to highly homogeneous 50Hz electromagnetic fields and IC(50) values were calculated from dose-response curves of tamoxifen at various field intensities." | ( Induction of tamoxifen resistance in breast cancer cells by ELF electromagnetic fields. Girgert, R; Gründker, C; Hanf, V; Körner, W; Schimming, H, 2005) | 0.89 |
" Eighty-six percent of patients achieved acceptable dosing of TAM." | ( Phase 2 trial of radiation plus high-dose tamoxifen for glioblastoma multiforme: RTOG protocol BR-0021. Brachman, DG; Choucair, AK; Demas, WF; Mehta, MP; Robins, HI; Schultz, CJ; Seiferheld, WF; Won, M, 2006) | 0.6 |
" Dose-response analyses revealed a structure-activity relationship where the larger the side-chain the higher the inhibitory potency." | ( Functional inhibition of intestinal and uterine muscles by non-permeant triphenylethylene derivatives. Díaz, M; García Marrero, B; Gómez, T; Marrero-Alonso, J, 2006) | 0.33 |
" If the results are further confirmed in the clinical trials, the tamoxifen dosage should be adjusted when tamoxifen is administered with quercetin or quercetin-containing dietary supplements in order to avoid potential drug interactions." | ( Enhanced bioavailability of tamoxifen after oral administration of tamoxifen with quercetin in rats. Choi, JS; Li, X; Shin, SC, 2006) | 0.86 |
" The compounds were dosed (s." | ( Histopathology and histomorphometry of the urogenital tract in 15-month old male and female rats treated neonatally with SERMs and estrogens. Karlsson, S, 2006) | 0.33 |
" Thirty-six women received TMX at a 20-mg dosage and 30 women received no ovulation-induction drugs." | ( Tamoxifen citrate for women with unexplained infertility. Shokeir, TA, 2006) | 1.78 |
": Forty-four eyes of 22 women receiving tamoxifen at a dosage of 20 mg/day for at least 6 months for the adjuvant treatment of breast cancer and 30 eyes of 15 healthy age-matched women were examined for corneal drug deposition by slitlamp after pupil dilation." | ( Clinical and in vivo confocal microscopy findings in patients receiving tamoxifen citrate. Kanpolat, A; Muftuoglu, O; Uçakhan, OO, 2006) | 0.83 |
" Liquid formulations (PG:PEG400:H2O) provided higher oral bioavailability than solid formulations dissolved and dosed as aqueous oral solutions." | ( Pharmacokinetics of tamoxifen after intravenous and oral dosing of tamoxifen-hydroxybutenyl-beta-cyclodextrin formulations. Buchanan, CM; Buchanan, NL; Edgar, KJ; Little, JL; Malcolm, MO; Ruble, KM; Wacher, VJ; Wempe, MF, 2007) | 0.66 |
" Low dosage endocrine agent-induced anthracycline sensitization may be independent of mitochondrial toxicity." | ( Medroxyprogesterone and tamoxifen augment anti-proliferative efficacy and reduce mitochondria-toxicity of epirubicin in FM3A tumor cells in vitro. Altinoz, MA; Bilir, A; Gedikoglu, G; Muslumanoglu, M; Oktem, G; Ozcan, E, 2007) | 0.65 |
"Adult, ovariectomized, female Macaca fascicularis, n = 3 per group, orally dosed for 12 weeks with vehicle; selective estrogen receptor modulator 393 (2, 4, or 8 mg/kg/day); selective estrogen receptor modulator 379 (4 mg/kg per day); raloxifene (3 mg/kg per day); tamoxifen (1 mg/kg per day); or ethinyl estradiol (3 microg/kg per day)." | ( Effects of two novel selective estrogen receptor modulators, raloxifene, tamoxifen, and ethinyl estradiol on the uterus, vagina and breast in ovariectomized cynomolgus monkeys (Macaca fascicularis). Brown, KH; Cline, JM; Hutchison, J; Lees, CJ; Lundeen, S; Register, TC; Sikoski, P, 2007) | 0.75 |
" In the present study, 84 breast cancer patients were randomized to receive a daily supplement of 100 mg coenzyme Q10 (CoQ10), 10 mg riboflavin and 50 mg niacin (CoRN) one dosage per day along with 10 mg tamoxifen (TAM) twice a day." | ( Effect of coenzyme Q10, riboflavin and niacin on serum CEA and CA 15-3 levels in breast cancer patients undergoing tamoxifen therapy. Gangadaran, SG; Premkumar, VG; Sachdanandam, P; Vijayasarathy, K; Yuvaraj, S, 2007) | 0.74 |
" Dose-response studies in the same rat model demonstrated that more than 90% inhibition of STS activity in tumors was necessary to induce tumor shrinkage." | ( A novel steroidal selective steroid sulfatase inhibitor KW-2581 inhibits sulfated-estrogen dependent growth of breast cancer cells in vitro and in animal models. Akinaga, S; Anazawa, H; Ishida, H; Kuwabara, T; Li, PK; Murakata, C; Nakata, T; Sato, N; Shiotsu, Y; Suzuki, M; Takebayashi, M; Tanaka, H; Terasaki, Y, 2007) | 0.34 |
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process." | ( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential. Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A, ) | 0.13 |
" In the present study, 84 breast cancer patients were randomized to receive a daily supplement of CoQ(10) 100 mg, riboflavin 10 mg and niacin 50 mg, one dosage per day along with tamoxifen 10 mg twice a day." | ( Serum cytokine levels of interleukin-1beta, -6, -8, tumour necrosis factor-alpha and vascular endothelial growth factor in breast cancer patients treated with tamoxifen and supplemented with co-enzyme Q(10), riboflavin and niacin. Gangadaran, SG; Premkumar, VG; Sachdanandam, P; Vijayasarathy, K; Yuvaraj, S, 2007) | 0.73 |
"The effects of subcutaneous dosing of neonatal CD-1 mice with tamoxifen on days 1-5 after birth at doses of 0, 5, 10, 25 or 50 microg/pup or with 4-hydroxyoestradiol at 2 microg/pup have been investigated." | ( Absence of uterine tumours in CD-1 mice treated neonatally with subcutaneous tamoxifen or 4-hydroxyoestradiol. Edwards, R; Greaves, P; Razvi, N; Styles, J; White, IN, 2007) | 0.81 |
" Interestingly, licoflavone C exhibited a dose-dependent antagonistic activity at concentrations up to 10(-4) M, but stimulated beta-galactosidase expression at higher concentrations resulting in a U-shaped-like dose-response curve." | ( Estradiol-antagonistic activity of phenolic compounds from leguminous plants. Bertoli, A; Garritano, S; Noccioli, C; Pinto, B; Pistelli, L; Reali, D, 2008) | 0.35 |
" Overall, the NMPC algorithm is suitable for dosing chemotherapeutics with regular administration schedules and may be adapted for regularly administered chemotherapeutics other than tamoxifen." | ( Nonlinear model predictive control for dosing daily anticancer agents using a novel saturating-rate cell-cycle model. Eiseman, JL; Florian, JA; Parker, RS, 2008) | 0.54 |
" 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) | 0.35 |
" It has been also proposed that negative results might be explained if tamoxifen acts in HCC via an estrogen receptor-independent pathway, that requires higher doses than those usually administered, but an Asian RCT conducted to assess dose-response effect was completely negative." | ( Is human hepatocellular carcinoma a hormone-responsive tumor? Daniele, B; De Maio, E; Di Maio, M; Gallo, C; Morabito, A; Perrone, F; Piccirillo, MC; Pignata, S, 2008) | 0.58 |
" In the present study, 84 breast cancer patients were randomized to receive a daily supplement of CoQ(10) 100 mg, riboflavin 10 mg and niacin 50 mg (CoRN), one dosage per day along with tamoxifen (TAM) 10 mg twice a day." | ( Anti-angiogenic potential of CoenzymeQ10, riboflavin and niacin in breast cancer patients undergoing tamoxifen therapy. Premkumar, VG; Sachdanandam, P; Sathish, S; Shanthi, P; Yuvaraj, S, ) | 0.54 |
" This may represent a novel approach to preparing convenient dosage forms of poorly soluble drugs." | ( Stable nanocolloids of poorly soluble drugs with high drug content prepared using the combination of sonication and layer-by-layer technology. Agarwal, A; Lvov, Y; Sawant, R; Torchilin, V, 2008) | 0.35 |
"All four assays performed well in the ZFL cells and led to reproducible dose-response curves for all test compounds." | ( Comparison of four different colorimetric and fluorometric cytotoxicity assays in a zebrafish liver cell line. Bopp, SK; Lettieri, T, 2008) | 0.35 |
" The increased bioavailability of tamoxifen in the presence of morin should be taken into consideration for dosage regimens due to potential drug interaction." | ( Effects of morin on the bioavailability of tamoxifen and its main metabolite, 4-hydroxytamoxifen, in rats. Choi, JS; Piao, YJ; Shin, SC, ) | 0.67 |
" The cumulative dosage of epirubicin that carries a 5% risk of cardiotoxicity was lower than previously assumed and was dependent on risks of both cardiotoxicity and overall mortality." | ( New insight into epirubicin cardiac toxicity: competing risks analysis of 1097 breast cancer patients. Andersen, PK; Cortese, G; Nielsen, D; Nielsen, G; Ryberg, M; Skovsgaard, T, 2008) | 0.35 |
" Further studies on higher animals and dosage and timing are required." | ( The effect of calmodulin antagonists on experimental scoliosis: a pinealectomized chicken model. Acaroglu, E; Akel, I; Alanay, A; Bozkurt, G; Kocak, O; Marcucio, R, 2009) | 0.35 |
" To be included in the meta-analysis, RCTs had to compare gabapentin with placebo in the treatment of hot flashes in women with natural or tamoxifen-induced menopause, regardless of the sample size, dosage used, duration of treatment, or frequency of the episodes." | ( Gabapentin for the treatment of hot flashes in women with natural or tamoxifen-induced menopause: a systematic review and meta-analysis. Goulis, DG; Kouvelas, D; Toulis, KA; Tzellos, T, 2009) | 0.79 |
" Careful attention to controls, reduced tamoxifen dosing and/or use of raloxifene is advised with this model." | ( Avoidance of transient cardiomyopathy in cardiomyocyte-targeted tamoxifen-induced MerCreMer gene deletion models. Bedja, D; Gabrielson, KL; Kass, DA; Koitabashi, N; Pinto, YM; Takimoto, E; Zaiman, AL; Zhang, M, 2009) | 0.86 |
" Mice survival rate after single peroral introduction of indomethofene radioprotective doses was comparable with that resulting from referencing preparation estrofeme, which is estradiol oral dosage from (under the assumption that in contrast to indometafene estrofeme was introduced repeatedly every other day from 3 till 21 day after irradiation)." | ( [Therapeutic action of radioprotector indometofen]. Mikhaĭlov, PP; Shliakov, TG, ) | 0.13 |
" 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 |
" Optical microscopy/spectroscopy, time-dependent dose-response data, and estrogen competition studies indicate that augmented activity is due to increased rates of intracellular tamoxifen transport by nanoparticle endocytosis, rather than by passive diffusion of the free drug." | ( Tamoxifen-poly(ethylene glycol)-thiol gold nanoparticle conjugates: enhanced potency and selective delivery for breast cancer treatment. Dreaden, EC; El-Sayed, MA; Mwakwari, SC; Oyelere, AK; Sodji, QH, 2009) | 1.99 |
" Therefore, her tamoxifen dosage was increased to 20 mg twice/day." | ( Tamoxifen malabsorption after Roux-en-Y gastric bypass surgery: case series and review of the literature. Bestul, D; Decker, D; Kuwajerwala, N; Wills, SM; Zekman, R, 2010) | 2.15 |
" Many factors contribute to adherence behavior, such as complex dosing or administration requirements, cost, and a lack of understanding of the importance of adherence." | ( Nonadherence in patients with breast cancer receiving oral therapies. Moore, S, 2010) | 0.36 |
" In pre-menopausal breast cancer PM or IM patients, an increase in dosage of tamoxifen or a treatment with LH-RH analogues with aromatase inhibitors (AI) may be beneficial instead of the actual recommendations of a 5-year tamoxifen therapy." | ( [CYP2D6 polymorphisms and tamoxifen: therapeutic perspectives in the management of hormonodependent breast cancer patients]. Barrière, J; Ferrero, JM; Formento, JL; Milano, G, 2010) | 0.89 |
" If these results are confirmed in clinical trials, the tamoxifen dosage should be adjusted when tamoxifen is administered with silybinin or silybinin-containing dietary supplements." | ( Effects of silybinin on the pharmacokinetics of tamoxifen and its active metabolite, 4-hydroxytamoxifen in rats. Choi, JS; Choi, SJ; Kim, CS; Li, C; Park, CY, 2010) | 0.86 |
" It is important that fertility preservation strategies are addressed before chemotherapy, because chemotherapy may induce premature ovarian failure (depending on the woman's age, the drugs used, the dosage and duration of treatment)." | ( Reproduction after breast cancer. Iatrakis, G; Navrozoglou, I; Zervoudis, S, 2010) | 0.36 |
"Increased coactivator mRNA levels seem to be an early response to tamoxifen without dose-response relationship in the 1- to 20-mg range." | ( Effect of low-dose tamoxifen on steroid receptor coactivator 3/amplified in breast cancer 1 in normal and malignant human breast tissue. Bonanni, B; De Censi, A; DeCensi, A; Gandini, S; Gjerde, J; Guerrieri-Gonzaga, A; Haugan Moi, LL; Hauglid Flågeng, M; Lazzeroni, M; Lien, EA; Mellgren, G, 2010) | 0.93 |
" We provide an important quantitative and statistical framework for designing CreER(T)-based experiments and choosing tamoxifen dosing paradigms." | ( Tamoxifen dose response and conditional cell marking: is there control? Ellisor, D; Zervas, M, 2010) | 2.01 |
" Well designed studies are needed to demonstrate superiority of pharmoacogenetics to conventional dosing regimes." | ( Pharmacogenetics in palliative care. Kleine-Brueggeney, M; Musshoff, F; Stamer, UM; Stuber, F, 2010) | 0.36 |
"Adenomyosis, which became more serious as age increased, was successfully induced in dosed ICR mice." | ( Accumulation of nerve growth factor and its receptors in the uterus and dorsal root ganglia in a mouse model of adenomyosis. Bao, L; Li, Y; Xia, X; Zhang, SF; Zou, SE, 2011) | 0.37 |
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts." | ( FDA-approved drug labeling for the study of drug-induced liver injury. Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011) | 0.37 |
" In this study, we evaluated the effect of valproic acid (VPA) in ICR mice with adenomyosis, induced by neonatal dosing with tamoxifen." | ( Valproic acid alleviates generalized hyperalgesia in mice with induced adenomyosis. Guo, SW; Liu, X, 2011) | 0.58 |
" This test could contribute to the personalization and optimization of tamoxifen treatment, but it needs additional validation and simplification before being applicable in future dosing strategies." | ( Dextromethorphan as a phenotyping test to predict endoxifen exposure in patients on tamoxifen treatment. Beijnen, JH; de Graan, AJ; de Jongh, FE; de Vos, AI; de Vos, FY; Loos, WJ; Mathijssen, RH; Seynaeve, C; Teunissen, SF; van Alphen, RJ; van der Holt, B; van Schaik, RH; Verweij, J, 2011) | 0.83 |
"We examined the feasibility of using CYP2D6 genotyping to determine optimal tamoxifen dose and investigated whether the key active tamoxifen metabolite, endoxifen, could be increased by genotype-guided tamoxifen dosing in patients with intermediate CYP2D6 metabolism." | ( Genotype-guided tamoxifen dosing increases active metabolite exposure in women with reduced CYP2D6 metabolism: a multicenter study. Anderson, SM; Canale, ST; Carey, LA; Chiu, WK; Corso, SW; Dees, EC; Desta, Z; Evans, JP; Flockhart, DA; Friedman, KJ; Graham, ML; Ibrahim, JG; Irvin, WJ; McLeod, HL; Moore, SG; Ogburn, ET; Olajide, OA; Peppercorn, JM; Raab, RE; Walko, CM; Weck, KE, 2011) | 0.94 |
"This study demonstrates the feasibility of genotype-driven tamoxifen dosing and demonstrates that doubling the tamoxifen dose can increase endoxifen concentrations in IM and PM patients." | ( Genotype-guided tamoxifen dosing increases active metabolite exposure in women with reduced CYP2D6 metabolism: a multicenter study. Anderson, SM; Canale, ST; Carey, LA; Chiu, WK; Corso, SW; Dees, EC; Desta, Z; Evans, JP; Flockhart, DA; Friedman, KJ; Graham, ML; Ibrahim, JG; Irvin, WJ; McLeod, HL; Moore, SG; Ogburn, ET; Olajide, OA; Peppercorn, JM; Raab, RE; Walko, CM; Weck, KE, 2011) | 0.96 |
" The dosage in patients with endoxifen <40 nmol/l and/or CYP2D6 MPA scores of 0 was increased to 30 mg/day and their metabolite isomers were monitored for up to 90 days." | ( Increasing tamoxifen dose in breast cancer patients based on CYP2D6 genotypes and endoxifen levels: effect on active metabolite isomers and the antiestrogenic activity score. Barginear, MF; Desnick, RJ; Jaremko, M; Kasai, Y; Kemeny, M; Peter, I; Raptis, G; Yu, C, 2011) | 0.76 |
" Rats in the acute E(2) dosing group (aE(2)) showed reduced inhibitory avoidance responses with prolong escape latencies compared to Ovx; while rats in the chronic E(2) dosing group (cE(2)) showed reduced inhibitory avoidance responses only." | ( Effect of the acute and chronic estrogen on anxiety in the elevated T-maze. Daendee, S; Kalandakanond-Thongsong, S; Srikiatkhachorn, A, 2012) | 0.38 |
" 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) | 0.38 |
" Rather, we show it is required for stable entry into both the cortical and medullary TEC differentiation programmes and subsequently is needed at increasing dosage for progression through successive differentiation states in both cortical and medullary TEC." | ( Foxn1 regulates lineage progression in cortical and medullary thymic epithelial cells but is dispensable for medullary sublineage divergence. Blackburn, CC; Bredenkamp, N; Heussen, R; Jin, X; Nowell, CS; Sheridan, JM; Smith, AJ; Stenhouse, FH; Tetélin, S; Tischner, C; Vaidya, H, 2011) | 0.37 |
"Tamoxifen dosage is based on the one-dose-fits-all approach." | ( Tissue distribution of 4-hydroxy-N-desmethyltamoxifen and tamoxifen-N-oxide. Aristarco, V; Decensi, A; Gandini, S; Gjerde, J; Guerrieri-Gonzaga, A; Haugan Moi, LL; Lien, EA; Mellgren, G, 2012) | 2.08 |
" Taken together, our data suggest that establishment of a complete range of AP positional identities in the limb requires integration of the spatial distribution, timing, and dosage of GLI2 and GLI3 activators and repressors." | ( Limb anterior-posterior polarity integrates activator and repressor functions of GLI2 as well as GLI3. Bao, X; Bowers, M; Eng, L; Joyner, AL; Lao, Z; Mackem, S; Riedel, E; Turnbull, RK, 2012) | 0.38 |
" The possibility of using this method for drug discovery applications is also demonstrated through the measurement of dose-response kinetics upon induction of autophagy with rapamycin and tamoxifen." | ( A novel image-based cytometry method for autophagy detection in living cells. Chan, E; Chan, LL; Kuksin, D; Lai, N; Lin, B; Patton, W; Qiu, J; Shen, D; Wilkinson, AR, 2012) | 0.57 |
" The plasma concentrations of TOR and its N-desmethyl (NDM) and 4-hydroxy (4-OH) metabolites during steady-state dosing with TOR were also determined." | ( Role and pharmacologic significance of cytochrome P-450 2D6 in oxidative metabolism of toremifene and tamoxifen. Barrett, CM; Bohl, CE; Coss, CC; Dalton, JT; He, Y; Kim, J; Li, CM; Mohler, ML; Veverka, KA, 2013) | 0.61 |
" The estrogenic potencies of the dyes and wastewater samples were evaluated by dose-response curves and compared to the dose-response curve of 17β-estradiol (E2), the reference compound." | ( Estrogenic and anti-estrogenic activity of 23 commercial textile dyes. Bartegi, A; Bazin, I; De Waard, M; Gonzalez, C; Haj Hamouda, Y; Ibn Hadj Hassine, A; Lopez-Ferber, M; Mnif, W, 2012) | 0.38 |
" Cancer cells are highly attractive to glucose [with a nanosize bimolecular structure 1nm] as an energy source more than normal cell and nanosized therapeutics due to possessing different pharmacokinetic and pharmacodynamic have advantageous over classical dosage forms in cancer therapy." | ( Nanosized tamoxifen-porphyrin-glucose [TPG] conjugate: novel selective anti-breast-cancer agent, synthesis and in vitro evaluations. Aghasadeghi, MR; Alaei-Beirami, M; Alavidjeh, MS; Amanlou, M; Arabzadeh, AJ; Ardestani, MS; Dashtbani-Roozbehani, A; Delbaz, SA; Ebrahimi, SE; Ghorbani, M; Hajmohammadi, M; Heidari, Z; Hekmat, S; Moghaddam, HF; Sadat, SM; Saraji, AA; Siadat, SD, 2013) | 0.79 |
" If the present rat data are extrapolated to humans, the alterations in tamoxifen absorption and metabolism should be considered in designing a dosage regimen for cancer patients with PCM and/or oral cysteine supplement." | ( Effects of cysteine on the pharmacokinetics of tamoxifen in rats with protein-calorie malnutrition. Choi, YH; Lee, MG; Lee, YK; Yoon, I, 2012) | 0.87 |
" In a first series of experiments using hemizygous tamoxifen-induced genetic inactivation of a floxed γ2 genomic locus we show that reducing the gene dosage at postnatal days (P)13/14 but not P27/28 results in altered behavior in both of these tests in adulthood, reminiscent of the anxious-depressive phenotype previously described for global heterozygous mice." | ( GABAergic control of critical developmental periods for anxiety- and depression-related behavior in mice. Fuchs, T; Luscher, B; Sahir, N; Shen, Q, 2012) | 0.63 |
"Mice deficient for CELF4, a neuronal RNA-binding protein, have a complex seizure disorder that includes both convulsive and non-convulsive seizures, and is dependent upon Celf4 gene dosage and mouse strain background." | ( Aberrant sodium channel activity in the complex seizure disorder of Celf4 mutant mice. Briese, M; Frankel, WN; Mahaffey, CL; Sun, W; Ule, J; Wagnon, JL, 2013) | 0.39 |
" A series of systemic biomarkers (including lipid and insulin-like growth factor levels) and tissue biomarkers (including Ki-67) are known to be favorably affected by conventional tamoxifen dosing and have been shown to be modulated in a direction consistent with a putative anti-cancer effect." | ( Oral low dose and topical tamoxifen for breast cancer prevention: modern approaches for an old drug. Decensi, A; Dunn, BK; Heckman-Stoddard, BM; Khan, S; Lazzeroni, M; Lee, O; Serrano, D, 2012) | 0.87 |
" Taken together, our study demonstrated a dose-dependent growth response to Tam in TAM-R cells, which will promote the understanding of the importance of the appropriate use and dosage of Tam in the clinic." | ( Dose-dependent effect of tamoxifen in tamoxifen-resistant breast cancer cells via stimulation by the ERK1/2 and AKT signaling pathways. Bai, E; Han, SX; Jing, GH; Li, M; Wang, LJ; Yang, AG; Zhao, J; Zhou, X; Zhu, Q, 2013) | 0.69 |
" Our results suggest that intermittent dosing regimes of drugs that restore wild-type tumor-suppressor function onto mutant, inactive p53 proteins will prove to be more efficacious than traditional chronic dosing by similarly reducing adaptive resistance." | ( Using a preclinical mouse model of high-grade astrocytoma to optimize p53 restoration therapy. Berger, MS; Evan, GI; Hanahan, D; Li, N; Lyubynska, N; Persson, AI; Rostker, F; Shchors, K; Swigart, LB; Tihan, T; Weiss, WA, 2013) | 0.39 |
" Adenomyosis was induced in 28 female ICR mice neonatally dosed with tamoxifen, while another 12 (group C) were dosed with solvent only, which served as a blank control." | ( Epigallocatechin-3-gallate reduces myometrial infiltration, uterine hyperactivity, and stress levels and alleviates generalized hyperalgesia in mice induced with adenomyosis. Chen, Y; Guo, SW; Liu, X; Zhang, H; Zhu, B, 2013) | 0.62 |
" After tamoxifen dosing of CDX2P-CreER(T2) mice, Cre activity was detected in the distal ileal, cecal, colonic, and rectal epithelium, with selected crypt base, transit amplifying, and surface cells all capable of activating Cre function." | ( Sox9 induction, ectopic Paneth cells, and mitotic spindle axis defects in mouse colon adenomatous epithelium arising from conditional biallelic Apc inactivation. Bommer, GT; Cho, KR; Fearon, ER; Feng, Y; Green, M; Sands, E; Sentani, K; Wiese, A, 2013) | 0.84 |
" The aim of this study was to assess the prognostic role of ESR1 gene dosage in a consecutive group of breast cancer patients and to correlate this feature with clinico-pathological factors." | ( Prognostic significance of ESR1 amplification and ESR1 PvuII, CYP2C19*2, UGT2B15*2 polymorphisms in breast cancer patients. Jaśkiewicz, J; Jassem, J; Markiewicz, A; Skokowski, J; Szade, J; Wełnicka-Jaśkiewicz, M; Zaczek, AJ, 2013) | 0.39 |
"Primary tumor samples from 281 stage I-III consecutive breast cancer patients were analyzed for ESR1 gene dosage using real-time PCR with locked nucleic acids hydrolysis probes." | ( Prognostic significance of ESR1 amplification and ESR1 PvuII, CYP2C19*2, UGT2B15*2 polymorphisms in breast cancer patients. Jaśkiewicz, J; Jassem, J; Markiewicz, A; Skokowski, J; Szade, J; Wełnicka-Jaśkiewicz, M; Zaczek, AJ, 2013) | 0.39 |
" Limiting the effects of the MetS-induced estrogen action via GPER could offer new perspectives in the management of BPH/LUTS, whereas tamoxifen dosing showed potential benefits in bladder." | ( Opposite effects of tamoxifen on metabolic syndrome-induced bladder and prostate alterations: a role for GPR30/GPER? Cellai, I; Comeglio, P; Corcetto, F; Corno, C; Filippi, S; Gacci, M; Maggi, M; Maneschi, E; Morelli, A; Sarchielli, E; Vannelli, GB; Vignozzi, L, 2014) | 0.93 |
"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) | 0.39 |
" A non-monotonic dose-response on cell viability was observed when HepG2 cells were exposed to TAM alone or in the presence of CIP." | ( In vitro tests aiding ecological risk assessment of ciprofloxacin, tamoxifen and cyclophosphamide in range of concentrations released in hospital wastewater and surface water. Albasi, C; Castillo, L; Faucet-Marquis, V; Geret, F; Mater, N; Pfohl-Leszkowicz, A, 2014) | 0.64 |
" There was wide variability in tamoxifen and metabolite concentrations within the dosing groups." | ( Tamoxifen dose and serum concentrations of tamoxifen and six of its metabolites in routine clinical outpatient care. Beijnen, JH; Jager, NG; Linn, SC; Rosing, H; Schellens, JH, 2014) | 2.13 |
" 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, ) | 0.13 |
" Importantly, decreasing Mdm2 gene dosage in mouse mammary epithelial cells potentiates estrogen-dependent AKT activation owing to HPIP stabilization." | ( MDM2 restrains estrogen-mediated AKT activation by promoting TBK1-dependent HPIP degradation. Bentires-Alj, M; Borgs, L; Brinkhaus, H; Chariot, A; Close, P; Göktuna, SI; Marine, JC; Nguyen, L; Olivier, F; Patrascu, F; Rammal, A; Shostak, K, 2014) | 0.4 |
" Monkeys were given 3-4 months of chronic TAM dosing scaled to be equivalent to the daily human dose." | ( Tamoxifen-DNA adduct formation in monkey and human reproductive organs. Cline, JM; Hernandez-Ramon, EE; John, K; Poirier, MC; Sandoval, NA; Wood, CE; Woodward, RA, 2014) | 1.85 |
" These candidates were subjected to a dose-response bioactivity assay, measuring an increase in α-tubulin K40 acetylation in two neuronal cell lines, which yielded five compounds bioactive in both cell lines and eight compounds bioactive in at least one of the cell lines tested." | ( Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors. Choi, SH; Kazantsev, AG; Khanfar, MA; Quinti, L; Silverman, RB; Wang, H, 2014) | 0.4 |
" The mean ovarian dysplasia score was significantly higher in the tamoxifen group whatever the dosage (p = 0." | ( Morphological and immunohistochemical analysis in ovaries and fallopian tubes of tamoxifen, letrozole and clomiphene-treated rats. Chene, G; Clemenson, A; Lacoste, CR; Lecointre, R; Lima, S; Peoc'h, M; Trombert, B, 2014) | 0.87 |
" One of the most widely studied drugs with regard to genomics-guided dosing options is the oral anticoagulant, warfarin." | ( Is personalized medicine a dream or a reality? Kim, RB; Morse, BL, 2015) | 0.42 |
" In all studied animals suffering from tumors, pharmacological tamoxifen treatment was administered, at a dosage of 2 mg/kg bodyweight." | ( VEGF and 17-β-estradiol levels after tamoxifen administration in canine hepatoid gland adenomas and hepatoid gland epitheliomas. Brodzki, A; Sobczyńska-Rak, A, ) | 0.64 |
" Reduction in tamoxifen dosing allowed for maintained gene deletion without any cardiomyopathy, possibly through activation of survival signalling through the related ERK pathway." | ( PI3Kα is essential for the recovery from Cre/tamoxifen cardiotoxicity and in myocardial insulin signalling but is not required for normal myocardial contractility in the adult heart. Basu, R; DesAulniers, J; Kassiri, Z; McLean, BA; Murray, AG; Oudit, GY; Parajuli, N; Patel, VB; Vanhaesebroeck, B; Zhabyeyev, P, 2015) | 1.04 |
" Adenomyosis was induced in 28 female ICR mice neonatally dosed with tamoxifen, while another 12 (group C) were dosed with solvent only, serving as a blank control." | ( Resveratrol Reduces Myometrial Infiltration, Uterine Hyperactivity, and Stress Levels and Alleviates Generalized Hyperalgesia in Mice With Induced Adenomyosis. Chen, Y; Guo, SW; Liu, X; Zhang, H; Zhu, B, 2015) | 0.65 |
" Kinase inhibitors preferentially targeting growth of fulvestrant resistant cells were identified and the growth inhibitory effect verified by dose-response cell growth experiments." | ( Aurora kinase B is important for antiestrogen resistant cell growth and a potential biomarker for tamoxifen resistant breast cancer. Bak, M; Duun-Henriksen, AK; Kirkegaard, T; Laenkholm, AV; Larsen, SL; Lykkesfeldt, AE; Rasmussen, BB; Yde, CW, 2015) | 0.63 |
" Additional research is needed to improve the prediction of CYP2D6 activity from genetic data for individualized dosing of CYP2D6 dependent drugs." | ( In vivo assessment of the metabolic activity of CYP2D6 diplotypes and alleles. Anderson, S; Carey, LA; Carrizosa, DR; Corso, S; Desta, Z; Evans, JP; Flockhart, DA; Hertz, DL; Ibrahim, JG; Irvin, WJ; Jones, DR; Magrinat, G; McLeod, HL; Moore, S; Olajide, O; Peppercorn, JM; Raab, R; Schwartz, G; Snavely, AC; Walko, CM; Weck, KE, 2015) | 0.42 |
"The dosage effect of adjuvant treatments, cancer staging, genetic or environmental confounders associated with the risk of depressive disorders were not comprehensively evaluated." | ( Adjuvant treatments of breast cancer increase the risk of depressive disorders: A population-based study. Chang, CH; Chen, SJ; Liu, CY, 2015) | 0.42 |
" The risk of fractures decreased with an increasing dosage of tamoxifen." | ( Tamoxifen use reduces the risk of osteoporotic fractures in women with breast cancer in Asia: a nationwide population-based cohort study. Chen, HT; Hsu, HC; Hwang, WL; Muo, CH; Tsai, CH; Tzeng, HE, 2015) | 2.1 |
" Therapeutic drug monitoring seems to be the most direct and promising approach, however, further clinical research is warranted to establish the added value of individual dosing in tamoxifen treatment optimization." | ( Tailored Tamoxifen Treatment for Breast Cancer Patients: A Perspective. Beijnen, JH; Jager, NG; Linn, SC; Schellens, JH, 2015) | 1.03 |
" Pharmacokinetic analysis was performed in mice, dosed at six different times (24-h period)." | ( Circadian variation in tamoxifen pharmacokinetics in mice and breast cancer patients. Binkhorst, L; Burger, H; Chaves, I; de Bruijn, P; de Wit, AS; Hamberg, P; Jager, A; Kloth, JSL; Koch, BCP; Lam, MH; Mathijssen, RHJ; van Alphen, RJ; van der Horst, GTJ; van Gelder, T; van Schaik, RHN; Wiemer, EAC, 2015) | 0.73 |
" ZB483 was demonstrated to be more efficacious than endoxifen in inhibiting xenograft tumor growth in mice at equal dosage but more so at lower dosage." | ( Boronic prodrug of endoxifen as an effective hormone therapy for breast cancer. Miele, L; Wang, G; Zhang, C; Zhang, Q; Zheng, S; Zhong, Q, 2015) | 0.42 |
"Combination therapy, which reduces the dosage intensity of the individual drugs while increasing their efficacy, is not a novel approach for the treatment of cancer." | ( The combination of methylsulfonylmethane and tamoxifen inhibits the Jak2/STAT5b pathway and synergistically inhibits tumor growth and metastasis in ER-positive breast cancer xenografts. Chang, SH; Cho, BW; Darvin, P; Hwang, TS; Joung, YH; Kang, DY; Kim, DN; Kim, HS; Kim, SY; Kim, WS; Lee, HK; Park, JH; Park, KD; S P, N; Yang, YM; Yoo, YB, 2015) | 0.68 |
"With increasing dosage of quercetin, significant decrease in proliferation and increase in apoptosis was observed." | ( Quercetin reverses tamoxifen resistance in breast cancer cells. Chen, T; Feng, D; Kong, H; Lin, Q; Qi, K; Tao, L; Wang, H; Wei, W; Zhang, H, ) | 0.46 |
"Proliferation inhibition and apoptosis in MCF-7Ca/TAM-R cells increase with increasing dosage of quercetin." | ( Quercetin reverses tamoxifen resistance in breast cancer cells. Chen, T; Feng, D; Kong, H; Lin, Q; Qi, K; Tao, L; Wang, H; Wei, W; Zhang, H, ) | 0.46 |
" By optimizing the timing and dosage of tamoxifen administration, we controlled Cre expression specifically in cranial NCCs." | ( Sox10ER(T2) CreER(T2) mice enable tracing of distinct neural crest cell populations. He, F; Soriano, P, 2015) | 0.68 |
"6 mg dosing suppresses estradiol (E2) production and has proven efficacy in pre-menopausal women with estrogen receptor (ER)-positive breast cancer." | ( Phase 3, open-label, randomized study comparing 3-monthly with monthly goserelin in pre-menopausal women with estrogen receptor-positive advanced breast cancer. Isidro, J; Itoh, Y; Jesena, A; Kim, HJ; Kim, KS; Lokejaroenlarb, S; Noguchi, S; Parmar, V; Sato, N; Shin, E; Wang, HC, 2016) | 0.43 |
" Further, ZB497 was more effective than tamoxifen at lowered dosage in inhibiting the growth of xenograft tumors in mice." | ( Boronic prodrug of 4-hydroxytamoxifen is more efficacious than tamoxifen with enhanced bioavailability independent of CYP2D6 status. Miele, L; Wang, G; Zhang, C; Zhang, Q; Zheng, S; Zhong, Q, 2015) | 0.98 |
" The drug is usually dosed 20 mg/d irrespective of interindividual variation in drug clearance." | ( Pronounced Interindividual But Not Intraindividual Variation in Tamoxifen and Metabolite Levels in Plasma During Adjuvant Treatment of Women With Early Breast Cancer. Fotoohi, AK; Hatschek, T; Karim, H; Lafolie, P; Östervall, J; Pohanka, A; Vitols, S, 2016) | 0.67 |
"Large interindividual variation of tamoxifen and endoxifen with stable intraindividual levels, and too low levels of endoxifen in a considerable proportion of patients strongly support that therapeutic drug monitoring and individualized dosing could lead to optimal exposure and hopefully better outcome." | ( Pronounced Interindividual But Not Intraindividual Variation in Tamoxifen and Metabolite Levels in Plasma During Adjuvant Treatment of Women With Early Breast Cancer. Fotoohi, AK; Hatschek, T; Karim, H; Lafolie, P; Östervall, J; Pohanka, A; Vitols, S, 2016) | 0.95 |
" The dosage of morphine was counted as defined daily dose and its effect was assessed by multivariable Cox proportional hazard regression controlling age, Charlson comorbidity index, outpatient department visits, antipsychotics, and breast cancer drugs." | ( Risk of type 2 diabetes mellitus in female breast cancer patients treated with morphine: A retrospective population-based time-dependent cohort study. Chang, YJ; Lai, SW; Lee, CW; Morisky, DE; Muo, CH; Wang, IK; Yang, SP, 2015) | 0.42 |
" Tamoxifen, an older, nonhematotoxic medication, has limited activity in systemic mastocytosis at the dosage used in this study." | ( Response of patients with indolent systemic mastocytosis to tamoxifen citrate. Butterfield, JH; Chen, D, 2016) | 1.59 |
" The treatment allowed dosing adjustments of methotrexate and capecitabine for pretreatment renal function." | ( Effect of Pretreatment Renal Function on Treatment and Clinical Outcomes in the Adjuvant Treatment of Older Women With Breast Cancer: Alliance A171201, an Ancillary Study of CALGB/CTSU 49907. Cirrincione, CT; Cohen, HJ; Gralow, J; Hurria, A; Jatoi, A; Lichtman, SM; Magrinat, G; Morganstern, DE; Muss, HB; Theodoulou, M; Wolff, AC, 2016) | 0.43 |
"Excluding from clinical trials patients with renal insufficiency but good performance status on the basis of concern of excessive hematologic toxicity or poor outcomes may not be justified with appropriate dosing modifications." | ( Effect of Pretreatment Renal Function on Treatment and Clinical Outcomes in the Adjuvant Treatment of Older Women With Breast Cancer: Alliance A171201, an Ancillary Study of CALGB/CTSU 49907. Cirrincione, CT; Cohen, HJ; Gralow, J; Hurria, A; Jatoi, A; Lichtman, SM; Magrinat, G; Morganstern, DE; Muss, HB; Theodoulou, M; Wolff, AC, 2016) | 0.43 |
" To address this, we set out to establish a safe and effective tamoxifen dosing regimen that can be used in newborn mouse pups subjected to injurious stimuli, such as exposure to elevated levels of environmental oxygen." | ( Tamoxifen dosing for Cre-mediated recombination in experimental bronchopulmonary dysplasia. Ahlbrecht, K; Herold, S; Mayer, K; Morty, RE; Rodríguez-Castillo, JA; Ruiz-Camp, J; Seeger, W; Tallquist, MD; Vadász, I, 2017) | 2.14 |
" 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) | 0.46 |
" 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) | 0.46 |
" 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 |
" The application of electroporation increased the uptake of tamoxifen into MCF-7 cells and reduced the minimal tamoxifen dosage which, is needed for the treatment of estrogen receptor positive breast cancer." | ( Effects of Electroporation on Tamoxifen Delivery in Estrogen Receptor Positive (ER+) Human Breast Carcinoma Cells. Canseven, AG; Coskun, A; Esmekaya, MA; Kayhan, H; Yagci, M, 2017) | 0.99 |
" These results suggest that fucoidan in the studied form and dosage could be taken concomitantly with letrozole and tamoxifen without the risk of clinically significant interactions." | ( The Effect of Undaria pinnatifida Fucoidan on the Pharmacokinetics of Letrozole and Tamoxifen in Patients With Breast Cancer. Fitton, JH; Lowenthal, RM; McGuinness, G; Olesen, I; Oliver, LJ; Patel, R; Peterson, GM; Shastri, M; Tocaciu, S, 2018) | 0.92 |
" Fulvestrant use was also assessed pre- and post-2010 (when fulvestrant 500 mg dosing was approved)." | ( Patient database analysis of fulvestrant 500 mg in the treatment of metastatic breast cancer: A European perspective. Berger, K; Gligorov, J; Lewis, J; Maass, N; MacDougall, F; Marchetti, P; Montonen, J, 2017) | 0.46 |
" Endoxifen steady-state fluctuations within a dosing interval were minimal (<6%)." | ( Exploiting Pharmacokinetic Models of Tamoxifen and Endoxifen to Identify Factors Causing Subtherapeutic Concentrations in Breast Cancer Patients. Csajka, C; Joerger, M; Kloft, C; Klopp-Schulze, L; Parra-Guillen, ZP; Ter Heine, R; Wicha, SG, 2018) | 0.75 |
" Thirty female Sprague-Dawley rats received a single medication dosage of 7,12-dimethylbenz[a]anthracene (DMBA) intragastrically." | ( The biochemical effects of nano tamoxifen and some bioactive components in experimental breast cancer. Abd El Azeem, AS; Abdelhamid, AO; El Awady, MK; Ezzat, A; Mohammed, DM, 2017) | 0.74 |
" Integration of clinician and genetic variables into individualized tamoxifen dosing algorithms would marginally improve their accuracy and potentially enhance tamoxifen treatment outcomes." | ( Comprehensive assessment of cytochromes P450 and transporter genetics with endoxifen concentration during tamoxifen treatment. Carey, LA; Danko, W; Deal, AM; Desta, Z; Hertz, DL; Ibrahim, JG; Irvin, WJ; Jones, DR; Marcath, LA; McLeod, HL; Van Wieren, E; Walko, CM; Weck, KE, 2017) | 0.9 |
"There is growing need to develop efficient methods for early-stage drug discovery, continuous manufacturing of drug delivery vehicles, and ultra-precise dosing of high potency drugs." | ( Printing of small molecular medicines from the vapor phase. Amidon, GE; Clarke, R; Fleck, E; Jones, CM; Mazzara, JM; Mehta, G; Raghavan, S; Rockwell, C; Schwendeman, A; Senabulya, N; Shalev, O; Shtein, M; Simopoulos, N; Sinko, PD, 2017) | 0.46 |
" Sex-related differential effects of the drugs call for a careful consideration for the drug and dosage selection in male and female patient populations." | ( Long-Term Treatment of Tamoxifen and Raloxifene Alleviates Dystrophic Phenotype and Enhances Muscle Functions of FKRP Dystroglycanopathy. Blaeser, A; Bollinger, LE; Harper, AD; Lu, P; Lu, QL; Shah, SN; Sparks, S; Wu, B, 2018) | 0.79 |
"The Tamoxifen Response by CYP2D6 Genotype-based Treatment-1 (TARGET-1) study (n = 180) was conducted from 2012-2017 in Japan to determine the efficacy of tamoxifen dosing guided by cytochrome P450 2D6 (CYP2D6) genotypes." | ( Application of PBPK Modeling and Virtual Clinical Study Approaches to Predict the Outcomes of CYP2D6 Genotype-Guided Dosing of Tamoxifen. Imamura, CK; Lee, W; Nakamura, T; Sugiyama, Y; Tanigawara, Y; Toshimoto, K, 2018) | 1.24 |
" Such a preparation was incubated in vitro with MCF-7 human breast cancer cells, showing a decrease in the TAM dosage for the reduction of cell viability." | ( Insights on the transport of tamoxifen by gold nanoparticles for MCF-7 breast cancer cells based on SERS spectroscopy. Costa, LAS; Lataliza, AAB; Raposo, NRB; Sant'Ana, AC; Teixeira, RAR, 2018) | 0.77 |
" Structure-based modification of mifepristone led to the discovery of ORIC-101 (28), a highly potent steroidal GR antagonist with reduced androgen receptor (AR) agonistic activity amenable for dosing in androgen receptor positive tumors and with improved CYP2C8 and CYP2C9 inhibition profile to minimize drug-drug interaction potential." | ( Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101). Chen, C; Du, X; Eksterowicz, J; Fantin, VR; Huang, E; Huang, T; Jackson, E; Jahchan, N; Kawai, H; McGee, LR; Medina, JC; Rew, Y; Sun, D; Sutimantanapi, D; Waszczuk, J; Yan, X; Ye, Q; Zavorotinskaya, T; Zhou, H; Zhu, L, 2018) | 0.48 |
"6 mg/mL JEKHT reversed their TAM resistance in dose-response studies in vitro." | ( Effects of Jaeumkanghwa-tang on tamoxifen responsiveness in preclinical ER+ breast cancer model. Carney, E; Clarke, R; De Oliveira Andrade, F; FitzGerald, K; Hilakivi-Clarke, L; Hu, R; Yu, W; Zhang, X, 2019) | 0.8 |
" In contrast, this dosage of tamoxifen did not induce noticeable changes in the energy metabolism and thermogenesis of adipose tissue in male mice under room temperature." | ( Even a low dose of tamoxifen profoundly induces adipose tissue browning in female mice. de Avila, JM; Du, M; Gomez, NA; Wang, B; Zhao, L; Zhu, MJ, 2020) | 1.18 |
" In conclusion, clinicians should carefully set the dosage of chemotherapy drugs to avoid the long-term side effects associated with such drugs." | ( A diffuse large B cell lymphoma emerging with breast cancer relapse. Altindal, S; Dogu, MH; Huq, G; Karismaz, A; Suyani, E; Yokus, O, 2018) | 0.48 |
" Identification of risk factors for relapse can be useful not only to modulate the choice, the dosage of first-line treatment and the duration of maintenance therapy but also for preventing a progressive loss of kidney function, as well." | ( Risk factors for relapse and long-term outcome of idiopathic retroperitoneal fibrosis. Barsotti, S; Capecchi, R; Cupisti, A; Francesca Egidi, M; Gaetano Tavoni, A; Giannese, D; Morganti, R; Moriconi, D; Orsitto, E, 2019) | 0.51 |
" There was little to no vaginal or systemic accumulation of tamoxifen following once-daily dosing for 28 days." | ( Vaginal tamoxifen for treatment of vulvar and vaginal atrophy: Pharmacokinetics and local tolerance in a rabbit model over 28 days. Chollet, J; Friend, DR; Mermelstein, F; Rocamboli, SC, 2019) | 1.19 |
" MATERIAL AND METHODS Using an Achilles tendon trauma-induced HO female mice model, we screened different doses of tamoxifen (1, 3, and 9 mg/kg) in mice to determine the optimal dosage on the inhibition of the HO formation." | ( Tamoxifen Inhibits the Progression of Trauma-Induced Heterotopic Ossification in Mice. Li, F; Mao, D; Mi, J; Pan, X; Rui, Y, 2019) | 2.17 |
" As results, quercetin showed contrasting dose-response to cellular behaviors dependent on the ROS-regulated p53 signaling pathways." | ( Quercetin exerts bidirectional regulation effects on the efficacy of tamoxifen in estrogen receptor-positive breast cancer therapy: An in vitro study. Huang, B; Pan, X; Xia, X; Xu, Z; Zhao, D; Zheng, X, 2020) | 0.79 |
" The objective of this study was to evaluate the efficacy of daily dosing of mirtazapine on cocaine-induced locomotor activity and sensitization in naive female rats compared to male rats." | ( Mirtazapine reduces the expression of cocaine-induced locomotor sensitization in male and female Wistar rats. Barbosa-Méndez, S; Osorio-Santiago, KL; Salazar-Juárez, A, 2020) | 0.56 |
"Male and female Wistar rats were daily dosed with 10 mg/kg of cocaine." | ( Mirtazapine reduces the expression of cocaine-induced locomotor sensitization in male and female Wistar rats. Barbosa-Méndez, S; Osorio-Santiago, KL; Salazar-Juárez, A, 2020) | 0.56 |
" However, there remains a lack of consensus on the optimal route and dosage of TAM administration in vivo." | ( Optimization of tamoxifen-induced Cre activity and its effect on immune cell populations. Chung, H; Creusot, RJ; Donocoff, RS; Shoulson, R; Teteloshvili, N, 2020) | 0.9 |
" Tamoxifen treatment duration longer than 1500 days or with cumulative dosage higher than 26 320 mg have especially lowered risk of meningioma." | ( Tamoxifen prevention of meningioma and its proposal for the treatment of meningioma. Revisiting old data in the light of recent epidemiological observations. Altinoz, MA, 2021) | 2.97 |
" There is insufficient evidence at present to recommend tailoring adjuvant endocrine therapy with use of specific AIs or for dosing modifications of AIs in this patient population." | ( Impact of obesity on clinical outcomes in hormone receptor-positive breast cancer: a systematic review. Pezo, RC; Shirdarreh, M, 2021) | 0.62 |
" Importantly, the result indicated that the low dosage does not induce significant systemic recombination in remote skeletal tissues." | ( Activation of creER recombinase in the mouse calvaria induces local recombination without effects on distant skeletal segments. Hou, J; Intini, G; Lin, CP, 2021) | 0.62 |
" She experienced severe tamoxifen-induced hypertriglyceridemia several months after dosing tamoxifen." | ( A case of tamoxifen-induced hypertriglyceridemia monitoring the changes in lipoprotein fractions over time. Isobe, H; Kaku, K; Kan, Y; Kaneto, H; Katakura, Y; Kimura, T; Kohara, K; Mune, T; Nakanishi, S; Obata, A; Shimoda, M; Tatsumi, F, 2021) | 1.33 |
" It is very important to evaluate the balance between benefit and risk before dosing tamoxifen and survey lipid profiles constantly during treatment to avoid life-threatening complication when prescription of tamoxifen is planned." | ( A case of tamoxifen-induced hypertriglyceridemia monitoring the changes in lipoprotein fractions over time. Isobe, H; Kaku, K; Kan, Y; Kaneto, H; Katakura, Y; Kimura, T; Kohara, K; Mune, T; Nakanishi, S; Obata, A; Shimoda, M; Tatsumi, F, 2021) | 1.25 |
", changing morning dosing to evening dosing or vice versa) can reduce side effects." | ( Does the Time of Day at Which Endocrine Therapy Is Taken Affect Breast Cancer Patient Outcomes? Beltran-Bless, AA; Clemons, M; Hutton, B; Ibrahim, MFK; Savard, MF; Shorr, R; Vandermeer, L, 2021) | 0.62 |
" A significant limitation of fulvestrant is the dosing regimen required for efficacy." | ( Discovery of GNE-502 as an orally bioavailable and potent degrader for estrogen receptor positive breast cancer. Blake, RA; Chang, J; Friedman, L; Goodacre, S; Hartman, SJ; Kiefer, JR; Kleinheinz, T; Labadie, S; Lai, T; Li, J; Liang, J; Liao, J; McLean, N; Metcalfe, C; Mody, V; Nannini, M; Ortwine, DF; Ran, Y; Ray, N; Rei Ingalla, E; Roussel, F; Sambrone, A; Sampath, D; Vinogradova, M; Wai, J; Wang, T; Wang, X; Yeap, K; Zbieg, JR; Zhang, B; Zheng, X; Zhong, Y, 2021) | 0.62 |
" Adenomyosis mice were given berberine by intraperitoneal injection with the dosage of 5, 10, and 20 mg/kg body weight, respectively, at 17 weeks after birth." | ( Berberine attenuates hyperalgesia in mice with adenomyosis. Chen, Y; Guo, M; Huang, L; Lin, T; Lu, Y; Pan, Q; Shen, X; Zhang, C; Zhang, H; Zhu, B, 2022) | 0.72 |
" For radiotherapy risks, searches for dose-response relationships and modern organ doses were also undertaken." | ( Adjuvant and neoadjuvant breast cancer treatments: A systematic review of their effects on mortality. Darby, SC; Dodwell, D; Duane, F; Holt, F; Kerr, AJ; Mannu, G; McGale, P; Taylor, CW, 2022) | 0.72 |
"Tamoxifen is prescribed for chronic mastalgia at a dosage of one 10- or 20-mg tablet for 3-6 months." | ( Tamoxifen in Mastalgia: A Meta-Analysis. Asharaf, AA; Barman, A; Jha, AK; Sahu, S; Sinha, MK, 2022) | 3.61 |
" Our purpose was to develop a prediction model for endoxifen concentrations, as a strategy to individualize tamoxifen treatment by model-informed dosing in order to prevent subtherapeutic exposure (endoxifen < 16 nmol/L) and thus potential failure of therapy." | ( Factors affecting inter-individual variability in endoxifen concentrations in patients with breast cancer: results from the prospective TOTAM trial. Abrams, S; Braal, CL; Buijs, SM; Jager, A; Koolen, SLW; Mathijssen, RHJ; Mulder, TAM; van Schaik, RHN; Westenberg, JD, 2022) | 0.93 |
" The remaining unexplained inter-individual variability is still high and therefore model-informed tamoxifen dosing should be accompanied by therapeutic drug monitoring." | ( Factors affecting inter-individual variability in endoxifen concentrations in patients with breast cancer: results from the prospective TOTAM trial. Abrams, S; Braal, CL; Buijs, SM; Jager, A; Koolen, SLW; Mathijssen, RHJ; Mulder, TAM; van Schaik, RHN; Westenberg, JD, 2022) | 0.94 |
" Oral dosing of ENDX resulted in substantially higher ENDX concentrations than a similar dose of TAM." | ( Bioavailability and Pharmacokinetics of Endoxifen in Female Rats and Dogs: Evidence to Support the Use of Endoxifen to Overcome the Limitations of CYP2D6-Mediated Tamoxifen Metabolism. Ames, MM; Buhrow, SA; Goetz, MP; Jia, L; Koubek, EJ; Reid, JM; Safgren, SL, 2023) | 1.11 |
" Our aim is to develop a population pharmacokinetic (POP-PK) model incorporating a continuous CYP2D6 activity scale to support model informed precision dosing (MIPD) of tamoxifen to determine the optimal tamoxifen starting dose." | ( Toward model-informed precision dosing for tamoxifen: A population-pharmacokinetic model with a continuous CYP2D6 activity scale. Agema, BC; Buijs, SM; Jager, A; Koch, BCP; Koolen, SLW; Mathijssen, RHJ; Mürdter, TE; Sassen, SDT; Schwab, M; van Schaik, RHN, 2023) | 1.37 |
" Thereafter, dosing cut-off values for MIPD were determined." | ( Toward model-informed precision dosing for tamoxifen: A population-pharmacokinetic model with a continuous CYP2D6 activity scale. Agema, BC; Buijs, SM; Jager, A; Koch, BCP; Koolen, SLW; Mathijssen, RHJ; Mürdter, TE; Sassen, SDT; Schwab, M; van Schaik, RHN, 2023) | 1.17 |
" After external validation and determination of dosing cut-off points, MIPD could reduce the proportion of patients with subtherapeutic endoxifen levels at from 22." | ( Toward model-informed precision dosing for tamoxifen: A population-pharmacokinetic model with a continuous CYP2D6 activity scale. Agema, BC; Buijs, SM; Jager, A; Koch, BCP; Koolen, SLW; Mathijssen, RHJ; Mürdter, TE; Sassen, SDT; Schwab, M; van Schaik, RHN, 2023) | 1.17 |
" Linear dose-response model indicated a direct significant association between dose and duration use of tamoxifen and EC (dose: exe(b) = 1." | ( Tamoxifen use and risk of endometrial cancer in breast cancer patients: A systematic review and dose-response meta-analysis. Akbari, A; Akbari, ME; Amin Amlashi, M; Ardehali, SH; Barragan-Carrillo, R; Chavarri-Guerra, Y; Ghanavati, M; Javid, Z; Khorshidi, Y; Rahmani, J; Shadnoush, M, 2023) | 2.57 |
" Our findings give new insights which may influence future dosing strategies of tamoxifen in both the adjuvant and preventive settings." | ( Side effects of low-dose tamoxifen: results from a six-armed randomised controlled trial in healthy women. Bäcklund, M; Bergqvist, J; Borgquist, S; Crippa, A; Czene, K; Discacciati, A; Eklund, M; Eriksson, M; Gabrielson, M; Hall, P; Hammarström, M; Lundholm, C; Tapia, J; Wengström, Y, 2023) | 1.44 |
" This review aimed to optimize tamoxifen administration regimens including its dosage and duration, to identify an optimal induction strategy that minimizes potential side effects while maintaining recombination efficacy." | ( A review of tamoxifen administration regimen optimization for Cre/loxp system in mouse bone study. Bai, MR; Chen, MY; Chu, WL; Zhang, DM; Zhao, FL, 2023) | 1.58 |
Role | Description |
---|---|
antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
estrogen receptor antagonist | An antagonist at the estrogen receptor. |
bone density conservation agent | An agent that inhibits bone resorption and/or favor bone mineralization and bone regeneration. Used to heal bone fractures and to treat bone diseases such as osteopenia and osteoporosis. |
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. |
estrogen antagonist | A compound which inhibits or antagonises the biosynthesis or actions of estrogens. |
angiogenesis inhibitor | An agent and endogenous substances that antagonize or inhibit the development of new blood vessels. |
EC 2.7.11.13 (protein kinase C) inhibitor | An EC 2.7.11.* (protein-serine/threonine kinase) inhibitor that interferes with the action of protein kinase C (EC 2.7.11.13). |
EC 1.2.3.1 (aldehyde oxidase) inhibitor | An EC 1.2.3.* (oxidoreductase acting on donor aldehyde/oxo group with oxygen as acceptor) inhibitor which interferes with the action of aldehyde oxidase (EC 1.2.3.1). |
[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 |
---|---|
tertiary amino compound | A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups. |
stilbenoid | Any olefinic compound characterised by a 1,2-diphenylethylene backbone. |
[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] |
Pathway | Proteins | Compounds |
---|---|---|
Metabolism | 1496 | 1108 |
Biological oxidations | 150 | 276 |
Phase I - Functionalization of compounds | 69 | 175 |
FMO oxidises nucleophiles | 3 | 13 |
Tamoxifen Action Pathway | 10 | 27 |
Tamoxifen Metabolism Pathway | 10 | 27 |
Female steroid hormones in cardiomyocyte energy metabolism | 7 | 3 |
Integrated breast cancer pathway | 98 | 18 |
Tamoxifen metabolism | 0 | 13 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 5.0119 | 0.0447 | 17.8581 | 100.0000 | AID485294 |
Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 44.6684 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 25.2855 | 5.6234 | 17.2929 | 31.6228 | AID485281 |
acetylcholinesterase | Homo sapiens (human) | Potency | 62.9594 | 0.0025 | 41.7960 | 15,848.9004 | AID1347397; AID1347398 |
phosphopantetheinyl transferase | Bacillus subtilis | Potency | 51.0204 | 0.1413 | 37.9142 | 100.0000 | AID1490; AID2701 |
hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 45.9079 | 3.1890 | 29.8841 | 59.4836 | AID1224846; AID1224894 |
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 29.3618 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
SMAD family member 2 | Homo sapiens (human) | Potency | 59.3536 | 0.1737 | 34.3047 | 61.8120 | AID1346859; AID1346924; AID1347035 |
Fumarate hydratase | Homo sapiens (human) | Potency | 35.4813 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
USP1 protein, partial | Homo sapiens (human) | Potency | 59.6649 | 0.0316 | 37.5844 | 354.8130 | AID504865 |
PPM1D protein | Homo sapiens (human) | Potency | 30.0883 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
SMAD family member 3 | Homo sapiens (human) | Potency | 59.3536 | 0.1737 | 34.3047 | 61.8120 | AID1346859; AID1346924; AID1347035 |
TDP1 protein | Homo sapiens (human) | Potency | 24.2049 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
GLI family zinc finger 3 | Homo sapiens (human) | Potency | 20.8408 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 18.8541 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
AR protein | Homo sapiens (human) | Potency | 40.8203 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID743035; AID743036; AID743053; AID743063 |
apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 35.4813 | 0.7079 | 12.1943 | 39.8107 | AID720542 |
DNA polymerase III, partial | Bacillus subtilis | Potency | 29.9349 | 1.0621 | 14.1528 | 26.6795 | AID485295 |
caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 44.3017 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 54.2918 | 0.0006 | 57.9133 | 22,387.1992 | AID1259377; AID1259378; AID1259394 |
nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 68.6943 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224839; AID1224893 |
progesterone receptor | Homo sapiens (human) | Potency | 68.9104 | 0.0004 | 17.9460 | 75.1148 | AID1346784; AID1346795; AID1347036 |
regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 11.0180 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 27.9814 | 0.0002 | 14.3764 | 60.0339 | AID720691; AID720692; AID720719 |
retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 50.1910 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553; AID1159555 |
retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 38.6097 | 0.0008 | 17.5051 | 59.3239 | AID1159527; AID1159531 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 34.6528 | 0.0015 | 30.6073 | 15,848.9004 | AID1224819; AID1224820; AID1224821; AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403 |
farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 49.5924 | 0.3758 | 27.4851 | 61.6524 | AID743217; AID743220; AID743239 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 12.0215 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 21.1571 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID1259383; AID743069; AID743075; AID743077; AID743078; AID743079; AID743080; AID743091 |
polyprotein | Zika virus | Potency | 35.4813 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
67.9K protein | Vaccinia virus | Potency | 8.9125 | 0.0001 | 8.4406 | 100.0000 | AID720580 |
glucocerebrosidase | Homo sapiens (human) | Potency | 24.7028 | 0.0126 | 8.1569 | 44.6684 | AID2101 |
bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 35.4813 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 54.9410 | 0.0010 | 24.5048 | 61.6448 | AID743212; AID743227 |
peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 58.9321 | 0.0010 | 19.4141 | 70.9645 | AID743094; AID743140; AID743191 |
vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 61.6448 | 0.0237 | 23.2282 | 63.5986 | AID743222; AID743241 |
arylsulfatase A | Homo sapiens (human) | Potency | 5.3582 | 1.0691 | 13.9551 | 37.9330 | AID720538 |
caspase-3 | Homo sapiens (human) | Potency | 44.3017 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
IDH1 | Homo sapiens (human) | Potency | 16.3601 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 14.8149 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 6.0250 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 64.0875 | 0.0016 | 28.0151 | 77.1139 | AID1259385; AID1259395 |
activating transcription factor 6 | Homo sapiens (human) | Potency | 44.0538 | 0.1434 | 27.6121 | 59.8106 | AID1159516; AID1159519 |
thyrotropin-releasing hormone receptor | Homo sapiens (human) | Potency | 27.3185 | 0.1549 | 17.8702 | 43.6557 | AID1346877; AID1346891 |
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 26.7063 | 19.7391 | 45.9784 | 64.9432 | AID1159509; AID1159518 |
v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 20.5188 | 0.0578 | 21.1097 | 61.2679 | AID1159526; AID1159528 |
Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 46.0876 | 0.0391 | 47.5451 | 146.8240 | AID1224845; AID1224896 |
Caspase-7 | Cricetulus griseus (Chinese hamster) | Potency | 39.4839 | 0.0067 | 23.4960 | 68.5896 | AID1346980 |
cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 31.6228 | 0.0020 | 7.5337 | 39.8107 | AID891 |
NPC intracellular cholesterol transporter 1 precursor | Homo sapiens (human) | Potency | 58.0479 | 0.0126 | 2.4518 | 25.0177 | AID485313 |
cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 31.6228 | 0.3162 | 12.4435 | 31.6228 | AID902; AID924 |
D(1A) dopamine receptor | Homo sapiens (human) | Potency | 6.0200 | 0.0224 | 5.9449 | 22.3872 | AID488981; AID488982 |
vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 46.4852 | 0.3548 | 28.0659 | 89.1251 | AID504847 |
chromobox protein homolog 1 | Homo sapiens (human) | Potency | 37.6460 | 0.0060 | 26.1688 | 89.1251 | AID488953; AID540317 |
transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 11.2202 | 0.7943 | 21.2757 | 50.1187 | AID624246 |
caspase-3 | Cricetulus griseus (Chinese hamster) | Potency | 39.4839 | 0.0067 | 23.4960 | 68.5896 | AID1346980 |
thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 12.1259 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743066; AID743067 |
heat shock protein beta-1 | Homo sapiens (human) | Potency | 54.9410 | 0.0420 | 27.3789 | 61.6448 | AID743210; AID743228 |
ras-related protein Rab-9A | Homo sapiens (human) | Potency | 91.9997 | 0.0002 | 2.6215 | 31.4954 | AID485297 |
serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 18.4982 | 0.0037 | 8.6189 | 23.2809 | AID2660; AID2666; AID2667; AID2668 |
nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 35.6184 | 0.0006 | 27.2152 | 1,122.0200 | AID743202; AID743219 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 23.7359 | 0.0079 | 8.2332 | 1,122.0200 | AID2546; AID2551 |
geminin | Homo sapiens (human) | Potency | 7.1474 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 31.6228 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 21.1923 | 0.1778 | 24.7352 | 79.4328 | AID488949 |
lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 31.6228 | 0.0200 | 10.7869 | 31.6228 | AID912 |
Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 6.3096 | 0.3162 | 12.7657 | 31.6228 | AID881 |
Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 4.4302 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
Interferon beta | Homo sapiens (human) | Potency | 30.0883 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 61.9149 | 0.0023 | 19.5956 | 74.0614 | AID651631; AID720552 |
Integrin beta-3 | Homo sapiens (human) | Potency | 31.6228 | 0.3162 | 11.4157 | 31.6228 | AID924 |
Integrin alpha-IIb | Homo sapiens (human) | Potency | 31.6228 | 0.3162 | 11.4157 | 31.6228 | AID924 |
Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 4.4302 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Alpha-synuclein | Homo sapiens (human) | Potency | 18.3564 | 0.5623 | 9.3985 | 25.1189 | AID652106 |
Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 6.3096 | 0.0063 | 8.2350 | 39.8107 | AID881 |
D(1A) dopamine receptor | Sus scrofa (pig) | Potency | 14.6892 | 0.0037 | 8.1081 | 23.2809 | AID2667 |
Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1.0000 | 12.2248 | 31.6228 | AID885 |
Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1.0000 | 12.2248 | 31.6228 | AID885 |
GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1.0000 | 12.2248 | 31.6228 | AID885 |
ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 61.3172 | 0.0119 | 17.9420 | 71.5630 | AID651632 |
Ataxin-2 | Homo sapiens (human) | Potency | 48.3405 | 0.0119 | 12.2221 | 68.7989 | AID588378; AID651632 |
Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1.0000 | 12.2248 | 31.6228 | AID885 |
[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) |
---|---|---|---|---|---|---|---|
Chain A, CES1 protein | Homo sapiens (human) | Ki | 15.2000 | 15.2000 | 15.2000 | 15.2000 | AID977610 |
ubiquitin-conjugating enzyme E2 N | Homo sapiens (human) | IC50 (µMol) | 20.0000 | 0.8730 | 10.7219 | 78.4000 | AID493155 |
ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 0.6315 | 4.4531 | 9.3000 | AID1473740 |
Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 0.2000 | 5.6774 | 10.0000 | AID1473741 |
5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 0.4600 | 0.0001 | 1.0076 | 8.7800 | AID625218 |
5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | Ki | 0.2410 | 0.0000 | 0.8871 | 10.0000 | AID625218 |
Serine/threonine-protein kinase D3 | Homo sapiens (human) | IC50 (µMol) | 10.5000 | 0.0001 | 1.1701 | 10.0000 | AID1323681; AID1323683 |
Bile salt export pump | Homo sapiens (human) | IC50 (µMol) | 63.3400 | 0.1100 | 7.1903 | 10.0000 | AID1443980; AID1449628; AID1473738; AID681139; AID681155 |
Epidermal growth factor receptor | Homo sapiens (human) | IC50 (µMol) | 3.5530 | 0.0000 | 0.5369 | 10.0000 | AID625184 |
Estrogen receptor | Homo sapiens (human) | IC50 (µMol) | 1.1796 | 0.0000 | 0.7237 | 32.7000 | AID103082; AID103918; AID106081; AID1170537; AID1170541; AID1251780; AID1251781; AID1284373; AID1312680; AID1323680; AID1387887; AID1387894; AID1387905; AID1395069; AID1401995; AID1401998; AID1443551; AID1464221; AID1464224; AID1469717; AID1502305; AID1530767; AID1602141; AID1666649; AID1666654; AID1768138; AID1830575; AID242722; AID248083; AID248163; AID344797; AID392616; AID482351; AID677849; AID68743; AID68744; AID70337; AID70338; AID70341; AID70499; AID759306 |
Estrogen receptor | Homo sapiens (human) | Ki | 0.0586 | 0.0000 | 0.4229 | 7.9070 | AID497602; AID68902; AID68906; AID68910 |
Receptor tyrosine-protein kinase erbB-2 | Homo sapiens (human) | IC50 (µMol) | 2.9490 | 0.0001 | 0.5453 | 10.0000 | AID625186 |
Protein kinase C gamma type | Homo sapiens (human) | IC50 (µMol) | 10.5000 | 0.0001 | 1.0354 | 10.0000 | AID1323681; AID1323683 |
Protein kinase C alpha type | Rattus norvegicus (Norway rat) | IC50 (µMol) | 75.0000 | 0.0000 | 0.2193 | 1.0000 | AID1323682 |
Protein kinase C beta type | Homo sapiens (human) | IC50 (µMol) | 10.5000 | 0.0001 | 0.5542 | 10.0000 | AID1323681; AID1323683 |
Tyrosine-protein kinase Lck | Homo sapiens (human) | IC50 (µMol) | 8.0330 | 0.0002 | 1.3173 | 10.0000 | AID625187 |
Tyrosine-protein kinase Fyn | Homo sapiens (human) | IC50 (µMol) | 1.1950 | 0.0002 | 1.6789 | 8.6800 | AID625185 |
Progesterone receptor | Homo sapiens (human) | IC50 (µMol) | 50.0644 | 0.0000 | 0.5807 | 10.0000 | AID1251782; AID1251783 |
Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.4720 | 0.0004 | 1.8773 | 10.0000 | AID625207 |
Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | Ki | 1.4590 | 0.0032 | 2.2887 | 9.3160 | AID625207 |
Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | IC50 (µMol) | 7.7930 | 0.0000 | 1.2326 | 7.7930 | AID625152 |
Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Ki | 2.7710 | 0.0000 | 0.6902 | 10.0000 | AID625152 |
Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | IC50 (µMol) | 4.8170 | 0.0000 | 1.1546 | 7.5858 | AID625154 |
Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | Ki | 0.6720 | 0.0000 | 0.7951 | 9.1201 | AID625154 |
ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 (µMol) | 19.7250 | 0.0002 | 2.3185 | 10.0000 | AID679077; AID681126; AID681127; AID681131 |
ATP-dependent translocase ABCB1 | Homo sapiens (human) | Ki | 0.1000 | 0.0200 | 2.3594 | 8.5900 | AID150616 |
Beta-1 adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 17.2890 | 0.0002 | 1.4681 | 9.0000 | AID625204 |
Beta-1 adrenergic receptor | Homo sapiens (human) | Ki | 9.9840 | 0.0001 | 1.3391 | 9.9840 | AID625204 |
Cytochrome P450 3A4 | Homo sapiens (human) | Ki | 0.2000 | 0.0001 | 1.4162 | 9.9000 | AID589145 |
Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | IC50 (µMol) | 2.5850 | 0.0001 | 0.9917 | 8.0000 | AID625155 |
Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | Ki | 1.8570 | 0.0000 | 0.7292 | 6.9183 | AID625155 |
Alpha-2A adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 1.9350 | 0.0000 | 1.4421 | 7.3470 | AID625201 |
Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 0.7260 | 0.0001 | 0.8074 | 10.0000 | AID625201 |
Protein kinase C delta type | Rattus norvegicus (Norway rat) | IC50 (µMol) | 75.0000 | 0.0000 | 0.2585 | 1.0000 | AID1323682 |
Protein kinase C epsilon type | Rattus norvegicus (Norway rat) | IC50 (µMol) | 75.0000 | 0.0000 | 0.2585 | 1.0000 | AID1323682 |
Protein kinase C zeta type | Rattus norvegicus (Norway rat) | IC50 (µMol) | 75.0000 | 0.0000 | 0.2585 | 1.0000 | AID1323682 |
Polyunsaturated fatty acid 5-lipoxygenase | Homo sapiens (human) | Ki | 0.0845 | 0.0001 | 0.0304 | 0.1570 | AID68902; AID68906 |
Adenosine receptor A3 | Homo sapiens (human) | IC50 (µMol) | 3.7010 | 0.0000 | 1.8940 | 8.5470 | AID625196 |
Adenosine receptor A3 | Homo sapiens (human) | Ki | 2.0920 | 0.0000 | 0.9306 | 10.0000 | AID625196 |
Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | IC50 (µMol) | 2.8290 | 0.0000 | 1.4039 | 10.0000 | AID625151 |
Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | Ki | 0.6810 | 0.0000 | 0.5972 | 9.1201 | AID625151 |
Steroid hormone receptor ERR1 | Homo sapiens (human) | IC50 (µMol) | 0.2000 | 0.0020 | 1.1663 | 9.6400 | AID728186 |
Transcriptional activator protein LuxR | Aliivibrio fischeri | IC50 (µMol) | 40.0000 | 1.3600 | 3.2533 | 7.0000 | AID493958 |
Angiotensin-converting enzyme | Oryctolagus cuniculus (rabbit) | IC50 (µMol) | 0.9670 | 0.0000 | 1.6129 | 10.0000 | AID625171 |
Angiotensin-converting enzyme | Oryctolagus cuniculus (rabbit) | Ki | 0.7922 | 0.0004 | 2.0337 | 8.6606 | AID625171 |
Beta-3 adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 7.7030 | 0.0023 | 3.2415 | 8.0600 | AID625206 |
Beta-3 adrenergic receptor | Homo sapiens (human) | Ki | 5.7780 | 0.0030 | 2.3098 | 6.0450 | AID625206 |
D(2) dopamine receptor | Homo sapiens (human) | IC50 (µMol) | 13.8850 | 0.0000 | 0.7472 | 8.0000 | AID625253 |
D(2) dopamine receptor | Homo sapiens (human) | Ki | 4.6280 | 0.0000 | 0.6518 | 10.0000 | AID625253 |
Androgen receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 17.3423 | 0.0010 | 1.9794 | 14.1600 | AID255211; AID625228 |
Androgen receptor | Rattus norvegicus (Norway rat) | Ki | 15.1080 | 0.0003 | 1.2185 | 8.9270 | AID625228 |
Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 3.7010 | 0.0002 | 1.8742 | 10.0000 | AID625196 |
Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 2.0920 | 0.0001 | 0.9490 | 10.0000 | AID625196 |
Protein kinase C alpha type | Homo sapiens (human) | IC50 (µMol) | 10.5000 | 0.0001 | 0.9720 | 10.0000 | AID1323681; AID1323683 |
Alpha-2B adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 3.5180 | 0.0000 | 1.2380 | 8.1590 | AID625202 |
Alpha-2B adrenergic receptor | Homo sapiens (human) | Ki | 1.6060 | 0.0002 | 0.7257 | 10.0000 | AID625202 |
5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 12.1600 | 0.0003 | 1.3833 | 8.4000 | AID625190 |
5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | Ki | 6.9490 | 0.0001 | 0.7396 | 10.0000 | AID625190 |
Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | IC50 (µMol) | 2.9740 | 0.0001 | 1.0104 | 9.9280 | AID625153 |
Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | Ki | 0.6300 | 0.0000 | 0.5405 | 7.7600 | AID625153 |
Cytochrome P450 2B6 | Homo sapiens (human) | Ki | 0.9000 | 0.0004 | 1.4160 | 10.0000 | AID589238 |
Substance-K receptor | Homo sapiens (human) | IC50 (µMol) | 3.6700 | 0.0001 | 3.1210 | 9.5530 | AID625227 |
Substance-K receptor | Homo sapiens (human) | Ki | 1.2230 | 0.0001 | 1.9242 | 9.7930 | AID625227 |
D(1A) dopamine receptor | Homo sapiens (human) | IC50 (µMol) | 8.5020 | 0.0003 | 1.8473 | 9.2250 | AID625252 |
D(1A) dopamine receptor | Homo sapiens (human) | Ki | 4.2510 | 0.0001 | 0.8363 | 10.0000 | AID625252 |
D(4) dopamine receptor | Homo sapiens (human) | IC50 (µMol) | 11.1610 | 0.0001 | 1.1423 | 9.3280 | AID625255 |
D(4) dopamine receptor | Homo sapiens (human) | Ki | 3.9130 | 0.0000 | 0.4362 | 10.0000 | AID625255 |
Prostaglandin G/H synthase 1 | Homo sapiens (human) | IC50 (µMol) | 4.3910 | 0.0002 | 1.5574 | 10.0000 | AID625243 |
Sodium-dependent noradrenaline transporter | Homo sapiens (human) | IC50 (µMol) | 1.4720 | 0.0008 | 1.5416 | 20.0000 | AID625207 |
Sodium-dependent noradrenaline transporter | Homo sapiens (human) | Ki | 1.4590 | 0.0003 | 1.4656 | 10.0000 | AID625207 |
Thromboxane-A synthase | Homo sapiens (human) | IC50 (µMol) | 0.9160 | 0.0009 | 1.2304 | 10.0000 | AID625229 |
Protein kinase C eta type | Homo sapiens (human) | IC50 (µMol) | 10.5000 | 0.0001 | 0.7971 | 10.0000 | AID1323681; AID1323683 |
Histamine H2 receptor | Homo sapiens (human) | IC50 (µMol) | 9.3960 | 0.0220 | 2.2987 | 10.0000 | AID625270 |
Histamine H2 receptor | Homo sapiens (human) | Ki | 9.2400 | 0.0006 | 2.1973 | 10.0000 | AID625270 |
Alpha-1D adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 4.9820 | 0.0002 | 0.7568 | 8.8970 | AID625200 |
Alpha-1D adrenergic receptor | Homo sapiens (human) | Ki | 2.4490 | 0.0000 | 0.3609 | 10.0000 | AID625200 |
Substance-P receptor | Homo sapiens (human) | IC50 (µMol) | 15.6560 | 0.0000 | 0.0952 | 6.8130 | AID625226 |
Substance-P receptor | Homo sapiens (human) | Ki | 8.5400 | 0.0000 | 0.7936 | 8.7470 | AID625226 |
5-hydroxytryptamine receptor 2A | Homo sapiens (human) | IC50 (µMol) | 4.8010 | 0.0001 | 0.8801 | 8.8500 | AID625192 |
5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Ki | 1.3720 | 0.0000 | 0.3855 | 10.0000 | AID625192 |
5-hydroxytryptamine receptor 2C | Homo sapiens (human) | IC50 (µMol) | 0.4600 | 0.0001 | 1.0302 | 9.0000 | AID625218 |
5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 0.2410 | 0.0001 | 0.9549 | 10.0000 | AID625218 |
5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | IC50 (µMol) | 12.1600 | 0.0005 | 1.4835 | 7.8000 | AID625190 |
5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | Ki | 6.9490 | 0.0003 | 1.2967 | 9.2440 | AID625190 |
Adenosine receptor A2a | Homo sapiens (human) | IC50 (µMol) | 7.0990 | 0.0007 | 1.5594 | 10.0000 | AID625195 |
Adenosine receptor A2a | Homo sapiens (human) | Ki | 3.9850 | 0.0000 | 1.0609 | 9.7920 | AID625195 |
B2 bradykinin receptor | Homo sapiens (human) | IC50 (µMol) | 20.3560 | 0.0004 | 0.0212 | 0.2800 | AID625213 |
B2 bradykinin receptor | Homo sapiens (human) | Ki | 12.0480 | 0.0000 | 0.7057 | 7.6740 | AID625213 |
Adenosine receptor A1 | Homo sapiens (human) | IC50 (µMol) | 23.7670 | 0.0002 | 0.6818 | 7.7010 | AID625194 |
Adenosine receptor A1 | Homo sapiens (human) | Ki | 13.8640 | 0.0002 | 0.9316 | 10.0000 | AID625194 |
Sodium-dependent serotonin transporter | Homo sapiens (human) | IC50 (µMol) | 2.3340 | 0.0001 | 0.8645 | 8.7096 | AID625222 |
Sodium-dependent serotonin transporter | Homo sapiens (human) | Ki | 1.2400 | 0.0000 | 0.7048 | 8.1930 | AID625222 |
Melanocortin receptor 4 | Homo sapiens (human) | IC50 (µMol) | 30.4810 | 0.0002 | 0.6413 | 6.1900 | AID625148 |
Melanocortin receptor 4 | Homo sapiens (human) | Ki | 29.3080 | 0.0000 | 0.3086 | 4.8860 | AID625148 |
C-8 sterol isomerase | Saccharomyces cerevisiae S288C | Ki | 1.5000 | 0.0000 | 0.9048 | 7.1500 | AID239296 |
Melanocortin receptor 5 | Homo sapiens (human) | IC50 (µMol) | 26.5290 | 0.0009 | 1.2566 | 9.5180 | AID625149 |
Melanocortin receptor 5 | Homo sapiens (human) | Ki | 24.8860 | 0.0005 | 3.5265 | 8.9290 | AID625149 |
Mu-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 17.5940 | 0.0001 | 0.8133 | 10.0000 | AID625163 |
Mu-type opioid receptor | Homo sapiens (human) | Ki | 7.1420 | 0.0000 | 0.4197 | 10.0000 | AID625163 |
D(3) dopamine receptor | Homo sapiens (human) | IC50 (µMol) | 1.0720 | 0.0001 | 1.0178 | 8.7960 | AID625254 |
D(3) dopamine receptor | Homo sapiens (human) | Ki | 0.3640 | 0.0000 | 0.6020 | 10.0000 | AID625254 |
Delta-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 13.3390 | 0.0002 | 0.7521 | 8.0140 | AID625161 |
Delta-type opioid receptor | Homo sapiens (human) | Ki | 4.7020 | 0.0000 | 0.5978 | 9.9300 | AID625161 |
Kappa-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 15.6290 | 0.0000 | 1.2011 | 10.0000 | AID625162 |
Kappa-type opioid receptor | Homo sapiens (human) | Ki | 6.2520 | 0.0000 | 0.3624 | 10.0000 | AID625162 |
5-hydroxytryptamine receptor 2B | Homo sapiens (human) | IC50 (µMol) | 2.0840 | 0.0001 | 1.1873 | 8.9125 | AID625217 |
5-hydroxytryptamine receptor 2B | Homo sapiens (human) | Ki | 1.3260 | 0.0003 | 0.7693 | 10.0000 | AID625217 |
Protein kinase C iota type | Homo sapiens (human) | IC50 (µMol) | 10.5000 | 0.0001 | 2.0378 | 10.0000 | AID1323681; AID1323683 |
Melanocortin receptor 3 | Homo sapiens (human) | IC50 (µMol) | 19.8560 | 0.0012 | 0.0166 | 0.0832 | AID625147 |
Melanocortin receptor 3 | Homo sapiens (human) | Ki | 17.3290 | 0.0001 | 0.2452 | 2.8650 | AID625147 |
Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 3.7010 | 0.0000 | 1.8194 | 10.0000 | AID625196 |
Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 2.0920 | 0.0000 | 0.9650 | 10.0000 | AID625196 |
5-hydroxytryptamine receptor 6 | Homo sapiens (human) | IC50 (µMol) | 2.6790 | 0.0017 | 0.8381 | 5.4200 | AID625221 |
5-hydroxytryptamine receptor 6 | Homo sapiens (human) | Ki | 1.1425 | 0.0002 | 0.5229 | 10.0000 | AID625221; AID691260 |
Estrogen-related receptor gamma | Homo sapiens (human) | IC50 (µMol) | 0.0622 | 0.0020 | 0.2273 | 2.0000 | AID1464223 |
Protein kinase C gamma type | Rattus norvegicus (Norway rat) | IC50 (µMol) | 75.0000 | 0.0000 | 0.2640 | 1.1000 | AID1323682 |
Protein kinase C beta type | Rattus norvegicus (Norway rat) | IC50 (µMol) | 75.0000 | 0.0000 | 0.2164 | 1.1000 | AID1323682 |
Phospholipase D1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 20.0000 | 0.0110 | 0.3438 | 1.0000 | AID498481 |
Sodium-dependent dopamine transporter | Homo sapiens (human) | IC50 (µMol) | 1.8410 | 0.0007 | 1.8419 | 46.0000 | AID625256 |
Sodium-dependent dopamine transporter | Homo sapiens (human) | Ki | 1.4620 | 0.0002 | 1.1115 | 8.0280 | AID625256 |
Protein kinase C epsilon type | Homo sapiens (human) | IC50 (µMol) | 10.5000 | 0.0001 | 0.8029 | 10.0000 | AID1323681; AID1323683 |
Protein kinase C theta type | Homo sapiens (human) | IC50 (µMol) | 10.5000 | 0.0001 | 0.9897 | 10.0000 | AID1323681; AID1323683 |
Protein kinase C zeta type | Homo sapiens (human) | IC50 (µMol) | 10.5000 | 0.0001 | 2.4453 | 10.0000 | AID1323681; AID1323683 |
Protein kinase C delta type | Homo sapiens (human) | IC50 (µMol) | 10.5000 | 0.0001 | 0.8448 | 10.0000 | AID1323681; AID1323683 |
Serine/threonine-protein phosphatase 2B catalytic subunit alpha isoform | Homo sapiens (human) | IC50 (µMol) | 30.5730 | 0.0148 | 0.0989 | 0.1830 | AID625183 |
Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 1.2759 | 0.0009 | 1.9014 | 10.0000 | AID576612; AID625171 |
Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | Ki | 0.7922 | 0.0021 | 1.8407 | 10.0000 | AID625171 |
Platelet-activating factor acetylhydrolase | Homo sapiens (human) | IC50 (µMol) | 0.9040 | 0.0000 | 0.3837 | 3.9000 | AID103918 |
Phospholipase D1 | Homo sapiens (human) | IC50 (µMol) | 20.0000 | 0.0010 | 1.0656 | 8.5000 | AID1799396 |
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase | Homo sapiens (human) | IC50 (µMol) | 0.0120 | 0.0120 | 0.0120 | 0.0120 | AID38614 |
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase | Homo sapiens (human) | Ki | 0.0050 | 0.0004 | 0.5490 | 6.7000 | AID239597 |
Serine/threonine-protein kinase D1 | Homo sapiens (human) | IC50 (µMol) | 10.5000 | 0.0001 | 1.2319 | 10.0000 | AID1323681; AID1323683 |
Protein kinase C eta type | Rattus norvegicus (Norway rat) | IC50 (µMol) | 75.0000 | 0.0000 | 0.2585 | 1.0000 | AID1323682 |
Nuclear receptor subfamily 3 group C member 3 | Bos taurus (cattle) | IC50 (µMol) | 0.9670 | 0.1048 | 2.8398 | 8.3173 | AID625171 |
Nuclear receptor subfamily 3 group C member 3 | Bos taurus (cattle) | Ki | 0.7922 | 0.0858 | 2.9542 | 8.6606 | AID625171 |
Estrogen receptor beta | Homo sapiens (human) | IC50 (µMol) | 1.2790 | 0.0001 | 0.5294 | 32.7000 | AID103082; AID103918; AID106081; AID1170538; AID1170542; AID1284374; AID1387888; AID1387894; AID1387906; AID1464222; AID1464227; AID1666650; AID1666655; AID242704; AID248083; AID248163; AID344798; AID482348; AID677850; AID68744; AID70030; AID70337 |
Estrogen receptor beta | Homo sapiens (human) | Ki | 0.0510 | 0.0000 | 0.1251 | 2.8760 | AID669589; AID68902; AID68906; AID68910 |
Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 2.4100 | 6.3433 | 10.0000 | AID1473739 |
Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | IC50 (µMol) | 0.0210 | 0.0003 | 0.7028 | 5.3660 | AID625223 |
Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | Ki | 0.0219 | 0.0000 | 0.4901 | 10.0000 | AID239347; AID625223 |
Emopamil-binding protein-like | Homo sapiens (human) | Ki | 0.0028 | 0.0028 | 0.0033 | 0.0039 | AID723649 |
7-dehydrocholesterol reductase | Homo sapiens (human) | IC50 (µMol) | 0.0120 | 0.0120 | 0.0120 | 0.0120 | AID38614 |
Protein kinase C theta type | Rattus norvegicus (Norway rat) | IC50 (µMol) | 75.0000 | 0.0000 | 0.2585 | 1.0000 | AID1323682 |
[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) |
---|---|---|---|---|---|---|---|
Spike glycoprotein | Betacoronavirus England 1 | EC50 (µMol) | 51.4950 | 0.0030 | 4.5755 | 9.8200 | AID1804127 |
Replicase polyprotein 1ab | Betacoronavirus England 1 | EC50 (µMol) | 51.4950 | 0.0030 | 4.5755 | 9.8200 | AID1804127 |
streptokinase A precursor | Streptococcus pyogenes M1 GAS | EC50 (µMol) | 78.0860 | 0.0600 | 8.9128 | 130.5170 | AID1902; AID1914 |
Transmembrane protease serine 2 | Homo sapiens (human) | EC50 (µMol) | 51.4950 | 0.0030 | 4.5168 | 9.8200 | AID1804127 |
Estrogen receptor | Homo sapiens (human) | EC50 (µMol) | 1.1568 | 0.0000 | 0.5305 | 4.4000 | AID1797989; AID1797992; AID747466 |
Lysosomal acid glucosylceramidase | Homo sapiens (human) | EC50 (µMol) | 2.5000 | 2.5000 | 2.5000 | 2.5000 | AID1646801 |
Estrogen receptor | Rattus norvegicus (Norway rat) | EC50 (µMol) | 150.0000 | 0.0060 | 22.3670 | 130.5170 | AID1914 |
Procathepsin L | Homo sapiens (human) | EC50 (µMol) | 51.4950 | 0.0030 | 4.4874 | 9.8200 | AID1804127 |
ATP-dependent translocase ABCB1 | Homo sapiens (human) | EC50 (µMol) | 56.5000 | 0.0160 | 0.6786 | 3.1000 | AID407205 |
Replicase polyprotein 1a | Severe acute respiratory syndrome-related coronavirus | EC50 (µMol) | 51.4950 | 0.0030 | 4.6136 | 9.8200 | AID1804127 |
Replicase polyprotein 1ab | Human coronavirus 229E | EC50 (µMol) | 51.4950 | 0.0030 | 4.6136 | 9.8200 | AID1804127 |
Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | EC50 (µMol) | 51.4950 | 0.0030 | 4.4554 | 9.8200 | AID1804127 |
Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | EC50 (µMol) | 51.4950 | 0.0030 | 4.1105 | 9.8200 | AID1804127 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | EC50 (µMol) | 51.4950 | 0.0030 | 4.5755 | 9.8200 | AID1804127 |
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase | Homo sapiens (human) | Kd | 0.0010 | 0.0010 | 0.0010 | 0.0010 | AID38728 |
Estrogen receptor beta | Rattus norvegicus (Norway rat) | EC50 (µMol) | 150.0000 | 0.0060 | 22.3670 | 130.5170 | AID1914 |
Estrogen receptor beta | Homo sapiens (human) | EC50 (µMol) | 0.9808 | 0.0000 | 0.4795 | 4.8900 | AID1797989; AID1797992; AID747465 |
Angiotensin-converting enzyme 2 | Homo sapiens (human) | EC50 (µMol) | 51.4950 | 0.0030 | 4.5755 | 9.8200 | AID1804127 |
7-dehydrocholesterol reductase | Homo sapiens (human) | Kd | 0.0010 | 0.0010 | 0.0010 | 0.0010 | AID38728 |
[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) |
---|---|---|---|---|---|---|---|
interferon gamma precursor | Homo sapiens (human) | AC50 | 35.2400 | 0.1280 | 15.1730 | 38.6100 | AID1259418 |
Estrogen receptor | Homo sapiens (human) | DC50 | 0.0910 | 0.0001 | 0.0304 | 0.0910 | AID1768139 |
Estrogen receptor | Rattus norvegicus (Norway rat) | A50 | 0.0200 | 0.0200 | 0.0200 | 0.0200 | AID69358 |
UDP-glucuronosyltransferase 1A4 | Homo sapiens (human) | Km | 32.0000 | 7.0000 | 7.0000 | 7.0000 | AID624633 |
Estrogen receptor beta | Rattus norvegicus (Norway rat) | A50 | 0.0200 | 0.0200 | 0.0200 | 0.0200 | AID69358 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1346880 | Human Estrogen receptor-beta (3A. Estrogen receptors) | 1997 | Endocrinology, Mar, Volume: 138, Issue:3 | Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta. |
AID1345880 | Human GPER (G protein-coupled estrogen receptor) | 2005 | Endocrinology, Feb, Volume: 146, Issue:2 | Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells. |
AID1346845 | Human Estrogen receptor-alpha (3A. Estrogen receptors) | 1997 | Endocrinology, Mar, Volume: 138, Issue:3 | Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta. |
AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 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. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
AID1768143 | Intrinsic clearance in human hepatocytes measured up to 60 mins by LC/MS/MS analysis | |||
AID677850 | Antagonist activity at ERbeta receptor LBD expressed in yeast AH109 cells assessed as inhibition of interaction with SRC1 after 24 hrs by alpha-galactosidase assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Discovery and structure-activity analysis of selective estrogen receptor modulators via similarity-based virtual screening. |
AID678713 | Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID1284678 | Cytotoxicity against human MOLT4 cells assessed as growth inhibition after 48 hrs by SRB assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism. |
AID131085 | Uterotrophic effect in BDF1 mouse measured as([weight of uterus (mg)/body weight (g)] *100) | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Ring-substituted [1,2-bis(4-hydroxyphenyl)ethylenediamine]dichloroplatinum (II) complexes: compounds with a selective effect on the hormone-dependent mammary carcinoma. |
AID1567372 | Cytotoxicity against human SiHa cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Tetrazole hybrids with potential anticancer activity. |
AID1164493 | Antiproliferative activity human MIAPaCa2 cells after 2 days by MTT assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Development of new estradiol-cationic lipid hybrids: ten-carbon twin chain cationic lipid is a more suitable partner for estradiol to elicit better anticancer activity. |
AID759309 | Cytotoxicity against african green monkey Vero cells assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Histone deacetylase inhibitors equipped with estrogen receptor modulation activity. |
AID324585 | Increase in long-lived protein degradation in human H4 cells after 24 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48 | Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
AID588218 | FDA HLAED, lactate dehydrogenase (LDH) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
AID1471123 | Displacement of fluoromone from full length recombinant human estrogen receptor alpha expressed in Spodoptera frugiperda measured after 2 hrs by fluorescence polarization assay relative to estradiol | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Design, synthesis, biological evaluation and molecular docking studies of novel 3-aryl-4-anilino-2H-chromen-2-one derivatives targeting ERα as anti-breast cancer agents. |
AID1217708 | Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID1310519 | Induction of apoptosis in human HeLa cells assessed as viable cells at 50 uM after 28 hrs by annexin V/FITC/propidium iodide staining-based flow cytometry (Rvb = 95.3%) | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | 4-(1,2-diarylbut-1-en-1-yl)isobutyranilide derivatives as inhibitors of topoisomerase II. |
AID1366609 | Induction of necrosis in human MCF7 cells after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.51 +/- 0.21%) | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | Syntheses of conformationally restricted benzopyran based triarylethylenes as growth inhibitors of carcinoma cells. |
AID1705310 | Antiproliferative activity against human K562 cells assessed as growth inhibition at 10 uM relative to control | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors. |
AID1302506 | Inhibition of Set7/9 in human MCF7 cells assessed as suppression of beta-estradiol-induced pS2 mRNA expression at 3 to 10 uM preincubated for 18 hrs followed by beta-estradiol addition measured after 24 hrs by RT-PCR analysis | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Identification of Cyproheptadine as an Inhibitor of SET Domain Containing Lysine Methyltransferase 7/9 (Set7/9) That Regulates Estrogen-Dependent Transcription. |
AID1327718 | Anticancer activity against human DLD1 cells measured after 48 hrs by SRB assay | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21 | Synthesis of 3,5-dihydroxy-7,8-dimethoxy-2-(4-methoxyphenyl)benzopyran-4-one derivatives as anticancer agents. |
AID625284 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID567405 | Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Synthesis and in vitro anti-tumor activity of new oxadiazole thioglycosides. |
AID588217 | FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
AID597269 | Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10 | Biomimetic syntheses and antiproliferative activities of racemic, natural (-), and unnnatural (+) glyceollin I. |
AID561040 | Antifungal activity against Cryptococcus neoformans NYS2 assessed as disruption of cell wall integrity-associated adenylate kinase release at 64 ug/ml by hemocytometry | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization. |
AID1284726 | Cytotoxicity against human UO31 cells assessed as growth inhibition after 48 hrs by SRB assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism. |
AID101920 | Effect on [3H]-thymidine incorporation into estrogen receptor positive MCF-7 human breast carcinoma cells at 10e-6 M (exp 1) | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | 2-Phenylindoles. Effect of N-benzylation on estrogen receptor affinity, estrogenic properties, and mammary tumor inhibiting activity. |
AID191588 | The compound was tested for serum prolactin level in rats at 10 mg/kg dose after peroral administration | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec |
AID106453 | Cell growth inhibition of MXT-ER+ breast cancer cells at a dose of 8 mg | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Ring-substituted [1,2-bis(4-hydroxyphenyl)ethylenediamine]dichloroplatinum (II) complexes: compounds with a selective effect on the hormone-dependent mammary carcinoma. |
AID1312680 | Displacement of fluorescein-labeled estrogen ligand from recombinant ER-alpha (unknown origin) incubated for 2 hrs by fluorescence polarization assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents. |
AID1395719 | Cytotoxicity against human A549 cells preincubated for 4 hrs followed by incubation in compound free media for 24 hrs by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Antiproliferative efficacy of curcumin mimics through microtubule destabilization. |
AID498480 | Stimulation of human PLD1 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins by exogenous substrate assay | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2 | Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. |
AID1559016 | Antitumor activity against human MCF7:TAM1 cells xenografted in athymic nude mouse assessed as tumor regression at 100 mg/kg, po measured after 4 weeks | 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. |
AID70499 | Displacement of radioligand from Estrogen receptor alpha | 2002 | Bioorganic & medicinal chemistry letters, May-06, Volume: 12, Issue:9 | Synthesis of a novel fluorescent probe for estrogen receptor. |
AID1371164 | Aqueous solubility of the compound in PBS after 2 hrs by turbidimetric method | 2017 | Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9 | Investigating the Antibacterial Activity of Biphenylthiazoles against Methicillin- and Vancomycin-Resistant Staphylococcus aureus (MRSA and VRSA). |
AID184113 | Minimum effective dose at which significant increase in uterine weight/body weight in rat was determined (in vivo); expressed as % increase relative to ovariectomized (OVX) controls | 1997 | Journal of medicinal chemistry, Jan-17, Volume: 40, Issue:2 | Structure-activity relationships of selective estrogen receptor modulators: modifications to the 2-arylbenzothiophene core of raloxifene. |
AID503305 | Antiproliferative activity against human PC3 cells at 500 nM after 120 hrs by MTT assay relative to DMSO | 2006 | Nature chemical biology, Jun, Volume: 2, Issue:6 | Identifying off-target effects and hidden phenotypes of drugs in human cells. |
AID1209454 | Inactivation of CYP2B6 (unknown origin) expressed in Escherichia coli C41 DE3 cells assessed as tryptic peptide 188FHYQDQE194 with site of adduct formation localized to Gln193 at 100 uM after 30 mins by LC-MS/MS analysis in presence of NADPH | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12 | Bioactivation of the cancer chemopreventive agent tamoxifen to quinone methides by cytochrome P4502B6 and identification of the modified residue on the apoprotein. |
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AID1061211 | Inhibition of PGPH-like activity of human 20S proteasome beta 1 subunit assessed as hydrolysis of Z-LLE-AMC fluorogenic substrate at 10 uM measured for 1 hr by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | A novel tamoxifen derivative, ridaifen-F, is a nonpeptidic small-molecule proteasome inhibitor. |
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AID1530773 | Effect on progesterone receptor mRNA expression in non-stimulated human MCF7 cells at 1 uM by SYBR green dye based RT-PCR analysis | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2. |
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AID1693874 | Cytotoxicity against ER and PR-positive human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Synthesis, antitumor activity and structure-activity studies of novel pyridoxine-based bioisosteric analogs of estradiol. |
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AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
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AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
AID69535 | Relative binding affinity determined by displacement of [3H]estradiol relative to unlabeled estradiol | 1983 | Journal of medicinal chemistry, Aug, Volume: 26, Issue:8 | Tricyclic triarylethylene antiestrogens: dibenz[b,f]oxepins, dibenzo[b,f]thiepins, dibenzo[a,e]cyclooctenes, and dibenzo[b,f]thiocins. |
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AID1768149 | Distribution coefficient, logD of the compound at pH 7.4 | |||
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AID1705373 | Antiproliferative activity against human breast cancer cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors. |
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AID68897 | Antiproliferative activity against estrogen receptor positive MCF-7 human breast cancer cell line at 10e-9 M. (p<0.05) | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2 | Synthesis and biological evaluation of a series of 1,1-dichloro-2,2,3-triarylcyclopropanes as pure antiestrogens. |
AID102273 | Inhibition of [3H]thymidine incorporation into hormone sensitive MCF-7 human breast cancer cells at 10e-5 M | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity. |
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AID1233701 | Cytotoxicity against human MDA-MB-435S cells assessed as cell viability by MTT assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Synthesis and cancer cell growth inhibitory activity of icaritin derivatives. |
AID234090 | Selectivity for relative binding affinity against estrogen receptor at 2 hrs and 5 hr in calf uterus cytosol | 1989 | Journal of medicinal chemistry, Sep, Volume: 32, Issue:9 | Effect of triphenylacrylonitrile derivatives on estradiol-receptor binding and on human breast cancer cell growth. |
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AID324365 | Induction of light chain 3-GFP level in human H4 cells at 4.4 uM after 24 hrs by high throughput fluorescence microscopy relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48 | Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
AID1694959 | Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | 2020 | RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2 | Development of potent CPP6-gemcitabine conjugates against human prostate cancer cell line (PC-3). |
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AID282034 | Decrease in DOX-TEG-TAM uptake in MDA-MB-435 cells after 1 hr | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Antiestrogen binding site and estrogen receptor mediate uptake and distribution of 4-hydroxytamoxifen-targeted doxorubicin-formaldehyde conjugate in breast cancer cells. |
AID124178 | Uterine weight after 9 day treatment at 4.2 ug by oral gavage to ovariectomised mice without estrone | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14 | (S)-(+)-4-[7-(2,2-dimethyl-1-oxopropoxy)-4-methyl-2-[4-[2-(1-piperidinyl)-ethoxy]phenyl]-2H-1-benzopyran-3-yl]-phenyl 2,2-dimethylpropanoate (EM-800): a highly potent, specific, and orally active nonsteroidal antiestrogen. |
AID1666649 | Displacement of fluorescent estrogen ligand from recombinant human full length untagged ERalpha expressed in baculovirus infected insect cells incubated in dark for 2 hrs by Beacon single-tube fluorescent polarization assay | 2020 | Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5 | Optimisation of estrogen receptor subtype-selectivity of a 4-Aryl-4H-chromene scaffold previously identified by virtual screening. |
AID1251784 | Antiproliferative activity against human MCF7 cells | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20 | Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregu |
AID1666655 | Antagonist activity at ERbeta (unknown origin) | 2020 | Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5 | Optimisation of estrogen receptor subtype-selectivity of a 4-Aryl-4H-chromene scaffold previously identified by virtual screening. |
AID451833 | Displacement of [3H]estradiol from rat estrogen receptor by radiometric assay relative to estradiol | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | Synthesis and biological evaluation of 2,3,4-triarylbenzopyran derivatives as SERM and therapeutic agent for breast cancer. |
AID1356852 | Reduction in uterine wet weight in ethynyl estradiol-stimulated CD-IGS rat at 60 mg/kg, po dosed daily for 3 days by gavage followed 15 mins later by 0.1 mg/kg, po ethynyl estradiol and measured 24 hrs after last dose by immature rat uterine wet weight as | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer. |
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AID1662871 | Cytotoxicity against human MCF7 cells | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Design and synthesis of amphiphilic 2-hydroxybenzylphosphonium salts with antimicrobial and antitumor dual action. |
AID68895 | Antiproliferative activity against estrogen receptor positive MCF-7 human breast cancer cell line at a dose of 10e-7 M. (p<0.05) | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2 | Synthesis and biological evaluation of a series of 1,1-dichloro-2,2,3-triarylcyclopropanes as pure antiestrogens. |
AID497607 | Cytotoxicity against human MCF7 cells assessed as reduction of cell proliferation at 6 uM after 96 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15 | Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha. |
AID68910 | Apparent inhibition constant for estrogen receptor in Human uterine cytosol in 3.3%ethanol | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14 | (S)-(+)-4-[7-(2,2-dimethyl-1-oxopropoxy)-4-methyl-2-[4-[2-(1-piperidinyl)-ethoxy]phenyl]-2H-1-benzopyran-3-yl]-phenyl 2,2-dimethylpropanoate (EM-800): a highly potent, specific, and orally active nonsteroidal antiestrogen. |
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AID70482 | Inhibition of estrogen receptor alpha mediated transcriptional activation; Not determined | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands. |
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AID1666654 | Antagonist activity at ERalpha (unknown origin) | 2020 | Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5 | Optimisation of estrogen receptor subtype-selectivity of a 4-Aryl-4H-chromene scaffold previously identified by virtual screening. |
AID625292 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
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AID150616 | Concentration giving half of the maximal ATPase activity calculated for the high-affinity binding site of the CHO P-Glycoprotein (P-gp) in two-affinity model | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis). |
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AID695960 | Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21 | New prenylated isoflavonoids as protein tyrosine phosphatase 1B (PTP1B) inhibitors from Erythrina addisoniae. |
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AID455711 | Anticancer activity against human SKOV3 cells after 24 hrs by SRB assay | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | Application of the McMurry coupling reaction in the synthesis of tri- and tetra-arylethylene analogues as potential cancer chemotherapeutic agents. |
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AID70167 | Inhibition of estrogen receptor beta mediated transcriptional activation; Not determined | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands. |
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AID268619 | Agonist activity at ERalpha assessed as inhibition of E2-induced luciferase gene transactivation in MCF7 cells at >10 uM | 2006 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15 | m-Carborane bisphenol structure as a pharmacophore for selective estrogen receptor modulators. |
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AID497602 | Displacement of [2,4,6,7-3H]estradiol from human ERalpha expressed in HeLa cells after 18 hrs by liquid scintillation counting | 2010 | Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15 | Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha. |
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AID103375 | Effective concentration against MCF-7 breast tumor cells using MCF-7 assay. | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands. |
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AID667227 | Cytotoxicity against human 850C cells after 96 hrs by SRB assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis and biological evaluation of novel (E) stilbene-based antitumor agents. |
AID723806 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent. |
AID1502307 | Cytotoxicity in human Ishikawa cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Novel SERMs based on 3-aryl-4-aryloxy-2H-chromen-2-one skeleton - A possible way to dual ERα/VEGFR-2 ligands for treatment of breast cancer. |
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AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
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AID1158152 | Antiproliferative activity against human U937 cells after 24 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and anticancer activity of γ-(triazolyl ethylidene)butenolides and polyfunctional pyrrolinones. |
AID480630 | Displacement of [3H]estradiol from human ERbeta expressed in african green monkey COS1 cells assessed as relative binding affinity after 2 hrs by liquid scintillation counting relative to estradiol | 2010 | Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10 | Synthesis and biological evaluation of phenolic 4,5-dihydroisoxazoles and 3-hydroxy ketones as estrogen receptor alpha and beta agonists. |
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AID1772392 | Inhibition of Escherichia coli DNA gyrase at 100 uM by fluorescence based assay relative to control | |||
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AID71132 | Relative binding affinity was measured on calf uterus estrogen receptor after 5 hr at 25C. | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Multivariate analysis by the minimum spanning tree method of the structural determinants of diphenylethylenes and triphenylacrylonitriles implicated in estrogen receptor binding, protein kinase C activity, and MCF7 cell proliferation. |
AID678714 | Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID681588 | TP_TRANSPORTER: ATPase assay in membrane vesicle from BCRP-expressing Lactococcus lactis cells | 2003 | The Journal of biological chemistry, Jun-06, Volume: 278, Issue:23 | Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. |
AID723802 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent. |
AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
AID1693880 | Cytotoxicity against ER-negative human MDA-MB-231 cells assessed as reduction in colony formation incubated for 7 days by crystal violet staining based assay | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Synthesis, antitumor activity and structure-activity studies of novel pyridoxine-based bioisosteric analogs of estradiol. |
AID324577 | Effect on FYVE-RFP+ vesicle intensity per cell in human H4 cells after 4 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48 | Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
AID673829 | Cytotoxicity against human T47D cells after 5 days | 2012 | ACS medicinal chemistry letters, Apr-06, Volume: 3, Issue:5 | Boron-Based 4-Hydroxytamoxifen Bioisosteres for Treatment of de Novo Tamoxifen Resistant Breast Cancer. |
AID1545844 | Antiproliferative activity against human HeLa cells by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
AID38612 | Relative binding affinity for antiestrogen binding site (AEBS) of calf uterus 2 hr incubation at 0C | 1989 | Journal of medicinal chemistry, Sep, Volume: 32, Issue:9 | Effect of triphenylacrylonitrile derivatives on estradiol-receptor binding and on human breast cancer cell growth. |
AID759311 | Cytotoxicity against ERalpha-deficient human DU145 cells expressing ERbeta assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Histone deacetylase inhibitors equipped with estrogen receptor modulation activity. |
AID620853 | Effect on secondary structure of bovine serum albumin assessed as turn structure content at 0.5 uM at pH 7.4 by circular dichroism method (Rvb = 12 %) | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Locating the binding sites of anticancer tamoxifen and its metabolites 4-hydroxytamoxifen and endoxifen on bovine serum albumin. |
AID188612 | The compound was tested for the growth of tumors at 10 mg/kg dose start of the experiment after peroral administration (experiment-2) | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec |
AID324575 | Induction of autophagy in human H4 cells | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48 | Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
AID1310510 | Cytotoxicity against human OVCAR5 cells assessed as cell growth inhibition after 72 hrs by MTS assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | 4-(1,2-diarylbut-1-en-1-yl)isobutyranilide derivatives as inhibitors of topoisomerase II. |
AID1254844 | Selectivity index, ratio of IC50 for normal human astrocytes to IC50 for human GBM2 cells | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM). |
AID71148 | Displacement of 5 nM [3H]-estradiol from the estrogen receptor of MCF-7 whole cell lysates | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8 | Synthesis of 2-(p-chlorobenzyl)-3-aryl-6-methoxybenzofurans as selective ligands for antiestrogen-binding sites. Effects on cell proliferation and cholesterol synthesis. |
AID491954 | Cytotoxicity against human HepG2 cells after 24 hrs by CellTiter-BlueCell viability assay | 2010 | Journal of natural products, Jul-23, Volume: 73, Issue:7 | Mayamycin, a cytotoxic polyketide from a Streptomyces strain isolated from the marine sponge Halichondria panicea. |
AID1284375 | Selectivity ratio of IC50 for human ER-alpha to IC50 for human ER-beta | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism. |
AID344794 | Antiproliferative activity against hormone independent human MDA-MB-231 cells upto 100 nM after 72 hrs by MTT assay | 2008 | Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21 | Synthesis, biological evaluation, structural-activity relationship, and docking study for a series of benzoxepin-derived estrogen receptor modulators. |
AID68906 | Inhibition of estradiol binding to estrogen receptor in Human Breast cancer cytosol (3.3% ethanol) | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14 | (S)-(+)-4-[7-(2,2-dimethyl-1-oxopropoxy)-4-methyl-2-[4-[2-(1-piperidinyl)-ethoxy]phenyl]-2H-1-benzopyran-3-yl]-phenyl 2,2-dimethylpropanoate (EM-800): a highly potent, specific, and orally active nonsteroidal antiestrogen. |
AID471240 | Antagonist activity at estrogen receptor in human MCF7 cells assessed as 17-beta-estradiol-induced cell proliferation after 24 hrs by [14C]thymidine incorporation assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Identification and structure-activity relationships of chromene-derived selective estrogen receptor modulators for treatment of postmenopausal symptoms. |
AID620852 | Effect on secondary structure of bovine serum albumin assessed as beta-sheet content at 0.5 uM at pH 7.4 by circular dichroism method (Rvb = 16 %) | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Locating the binding sites of anticancer tamoxifen and its metabolites 4-hydroxytamoxifen and endoxifen on bovine serum albumin. |
AID1366597 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | Syntheses of conformationally restricted benzopyran based triarylethylenes as growth inhibitors of carcinoma cells. |
AID1705311 | Antiproliferative activity against human MOLT-4 cells assessed as growth inhibition at 10 uM relative to control | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors. |
AID561043 | Antifungal activity against Saccharomyces cerevisiae BY4741 expressing CMD1 at 62 to 125 ug/mL after 3 days by photographic analysis | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization. |
AID482354 | Selectivity ratio for ERalpha to ERbeta | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Discovery of potent ligands for estrogen receptor beta by structure-based virtual screening. |
AID1705361 | Antiproliferative activity against human BT-549 cells assessed as growth inhibition at 10 uM relative to control | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors. |
AID1628322 | Antiestrogenic activity in human T47D cells assessed as compound concentration required to decrease 100 pM E2-induced cell proliferation to equivalent levels induced by 1 pM E2 after 96 hrs by alamar blue assay | 2016 | Journal of natural products, 05-27, Volume: 79, Issue:5 | Furofuran Lignan Glucosides with Estrogen-Inhibitory Properties from the Bangladeshi Medicinal Plant Terminalia citrina. |
AID1254841 | Antiproliferative activity against human GBM2 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM). |
AID188611 | The compound was tested for the growth of tumors at 10 mg/kg dose finish of the experiment after peroral administration (experiment-2) | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec |
AID1686038 | Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 4 hrs by CellTiter-Glo assay | 2016 | Journal of medicinal chemistry, Oct-13, Volume: 59, Issue:19 | Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders. |
AID1518642 | Antiproliferative activity against human MCF7 cells by fluorescence based viable cell counting method | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | New 2,6-diaminopyridines containing a sterically hindered benzylphosphonate moiety in the aromatic core as potential antioxidant and anti-cancer drugs. |
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. |
AID1524896 | Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 24 hrs by resazurin dye based fluorimetric assay | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9 | Phosphonodiamidate prodrugs of N-alkoxy analogs of a fosmidomycin surrogate as antimalarial and antitubercular agents. |
AID103526 | Inhibition of estrogen receptor positive MCF-7 cell proliferation as cell number after 10 days at 10e-6 M | 1981 | Journal of medicinal chemistry, Oct, Volume: 24, Issue:10 | Potential antiestrogens. Synthesis and evaluation of mammary tumor inhibiting activity of 1,2-dialkyl-1,2-bis(3'-hydroxyphenyl)ethanes. |
AID1217729 | Intrinsic clearance for reactive metabolites formation assessed as summation of [3H]GSH adduct formation rate-based reactive metabolites formation and cytochrome P450 (unknown origin) inactivation rate-based reactive metabolites formation | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID1693882 | Selectivity index, ratio of IC50 for inhibition of colony formation in ER-negative human MDA-MB-231 cells to IC50 for inhibition of colony formation in ER and PR-positive human MCF7 cells | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Synthesis, antitumor activity and structure-activity studies of novel pyridoxine-based bioisosteric analogs of estradiol. |
AID69514 | Relative binding affinity(RBA) against estrogen (ER) in rat liver | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8 | Synthesis of 2-(p-chlorobenzyl)-3-aryl-6-methoxybenzofurans as selective ligands for antiestrogen-binding sites. Effects on cell proliferation and cholesterol synthesis. |
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. |
AID1705321 | Antiproliferative activity against human NCI-H522 cells assessed as growth inhibition at 10 uM relative to control | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors. |
AID1193494 | Thermodynamic equilibrium solubility, log S of the compound in simulated gastric fluid at pH 1.2 at RT after 4 hrs by 96 well plate method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID191676 | Uterotrophic effect in rats uterine at 1 ug/day dose | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent. |
AID1660979 | Inhibition of Escherichia coli shiga toxin | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Structure-Activity Relationship Studies of Retro-1 Analogues against Shiga Toxin. |
AID239347 | Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening. |
AID1688066 | Antiproliferative activity against human MCF-7 cells assessed as proportion of dead cells at 1.07 ug/ml measured after 3 weeks by crystal violet staining based soft agar colony formation assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition. |
AID1471126 | Antiproliferative activity against human Ishikawa cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Design, synthesis, biological evaluation and molecular docking studies of novel 3-aryl-4-anilino-2H-chromen-2-one derivatives targeting ERα as anti-breast cancer agents. |
AID491597 | Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13 | Synthesis and anti breast cancer activity of biphenyl based chalcones. |
AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
AID728186 | Antagonist activity at ERalpha receptor in human MCF7 cells assessed as inhibition of cell growth after 6 days by crystal violet staining method | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7 | Synthesis of novel estrogen receptor antagonists using metal-catalyzed coupling reactions and characterization of their biological activity. |
AID103535 | Inhibition of estrogen receptor positive MCF-7 cell proliferation as cell number after 10 days at 10e-8 M | 1981 | Journal of medicinal chemistry, Oct, Volume: 24, Issue:10 | Potential antiestrogens. Synthesis and evaluation of mammary tumor inhibiting activity of 1,2-dialkyl-1,2-bis(3'-hydroxyphenyl)ethanes. |
AID1833429 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay | |||
AID243422 | log (1/Km) value for human liver microsome cytochrome P450 3A4 | 2005 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18 | Modeling K(m) values using electrotopological state: substrates for cytochrome P450 3A4-mediated metabolism. |
AID1158153 | Cytotoxicity against human HEK293 cells after 24 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and anticancer activity of γ-(triazolyl ethylidene)butenolides and polyfunctional pyrrolinones. |
AID227718 | Binding energy by using the equation deltaG obsd = -RT ln KD | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Functional group contributions to drug-receptor interactions. |
AID1833412 | Toxicity in Sprague-Dawley rat inoculated with rat LA7 cells assessed as increase in uterine tissue at 10 mg/kg administered daily for 21 days | |||
AID1530771 | Stimulation of cell proliferation in human Ishikawa cells at 1 to 10 uM after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2. |
AID1465924 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability at 5 uM after 24 hrs by MTT assay relative to control | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Structural Basis of Inhibition of ERα-Coactivator Interaction by High-Affinity N-Terminus Isoaspartic Acid Tethered Helical Peptides. |
AID344802 | Antiestrogenic activity in human Ishikawa cells assessed as inhibition of estrogen-induced alkaline phosphatase activity after 72 hrs | 2008 | Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21 | Synthesis, biological evaluation, structural-activity relationship, and docking study for a series of benzoxepin-derived estrogen receptor modulators. |
AID124168 | Uterine weight after 9 day treatment at 0.42 ug by oral gavage to ovariectomised mice with estrone | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14 | (S)-(+)-4-[7-(2,2-dimethyl-1-oxopropoxy)-4-methyl-2-[4-[2-(1-piperidinyl)-ethoxy]phenyl]-2H-1-benzopyran-3-yl]-phenyl 2,2-dimethylpropanoate (EM-800): a highly potent, specific, and orally active nonsteroidal antiestrogen. |
AID548941 | Growth inhibition of human MCF7 cells at 50 ug/ml after 24 hrs by MTT colorimetric assay | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Isochaihulactone analogues: synthesis and anti-proliferative activity of novel dibenzylbutyrolactones. |
AID1530774 | Antagonist activity at ERalpha in human MCF7 cells assessed as reduction in E2-induced progesterone receptor mRNA expression at 1 uM by SYBR green dye based RT-PCR method | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2. |
AID102757 | Effect on hormone-dependent MCF-7 human breast cancer cell proliferation at 1x10E-6M | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Indolo[2,1-a]isoquinolines. Syntheses, steroid hormone receptor binding affinities, and cytostatic activity. |
AID781329 | pKa (acid-base dissociation constant) as determined by other workers | 2014 | Pharmaceutical research, Apr, Volume: 31, Issue:4 | Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds. |
AID1348843 | Growth inhibition of human MCF7 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | New estrogen receptor antagonists. 3,20-Dihydroxy-19-norpregna-1,3,5(10)-trienes: Synthesis, molecular modeling, and biological evaluation. |
AID678716 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID1578359 | Antimycobacterial activity activity against Mycobacterium tuberculosis H37Rv after 7 days by rezasurin-dye based spectrophotometric analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Novel thiazolidinedione-hydroxamates as inhibitors of Mycobacterium tuberculosis virulence factor Zmp1. |
AID1754977 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Design, synthesis and broad spectrum antibreast cancer activity of diarylindoles via induction of apoptosis in aggressive breast cancer cells. |
AID491600 | Cytotoxicity against HEK293 cells after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13 | Synthesis and anti breast cancer activity of biphenyl based chalcones. |
AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
AID1310518 | Induction of apoptosis in human HeLa cells assessed as early apoptotic cells at 50 uM after 28 hrs by annexin V/FITC/propidium iodide staining-based flow cytometry (Rvb = 2.6%) | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | 4-(1,2-diarylbut-1-en-1-yl)isobutyranilide derivatives as inhibitors of topoisomerase II. |
AID643383 | Induction of phospholipidosis in bovine corneal fibroblasts assessed as lamellar inclusion bodies after 72 hrs by light microscopy | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | In silico assay for assessing phospholipidosis potential of small druglike molecules: training, validation, and refinement using several data sets. |
AID103745 | Inhibition of [3H]thymidine incorporation into MCF-7 cells | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8 | Synthesis of 2-(p-chlorobenzyl)-3-aryl-6-methoxybenzofurans as selective ligands for antiestrogen-binding sites. Effects on cell proliferation and cholesterol synthesis. |
AID188737 | The compound was tested for the progression of no of tumors at 10 mg/kg dose after peroral administration (experiment-2) | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec |
AID302174 | Antiproliferative activity against human HL60 cells assessed as cell viability after 4 hrs by MTT assay | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | An expeditious synthesis of tamoxifen, a representative SERM (selective estrogen receptor modulator), via the three-component coupling reaction among aromatic aldehyde, cinnamyltrimethylsilane, and beta-chlorophenetole. |
AID681126 | TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells | 2001 | Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2 | Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. |
AID191680 | Uterotrophic effect in rats uterine at 10 ug/day dose in presence of 0.16 ug estradiol | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent. |
AID136040 | Relative tumor weight in treated compared to control mice bearing hormone-dependent transplanted MXT mammary tumors at 8.8mg | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | 2-Phenylindole-linked [2-(aminoalkyl)pyridine]dichloroplatinum(II): complexes with a selective action on estrogen receptor positive mammary tumors. |
AID398078 | Displacement of [3H]estradiol form ERalpha in rat uterine cytosol after 22 hrs by charcol adsorption method relative to 17-beta-estradiol | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | Synthesis and biological evaluation of 3,4,6-triaryl-2-pyranones as a potential new class of anti-breast cancer agents. |
AID470168 | Antiestrogenic activity in human T47D cells assessed as drug level causing inhibition of 100 pM E2-enhanced cell proliferation to level equivalent to 1 pM E2 after 96 hrs by alamar blue assay | 2009 | Journal of natural products, Nov, Volume: 72, Issue:11 | Antiestrogenic constituents of the Thai medicinal plants Capparis flavicans and Vitex glabrata. |
AID1401998 | Inhibition of estrogen receptor (unknown origin) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Tamoxifen a pioneering drug: An update on the therapeutic potential of tamoxifen derivatives. |
AID103267 | Inhibition of estrogen-induced proliferation in human MCF-7 breast cancer cells | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10 | Discovery and synthesis of [6-hydroxy-3-[4-[2-(1-piperidinyl)ethoxy]phenoxy]-2-(4-hydroxyphenyl)]b enzo[b]thiophene: a novel, highly potent, selective estrogen receptor modulator. |
AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
AID1366607 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 10 uM after 24 to 48 hrs by propidium iodide staining based flow cytometry (Rvb = 10.68 +/- 0.23%) | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | Syntheses of conformationally restricted benzopyran based triarylethylenes as growth inhibitors of carcinoma cells. |
AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
AID1348845 | Growth inhibition of human MCF10A cells at <25 uM after 72 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | New estrogen receptor antagonists. 3,20-Dihydroxy-19-norpregna-1,3,5(10)-trienes: Synthesis, molecular modeling, and biological evaluation. |
AID1323680 | Displacement of Fluormone ES2 Green from human recombinant full length ERalpha expressed in insect cells measured up to 4 hrs by fluorescence polarization assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Design and synthesis of triarylacrylonitrile analogues of tamoxifen with improved binding selectivity to protein kinase C. |
AID1530769 | Antiproliferative activity against HUVEC after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2. |
AID176940 | Dose required to reduce serum cholesterol by 50% relative to OVX controls was determined (in vivo) | 1997 | Journal of medicinal chemistry, Jan-17, Volume: 40, Issue:2 | Structure-activity relationships of selective estrogen receptor modulators: modifications to the 2-arylbenzothiophene core of raloxifene. |
AID540237 | Phospholipidosis-positive literature compound observed in rat | |||
AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
AID561227 | Antifungal activity against Candida dubliniensis CD1 after 24 hrs by CLSI method | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization. |
AID1688053 | Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 48 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition. |
AID1140199 | Displacement of fluorescent estrogen from recombinant ERalpha (unknown origin) at 0.1 mg/ml by competition binding assay | 2014 | Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9 | Synthesis and biological evaluation of 2,3-diaryl isoquinolinone derivatives as anti-breast cancer agents targeting ERα and VEGFR-2. |
AID1323678 | Inhibition of PKC in human SH-SY5Y cells assessed as inhibition of PMA-stimulated MARCKS phosphorylation at 3 uM preincubated for 1 hr followed by PMA-stimulation for 15 mins by Western blot analysis relative to control | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Design and synthesis of triarylacrylonitrile analogues of tamoxifen with improved binding selectivity to protein kinase C. |
AID184853 | Minimally effective dose(MED) (mg/kg body weight) at which a statistically significant (p<= 0.05) increase in uterine weight/body weight was observed | 1998 | Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8 | Synthesis and pharmacology of conformationally restricted raloxifene analogues: highly potent selective estrogen receptor modulators. |
AID1705312 | Antiproliferative activity against human RPMI-8226 cells assessed as growth inhibition at 10 uM relative to control | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors. |
AID548942 | Growth inhibition of human T47D cells at 25 ug/ml after 24 hrs by MTT colorimetric assay | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Isochaihulactone analogues: synthesis and anti-proliferative activity of novel dibenzylbutyrolactones. |
AID1693876 | Cytotoxicity against human HSF cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Synthesis, antitumor activity and structure-activity studies of novel pyridoxine-based bioisosteric analogs of estradiol. |
AID1530767 | Displacement of fluorescent estrogen ligand from recombinant human full length untagged ERalpha expressed in Spodoptera frugiperda insect cells measured after 2 hrs by fluorescence polarization assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2. |
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AID681613 | TP_TRANSPORTER: intracellular accumulation in MDR1-expressing LLC-PK1 cells | 2000 | Molecular pharmacology, Jan, Volume: 57, Issue:1 | Cloning and expression of murine sister of P-glycoprotein reveals a more discriminating transporter than MDR1/P-glycoprotein. |
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AID1545837 | Cytotoxicity against HEK293 cells by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
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AID101601 | Inhibition of estrogen receptor positive MCF-7 breast cancer cell proliferation | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Design, synthesis, and biological evaluation of doxorubicin-formaldehyde conjugates targeted to breast cancer cells. |
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AID1705332 | Antiproliferative activity against human SNB-75 cells assessed as growth inhibition at 10 uM relative to control | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors. |
AID1387898 | Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length estrogen receptor beta after 2 hrs by fluorescence polarization assay relative to estradiol | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2 | Lead Optimization of Benzoxepin-Type Selective Estrogen Receptor (ER) Modulators and Downregulators with Subtype-Specific ERα and ERβ Activity. |
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AID765189 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Design, synthesis, and anti-tumor activities of novel triphenylethylene-coumarin hybrids, and their interactions with Ct-DNA. |
AID1170538 | Displacement of fluorescein-labeled estrogen from human recombinant ERbeta by fluorescence polarization based competitive binding affinity assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | β-Lactam estrogen receptor antagonists and a dual-targeting estrogen receptor/tubulin ligand. |
AID103083 | Inhibition of MCF-7 cell proliferation at 5 uM | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | Antiestrogenically active 1,1,2-tris(4-hydroxyphenyl)alkenes without basic side chain: synthesis and biological activity. |
AID188603 | The compound was tested for no of tumors with partial remission at 10 mg/kg dose after peroral administration (experiment-2) | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec |
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. |
AID678554 | Cytotoxicity against human MCF7 cells after 72 hrs by WST1 assay in presence of 20% FBS | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Synthesis and cytotoxic activity of non-naturally substituted 4-oxycoumarin derivatives. |
AID628346 | Antiestrogenic activity in human ER-positive MCF7 cells assessed as inhibition of 17beta estradiol-induced secreted alkaline phosphatase activity at 20 nM after 48 hrs by phospha-light reporter chemiluminescence assay | 2011 | Journal of natural products, Aug-26, Volume: 74, Issue:8 | Using the pER8:GUS reporter system to screen for phytoestrogens from Caesalpinia sappan. |
AID106463 | Median tumor weight of MXT ER+ (mammary carcinoma) determined at the end of 6 week therapy at a dose of 8 mg | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Ring-substituted [1,2-bis(4-hydroxyphenyl)ethylenediamine]dichloroplatinum (II) complexes: compounds with a selective effect on the hormone-dependent mammary carcinoma. |
AID26936 | Dissociation constant was evaluated. | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent. |
AID69366 | Relative binding affinity against estrogen receptor in whole cell assay | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Synthesis and estrogen receptor binding of 6,7-dihydro-8-phenyl-9-[4-[2-(dimethylamino)ethoxy] phenyl]-5H-benzocycloheptene, a nonisomerizable analogue of tamoxifen. X-ray crystallographic studies. |
AID1069846 | Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis of neolignans as microtubule stabilisers. |
AID374714 | Cytotoxicity against estrogen receptor deficient human SKBR3 cells overexpressing human epidermal growth factor receptor 2 after 72 hrs by SRB assay | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11 | Antitumor agents. 266. Design, synthesis, and biological evaluation of novel 2-(furan-2-yl)naphthalen-1-ol derivatives as potent and selective antibreast cancer agents. |
AID1424439 | Induction of apoptosis in human MCF7 cells incubated for 24 hrs by flow cytometry | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | From the hive: Honey, a novel weapon against cancer. |
AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
AID270141 | Cytotoxicity against human MDA-MB-231 cells lacking ER | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Antitumor agents. 254. Synthesis and biological evaluation of novel neo-tanshinlactone analogues as potent anti-breast cancer agents. |
AID191698 | Uterotrophic effect in rats uterine at 50 ug/day dose in the presence of 0.5 ug hexestrol | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent. |
AID1251782 | Agonist activity at progesterone receptor in human MCF7 cells | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20 | Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregu |
AID70337 | Inhibition of [3H]E2 binding to estrogen receptor alpha in MCF-7 cell lysate | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Design, synthesis, and biological evaluation of doxorubicin-formaldehyde conjugates targeted to breast cancer cells. |
AID561218 | Antifungal activity against Saccharomyces cerevisiae BY4741 assessed as inhibition fungal bud formation at 8 ug/ml | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization. |
AID1327721 | Anticancer activity against human FADU cells measured after 48 hrs by SRB assay | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21 | Synthesis of 3,5-dihydroxy-7,8-dimethoxy-2-(4-methoxyphenyl)benzopyran-4-one derivatives as anticancer agents. |
AID669589 | Displacement of [3H]estradiol from ERbeta after 4 hrs by scintillation counting | 2012 | ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3 | Hydrophobic Interactions Improve Selectivity to ERα for Ben-zothiophene SERMs. |
AID437140 | Cytotoxicity against HEK293 cells after 18 hrs by MTT assay | 2009 | European journal of medicinal chemistry, Oct, Volume: 44, Issue:10 | In vitro and in vivo anticancer activity of 2-deacetoxytaxinine J and synthesis of novel taxoids and their in vitro anticancer activity. |
AID101645 | Effect on [3H]-thymidine incorporation into MDA-MB 231 human breast cancer cells at 1x10E-6M | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Indolo[2,1-a]isoquinolines. Syntheses, steroid hormone receptor binding affinities, and cytostatic activity. |
AID104076 | In vitro cytotoxicity against hormone-responsive MCF-7 cell line. | 1995 | Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2 | Rationally designed analogues of tamoxifen with improved calmodulin antagonism. |
AID164972 | Percent stimulation or inhibition of protein kinase C III activity for protamine sulfate in the presence of EGTA. | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Multivariate analysis by the minimum spanning tree method of the structural determinants of diphenylethylenes and triphenylacrylonitriles implicated in estrogen receptor binding, protein kinase C activity, and MCF7 cell proliferation. |
AID68739 | Estrogenic activity in MCF-7-2a cells as percent activation of 10e-8 M estradiol | 2002 | Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24 | Investigations on estrogen receptor binding. The estrogenic, antiestrogenic, and cytotoxic properties of C2-alkyl-substituted 1,1-bis(4-hydroxyphenyl)-2-phenylethenes. |
AID470163 | Antiestrogenic activity in human MCF7 cells assessed as drug level causing inhibition of 100 pM E2-enhanced cell proliferation to level equivalent to 50 pM E2 after 96 hrs by alamar blue assay | 2009 | Journal of natural products, Nov, Volume: 72, Issue:11 | Antiestrogenic constituents of the Thai medicinal plants Capparis flavicans and Vitex glabrata. |
AID493960 | Inhibition of LuxR-dependent quorum sensing in Vibrio fischeri assessed as reduction of 3-oxo-C6-HSL-induced bioluminescence intensity at 40 uM | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | LuxR-dependent quorum sensing: computer aided discovery of new inhibitors structurally unrelated to N-acylhomoserine lactones. |
AID186917 | The compound was tested for anti-uterotrophic activity in immature rats(Dosage 1000 ug) | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec |
AID242378 | Inhibition of [3H]estradiol binding to human estrogen receptor alpha expressed in HeLa cells; not determined | 2005 | Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2 | Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands. |
AID134367 | In vitro estrogenic effect in immature mice at 10 ug | 1986 | Journal of medicinal chemistry, Aug, Volume: 29, Issue:8 | Catechol estrogens of the 1,1,2-triphenylbut-1-ene type: relationship between structure, estradiol receptor affinity, estrogenic and antiestrogenic properties, and mammary tumor inhibiting activities. |
AID723800 | Antiproliferative activity against mouse fibroblasts after 48 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent. |
AID1217709 | Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID1768145 | Clearance in Sprague-Dawley rat at 1 mg/kg, iv or po measured after 0.033 to 24 hrs by LC/MS/MS analysis | |||
AID1646805 | Metabolic stability in human liver microsomes assessed as half life | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 | Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells. |
AID1061217 | Inhibition of chymotrypsin-like activity of human 20S proteasome beta 5 subunit assessed as hydrolysis of succinyl-LLVY-AMC fluorogenic substrate at 10 uM measured for 1 hr by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | A novel tamoxifen derivative, ridaifen-F, is a nonpeptidic small-molecule proteasome inhibitor. |
AID620851 | Effect on secondary structure of bovine serum albumin assessed as beta antiparallel content at 0.5 uM at pH 7.4 by circular dichroism method (Rvb = 3 %) | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Locating the binding sites of anticancer tamoxifen and its metabolites 4-hydroxytamoxifen and endoxifen on bovine serum albumin. |
AID1545836 | Antiproliferative activity against human MDA-MB-231 cells by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
AID392616 | Antiestrogenic activity in human T47D cells expressing estrogen receptor assessed as estrogen-dependent transcription by luciferase reporter gene assay | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4 | N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1). |
AID1464226 | Agonist activity at full length ERalpha (unknown origin) expressed in human HeLa cells incubated for 24 hrs by ERE-driven luciferase reporter gene assay | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Design and synthesis of benzoacridines as estrogenic and anti-estrogenic agents. |
AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID186918 | The compound was tested for anti-uterotrophic activity in immature rats(Dosage 100 ug) | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec |
AID1705347 | Antiproliferative activity against human NCI/ADR-RES cells assessed as growth inhibition at 10 uM relative to control | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors. |
AID1277627 | Antiproliferative activity against human BxPC3 cells assessed as cell viability at 10 uM after 48 hrs by MTS assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Identification of initial leads directed at the calmodulin-binding region on the Src-SH2 domain that exhibit anti-proliferation activity against pancreatic cancer. |
AID187053 | The compound was tested for uterotropic activity in immature rats(Dosage 10 ug) | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec |
AID1688068 | Antiproliferative activity against human MCF-7 cells assessed as proportion of dead cells at 26.95 ug/ml measured after 3 weeks by crystal violet staining based soft agar colony formation assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition. |
AID191677 | Uterotrophic effect in rats uterine at 1 ug/day dose in presence of estradiol | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent. |
AID480631 | Selectivity ratio of relative binding affinity for human ERalpha to relative binding affinity for human ERbeta | 2010 | Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10 | Synthesis and biological evaluation of phenolic 4,5-dihydroisoxazoles and 3-hydroxy ketones as estrogen receptor alpha and beta agonists. |
AID172431 | Change in DMBA-induced mammary tumor area in rats after 28 day therapy at 3 mg dose (experiment-1) | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity. |
AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
AID1545842 | Antiproliferative activity against human A549 cells by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
AID1284733 | Cytotoxicity against human T47D cells assessed as growth inhibition after 48 hrs by SRB assay | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism. |
AID134364 | Antiestrogenic effect in immature mouse at a dose of 25 ug. | 1986 | Journal of medicinal chemistry, Aug, Volume: 29, Issue:8 | Catechol estrogens of the 1,1,2-triphenylbut-1-ene type: relationship between structure, estradiol receptor affinity, estrogenic and antiestrogenic properties, and mammary tumor inhibiting activities. |
AID187687 | Final tumor number in DMBA-induced tumor bearing rats at 3 mg dose (experiment-1) | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity. |
AID501531 | Antagonist activity at human wild type ERalpha expressed in human HeLa cells co-expressing ERE assessed as inhibition of transactivation activity by luciferase reporter gene assay | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | A mutant selective anti-estrogen is a pure antagonist on EREs and AP-1 response elements. |
AID1866705 | Antiproliferative activity against human MCF7 cells assessed as cell viability after 24 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 64 | Rational design, synthesis, antiproliferative activity against MCF-7, MDA-MB-231 cells, estrogen receptors binding affinity, and computational study of indenopyrimidine-2,5-dione analogs for the treatment of breast cancer. |
AID1312622 | Antiproliferative activity against human PC3 cells | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Recent developments of C-4 substituted coumarin derivatives as anticancer agents. |
AID699539 | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID1350706 | Apparent permeability cross basolateral to apical side in MDCK-MDR1 cells at 5 uM after 90 mins by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14 | Optimization of Isothiazolo[4,3- b]pyridine-Based Inhibitors of Cyclin G Associated Kinase (GAK) with Broad-Spectrum Antiviral Activity. |
AID1636506 | Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 27.5 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of N | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
AID1164495 | Antiproliferative activity mouse NIH/3T3 cells after 2 days by MTT assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Development of new estradiol-cationic lipid hybrids: ten-carbon twin chain cationic lipid is a more suitable partner for estradiol to elicit better anticancer activity. |
AID1129457 | Solubility of the compound in PBS buffer after 16 hrs | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors. |
AID1534873 | Binding affinity to rRNA-A site in human MDA-MB-231 cells assessed as inhibition of protein translation | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Synthesis, antimicrobial activity, attenuation of aminoglycoside resistance in MRSA, and ribosomal A-site binding of pyrene-neomycin conjugates. |
AID187054 | The compound was tested for uterotropic activity in immature rats(Dosage 1 ug) | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]-phenyl]methanone hydrochloride (LY156758), a remarkably effec |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
AID1801141 | Exogenous PldA Assay from Article 10.1021/cb500828m: \\Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes.\\ | 2015 | ACS chemical biology, Feb-20, Volume: 10, Issue:2 | Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes. |
AID1804127 | No assay is provided from Article 10.1002/med.21724: \\The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.\\ | 2021 | Medicinal research reviews, 01, Volume: 41, Issue:1 | The recent outbreaks of human coronaviruses: A medicinal chemistry perspective. |
AID1797989 | ER-alpha Radioligand Binding Assay and ERE-Luciferase Reporter Assay. from Article 10.1021/jm030086h: \\Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.\\ | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands. |
AID1799396 | d.311 Enzymatic Inhibition Assay from Article 10.1038/nchembio.140: \\Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.\\ | 2009 | Nature chemical biology, Feb, Volume: 5, Issue:2 | Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. |
AID1801851 | LoxA HTP Assay from Article 10.1021/acs.biochem.6b00338: \\Biochemical and Cellular Characterization and Inhibitor Discovery of Pseudomonas aeruginosa 15-Lipoxygenase.\\ | 2016 | Biochemistry, 06-14, Volume: 55, Issue:23 | Biochemical and Cellular Characterization and Inhibitor Discovery of Pseudomonas aeruginosa 15-Lipoxygenase. |
AID1797992 | ER-alpha Radioligand Binding Assay and ERE-Luciferase Reporter Assay. from Article 10.1021/jm040858p: \\Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective | 2005 | Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2 | Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands. |
AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 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. |
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. |
AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2005 | Journal of molecular biology, Sep-09, Volume: 352, Issue:1 | Structural insights into drug processing by human carboxylesterase 1: tamoxifen, mevastatin, and inhibition by benzil. |
AID1811 | Experimentally measured binding affinity data derived from PDB | 2005 | Journal of molecular biology, Sep-09, Volume: 352, Issue:1 | Structural insights into drug processing by human carboxylesterase 1: tamoxifen, mevastatin, and inhibition by benzil. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 2501 (12.80) | 18.7374 |
1990's | 4322 (22.11) | 18.2507 |
2000's | 5883 (30.10) | 29.6817 |
2010's | 5476 (28.02) | 24.3611 |
2020's | 1363 (6.97) | 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 (110.33) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 2,227 (10.79%) | 5.53% |
Reviews | 2,768 (13.42%) | 6.00% |
Case Studies | 1,253 (6.07%) | 4.05% |
Observational | 61 (0.30%) | 0.25% |
Other | 14,321 (69.42%) | 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 | ||
---|---|---|---|---|---|---|---|
Breast Cancer Adjuvant Hormonotherapy : Tamoxifen and the Anti-aromatases Pharmacokinetics, Correlation With the Pharmacogenetic Characteristics PHACS Protocol : Pharmacology of Adjuvant Hormonotherapy in Breast Cancer [NCT01127295] | Phase 4 | 2,000 participants (Actual) | Interventional | 2010-06-17 | Completed | ||
Genotype and Phenotype Guided Supplementation of TAMoxifen Standard Therapy With ENDOXifen in Breast Cancer Patients (TAMENDOX) [NCT03931928] | Phase 2 | 356 participants (Actual) | Interventional | 2019-09-10 | Completed | ||
Association Between Genetic Polymorphisms of CYP2D6 and Outcomes in Breast Cancer Patients With Tamoxifen Treatment [NCT01169792] | 0 participants | Observational | Completed | ||||
A Clinical Trial Comparing Anastrozole With Tamoxifen in Postmenopausal Patients With Ductal Carcinoma in Situ (DCIS) Undergoing Lumpectomy With Radiation Therapy [NCT00053898] | Phase 3 | 3,104 participants (Actual) | Interventional | 2003-01-31 | Completed | ||
Study on the Efficacy and Toxicity of Pamiparib Combined With Tamoxifen in the Treatment of Epithelial Ovarian Cancer Patients With Biochemical Recurrence During First-line PARPi Maintenance Therapy [NCT05669768] | Phase 2 | 46 participants (Anticipated) | Interventional | 2023-01-01 | Not yet recruiting | ||
Randomized Phase III Study Of Exemestane (Aromasin) For 5 Years Versus Tamoxifen For 2.5- 3 Years Followed By Exemestane (Aromasin) For A Total Of 5 Years As Adjuvant Therapy For Postmenopausal, Receptor Positive, Node Negative or Node Positive Breast Can [NCT00036270] | Phase 3 | 9,779 participants (Actual) | Interventional | 2001-08-31 | Completed | ||
A Randomized Phase II Trial of Tamoxifen Versus Z-Endoxifen HCL in Postmenopausal Women With Metastatic Estrogen Receptor Positive, HER2 Negative Breast Cancer [NCT02311933] | Phase 2 | 81 participants (Actual) | Interventional | 2015-03-06 | Active, not recruiting | ||
A Phase III, Randomized Clinical Trial of Standard Adjuvant Endocrine Therapy +/- Chemotherapy in Patients With 1-3 Positive Nodes, Hormone Receptor-Positive and HER2-Negative Breast Cancer With Recurrence Score (RS) of 25 or Less. RxPONDER: A Clinical Tr [NCT01272037] | Phase 3 | 5,018 participants (Actual) | Interventional | 2011-01-15 | Active, not recruiting | ||
Phase II Study Evaluating According to the Polymorphism of CYP2D6, the Rate of Biological Response to Treatment With Tamoxifen (TAM) Administered in Pre-operative Situation in Patients With Breast Cancer Non Metastatic HR+ [NCT01220076] | Phase 2 | 140 participants (Actual) | Interventional | 2009-09-30 | Completed | ||
Phase III Randomized Study of Immediate Versus Luteal Phase Adjuvant Oophorectomy and Tamoxifen in Premenopausal Women With Hormone Receptor-positive Breast Cancer [NCT00201851] | Phase 3 | 740 participants (Actual) | Interventional | 2004-01-31 | Completed | ||
A Phase II Study of Pembrolizumab And Tamoxifen Among Women With Advanced Hormone Receptor Positive Breast Cancer And Esr1 Mutation [NCT03879174] | Phase 2 | 25 participants (Anticipated) | Interventional | 2019-08-01 | Not yet recruiting | ||
PharmacoKINEtics of TAMoxifen and Its Metabolites in Breast Cancer Patients: the Influence of a Dose Increase in Phenotypic Poor Metabolizers of CYP2D6 (KINETAM) [NCT01192308] | Phase 1 | 42 participants (Actual) | Interventional | 2010-07-31 | Completed | ||
Tamoxifen Versus Estradiol in the Prevention of Unscheduled Bleeding in Etonogestrel Implant Users, a Randomized Controlled Pilot Trial [NCT04933240] | Phase 4 | 0 participants (Actual) | Interventional | 2022-05-31 | Withdrawn(stopped due to Anticipated funding was not received) | ||
A Phase III Trial Evaluating the Role of Chemotherapy as Adjuvant Therapy for Premenopausal Women With Endocrine Responsive Breast Cancer Who Receive Endocrine Therapy [NCT00066807] | Phase 3 | 29 participants (Actual) | Interventional | 2003-08-31 | Terminated(stopped due to Poor accrual, patients were followed until completion of 5 yrs treatment) | ||
Sensitivity Detection and Drug Resistance Mechanism of Breast Cancer Therapeutic Drugs Based on Organ-like Culture [NCT03925233] | 300 participants (Anticipated) | Observational | 2019-01-02 | Enrolling by invitation | |||
TAM4MTM: A Phase 1/2 Randomized, Placebo-Controlled, Double-Blinded, Single Crossover Study to Determine the Safety and Efficacy of Tamoxifen Therapy for Myotubular Myopathy (XLMTM) [NCT04915846] | Phase 1/Phase 2 | 16 participants (Anticipated) | Interventional | 2020-12-18 | Recruiting | ||
A Phase IIB Randomized Trial of Oral Tamoxifen vs. Topical 4-hydroxytamoxifen Gel vs. Control in Women With Atypical Hyperplasia or Lobular Carcinoma In Situ [NCT04570956] | Phase 2/Phase 3 | 104 participants (Anticipated) | Interventional | 2021-07-26 | Recruiting | ||
Chemotherapy-free Trastuzumab and Pertuzumab in HER2-positive (Human Epidermal Receptor) Breast Cancer: FDG-PET Response-adapted Strategy. The PHERGain Study [NCT03161353] | Phase 2 | 377 participants (Actual) | Interventional | 2017-06-26 | Completed | ||
H-16848 - Phase II Pilot Study With Correlative Markers of Tamoxifen for Progressive Transitional Cell Carcinoma Following Previous Chemotherapy [NCT00710970] | Phase 2 | 28 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
A Randomized, Double-blind, Placebo Controlled Trial of 4-Hydroxytamoxifen Gel for Reducing Breast Tissue Density in Women With BI-RADS Breast Density Categories C or D [NCT03199963] | Phase 3 | 223 participants (Actual) | Interventional | 2017-08-21 | Terminated(stopped due to Administrative - change in development strategy) | ||
The TEEL Study: A Phase I Trial of Tamoxifen With Ribociclib (LEE011) in Adult Patients With Advanced ER+ (HER2 Negative) Breast Cancer [NCT02586675] | Phase 1 | 7 participants (Actual) | Interventional | 2016-02-23 | Completed | ||
DCIS: RECAST Trial -Ductal Carcinoma In Situ: Re-Evaluating Conditions for Active Surveillance Suitability as Treatment: a Breast Cancer Prevention Pilot Study [NCT06075953] | Phase 2 | 400 participants (Anticipated) | Interventional | 2023-11-30 | Recruiting | ||
[NCT02132000] | Phase 2/Phase 3 | 3,036 participants (Anticipated) | Interventional | 2014-04-30 | Recruiting | ||
A Randomized Controlled Study to Evaluate Exemestane Tablets Combined With Ovarian Function Suppression/Ablation in Treatment of Premenopausal Breast Cancer Patients With CYP2D6*10 Mutations (STEP) [NCT03137368] | Phase 3 | 300 participants (Anticipated) | Interventional | 2018-08-09 | Enrolling by invitation | ||
Tamoxifen to Reduce Unscheduled Bleeding in New Users of the Levonorgestrel-releasing Intrauterine System (LNG-IUS) [NCT02824224] | Phase 4 | 42 participants (Actual) | Interventional | 2016-09-06 | Completed | ||
The Study of Tamoxifen Treatment in Patients With Motor Neuron Disease [NCT02166944] | Phase 1/Phase 2 | 20 participants (Actual) | Interventional | 2014-04-30 | Completed | ||
Effectiveness of Tocotrienol-rich Fraction Combined With Tamoxifen in the Management of Women With Early Breast Cancer: A Pilot Clinical Trial [NCT01157026] | 240 participants (Actual) | Interventional | 2001-11-30 | Completed | |||
A Multi-Centre Study of Tamoxifen Dose Escalation Study in Breast Cancer Patients With CYP2D6 Polymorphisms [NCT01075802] | 121 participants (Actual) | Interventional | 2010-03-31 | Completed | |||
Phase II Feasibility Trial Incorporating Bevacizumab Into Dose Dense Doxorubicin and Cyclophosphamide Followed by Paclitaxel in Patients With Lymph Node Positive Breast Cancer [NCT00119262] | Phase 2 | 226 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
A Phase II Trial of Tamoxifen and Bortezomib in Patients With Recurrent High-Grade Gliomas [NCT00108069] | Phase 2 | 43 participants (Actual) | Interventional | 2005-04-30 | Completed | ||
Asian, International, Multicenter, Randomized, Double-Blind, Placebo-Controlled, Phase 3 Trial of Tamoxifen With or Without Palbociclib ± Goserelin in Women With Hormone Receptor-Positive, HER2-Negative Advanced or Metastatic Breast Cancer [NCT03423199] | Phase 3 | 180 participants (Anticipated) | Interventional | 2018-02-09 | Active, not recruiting | ||
A Phase III Trial Evaluating the Role of Ovarian Function Suppression and the Role of Exemestane as Adjuvant Therapies for Premenopausal Women With Endocrine Responsive Breast Cancer [NCT00066690] | Phase 3 | 3,066 participants (Actual) | Interventional | 2003-12-17 | Active, not recruiting | ||
Multicenter Prospective, Parallel-controlled Phase III Clinical Study on Comparing Efficacy of Tamoxifen Versus Toremifene in CYP2D6 Intermediate/Poor Metabolizers of Premenopausal Patients With ER-positive Early Breast Cancer [NCT03351062] | Phase 3 | 844 participants (Anticipated) | Interventional | 2017-11-30 | Recruiting | ||
Analysis of Sleep and Activity Patterns in Pre-menopausal Breast Cancer Patients After Taking Tamoxifen Using a Wrist-worn Internet of Things Device [NCT04116827] | 20 participants (Anticipated) | Observational [Patient Registry] | 2018-08-10 | Recruiting | |||
CYP2D6 Genotypes and Breast Cancer Clinical Outcomes in the Indonesian Population (Pengaruh Genotipe CYP2D6 Terhadap Efektivitas Penggunaan Tamoksifen Untuk Pasien Kanker Payudara ER+ Pada Populasi Indonesia) [NCT05501158] | 150 participants (Actual) | Interventional | 2021-01-01 | Active, not recruiting | |||
Clomiphene Citrate Versus Tamoxifen for Induction of Ovulation in Women With Polycystic Ovary Syndrome: Randomized Controlled Trial [NCT02479256] | Phase 4 | 600 participants (Actual) | Interventional | 2015-06-30 | Completed | ||
A Window of Opportunity Study of Endocrine Therapy With and Without Prometrium in Postmenopausal Women With Early Stage Hormone Receptor-positive Breast Cancer. [NCT03906669] | Phase 2 | 200 participants (Anticipated) | Interventional | 2018-03-20 | Recruiting | ||
Phase III Randomized Study of the Effects on Bone Mineral Density of Tamoxifen, Letrozole, and Letrozole + Zoledronic Acid as Adjuvant Treatment of Patients With Early Breast Cancer; VERSION 2 AMENDED Phase 3 Study of Triptorelin and Tamoxifen, Letrozole, [NCT00412022] | Phase 3 | 1,294 participants (Actual) | Interventional | 2004-03-31 | Active, not recruiting | ||
A Randomized, Multicenter, Open Phase III Study Comparing a Dose-Intensified 8 Week Schedule of Adriamycin and Docetaxel (ADOC) With a Sequential 24 Week Schedule of Adriamycin/Cyclophosphamide Followed by Docetaxel (AC-DOC) Regimen as Preoperative Therap [NCT00793377] | Phase 3 | 913 participants (Actual) | Interventional | Completed | |||
Molecularly Stratified Parallel Cohort, Single Arm Phase II Trial of the Phosphoinositide 3-kinase (PI3K) Inhibitor Buparlisib (BKM120) in Combination With Tamoxifen in Patients With Hormone Receptor-positive, HER2-negative Inoperable (Locally Advanced or [NCT02404844] | Phase 2 | 48 participants (Actual) | Interventional | 2014-12-31 | Completed | ||
Palbociclib in Combination With Fulvestrant or Tamoxifen as Treatment for Hormone Receptor Positive Metastatic Breast Cancer Previously Exposed to Inhibitors of the PI3K Pathway: A Phase II Study With Pharmacodynamics Markers [NCT02384239] | Phase 2 | 70 participants (Actual) | Interventional | 2015-10-19 | Completed | ||
Safety of Toremifene and Tamoxifen Therapy in Premenopausal Patients With Operable Breast Cancer: A Randomized, Controlled, Prospective, Observational Study [NCT02344940] | Phase 4 | 104 participants (Actual) | Interventional | 2014-12-31 | Completed | ||
Comparison of the Efficacy of the Tamoxifen and Tamoxifen With Antioxidants on Semen Quality of Infertile Male With Abnormal Semen Parameters. [NCT05200663] | Phase 2 | 110 participants (Anticipated) | Interventional | 2021-10-15 | Recruiting | ||
Tamoxifen to Treat Barrett's Metaplasia [NCT02089386] | Early Phase 1 | 7 participants (Actual) | Interventional | 2014-07-09 | Terminated(stopped due to Insufficient funding) | ||
A Phase 1B Study of Infigratinib in Combination With Tamoxifen in Hormone Receptor Positive, HER2 Negative, FGFR Altered Advanced Breast Cancer [NCT04504331] | Phase 1 | 4 participants (Actual) | Interventional | 2020-10-13 | Terminated(stopped due to Drug manufacturer decision to terminate development.) | ||
An Open, Single-center, Exploratory Cohort Study of Chidamide in Combination With Endocrine in Maintenance Therapy After First-line Chemotherapy for HR+/HER2- Breast Cancer [NCT05890287] | 60 participants (Anticipated) | Interventional | 2023-05-16 | Recruiting | |||
An Open-label, Single-institution, Dose-determining (Part 1) and Dose-confirmatory (Part II) Study to Investigate the Optimal Dose of Tamoxifen in Breast Cancer Patients Harboring Different TCF20 rs932376 Variant Alleles [NCT04961632] | Phase 1 | 75 participants (Actual) | Interventional | 2020-12-23 | Active, not recruiting | ||
Low-Dose Tamoxifen for Radiation-Induced Breast Cancer Risk Reduction: A Phase IIB Randomized Placebo-Controlled Trial [NCT01196936] | Phase 2 | 84 participants (Actual) | Interventional | 2010-09-30 | Active, not recruiting | ||
Treatment of Canadian Men and Pre/Postmenopausal Women With ER+ Advanced Breast Cancer in the Real-World Setting With Hormone Therapy ± Targeted Therapy [NCT02753686] | 440 participants (Actual) | Observational [Patient Registry] | 2016-03-15 | Completed | |||
The Effect of Tamoxifen on Endometrial Thickness and Pregnancy Outcome in Women With Thin Endometrium Undergoing Frozen Thawed Cycle. [NCT03060304] | Phase 4 | 100 participants (Anticipated) | Interventional | 2017-03-31 | Not yet recruiting | ||
Therapeutic Dose Monitoring (TDM) of Tamoxifen and Its Active Metabolites in Combination With Patient-reported Symptom Scores Among Patients With Breast Cancer Receiving Adjuvant Tamoxifen Treatment [NCT05133674] | Phase 2 | 40 participants (Actual) | Interventional | 2022-04-04 | Active, not recruiting | ||
Randomized Placebo-controlled Phase III Trial of Low Dose Tamoxifen in Women With Breast Intraepithelial Neoplasia - Long Term Follow-up [NCT01357772] | Phase 3 | 500 participants (Actual) | Interventional | 2008-11-12 | Active, not recruiting | ||
Prognostic Evaluation of Changing Endocrine Therapy in Perimenopausal and Recently Postmenopausal Women With Early-stage Hormone Receptor-Positive Breast Cancer [NCT02097459] | Phase 3 | 600 participants (Anticipated) | Interventional | 2014-03-31 | Recruiting | ||
A Trial of Endocrine Response in Women With Invasive Lobular Breast Cancer [NCT02206984] | Phase 2 | 201 participants (Anticipated) | Interventional | 2015-09-30 | Recruiting | ||
A Phase II Trial for Patients With Inflammatory (Stage IIIB) and Responsive Metastatic Stage IV Breast Cancer Using Busulfan, Melphalan and Thiotepa Followed by Autologous or Syngeneic PBSC Rescue and 12 Weeks of Post-Engraftment Immunotherapy With Low-Do [NCT00003199] | Phase 2 | 50 participants (Actual) | Interventional | 1997-11-30 | Completed | ||
EMBER-4: A Randomized, Open-Label, Phase 3 Study of Adjuvant Imlunestrant vs Standard Adjuvant Endocrine Therapy in Patients Who Have Previously Received 2 to 5 Years of Adjuvant Endocrine Therapy for ER+, HER2- Early Breast Cancer With an Increased Risk [NCT05514054] | Phase 3 | 6,000 participants (Anticipated) | Interventional | 2022-10-04 | Recruiting | ||
Endocrine Therapy With or Without Anti-VEGF Therapy: A Randomized, Phase III Trial of Endocrine Therapy Alone or Endocrine Therapy Plus Bevacizumab (NSC 704865) for Women With Hormone Receptor-Positive Advanced Breast Cancer [NCT00601900] | Phase 3 | 394 participants (Actual) | Interventional | 2008-05-15 | Active, not recruiting | ||
A Phase 2 Single-Arm Open-Label Pilot Trial Evaluating Zanidatamab (ZW25) in Patients With Early Stage HER2/Neu Positive (HER2+) Breast Cancer (BC) [NCT05035836] | Phase 2 | 20 participants (Actual) | Interventional | 2021-11-16 | Active, not recruiting | ||
Analgesic Efficacy of Pulsed Radiofrequency in Non-cyclic Mastalgia [NCT03715413] | Phase 2 | 64 participants (Actual) | Interventional | 2018-08-15 | Completed | ||
Prospective Randomized Controlled Study on the Risk and Clinical Benefit of Chemotherapy and Intensive Endocrine Therapy for Luminal B1 Early-stage Breast Cancer [NCT03373708] | Phase 2/Phase 3 | 200 participants (Anticipated) | Interventional | 2017-12-20 | Not yet recruiting | ||
Comparative Evaluation of Efficacy and Safety of Toremifene, Tamoxifen, and Aromatase Inhibitor Plus Ovarian Suppression in Hormone Receptor-Positive Early Breast Cancer Among Non-Low-Risk Premenopausal Women: A Real-World Study [NCT05801705] | 700 participants (Anticipated) | Observational | 2023-06-01 | Not yet recruiting | |||
The Effects of Adjuvant Zoladex Plus Tamoxifen on Breast Density in Pre- or Peri-menopausal Women With Early-stage Breast Cancer [NCT00827307] | 100 participants (Anticipated) | Interventional | 2008-06-30 | Completed | |||
Choosing Neoadjuvant Chemotherapy Versus Hormonal Therapy for Breast Cancer Based on Gene Expression Profile [NCT01293032] | 59 participants (Actual) | Interventional | 2011-04-30 | Completed | |||
Open-label, Safety Extension Study for Subjects With HR+, HER2-Negative Breast Cancer Who Have Completed the OVarian Suppression Evaluating Subcutaneous LeuprolIde Acetate in Breast Cancer OVELIA Study [NCT05645536] | Phase 3 | 250 participants (Anticipated) | Interventional | 2022-12-28 | Enrolling by invitation | ||
Phase 3,Single Arm,Open-Label Study Evaluating Ovarian Suppression Following 3 Month Leuprolide Acetate For Injectable Suspension (TOL2506) in Combination With Endocrine Therapy in Premenopausal Subjects With Hormone-Receptor-Positive (HR+),Human Epiderma [NCT04906395] | Phase 3 | 250 participants (Anticipated) | Interventional | 2021-07-01 | Recruiting | ||
A Randomized Phase II Trial of Temsirolimus (NCI-Supplied Agent, NSC # 683864) or the Combination of Hormonal Therapy Plus Temsirolimus in Women With Advanced, Persistent, or Recurrent Endometrial Carcinoma [NCT00729586] | Phase 2 | 73 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
[NCT02866955] | Phase 2 | 100 participants (Actual) | Interventional | 2011-06-15 | Completed | ||
Comparison of Tamoxifen and Clomiphene Citrate in Mild Stimulation IVF: a Prospective Cohort Study [NCT02690870] | Phase 4 | 210 participants (Anticipated) | Interventional | 2017-01-31 | Not yet recruiting | ||
A Phase I/II Trial Investigating the Tolerability, Toxicity and Efficacy of Tamoxifen and SUBA-Itraconazole in Patients With Platinum Resistant Recurrent Epithelial Ovarian Cancer [NCT05156892] | Phase 1 | 44 participants (Anticipated) | Interventional | 2022-09-04 | Recruiting | ||
Genetic Study of CYP2D6 Enzyme and Therapeutic Drug Monitoring of Tamoxifen in Premenopausal Women With Breast Cancer [NCT03582865] | 100 participants (Anticipated) | Observational | 2019-09-01 | Not yet recruiting | |||
A Phase III, Open-Label, Randomised Study to Assess the Efficacy and Safety of Extended Therapy With Camizestrant Versus Standard Endocrine Therapy (Aromatase Inhibitor or Tamoxifen) in Patients With ER+/HER2- Early Breast Cancer [NCT05774951] | Phase 3 | 4,300 participants (Anticipated) | Interventional | 2023-03-31 | Recruiting | ||
Comparison of Adjuvant Monotherapy With Endocrine Therapy or Accelerated Partial Breast Irradiation Following Lumpectomy for Low Risk Breast Cancer Patients Over 65 (CAMERAN) [NCT05472792] | Phase 2 | 90 participants (Anticipated) | Interventional | 2022-05-17 | Recruiting | ||
Herceptin and Paclitaxel in Locally Advanced Breast Cancer With Her-2 Overexpression [NCT00009997] | Phase 1 | 0 participants | Interventional | 1999-03-31 | Completed | ||
An Open Label Randomized Phase 2 Trial of Amcenestrant (SAR439859), Versus Endocrine Monotherapy as Per Physician's Choice in Patients With Estrogen Receptor-positive, HER2-Negative Locally Advanced or Metastatic Breast Cancer With Prior Exposure to Hormo [NCT04059484] | Phase 2 | 363 participants (Actual) | Interventional | 2019-10-22 | Active, not recruiting | ||
A Randomized Phase II/III Study to Assess the Efficacy of Trametinib (GSK 1120212) in Patients With Recurrent or Progressive Low-Grade Serous Ovarian Cancer or Peritoneal Cancer [NCT02101788] | Phase 2/Phase 3 | 260 participants (Actual) | Interventional | 2014-02-27 | Active, not recruiting | ||
Preoperative Window of Opportunity Study With Giredestrant (GDC-9545) or Tamoxifen in Premenopausal Women With Estrogen Receptor-Positive/Human Epidermal Growth Factor Receptor 2-Negative & Ki67≥10% Early Breast Cancer [NCT05659563] | Phase 2 | 92 participants (Anticipated) | Interventional | 2023-07-20 | Recruiting | ||
Randomized Double-blind Study to Compare Two Neo-adjuvant Treatments: an Anti-aromatase vs SERM for Postmenopausal Women With ER+ Breast Adenocarcinoma: Effect on Intermediate Predictive Biological Response to Treatment. [NCT00949598] | Phase 3 | 177 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
A Phase II Study of Sulindac and Tamoxifen in Patients With Desmoid Tumors That Are Recurrent or Not Amenable to Standard Therapy [NCT00068419] | Phase 2 | 70 participants (Actual) | Interventional | 2004-02-29 | Completed | ||
A Phase III Trial Evaluating The Role Of Exemestane Plus GnRH Analogue As Adjuvant Therapy For Premenopausal Women With Endocrine Responsive Breast Cancer [NCT00066703] | Phase 3 | 2,672 participants (Actual) | Interventional | 2003-11-03 | Active, not recruiting | ||
Randomized Double-Blind Trial In Postmenopausal Women With Primary Breast Cancer Who Have Received Adjuvant Tamoxifen For 2-3 Years, Comparing Subsequent Adjuvant Exemestane Treatment With Further Tamoxifen [NCT00038467] | Phase 3 | 4,740 participants (Actual) | Interventional | 1998-02-28 | Completed | ||
Radiotherapy Versus Low-Dose Tamoxifen Following Breast Conserving Surgery for Low-Risk and Estrogen Receptor-Positive Ductal Carcinoma in Situ of Breast: an International Open-label Randomized Non-inferiority Trial [NCT04046159] | Phase 3 | 810 participants (Anticipated) | Interventional | 2019-04-30 | Recruiting | ||
A Phase III Randomized, Double-blind, Placebo-controlled Study of LEE011 or Placebo in Combination With Tamoxifen and Goserelin or a Non-steroidal Aromatase Inhibitor (NSAI) and Goserelin for the Treatment of Premenopausal Women With Hormone Receptor Posi [NCT02278120] | Phase 3 | 672 participants (Actual) | Interventional | 2014-11-20 | Completed | ||
A Randomized Study Of Tamoxifen Versus Thalidomide (NSC# 66847) In Patients With Biochemical-Recurrence-Only Epithelial Ovarian Cancer, Cancer Of The Fallopian Tube, And Primary Peritoneal Carcinoma After First Line Chemotherapy [NCT00041080] | Phase 3 | 139 participants (Actual) | Interventional | 2003-02-28 | Completed | ||
A Pilot Trial of Sequential Primary (Neoadjuvant) Combination Chemotherapy With Docetaxel/Capecitabine (TX) and Doxorubicin/Cyclophosphamide (AC) in Primary Breast Cancer With Evaluation of Chemotherapy Effects on Gene Expression [NCT00005908] | Phase 2 | 30 participants (Actual) | Interventional | 2000-06-30 | Completed | ||
A Randomized Trial of Concurrent Versus Sequential Tamoxifen With Radiotherapy to Assess the Extent of Pulmonary Fibrosis and Disease Related Control and Survival in Breast Cancer Patients [NCT00896155] | Phase 3 | 260 participants (Anticipated) | Interventional | 2008-12-31 | Recruiting | ||
Tamoxifen Resistance in Breast Cancer [NCT00899197] | 2 participants (Actual) | Observational | 2007-05-31 | Terminated | |||
A Pilot Study of FES Imaging to Optimize Tamoxifen Dose for Metastatic Breast Cancer Patients With ESR1 Mutations [NCT04174352] | Early Phase 1 | 12 participants (Anticipated) | Interventional | 2020-10-20 | Recruiting | ||
Randomized Study of the Use of Tamoxifen Versus Ointment Lidocaine for Reducing the Pain and Discomfort in Mammography [NCT02801786] | Phase 2/Phase 3 | 450 participants (Anticipated) | Interventional | 2018-11-30 | Not yet recruiting | ||
Randomised, Double-blind, Placebo Controlled, Parallel-group, Multicentre Phase II Study to Assess Dose Response Relationship of Nolvadex (Oral Tablet) in Prophylactic Treatment of Gynaecomastia and Breast Pain Associated With CASODEX 150 mg (Oral Tablet) [NCT00637871] | Phase 2 | 0 participants | Interventional | 2002-11-30 | Completed | ||
A Randomized, Open-label, Multi-center Phase IV Study Evaluating Palbociclib Plus Endocrine Treatment Versus a Chemotherapy-based Treatment Strategy in Patients With Hormone Receptor Positive / HER2 Negative Breast Cancer in a Real World Setting (GBG 93 - [NCT03355157] | Phase 4 | 150 participants (Anticipated) | Interventional | 2018-03-01 | Recruiting | ||
A Randomized Study of Chemotherapy Versus Hormonal Treatment in Patients With Ovarian Cancer Resistant or Refractory to Platinum and Taxane [NCT02728622] | Phase 3 | 241 participants (Actual) | Interventional | 2002-03-31 | Completed | ||
Preoperative Hormone Therapy for Postmenopausal Women With ER+ Clinical Stage T2-4 Tumors. A Phase II Study to Identify Molecular Predictors for Hormone Responsiveness and/or Resistance. [NCT01831076] | Phase 2 | 36 participants (Actual) | Interventional | 2002-04-30 | Completed | ||
Pre-Operative Window of Adjuvant Endocrine Therapy to Inform Radiation Therapy Decisions In Older Women With Early-Stage Breast Cancer [NCT04272801] | Phase 2 | 83 participants (Anticipated) | Interventional | 2020-04-07 | Recruiting | ||
PErsonalized TREatment of High-risk MAmmary Cancer - the PETREMAC Trial [NCT02624973] | Phase 2 | 200 participants (Actual) | Interventional | 2016-04-15 | Active, not recruiting | ||
Impact of Neoadjuvant Hormonal Therapy on the Surgical Management of Extensive Ductal Carcinomas in Situ [NCT04666961] | Phase 2 | 262 participants (Anticipated) | Interventional | 2021-02-03 | Recruiting | ||
Randomized Phase II/III Study of Second-line Endocrine Treatment Followed by Capecitabine Versus Capecitabine Followed by Endocrine Treatment in Patients With Metastatic Estrogen Receptor Positive Breast Cancer [NCT00684216] | Phase 2/Phase 3 | 10 participants (Actual) | Interventional | 2008-04-30 | Terminated(stopped due to acrual too slow) | ||
A Phase 2 Pilot Feasibility Study of Palbociclib in Combination With Adjuvant Endocrine Therapy for Hormone Receptor Positive Invasive Breast Carcinoma [NCT02040857] | Phase 2 | 162 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
Multi-centre, Randomised, Double-blind, Parallel-group Study to Compare Efficacy and Safety Between Anastrozole (ZD1033) and Tamoxifen in Pre- and Post-operative Administration Under Goserelin Acetate Treatment for Premenopausal Breast Cancer Patients [NCT00605267] | Phase 3 | 197 participants (Actual) | Interventional | 2007-10-31 | Completed | ||
Phase III Comparison of Adjuvant Chemoendocrine Therapy With CAF and Concurrent or Delayed Tamoxifen to Tamoxifen Alone in Postmenopausal Patients With Involved Axillary Lymph Nodes and Positive Receptors [NCT00929591] | Phase 3 | 1,558 participants (Actual) | Interventional | 1989-05-31 | Completed | ||
Efficacy and Safety of High Dose Tamoxifen to Advanced Hormone Receptor-High Expressed Endocrine Therapy Resisted Breast Cancer [NCT03045653] | Phase 2 | 30 participants (Actual) | Interventional | 2017-09-01 | Completed | ||
Tamoxifen Metabolism and the Impact of Tamoxifen Dose on the Level of the Active Metabolites in Endocrine Sensitive Breast Cancer Patients [NCT00963209] | Phase 3 | 140 participants (Anticipated) | Interventional | 2009-06-30 | Recruiting | ||
Impact of CYP2D6 Genotype on the Clinical Effects of Tamoxifen Using With Samples From Prospective Randomized Multicenter Study [NCT00973037] | 922 participants (Anticipated) | Observational | 2009-03-31 | Recruiting | |||
A Phase II Study of GW572016 and Tamoxifen in Patients With Metastatic Breast Cancer Resistant to Single-Agent Tamoxifen [NCT00118157] | Phase 2 | 19 participants (Actual) | Interventional | 2005-05-31 | Completed | ||
Randomized, Double-blind, Parallel-controlled Phase III Trial to Evaluate the Efficacy and Safety of TQB3616 Combined With Endocrine Therapy Versus Placebo Combined With Endocrine Therapy in Hormone Receptors (HR)-Positive and Human Epidermal GrowthFactor [NCT05780567] | Phase 3 | 1,946 participants (Anticipated) | Interventional | 2023-03-30 | Recruiting | ||
A Randomised Phase III Study for Evaluating the Role of the Addition of Ovarian Function Suppression to Tamoxifen in Young Women With Hormone-Sensitive Breast Cancer Who Remain in Premenopause or Regain Menstruation After Chemotherapy [NCT00912548] | Phase 3 | 1,234 participants (Anticipated) | Interventional | 2009-05-31 | Enrolling by invitation | ||
Validating CYP2D6 Genotype-Guided Tamoxifen Therapy for a Multiracial U.S. Population [NCT00764322] | Phase 2 | 501 participants (Actual) | Interventional | 2008-06-18 | Completed | ||
Phase 2 Randomized, Multicenter Study of IMC-A12 as a Single Agent or in Combination With Antiestrogens in Postmenopausal Women With Hormone Receptor-Positive Advanced or Metastatic Breast Cancer After Progression on Antiestrogen Therapy [NCT00728949] | Phase 2 | 93 participants (Actual) | Interventional | 2008-08-31 | Completed | ||
A Randomized, Open Pilot Study to Investigate the Mammographic Density Reduction on Healthy Women, Within the Karma Cohort, for Two Different Doses of Tamoxifen [NCT04079517] | Phase 1/Phase 2 | 42 participants (Actual) | Interventional | 2015-03-31 | Completed | ||
Phase II Study of Soy Protein to Treat Vasomotor Symptoms in Postmenopausal Women Taking Tamoxifen [NCT00031720] | Phase 2 | 112 participants (Actual) | Interventional | 2002-03-31 | Completed | ||
PREDIX Luminal B - Neoadjuvant Response-guided Treatment of ER Positive Tumors With High Proliferation or Low Proliferation With Metastatic Nodes. Part of a Platform of Translational Phase II Trials Based on Molecular Subtypes [NCT02603679] | Phase 2 | 181 participants (Actual) | Interventional | 2015-02-28 | Active, not recruiting | ||
A Randomized, Prospective Trial of 2-6 Weeks Pre-operative Hormonal Treatment for Hormone Receptor Positive Breast Cancer: Anastrozole +/- Fulvestrant or Tamoxifen Exposure - Response in Molecular Profile (AFTER-study). [NCT00738777] | Phase 2 | 250 participants (Anticipated) | Interventional | 2008-07-31 | Suspended(stopped due to in preparation for an amendment) | ||
A Single Blinded Randomized Controlled Trial of the Comparative Effects of Tamoxifen and Evening Primrose Oil in Premenopausal Non-high Risk Patients With Benign Breast Disease With Respect to the Estrogen Receptor Status. [NCT00999921] | Phase 4 | 256 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
Investigating Cognitive Function for Patients Participating in the SOFT Trial in Selected Centers [NCT00659373] | Phase 3 | 86 participants (Actual) | Interventional | 2007-12-31 | Completed | ||
Efficacy and Safety of Mecapegfilgrastim for Prophylaxis of Dalpiciclib -Induced Neutropenia in Patients With Advanced HR+/HER2- Breast Cancer: a Open-label, Multicenter, Investigator-initiated, Randomized Controlled Phase II Trial [NCT05463601] | Phase 2 | 132 participants (Anticipated) | Interventional | 2022-08-01 | Recruiting | ||
Pre-surgical Phase IIb Trial of Transdermal 4-Hydroxytamoxifen vs. Oral Tamoxifen in Women With Ductal Carcinoma in Situ of the Breast [NCT00952731] | Phase 2 | 27 participants (Actual) | Interventional | 2009-12-31 | Completed | ||
A Randomised, Double Blind Trial to Assess the Incidence of Endometrial Changes With Arimidex Alone, Nolvadex Alone, or Arimidex and Nolvadex in Combination, When Used as Adjuvant Treatment for Breast Cancer in Postmenopausal Women [NCT00814125] | Phase 3 | 285 participants (Actual) | Interventional | 1997-06-30 | Completed | ||
Pilot Study to Analyze a Novel Mechanism Underlying Response to Tamoxifen Therapy in Breast Cancer Patients [NCT01027416] | 59 participants (Actual) | Interventional | 2009-12-14 | Completed | |||
Hormone Replacement Versus Tamoxifen Combined Of Hormone Replacement in Women With a Thin Endometrium Undergoing Frozen-thawed Embryo Transfer [NCT04292886] | 120 participants (Anticipated) | Interventional | 2019-10-01 | Recruiting | |||
Selective Estrogen Receptor Modulators to Enhance the Efficacy of Viral Reactivation With Histone Deacetylase Inhibitors [NCT03382834] | Phase 2 | 31 participants (Actual) | Interventional | 2018-04-26 | Active, not recruiting | ||
Anastrozole Adjuvant Trial - Study of Anastrozole Compared to NOLVADEX (Tamoxifen Citrate) for Adjuvant Treatment of Early Breast Cancer (Clinical Studies), Tamoxifen Citrate Was Added to Adjunct Cytotoxic Chemotherapy- Treatment of Malignant Joint Tumor. [NCT06154590] | 100 participants (Anticipated) | Observational [Patient Registry] | 2024-07-31 | Not yet recruiting | |||
COX Inhibition and Biomarkers of Response During Neoadjuvant Chemoendocrine Therapy for Estrogen Receptor Positive, Human Epidermal Growth Factor Receptor 2 Negative Stage I-III Breast Cancer [NCT04038489] | Phase 2 | 0 participants (Actual) | Interventional | 2019-10-18 | Withdrawn(stopped due to Lack of accrual) | ||
A Prospective, Randomized, Open-label, Multicenter Study Evaluating the Effects on Cognitive Functions of Adjuvant Endocrine Therapy in Postmenopausal Women With Breast Cancer. [NCT00893061] | Phase 3 | 60 participants (Anticipated) | Interventional | 2009-02-28 | Recruiting | ||
A Randomised, Double-Blind, Parallel Group Trial to Assess Quality of Life With Arimidex Alone, Nolvadex Alone, or Arimidex and Nolvadex in Combination, When Used as Adjuvant Treatment for Breast Cancer in Postmenopausal Women [NCT00784680] | Phase 3 | 308 participants (Actual) | Interventional | 1998-04-30 | Completed | ||
Fourteen Day Safety of Low-Dose Tamoxifen in Patients With Chronic Hepatitis C Who Have Failed Standard Medical Therapy [NCT00749138] | Phase 1 | 18 participants (Anticipated) | Interventional | 2008-11-30 | Completed | ||
A Phase III Study Comparing Anastrozole, Letrozole and Exemestane, Upfront (for 5 Years) or Sequentially (for 3 Years After 2 Years of Tamoxifen), as Adjuvant Treatment of Postmenopausal Patients With Endocrine-responsive Breast Cancer [NCT00541086] | Phase 3 | 3,697 participants (Actual) | Interventional | 2007-03-31 | Active, not recruiting | ||
A Randomised, Double Blind Trial to Assess the Pharmacokinetics of Arimidex Alone, Nolvadex Alone, or Arimidex and Nolvadex in Combination, When Used as Adjuvant Treatment for Breast Cancer in Postmenopausal Women [NCT00784862] | Phase 3 | 9,358 participants (Actual) | Interventional | 1998-06-30 | Completed | ||
A Randomised, Double-Blind Trial to Assess the Effects on Bone Mineral Density and Metabolism of Arimidex Alone, Nolvadex Alone, or Arimidex and Nolvadex in Combination, (in Comparison to a Control Group) When Used as Adjuvant Treatment for Breast Cancer [NCT00784940] | Phase 3 | 308 participants (Actual) | Interventional | 1998-06-30 | Completed | ||
An Umbrella, Randomized, Controlled, Pre-Operative Trial Testing Integrative Subtype-Targeted Therapeutics in Hormone Receptor-Positive, HER2-Negative Breast Cancer [NCT05101564] | Phase 2 | 150 participants (Anticipated) | Interventional | 2023-03-20 | Recruiting | ||
Phase II Study Evaluating the Effectiveness of the Exemestane (Aromasin) With Tamoxifen on the Rate of Clinical Response Menopausal in Patients With Locally Advanced Breast Tumors [NCT00919399] | Phase 2 | 15 participants (Actual) | Interventional | 2002-01-31 | Completed | ||
Tamoxifen in Duchenne Muscular Dystrophy: A Multicenter, Randomised, Double-blind, Placebo-controlled, Phase 3 Safety and Efficacy 48-week Trial [NCT03354039] | Phase 3 | 93 participants (Actual) | Interventional | 2018-06-12 | Completed | ||
A Post-trial Access Roll-over Study to Allow Access to Ribociclib (LEE011) for Patients Who Are on Ribociclib Treatment in Novartis-sponsored Study [NCT05161195] | Phase 4 | 137 participants (Anticipated) | Interventional | 2022-07-07 | Recruiting | ||
Dose-Intense Chemotherapy and Stem Cell Rescue in the Treatment of Inflammatory Breast Carcinoma [NCT00003042] | Phase 2 | 41 participants (Actual) | Interventional | 1997-05-30 | Active, not recruiting | ||
The TRADE Study: A Phase 2 Trial to Assess the ToleRability of Abemaciclib Dose Escalation in Patients With Early-Stage HR-positive and HER2-negative Breast Cancer [NCT06001762] | Phase 2 | 90 participants (Anticipated) | Interventional | 2024-02-29 | Recruiting | ||
A Phase IB Randomized Study of an Antiestrogen in Women With Newly Diagnosed Breast Cancer [NCT00005886] | Phase 1 | 0 participants | Interventional | 2000-07-31 | Completed | ||
A Randomised, Double Blind Trial Comparing Arimidex Alone With Nolvadex Alone With Arimidex and Nolvadex in Combination, as Adjuvant Treatment in Post-Menopausal Women With Breast Cancer [NCT00849030] | Phase 3 | 9,358 participants (Actual) | Interventional | 1996-07-31 | Completed | ||
Phase III Trial of Doxorubicin and Cyclophosphamide (AC) Followed by Weekly Paclitaxel With or Without Trastuzumab as Adjuvant Treatment for Women With HER-2 Over-Expressing or Amplified Node Positive or High-Risk Node Negative Breast Cancer [NCT00005970] | Phase 3 | 3,436 participants (Actual) | Interventional | 2000-05-19 | Completed | ||
A Phase II Trial of High Dose Tamoxifen For The Treatment of Newly Diagnosed Supratentorial Glioblastoma Multiforme (GBM) [NCT00006388] | Phase 2 | 77 participants (Actual) | Interventional | 2000-12-31 | Completed | ||
A Phase I Pharmacokinetic, Pharmacodynamic, and Clinical Study of the Combination of the Angiogenesis Inhibitor SU5416 and Doxorubicin in Inflammatory Breast Cancer [NCT00005822] | Phase 1 | 21 participants (Actual) | Interventional | 2000-04-30 | Completed | ||
A 2X2X2 Factorial Randomized Phase III Trial Of Multimodality Therapy Comparing 4 Cycles Of Doxorubicin And Cyclophosphamide With Or Without Dexrazoxane (AC+/-Z) Followed By 12 Weeks Of Weekly Paclitaxel With Or Without Trastuzumab (T+/-H) Followed By Loc [NCT00016276] | Phase 3 | 396 participants (Actual) | Interventional | 2001-05-31 | Terminated(stopped due to Administratively complete.) | ||
The Comparative Trial of UFT + TAM With CMF + TAM in Adjuvant Therapy for Breast Cancer (CUBC) [NCT00152178] | Phase 3 | 680 participants (Anticipated) | Interventional | 1996-07-31 | Completed | ||
PREDIX Luminal A - Neoadjuvant Response-guided Treatment of Slowly Proliferating Hormone Receptor Positive Tumors. Part of a Platform of Translational Phase II Trials Based on Molecular Subtypes [NCT02592083] | Phase 2 | 10 participants (Actual) | Interventional | 2015-10-31 | Active, not recruiting | ||
A Pilot Study of Varying Doses of Tamoxifen in the Setting of Genetic Polymorphisms of CYP2D6 [NCT00900744] | 121 participants (Actual) | Observational | 2009-01-31 | Completed | |||
[NCT00538330] | 2,000 participants (Anticipated) | Interventional | 2007-09-30 | Active, not recruiting | |||
Efficacy and Safety of Ospemifene in the Treatment of Vulvar and Vaginal Atrophy (VVA) in Postmenopausal Women: A 12-Week, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Study Comparing Oral Ospemifene 30 and 60 Mg Daily Doses With Placebo [NCT00276094] | Phase 3 | 826 participants (Actual) | Interventional | 2006-01-31 | Completed | ||
Primary Hormonal Therapy for Ductal Carcinoma in Situ: Exploration of a Novel Approach to the Clinical Management of Noninvasive Breast Cancer [NCT00290745] | Phase 1/Phase 2 | 79 participants (Actual) | Interventional | 2002-02-19 | Completed | ||
A Phase Ib/II, Open-Label, Multicenter, Randomized Umbrella Study Evaluating the Efficacy and Safety of Multiple Immunotherapy-Based Treatment Combinations in Patients With Hormone Receptor-Positive HER2-Negative Breast Cancer (MORPHEUS-HR+ Breast Cancer) [NCT03280563] | Phase 1/Phase 2 | 138 participants (Actual) | Interventional | 2017-12-26 | Active, not recruiting | ||
A Comparative Trial of the Efficacy of Two Different Nolvadex (NDX) Dosing and Scheduling Regimens in Preventing Gynecomastia Induced by Casodex (CDX) 150 Monotherapy in Prostate Cancer Patients. An Open, Multicenter, Phase III Trial. [NCT00233610] | Phase 3 | 180 participants | Interventional | 2003-12-31 | Completed | ||
Anti-Estrogens - A Potential Treatment for Bipolar Affective Disorder in Women? [NCT00206544] | Phase 2 | 51 participants (Actual) | Interventional | 2004-01-31 | Completed | ||
A Pilot Trial Correlating Metabolic Profile of Tamoxifen With Pharmacogenetic Predictors and Clinical Effects [NCT00228930] | 297 participants (Actual) | Observational | 2002-09-30 | Completed | |||
A Neoadjuvant Phase II Trial of ZD1839 (Iressa) and Tamoxifen in Inoperable Locally Advanced HER2-Overexpressing, ER-Positive Breast Cancer Patients: Biologic Correlative Study (AZ #1839US/0303) [NCT00206492] | Phase 2 | 3 participants (Actual) | Interventional | 2003-07-31 | Terminated(stopped due to halted by the PI only 3 of 45 subjects were accrued.) | ||
Higher Dose taMOxifen in Premenopausal bREast Cancer Patients: a preoperaTive Window Trial (MORE-T Trial) [NCT04997941] | Phase 2 | 238 participants (Anticipated) | Interventional | 2021-10-21 | Recruiting | ||
A Randomized, Double-Blind, Placebo-Controlled Study of 4-hydroxytamoxifen Topical Gel in Women With Mammographically Dense Breast [NCT03063619] | Phase 2 | 194 participants (Actual) | Interventional | 2017-05-01 | Active, not recruiting | ||
A Multicentre, Randomized Study of Trastuzumab Combined With Chemotherapy or Endocrine Therapy as the First Line Treatment for Patients With Metastatic Luminal B2 Breast Cancer Subtype [NCT01950182] | Phase 3 | 392 participants (Actual) | Interventional | 2013-09-16 | Completed | ||
A Double-blind, Randomized, Multicentre Trial Comparing the Efficacy and Tolerability of 250mg of Faslodex (Long Acting ICI 182,780) With 20mg of Nolvadex (Tamoxifen) in Postmenopausal Women With Advanced Breast Cancer [NCT00241449] | Phase 3 | 51 participants (Actual) | Interventional | 1998-11-30 | Completed | ||
Surgical Therapy With or Without Axillary Node Clearance for Breast Cancer in the Elderly Who Receive Adjuvant Therapy With Tamoxifen. [NCT00002528] | Phase 3 | 473 participants (Actual) | Interventional | 1993-05-31 | Completed | ||
A Phase I, First-in-Human, Dose Escalation Trial of MSC2363318A, a Dual p70S6K/Akt Inhibitor, in Subjects With Advanced Malignancies [NCT01971515] | Phase 1 | 101 participants (Actual) | Interventional | 2013-12-13 | Completed | ||
PAMELA: PAM50 HER2-enriched Phenotype as a Predictor of Early Response to Neoadjuvant Lapatinib Plus Trastuzumab in Stage I to IIIA HER2-positive Breast Cancer [NCT01973660] | Phase 2 | 151 participants (Actual) | Interventional | 2013-10-31 | Completed | ||
Randomized Phase II Study Comparing Two Different Schedules of Palbociclib Plus Second Line Endocrine Therapy in Women With Estrogen Receptor Positive, HER2 Negative Advanced/Metastatic Breast Cancer [NCT02630693] | Phase 2 | 180 participants (Actual) | Interventional | 2016-04-08 | Completed | ||
A Phase I Trial of Sequential High Dose Chemotherapy Regimens Followed by Autologous or Syngeneic Peripheral Blood Stem Cell (PBSC) Rescue in Patients With Persistent Stage III/IV Ovarian Cancer [NCT00003080] | Phase 1 | 0 participants | Interventional | 1996-09-30 | Completed | ||
A Phase II Study of a Selective Estrogen Receptor Modulator (LY353381) vs. Tamoxifen vs. Placebo in Premenopausal Women With and Increased Risk for Breast Cancer [NCT00253539] | Phase 2 | 3 participants (Actual) | Interventional | 2002-01-31 | Completed | ||
Pilot Study of Preservation of Fertility by Ovarian Stimulation Associated With Tamoxifen, and Freezing Oocyte or Embryo Prior Chemotherapy for Breast Cancer [NCT02890082] | Phase 2 | 102 participants (Actual) | Interventional | 2014-02-28 | Active, not recruiting | ||
Tamoxifen Dose Adjustment on ER+ Breast Cancer Patients Based on Genomic and Metabolite Concentrations Analysis [NCT04312347] | 151 participants (Actual) | Interventional | 2019-09-06 | Completed | |||
Protocol of a Randomized Trial for the Management of Small Well-Differentiated and Special Type Carcinomas of the Breast [NCT00006030] | Phase 3 | 0 participants | Interventional | 1992-01-31 | Active, not recruiting | ||
[NCT00000529] | Phase 3 | 0 participants | Interventional | 1992-05-31 | Completed | ||
A Phase II Trial to Evaluate Functional Imaging in Prediction of Response to Abemaciclib for Advanced Hormone Receptor-Positive, HER2-Negative Breast Cancer [NCT06179303] | Phase 2 | 60 participants (Anticipated) | Interventional | 2024-06-01 | Not yet recruiting | ||
A Study to Evaluate the Effect of Letrozole and Tamoxifen on Bone and Lipids in Postmenopausal Women With Breast Cancer [NCT00171704] | Phase 3 | 263 participants (Actual) | Interventional | 2005-04-30 | Completed | ||
A Phase I Study to Evaluate the Safety, Tolerability and Pharmacokinetic Characteristics of TY-302 Capsules in Patients With Advanced Solid Tumors in China [NCT04433494] | Phase 1 | 60 participants (Anticipated) | Interventional | 2020-12-07 | Recruiting | ||
A Randomised, Double-blind, Study Comparing ARIMIDEX™ With NOLVADEX™ as Neo-adjuvant and Adjuvant Treatment in Post-menopausal Women With Large Operable (T2 (≥3cm), T3, N0-2, M0) or Potentially-operable, Locally Advanced (T4b, N0-2, M0), ER+ and/or PR+ Br [NCT00232661] | Phase 3 | 452 participants (Actual) | Interventional | 2000-08-31 | Completed | ||
Pilot Study to Evaluate the Impact of the Use of Alternative and Complementary Therapies on Therapeutic Adherence in Patients Treated With taMoxifen for Early Stage Breast Cancer [NCT04740697] | 200 participants (Anticipated) | Interventional | 2021-02-12 | Recruiting | |||
A Phase 1b Study of Abemaciclib in Combination With Therapies for Patients With Metastatic Breast Cancer [NCT02057133] | Phase 1 | 198 participants (Anticipated) | Interventional | 2014-03-10 | Active, not recruiting | ||
A Randomized, Open-Label, Phase 2 Study of Abemaciclib Plus Tamoxifen or Abemaciclib Alone, in Women With Previously Treated Hormone Receptor-Positive, HER2-Negative, Metastatic Breast Cancer [NCT02747004] | Phase 2 | 234 participants (Actual) | Interventional | 2016-09-14 | Active, not recruiting | ||
A Randomized, Open-Label, Phase 2 Study of the IDO Inhibitor Epacadostat Versus Tamoxifen for Subjects With Biochemical-Recurrent-Only Epithelial Ovarian Cancer, Primary Peritoneal Carcinoma, or Fallopian Tube Cancer Following Complete Remission With Firs [NCT01685255] | Phase 2 | 83 participants (Actual) | Interventional | 2012-08-31 | Terminated(stopped due to Study was terminated by the sponsor for lack of evidence of superiority and slow study accrual.) | ||
A Phase 1 Open-Label Fixed-Sequence Two-Period Crossover Study Of The Effect Of Multiple Doses Of Tamoxifen On PD-0332991 Pharmacokinetics In Healthy Male Volunteers [NCT01821066] | Phase 1 | 25 participants (Actual) | Interventional | 2013-04-30 | Completed | ||
A Prospective, Randomized, Multicentre, Comparative and Open-label Study on Hepatotoxicity of ARIMIDEX Compared With Tamoxifen in Adjuvant Therapy in Postmenopausal Women With Hormone Receptor+ Early Breast Cancer [NCT00537771] | Phase 4 | 384 participants (Actual) | Interventional | 2007-09-30 | Completed | ||
¹³C - Dextromethorphan (DM) Breath Test for Determination of CYP2D6 Enzyme Activity in Patients Receiving Tamoxifen [NCT00873366] | 92 participants (Actual) | Observational | 2009-05-31 | Terminated(stopped due to Funding issues) | |||
CAMBRIA-2: A Phase III, Open-Label, Randomised Study to Assess the Efficacy and Safety of Camizestrant (AZD9833, a Next Generation, Oral Selective Estrogen Receptor Degrader) vs Standard Endocrine Therapy (Aromatase Inhibitor or Tamoxifen) as Adjuvant Tre [NCT05952557] | Phase 3 | 5,500 participants (Anticipated) | Interventional | 2023-10-05 | Recruiting | ||
A Phase III, Randomized, Open-Label, Multicenter Study Evaluating the Efficacy and Safety of Giredestrant Plus Everolimus Compared With The Physician's Choice of Endocrine Therapy Plus Everolimus in Patients With Estrogen Receptor-Positive, HER2-Negative, [NCT05306340] | Phase 3 | 320 participants (Anticipated) | Interventional | 2022-08-03 | Recruiting | ||
An Open-Label, 2-Period Sequential Drug Interaction Study To Evaluate The Effect Of A 100 Mg Dose Of Desvenlafaxine SR On The Pharmacokinetics Of Tamoxifen When Co-Administered In Healthy Post-Menopausal Female Subjects [NCT01189500] | Phase 4 | 30 participants (Actual) | Interventional | 2010-08-31 | Completed | ||
SHORT-HER: MULTICENTRIC RANDOMISED PHASE III TRIAL OF 2 DIFFERENT ADJUVANT CHEMOTHERAPY REGIMENS PLUS 3 VS 12 MONTHS OF TRASTUZUMAB IN HER2 POSITIVE BREAST CANCER PATIENTS [NCT00629278] | Phase 3 | 2,500 participants (Anticipated) | Interventional | 2007-12-31 | Recruiting | ||
Randomized Phase III Crossover Trial of Chemotherapy (Doxorubicin/Cisplatin/Paclitaxel and G-CSF) Versus Hormonal Therapy (Tamoxifen/Megestrol Acetate) in Patients With Stage III & IV or Recurrent Endometrial Cancer [NCT00016341] | Phase 3 | 0 participants | Interventional | 2001-05-31 | Terminated | ||
Phase I/Prospective Randomized Phase II Trial Of the Safety and Efficacy of Tamoxifen in Combination With GDC-0032 Compared With Tamoxifen alONe. [NCT02285179] | Phase 1/Phase 2 | 189 participants (Actual) | Interventional | 2014-11-30 | Completed | ||
An Open Label Trial of Perifosine in Patients Currently Being Treated on Perifosine Trials in Solid Tumors or Multiple Myeloma [NCT00847366] | 10 participants (Actual) | Interventional | 2008-05-31 | Completed | |||
A Feasibility Study of Tamoxifen Prevention of Breast Cancer in Hodgkin's Disease Survivors [NCT00165308] | 29 participants (Actual) | Interventional | 2001-04-30 | Completed | |||
a Phase 3 Randomized Double Blind Evaluation of LY353381 Compared With Tamoxifen in Women With Locally Advanced or Metastatic Breast Cancer. [NCT00034125] | Phase 3 | 0 participants | Interventional | Completed | |||
ExclUsive endocRine Therapy Or Radiation theraPy for Women Aged ≥70 Years With Luminal A-like Early Stage Breast Cancer (EUROPA): a Randomized Phase 3 Trial [NCT04134598] | Phase 3 | 926 participants (Anticipated) | Interventional | 2021-02-08 | Recruiting | ||
Assessing REsponse to Neoadjuvant Taxotere and Trastuzumab in Nigerian Women With HER2-positive Breast Cancer (ARETTA) [NCT03879577] | Phase 2 | 60 participants (Anticipated) | Interventional | 2019-11-25 | Recruiting | ||
Refining Tamoxifen Dose for Premenopausal Breast Cancer Risk Reduction (RENAISSANCE): A Phase II Single Arm Trial [NCT06184750] | Phase 2 | 200 participants (Anticipated) | Interventional | 2024-06-10 | Not yet recruiting | ||
Phase III Comparison of Adjuvant Chemotherapy W/High-Dose Cyclophosphamide Plus Doxorubicin (AC) vs Sequential Doxorubicin Fol by Cyclophosphamide (A-C) in High Risk Breast Cancer Patients With 0-3 Positive Nodes (Intergroup, CALGB 9394) [NCT00590785] | Phase 3 | 60 participants (Anticipated) | Interventional | 1996-08-13 | Completed | ||
Phase 2 Randomized Single-blind Escalating Dose Response Clinical Trial of Tamoxifen Therapy on Mean Percent Predicted Isometric Strength in Amyotrophic Lateral Sclerosis [ALS] [NCT00214110] | Phase 2 | 100 participants | Interventional | 2001-01-31 | Completed | ||
A Randomized, Open-label, Comparative, Multicenter, Phase II Study of the Efficacy and Safety of REGorafenib Versus Tamoxifen in Patients With Platinum-sensitive OVARian Carcinoma and Isolated Biological Progression [NCT02584465] | Phase 2 | 68 participants (Actual) | Interventional | 2015-08-28 | Completed | ||
Phase II Trial of Suberoylanilide Hydroxamic Acid (SAHA, Vorinostat) in Combination With Tamoxifen for Patients With Advanced Breast Cancer Who Have Failed Prior Anti-hormonal Therapy. [NCT00365599] | Phase 2 | 43 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
A Clinical Study for the Evaluation of the Association Between CYP2D6 Genetic Polymorphisms and the Treatment Effect of Tamoxifen in Patients With Metastatic Breast Cancer [NCT00532454] | Phase 2 | 21 participants (Actual) | Interventional | 2006-06-30 | Terminated(stopped due to planned to design a prospective study) | ||
PROTOCOL FOR THE SCOTTISH PREMENOPAUSAL CHEMO-ENDOCRINE TRIAL [NCT00002580] | Phase 3 | 1,000 participants (Anticipated) | Interventional | 1993-06-30 | Completed | ||
Prospective Randomized Study of Ovulation Induction Using Either Tamoxifen or Clomiphene Citrate for Women Who Had Thin Endometrium During Previous Treatment With Clomiphene Citrate [NCT00449514] | 100 participants (Anticipated) | Interventional | 2007-05-31 | Recruiting | |||
A Randomised Trial of Prednisone and Tamoxifen in Patients With Idiopathic Retroperitoneal Fibrosis [NCT00440349] | Phase 2 | 38 participants | Interventional | 2000-10-31 | Active, not recruiting | ||
A Phase II Pilot Trial of Radiation Therapy With Concurrent and Adjuvant Temozolomide, Tamoxifen and Carboplatin (T2C) in the Treatment of Patients With Primary Central Nervous System Malignant Gliomas [NCT00492687] | Phase 2 | 80 participants (Anticipated) | Interventional | 2006-12-31 | Recruiting | ||
A Phase II Pilot Trial of Sutent, Tamoxifen, and Cisplatin in Patients With High-Risk Ocular Melanoma [NCT00489944] | Phase 2 | 50 participants (Anticipated) | Interventional | 2007-05-31 | Recruiting | ||
Phase 2 Study Assessing the Tolerance and Efficacy of Tamoxifen Alone Versus the Association Tamoxifen-RAD001 (Everolimus) in Patients With Anti-aromatase Resistant Breast Metastatic Cancer [NCT01298713] | Phase 2 | 111 participants (Actual) | Interventional | 2008-03-31 | Completed | ||
Effect of Endocrine Therapy Duration on Clinical Outcome of Patients With Hormone Receptor-positive Intraductal Carcinoma of the Breast: A Multicenter, Retrospective, Real-world Study [NCT04666805] | 1,354 participants (Anticipated) | Observational | 2020-07-01 | Active, not recruiting | |||
Pharmacokinetics Study of Combined Treatment Lapatinib and Tamoxifen in Advanced/Metastatic Breast Cancer [NCT00424164] | Phase 1 | 20 participants (Anticipated) | Interventional | 2006-11-30 | Active, not recruiting | ||
A Phase 1 Study of Maprotiline in Combination With Tamoxifen and Temozolomide for Recurrent Glioblastoma [NCT04200066] | Phase 1 | 0 participants (Actual) | Interventional | 2022-06-01 | Withdrawn(stopped due to One of the drugs for the study is not commercially available.) | ||
Epigenetic Priming for Immune Therapy in ER-Positive Breast Cancer in Biomarker Select Population [NCT04190056] | Phase 2 | 1 participants (Actual) | Interventional | 2021-03-11 | Terminated(stopped due to Change in practice patterns) | ||
Phase III Randomized Study of Adjuvant Therapy With Tamoxifen vs Endocrine Ablation vs Tamoxifen Plus Endocrine Ablation vs No Adjuvant Therapy in Patients Under Age 50 With Operable Breast Cancer [NCT00002460] | Phase 3 | 0 participants | Interventional | 1987-09-30 | Active, not recruiting | ||
PHASE III DOUBLE-BLIND, PLACEBO-CONTROLLED, PROSPECTIVE RANDOMIZED COMPARISON OF ADJUVANT THERAPY WITH TAMOXIFEN VS. TAMOXIFEN AND FENRETINIDE IN POSTMENOPAUSAL WOMEN WITH INVOLVED AXILLARY LYMPH NODES AND POSITIVE RECEPTORS [NCT00002646] | Phase 3 | 1,500 participants (Anticipated) | Interventional | 1995-10-31 | Completed | ||
A Comparison of Intensive Sequential Chemotherapy Using Doxorubicin Plus Paclitaxel Plus Cyclophosphamide With High Dose Chemotherapy and Autologous Hematopoietic Progenitor Cell Support for Primary Breast Cancer in Women With 4-9 Involved Axillary Lymph [NCT00002772] | Phase 3 | 602 participants (Actual) | Interventional | 1996-07-31 | Terminated(stopped due to poor accrual) | ||
Randomized Trial of High-dose Epirubicin and Cyclophosphamide x 3 Supported by Peripheral Blood Progenitor Cells Versus Anthracycline and Cyclophosphamide x 4 Followed by Cyclophosphamide, Methotrexate, and 5-fluorouracil x 3 as Adjuvant Treatment for Hig [NCT00002784] | Phase 3 | 344 participants (Actual) | Interventional | 1996-06-30 | Completed | ||
A Large, Uniquely Simple, Randomised Study to Assess Much More Reliably the Balance of Benefits and Risks of Prolonging Adjuvant Tamoxifen Treatment in Early Breast Cancer [NCT00003678] | Phase 3 | 20,000 participants (Anticipated) | Interventional | 1991-05-31 | Active, not recruiting | ||
Study of Tamoxifen and Raloxifene (STAR) for the Prevention of Breast Cancer [NCT00003906] | Phase 3 | 19,747 participants (Actual) | Interventional | 1999-05-31 | Completed | ||
A Phase III Study of High-Dose Chemotherapy Using Busulfan, Melphalan and Thiotepa Versus Cyclophosphamide,Thiotepa, Carboplatin Followed by Autologous Stem Cell Transplantation in Patients With High-Risk Primary Stage II or III (Non-Inflammatory) Breast [NCT00003972] | Phase 3 | 280 participants (Anticipated) | Interventional | 1998-07-31 | Completed | ||
Evaluating Multiparameter Gene Testing as a Predictor of Short Term Endocrine Therapy Response in Hormone Receptor Positive Breast Cancers: The EMPOwER Study [NCT03211572] | Phase 2 | 82 participants (Anticipated) | Interventional | 2017-08-31 | Not yet recruiting | ||
Program for the Assessment of Clinical Cancer Tests (PACCT-1): Trial Assigning Individualized Options for Treatment:The TAILORx Trial [NCT00310180] | Phase 3 | 10,273 participants (Actual) | Interventional | 2006-04-07 | Active, not recruiting | ||
An Exploratory Study to Identify Potential Surrogate Endpoint Biomarkers That Are Modulated by Tamoxifen vs. Placebo in Women With an Increased Risk for Breast Cancer [NCT00096369] | Phase 2 | 130 participants (Anticipated) | Interventional | 2000-02-29 | Terminated(stopped due to accrual goal not met) | ||
Multicenter, Randomized, Open-Label Study To Compare The Efficacy, Tolerance And Quality Of Life Of 5 Years Of Adjuvant Exemestane (Aromasin) Therapy With 2.5 To 3 Years Of Adjuvant Tamoxifen Therapy, Followed By 2 To 2.5 Years Of Exemestane For A Total D [NCT00279448] | Phase 3 | 9,779 participants (Actual) | Interventional | 2002-01-31 | Completed | ||
Randomised Trial Testing Observation (No Radiotherapy) Against Radiotherapy In Women With Low-Risk Completely Excised ER Positive Ductal Carcinoma In Situ (DCIS) Of The Breast On Adjuvant Endocrine Therapy [NCT00077168] | Phase 2 | 2,000 participants (Anticipated) | Interventional | 2004-04-30 | Active, not recruiting | ||
An Open Randomised Clinical Study Comparing ARIMIDEX™ With NOLVADEX™ as Adjuvant Therapies in Post-Menopausal Women With Breast Cancer Already Being Treated With NOLVADEX for at Least Two Years [NCT00286117] | Phase 3 | 448 participants (Actual) | Interventional | 1998-03-31 | Completed | ||
Levels of Circulating Tumor DNA as a Predictive Marker for Early Switch in Treatment for Patients With Metastatic (Stage IV) Breast Cancer: A Phase 2 Randomized, Open-Label Study [NCT05826964] | Phase 2 | 500 participants (Anticipated) | Interventional | 2023-06-12 | Recruiting | ||
A Phase II Pilot Trial of Sorafenib, Tamoxifen and Cisplatin as Adjuvant Therapy for Patients With Stage III Malignant Melanoma [NCT00492505] | Phase 2 | 200 participants (Anticipated) | Interventional | 2007-04-30 | Recruiting | ||
Effects of Selective Estrogen Receptor Modulators on Cognitive Aging: Cognition in the Study of Tamoxifen and Raloxifene [NCT00687102] | Phase 3 | 1,498 participants (Actual) | Interventional | 2001-10-31 | Completed | ||
Treatment of Metastatic Breast Cancer With Fulvestrant Plus Palbociclib or Tamoxifen Plus Palbociclib: A Randomized Pilot Trial With ESR1 Mutation Tested in Circulating Tumor DNA. [NCT02913430] | Early Phase 1 | 7 participants (Actual) | Interventional | 2018-04-24 | Active, not recruiting | ||
A Pilot Study of Tamoxifen, Carboplatin and Topotecan in the Treatment of Recurrent or Refractory Primary Brain or Spinal Cord Tumors or Metastatic Epithelial Cancers With Central Nervous System Metastases [NCT00541138] | Phase 2 | 50 participants (Anticipated) | Interventional | 2003-05-31 | Completed | ||
A Randomised, Controlled, Open Phase II b Study Comparing a Combination of Dose-Intensified Doxorubicin and Docetaxel With or Without Tamoxifen as Preoperative Therapy in Patients With Operable Carcinoma of the Breast (T>=3cm N0-2 M0) [NCT00543829] | Phase 2 | 250 participants (Actual) | Interventional | 1998-04-30 | Completed | ||
A Pilot Clinical Trial to Evaluate the Biological Activity of Fulvestrant (Faslodex) in Breast Ductal Carcinoma (DCIS) [NCT00126464] | 100 participants (Anticipated) | Interventional | 2004-11-30 | Active, not recruiting | |||
Double Blind Placebo Controlled Trial of a Protein Kinase C Inhibitor: Tamoxifen Citrate in Treatment of Acute Mania [NCT00411203] | Phase 3 | 66 participants (Actual) | Interventional | 2003-04-30 | Completed | ||
Phase III Randomized, Placebo-Controlled Clinical Trial Evaluating the Use of Adjuvant Endocrine Therapy +/- One Year of Everolimus in Patients With High-Risk, Hormone Receptor-Positive and HER2/Neu Negative Breast Cancer [NCT01674140] | Phase 3 | 1,939 participants (Actual) | Interventional | 2013-09-12 | Active, not recruiting | ||
Phase 2 Selection Trial of High Dosage Creatine and Two Dosages of Tamoxifen in Amyotrophic Lateral Sclerosis (ALS) [NCT01257581] | Phase 2 | 60 participants (Actual) | Interventional | 2011-03-31 | Completed | ||
A Phase III Clinical Trial Evaluating De-Escalation of Breast Radiation for Conservative Treatment of Stage I, Hormone Sensitive, HER-2 Negative, Oncotype Recurrence Score Less Than or Equal to 18 Breast Cancer [NCT04852887] | Phase 3 | 1,670 participants (Anticipated) | Interventional | 2021-06-07 | Recruiting | ||
PreOperative Endocrine Therapy for Individualised Care With Abemaciclib [NCT04584853] | Phase 3 | 2,500 participants (Anticipated) | Interventional | 2020-12-23 | Recruiting | ||
The Effect of Antidepressants and Gabapentin on Tamoxifen Pharmacokinetics: A Prospective Study [NCT00667121] | 85 participants (Anticipated) | Observational | 2011-03-16 | Active, not recruiting | |||
A Multi-Institutional Phase II Study Evaluating Surrogate Biomarkers of Response to Short Term Oral Vorinostat and Tamoxifen in Women With Newly Diagnosed Breast Cancer [NCT01194427] | Phase 2 | 2 participants (Actual) | Interventional | 2011-03-31 | Terminated(stopped due to Difficulty meeting patient accrual goals) | ||
Feasibility Study for the Determination of Oxysterols in Patients With Breast Cancer Receiving Hormonal Therapy With Tamoxifen or Not [NCT01553903] | Phase 4 | 29 participants (Actual) | Interventional | 2011-12-31 | Completed | ||
Weekly Paclitaxel During Radiation Therapy for Locally Advanced Breat Cancer [NCT00003050] | Phase 2 | 46 participants (Actual) | Interventional | 1997-04-30 | Completed | ||
PROTOCOL FOR THE SCOTTISH POSTMENOPAUSAL CHEMO-ENDOCRINE TRIAL [NCT00002581] | Phase 3 | 1,000 participants (Anticipated) | Interventional | 1993-06-30 | Completed | ||
A Randomised Comparative Trial of Highly Intensive Chemotherapy With Stem Cell Support vs. Relatively Intensive Chemotherapy (CMF 8 Cycles) in Breast Cancer Patients Node Positive Surgery, Having Received Primary Medical Therapy With an Anthracycline Regi [NCT00003680] | Phase 3 | 300 participants (Anticipated) | Interventional | 1998-11-30 | Active, not recruiting | ||
European Cooperative Study of Chemotherapy and Surgery Comparing Adjuvant Doxorubicin Followed by CMF vs. Adjuvant Doxorubicin/Paclitaxel Followed by CMF vs. Primary Doxorubicin/Paclitaxel Followed by CMF in Women With Operable Breast Cancer and T>2 cm [NCT00003013] | Phase 3 | 450 participants (Anticipated) | Interventional | 1996-10-31 | Completed | ||
A Phase II Study Of Safety And Tolerability Of Adjuvant Chemotherapy With Continuous Infusion Paclitaxel And Dose Intense Cyclophosphamide And Hematopoietic Growth Factor Support Followed By Doxorubicin For Stage II-IIIA Breast Cancer Involving Greater Th [NCT00007904] | Phase 2 | 16 participants (Actual) | Interventional | 2000-07-31 | Completed | ||
A Multicenter Randomized Trial of Sequential Epirubicin and Docetaxel Versus Epirubicin in Node Positive Postmenopausal Breast Cancer Patients [NCT00010140] | Phase 3 | 0 participants | Interventional | 1997-08-31 | Active, not recruiting | ||
A Phase I Study of OncoLAR® (Registered Trademark) (NSC 685403) With/Without Tamoxifen in Patients With Osteosarcoma [NCT00001436] | Phase 1 | 24 participants | Interventional | 1995-05-31 | Completed | ||
STEM: A Multicentre Phase 2 Study of SFX-01 Treatment and Evaluation in Patients With Estrogen Receptor (ER) Positive and Human Epidermal Growth Factor Receptor 2 (HER2) Negative Metastatic Breast Cancer Progressing on Either an Aromatase Inhibitor (AI) o [NCT02970682] | Phase 2 | 60 participants (Anticipated) | Interventional | 2016-10-31 | Completed | ||
Randomized And Multicentric Phase III Study Evaluating The Benefit By Using A Chemotherapy With FEC 100 And Docetaxel In Non Metastatic Breast Cancer Which Has Relapsed After A Conservative Surgery [NCT00053911] | Phase 3 | 0 participants | Interventional | 2002-11-30 | Terminated | ||
ZD1839 (IRESSA) In Tamoxifen-Resistant Metastatic Breast Cancer [NCT00080743] | Phase 2 | 2 participants (Actual) | Interventional | 2004-01-31 | Completed | ||
Treatment of Children With Newly Diagnosed Diffuse Pontine Gliomas Using Conventional Radiotherapy and High Dose Tamoxifen [NCT00024336] | Phase 2 | 0 participants | Interventional | 1999-08-31 | Active, not recruiting | ||
An Open Label, Randomized Multicenter Comparative Trial Of 5 Years Adjuvant Exemestane Treatment Versus 5 Years Adjuvant Tamoxifen Treatment In Postmenopausal Women With Early Breast Cancer [NCT00032136] | Phase 3 | 4,400 participants (Anticipated) | Interventional | 2001-12-31 | Completed | ||
Circulating miRNAs as Biomarkers of Hormone Sensitivity in Breast Cancer? Pilot Study. [NCT01612871] | Phase 4 | 39 participants (Actual) | Interventional | 2012-06-27 | Completed | ||
A Phase 1b Study of Talimogene Laherparepvec (T-VEC) in Combination With Chemotherapy or Endocrine Therapy in Patients With Metastatic, Unresectable, or Locoregionally Recurrent HER2-negative Breast Cancer [NCT03554044] | Phase 1 | 20 participants (Actual) | Interventional | 2020-02-05 | Active, not recruiting | ||
A Phase II Trial Of Tipifarnib (R15777, ZARNESTRA) In Combination With Tamoxifen In Subjects With Metastatic Breast Cancer [NCT00052728] | Phase 2 | 0 participants | Interventional | 2002-12-31 | Completed | ||
A Double-Blind Study Examining the Efficacy of the Protein Kinase C Inhibitor Tamoxifen in the Treatment of Acute Mania [NCT00026585] | Phase 2 | 50 participants | Interventional | 2001-11-09 | Completed | ||
A Randomised Trial Of Standard Anthracycline-Based Chemotherapy With Fluorouracil, Epirubicin And Cyclophosphamide (FEC) Or Epirubicin And CMF (Epi-CMF) Versus FEC Followed By Sequential Docetaxel As Adjuvant Treatment For Women With Early Breast Cancer [NCT00033683] | Phase 2 | 0 participants | Interventional | 2001-02-28 | Active, not recruiting | ||
International Breast Cancer Intervention Study II (IBIS-II) (DCIS) [NCT00072462] | Phase 3 | 2,980 participants (Actual) | Interventional | 2003-09-30 | Completed | ||
Open, Single-Arm Phase II Study Assessing Efficacy of ZARNESTRA™ Combined With Tamoxifen in Patients With Advanced or Metastatic Breast Cancer Expressing the Estrogen and/or Progesterone Receptor [NCT00210028] | Phase 2 | 40 participants | Interventional | 2003-08-31 | Terminated | ||
A Pragmatic Randomised, Multicentre Trial Evaluating Optimal Timing of Endocrine Therapy and Radiation Therapy in Early-stage Breast Cancer (REaCT-RETT) [NCT03948568] | Phase 4 | 262 participants (Actual) | Interventional | 2019-09-17 | Completed | ||
A Randomized Phase III Trial Comparing FEC-Chemotherapy vs. EC-Doc-Chemotherapy in Patients With Primary Breast Cancer [NCT00047099] | Phase 3 | 446 participants (Anticipated) | Interventional | 2001-08-31 | Completed | ||
Phase III Randomized Study of Trastuzumab (Herceptin) With or Without Tamoxifen in Women With Progressive, Stage IV, Estrogen or Progesterone Receptor- and HER2/Neu-Positive Breast Cancer [NCT00053339] | Phase 3 | 0 participants (Actual) | Interventional | Withdrawn(stopped due to The study was not activated.) | |||
Evaluation of Response Rate to Pre-Operative Docetaxel + Herceptin Study Part A and Docetaxel Study Part B in Locally Advanced Breast Cancer Patients, Stratified by HER2-Status Trial - PHASE II [(Herceptin Docetaxel Neoadjuvant) HEDON] [NCT00398489] | Phase 2 | 94 participants (Anticipated) | Interventional | 2006-10-31 | Active, not recruiting | ||
A Phase II Study of ZD1839 and Tamoxifen in Patients With Epithelial Ovarian Carcinoma, Cancer of the Fallopian Tube or the Peritoneum Refractory to Platinum- and Taxane-based Therapy [NCT00189358] | Phase 2 | 0 participants | Interventional | Completed | |||
A Randomized Trial of Tamoxifen Combined With Amphotericin B and Fluconazole for Cryptococcal Meningitis [NCT03112031] | Phase 2 | 50 participants (Actual) | Interventional | 2017-10-10 | Completed | ||
A Single Arm Phase II Study of Palbociclib in Combination With Tamoxifen as First Line Therapy for Metastatic Hormone Receptor Positive Breast Cancer: Big Ten Cancer Research Consortium BTCRC-BRE15-016 [NCT02668666] | Phase 2 | 49 participants (Actual) | Interventional | 2016-06-30 | Active, not recruiting | ||
Phase IIB Pre-Surgical Trial of Oral Tamoxifen Versus Transdermal 4-hydroxytamoxifen in Women With DCIS of the Breast [NCT02993159] | Phase 2 | 100 participants (Anticipated) | Interventional | 2017-05-31 | Recruiting | ||
The Study of Avastin (Bevacizumab) to Reverse Acquired Estrogen Independence in Metastatic Breast Cancer Patients Previously Responsive to Hormonal Therapy: A Phase II Trial [NCT00240071] | Phase 2 | 30 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
Preoperative Window of Endocrine Therapy Provides Information to Increase Compliance [NCT01614210] | Phase 2 | 52 participants (Actual) | Interventional | 2012-08-31 | Completed | ||
Palbociclib and Endocrine Therapy for LObular Breast Cancer Preoperative Study (PELOPS): A Randomized Phase II Study of Palbociclib With Letrozole Versus Letrozole Alone for Invasive Lobular Carcinoma and Invasive Ductal Carcinoma [NCT02764541] | Phase 2 | 195 participants (Actual) | Interventional | 2016-05-24 | Active, not recruiting | ||
Phase 2 Study of Neoadjuvant Endocrine Therapy in ER-positive, HER2-negative Early Stage Breast Cancer [NCT05150652] | Phase 2 | 70 participants (Anticipated) | Interventional | 2022-02-18 | Recruiting | ||
A Phase II Randomised, Double-Blind, Stratified, Multi-Centre Trial Comparing the Nolvadex 20 Mg And Placebo Combination To The Nolvadex 20 Mg and ZD1839 (IRESSA™) 250 MG Combination In Patients With Metastatic Breast Cancer And Estrogen Receptor (ER) and [NCT00229697] | Phase 2 | 317 participants (Actual) | Interventional | 2003-10-31 | Completed | ||
A Prospective, Randomized, Open-label Phase III Clinical Study of the Efficacy and Safety of Fluzoparib Combined With Adjuvant Endocrine Therapy Versus Adjuvant Endocrine Therapy for HR+/HER2- SNF3-subtype Early Breast Cancer [NCT05891093] | Phase 3 | 766 participants (Anticipated) | Interventional | 2023-06-01 | Recruiting | ||
Adjuvant Endocrine Therapy in Postmenopausal Patients With HR +ve BC With Good to Moderate Differentiation - ARNO (Arimidex + Nolvadex). Primary Treatment for 2 Years With Tamoxifen Thereafter Randomisation to: Tamoxifen 3 Years or Anastrozole 3 Years. [NCT00291759] | Phase 3 | 3,858 participants (Actual) | Interventional | 1996-01-31 | Completed | ||
A Prospective, Multi-Centre, Randomised, Open Parallel Group Study to Compare the Effectiveness and Compatibility of ARIMIDEX (ZD 1033) With NOLVADEX After a Prior 2 Years' Treatment With Tamoxifen in Adjuvant Therapy of Breast Carcinoma in Postmenopausal [NCT00287534] | Phase 2 | 1,059 participants (Anticipated) | Interventional | 1996-11-30 | Completed | ||
20-347 NCT Number Title A Single Arm Phase II Study of ADjuvant Endocrine Therapy, Pertuzumab, and Trastuzumab for Patients With Anatomic Stage I Hormone Receptor-positive, HER2-positive Breast Cancer (ADEPT) [NCT04569747] | Phase 2 | 375 participants (Anticipated) | Interventional | 2021-01-11 | Recruiting | ||
A Prospective, Randomized, Multicenter, Open-label Comparison of Pre-surgical Combination of Trastuzumab and Pertuzumab With Concurrent Taxane Chemotherapy or Endocrine Therapy Given for Twelve Weeks With a Quality of Life Assessment of Trastuzumab, Pertu [NCT03272477] | Phase 2 | 257 participants (Actual) | Interventional | 2017-10-05 | Active, not recruiting | ||
Cancer Risk and Biomarkers of Tamoxifen Chemoprevention [NCT00295100] | Phase 2 | 78 participants | Interventional | 2000-09-30 | Completed | ||
Use of Changes in CA 125 Doubling Time to Detect Activity of Cytostatic Agents in Women Relapsing With Ovarian Carcinoma. Study 1-Tamoxifen [NCT00305838] | Phase 2 | 200 participants (Anticipated) | Interventional | 2004-03-31 | Recruiting | ||
A Randomized Phase III Study Comparing Tamoxifen vs. Tamoxifen + Aminoglutethimide in Postmenopausal, Hormone Receptor-positive Patients [NCT00309491] | Phase 3 | 2,021 participants (Actual) | Interventional | 1990-12-31 | Completed | ||
Comparison of the Effectiveness of Neoadjuvant Chemotherapy and the Outcomes Associated With Chemo-induced Amenorrhea Between Docetaxel Plus Epirubicin, and Docetaxel Plus Epirubicin Plus Cyclophosphamide as Neoadjuvant Chemotherapy for Operable Premenopa [NCT01503905] | 600 participants (Anticipated) | Interventional | 2011-12-31 | Recruiting | |||
A Phase III, Open-Label, Prospective, Randomized, Multicenter, Neo-adjuvant Study of Chemotherapy Versus Endocrine Therapy in Premenopausal Patient With Hormone Responsive, HER2 Negative, Lymph Node Positive Breast Cancer [NCT01622361] | Phase 3 | 290 participants (Anticipated) | Interventional | 2012-06-30 | Recruiting | ||
A Prospective, Randomised, Multi-centre Phase II Study Evaluating the Adjuvant, Neoadjuvant or Palliative Treatmant With Tamoxifen +/- GnRH Analogue Versus Aromatase Inhibitor + GnRH Analogue in Male Breast Cancer Patients [NCT01638247] | Phase 3 | 56 participants (Actual) | Interventional | 2012-08-31 | Completed | ||
UKCCCR RANDOMISED TRIAL OF ADJUVANT ENDOCRINE THERAPY AND CHEMOTHERAPY IN WOMEN WITH EARLY BREAST CANCER, THE ADJUVANT BREAST CANCER (ABC) TRIAL [NCT00002582] | Phase 3 | 6,000 participants (Anticipated) | Interventional | 1993-06-30 | Completed | ||
Neoadjuvant Endocrine Therapy in Breast Cancer. Real Clinical Practice in Russia [NCT05800197] | 300 participants (Anticipated) | Observational | 2014-04-15 | Recruiting | |||
Impact of Obesity on the Efficacy of Endocrine Therapy With Aromatase Inhibitors in Postmenopausal Patients With Early Breast Cancer [NCT01758146] | Phase 3 | 412 participants (Anticipated) | Interventional | 2012-01-31 | Recruiting | ||
Comparative Study for the Degree of Biological Changes After Short-term 2 Weeks and 4 Weeks Preoperative Endocrine Therapy in Luminal Breast Cancer [NCT04023292] | Phase 2 | 185 participants (Anticipated) | Interventional | 2019-07-31 | Recruiting | ||
A Randomized Proof-of-concept Phase II Trial Comparing Therapy Based on Tumor Molecular Profiling Versus Conventional Therapy in Patients With Refractory Cancer. [NCT01771458] | Phase 2 | 742 participants (Actual) | Interventional | 2012-10-31 | Active, not recruiting | ||
Combination Therapy With Isotretinoin and Tamoxifen Expected to Provide Complete Protection Against Severe Acute Respiratory Syndrome Coronavirus [NCT04389580] | Phase 2 | 160 participants (Anticipated) | Interventional | 2021-09-30 | Not yet recruiting | ||
Neoadjuvant Intratumoral Injection of Dendritic Cells in Breast Cancer Translation of Biotechnology Into the Clinic [NCT00499083] | Phase 2 | 17 participants (Actual) | Interventional | 2006-05-01 | Completed | ||
Phase IIA Trial of Acolbifene (20 mg) vs Low Dose Tamoxifen (5 mg) in Pre-Menopausal Women at High Risk for Development of Breast Cancer [NCT05941520] | Phase 2 | 80 participants (Anticipated) | Interventional | 2024-03-01 | Not yet recruiting | ||
Treatment of Unfavorable Bleeding Patterns in Contraceptive Implant Users [NCT02903121] | Phase 4 | 109 participants (Actual) | Interventional | 2017-01-20 | Completed | ||
Preoperative Neoadjuvant Hormonal Therapy and Neoadjuvant Chemotherapy for Stage IIIB and IV Breast Cancer Patients in Dharmais National Cancer Center Hospital, Indonesia [NCT02995772] | Phase 3 | 122 participants (Actual) | Interventional | 2011-11-30 | Completed | ||
A Randomized Controlled Trial of Tamoxifen Versus Etoposide for Patients With First Recurrence of Glioblastoma Multiforme [NCT04765098] | Phase 2 | 60 participants (Anticipated) | Interventional | 2022-01-28 | Recruiting | ||
A Pilot Clinical Trial to Evaluate the Biological Activity of Fulvestrant in Breast Ductal Carcinoma in Situ (DCIS) [NCT00183963] | Phase 2 | 4 participants (Actual) | Interventional | 2006-08-31 | Terminated(stopped due to Insufficient accrual) | ||
ETHAN: A Phase II Study Comparing Different Endocrine THerapies for mAle Breast caNcer [NCT05501704] | Phase 2 | 60 participants (Anticipated) | Interventional | 2023-10-11 | Recruiting | ||
Adjuvant Therapy for Post/Perimenopausal Patients With Node Positive Breast Cancer Who Are Suitable for Endocrine Therapy Alone. [NCT00002529] | Phase 3 | 452 participants (Actual) | Interventional | 1993-05-31 | Completed | ||
Sequential Adjuvant Chemotherapy With Doxorubicin, Taxol, and Cyclophosphamide for Stage II or III Resectable Breast Cancer With Four or More Involved Axillary Lymph Nodes [NCT00002679] | Phase 2 | 89 participants (Actual) | Interventional | 1994-02-28 | Completed | ||
Tamoxifen Versus Anastrozole, Alone or in Combination With Zoledronic Acid, in Premenopausal, Hormone Receptor-positive Breast Cancer Patients (Stage I, II) [NCT00295646] | Phase 3 | 1,803 participants (Actual) | Interventional | 1999-06-30 | Completed | ||
[NCT00375622] | Phase 2 | 60 participants | Interventional | 2005-02-28 | Completed | ||
Neoadjuvant Endocrine Therapy in Hormone Receptor-Positive HER2-Negative Node-Negative Breast Cancer Patients to Assess Responses and Mechanisms of Endocrine Resistance [NCT03219476] | Phase 2 | 37 participants (Actual) | Interventional | 2017-02-05 | Active, not recruiting | ||
MINDACT (Microarray In Node-Negative and 1 to 3 Positive Lymph Node Disease May Avoid Chemotherapy): A Prospective, Randomized Study Comparing the 70-Gene Signature With the Common Clinical-Pathological Criteria in Selecting Patients for Adjuvant Chemothe [NCT00433589] | Phase 3 | 6,600 participants (Anticipated) | Interventional | 2007-02-28 | Completed | ||
Comparison in the Change of Proliferation Index Between Fulvestrant and Tamoxifen in Cyclin D1 +, Estrogen Receptor + Breast Cancer [NCT02936206] | Phase 1 | 2 participants (Actual) | Interventional | 2016-10-31 | Terminated(stopped due to low accrual rate) | ||
Low-Dose Tamoxifen to Reduce High Background Parenchymal Uptake on Molecular Breast Imaging [NCT02979301] | 22 participants (Actual) | Interventional | 2017-03-01 | Completed | |||
A Phase II Study of the Determinants of Transdermal Drug Delivery to the Normal and the Radiated Breast [NCT04009044] | Phase 2 | 156 participants (Anticipated) | Interventional | 2020-02-17 | Recruiting | ||
Double-Blind Randomized Trial of Tamoxifen Versus Placebo in Patients With Node Positive or High Risk Node Negative Breast Cancer Who Have Completed CMF, CEF, or AC Adjuvant Chemotherapy [NCT00002542] | Phase 3 | 672 participants (Actual) | Interventional | 1993-07-20 | Completed | ||
Phase II Trial of Sequential High-Dose Alkylating Agents in Metastatic Breast Cancer [NCT00002680] | Phase 2 | 40 participants (Actual) | Interventional | 1994-02-28 | Completed | ||
A Randomized Comparison Of Medroxyprogesterone Acetate (MA) And Observation For Prevention Of Endometrial Pathology In Postmenopausal Breast Cancer Patients Treated With Tamoxifen, Phase III [NCT00002920] | Phase 3 | 313 participants (Actual) | Interventional | 1997-03-31 | Completed | ||
Randomized Double-Blind Trial in Postmenopausal Women With Primary Breast Cancer Who Have Received Adjuvant Tamoxifen for 2-3 Years, Comparing Subsequent Adjuvant Exemestane Treatment With Further Tamoxifen [NCT00003418] | Phase 3 | 4,400 participants (Anticipated) | Interventional | 1998-02-28 | Active, not recruiting | ||
Randomised Trial of Tamoxifen Versus Placebo for the Treatment of Inoperable Hepatocellular Carcinoma [NCT00003424] | Phase 3 | 300 participants (Anticipated) | Interventional | 1997-04-30 | Completed | ||
Reliable Assessment of the Efficacy and Safety of Prolonging the Use of Adjuvant Tamoxifen: A Large, Simple, Randomised Study [NCT00003016] | Phase 3 | 20,000 participants (Anticipated) | Interventional | 1995-10-31 | Active, not recruiting | ||
Efficacy and Safety of Ospemifene in the Treatment of Vulvar and Vaginal Atrophy (VVA) in Postmenopausal Women: A Phase II Dose Ranging, 12-Week, Randomized , Double-Blind, Placebo-Controlled, Parallel-Group Study Comparing Oral Ospemifene 5 mg, 15 mg and [NCT00630539] | Phase 2 | 126 participants (Actual) | Interventional | 2007-08-31 | Completed | ||
LA LEAST- Luminal A, Limited Endocrine Adjuvant Systemic Therapy. A Trial of Abbreviated Hormone Therapy for Low Risk Hormone Receptor Positive, HER2 Negative Early Breast Cancer [NCT03917082] | Phase 2 | 290 participants (Anticipated) | Interventional | 2019-09-23 | Active, not recruiting | ||
A Phase III Study of Doxorubicin-Cyclophosphamide Therapy Followed by Paclitaxel or Docetaxel Given Weekly or Every 3 Weeks in Patients With Axillary Node-Positive Breast Cancer [NCT00004125] | Phase 3 | 0 participants | Interventional | 1999-11-16 | Completed | ||
Phase I Study of Z-Endoxifen as a Hormonal Therapy for Breast Cancer [NCT01327781] | Phase 1 | 62 participants (Actual) | Interventional | 2011-03-25 | Active, not recruiting | ||
A Study of Weekly Doxorubicin and Daily Oral Cyclophosphamide Plus G-CSF Followed by Weekly Paclitaxel as Neoadjuvant Therapy for Resectable, Hormone Receptor Negative or Hormone Receptor Positive, HER-2/Neu Positive Breast Cancer Followed by a Novel Regi [NCT00194779] | Phase 2 | 50 participants (Actual) | Interventional | 2003-10-31 | Completed | ||
Phase 1/2 Study of Intravaginal Tamoxifen (DARE-VVA1): Randomized, Double-blind, Placebo-controlled Study of Safety, Pharmacokinetics and Pharmacodynamics in Postmenopausal Participants With Moderate to Sever Vulvar and Vaginal Atrophy [NCT05378269] | Phase 1/Phase 2 | 17 participants (Actual) | Interventional | 2021-11-22 | Completed | ||
Assessing the REsponse Rate of Weekly Neo-adjuvanT pacliTAxel (Taxol) in Nigerian Women With Breast Cancer (ARETTA) [NCT03058939] | Phase 2 | 0 participants (Actual) | Interventional | 2018-11-30 | Withdrawn(stopped due to Study never activated to enrollment.) | ||
Analysis of Therapy Sequence in Women With Hormone Receptor-positive, HER2-negative Metastatic Breast Cancer in Russia: A Multicentre Retrospective Observational Real-life Study. [NCT04852081] | 1,000 participants (Anticipated) | Observational | 2021-01-01 | Recruiting | |||
Treatment Effect of Tamoxifen on Patients With DMD [NCT02835079] | Phase 1 | 19 participants (Actual) | Interventional | 2016-11-30 | Completed | ||
Tamoxifen Therapy to Treat Pulmonary Arterial Hypertension [NCT03528902] | Phase 2 | 18 participants (Actual) | Interventional | 2018-10-01 | Completed | ||
Fertility Preservation Using Tamoxifen and Letrozole in Estrogen Sensitive Tumors Trial [NCT03011684] | Phase 3 | 144 participants (Anticipated) | Interventional | 2016-07-21 | Recruiting | ||
Efficacy Of Tocotrienol a Natural Vitamin E In Biopsy Wound. [NCT01579227] | 101 participants (Anticipated) | Observational | 2012-01-31 | Active, not recruiting | |||
Cisplatin, Doxorubicin and Tamoxifen in the Treatment of Incurable Soft Tissue and Endocrine Malignancies [NCT00002608] | Phase 2 | 30 participants (Anticipated) | Interventional | 1994-05-31 | Completed | ||
The HOT Study: Hormone Replacement Therapy Opposed by Low Dose Tamoxifen. A Phase III Trial of Breast Cancer Prevention With Low Dose Tamoxifen in HRT Users. [NCT01579734] | Phase 3 | 1,884 participants (Actual) | Interventional | 2002-03-31 | Active, not recruiting | ||
A Phase II Prospective Trial Correlating Progression Free Survival With CYP2D6 Activity in Patients With Metastatic Breast Cancer Treated With Single Agent Tamoxifen [NCT01124695] | Phase 2 | 124 participants (Actual) | Interventional | 2011-01-07 | Completed | ||
Adjuvant Ovarian Suppression Plus Aromatase Inhibitor or Tamoxifen for Hormone Receptor-Positive Breast Cancer in Women Younger Than 35: A Multicenter Randomized Clinical Trial [NCT02914158] | Phase 3 | 680 participants (Anticipated) | Interventional | 2016-03-30 | Recruiting | ||
Phase II Open Label Study of Everolimus in Combination With Anti-estrogen Therapy in Hormone Receptor-Positive HER2-Negative Advanced Breast Cancer [NCT02291913] | Phase 2 | 48 participants (Actual) | Interventional | 2014-12-18 | Completed | ||
QUADRANTECTOMY PLUS AXILLARY DISSECTION VERSUS QUADRANTECTOMY ALONE IN MAMMOGRAPHIC STAGE T1N0 BREAST CANCER PATIENTS AGED OVER 65 YEARS [NCT00002720] | Phase 3 | 642 participants (Anticipated) | Interventional | 1995-12-31 | Completed | ||
A Randomized Trial of High-Dose Chemotherapy and Autologous Stem Cell Therapy Versus Standard Therapy in Women With Metastatic Breast Cancer Who Have Responded to Anthracycline or Taxane-Based Induction Chemotherapy [NCT00003032] | Phase 3 | 224 participants (Actual) | Interventional | 1997-04-25 | Completed | ||
A Randomized Trial of Antiestrogen Therapy Versus Combined Antiestrogen and Octreotide Therapy in the Adjuvant Treatment of Breast Cancer in Post-Menopausal Women [NCT00002864] | Phase 3 | 667 participants (Actual) | Interventional | 1996-09-24 | Completed | ||
A RANDOMIZED TRIAL COMPARING PREOPERATIVE DOXORUBICIN (ADRIAMYCIN)/CYCLOPHOSPHAMIDE (AC) TO PREOPERATIVE AC FOLLOWED BY PREOPERATIVE DOCETAXEL (TAXOTERE) AND TO PREOPERATIVE AC FOLLOWED BY POSTOPERATIVE DOCETAXEL IN PATIENTS WITH OPERABLE CARCINOMA OF THE [NCT00002707] | Phase 3 | 2,411 participants (Actual) | Interventional | 1995-12-31 | Completed | ||
PROSPECTIVE RANDOMISED EVALUATION OF HIGH-INTENSITY CHEMOTHERAPY WITH PERIPHERAL BLOOD PROGENITOR SUPPORT IN PATIENTS WITH HIGH RISK BREAST CANCER [NCT00002755] | Phase 3 | 600 participants (Anticipated) | Interventional | 1995-11-30 | Completed | ||
Reversing Therapy Resistance With Epigenetic-immune Modification: Phase II Trial of Vorinostat, Tamoxifen and Pembrolizumab in Hormone Receptor Expressing Advanced Breast Cancer [NCT02395627] | Phase 2 | 38 participants (Actual) | Interventional | 2015-05-04 | Terminated(stopped due to Insufficient efficacy in an unselected patient population) | ||
Long-Term Safety of 30 mg and 60 mg Oral Daily Dose of Ospemifene in the Treatment of Vulvar and Vaginal Atrophy (VVA) in Postmenopausal Women With Intact Uterus: A 40 Week Randomized, Double Blind, Placebo Controlled, Follow-Up to Protocol 15-50310. [NCT01585558] | Phase 3 | 180 participants (Actual) | Interventional | 2006-05-16 | Completed | ||
Combination of Chemopreventive Agents (All- Trans Retinoic Acid and Tamoxifen) as Potential Treatment for the Lung Complication of COVID-19 [NCT04568096] | Phase 2 | 160 participants (Anticipated) | Interventional | 2020-11-30 | Not yet recruiting | ||
A Randomised Comparative Trial of Adriamycin + Taxotere vs. Adriamycin + Cyclophosphamide as Primary Medical Therapy for Patients With Potentially Operable Breast Cancer Greater Than or Equal to 3 cm Diameter, Locally Advanced, or Inflammatory Disease [NCT00003679] | Phase 3 | 350 participants (Anticipated) | Interventional | 1998-11-30 | Active, not recruiting | ||
RANDOMIZED PHASE II STUDY IN FIRST LINE HORMONAL TREATMENT FOR METASTATIC BREAST CANCER WITH EXEMESTANE OR TAMOXIFEN IN POSTMENOPAUSAL PATIENTS [NCT00002777] | Phase 3 | 342 participants (Anticipated) | Interventional | 1996-05-31 | Completed | ||
A Clinical Trial to Evaluate the Benefit of Adding Octreotide (SMS 201-995 PA LAR) to Tamoxifen Alone or to Tamoxifen and Chemotherapy in Patients With Axillary Node-Negative, Estrogen-Receptor-Positive, Primary Invasive Breast Cancer [NCT00002967] | Phase 3 | 0 participants | Interventional | 1997-05-31 | Completed | ||
Phase II Clinical Trial of N-(4-hydroxyphenyl) Retinamide (4-HPR) and Tamoxifen in Breast Neoplasia, Administration During the Period Between the Diagnostic Core Biopsy and Definitive Surgery [NCT00003099] | Phase 2 | 52 participants (Actual) | Interventional | 1996-05-31 | Completed | ||
Tamoxifen for the Treatment of Unfavorable Bleeding Patterns in Etonogestrel Contraceptive Implant Users [NCT02070692] | Phase 4 | 56 participants (Actual) | Interventional | 2014-02-28 | Completed | ||
A Randomized Phase III Study Comparing Cyclophosphamide + Methotrexate + Fluorouracil vs. Goserelin + Tamoxifen in Premenopausal, Hormone Receptor-positive, Lymph Node-positive or -Negative Patients [NCT00309478] | Phase 3 | 1,099 participants (Actual) | Interventional | 1990-12-31 | Completed | ||
[NCT02062489] | Phase 3 | 688 participants (Anticipated) | Interventional | 2014-05-31 | Recruiting | ||
Neoadjuvant Endocrine Therapy in Locally Advanced Hormone Receptor Positive Breast Cancer in a Low-Resource, Middle-Income Setting (Guatemala) [NCT02806544] | Phase 2 | 35 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
Phase II Study of Hormone Therapy With Tamoxifen in Patients With Well Differentiated Neuroendocrine Tumors and Hormone Receptor Positive Expression [NCT03870399] | Phase 2 | 23 participants (Actual) | Interventional | 2019-03-13 | Active, not recruiting | ||
Open Label, Phase II Trial of Neoadjuvant TAK-228 Plus Tamoxifen in Patients With Estrogen Receptor (ER)-Positive, Human Epidermal Growth Factor Receptor 2 (HER2)-Negative Breast Cancer [NCT02988986] | Phase 2 | 28 participants (Actual) | Interventional | 2017-04-24 | Completed | ||
Phase I/II Trial of Tamoxifen Following Epigenetic Regeneration of Estrogen Receptor Using Decitabine and LBH 589 in Patients With Triple Negative Metastatic Breast Cancer [NCT01194908] | Phase 1/Phase 2 | 5 participants (Actual) | Interventional | 2010-07-31 | Terminated(stopped due to Slow accrual) | ||
Why Antiprogestrone (Mifepristone) and Cyp 26 Inhibitor Must be Combined With Tamoxifen or ( Tamoxifen and Retinoic Acid) for Treating Early Breast Cancer [NCT05016349] | Phase 3 | 160 participants (Anticipated) | Interventional | 2021-08-31 | Not yet recruiting | ||
An Investigator Initiated Registry of Simple Oral Therapy for Low Risk Breast Cancer (SOLR) [NCT03238703] | Phase 4 | 0 participants (Actual) | Interventional | 2018-09-01 | Withdrawn(stopped due to Administrative closure based on sponsor recommendation, prior to subject enrollment) | ||
A Randomized, Multicenter, Double-blind, Phase 3 Study of Amcenestrant (SAR439859) Versus Tamoxifen for the Treatment of Patients With Hormone Receptor-positive, Human Epidermal Growth Factor Receptor 2-negative or Positive, Stage IIB-III Breast Cancer Wh [NCT05128773] | Phase 3 | 3 participants (Actual) | Interventional | 2022-02-17 | Terminated(stopped due to Sponsor decision to prematurely stop the study, not linked to any safety concern) | ||
Pilot Trial of Paclitaxel-Herceptin Adjuvant Therapy for Early Stage Breast Cancer [NCT00003992] | Phase 2 | 200 participants (Actual) | Interventional | 1999-08-31 | Completed | ||
Predicting an Accurate Tamoxifen Dose: a Feasibility Study in Patients With Hormone Sensitive Breast Cancer [NCT05525481] | Phase 4 | 100 participants (Anticipated) | Interventional | 2022-11-01 | Recruiting | ||
A Phase III Study to Evaluate Letrozole as Adjuvant Endocrine Therapy for Postmenopausal Women With Receptor (ER and/or PgR) Positive Tumors [NCT00004205] | Phase 3 | 8,028 participants (Actual) | Interventional | 1998-03-31 | Completed | ||
PROTOCOL FOR THE SCOTTISH CHEMO-ENDOCRINE TRIAL D [NCT00002579] | Phase 3 | 2,000 participants (Anticipated) | Interventional | 1993-03-31 | Completed | ||
Twin Cities Brachytherapy Study for Ductal Carcinoma in Situ A Phase II Trial [NCT00290654] | Phase 2 | 45 participants (Actual) | Interventional | 2002-12-31 | Terminated(stopped due to Unable to recruit further patients.) | ||
Phase III Randomized Study of Luteal Phase vs. Follicular Phase Surgical Oophorectomy and Tamoxifen in Premenopausal Women With Metastatic Hormone Receptor-Positive Breast Cancer [NCT00293540] | Phase 3 | 249 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
A Randomized Phase II Trial of Everolimus and Letrozole or Hormonal Therapy (Tamoxifen/Medroxyprogesterone Acetate) in Women With Advanced, Recurrent, or Persistent Endometria Carcinoma [NCT02228681] | Phase 2 | 74 participants (Actual) | Interventional | 2015-02-28 | Active, not recruiting | ||
A Phase 1 Study of an Oral p38 MAPK Inhibitor in Patients With Advanced Cancer [NCT01393990] | Phase 1 | 89 participants (Actual) | Interventional | 2008-09-04 | Completed | ||
A Pilot Study Evaluating Megestrol Acetate Modulation in Advanced Breast Cancer With Positive Hormonal Receptor [NCT03024580] | Phase 2 | 20 participants (Anticipated) | Interventional | 2017-03-06 | Recruiting | ||
PROMOTE Study: Prediction of Response Of HorMOnal Treatment in Advanced and Recurrent Endometrial Cancer [NCT03621904] | 150 participants (Anticipated) | Observational [Patient Registry] | 2022-10-15 | Recruiting | |||
International Breast Cancer Intervention Study: A Multicentre Trial of Tamoxifen to Prevent Breast Cancer [NCT00002644] | Phase 3 | 7,154 participants (Actual) | Interventional | 1994-01-31 | Active, not recruiting | ||
The Effects of Short-term Preoperative Treatment With Hormonal Therapy on Gene Profiles in Breast Cancer [NCT04129216] | Phase 2 | 30 participants (Anticipated) | Interventional | 2019-02-20 | Active, not recruiting | ||
Evaluation of the Relationship Between Drug Therapy, Food Consumption, Body Composition and Plasma Micronutients Levels With the Expression of Genes Related to Metabolism, Aging and Immunity in Women With Breast Cancer. [NCT04389424] | 300 participants (Anticipated) | Observational | 2017-09-01 | Recruiting | |||
A Phase II Multi-Institutional Study of Concurrent Radiotherapy, Palbociclib, and Hormone Therapy for Treatment of Bone Metastasis in Breast Cancer Patients [NCT03691493] | Phase 2 | 38 participants (Actual) | Interventional | 2019-02-08 | Completed | ||
A Pilot Trial Comparing Doxorubicin and Paclitaxel Induced Apoptosis in Locally Advanced Breast Cancer [NCT00003035] | Phase 2 | 40 participants (Anticipated) | Interventional | 1997-03-31 | Completed | ||
A Phase II Study of Preoperative Dose-Dense Chemotherapy With Sequential Doxorubicin and Docetaxel for Initial Treatment of Operable and Inoperable Stage II-IIIB Breast Cancer [NCT00003953] | Phase 2 | 39 participants (Actual) | Interventional | 1999-02-28 | Completed | ||
A Phase Ib Dose Escalation Study of the Combination of LEE011 With Letrozole and Dose Expansion of LEE011 With Hormonal Therapy for the Treatment of Pre-(With Goserelin) and Postmenopausal Women With Hormone Receptor Positive, HER2-negative, Advanced Brea [NCT02333370] | Phase 1 | 88 participants (Actual) | Interventional | 2015-02-04 | Completed | ||
An Open-Label, Non-randomised, Parallel Group, Multicentre, Phase I Study to Assess the Safety and Effect of Olaparib at Steady State on the Pharmacokinetics of the Anti-hormonal Agents Anastrozole, Letrozole and Tamoxifen at Steady State, and the Effect [NCT02093351] | Phase 1 | 79 participants (Actual) | Interventional | 2014-09-01 | Completed | ||
A Prospective Assessment of Loss of Grip Strength by Baseline BMI in Breast Cancer Patients Receiving Adjuvant Third-generation Aromatase Inhibitors and Tamoxifen [NCT01896050] | 115 participants (Actual) | Observational | 2009-09-30 | Completed | |||
A Randomised, Double Blinded, Six-armed Placebo Controlled Study to Investigate Optimal Dose of Tamoxifen With the Most Favourable Side Effect Spectre and With Mammography Density Reduction Non-inferior to That of 20 mg Tamoxifen (Karisma 2) [NCT03346200] | Phase 2 | 1,440 participants (Actual) | Interventional | 2016-11-30 | Completed | ||
Low Dose TamOxifen and LifestylE Changes for bReast cANcer prevenTion: a Randomized Phase II Biomarker Trial in Subjects at Increased Risk [NCT06033092] | Phase 2 | 200 participants (Anticipated) | Interventional | 2023-09-01 | Not yet recruiting | ||
Phase I Trial of Endoxifen Gel Versus Placebo Gel in Women Undergoing Breast Surgery [NCT03317405] | Phase 1 | 32 participants (Actual) | Interventional | 2018-10-31 | Active, not recruiting | ||
An Open, Randomized, Multi-center, Phase 2 Trial of Tamoxifen and Letrozole in Recurrent and Persistent Squamous Cell Carcinoma of the Cervix: the Efficacy and New Biomarkers [NCT02482740] | Phase 2 | 44 participants (Anticipated) | Interventional | 2015-05-31 | Recruiting | ||
Effects of Cimicifuga Racemosa L. Nutt Sexuality of Women With Breast Cancer Using Tamoxifen or Aromatase Inhibitor [NCT02467686] | Phase 4 | 60 participants (Anticipated) | Interventional | 2014-01-31 | Recruiting | ||
Endocrine Treatment Alone as Primary Treatment for Elderly Patients With Estrogen Receptor Positive Operable Breast Cancer and Low Recurrence Score [NCT02476786] | Phase 2 | 50 participants (Anticipated) | Interventional | 2017-01-17 | Recruiting | ||
A Randomized Open-label Phase II Multicenter Trial Assessing the Efficacy and Safety of tamOxifen Plus LY2228820 in Advanced or Metastatic Breast Cancer Progressing on aromatasE Inhibitors [NCT02322853] | Phase 2 | 8 participants (Actual) | Interventional | 2015-01-31 | Terminated(stopped due to lack of recruitment) | ||
Phase III Trial of Tamoxifen Alone vs. Tamoxifen Plus Radiation Therapy for Good Risk Duct Carcinoma In-Situ (DCIS) of the Female Breast [NCT00003857] | Phase 3 | 636 participants (Actual) | Interventional | 1999-12-31 | Completed | ||
Neoadjuvant Treatment of Breast Cancer - a Prospective Observational Study, PANnon ONCology (PANONC) Group Non-commercial Clinical Trial [NCT05131893] | 300 participants (Anticipated) | Observational [Patient Registry] | 2022-03-31 | Not yet recruiting | |||
Elacestrant for Treating ER+/HER2- Breast Cancer Patients With ctDNA Relapse [NCT05512364] | Phase 3 | 220 participants (Anticipated) | Interventional | 2023-12-15 | Not yet recruiting | ||
A Randomised Trial of Early Detection of Molecular Relapse With Circulating Tumour DNA Tracking and Treatment With Palbociclib Plus Fulvestrant Versus Standard Endocrine Therapy in Patients With ER Positive HER2 Negative Breast Cancer [NCT04985266] | Phase 2 | 1,100 participants (Anticipated) | Interventional | 2022-03-30 | Recruiting | ||
Phase II Study of Bicalutamide and Dutasteride for Prostate Cytoreduction Prior to Permanent Implant I-125 Prostate Brachytherapy [NCT00866554] | Phase 2 | 60 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
Utilization of Decision Aids for Tamoxifen Treatment in Breast Cancer Patients: A Randomized Controlled Trial. [NCT02488603] | 360 participants (Anticipated) | Interventional | 2015-08-31 | Not yet recruiting | |||
A Pilot Study of Tamoxifen in Oesophageal Cancer [NCT02513849] | Phase 1 | 20 participants (Anticipated) | Interventional | 2015-12-31 | Recruiting | ||
Phase II Trial of Estrogen Receptor Targeted Treatment of Non-Muscle Invasive Bladder Cancer With Tamoxifen. [NCT02197897] | Phase 2 | 15 participants (Actual) | Interventional | 2015-04-01 | Completed | ||
Phase II Study of Everolimus Beyond Progression in Postmenopausal Women With Advanced, Hormone Receptor Positive Breast Cancer [NCT02269670] | Phase 2 | 3 participants (Actual) | Interventional | 2014-11-25 | Terminated(stopped due to Slow to accrual) | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |