Page last updated: 2024-11-09

tamoxifen

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID2733526
CHEMBL ID83
CHEBI ID41774
SCHEMBL ID4084
MeSH IDM0021024

Synonyms (188)

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

Research Excerpts

Overview

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.

ExcerptReferenceRelevance
"Tamoxifen is a selective estrogen receptor modulator widely used in oncology and reproductive endocrinology. "( Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha.
Bravo-Gómez, ME; Camacho, J; Cooney, AJ; García-Becerra, R; Hernández-Gallegos, E; Larrea, F; Morales-Ríos, MS; Ordaz-Rosado, D; Pérez-Alvarez, V; Rivera-Guevara, C, 2010
)
2.07
"Tamoxifen (TAM) is a widely used drug in the prophylaxis and treatment of breast cancer. "( Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
Abadi, AH; Ahmed, NS; Elghazawy, NH; ElHady, AK; Engel, M; Hartmann, RW, 2016
)
2.17
"Tamoxifen (TAM) is a selective estrogen receptor modulator (SERM) used in estrogen receptor-alpha (ERα)-dependent breast cancers and off-target indications such as infections, although the immune activity of TAM and its active metabolite, 4-OH tamoxifen (4HT), is poorly characterized."( ERα-independent NRF2-mediated immunoregulatory activity of tamoxifen.
Battaglia, G; Brunialti, E; Ciana, P; Locati, M; Maggi, A; Mornata, F; Pepe, G; Pinna, C; Rizzello, L; Rovati, G; Sfogliarini, C; Vegeto, E, 2021
)
1.59
"Tamoxifen is a commonly used drug in the treatment of ER + ve breast cancers since 1970. "( p21 activated kinase-1 and tamoxifen - A deadly nexus impacting breast cancer outcomes.
Inemai, E; Murugan, S; Rajendran, S; Rayala, SK; Roy, J; Swaroop, SS; Venkatraman, G, 2022
)
2.46
"Tamoxifen (TAM) is a selective estrogen receptor modulator (SERM) with potential clinical benefits for all stages of breast cancer. "( Flexible Etherified and Esterified Triphenylethylene Derivatives and Their Evaluation on ER-positive and Triple-Negative Breast Cancer Cell Lines.
Abadi, AH; Ahmed, NS; Hassan, AS; Vollmer, G; Wober, J, 2022
)
2.16
"Tamoxifen is a selective oestrogen receptor modulator; in the breast, it decreases the growth and proliferation of breast epithelial cells. "( Association Of Weight Change In Breast Cancer Patients Undergoing Tamoxifen Treatment At A Tertiary Care Centre, Sindh, Pakistan.
Abbas, K; Ahmed, M; Haider, G; Mehar, K; Nouman, M; Pavan, B; Rahool, R; Shahid, A; Shaikh, MR; Zahoor, S,
)
1.81
"Tamoxifen is an effective breast cancer therapy in postmenopausal women. "( Alteration in glucose metabolism in the brain associated with tamoxifen treatment: Study in postmenopausal animal model.
Bellozi, PMQ; Itinose, AM; Koerich, S; Marek, CB; Sandrini, F; Schneider, SCS; Silva, FC, 2022
)
2.4
"Tamoxifen is a frequently used anticancer drug that acts by selective modulation of the estrogen receptor in patients with breast cancer."( Acute pancreatitis secondary to tamoxifen-associated hypertriglyceridemia: A clinical update.
Abbasi, EUH; Amin, MK; Ashraf, MJ; Goraya, MHN; Hussain, N; Inayat, F; Malik, A; Nawaz, G; Qayyum, M; Zaman, MA, 2023
)
1.92
"Tamoxifen is a first-line endocrine agent and is often used to treat estrogen receptor-positive (ER+) breast cancer. "( DLGAP1-AS2 promotes estrogen receptor signalling and confers tamoxifen resistance in breast cancer.
Fang, Z; Liang, X; Shao, N; Shi, Y; Yu, L; Zhai, D; Zhang, M; Zhao, Y, 2022
)
2.41
"Tamoxifen is a widely used estrogen receptor inhibitor, whose clinical success is limited by the development of acquired resistance. "( Lactate is a potential promoter of tamoxifen resistance in MCF7 cells.
Di Stefano, G; Farabegoli, F; Govoni, M; Rossi, V, 2022
)
2.44
"Tamoxifen is a commonly prescribed drug in both early and metastatic breast cancer. "( Tamoxifen use and potential effects on liver parenchyma: A long-term prospective transient elastographic evaluation.
Braal, CL; de Knegt, RJ; Eechoute, K; Jager, A; Koolen, SLW; Mathijssen, RHJ, 2022
)
3.61
"Tamoxifen is a widely used drug for breast cancer therapy; however, concerns and controversies regarding its efficiency arise as it induces various side effects, including endometrial cancer. "( Molecular Docking and in silico Pharmacological Screening of Oleosin from Cocos Nucifera Complexed with Tamoxifen in Developing Potential Breast Chemotherapeutic Leads.
Dela Cruz, JMD; Dones, SAA; Labrador, AM; Santiago-Bautista, MR; Villanueva, RC, 2022
)
2.38
"Tamoxifen is a selective estrogen receptor (ER) modulator that is used to treat ER-positive breast cancer, but that at high doses kills both ER-positive and ER-negative breast cancer cells. "( Bacterial diet modulates tamoxifen-induced death via host fatty acid metabolism.
Diot, C; Doyle, H; García-González, AP; Honeywell, M; Lee, M; Na, H; Olsen, CP; Ponomarova, O; Rivera, Y; Vieira, AF; Walhout, AJM; Walker, M; Zhang, H, 2022
)
2.47
"Tamoxifen (TAM) is a frequently-used treatment for breast cancer (BC). "( Knockdown circTRIM28 enhances tamoxifen sensitivity via the miR-409-3p/HMGA2 axis in breast cancer.
Li, Y; Liu, W; Lu, N; Yang, S; Yang, X; Zhang, G; Zou, C, 2022
)
2.45
"Tamoxifen (TAM) is a selective estrogen receptor modulator and was recently reported to have antifibrotic actions."( Tamoxifen Alters TGF-β1/Smad Signaling in Vocal Fold Injury.
Branski, RC; Hashimoto, K; Hirano, S; Kaneko, M; Kinoshita, S; Matsushita, H; Mukudai, S; Ozawa, S; Sugiyama, Y, 2023
)
3.07
"Tamoxifen is an antiestrogen for breast cancer therapy known for adverse drug reactions (ADRs)."( Impact of organic anion transporting polypeptide, P-glycoprotein, and breast cancer resistance protein transporters on observed tamoxifen and endoxifen concentration and adverse effects.
Keller, DN; Kim, RB; Medwid, SJ; Ross, CD; Wigle, TJ, 2023
)
1.84
"Tamoxifen is a first-line therapeutic drug for oestrogen-receptor positive breast cancer; however, like other therapeutics, its clinical use is limited by acquired resistance. "( GPER-mediated stabilization of HIF-1α contributes to upregulated aerobic glycolysis in tamoxifen-resistant cells.
Chen, Y; Fan, S; Liu, X; Peng, X; Qi, Q; Ren, S; Shen, X; Song, Y; Zhang, M; Zhang, Y; Zhang, Z, 2023
)
2.58
"Tamoxifen (TAM) is a selective estrogen receptor modulator that is used in the treatment of breast cancer. "( Tamoxifen retinopathy.
Bazvand, F; Mahdizad, Z; Mirghorbani, M; Modjtahedi, BS; Mohammadi, N; Riazi-Esfahani, H; Shahi, F,
)
3.02
"Tamoxifen is a drug used for hormone receptor-positive breast cancers, primarily metabolised by the CYP2D6 enzyme into active metabolites such as endoxifen. "( Early increase in tamoxifen dose in CYP2D6 poor metaboliser breast cancer patients and survival: A propensity score matching analysis.
Blancas, I; Garrido, JM; Herrero-Vicent, C; Linares-Rodríguez, M; Martínez de Dueñas, E; Molero-Mir, MD; Rodríguez-Serrano, F, 2023
)
2.69
"Tamoxifen (TAM) is an accredited drug used for treatment and prevention of breast cancer. "( Maternal tamoxifen exposure leads to abnormal primordial follicle assembly.
Shen, W; Shi, D; Sun, X; Sun, Y; Wang, R; Zhang, J; Zhao, J, 2023
)
2.77
"Tamoxifen (TAM) is a selective estrogen receptor modulator that was previously suggested as a protective agent against chemotherapy-induced ovarian failure."( Tamoxifen decreases ovarian toxicity without compromising cancer treatment in a rat model of mammary cancer.
Ciereszko, RE; Kurowicka, B; Molcan, T; Myszczynski, K; Nynca, A; Orlowska, K; Otrocka-Domagala, I; Paździor-Czapula, K; Petroff, BK; Ruszkowska, M; Sadowska, A; Swigonska, S, 2023
)
3.07
"Tamoxifen is a selective estrogen receptor modulator used mainly for the treatment of breast cancer. "( Tamoxifen retinopathy: A comprehensive review.
Chen, MY; Oboh-Weilke, A; Tenney, S; Wagner, D,
)
3.02
"Tamoxifen is an established treatment for breast cancer, but its long-term effects on survival and on secondary cancers are not fully evaluated."( Breast cancer survival and incidence of second primary cancers after 30 years in a randomized study of two versus five years of adjuvant tamoxifen therapy.
Bengtsson, NO; Fohlin, H; Fornander, T; Hatschek, T; Lindman, H; Malmström, P; Nordenskjöld, A; Nordenskjöld, B; Rosell, J; Rydén, L; Stål, O; Wallgren, A, 2023
)
2.56
"Tamoxifen (TMX) is a selective estrogen receptor modulator (SERM) that inhibits the expression of estrogen-regulated genes, including growth and angiogenic factors secreted by tumor cells."( Tamoxifen as a modulator of CXCL12-CXCR4-CXCR7 chemokine axis: A breast cancer and glioblastoma view.
de Araújo, LP; Gonçalves, TL; Pereira Ferrer, V, 2023
)
3.07
"Tamoxifen is a drug used for treating breast cancer (BC), especially for individuals diagnosed with estrogen receptor-positive (ER+) BC. "( Candidate Oligo Therapeutic Target, miR-330-3p, Induces Tamoxifen Resistance in Estrogen Receptor-Positive Breast Cancer Cells via HDAC4.
Fu, Z; Gao, S; Jiang, Z; Ma, J; Wang, M; Zhang, M, 2023
)
2.6
"Tamoxifen (TAM) is an effective anticancer drug for breast and ovarian cancer. "( Tamoxifen induced cardiac damage via the IL-6/p-STAT3/PGC-1α pathway.
Chen, J; Li, Y; Liu, A; Meng, T; Song, C; Su, G; Tian, P; Zhang, D; Zhang, Y; Zheng, Y, 2023
)
3.8
"Tamoxifen (TAM) is a chemotherapeutic drug widely utilized to treat breast cancer. "( Pioglitazone attenuates tamoxifen-induced liver damage in rats via modulating Keap1/Nrf2/HO-1 and SIRT1/Notch1 signaling pathways: In-vivo investigations, and molecular docking analysis.
Elariny, HA; Kamel, GAM, 2023
)
2.66
"Tamoxifen (TAM) is a drug commonly used in patients with breast cancer. "( Molecular Action of Tamoxifen in the Ovaries of Rats with Mammary Neoplasia.
Ciereszko, RE; Molcan, T; Nynca, A; Petroff, BK; Swigonska, S, 2023
)
2.68
"Tamoxifen is a selective oestrogen receptor modulator widely used in breast cancer treatment, with good survival rates. "( Retained products of conception in hysteroscopy in a patient with breast cancer on tamoxifen.
Chua, M; Qadir, D; Sulaiman, S, 2019
)
2.18
"Tamoxifen is a clinical drug for estrogen receptor (ER)-positive breast cancer. "( Tamoxifen-induced hepatotoxicity via lipid accumulation and inflammation in zebrafish.
Cai, Y; Huo, J; Jiang, Z; Liu, K; Xiang, T; Yu, Q; Zhang, L; Zhang, Y, 2020
)
3.44
"Tamoxifen is a mixed agonist/antagonist estrogen analogue that is frequently used to induce conditional gene deletion in mice using Cre-loxP mediated gene recombination. "( Tamoxifen suppresses pancreatic β-cell proliferation in mice.
Ahn, SH; Cox, AR; Granger, A; Kushner, JA; Lam, CJ; Rankin, MM, 2019
)
3.4
"Tamoxifen is an effective drug for patients with estrogen receptor-positive breast cancer, but the development of resistance is common."( SIRT4 enhances the sensitivity of ER-positive breast cancer to tamoxifen by inhibiting the IL-6/STAT3 signal pathway.
Fu, L; Gai, J; Guan, J; Li, J; Li, Q; Xing, J, 2019
)
1.47
"Tamoxifen is a selective estrogen receptor regulator, and shows antioxidant actions and regulatory roles in the calcium homeostasis besides its antitumor activity."( Tamoxifen in Duchenne muscular dystrophy (TAMDMD): study protocol for a multicenter, randomized, placebo-controlled, double-blind phase 3 trial.
Bieri, O; Fischer, D; Hafner, P; Nagy, S; Rubino-Nacht, D; Schädelin, S; Schmidt, S, 2019
)
2.68
"Tamoxifen is an oestrogen receptor modulator that is widely used for the treatment of early stage breast cancer and reduction of recurrences. "( Tamoxifen activity against Plasmodium in vitro and in mice.
Fisher, E; Gallego-Delgado, J; Gomes, C; Gonzalez, S; Nikain, C; Rodriguez, A; Sherman, J; Weinstock, A, 2019
)
3.4
"Tamoxifen is a prodrug and cytochrome P450 2C9 (CYP2C9) has a significant role in the formation of a therapeutically more potent metabolite (4-hydroxytamoxifen) than tamoxifen. "( Cytochrome P450 2C9 polymorphism: Effect of amino acid substitutions on protein flexibility in the presence of tamoxifen.
Lynn, AM; Manish, M; Mishra, S, 2020
)
2.21
"Tamoxifen is a selective oestrogen receptor modulator (SERM). "( Stimulation of Leydig and Sertoli Cellular Secretory Function by Anti-Oestrogens: Tamoxifen.
Dimakopoulou, A; Foran, D; Jayasena, CN; Minhas, S,
)
1.8
"Tamoxifen (TAM) is a hydrophobic anticancer agent and a selective estrogen modulator (SERM), approved by the FDA for hormone therapy of BC."( Novel Tamoxifen Nanoformulations for Improving Breast Cancer Treatment: Old Wine in New Bottles.
Day, CM; Garg, S; Hickey, SM; Plush, SE; Song, Y, 2020
)
1.76
"Tamoxifen is an estrogen modulator widely used in the treatment of patients with ESR/ER-positive breast cancer; however, resistance limits its clinical application. "( GLUT1 participates in tamoxifen resistance in breast cancer cells through autophagy regulation.
Duan, Y; Ji, H; Ma, Y; Sun, M; Wang, Y; Zhang, Q; Zhao, S, 2021
)
2.38
"Tamoxifen resistance is a major roadblock in the treatment of patients with breast cancer. "( Acquired tamoxifen resistance is surmounted by GW8510 through ribonucleotide reductase M2 downregulation-mediated autophagy induction.
Chen, CG; Li, J; Li, MY; Li, XQ; Li, ZN; Shu, Y; Wang, S; Zhao, XH, 2020
)
2.42
"Tamoxifen is a widely used hormonal based therapy for breast cancer in the adjuvant and metastatic setting, prolonging overall and recurrence-free survival. "( Does tamoxifen have a therapeutic role outside of breast cancer? A systematic review of the evidence.
Blower, E; Bowden, D; Clifford, RE; Kirwan, CC; Vimalachandran, D, 2020
)
2.51
"Tamoxifen is a P-glycoprotein inhibitor, independent of its effect on estrogen receptors."( COVID-19 infection can cause chemotherapy resistance development in patients with breast cancer and tamoxifen may cause susceptibility to COVID-19 infection.
Cumhur Cure, M; Cure, E; Kadiyoran, C; Vatansev, H, 2020
)
1.5
"Tamoxifen is a potent inducer of ovarian function and consequent hyperestrogenism in premenopausal women."( Risk Factors for Tamoxifen-Induced Ovarian Hyperstimulation in Breast Cancer Patients.
Kim, MK; Shin, HC, 2020
)
1.62
"Tamoxifen citrate is a very prevalent drug marketed under several trade names like Apo-Tamox, Nolvadex, Tamec, Tamizam, and Tamoplex. "( Antimicrobial, Antitumor and Side Effects Assessment of a Newly Synthesized Tamoxifen Analog.
Abdmouleh, F; Ali, MB; Amara, IB; El Arbi, M; Gupta, GK; Hammami, R; Hassen, HB; Jaouen, G; Jellali, K; Ketata, E; Pigeon, P; Saad, HB; Top, S, 2020
)
2.23
"Tamoxifen exposure is a recognised risk for primary endometrial cancer. "( Recurrence of endometrial cancer in a hysterectomised patient treated with tamoxifen for breast cancer: a case report.
Davis, M; Rahimi, S; Woolas, J, 2020
)
2.23
"Tamoxifen is an antagonist of estrogen receptor (ERα), a transcription factor expressed in over 50% of breast cancers."( Inhibition of O-GlcNAc transferase activates tumor-suppressor gene expression in tamoxifen-resistant breast cancer cells.
Barkovskaya, A; Itkonen, HM; Mills, IG; Moestue, SA; Prasmickaite, L; Seip, K, 2020
)
1.51
"Tamoxifen is an antineoplastic agent, working as an estrogen receptor antagonist, also called a selective estrogen receptor modulator."( First report of tamoxifen-induced baboon syndrome.
Ghasemi, M; Ghobadiaski, S; Hashemi, N; Jahani Amiri, K; Jallab, N; Kränke, B; Mofarrah, R; Rahmani, M; Rahmani, N, 2021
)
1.69
"Tamoxifen is a synthetic, nonsteroidal antiestrogen widely used in the treatment of hormone-sensitive breast cancer that has also been shown to inhibit the enzyme protein kinase C (PKC). "( Switch to Hypomania After Discontinuation of Tamoxifen: A Case Report.
Avari, JN; Kotbi, N; Mora, HA, 2021
)
2.32
"Tamoxifen (TAM) is a selective estrogen receptor modulator used for breast cancer patients. "( CSNK1G2 differently sensitizes tamoxifen-induced decrease in PI3K/AKT/mTOR/S6K and ERK signaling according to the estrogen receptor existence in breast cancer cells.
Hoe, KL; Lee, SJ; Nguyen Hoang, AT, 2021
)
2.35
"Tamoxifen (TAMO) is a chemotherapeutic drug used for the treatment of breast cancer. "( Cyanocobalamin and/or calcitriol mitigate renal damage-mediated by tamoxifen in rats: Implication of caspase-3/NF-κB signaling pathways.
Alharbi, FMB; AlHarthii, A; Alhusaini, AM; Alshanwani, AR; Arafah, MM; Badr, AM; Faddah, LM; Hagar, H; Mohamed, AM; Shaheen, S, 2021
)
2.3
"Tamoxifen is a selective estrogen receptor modulator and is a common endocrine therapy treatment for breast cancer."( Effects of tamoxifen on cognition and language in women with breast cancer: A systematic search and a scoping review.
Bloss, JE; Jebahi, F; Sharma, S; Wright, HH, 2021
)
1.73
"Tamoxifen is a selective estrogen receptor modulator used to activate the CREERT2 recombinase, allowing tissue-specific and temporal control of the somatic mutagenesis to generate transgenic mice. "( Tamoxifen Treatment in the Neonatal Period Affects Glucose Homeostasis in Adult Mice in a Sex-Dependent Manner.
Bron, C; Duboeuf, F; Estrada-Meza, J; Gautier-Stein, A; Mithieux, G; Peyruchaud, O; Rajas, F; Saint-Béat, C; Silva, M; Videlo, J, 2021
)
3.51
"Tamoxifen gavage is a commonly used method to induce genetic modifications in cre-loxP systems. "( Double-edged effects of tamoxifen-in-oil-gavage on an infectious murine model for multiple sclerosis.
Allnoch, L; Baumgärtner, W; Flügel, A; Hansmann, F; Herder, V; Hülskötter, K; Jin, W; Lühder, F; Rohn, K; Schmidtke, D, 2021
)
2.37
"Tamoxifen is a selective estrogen receptor modulator widely used for treatment and prevention of estrogenic receptor-positive breast cancer. "( Prescribing Tamoxifen in Patients With Mood Disorders: A Systematic Review of Potential Antimanic Versus Depressive Effects.
Carmassi, C; Cordone, A; Dell'Osso, L; Dell'Oste, V; Pardini, F; Pedrinelli, V; Simoncini, M,
)
1.95
"Tamoxifen is a pro-drug some of whose metabolites interact with the nuclear estrogen receptor, leading to anti-fibrotic and muscle-protective effects as has been demonstrated in a murine model of DMD."( Safety and clinical outcome of tamoxifen in Duchenne muscular dystrophy.
Avrahami, R; Ben-Sasson, S; Dor, T; Eliav, O; Lavi, E; Simchovitz, E; Tsabari, R, 2021
)
1.63
"Tamoxifen (TAM) is a life-saving and cost-effective drug widely used in the prevention and treatment of breast cancer. "( Vitamin D modulates hepatic microRNAs and mitigates tamoxifen-induced steatohepatitis in female rats.
Abd El-Haleim, EA; Sallam, NA, 2022
)
2.41
"Tamoxifen is an estrogen receptor (ER) ligand with widespread use in clinical and basic research settings. "( Developmental malformations resulting from high-dose maternal tamoxifen exposure in the mouse.
Lipinski, RJ; Martin, AA; Steward, AC; Sun, MR; Sweet, EA, 2021
)
2.3
"Tamoxifen is an estrogen receptor (ER) antagonist that is most commonly used for the treatment of ER-positive breast cancer. "( Network-based approach to identify prognosis-related genes in tamoxifen-treated patients with estrogen receptor-positive breast cancer.
Gong, X; Wang, Y; Zhang, Y, 2021
)
2.3
"Tamoxifen acts as an estrogen antagonist within the breast tissue. "( High Incidence of Carcinosarcoma among Patients Previously Treated with Tamoxifen.
Arnon, E; Auslender, R; Gemer, O; Goldberg, Y; Kaldawy, A; Lavie, O; Segev, Y; Siegler, E, 2017
)
2.13
"Tamoxifen is an estrogen modulator that acts to competitively inhibit the binding of endogenous estrogens. "( Mechanism of Off-Target Interactions and Toxicity of Tamoxifen and Its Metabolites.
Alisaraie, L; Flynn, M; Heale, KA, 2017
)
2.15
"Tamoxifen is a selective estrogen receptor modulator widely used in the treatment of breast cancer. "( The Effects of Tamoxifen on Plasma Lipoprotein(a) Concentrations: Systematic Review and Meta-Analysis.
Banach, M; Gurban, C; Jones, SR; Kostner, K; Kotani, K; Lippi, G; Penson, P; Rizzo, M; Rysz, J; Sahebkar, A; Serban, MC; Toth, PP; Ursoniu, S, 2017
)
2.25
"Tamoxifen (Tam) is an effective drug that competitively binds to the ER and is routinely used for the treatment of ER-positive BC."( Improving the efficacy of hormone therapy in breast cancer: The role of cholesterol metabolism in SERM-mediated autophagy, cell differentiation and death.
Dalenc, F; Leignadier, J; Poirot, M; Silvente-Poirot, S, 2017
)
1.18
"Tamoxifen resistance is a major clinical challenge in breast cancer treatment. "( GPER promotes tamoxifen-resistance in ER+ breast cancer cells by reduced Bim proteins through MAPK/Erk-TRIM2 signaling axis.
Li, Q; Liu, M; Tu, G; Wen, S; Yang, G; Yin, H; Yuan, J; Zhu, Q, 2017
)
2.26
"Tamoxifen (TAM) is a selective estrogen receptor modulator, widely used in the treatment and prevention of estrogen-dependent breast cancer. "( Effects of tamoxifen on neuronal morphology, connectivity and biochemistry of hypothalamic ventromedial neurons: Impact on the modulators of sexual behavior.
Fonseca, BM; Sá, SI; Teixeira, N, 2018
)
2.31
"Tamoxifen is a selective estrogen receptor modulator that elicits potent anti-breast cancer effects."( Skeletal and Uterotrophic Effects of Endoxifen in Female Rats.
Gingery, A; Goetz, MP; Hawse, JR; Ingle, JN; Iwaniec, UT; Marler, RJ; McGovern, RM; Pitel, KS; Reid, JM; Subramaniam, M; Turner, RT, 2017
)
1.18
"Tamoxifen (TMX) is a selective estrogen receptor modulator, possessing agonist or antagonistic activity in different tissues."( Agonistic activity of tamoxifen, a selective estrogen-receptor modulator (SERM), on arthritic ovariectomized mice.
Araujo, JMD; Camargo, EA; Felix, FB; Grespan, R; Silva, LAS; Souza, EV, 2017
)
1.49
"Tamoxifen retinopathy is a condition rarely observed in clinical practice. "( TAMOXIFEN RETINOPATHY DURING TREATMENT OF AN INOPERABLE DESMOID TUMOR.
Araujo, D; Furst, M; Harper, CA; Somogyi, MB; Wong, RW, 2020
)
3.44
"Tamoxifen (TX) is a non-steroidal estrogen receptor modulator with effects on cell growth and survival."( Tamoxifen induces apoptotic neutrophil efferocytosis in horses.
Folch, H; Henriquez, C; Morales, N; Moran, G; Olave, C; Ortloff, A; Sarmiento, J; Uberti, B, 2018
)
2.64
"Tamoxifen is a standard anti-hormone treatment in estrogen receptor positive breast carcinoma patients. "( Altered DNA methyltransferases promoter methylation and mRNA expression are associated with tamoxifen response in breast tumors.
Emami Razavi, A; Jahangiri, R; Jamialahmadi, K; Mosaffa, F; Teimoori-Toolabi, L, 2018
)
2.14
"Tamoxifen is a first-line drug for hormone therapy (HT) in oestrogen receptor-positive breast cancer patients. "( Elevated CRB3 expression suppresses breast cancer stemness by inhibiting β-catenin signalling to restore tamoxifen sensitivity.
Cao, F; Chen, H; Feng, C; Jiang, Y; Li, P; Liu, J; Liu, P, 2018
)
2.14
"Tamoxifen is a prodrug, and most of the therapeutic effect in treating breast cancer stems from its metabolite, endoxifen. "( The Underrated Risks of Tamoxifen Drug Interactions.
Hansten, PD, 2018
)
2.23
"Tamoxifen is a frontline therapy for estrogen receptor (ER)-positive breast cancer in premenopausal women. "( C-Cbl reverses HER2-mediated tamoxifen resistance in human breast cancer cells.
Che, X; Hou, K; Li, H; Li, W; Liu, Y; Qu, X; Shi, S; Song, N; Teng, Y; Wen, T; Xin, X; Xu, L; Yang, Y; Zeng, X; Zhang, Y; Zhou, L, 2018
)
2.21
"Tamoxifen is a first targeted drug that continues to be the gold standard in treatment of estrogen receptor positive breast cancer for almost 50 years. "( Tamoxifen Never Ceases to Amaze: New Findings on Non-Estrogen Receptor Molecular Targets and Mediated Effects.
Bogush, EA; Bogush, TA; Mamichev, IA; Polezhaev, BB; Polotsky, BE; Ryabov, AB; Tjulandin, SA, 2018
)
3.37
"Tamoxifen is a widely used personalized medicine for estrogen receptor (ER)-positive breast cancer, but approximately 30% of patients receiving the treatment relapse due to tamoxifen resistance (TamR). "( Downregulation of LINC00894-002 Contributes to Tamoxifen Resistance by Enhancing the TGF-β Signaling Pathway.
Sun, H; Wang, M; Wang, X; Zhang, X; Zhu, T, 2018
)
2.18
"Tamoxifen is a selective estrogen- receptor modulator commonly associated with an increased risk of thrombotic events, including cere- bral venous thrombosis. "( Superior Sagittal Sinus Thrombosis Related to the Use of Tamoxifen: A Case Report and Review of Literature.
Phuong, L; Shimanovsky, A, 2016
)
2.12
"Tamoxifen (TAM) is an endocrine therapy commonly used in the treatment of patients with breast cancer expressing estrogen receptor α."( MicroRNA‑663b mediates TAM resistance in breast cancer by modulating TP73 expression.
Cheng, L; Hu, P; Jiang, H; Liu, R, 2018
)
1.2
"Tamoxifen is a prodrug and requires bioactivation by CYP2D6."( CYP2D6 genotype and endoxifen plasma concentration do not predict hot flash severity during tamoxifen therapy.
Jansen, LE; Kim, RB; Lizotte, DJ; Rose, RV; Teft, WA, 2018
)
1.42
"Tamoxifen is an estrogen receptor (ER) antagonist used as first-line chemotherapy in breast cancer. "( Tamoxifen inhibits the proliferation of non‑melanoma skin cancer cells by increasing intracellular calcium concentration.
Akatsuka, K; Hasegawa, G; Higo, N; Nakashima, Y; Shimonaka, M; Yokoe, Y, 2018
)
3.37
"Tamoxifen (TMX) is an antiestrogen drug that is used in the treatment and prevention of all stages of estrogen-dependent breast cancer. "( Osthole prevents tamoxifen-induced liver injury in mice.
Cai, Y; Li, H; Sun, W; Zhang, XX; Zhou, WB, 2019
)
2.3
"Tamoxifen (TX) is a nonsteroidal estrogen receptor modulator with immunomodulatory effects and induces early apoptosis of blood and bronchoalveolar lavage neutrophils from horses with acute lung inflammation."( Tamoxifen induces apoptosis and inhibits respiratory burst in equine neutrophils independently of estrogen receptors.
Alvarez, P; Folch, H; Henriquez, C; Morales, N; Moran, G; Olave, C; Sarmiento, J; Uberti, B, 2019
)
2.68
"Tamoxifen is an antiestrogen drug that is widely used in the adjuvant chemotherapy of estrogen receptor-α (ERα)-positive breast cancer. "( Predicting the Effects of Different Triazole Antifungal Agents on the Pharmacokinetics of Tamoxifen.
Chen, L; Li, M; Li, N; Qi, F; Wang, N; Zhu, L, 2019
)
2.18
"Tamoxifen is an oral medication that has been proposed as a potential treatment for bipolar disorder. "( Tamoxifen for bipolar disorder: Systematic review and meta-analysis.
Palacios, J; Taylor, MJ; Yildiz, A; Young, AH, 2019
)
3.4
"Tamoxifen appears to be a promising potential treatment for episodes of mania. "( Tamoxifen for bipolar disorder: Systematic review and meta-analysis.
Palacios, J; Taylor, MJ; Yildiz, A; Young, AH, 2019
)
3.4
"Tamoxifen (TAM) is a frequently used hormonal prodrug for patients with breast cancer that needs to be activated by cytochrome P450 2D6 (CYP2D6) into Zusammen-endoxifen (Z-END)."( Association of CYP2D6*10 (c. 100 C>T) Genotype with Z-END Concentration in Patients with Breast Cancer Receiving Tamoxifen Therapy in Indonesian Population.
Andalusia, R; Hidayat, A; Louisa, M; Panigoro, SS; Purwanto, DJ; Setiabudy, R, 2019
)
2.17
"Tamoxifen is an anti-estrogen in the breast used for treatment and prevention of breast cancer, with estrogen agonist activity in the uterus."( Beyond estrogen: advances in tissue selective estrogen complexes and selective estrogen receptor modulators.
Conner, EA; Pinkerton, JV, 2019
)
1.24
"Tamoxifen is an important targeted endocrine therapy in breast cancer. "( Drug monitoring of tamoxifen metabolites predicts vaginal dryness and verifies a low discontinuation rate from the Norwegian Prescription Database.
Aas, T; Bifulco, E; Gjerde, J; Gripsrud, BH; Hagen, KB; Haugstøyl, ME; Helland, T; Hustad, S; Janssen, EAM; Jonassen, J; Jonsdottir, K; Kvaløy, JT; Lende, TH; Lien, EA; Lind, RA; Lode, K; Lunde, S; Mellgren, G; Søiland, H, 2019
)
2.29
"Tamoxifen (TAM) is a first generation-SERM administered for hormone receptor-positive (HER+) breast cancer in both pre- and post-menopausal patients and may undergo metabolic activation in organisms that share similar receptors and thus face comparable mechanisms of response. "( Impacts of in vivo and in vitro exposures to tamoxifen: Comparative effects on human cells and marine organisms.
Abessa, DMS; Bebianno, MJ; Carriço, T; Fernandes, E; Fonseca, TG; Tavares, A, 2019
)
2.22
"Tamoxifen (TAM) is an antiestrogenic agent and can enter the aquatic environment in wastewater. "( Tamoxifen affects the histology and hepatopancreatic lipid metabolism of swimming crab Portunus trituberculatus.
Feng, Q; Francis, DS; Liu, M; Turchini, GM; Wu, X; Zeng, C, 2019
)
3.4
"Tamoxifen resistance is a major hurdle in the treatment of estrogen receptor (ER)-positive breast cancer. "( Autoantibodies Specific to ERα are Involved in Tamoxifen Resistance in Hormone Receptor Positive Breast Cancer.
Barba, M; Carè, A; Cirulli, F; Gabriele, L; Iessi, E; Macchia, D; Maselli, A; Matarrese, P; Ortona, E; Pagano, MT; Parlato, S; Pierdominici, M; Pizzuti, L; Pontecorvi, G; Puglisi, R; Raggi, C; Spada, M; Vici, P, 2019
)
2.21
"Tamoxifen is a selective estrogen receptor modulator used widely for the treatment of breast cancer. "( Tamoxifen-induced vasculitis.
Kulkarni, U; Nayak, V; Prabhu, MM; Rao, R, 2020
)
3.44
"Tamoxifen is a selective estrogen receptor modulator widely used in the treatment of hormone-responsive breast cancer. "( Branch retinal vein occlusion associated with tamoxifen use.
Karatas, A; Kaya, E; Kaya, M; Kilic, AC; Kose, SA; Onder, Hİ; Tunc, M, 2013
)
2.09
"Tamoxifen (Tam) is a selective estrogen receptor modulator (SERM) that remains one of the major drugs used in the hormonotherapy of breast cancer (BC). "( 5,6-Epoxy-cholesterols contribute to the anticancer pharmacology of tamoxifen in breast cancer cells.
Dalenc, F; de Medina, P; Iuliano, L; Jordan, VC; Noguer, E; Paillasse, MR; Payré, B; Poirot, M; Record, M; Segala, G; Silvente-Poirot, S; Zerbinati, C, 2013
)
2.07
"Tamoxifen is an antiestrogenic drug with cysticidal action on Taenia crassiceps, a close relative of T."( Tamoxifen treatment in hamsters induces protection during taeniosis by Taenia solium.
Escobedo, G; López-Griego, L; Morales-Montor, J; Olivos, A; Palacios-Arreola, MI, 2013
)
2.55
"Tamoxifen is a widely utilized adjuvant anti-estrogen agent for hormone receptor-positive breast cancer, known to undergo CYP2D6-mediated bioactivation to endoxifen. "( CYP3A4 and seasonal variation in vitamin D status in addition to CYP2D6 contribute to therapeutic endoxifen level during tamoxifen therapy.
Brackstone, M; Choi, YH; Dingle, B; Gong, IY; Kim, RB; Legan, RM; Perera, FE; Potvin, K; Teft, WA; Tirona, RG; Vandenberg, TA; Younus, J; Zou, G, 2013
)
2.04
"Tamoxifen is a potent antioxidant that also modulates some ionic transport pathways."( Electrophysiological effects of tamoxifen: mechanism of protection against reperfusion arrhythmias in isolated rat hearts.
Carrión, AM; Diez, ER; Miatello, RM; Petrich, ER; Ponce Zumino, AZ; Prado, NJ, 2013
)
1.39
"Tamoxifen is a widely prescribed adjuvant anti-estrogen agent for estrogen receptor-positive breast cancer. "( Determination of clinically therapeutic endoxifen concentrations based on efficacy from human MCF7 breast cancer xenografts.
Alicke, B; Chen, YH; Choo, EF; Gong, IY; Kim, RB; Ly, J; Teft, WA, 2013
)
1.83
"Tamoxifen (TAM) is a selective estrogen receptor modulator (SERM) used in the treatment of breast cancer; however many women complain of weight gain during TAM treatment. "( Effect of chronic administration of tamoxifen and/or estradiol on feeding behavior, palatable food and metabolic parameters in ovariectomized rats.
Arcego, DM; da Costa Lima, IF; Dalmaz, C; Diehl, LA; Krolow, R; Lampert, C; Laureano, DP; Pettenuzzo, LF; Vendite, D, 2013
)
2.11
"Tamoxifen is a selective estrogen receptor modulator extensively used on estrogen receptor-positive breast cancer treatment. "( Unique SERM-like properties of the novel fluorescent tamoxifen derivative FLTX1.
Boto, A; Cury, D; Díaz, M; Fernández-Pérez, L; García Marrero, B; Gómez, T; Lahoz, F; Marín, R; Marrero-Alonso, J; Morales, A, 2013
)
2.08
"Tamoxifen is a largely inactive pro-drug, requiring metabolism into its most important metabolite endoxifen. "( Unjustified prescribing of CYP2D6 inhibiting SSRIs in women treated with tamoxifen.
Bannink, M; Binkhorst, L; Jager, A; Mathijssen, RH; van Gelder, T; van Herk-Sukel, MP; Wiemer, EA, 2013
)
2.06
"Tamoxifen is a synthetic, non-steroidal, anti-estrogen agent that is widely used for treating all stages of breast cancer and has been approved for the prevention of breast cancer in high-risk women."( Apoptotic effects of tamoxifen on leukocytes from horse peripheral blood and bronchoalveolar lavage fluid.
Folch, H; Galecio, JS; Henriquez, C; Morales, N; Morán, G; Perez, B; Sarmiento, J; Vidal, L, 2013
)
1.43
"Tamoxifen (TMX) is a selective estrogen receptor modulator that is used as an estrogen receptor antagonist for the treatment and prevention of breast cancer. "( Tamoxifen improves cholinergically modulated cognitive performance in postmenopausal women.
Albert, K; Astur, R; Dumas, J; Johnson, J; Naylor, M; Newhouse, P, 2013
)
3.28
"Tamoxifen is an anti-estrogen molecule with anti-neoplastic effects whose role is under investigation."( Continuous tamoxifen and dose-dense temozolomide in recurrent glioblastoma.
Caroli, M; Carrabba, G; DI Cristofori, A; Lanfranchi, G; Menghetti, C; Rampini, P, 2013
)
1.5
"Tamoxifen is an effective alternative."( Endocrine therapy for advanced/metastatic breast cancer.
Schiavon, G; Smith, IE, 2013
)
1.11
"Tamoxifen is a pro-drug widely used in breast cancer patients to prevent tumor recurrence. "( Relationship between genotypes Sult1a2 and Cyp2d6 and tamoxifen metabolism in breast cancer patients.
Bandrés, F; Chicharro, LM; Fernández-Santander, A; Gaibar, M; Novillo, A; Romero-Lorca, A; Rubio, M; Tejerina, A, 2013
)
2.08
"Tamoxifen is an anticancer agent widely used for treatment of estrogen receptor (ERα)-positive breast cancer. "( Ridaifen-SB8, a novel tamoxifen derivative, induces apoptosis via reactive oxygen species-dependent signaling pathway.
Dan, S; Guo, WZ; Ohashi, Y; Shiina, I; Uetake, S; Umeda, E; Wang, Y; Watanabe, C; Yamori, T, 2013
)
2.15
"Tamoxifen (TMX) is a selective estrogen receptor modulator that can mimic the neuroprotective effects of estrogen but lacks its systemic adverse effects. "( The cancer drug tamoxifen: a potential therapeutic treatment for spinal cord injury.
Guptarak, J; Nesic, O; Paulucci-Holthauzen, AA; Sadygov, RG; Vergara, L; Wiktorowicz, JE; Zivadinovic, D, 2014
)
2.19
"Tamoxifen is a substrate for ATP-binding cassette transporter proteins."( Metabolism and transport of tamoxifen in relation to its effectiveness: new perspectives on an ongoing controversy.
Cronin-Fenton, DP; Damkier, P; Lash, TL, 2014
)
1.42
"Tamoxifen is a well-known anti-breast cancer drug; however, its molecular function is poorly understood."( Premature senescence in human breast cancer and colon cancer cells by tamoxifen-mediated reactive oxygen species generation.
Bae, YS; Kang, BS; Lee, YH, 2014
)
1.36
"Tamoxifen is a key therapeutic option for breast cancer treatment. "( Extraction of tamoxifen and its metabolites from formalin-fixed, paraffin-embedded tissues: an innovative quantitation method using liquid chromatography and tandem mass spectrometry.
Kangarloo, SB; Konno, M; Magliocco, AM; Ng, ES; Paterson, A, 2014
)
2.21
"Tamoxifen is a mainly inactive prodrug, necessitating metabolism by the cytochrome P450 (CYP450) pathway, predominantly the Cytochrome P450 2D6 (CYP2D6), into the active metabolites 4-hydroxytamoxifen and, in particular, endoxifen to achieve its therapeutic effect."( Successful use of agomelatine in the treatment of major depression in a woman taking tamoxifen: a case report.
Brucchi, M; De Berardis, D; Di Giannantonio, M; Fornaro, M; Martinotti, G; Mazza, M; Serroni, N; Valchera, A,
)
1.08
"Tamoxifen is a triphenylethylene nonsteroidal estrogen receptor (ER) antagonist used worldwide as an adjuvant hormone therapeutic agent in the treatment of breast cancer. "( Tamoxifen enhances erlotinib-induced cytotoxicity through down-regulating AKT-mediated thymidine phosphorylase expression in human non-small-cell lung cancer cells.
Chen, CY; Chiu, HC; Huang, YJ; Jian, YJ; Jian, YT; Ko, JC; Lin, YW; Syu, JJ; Wo, TY, 2014
)
3.29
"Tamoxifen seems to be a key strategy in prevention, but caution should be used in interpreting our results."( Can EPS development be avoided with early interventions? The potential role of tamoxifen--a single-center study.
Alvarez, L; Bajo, MA; Bellon, T; De Sousa-Amorim, E; Del Peso, G; Gil, F; Ossorio, M; Selgas, R,
)
1.08
"Tamoxifen is an unlikely pioneering medicine in medical oncology. "( Tamoxifen as the first targeted long-term adjuvant therapy for breast cancer.
Jordan, VC, 2014
)
3.29
"Tamoxifen is a partial agonist at GPER in vitro."( Lack of G protein-coupled estrogen receptor (GPER) in the plasma membrane is associated with excellent long-term prognosis in breast cancer.
Fernö, M; Fornander, T; Grabau, D; Hartman, L; Leeb-Lundberg, LM; Malmström, P; Nordenskjöld, B; Sgroi, DC; Sjöström, M; Skoog, L; Stål, O, 2014
)
1.12
"Tamoxifen is an endocrine therapy which is administered to up to 70% of all breast cancer patients with oestrogen receptor alpha (ERα) expression. "( MicroRNA-519a is a novel oncomir conferring tamoxifen resistance by targeting a network of tumour-suppressor genes in ER+ breast cancer.
Balwierz, A; König, R; Sahin, O; Shukla, K; Soons, Z; Ward, A; Wiemann, S, 2014
)
2.11
"Tamoxifen resistance is a major problem in the treatment of estrogen receptor (ER) α -positive breast cancer patients. "( Epidermal growth factor receptor signalling in human breast cancer cells operates parallel to estrogen receptor α signalling and results in tamoxifen insensitive proliferation.
Meerman, JH; Moerkens, M; van de Water, B; Wester, L; Zhang, Y, 2014
)
2.05
"Tamoxifen is a PKC inhibitor."( Beneficial role of tamoxifen in experimentally induced cardiac hypertrophy.
Desai, VJ; Patel, BM, 2014
)
1.45
"Tamoxifen is a prodrug, requiring cytochrome P450 enzyme-mediated metabolism to form the active metabolite endoxifen. "( Profound reduction in the tamoxifen active metabolite endoxifen in a patient on phenytoin for epilepsy compared with a CYP2D6 genotype matched cohort.
Gryn, SE; Kim, RB; Teft, WA, 2014
)
2.15
"Tamoxifen (Tam) is a selective estrogen receptor modulator used to inhibit breast tumor growth. "( A potential role for human UDP-glucuronosyltransferase 1A4 promoter single nucleotide polymorphisms in the pharmacogenomics of tamoxifen and its derivatives.
Bratton, SM; Dates, CR; Dhakal, IB; Edavana, VK; Finel, M; Greer, AK; Kadlubar, SA; Radominska-Pandya, A; Starlard-Davenport, A, 2014
)
2.05
"Tamoxifen is a selective antagonist of estrogen receptors."( Antiarrhythmic effect of tamoxifen on the vulnerability induced by hyperthyroidism to heart ischemia/reperfusion damage.
Buelna-Chontal, M; Chávez, E; Hernández-Esquivel, L; Pavón, N, 2014
)
1.43
"Tamoxifen resistance is a major clinical challenge in breast cancer treatment. "( Tamoxifen through GPER upregulates aromatase expression: a novel mechanism sustaining tamoxifen-resistant breast cancer cell growth.
Andò, S; Barone, I; Bonofiglio, D; Catalano, S; Chemi, F; Fuqua, SA; Giordano, C; Lanzino, M; Maggiolini, M; Panza, S; Rizza, P; Romeo, F, 2014
)
3.29
"Tamoxifen (TAM) is an anti-estrogen used in the treatment and prevention of hormone-dependent breast cancer."( Protective role of thymoquinone against liver damage induced by tamoxifen in female rats.
Suddek, GM, 2014
)
1.36
"Tamoxifen is a prodrug that is metabolically activated by 4-hydroxylation to the potent primary metabolite 4-hydroxytamoxifen (4OHT) or via another primary metabolite N-desmethyltamoxifen (NDMTAM) to a biologically active secondary metabolite endoxifen through a cytochrome P450 2D6 variant system (CYP2D6). "( Simulation with cells in vitro of tamoxifen treatment in premenopausal breast cancer patients with different CYP2D6 genotypes.
Bhatta, P; Fernandes, DJ; Flockhart, DA; Jordan, VC; Korostyshevskiy, VR; Maximov, PY; McDaniel, RE; Mürdter, TE, 2014
)
2.12
"Tamoxifen is an alternative in the medical treatment of RPF, especially if patients want to avoid glucocorticoids. "( Tamoxifen monotherapy in the treatment of retroperitoneal fibrosis.
Brandt, AS; Haage, P; Kamper, L; Kukuk, S; Roth, S, 2014
)
3.29
"Tamoxifen is a non-steroidal anti-estrogenic drug widely used for the treatment and prevention of breast cancer in women; however, there is evidence that tamoxifen is hepatocarcinogenic in rats, but not in mice. "( Genotoxic, epigenetic, and transcriptomic effects of tamoxifen in mouse liver.
Beland, FA; Churchwell, MI; de Conti, A; Latendresse, JR; Melnyk, S; Muskhelishvili, L; Pogribny, IP; Tryndyak, V, 2014
)
2.09
"Tamoxifen citrate is a selective estrogen receptor modulator, which is one of the adjuvant treatment choices for breast cancer."( Tamoxifen citrate: a glimmer of hope for silicosis.
Akbiyik, F; Akin, T; Alici, IO; Bilgin, BC; Karaca, N; Karaca, T; Simsek, GG; Uzdogan, A; Yilmaz, OH; Yoldas, O; Yoldas, S, 2015
)
2.58
"Tamoxifen is an effective endocrine treatment for early breast cancer (EBC) but increases the risk of venous thromboembolism. "( No increased venous thromboembolism risk in Asian breast cancer patients receiving adjuvant tamoxifen.
Chen, HM; Chen, TW; Cheng, AL; Huang, CS; Lai, MS; Lin, CH; Lu, YS, 2014
)
2.07
"Tamoxifen is a selective estrogen receptor modulator."( Beneficial role of tamoxifen in isoproterenol-induced myocardial infarction.
Patel, BM; Rayabarapu, N, 2014
)
1.45
"Tamoxifen is a nonsteroidal antiestrogen that blocks estrogen-stimulated tumor growth."( Linking estrogen-induced apoptosis with decreases in mortality following long-term adjuvant tamoxifen therapy.
Jordan, VC, 2014
)
1.34
"Tamoxifen (TAM) is a standard adjuvant endocrine therapy in postmenopausal breast cancer patients, but innate or acquired TAM resistance has remained to be a therapeutic challenge for clinicians. "( Effect of angiotensin receptor blockade on prevention and reversion of tamoxifen-resistant phenotype in MCF-7 cells.
Arabsolghar, R; Hosseini, A; Jaberipour, M; Namazi, S; Razmkhah, M; Rostami-Yalmeh, J; Sahebi, E, 2015
)
2.09
"Tamoxifen is a major treatment modality for estrogen receptor positive breast cancer, but the occurrence of resistance remains a problem. "( Synergy of leptin/STAT3 with HER2 receptor induces tamoxifen resistance in breast cancer cells through regulation of apoptosis-related genes.
Dubos, S; Palianopoulou, M; Papanikolaou, V; Papathanasiou, I; Stefanou, N; Tsezou, A; Valiakou, V, 2015
)
2.11
"Tamoxifen (TMX) is a nonsteroidal estrogen antagonist drug used for the treatment of breast cancer. "( Study of tamoxifen urinary metabolites in rat by ultra-high-performance liquid chromatography time-of-flight mass spectrometry.
Beneito-Cambra, M; Del Moral-Leal, ML; Domínguez-Romero, JC; García-Reyes, JF; Martinez-Lara, E; Martínez-Romero, R; Molina-Díaz, A, 2015
)
2.28
"Tamoxifen citrate is an anti-estrogen agent used in the treatment of breast carcinoma. "( Crystalline deposits in the macula - tamoxifen maculopathy or macular telangiectasia?
Nakhwa, C; Rijal, RK; Sindal, MD,
)
1.85
"Tamoxifen is a selective estrogen receptor modulator and used for patients with breast cancer."( Tamoxifen induces the development of hernia in mice by activating MMP-2 and MMP-13 expression.
Chen, Y; Duan, Y; Han, J; Li, X; Liu, M; Liu, Y; Ma, X; Wang, Q; Wei, Y; Xiang, R, 2015
)
2.58
"Tamoxifen (TAM) is a selective estrogen receptor modulator with tissue-specific effects on estrogen signaling used predominantly for treatment and chemoprevention of breast cancers. "( Challenges and Potential for Ovarian Preservation with SERMs.
Petroff, BK; Ting, AY, 2015
)
1.86
"Tamoxifen is an anti-estrogen drug used in treatment of Estrogen Receptor (ER) positive breast cancer. "( The active tamoxifen metabolite endoxifen (4OHNDtam) strongly down-regulates cytokeratin 6 (CK6) in MCF-7 breast cancer cells.
Bozickovic, O; Dankel, S; Drangevåg, A; Fenne, IS; Flågeng, MH; Gjerde, J; Helland, T; Lien, EA; Mellgren, G; Skartveit, L; Søiland, H, 2015
)
2.25
"Tamoxifen is a broadly used anti-estrogen for early and advanced ER+ breast cancers in women and the most common hormone treatment for male breast cancer."( Formulation of Anti-miR-21 and 4-Hydroxytamoxifen Co-loaded Biodegradable Polymer Nanoparticles and Their Antiproliferative Effect on Breast Cancer Cells.
Devulapally, R; Paulmurugan, R; Sekar, TV, 2015
)
1.41
"Tamoxifen is a commercially available therapeutic agent for breast malignancies."( 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
)
1.4
"Tamoxifen citrate is an anticancer drug slightly soluble in water. "( Ex vivo permeation of tamoxifen and its 4-OH metabolite through rat intestine from lecithin/chitosan nanoparticles.
Barbieri, S; Bettini, R; Buttini, F; Colombo, G; Colombo, P; Ponchel, G; Rossi, A; Sonvico, F, 2015
)
2.17
"Tamoxifen is a selective estrogen receptor (ER) modulator which is widely used to generate inducible conditional transgenic mouse models. "( Tamoxifen affects glucose and lipid metabolism parameters, causes browning of subcutaneous adipose tissue and transient body composition changes in C57BL/6NTac mice.
Berger, C; Blüher, M; Gericke, M; Hesselbarth, N; Klöting, N; Kunath, A; Pettinelli, C; Stumvoll, M, 2015
)
3.3
"Tamoxifen is a mainstay in the treatment of estrogen receptor-positive breast cancer and is metabolized to more than 30 different compounds. "( Highly sensitive simultaneous quantification of estrogenic tamoxifen metabolites and steroid hormones by LC-MS/MS.
Brauch, H; Eichelbaum, M; Heinkele, G; Johänning, J; Mürdter, TE; Precht, JC; Schroth, W; Schwab, M, 2015
)
2.1
"Tamoxifen (Tmx) is a selective estrogen-receptor modulator used in hormone replacement therapy, the effects of which are unknown in fish immunity."( Tamoxifen persistently disrupts the humoral adaptive immune response of gilthead seabream (Sparus aurata L.).
Abellán, E; Cabas, I; García-Ayala, A; Meseguer, J; Mulero, V; Rodenas, MC, 2015
)
2.58
"Tamoxifen is a safe and reliable treatment of breast cancer, but data suggest an association with endometrial polyps, hyperplasia, metaplasia and carcinoma. "( Endometrial tubal metaplasia in a young puerperal woman after breast cancer.
Caserta, D; Di Benedetto, L; Giovanale, V, 2015
)
1.86
"Tamoxifen is an endocrine-active pharmaceutical (EAP) that is used world-wide. "( Approaches for predicting effects of unintended environmental exposure to an endocrine active pharmaceutical, tamoxifen.
Gutjahr-Gobell, RE; Henderson, WM; Horowitz, DB; Jayaraman, S; Laws, SC; Mills, LJ; Zaroogian, GE, 2016
)
2.09
"Tamoxifen is an anticancer drug known to act on an estrogen receptor (ER) and other proteins."( Ridaifen G, tamoxifen analog, is a potent anticancer drug working through a combinatorial association with multiple cellular factors.
Dan, S; Ikeda, K; Kamisuki, S; Kusayanagi, T; Mizusawa, A; Morohashi, K; Ota, N; Sasaki, T; Shiina, I; Sugawara, F; Takakusagi, Y; Tsukuda, S; Uetake, S; Yamori, T, 2015
)
1.52
"Tamoxifen resistance is a major clinical problem for ER-positive breast cancer, but the underlying mechanism is not completely elucidated. "( Mitogen-activated protein kinase phosphatase 1 is involved in tamoxifen resistance in MCF7 cells.
Bai, J; He, J; Liu, P; Ma, G; Pan, Y; Ren, Y; Sun, R; Zhou, C, 2015
)
2.1
"Tamoxifen resistance is a multifaceted phenomenon, characterized by the constitutive activation of multiple signaling cascades that provide an additional survival advantage to cells. "( BI2536--A PLK inhibitor augments paclitaxel efficacy in suppressing tamoxifen induced senescence and resistance in breast cancer cells.
Bharti, R; Mandal, M; Parida, S; Prashanth Kumar, BN; Rajput, S, 2015
)
2.1
"Tamoxifen is a selective estrogen receptor modulator that has been used in the treatment of pubertal gynecomastia."( The effect of tamoxifen on pubertal bone development in adolescents with pubertal gynecomastia.
Akgül, S; Derman, O; Kanbur, N, 2016
)
1.52
"Tamoxifen (TMX) is a selective estrogen receptor modulator (SERM) used in the treatment of breast cancer. "( Memory enhancement by Tamoxifen on amyloidosis mouse model.
Banerjee, S; Basu, M; Mishra, N; Pandey, D, 2016
)
2.19
"Tamoxifen is a cornerstone component of adjuvant endocrine therapy for patients with hormone-receptor-positive breast cancer. "( Pigment Epithelium-Derived Factor Alleviates Tamoxifen-Induced Endometrial Hyperplasia.
Bar-Joseph, H; Ben-Aharon, I; Chuderland, D; Goldberg, K; Grossman, H; Hasky, N; Shalgi, R; Stemmer, SM; Uri-Belapolsky, S, 2015
)
2.12
"Tamoxifen is a selective oestrogen receptor modulator widely used for the treatment of breast cancer. "( Tamoxifen augments the innate immune function of neutrophils through modulation of intracellular ceramide.
Chang, JT; Corriden, R; Derieux, J; Gonzalez, DJ; Hollands, A; Lopez, J; Nizet, V; Olson, J, 2015
)
3.3
"Tamoxifen is a widely used anticancer drug with both an estrogen agonist and antagonist effect. "( Transcriptional and morphological effects of tamoxifen on the early development of zebrafish (Danio rerio).
Xia, L; Zheng, L; Zhou, JL, 2016
)
2.14
"Tamoxifen is a selective estrogen receptor modulator that competitively binds the ligand-binding domain of estrogen receptors. "( Colocalization of Estrogen Receptors with the Fluorescent Tamoxifen Derivative, FLTX1, Analyzed by Confocal Microscopy.
Boto, A; Díaz, M; Marín, R; Marrero-Alonso, J; Morales, A, 2016
)
2.12
"Tamoxifen (TAM) is an important cancer therapeutic and an experimental tool for effecting genetic recombination using the inducible Cre-Lox technique. "( Tamoxifen induces cellular stress in the nervous system by inhibiting cholesterol synthesis.
Bogdanov, Y; Denk, F; Erskine, EL; McMahon, SB; Nassar, MA; Ramer, LM; Ramer, MS; Signore, M; Wood, JN, 2015
)
3.3
"Tamoxifen is an important adjunct therapy in breast cancer treatment; however, it has been implicated in increasing microvascular flap complications. "( The Effects of Perioperative Tamoxifen Therapy on Microvascular Flap Complications in Transverse Rectus Abdominis Myocutaneous/Deep Inferior Epigastric Perforator Flap Breast Reconstruction.
Bokarius, AV; Evans, GR; Gu, J; Kobayashi, MR; Lee, Y; Paydar, KZ; Salibian, AA; Wirth, GA, 2016
)
2.17
"Tamoxifen is a widely used in anti-oestrogen treatment of breast cancer. "( Concurrent tamoxifen-related Müllerian adenofibromas in uterus and ovary.
Chen, X; Lv, B; Shi, H; Zhang, X, 2015
)
2.25
"Tamoxifen is an antagonist of the estrogen receptor and currently used for the treatment of breast cancer. "( Tamoxifen Induces Apoptosis of Leishmania major Promastigotes in Vitro.
Abbasi, A; Delavari, M; Doroodgar, A; Doroodgar, M; Taherian, AA, 2016
)
3.32
"Tamoxifen is an estrogen receptor modulator and has been shown to increase risk for microvascular flap complications. "( Tamoxifen-Related Thrombosis: An Experimental Study in Rat Venous Microvascular Anastomosis Model.
Aksam, B; Aksam, E; Ceran, C; Demirseren, ME; Suludere, Z; Yenidünya, S, 2017
)
3.34
"Tamoxifen (TAM) is an established endocrine treatment for all stages of oestrogen receptor (ER)-positive breast cancer. "( Pharmacogenetics of UGT1A4, UGT2B7 and UGT2B15 and Their Influence on Tamoxifen Disposition in Asian Breast Cancer Patients.
Ang, PCS; Cheung, YB; Chowbay, B; Dent, R; Khor, CC; Lim, JSL; Muerdter, TE; Ng, RCH; Schroth, W; Schwab, M; Singh, O; Sutiman, N; Wong, NS; Yap, YS, 2016
)
2.11
"Tamoxifen is an off-label option to treat men for breast cancer, infertility, and idiopathic gynecomastia. "( Tamoxifen in men: a review of adverse events.
Hollis, N; Pollock, PA; Wassersug, RJ; Wibowo, E, 2016
)
3.32
"Tamoxifen is a pharmacological estrogen inhibitor that binds to the estrogen receptor (ER) in breast cells. "( Effects of SULT1A1 Copy Number Variation on Estrogen Concentration and Tamoxifen-Associated Adverse Drug Reactions in Premenopausal Thai Breast Cancer Patients: A Preliminary Study.
Areepium, N; Ayudhya, DP; Charoenchokthavee, W; Sriuranpong, V, 2016
)
2.11
"Tamoxifen (TAM) is a non-steroidal estrogen receptor antagonist that enhances erlotinib (ERL)-induced cytotoxicity in the treatment of NSCLC. "( Simultaneous determination of erlotinib and tamoxifen in rat plasma using UPLC-MS/MS: Application to pharmacokinetic interaction studies.
Alzoman, NZ; Maher, HM; Shehata, SM, 2016
)
2.14
"Tamoxifen is an effective anti-estrogen treatment for patients with estrogen receptor-positive (ER+) breast cancer, however, tamoxifen resistance is frequently observed. "( Integrative analysis of miRNA and gene expression reveals regulatory networks in tamoxifen-resistant breast cancer.
Alves, CL; Brünner, N; Ditzel, HJ; Elias, D; Gupta, R; Joshi, T; Lykkesfeldt, AE; Lyng, MB; Stenvang, J; Teng, F; Wang, J; Workman, CT, 2016
)
2.1
"Tamoxifen is a well-established drug and is thus a promising candidate for a drug to regenerate myelin, as it will not require extensive safety testing."( Tamoxifen accelerates the repair of demyelinated lesions in the central nervous system.
Amaral, AI; Gonzalez, GA; Hofer, MP; Kotter, MRN; Rahman, S; Rundle, J; Syed, YA; Zhao, C, 2016
)
2.6
"Tamoxifen (TMX) is a drug used in chemotherapy for breast cancer and associated with poor cognitive performances."( Evidence for an expanded time-window to mitigate a reactivated fear memory by tamoxifen.
Andreatini, R; Bertoglio, LJ; da Silva, TR; Stern, CA; Takahashi, RN, 2016
)
1.38
"Tamoxifen is an estrogen receptor antagonist used in the treatment of breast cancer. "( Application of Mice Humanized for CYP2D6 to the Study of Tamoxifen Metabolism and Drug-Drug Interaction with Antidepressants.
Henderson, CJ; MacLeod, AK; McLaughlin, LA; Wolf, CR, 2017
)
2.14
"Tamoxifen (Tam) is a selective estrogen receptor (ER) modulator (SERM) that is an essential drug to treat ER-positive breast cancer. "( Tamoxifen Isomers and Metabolites Exhibit Distinct Affinity and Activity at Cannabinoid Receptors: Potential Scaffold for Drug Development.
Ford, BM; Franks, LN; Prather, PL; Radominska-Pandya, A, 2016
)
3.32
"Tamoxifen is a standard endocrine therapy for estrogen receptor positive breast cancer patients. "( Pharmacological inhibition of Rac1-PAK1 axis restores tamoxifen sensitivity in human resistant breast cancer cells.
Alonso, DF; Cardama, GA; Comin, MJ; Gomez, DE; Gonzalez, N; Menna, PL; Pifano, M; Segatori, VI, 2017
)
2.15
"Tamoxifen (Tmf), is a standard of care for women with estrogen receptor positive (ER+) breast cancer. "( [Antidepressants agents in breast cancer patients using tamoxifen: review of basic and clinical evidence].
Gaete G, L; Irarrázaval O, ME, 2016
)
2.12
"Tamoxifen is a well established treatment for breast cancer, but its long-term effects on the incidence of secondary cancers are not fully evaluated."( Long-term effects on the incidence of second primary cancers in a randomized trial of two and five years of adjuvant tamoxifen.
Bengtsson, NO; Carstensen, J; Fornander, T; Hatschek, T; Lindman, H; Malmström, PO; Nordenskjöld, B; Rosell, J; Stål, O; Wallgren, A, 2017
)
2.11
"Tamoxifen is a common adjuvant treatment for estrogen receptor (ER)α-positive patients with breast cancer; however, acquired resistance abrogates the efficacy of this therapeutic approach. "( IGF-1 Receptor Modulates FoxO1-Mediated Tamoxifen Response in Breast Cancer Cells.
Houston, KD; Vaziri-Gohar, A; Zheng, Y, 2017
)
2.17
"Tamoxifen is a selective estrogen receptor modulator that is widely used for the treatment of breast cancer."( Tamoxifen Directly Inhibits Platelet Angiogenic Potential and Platelet-Mediated Metastasis.
Battinelli, EM; Ceglowski, JR; El-Husayni, S; Forward, JA; Italiano, JE; Johnson, KE; Kulenthirarajan, R; Machlus, KR; Mayer, EL; Tippy, MD, 2017
)
2.62
"Tamoxifen (TX) is a non-steroidal estrogen receptor modulator with effects on cell growth and survival."( In Vitro effects of tamoxifen on equine neutrophils.
Borlone, C; Folch, H; Henriquez, C; Morales, N; Moran, G; Olave, C; Sarmiento, J; Uberti, B, 2017
)
1.5
"Tamoxifen is a widely applied therapy in breast cancer that affects ERα interactions with coregulators and shifts the DNA-binding signature of ERα upon prolonged exposure in breast cancer."( Estrogen receptor α wields treatment-specific enhancers between morphologically similar endometrial tumors.
Dackus, GM; Droog, M; Fles, R; Hollema, H; Kim, Y; Linn, SC; Mourits, MJ; Nederlof, PM; Nevedomskaya, E; van Boven, HH; van Leeuwen, FE; Wessels, LF; Zwart, W, 2017
)
1.18
"Tamoxifen is a selective estrogen receptor modulator (SERM) that is widely used in the treatment of patients with breast cancer and for chemoprophylaxis in high risk women. "( The effect of tamoxifen on the genital tract.
Ascher, SM; Polin, SA, 2008
)
2.15
"Tamoxifen is a nonsteroidal antiestrogen used as the current adjuvant endocrine treatment of choice for premenopausal women treated for breast cancer and its potential for causing fetal harm during pregnancy remains inconclusive. "( Pierre Robin sequence associated with first trimester fetal tamoxifen exposure.
Berger, JC; Clericuzio, CL, 2008
)
2.03
"Tamoxifen is a selective oestrogen receptor modulator (SERM) with an established role in the treatment and chemoprevention of hormone-related breast cancer. "( The multiple applications of tamoxifen: an example pointing to SERM modulation being the aspirin of the 21st century.
Martin, FL; Martin-Hirsch, PL; Singh, MN, 2008
)
2.08
"Tamoxifen is an important selective estrogen receptor (ER) modulator for treatment of steroid hormone positive breast cancer. "( Early aberrant insulin-like growth factor signaling in the progression to endometrial carcinoma is augmented by tamoxifen.
Beckmann, MW; Ellmann, S; Fasching, PA; Hartmann, A; Loprich, E; Stiegler, E; Strick, R; Strissel, PL; Thiel, F, 2008
)
2
"Tamoxifen is a nonsteroidal estrogen-receptor modulator widely used in the treatment of breast cancer. "( Studies on tamoxifen encapsulated in lipid vesicles: effect on the growth of human breast cancer MCF-7 cells.
Bhatia, A; Bhushan, S; Katare, OP; Singh, B, 2009
)
2.19
"Tamoxifen is a partial ER antagonist that is highly effective in the treatment of receptor positive breast cancer. "( HER2 overexpression and activation, and tamoxifen efficacy in receptor-positive early breast cancer.
Fink-Retter, A; Gschwantler-Kaulich, D; Helmy, S; Hudelist, G; Kubista, E; Lamm, W; Pfeiler, G; Singer, CF; Spiess, AC; Walter, I, 2009
)
2.06
"Tamoxifen therapy is a standard in the treatment of estrogen receptor (ER)-positive breast cancer; however, its efficacy varies widely among patients. "( A polymorphism in the TC21 promoter associates with an unfavorable tamoxifen treatment outcome in breast cancer.
Amaral, SM; Antoniadou, L; Brauch, H; Eichelbaum, M; Fritz, P; Glavac, D; Rokavec, M; Schroth, W; Schwab, M; Simon, W, 2008
)
2.02
"Tamoxifen appears to be an effective agent for the treatment of epistaxis due to HHT."( Antiestrogen therapy for hereditary hemorrhagic telangiectasia: a double-blind placebo-controlled clinical trial.
Hadar, T; Haddad, M; Preis, M; Shvero, J; Yaniv, E, 2009
)
1.8
"Tamoxifen (TAM) is a selective estrogen receptor modulator widely used in the prevention and treatment of breast cancer. "( Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites.
Amin, S; Blevins-Primeau, AS; Chen, G; Gallagher, CJ; Lazarus, P; Sharma, AK; Sun, D, 2009
)
2.02
"Tamoxifen (TAM) is a selective estrogen receptor modulator that is widely used in the prevention and treatment of estrogen receptor-positive (ER(+)) breast cancer. "( Potential role of UGT pharmacogenetics in cancer treatment and prevention: focus on tamoxifen.
Blevins-Primeau, AS; Lazarus, P; Sun, D; Zheng, Y, 2009
)
2.02
"Tamoxifen resistance is a major cause of death in patients with recurrent breast cancer. "( Identification of a putative protein profile associated with tamoxifen therapy resistance in breast cancer.
den Bakker, MA; Foekens, JA; Jaitly, N; Kang, H; Look, MP; Luider, TM; Martens, JW; Meijer-van Gelder, ME; Pasa-Tolić, L; Timmermans, AM; Umar, A, 2009
)
2.04
"Tamoxifen is a first-generation selective estrogen-receptor modulator that has been shown to decrease recurrence and prolong survival among premenopausal women with breast cancer; however, it also results in estrogen-insufficiency symptoms, the most common being hot flushes."( Acute tamoxifen-induced depression and its prevention with venlafaxine.
Bourque, F; Cohen, V; Karama, S; Looper, K,
)
2.05
"Tamoxifen (TAM) is a nonsteroidal antiestrogen that has been used in the treatment of breast cancer for over 30years. "( Antiproliferation and apoptosis induced by tamoxifen in human bile duct carcinoma QBC939 cells via upregulated p53 expression.
Chen, QX; Han, P; Hu, SX; Kang, JH; Li, HL; Li, WG; Lian, HH; Qiu, PP; Zhang, J, 2009
)
2.06
"Tamoxifen is a standard endocrine therapy for the prevention and treatment of steroid hormone receptor-positive breast cancer."( Pharmacogenomics of tamoxifen therapy.
Brauch, H; Eichelbaum, M; Mürdter, TE; Schwab, M, 2009
)
2.12
"Tamoxifen is a selective estrogen receptor modulator (SERM), which is used for the treatment of primary breast cancer and for the prevention of contralateral breast cancer."( Tamoxifen and the risk of ovarian cancer in BRCA1 mutation carriers.
Domchek, S; Isaacs, C; Kauff, ND; Lubinski, J; Lynch, HT; Narod, SA; Rosen, B; Sun, P; Tung, N; Vicus, D, 2009
)
2.52
"Tamoxifen resistance is a major clinical problem in the treatment of estrogen receptor alpha-positive breast tumors. "( The antipsychotic drug chlorpromazine enhances the cytotoxic effect of tamoxifen in tamoxifen-sensitive and tamoxifen-resistant human breast cancer cells.
Bennetzen, MV; Clausen, MP; Guerra, B; Lykkesfeldt, AE; Mouritsen, OG; Yde, CW, 2009
)
2.03
"Tamoxifen is a standard endocrine therapy for the treatment of steroid receptor positive breast cancer. "( Targeting of tamoxifen to enhance antitumour action for the treatment and prevention of breast cancer: the 'personalised' approach?
Brauch, H; Jordan, VC, 2009
)
2.16
"Tamoxifen citrate is an antiestrogen for peroral breast cancer treatment. "( Self-nanoemulsifying drug delivery systems of tamoxifen citrate: design and optimization.
Abdallah, OY; El-Massik, MA; Elnaggar, YS, 2009
)
2.05
"Tamoxifen is a widely known anti-estrogen which has been employed in adjuvant treatment of early-stage, estrogen-sensitive breast cancer for over 20 years. "( The effects of tamoxifen on immunity.
Behjati, S; Frank, MH, 2009
)
2.15
"Tamoxifen is a synthetic non steroidal anti-estrogen used to treat patients with breast cancer and healthy subjects with high risk of breast cancer. "( Acute tamoxifen treatment increases nitric oxide level but not total antioxidant capacity and adenosine deaminase activity in the plasma of rabbits.
Atakisi, E; Atakisi, O; Kart, A; Topcu, B,
)
2.05
"Tamoxifen is a nonsteroidal estrogen receptor modulator indicated in the treatment of breast cancer. "( Tamoxifen-encapsulated vesicular systems: cytotoxicity evaluation in human epidermal keratinocyte cell line.
Bhatia, A; Bhushan, S; Katare, OP; Singh, B, 2010
)
3.25
"Tamoxifen (TAM) is a selective estrogen-receptor modulator that is widely used in the prevention and treatment of estrogen-receptor-positive breast cancer. "( Potential role of UGT pharmacogenetics in cancer treatment and prevention: focus on tamoxifen and aromatase inhibitors.
Lazarus, P; Sun, D, 2010
)
2.03
"Tamoxifen is an orally active selective estrogen receptor modulator that is used in the treatment of breast cancer and is currently the world's largest selling drug for that purpose. "( Tamoxifen and arrhythmia.
Kopecky, J; Petera, J; Priester, P; Slovacek, L, 2010
)
3.25
"Tamoxifen is a drug of choice for endocrine-responsive breast tumor patients. "( Combinational treatment of gap junctional activator and tamoxifen in breast cancer cells.
Gakhar, G; Hua, DH; Nguyen, TA, 2010
)
2.05
"Tamoxifen is a widely used chemotherapeutic agent, which has been associated with prolongation of the QT interval. "( 4-Hydroxytamoxifen inhibits K(+) currents in mouse ventricular myocytes.
El Gebeily, G; Fiset, C, 2010
)
2.22
"Tamoxifen is a prodrug mainly metabolized by the CY2D6 cytochrome. "( [CYP2D6 polymorphisms and tamoxifen: therapeutic perspectives in the management of hormonodependent breast cancer patients].
Barrière, J; Ferrero, JM; Formento, JL; Milano, G, 2010
)
2.1
"Tamoxifen is an important drug for treating breast cancer. "( Tamoxifen for relapse of ovarian cancer.
Bryant, A; Simera, I; Williams, C, 2010
)
3.25
"Tamoxifen (TAM) is a selective OR modulator."( Tamoxifen-loaded liposomal topical formulation arrests hair growth in mice.
Amarji, B; Bhatia, A; Katare, OP; Singh, B, 2010
)
2.52
"Tamoxifen seems to be an effective agent in the prevention of HTSs after surgery."( Evaluating tamoxifen effect in the prevention of hypertrophic scars following surgical incisions.
Aminseresht, M; Behjoo, S; Mousavi, SR; Raaiszadeh, M, 2010
)
2.19
"Tamoxifen is an anti-estrogen drug widely used for the treatment of hormone-sensitive breast cancer. "( Tamoxifen induces triacylglycerol accumulation in the mouse liver by activation of fatty acid synthesis.
Cole, LK; Jacobs, RL; Vance, DE, 2010
)
3.25
"Tamoxifen is a synthetic non-steroidal Selective Estrogen Receptor Modulator used in the treatment of breast cancer and in treatment of male fertility. "( Chromosomal aberration in the post-implantation embryos sired by tamoxifen treated male rats.
Balasinor, NH; Kedia-Mokashi, N; Makawy, AE; Saxena, M, 2010
)
2.04
"Tamoxifen is an antagonist of estrogen receptor as well."( Double-blind, randomized, placebo-controlled 6-week study on the efficacy and safety of the tamoxifen adjunctive to lithium in acute bipolar mania.
Ahmadi-Abhari, SA; Akhondzadeh, S; Amrollahi, Z; Esfandiari, GR; Ghebleh, F; Maroufi, A; Modabbernia, AH; Naderi, M; Rezaei, F; Sadeghi, M; Salehi, B; Tabrizi, M, 2011
)
2.03
"Tamoxifen is an antiestrogenic agent used widely in the treatment of estrogen receptor-positive breast cancer. "( Gene expression profiling of murine hepatic steatosis induced by tamoxifen.
Kang, KS; Kim, JH; Kim, JW; Kong, G; Lee, MH; Lee, MO, 2010
)
2.04
"Tamoxifen is a high risk factor for an increased risk of endometrial lesions for menopausal women and ovarian cysts for premenopausal women. "( [Follow-up of benign gynecologic diseases in patients treated with tamoxifen for breast cancer].
Jiang, HC; Li, J; Li, L; Wang, SZ; Zhai, Y; Zhang, ZY, 2010
)
2.04
"Tamoxifen is an estrogen receptor (ER) blocker that is used for ER positive breast cancer treatment."( Chemo-resistant melanoma sensitized by tamoxifen to low dose curcumin treatment through induction of apoptosis and autophagy.
Chatterjee, SJ; Pandey, S, 2011
)
1.36
"Tamoxifen is a non-steroidal anti-estrogen drug widely used in the treatment of patients with estrogen receptor-positive breast cancer."( Effects of various agents on DNA fragmentation and telomerase enzyme activities in adenocarcinoma cell lines.
Basaran, A; Cosan, DT; Degirmenci, I; Gunes, HV; Sahin, FM; Soyocak, A, 2011
)
1.09
"Tamoxifen is a selective estrogen receptor modulator widely used in the treatment of hormone-responsive breast cancer. "( Crystalline maculopathy: a rare complication of tamoxifen therapy.
Krishnaswamy, M; Mukesh, S; Srikantia, N,
)
1.83
"Tamoxifen is a selective oestrogen receptor modulator widely used in the prevention and treatment of breast cancer. "( Upregulation of ventricular potassium channels by chronic tamoxifen treatment.
El Gebeily, G; Fiset, C, 2011
)
2.06
"Tamoxifen (TAM) is a nonsteroidal antiestrogen that has been widely used in the treatment of breast cancer through its anti-estrogen activity. "( Ubiquitin ligase c-Cbl is involved in tamoxifen-induced apoptosis of MCF-7 cells by downregulating the survival signals.
Hou, KZ; Liu, J; Liu, YP; Qu, JL; Qu, XJ; Teng, YE; Xu, L; Yan, SC; Zhang, LY; Zhang, Y, 2011
)
2.08
"Tamoxifen citrate is a selective inhibitor of oestrogen receptors and exerts a potent anti-oestrogen effect on the mammary gland."( Evaluation of adverse effects in tamoxifen exposed healthy female dogs.
Bertagnolli, AC; Carneiro, RA; Cassali, GD; Cavalcanti, GA; Figueiredo, MS; Lavalle, GE; Melo, MM; Paes, PR; Souza, AG; Tavares, WL; Viana, FA, 2010
)
1.36
"Tamoxifen is a pro-drug that is metabolised to its active metabolites by the cytochrome P450 (CYP) enzymes including CYP2D6, CYP3A, CYP2B6, and CYP2C19."( Tamoxifen, cytochrome P450 genes and breast cancer clinical outcomes.
Francis, PA; Michael, M; Singh, MS, 2011
)
2.53
"Tamoxifen is a triphenylethylene derivative commonly used in the treatment of breast cancer The Wistar rats (9 weeks old, 180-200 g body weight) used in these trials were divided into two groups of 20 animals each (control and experimental group). "( Ultrastructural effects of tamoxifen on uterus in rats.
Deveci, E; Deveci, S; Nasir, Y, 2009
)
2.09
"Tamoxifen is a nonsteroidal antiestrogen that is currently and widely used in the treatment of breast cancer in all of its stages, in adjuvant therapy as a long-term suppressant of tumor recurrence and also as a chemopreventive agent in women that are in high risk of developing this type of estrogen-dependent cancer. "( An electrochemical outlook on tamoxifen biotransformation: current and future prospects.
Borges, F; Garrido, JM; Garrido, PJ; Manuela, E; Oliveira-Brett, AM, 2011
)
2.1
"Tamoxifen resistance is a major problem in the treatment of estrogen receptor (ER)-positive patients. "( HEXIM1 is a critical determinant of the response to tamoxifen.
Albert, JM; Ketchart, W; Kresak, A; Montano, MM; Ogba, N; Pink, JJ, 2011
)
2.06
"Tamoxifen is a selective estrogen receptor (ER) modulator, but it is also a deactivating ligand for estrogen-related receptor-γ (ERRγ) and a full agonist for the G protein-coupled estrogen receptor (GPER). "( Tamoxifen regulation of bone growth and endocrine function in the ovariectomized rat: discrimination of responses involving estrogen receptor α/estrogen receptor β, G protein-coupled estrogen receptor, or estrogen-related receptor γ using fulvestrant (ICI
Fitts, JM; Klein, RM; Powers, CA, 2011
)
3.25
"Tamoxifen is a non-steroid antiestrogen, used as adjuvant therapy for breast carcinoma in women with positive estrogen receptor (ER+). "( [Tamoxifen and endometrial pathology].
Mihailovici, MS; Negoiţă, M; Terinte, C,
)
2.48
"Tamoxifen is a selective estrogen receptor (ER) modulator which is widely used to treat and prevent breast cancer."( The effect of renin angiotensin system on tamoxifen resistance.
Abedtash, H; Ardeshir-Rouhani-Fard, S; Namazi, S, 2011
)
1.35
"Tamoxifen (TAM) is a non-steroidal antiestrogen used in the treatment and prevention of hormone-dependent breast cancer. "( The effect of the oral iron chelator deferiprone on the liver damage induced by tamoxifen in female rats.
Cerná, P; Eybl, V; Kotyzová, D, 2011
)
2.04
"Tamoxifen is a selective estrogen receptor modulator. "( Tamoxifen treatment for intracerebral hemorrhage.
Guan, J; Hua, Y; Keep, RF; Wu, G; Xi, G; Xie, Q, 2011
)
3.25
"Tamoxifen appears to be an effective agent for the treatment of epistaxis due to HHT."( Anti-estrogen therapy for hereditary hemorrhagic telangiectasia - a long-term clinical trial.
Hadar, T; Nageris, B; Preis, M; Shevro, J; Yaniv, E, 2011
)
1.81
"Tamoxifen is a known anti-cancer drug and established estrogen receptor modulator. "( Anti-thrombotic effects of selective estrogen receptor modulator tamoxifen.
Dash, D; Kumar, A; Nayak, MK; Prakash, V; Roy, A; Singh, SK, 2011
)
2.05
"Tamoxifen is a selective estrogen receptor antagonist that is widely used for treatment and prevention of breast cancer. "( Tamoxifen promotes superoxide production in platelets by activation of PI3-kinase and NADPH oxidase pathways.
Blackmore, PF; Chegini, HA; Dobrydneva, Y; Shah, VP; Vishneski, SR; Weatherman, RV, 2012
)
3.26
"Tamoxifen is a substrate of P-glycoprotein (P-gp) and microsomal cytochrome P450 (CYP) 3A, and biochanin A (BCA) is an inhibitor of P-gp and CYP3A."( Liquid chromatography-mass spectrometry method for the quantification of tamoxifen and its metabolite 4-hydroxytamoxifen in rat plasma: application to interaction study with biochanin A (an isoflavone).
Ali, MM; Jain, GK; Kohli, K; Singh, SP, 2011
)
1.32
"Tamoxifen is an essential drug in treating hormone receptor-positive breast cancer and has been used successfully for the past three decades. "( Adherence to long-term adjuvant hormonal therapy for breast cancer.
Dunn, J; Gotay, C, 2011
)
1.81
"Tamoxifen is a triphenylethylene non-steroidal oestrogen antagonist widely used in oestrogen receptor-positive breast cancer, with well-documented ocular side-effects. "( Tamoxifen keratopathy as seen with in-vivo confocal microscopy.
Collins, CE; Lim, LT; Ramaesh, K; Tarafdar, S,
)
3.02
"Tamoxifen is a selective estrogen-receptor modulator that is commonly utilized in the treatment and prevention of endocrine receptor-positive breast cancer. "( Use of CYP2D6 genotyping in practice: tamoxifen dose adjustment.
McLeod, H; Walko, CM, 2012
)
2.09
"Tamoxifen is an effective antiestrogen used in the treatment of hormone receptor-positive breast cancer. "( Tamoxifen and CYP2D6: a contradiction of data.
Hertz, DL; Irvin, WJ; McLeod, HL, 2012
)
3.26
"Tamoxifen is a selective oestrogen receptor modulator used in pre-menopausal oestrogen receptor positive breast cancer patients as adjuvant endocrine treatment. "( Stopping tamoxifen peri-operatively for VTE risk reduction: a proposed management algorithm.
Hussain, T; Kneeshaw, PJ, 2012
)
2.24
"Tamoxifen (TAM) is a non-steroidal estrogen receptor modulator known for its anticancer activity. "( Tamoxifen-loaded novel liposomal formulations: evaluation of anticancer activity on DMBA-TPA induced mouse skin carcinogenesis.
Amarji, B; Bhatia, A; Katare, OP; Raza, K; Shukla, A; Singh, B, 2012
)
3.26
"Tamoxifen is a mainstay in the treatment of hormone-receptor sensitive breast cancer. "( Impact of CYP2D6 polymorphism on tamoxifen therapy: where are we?
Aigner, I; Haschke-Becher, E; Huber-Wechselberger, AE; Niedetzky, P, 2012
)
2.1
"Tamoxifen is an effective treatment for breast cancer but an undesirable side-effect is an increased risk of endometrial cancer, particularly rare tumor types associated with poor prognosis. "( Endometrial cancer survival after breast cancer in relation to tamoxifen treatment: pooled results from three countries.
Bernstein, L; Hollema, H; Hoogendoorn, WE; Jones, ME; Mourits, MJ; Press, MF; Swerdlow, AJ; van Boven, H; van Leeuwen, FE, 2012
)
2.06
"Tamoxifen is a selective estrogen receptor modulator widely used in the treatment of hormone-responsive breast cancer. "( The eyes have it! Tamoxifen maculopathy revisited: a case report.
Das, D; Gandhi, RA; Goyal, A; Nair, AG, 2012
)
2.16
"Tamoxifen is a selective estrogen receptor modulator (SERM) that is used widely in the treatment of estrogen receptor positive breast cancer (ER+). "( Therapeutic drug monitoring of tamoxifen using LC-MS/MS.
Lynch, KL; Tchu, SM; Wu, AH, 2012
)
2.11
"Tamoxifen is a standard therapeutical treatment in patients with estrogen receptor positive breast carcinoma. "( The impact of PTEN tumor suppressor gene on acquiring resistance to tamoxifen treatment in breast cancer patients.
Davidovic, R; Dimitrijevic, B; Dramicanin, T; Dzodic, R; Juranic, Z; Milovanovic, Z; Plesinac-Karapandzic, V; Susnjar, S; Tanic, N; Tatic, S, 2012
)
2.06
"Tamoxifen (TAM) is a selective estrogen receptor modulator."( Hepatoprotective effect of tamoxifen on steatosis and non-alcoholic steatohepatitis in mouse models.
Fukami, T; Miyashita, T; Nakajima, M; Toyoda, Y; Tsuneyama, K; Yokoi, T, 2012
)
1.4
"Tamoxifen is a triphenylethylene non-steroidal antiestrogen anticancer agent. "( Tamoxifen inhibits migration of estrogen receptor-negative hepatocellular carcinoma cells by blocking the swelling-activated chloride current.
Chen, L; Jin, X; Li, H; Mao, J; Wang, L; Xu, B; Yuan, J; Zhang, H; Zhu, J, 2013
)
3.28
"Tamoxifen (Tmx) is a nonsteroidal selective estrogen receptor antagonist and is frequently used in the treatment and prevention of breast cancer. "( Voltage-dependent open-channel block of G protein-gated inward-rectifying K(+) (GIRK) current in rat atrial myocytes by tamoxifen.
Kienitz, MC; Pott, L; Vanheiden, S, 2012
)
2.03
"Tamoxifen is a drug that has been in worldwide use for the treatment of estrogen receptor (ER)-positive breast cancer for over 30 years; it has been used in both the metastatic and adjuvant settings. "( 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
)
2.12
"Tamoxifen is a safe and viable therapeutic option in the treatment of iRPF."( Long-term safety and efficacy of a tamoxifen-based treatment strategy for idiopathic retroperitoneal fibrosis.
Hendriksz, TR; Pelkmans, LG; van Bommel, EF; van Damme, H, 2013
)
2.11
"Tamoxifen acts as an estrogen inhibitor on the mammary gland, but stimulates postmenopausal uterine mucosa in about 25% of cases while decreasing the risk of osteoporosis."( Similarity of uterine mucosa changes in patients treated by raloxifen and tamoxifen.
Lindahl, B; Willèn, H; Willèn, R,
)
1.08
"Tamoxifen is a selective estrogen receptor modulator (SERM) with pro- and anti-estrogenic properties. "( [Tamoxifen and breast cancer].
Nechushtan, H; Peretz, T, 2002
)
2.67
"Tamoxifen is a potent hepatocarcinogen in the rat, probably via a genotoxic mechanism."( The mutational signature of alpha-hydroxytamoxifen at Hprt locus in Chinese hamster cells.
Boobis, AR; Davies, DS; Yadollahi-Farsani, M, 2002
)
1.3
"Tamoxifen is a selective estrogen-receptor modulator with estrogen-like effects on cardiovascular risk factors but as-yet unexplored effects on carotid artery structure."( Influence of tamoxifen on carotid intima-media thickness in postmenopausal women.
Boutouyrie, P; Jaillon, P; Laloux, B; Laurent, S; Simon, JM; Simon, T; Tournigand, C; Tropeano, AI, 2002
)
1.41
"Tamoxifen (TAM) is an important chemotherapeutic agent for the treatment of breast cancer. "( 4-Hydroxytamoxifen sulfation metabolism.
Chen, G; Maiti, S; Shao, X; Yin, S, 2002
)
2.17
"Tamoxifen alone is an adequate alternative treatment in very old or frail patients."( Tamoxifen alone versus adjuvant tamoxifen for operable breast cancer of the elderly: long-term results of the phase III randomized controlled multicenter GRETA trial.
Ceccherini, R; De Matteis, A; Farris, A; Maiorino, L; Milani, S; Mustacchi, G; Pluchinotta, A; Sasso, F; Scanni, A, 2003
)
2.48
"Tamoxifen is a widely used breast cancer therapeutic and preventative agent. "( Tamoxifen functions as a molecular agonist inducing cell cycle-associated genes in breast cancer cells.
Afshari, CA; Aldaz, CM; Bennett, L; Bushel, PR; Cook, JD; Hodges, LC; Li, L; Lobenhofer, EK; Walker, CL, 2003
)
3.2
"Tamoxifen is an estrogen receptor antagonist used in the treatment of breast cancer. "( Tamoxifen inhibits Na+ and K+ currents in rat ventricular myocytes.
He, J; Kargacin, GJ; Kargacin, ME; Ward, CA, 2003
)
3.2
"Tamoxifen is a non-steroidal triphenylethylene derivate, with clear antioestrogenic effects on the breast, that is orally administrated for the treatment of breast cancer and its prevention in a high-risk population. "( Effects of tamoxifen on the human female genital tract: review of the literature.
Akrivis, Ch; Polyzos, D; Varras, M, 2003
)
2.15
"Tamoxifen is a nonsteroidal antiestrogen that is commonly used in the treatment of breast cancer. "( Inhibition of cloned HERG potassium channels by the antiestrogen tamoxifen.
Gut, B; Karle, CA; Karsai, S; Kathöfer, S; Katus, HA; Kiehn, J; Schoels, W; Thomas, D; Wendt-Nordahl, G; Wimmer, AB; Wu, K; Zhang, W, 2003
)
2
"Tamoxifen (TX) is an antiestrogen with varying levels of antagonist/agonist activity on the reproductive axis of the rat. "( Tamoxifen induces gonadotropin-releasing hormone self-priming through an estrogen-dependent progesterone receptor expression in the gonadotrope of the rat.
Aguilar, R; Alonso, R; Bellido, C; Martín de las Mulas, J; Sánchez-Criado, JE; Tena-Sempere, M, 2003
)
3.2
"Tamoxifen is an adjuvant chemotherapeutic agent for the treatment of breast cancer and a chemoprotective agent for breast cancer prevention. "( Synthesis and investigation of alpha-hydroxy-N,N-didesmethyltamoxifen as a proximate carcinogen in the metabolic activation of tamoxifen.
Beland, FA; Freeman, JP; Gamboa da Costa, G; Marques, MM, 2003
)
2
"Tamoxifen is a selective estrogen receptor modulator (SERM) used for the treatment and prevention of breast cancer. "( Tamoxifen is a potent inhibitor of cholesterol esterification and prevents the formation of foam cells.
Bernad, J; Bosser, I; de Medina, P; Favre, G; Faye, JC; Payré, BL; Pipy, B; Poirot, M; Silvente-Poirot, S, 2004
)
3.21
"Oral tamoxifen is an effective treatment for physiological gynaecomastia, especially for the lump type."( Management of physiological gynaecomastia with tamoxifen.
Blamey, RW; Khan, HN; Rampaul, R, 2004
)
1.09
"Tamoxifen is a synthetic, nonsteroidal Type I antiestrogenic compound that competitively blocks estrogen receptors with a mixed antagonist-agonist effect. "( Effect of tamoxifen citrate on reproductive parameters of male dogs.
Arias, D; Corrada, Y; Fava, F; Gobello, C; Rodríguez, R; Spaini, E, 2004
)
2.17
"Tamoxifen is an effective and relatively non-toxic compound used in palliative and adjuvant treatment of breast cancer. "( The effects of tamoxifen on the female genital tract.
Jassem, J; Konefka, T; Senkus-Konefka, E, 2004
)
2.12
"Tamoxifen is a selective estrogen receptor (ER) modulator that is clinically used as an antagonist to treat estrogen-dependent breast cancers but displays unwanted agonistic effects in other tissues. "( Identification of tamoxifen-induced coregulator interaction surfaces within the ligand-binding domain of estrogen receptors.
Buehrer, B; Gustafsson, JA; Heldring, N; Nilsson, M; Treuter, E, 2004
)
2.1
"Tamoxifen is an effective second-line therapy after anastrozole."( Anastrozole ('Arimidex') versus tamoxifen as first-line therapy in postmenopausal women with advanced breast cancer: results of the double-blind cross-over SAKK trial 21/95--a sub-study of the TARGET (Tamoxifen or 'Arimidex' Randomized Group Efficacy and
Aebi, S; Ballabeni, P; Goldhirsch, A; Hess, D; Köberle, D; Pagani, O; Perey, L; Rochlitz, C; Senn, I; Thürlimann, B, 2004
)
1.33
"Tamoxifen (TAM) is an anti-oestrogen used for treatment and prevention of human breast cancer, but it is also related to human endometrial and uterine cancer. "( 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
)
2.11
"Tamoxifen is a selective estrogen receptor modulator with estrogenic effects on cardiovascular risk factors, but its long-term impacts on cerebral vasculature are unknown."( Estrogen and tamoxifen modulate cerebrovascular tone in ovariectomized female rats.
Chan, FL; Chen, ZY; Huang, Y; Laher, I; Tsang, SY; Wong, CM; Yao, X, 2004
)
1.41
"Tamoxifen is a selective estrogen receptor modulator widely used for the prophylactic treatment of breast cancer. "( Molecular characterization of the microsomal tamoxifen binding site.
de Médina, P; Favre, G; Faye, JC; Kedjouar, B; Oulad-Abdelghani, M; Payré, B; Poirot, M; Silvente-Poirot, S, 2004
)
2.03
"Tamoxifen is a selective estrogen-receptor modulator shown to improve several cardiovascular risk factors in postmenopausal women with breast cancer. "( Tamoxifen improves endothelial function and reduces carotid intima-media thickness in postmenopausal women.
Aznaouridis, K; Kumar, S; Lekakis, JP; Papaioannou, TG; Papamichael, CM; Poulakaki, NA; Protogerou, AD; Stamatelopoulos, KS; Stamatelopoulos, SF; Venetsanou, K, 2004
)
3.21
"Tamoxifen (TAM) is a non-steroidal anti-estrogen used to treat patients with estrogen receptor-positive breast cancer and as a chemopreventive agent against breast cancer in high risk pre- and post-menopausal women. "( Cytotoxicity of tamoxifen in normal and tumoral cell lines and its ability to induce cellular transformation in vitro.
de Carvalho, JE; Genari, SC; Kohn, LK; Petinari, L, 2004
)
2.11
"Tamoxifen is a selective estrogen receptor modulator used in estrogen receptor-positive breast cancer. "( Lack of attenuation in the antitumor effect of tamoxifen by chronic CYP isoform inhibition.
Duggan, D; Lehmann, D; Nelsen, J; Newman, N; Ramanath, V; Smith, A, 2004
)
2.02
"Tamoxifen (TAM) is a nonsteroidal antiestrogenic drug that is widely used for the treatment of estrogen receptor-dependent breast cancer. "( Interactions of the stereoisomers of alpha-hydroxytamoxifen with human hydroxysteroid sulfotransferase SULT2A1 and rat hydroxysteroid sulfotransferase STa.
Apak, TI; Duffel, MW, 2004
)
2.02
"Tamoxifen acts as an agonist on genes under the control of an AP-1 response elements when ERalpha or ERbeta is expressed."( Possible interaction between activator protein-1 and proto-oncogene B-cell lymphoma gene 6 in breast cancer patients resistant to tamoxifen.
Altundag, K; Altundag, O; Arun, B; Gunduz, M, 2004
)
1.25
"Tamoxifen is a well-known antiestrogen used for the hormonotherapy of estrogen receptor positive breast cancer. "( Multiple targeting by the antitumor drug tamoxifen: a structure-activity study.
de Médina, P; Favre, G; Poirot, M, 2004
)
2.03
"Tamoxifen is a selective estrogen receptor modulator (SERM) shown in randomized controlled trials to reduce the incidence of estrogen receptor (ER)-positive breast cancer in high-risk healthy women."( Risk-reducing strategies for breast cancer--a review of recent literature.
Mokbel, K,
)
0.85
"Tamoxifen is an effective drug for the treatment and prevention of breast cancer. "( 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
)
2.05
"Tamoxifen (TAM) is a nonsteroidal antioestrogen that is widely used in adjuvant therapy for all stages of breast carcinoma."( Therapeutic effect of tamoxifen and energy-modulating vitamins on carbohydrate-metabolizing enzymes in breast cancer.
Perumal, SS; Sachdanandam, P; Shanthi, P, 2005
)
1.36
"Tamoxifen (TMX) is a nonsteroidal triphenylene derivate with clear antiestrogenic properties on the breast which is used as adjuvant treatment for breast cancer; potential adverse effects include endometrial lesions."( Antiestrogenic therapy in breast cancer and endometrial modifications.
Hannuna, K; Iuele, T; Marziani, R; Melluso, J; Mossa, B; Napolitano, C, 2005
)
1.05
"Tamoxifen is an antiestrogen used in the adjuvant endocrine therapy of early breast cancer and malignant breast disorders. "( Detection of tamoxifen metabolites by GC-MSD.
Báez, H; Camargo, C; Osorio, H; Umpiérrez, F,
)
1.94
"Tamoxifen is an anti-oestrogen widely used in the adjuvant therapy of breast cancer and is also used as a prophylactic to prevent the disease in high-risk women. "( Organ specificity of DNA adduct formation by tamoxifen and alpha-hydroxytamoxifen in the rat: implications for understanding the mechanism(s) of tamoxifen carcinogenicity and for human risk assessment.
Arlt, VM; Churchill, C; Cole, KJ; Hewer, A; Osborne, MR; Phillips, DH, 2005
)
2.03
"Tamoxifen is a widely used drug for chemotherapy and chemoprevention of breast cancer worldwide. "( Investigating DNA adduct-targeted mutagenicity of tamoxifen: preferential formation of tamoxifen-DNA adducts in the human p53 gene in SV40 immortalized hepatocytes but not endometrial carcinoma cells.
Besaratinia, A; Pfeifer, GP, 2005
)
2.02
"Tamoxifen citrate is an anti-estrogenic drug used for the treatment of breast cancer. "( The effect of dimethyl dimethoxy biphenyl dicarboxylate (DDB) against tamoxifen-induced liver injury in rats: DDB use is curative or protective.
El-Beshbishy, HA, 2005
)
2
"Tamoxifen is a widely used adjuvant treatment of breast carcinoma with partial estrogenic agonist effect. "( Metastatic breast lobular carcinoma to tamoxifen-associated endometrial polyp: case report and literature review.
Al-Brahim, N; Elavathil, LJ, 2005
)
2.04
"Tamoxifen is a selective oestrogen receptor modulator (SERM) with anti-oestrogenic activity in the breast and oestrogenic effects in various tissues such as the endometrium, bone and cardiovascular territory. "( Tamoxifen and endometrial cancer. Is screening necessary? A review of the literature.
Abad, L; León, JP; Machado, F; Parrilla, JJ; Rodríguez, JR, 2005
)
3.21
"Tamoxifen (TAM) is a potent antioxidant and a non-steroidal antiestrogen drug most used in the chemotherapy and chemoprevention of breast cancer."( Combined efficacy of tamoxifen and coenzyme Q10 on the status of lipid peroxidation and antioxidants in DMBA induced breast cancer.
Perumal, SS; Sachdanandam, P; Shanthi, P, 2005
)
1.37
"Tamoxifen is a widely used anticancer drug for breast cancer with frequent gastrointestinal side effects. "( [Effects of tamoxifen on the voltage-dependent ionic currents in mouse colonic smooth muscle cells].
Chang, SJ; Choi, S; Jun, JY; Kim, MW; Lee, DM; Lim, GH; Park, CG; Yeum, CH; Yoon, PJ, 2005
)
2.15
"Tamoxifen is an effective treatment for hormone responsive breast cancer and can prevent breast cancer in high-risk women."( [Selective estrogen receptors modulators (SERMs): biochemistry, pharmacology, and clinical use in gynecology].
Teppa Garrán, AD; Terán Dávila, J, 2005
)
1.05
"Tamoxifen is an anti-estrogenic agent for the treatment of breast cancer, while exhibiting estrogenic activity in such tissues as the uterus. "( Assessment of anti-estrogenic activity of tamoxifen in transgenic mice expressing an enhanced green fluorescent protein gene regulated by estrogen response element.
Enzan, H; Hayashi, Y; Okada, T; Saibara, T; Toda, K, 2006
)
2.04
"Tamoxifen acts as an oestrogen antagonist in the breast reducing cell proliferation, but in the uterus as an oestrogen agonist resulting in increased cell proliferation. "( Influence of oestradiol and tamoxifen on oestrogen receptors-alpha and -beta protein degradation and non-genomic signalling pathways in uterine and breast carcinoma cells.
Guerin, CJ; Horner-Glister, E; Johnson, SM; Maleki-Dizaji, M; Styles, J; White, IN, 2005
)
2.07
"Tamoxifen is a known hepatocarcinogen in rats and is associated with an increased incidence of endometrial cancer in patients. "( Characterization of the human cytochrome P450 forms involved in metabolism of tamoxifen to its alpha-hydroxy and alpha,4-dihydroxy derivatives.
Crewe, KH; Gillam, EM; Lennard, MS; Notley, LM; Taylor, PJ, 2005
)
2
"Tamoxifen is a non-steroidal anti-estrogen used for the treatment of breast cancer and, more recently, as a chemopreventive agent in healthy women at high risk of developing breast cancer. "( Effect of long-term tamoxifen exposure on genotoxic and epigenetic changes in rat liver: implications for tamoxifen-induced hepatocarcinogenesis.
Beland, FA; Churchwell, MI; Kovalchuk, O; Montgomery, B; Muskhelishvili, L; Pogribny, IP; Rodriguez-Juarez, R; Ross, SA; Tryndyak, VP, 2006
)
2.1
"Tamoxifen (TAM) is an important endocrine therapeutic drug used in combined treatment for breast cancer. "( [Involvement of epidermal growth factor receptor signaling pathway in tamoxifen resistance of MCF-7 cells].
Wang, XY; Wu, ZY; Zhen, LL; Zheng, W; Zhu, X, 2006
)
2.01
"Tamoxifen is a prototypic cancer chemopreventive agent, yet clinical trials have not evaluated its effect on mortality or the impact of drug pricing on its cost-effectiveness."( Chemoprevention: drug pricing and mortality: the case of tamoxifen.
Barnato, A; Birch, S; Helms, LJ; Kuenneth, C; Kuppermann, M; Melnikow, J; Nuovo, J, 2006
)
2.02
"Tamoxifen (TAM) is an antiestrogen widely used in the treatment and prevention of breast cancer in women. "( Characterization of tamoxifen and 4-hydroxytamoxifen glucuronidation by human UGT1A4 variants.
Chen, G; Dellinger, RW; Duncan, K; Fang, JL; Lazarus, P; Sun, D, 2006
)
2.1
"Tamoxifen is an important estrogen receptor antagonist used successfully for the treatment and prevention of breast cancer. "( Quantification of tamoxifen and metabolites and soy isoflavones in human plasma using liquid chromatography with electrospray ionization tandem mass spectrometry.
Churchwell, MI; Doerge, DR; Twaddle, NC; Williams, LD,
)
1.91
"Tamoxifen is an effective drug, but its role in prevention is limited by its adverse effect profile. "( Influence of hormone replacement therapy on tamoxifen-induced vasomotor symptoms.
Cuzick, J; Edwards, R; Forbes, J; Kealy, R; Sestak, I, 2006
)
2.04
"Tamoxifen is a nontoxic inhibitor of P-glycoprotein."( Randomized study of paclitaxel and tamoxifen deposition into human brain tumors: implications for the treatment of metastatic brain tumors.
Balmaceda, C; Bertino, JS; Bruce, JN; Chen, J; Desai, M; Fetell, MR; Fine, RL; Goodman, RR; Huang, M; McKhann, GM; Nafziger, AN; Sisti, MB, 2006
)
1.33
"Tamoxifen is a cheap and effective estrogen-receptor antagonist, used as the adjuvant hormonal treatment of choice in women with estrogen-receptor-positive breast cancer. "( Tamoxifen-induced non-alcoholic steatohepatitis: where are we now and where are we going?
Ahmed, MH; Osman, KA; Osman, MM, 2007
)
3.23
"Tamoxifen is an anticancer drug that induces oxidative stress and apoptosis via mitochondria-dependent and nitric oxide (NO)-dependent pathways. "( Tamoxifen induces oxidative stress and mitochondrial apoptosis via stimulating mitochondrial nitric oxide synthase.
Alidema, E; Choi, J; Ghafourifar, P; Larson, SK; Nazarewicz, RR; Parihar, A; Zenebe, WJ, 2007
)
3.23
"Tamoxifen (TAM) is a synthetic non-steroidal anti-estrogen compound that is widely used as an effective chemotherapeutic agent for treatment and prevention of breast cancer. "( Tamoxifen-induced activation of p21Waf1/Cip1 gene transcription is mediated by Early Growth Response-1 protein through the JNK and p38 MAP kinase/Elk-1 cascades in MDA-MB-361 breast carcinoma cells.
Choi, BH; Kim, CG; Lee, YH; Shin, SY; Son, SW; Yi, SJ, 2007
)
3.23
"Tamoxifen is a selective estrogen receptor modulator that is used to treat and to prevent breast cancer; however, its use is associated with an increased risk of endometrial cancer. "( Association between CYP3A4 genotype and risk of endometrial cancer following tamoxifen use.
Chu, W; Fyles, A; McCready, DR; Murphy, J; Narod, SA; Pal, T; Sellers, EM, 2007
)
2.01
"Tamoxifen is a mixed estrogen agonist and antagonist, which is used in treatment and prevention of breast cancer as an estrogen antagonist."( Role of endothelin-1 in tamoxifen resistance: Mechanism for a new possible treatment strategy in breast cancer.
Abedtash, H; Namazi, S; Rouhani Fard, SA, 2008
)
1.37
"Tamoxifen (TAM) is a non-steroidal anti-estrogen used widely in the treatment and chemoprevention of breast cancer. "( The DNA-damaging potential of tamoxifen in breast cancer and normal cells.
Blasiak, J; Blasinska-Morawiec, M; Kolacinska, A; Morawiec, Z; Morawiec-Bajda, A; Wozniak, K; Zadrozny, M, 2007
)
2.07
"Tamoxifen (TAM) is a non-steroidal antiestrogen drug, which is widely used to prevent and treat breast, liver, pancreas and brain cancers. "( Concentration dependent different action of tamoxifen on membrane fluidity.
Kazanci, N; Severcan, F, 2007
)
2.04
"Tamoxifen (TAM) is a nonsteroidal triphenylethylene antiestrogenic drug widely used in the treatment and prevention of breast cancer. "( Catechin as an antioxidant in liver mitochondrial toxicity: Inhibition of tamoxifen-induced protein oxidation and lipid peroxidation.
Banerjee, BD; Parvez, S; Raisuddin, S; Rehman, H; Tabassum, H, 2007
)
2.01
"Tamoxifen (TAM) is a nonsteroidal antiestrogen that prevents estrogen receptor-positive breast cancer in rodents and humans. "( Subchronic toxicity and toxicogenomic evaluation of tamoxifen citrate + bexarotene in female rats.
Crowell, JA; Cwik, MJ; Detrisac, CJ; Horn, TL; Kapetanovic, IM; Lubet, RA; McCormick, DL; Naylor, JM; Torres, KE, 2007
)
2.03
"Tamoxifen (TAM) is an antiestrogen that has been widely used in the treatment and prevention of breast cancer in women. "( Glucuronidation of active tamoxifen metabolites by the human UDP glucuronosyltransferases.
Amin, S; Balliet, RM; Blevins-Primeau, AS; Boyiri, T; Chen, G; Dellinger, RW; Lazarus, P; Sharma, AK; Sun, D, 2007
)
2.08
"Tamoxifen (TAM) is a non-steroidal anti-estrogen drug most widely used as an adjuvant hormonal therapy in breast cancer."( Augmented antioxidant status in Tamoxifen treated postmenopausal women with breast cancer on co-administration with Coenzyme Q10, Niacin and Riboflavin.
Gangadaran, SG; Premkumar, VG; Sachdanandam, P; Vijayasarathy, K; Yuvaraj, S, 2008
)
1.35
"Tamoxifen (TAM) is an anti-neoplastic drug used for the treatment of breast cancer. "( Nephrotoxicity and its prevention by taurine in tamoxifen induced oxidative stress in mice.
Dev Banerjee, B; Parvez, S; Raisuddin, S; Rehman, H; Siemen, D; Tabassum, H, 2007
)
2.04
"Tamoxifen is a widely used anti-estrogenic drug for chemotherapy and, more recently, for the chemoprevention of breast cancer. "( Gene expression profiling reveals underlying molecular mechanisms of the early stages of tamoxifen-induced rat hepatocarcinogenesis.
Bagnyukova, TV; Beland, FA; Fuscoe, JC; Han, T; Kovalchuk, O; Muskhelishvili, L; Pogribny, IP; Rodriguez-Juarez, R; Ross, SA; Tryndyak, VP, 2007
)
2
"Tamoxifen continues to be a standard endocrine therapy for the prevention and treatment of estrogen receptor (ER)-positive breast cancer. "( Tamoxifen pharmacogenomics: the role of CYP2D6 as a predictor of drug response.
Ames, MM; Goetz, MP; Kamal, A, 2008
)
3.23
"Tamoxifen is an alternative approach only for BRCA2 mutation carriers."( Individualized preventive and therapeutic management of hereditary breast ovarian cancer syndrome.
Briasoulis, E; Roukos, DH, 2007
)
1.06
"Tamoxifen (TAM) is a selective estrogen receptor modulator (SERM) that is widely used as adjuvant therapy in breast cancer patients; however, it is also associated with undesirable side effects. "( Profiles of tamoxifen-related side effects by race and smoking status in women with breast cancer.
Flaws, JA; Gallicchio, L; Lewis, LM; Royak-Schaler, R; Tkaczuk, K; Zhan, M, 2007
)
2.16
"Tamoxifen is an antagonist of estrogen receptor, which is used widely as an estrogen receptor-positive breast cancer drug that blocks growth signals and provokes apoptosis. "( Induction of mitochondria-involved apoptosis in estrogen receptor-negative cells by a novel tamoxifen derivative, ridaifen-B.
Ikekita, M; Miyamoto, T; Nagahara, Y; Nakata, K; Sasaki, A; Shiina, I, 2008
)
2.01
"Tamoxifen is an antioestrogen widely used in the breast cancer treatment. "( [Malignant mixed müllerian tumor of the uterus following tamoxifen for breast cancer: case report].
Akerman, G; Barranger, E; Cote, JF; Gray, F; Malartic, C; Morel, O; Saim, M, 2008
)
2.03
"Tamoxifen is a selective oestrogen receptor modulator widely used in the treatment of breast cancer. "( Taurine prevents tamoxifen-induced mitochondrial oxidative damage in mice.
Banerjee, BD; Parvez, S; Raisuddin, S; Tabassum, H, 2008
)
2.13
"Tamoxifen is a mainstay in the treatment of estrogen receptor (ER)-positive breast cancer patients. "( Sensitizing estrogen receptor-negative breast cancer cells to tamoxifen with OSU-03012, a novel celecoxib-derived phosphoinositide-dependent protein kinase-1/Akt signaling inhibitor.
Brueggemeier, RW; Chen, CS; Kashida, Y; Kulp, SK; Shapiro, CL; Wang, D; Weng, SC, 2008
)
2.03
"Tamoxifen is a nonsteroidal antiestrogen which is used as an adjuvant form of chemotherapy for breast carcinomas containing estrogen receptors. "( Effect of tamoxifen treatment on liver, lung and intestinal mixed-function oxidases in male and female rats.
Al-Turk, WA; Roche, EB; Stohs, SJ,
)
1.98
"Tamoxifen appears to be a useful and safe treatment for recurrent breast cancer."( [A case of recurrent breast cancer responding to long-term administration of tamoxifen].
Inaji, H; Kobayashi, T; Maeura, Y; Mori, T; Yayoi, E, 1984
)
1.22
"Tamoxifen is a potent inhibitor of specific oestrogen-induced yolk protein synthesis by chicken liver. "( High affinity binding of anti-oestrogen to the chick liver nuclear oestrogen receptor.
Jordan, VC; Lazier, CB, 1982
)
1.71
"Tamoxifen seemed to be a useful alternative treatment for this group of patients."( Treatment of early localized breast cancer in elderly patients by Tamoxifen.
Helleberg, A; Lundgren, B; Norin, T; Sander, S, 1982
)
1.22
"Tamoxifen is a commonly used chemotherapeutic agent in human breast cancer, although some tumours develop resistance. "( Tamoxifen and somatostatin affect tumours by inducing apoptosis.
Candi, E; De Laurenzi, V; Guerrieri, P; Knight, RA; Melino, G; Piacentini, M; Spinedi, A, 1995
)
3.18
"4-OH-tamoxifen is an active metabolite of tamoxifen that is detectable in the serum and tumour tissue of patients treated by oral tamoxifen. "( Phase I study of percutaneous 4-hydroxy-tamoxifen with analyses of 4-hydroxy-tamoxifen concentrations in breast cancer and normal breast tissue.
Fournier, S; Fourtillan, JB; Girault, J; Grenier, J; Pujol, H; Pujol, JL; Rouanet, P; Simony, J, 1995
)
1.07
"Tamoxifen is a nonsteroidal antiestrogen that has been shown to reverse drug resistance in vitro in some cancer models through pathways not related to its antiestrogenic effect."( Tamoxifen enhances the chemosensitivity of bladder carcinoma cells.
Cheng, AL; Hsieh, CY; Hsieh, TS; Lai, MK; Pu, YS; Su, IJ; Tsai, TC, 1995
)
2.46
"Tamoxifen was shown to be a good chemosensitizer in a bladder cancer cell model and may well be tried in combination with systemic chemotherapy for metastatic human bladder cancers in the clinical setting."( Tamoxifen enhances the chemosensitivity of bladder carcinoma cells.
Cheng, AL; Hsieh, CY; Hsieh, TS; Lai, MK; Pu, YS; Su, IJ; Tsai, TC, 1995
)
3.18
"Tamoxifen acts as an oestrogen both on genital organs and bones."( [Quality of life analysis in patients treated for breast cancers].
Antoine, JM; Dormont, D; Dutranoy, G; Ferrand, S; Madelenat, P; Ravina, JH; Salat-Baroux, J; Uzan, S; Zylberberg, B, 1994
)
1.73
"Tamoxifen is a specific therapy."( Estrogen dermatitis.
Santoso-Pham, J; Shelley, ED; Shelley, WB; Talanin, NY, 1995
)
1.01
"Tamoxifen alone is an adequate alternative in frail patients."( Tamoxifen or surgery plus tamoxifen as primary treatment for elderly patients with operable breast cancer: The G.R.E.T.A. Trial. Group for Research on Endocrine Therapy in the Elderly.
De Matteis, A; Milani, S; Mustacchi, G; Perrota, A; Pluchinotta, A; Rubagotti, A,
)
2.3
"Tamoxifen is an anti-oestrogen which is currently being assessed as a prophylactic for women at high risk of breast cancer. "( Interaction of tamoxifen with the multidrug resistance P-glycoprotein.
Callaghan, R; Higgins, CF, 1995
)
2.09
"Tamoxifen is an antiestrogen drug used in the treatment of patients with breast cancer that is being studied for use in patients at high risk for developing breast cancer. "( Screening for ocular toxicity in asymptomatic patients treated with tamoxifen.
Dragoo, RA; Enzenauer, RW; Heier, JS; Waterhouse, WJ, 1994
)
1.97
"Tamoxifen is an estrogen antagonist/agonist often associated with antiestrogenic effects such as hot flushes and vaginal dryness in premenopausal women. "( Endometriosis and tamoxifen therapy.
Gincherman, Y; Mikuta, JJ; Morgan, MA, 1994
)
2.07
"Tamoxifen is an antiestrogen frequently used in the treatment of breast cancer and is currently being assessed as a prophylactic for those at high risk of developing tumors. "( Tamoxifen blocks chloride channels. A possible mechanism for cataract formation.
Gill, DR; Hardy, SP; Higgins, CF; Hyde, SC; Jacob, TJ; Mintenig, GM; Sepúlveda, FV; Trezise, AE; Valverde, MA; Zhang, JJ, 1994
)
3.17
"Tamoxifen is an inhibitor of protein kinase C (PKC), a calcium- and phospholipid-dependent serine kinase which plays a critical role in the proliferation of certain cell lines."( A comparison of the relative chemosensitivity of human gliomas to tamoxifen and n-desmethyltamoxifen in vitro.
Kristofik, MP; Randall, MS; Rehn, T; Selker, RG; Vertosick, FT, 1994
)
1.25
"Tamoxifen citrate is a synthetic antiestrogen that provides survival benefit when given as adjuvant treatment in postmenopausal women with breast cancer. "( Protein S and protein C level changes with adjuvant tamoxifen therapy in postmenopausal women.
Feyzi, JM; Love, RR; Mamby, CC, 1994
)
1.98
"Tamoxifen flare is a relatively seldom occurring phenomenon but it can force to therapeutical consequences. "( [Tamoxifen flare].
Görlich, M, 1994
)
2.64
"Tamoxifen (TAM) is a triphenylethylene antiestrogen used for the treatment, and in clinical trials for the prevention, of breast cancer in women. "( Frequent and specific mutations of the rat p53 gene in hepatocarcinomas induced by tamoxifen.
Lazarus, P; Vancutsem, PM; Williams, GM, 1994
)
1.96
"Tamoxifen is an antiestrogen used in adjuvant therapy of breast carcinoma and could potentially prevent the development of mammary cancer. "( Tamoxifen restores the E-cadherin function in human breast cancer MCF-7/6 cells and suppresses their invasive phenotype.
Bracke, ME; Bruyneel, EA; Castronovo, V; Charlier, C; Labit, C; Mareel, MM, 1994
)
3.17
"Tamoxifen is a known structural-mimic of cholesterol, which were both found to be similarly effective in preventing drug release from liposomes."( Tamoxifen decreases drug efflux from liposomes: relevance to its ability to reverse multidrug resistance in cancer cells?
Kayyali, R; Marriott, C; Wiseman, H, 1994
)
2.45
"Tamoxifen is a potent liver carcinogen in rats and has been shown to form covalent DNA adducts in the livers of several species of rodent. "( Co-chromatography of a tamoxifen epoxide-deoxyguanylic acid adduct with a major DNA adduct formed in the livers of tamoxifen-treated rats.
Farmer, PB; Hewer, A; Phillips, DH; White, IN, 1994
)
2.04
"Tamoxifen is an important medicine with beneficial influence on the fibrinolytic system, without affecting the serous coagulation system."( The influence of tamoxifen on plasma coagulation and serous fibrinolysis.
Boryska, M; Jankowski, J; Kopczynski, Z; Ramlau, C, 1993
)
1.35
"Tamoxifen is an established adjuvant therapy for breast cancer. "( [Adverse effects of tamoxifen on the female genital tract].
Anteby, E; Hochner-Celnikier, D; Palti, Z; Yagel, S; Zacut, D, 1993
)
2.05
"Tamoxifen (TAM) is an antiestrogen useful in the treatment and control of breast cancer. "( Structural characterization and biological effects of photocyclized products of tamoxifen irradiation.
Ruenitz, PC; Wilson, S, 1993
)
1.96
"Tamoxifen is a safe and reliable treatment of breast cancer, but data suggest an association with endometrial cancer. "( Gynecologic tumors in tamoxifen-treated women with breast cancer.
Johnson, J; Seoud, MA; Weed, JC, 1993
)
2.04
"Tamoxifen is an antioestrogen drug used widely in the management of oestrogen-dependent metastatic breast carcinoma. "( Ocular toxicity of tamoxifen.
Nagarajan, R; Sekhar, GC, 1995
)
2.06
"Tamoxifen is an oral antiestrogen first used in metastatic breast cancer in the early 1970s. "( Tamoxifen's role in chemoprevention of breast cancer: an update.
Nayfield, SG, 1995
)
3.18
"Tamoxifen is an effective treatment for metastatic and primary breast cancer and is now being evaluated as a chemoprevention agent in healthy women. "( Effect of tamoxifen on bone mineral density measured by dual-energy x-ray absorptiometry in healthy premenopausal and postmenopausal women.
Ashley, S; Hickish, T; Kanis, JA; Powles, TJ; Tidy, A, 1996
)
2.14
"Tamoxifen is a nonsteroidal antiestrogenic drug that has been used successfully for 15 years in the treatment of all stages of breast carcinoma. "( The effects of tamoxifen treatment on the endometrium.
Bar-Am, A; Daniel, Y; Inbar, M; Lessing, JB; Peyser, MR, 1996
)
2.09
"Tamoxifen is a partial agonist, leading to the increase in transcriptional activity."( [Strategy of drug development for hormone-dependent tumor].
Kudoh, M, 1996
)
1.02
"Tamoxifen is an anti-estrogen with proven efficacy and low toxicity in the treatment of breast cancer. "( Radiotherapy-related lung fibrosis enhanced by tamoxifen.
Bentzen, SM; Overgaard, J; Overgaard, M; Skoczylas, JZ, 1996
)
1.99
"Tamoxifen is an effective antioxidant and protects membranes and low-density lipoprotein (LDL) particles against oxidative damage."( Tamoxifen as an antioxidant and cardioprotectant.
Wiseman, H, 1995
)
2.46
"Tamoxifen is a nonsteroidal anti-estrogen frequently used in breast cancer therapy. "( [Surveillance of patients treated with tamoxifen].
Khairallah, T; Salat-Baroux, J; Sananes, S; Touboul, E; Uzan, S, 1996
)
2.01
"Tamoxifen is an oestrogen antagonist with partial agonistic effects that is used extensively in the treatment of mammary carcinoma. "( [Tamoxifen and endometrial cancer. A case report].
Lindal, S; Mortensen, E; Orbo, A, 1996
)
2.65
"Tamoxifen (TAM) is a triphenylethylene anti-oestrogen, commonly used in the treatment of breast cancer. "( Solid-phase extraction and high-performance liquid chromatographic determination of tamoxifen and its major metabolites in plasma.
Cummings, J; Dixon, JM; MacCallum, J; Miller, WR, 1996
)
1.96
"Tamoxifen is a synthetic oestrogen antagonist commonly used as an adjuvant therapy for breast cancer."( Elemental composition of bone minerals in women with breast cancer treated with adjuvant tamoxifen.
Glaros, D; Hatzikonstantinou, I; Kalef-Ezra, JA; Karantanas, A; Klouvas, G; Pavlidis, N, 1996
)
1.24
"Tamoxifen is an effective form of hormonal therapy for breast cancer, although the mechanism by which tamoxifen inhibits tumor growth is not well understood and may involve mechanisms other than the action of tamoxifen as an estrogen antagonist."( Presence of an insulin-like growth factor I autocrine loop predicts uterine fibroid responsiveness to tamoxifen.
Ethier, SP; Howe, SR; Matthews, WJ; Pass, HI; Walker, C, 1996
)
1.23
"Tamoxifen is a non-steroidal antiestrogen that possesses antagonistic as well a agonistic properties, while RU39411 is an antiestrogen that is known to possess only antagonistic properties. "( Tamoxifen and RU39411 synergize with mifepristone to produce preimplantation pregnancy loss by increasing embryo transport (rat).
Bardin, CW; Kaplan-Kraicer, R; Kostovetsky, I; Shalgi, R, 1996
)
3.18
"Tamoxifen is an antiestrogen drug which is used for adjuvant therapy of patients with estrogen positive receptors in breast cancer. "( [Tamoxifen: modern drug therapy of estrogen-dependent breast tumors].
Beleslin, DB; Jovanović-Mićić, D; Nikolić, SS, 1996
)
2.65
"Tamoxifen is a synthetic antiestrogen with both agonist and antagonist properties. "( Tamoxifen in postmenopausal women a safety perspective.
Kimmick, GG; Muss, HB; Robinson, E, 1996
)
3.18
"Tamoxifen is a widely used, effective, and well-tolerated agent in the treatment of primary and recurrent breast cancer. "( Scientific review of tamoxifen. Overview from a medical oncologist.
Carlson, RW, 1997
)
2.06
"Tamoxifen is an effective treatment for early and advanced disease, it has few side effects, it has a low cost, and it is easy to administer."( The control of breast cancer: the role of tamoxifen.
Forbes, JF, 1997
)
1.28
"Tamoxifen is a substituted triphenylethylene antiestrogen used in the adjuvant therapy and chemoprevention of breast cancer. "( Antagonistic and agonistic effects of tamoxifen: significance in human cancer.
Gallo, MA; Kaufman, D, 1997
)
2.01
"Tamoxifen is a highly potent inhibitor of the contractile activity of the human nonpregnant myometrium and uterine arteries. "( Potent inhibition by tamoxifen of spontaneous and agonist-induced contractions of the human myometrium and intramyometrial arteries.
Batra, S; Kostrzewska, A; Laudañski, T, 1997
)
2.06
"Tamoxifen is a mixed estrogen agonist/antagonist that has a proliferative effect on the endometrium."( Benign and hyperplastic endometrial changes associated with tamoxifen use.
Barakat, RR, 1997
)
1.26
"Tamoxifen is a nonsteroidal compound with mixed estrogen agonist and antagonist properties."( Tamoxifen inhibits arterial accumulation of LDL degradation products and progression of coronary artery atherosclerosis in monkeys.
Adams, MR; Golden, DL; Li, Z; Wagner, JD; Williams, JK, 1997
)
2.46
"Tamoxifen is a clinically useful estrogen antagonist at or below 10(-6) M concentration. "( Tamoxifen induces deregulation of [Ca2+] in human breast cancer cells.
Jain, PT; Trump, BF,
)
3.02
"Tamoxifen appears to be an estrogen agonist concerning cathepsin D regulation, whereas ICI 182,780 is a true antagonist."( Western immunoblotting and enzymatic activity analysis of cathepsin D in human breast cancer cell lines of different invasive potential. Regulation by 17beta-estradiol, tamoxifen and ICI 182,780.
Couissi, D; Dubois, V; Remacle, C; Schonne, E; Trouet, A, 1997
)
1.21
"Tamoxifen is a better drug than clomiphene for ovulation induction in women with poor cervical mucus quality."( Effect of two anti-estrogens, clomiphene citrate and tamoxifen, on cervical mucus and sperm-cervical mucus interaction.
Annapurna, V; Dhaliwal, LK; Gopalan, S,
)
1.82
"Tamoxifen is a synthetic estrogen analog which may regulate osteogenesis in vivo by virtue of its antiglucocorticoid properties. "( Tamoxifen attenuates glucocorticoid actions on bone formation in vitro.
Binkert, C; Kohno, H; McCulloch, CA; Rotenberg, B; Sukhu, B; Tenenbaum, HC; Zohar, R, 1997
)
3.18
"Tamoxifen treatment is a proven therapy for breast cancer that produces a survival advantage when used as an adjuvant, and reduces the incidence of recurrences and controlateral tumor evolution. "( Acute leukaemia during tamoxifen therapy.
Demiroğlu, H; Güllü, I; Tekuzman, G; Yalçin, S, 1997
)
2.05
"Tamoxifen is a nonsteroidal antiestrogenic drug used successfully to reduce recurrences in all stages of breast carcinoma. "( Endometrial changes with chronic tamoxifen use.
Loret de Mola, JR, 1997
)
2.02
"Tamoxifen is an effective agent preventing mammary carcinogenesis in rats but causing liver tumours. "( Idoxifene is equipotent to tamoxifen in inhibiting mammary carcinogenesis but forms lower levels of hepatic DNA adducts.
Bliss, J; Coombes, RC; Hewer, A; Jarman, M; Pace, P; Phillips, D, 1997
)
2.04
"Tamoxifen is a mixed estrogen agonist/antagonist with as yet unexplored effects on vascular function."( Contrasting effects of conjugated estrogens and tamoxifen on dilator responses of atherosclerotic epicardial coronary arteries in nonhuman primates.
Adams, MR; Honoré, EK; Williams, JK, 1997
)
1.27
"Tamoxifen is an antiestrogen widely used for the treatment of breast cancer. "( Neonatal treatment with tamoxifen causes immediate alterations of the sexually dimorphic nucleus of the preoptic area and medial preoptic area in male rats.
Roessler, ML; Vancutsem, PM, 1997
)
2.05
"Tamoxifen is a liver carcinogen in rats and has been shown to increase the risk of endometrial cancer in women. "( Identification of tamoxifen-DNA adducts formed by 4-hydroxytamoxifen quinone methide.
Beland, FA; Marques, MM, 1997
)
2.07
"Tamoxifen is an antiestrogen drug widely utilized for the adjuvant hormonal treatment of breast carcinoma. "( Study of the action of tamoxifen on the mammary gland epithelium of premenopausal patients by lysosome quantification.
de Lima, GR; Gebrim, LH; Simões, Mde D; Tanaka, CI,
)
1.88
"Tamoxifen is a non-steroidal estrogen antagonist used mainly in the adjuvant therapy of breast cancer. "( [Follow up examination of the endometrium during tamoxifen therapy].
Bacskó, G; Fülöp, B; Jakab, A; Juhász, B; Major, T, 1998
)
2
"Tamoxifen is an anti-oestrogenic drug which is widely used in the treatment of patients with breast cancer. "( Body composition measurements using DXA and other techniques in tamoxifen-treated patients.
al-Ghorabie, FH; Ali, PA; el-Sharkawi, AM; Evans, CJ; Hancock, DA,
)
1.81
"Tamoxifen is a non steroidal antiestrogen drug extensively used in the prevention and treatment of hormone-dependent breast cancer. "( Interaction of the anticancer drug tamoxifen with the human erythrocyte membrane and molecular models.
Aguilar, F; Hernández, P; Sotomayor, CP; Suwalsky, M; Villena, F,
)
1.85
"Tamoxifen is an effective inhibitor of HPCC growth in vitro and warrants further in vivo study."( Cell cycle regulation of human pancreatic cancer by tamoxifen.
Abbruzzese, JL; Chiao, PJ; Evans, DB; Grau, AM; Grimm, EA; Robinson, EK; Smid, CM, 1998
)
1.27
"Tamoxifen is a candidate chemopreventive agent in breast cancer, although the drug may be associated with the development of endometrial cancer. "( Prevention of breast cancer with tamoxifen: preliminary findings from the Italian randomised trial among hysterectomised women. Italian Tamoxifen Prevention Study.
Boyle, P; Costa, A; Maisonneuve, P; Maltoni, C; Robertson, C; Rotmensz, N; Sacchini, V; Veronesi, U, 1998
)
2.02
"Tamoxifen is a highly lipophilic drug that is widely used in breast malignancies and also as a prophylactic therapy in women at high risk for the development of this disease. "( In vitro percutaneous absorption enhancement of a lipophilic drug tamoxifen by terpenes.
Gao, S; Singh, J, 1998
)
1.98
"Tamoxifen (TAM) is a synthetic, nonsteroidal antiestrogenic agent that is widely prescribed in the treatment of estrogen-dependent neoplasias, including breast cancer. "( Tamoxifen inhibits induction of the mitochondrial permeability transition by Ca2+ and inorganic phosphate.
Custodio, JB; Moreno, AJ; Wallace, KB, 1998
)
3.19
"Tamoxifen is an antiestrogen drug commonly used to treat breast cancer and has been shown to cause prolongation of the electrocardiographic QT interval in humans. "( The antiestrogen tamoxifen blocks the delayed rectifier potassium current, IKr, in rabbit ventricular myocytes.
Ebert, SN; Katchman, A; Liu, XK; Woosley, RL, 1998
)
2.08
"Tamoxifen is a nonsteroidal triphenylethylene derivate with a predominant antiestrogen activity, used in the endocrine treatment of breast and endometrial cancer. "( Effects of tamoxifen on steroid hormone receptors and hormone concentration and the results of DNA analysis by flow cytometry in endometrial carcinoma.
Babić, D; Dotlić, S; Ilić-Forko, J; Jukić, S; Marusić, M; Nola, M; Petrovecki, M; Skrablin, S; Suchanek, E; Uzarević, B, 1999
)
2.14
"Tamoxifen is a liver carcinogen in rats and has been associated with an increased risk of endometrial cancer in women. "( Comparison of the DNA adducts formed by tamoxifen and 4-hydroxytamoxifen in vivo.
Beland, FA; Marques, MM; McDaniel, LP, 1999
)
2.01
"Tamoxifen is a non-steroidal anti-estrogen widely used in breast cancer treatment."( p53 expression in breast and endometrium during estrogen and tamoxifen treatment of surgically postmenopausal cynomolgus macaques.
Cline, JM; Isaksson, E; Skoog, L; Söderqvist, G; von Schoultz, B; von Schoultz, E; Wilking, N, 1999
)
1.27
"Tamoxifen is a nonsteroidal anti-oestrogen with gynaecological side-effects. "( Ovarian cysts in women receiving tamoxifen for breast cancer.
de Bruijn, HW; de Vries, EG; Hollema, H; Mourits, MJ; Sluiter, WJ; ten Hoor, KA; van der Zee, AG; Willemse, PH, 1999
)
2.03
"Tamoxifen is a nonsteroidal antiestrogen drug which has some estrogen agonist activity on the female genital tract. "( [Benign endometrial lesions induced by tamoxifen].
De Muylder, X, 1999
)
2.02
"Tamoxifen is an agent that can abrogate MDR and potentially enhance the effect of paclitaxel."( Paclitaxel and tamoxifen: An active regimen for patients with metastatic melanoma.
Berd, D; Mastrangelo, MJ; Nathan, FE; Sato, T, 2000
)
1.38
"Tamoxifen citrate is an orally administered, nonsteroidal antiestrogen agent that is widely used for the treatment of breast cancer and that has recently been found to prevent breast cancer in some high-risk populations. "( Tamoxifen-induced uterine abnormalities: the role of imaging.
Ascher, SM; Imaoka, I; Lage, JM, 2000
)
3.19
"Tamoxifen is an important drug for treating breast cancer. "( Tamoxifen for relapse of ovarian cancer.
Williams, CJ, 2000
)
3.19
"Tamoxifen is an oral anti-estrogen used in the treatment of breast cancer and recently approved to reduce the incidence of breast cancer in high risk women. "( Eye problems in breast cancer patients treated with tamoxifen.
Clark, LJ; Paganini-Hill, A, 2000
)
2
"Tamoxifen is an antiestrogenic drug which is used in the treatment of breast cancer and nonmalignant breast disorders. "( Identification of tamoxifen and metabolites in human male urine by GC/MS.
Aboul-Enein, HY; Efstatide, MD; Mihailescu, R, 2000
)
2.08
"Tamoxifen is a widely used selective oestrogen receptor modulator in women with breast cancer, which has been shown an agonistic profile in bone."( Skeletal effects of selective oestrogen receptor modulators (SERMs).
Díez, JL,
)
0.85
"Tamoxifen is a hepatic genotoxin in rats and mice but a hepatocarcinogen only in rats. "( Major inter-species differences in the rates of O-sulphonation and O-glucuronylation of alpha-hydroxytamoxifen in vitro: a metabolic disparity protecting human liver from the formation of tamoxifen-DNA adducts.
Boocock, DJ; Brown, K; Maggs, JL; Park, BK; White, IN, 2000
)
1.97
"Tamoxifen is a mixed antagonist, having both agonist and antagonist properties."( Nuclear receptor conformation, coregulators, and tamoxifen-resistant breast cancer.
Bain, DL; Graham, JD; Horwitz, KB; Jackson, TA; Richer, JK; Tung, L,
)
1.11
"Tamoxifen is an anti-estrogen used in the treatment of breast cancer and to reduce the incidence of breast cancer in high risk women. "( Preliminary assessment of cognitive function in breast cancer patients treated with tamoxifen.
Clark, LJ; Paganini-Hill, A, 2000
)
1.97
"Tamoxifen is a synthetic non-steroid anti-estrogen that has been used effectively for several years in the adjuvant treatment of breast cancer. "( [Tamoxifen and giant endometrial polyps].
Caragliano, L; Caschetto, S; Cassaro, N; Consalvo, P, 2000
)
2.66
"Tamoxifen is an important drug for treating breast cancer. "( Tamoxifen for relapse of ovarian cancer.
Williams, CJ, 2001
)
3.2
"Tamoxifen is a non-steroid estrogenic antagonist, used in post-surgical therapy of breast cancer. "( [Endometrial adenocarcinoma appearing during tamoxifen therapy. Report of a clinical case].
Corticelli, A; Fulcheri, E; Giannesi, A; Menada, MV; Nicoletti, L; Podesta, M; Rissone, R, 2000
)
2.01
"Tamoxifen is an example of a drug-induced increase of serum triglyceride levels."( Tamoxifen-induced hypertriglyceridemia in association with diabetes mellitus.
Elisaf, MS; Liberopoulos, EN; Milionis, HJ, 2001
)
2.47
"Tamoxifen (TAM) is a highly effective selective estrogen receptor (ER) modulator used extensively for the treatment and prevention of breast cancer. "( Tamoxifen-induced antitumorigenic/antiestrogenic action synergized by a selective aryl hydrocarbon receptor modulator.
Calvin, J; McDougal, A; Safe, S; Wormke, M, 2001
)
3.2
"Tamoxifen is an anti-oestrogenic drug widely used for adjuvant therapy of breast cancer. "( Understanding the genotoxicity of tamoxifen?
Phillips, DH, 2001
)
2.03
"Tamoxifen does not seem to be a useful adjunct in the treatment of symptomatic uterine leiomyomata and its use for this indication should be discouraged."( The role of tamoxifen in the treatment of symptomatic uterine leiomyomata -- a pilot study.
Debby, A; Ginath, S; Glezerman, M; Rotmensch, S; Sadan, O; Sofer, D; Zakut, H, 2001
)
1.41
"Tamoxifen is a valuable therapeutic agent with applications in the treatment and prevention of breast cancer. "( Control of the estrogen-like actions of the tamoxifen-estrogen receptor complex by the surface amino acid at position 351.
Bentrem, DJ; Jordan, VC; Levenson, AS; MacGregor Schafer, JI; Pease, KM,
)
1.84
"Tamoxifen is a nonsteroidal anti-estrogenic drug used for adjuvant treatment of breast cancer and recently as a chemopreventative agent for breast cancer and, on an investigational basis, for other cancers. "( Relationships between tamoxifen use, liver fat and body fat distribution in women with breast cancer.
Banerji, MA; Gordon, DH; Kral, JG; Nguyen, MC; Stewart, RB, 2001
)
2.07
"Tamoxifen (tmx) is a non-steroidal triphenylethylene derivative that is predominantly known as a competitive antagonist at the estrogen receptor and is used in the treatment of breast cancer. "( Inhibition of glial Na+ and K+ currents by tamoxifen.
Smitherman, KA; Sontheimer, H, 2001
)
2.02
"Tamoxifen is a selective oestrogen receptor modulator (SERM) with anti-oestrogenic properties in the breast and oestrogenic effects in tissues such as bone and the cardiovascular system. "( Tamoxifen, screening and new oestrogen receptor modulators.
Neven, P; Vergote, I, 2001
)
3.2
"Tamoxifen is an antiestrogen drug used to treat breast cancer. "( Biomonitoring of urinary tamoxifen and its metabolites from breast cancer patients using nonaqueous capillary electrophoresis with electrospray mass spectrometry.
Carter, SJ; Dovichi, NJ; Hanson, J; Li, XF; Mackey, JR; Modi, S, 2001
)
2.06
"Tamoxifen is a potent rat liver carcinogen, currently being used as a long-term chemopreventative for breast cancer in healthy women. "( 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
)
2.06
"Tamoxifen is an antiestrogen used in women who have estrogen receptor (ER)-alpha-positive breast cancer. "( A new antiestrogen, 2-(4-hydroxy-phenyl)-3-methyl-1-[4-(2-piperidin-1-yl-ethoxy)-benzyl]-1H-indol-5-ol hydrochloride (ERA-923), inhibits the growth of tamoxifen-sensitive and -resistant tumors and is devoid of uterotropic effects in mice and rats.
Annable, T; Collins, KI; Frost, P; Greenberger, LM; Komm, BS; Lyttle, CR; Miller, CP; Satyaswaroop, PG; Zhang, Y, 2001
)
1.95
"Tamoxifen is a mixed estrogen antagonist and agonist. "( Tamoxifen is an acute, estrogen-like, coronary vasodilator of porcine coronary arteries in vitro.
Chatterjee, K; Chou, TM; Hutchison, SJ; Sudhir, K, 2001
)
3.2
"Tamoxifen resistance is a serious clinical problem commonly encountered in the management of patients with breast cancer. "( Genetic events during the transformation of a tamoxifen-sensitive human breast cancer cell line into a drug-resistant clone.
Achuthan, R; Bell, SM; Horgan, K; Leek, JP; MacLennan, KA; Markham, AF; Roberts, P; Speirs, V, 2001
)
2.01
"Tamoxifen (TAM) is a first-line endocrine treatment for all stages of postmenopausal breast cancer. "( Molecular and pharmacokinetic evaluation of rat hepatic and gastrointestinal cytochrome p450 induction by tamoxifen.
Cotreau, MM; Greenblatt, DJ; Harmatz, JS; von Moltke, LL, 2001
)
1.97
"Tamoxifen is a selective estrogen receptor modulator (SERM) that produces antiestrogenic actions in the breast but estrogen-like actions in bone and lowers serum cholesterol."( Chemoprevention with antiestrogens: the beginning of the end for breast cancer. Daniel G. Miller Lecture.
Jordan, VC, 2001
)
1.03
"Tamoxifen is an effective treatment for breast cancer; however, as well as exerting antagonistic effects on the estrogen receptor (ER), tamoxifen acts as a partial agonists in estrogen-sensitive tissues, resulting in stimulation of the endometrium and tumor growth in some patients who become resistant to treatment.ICI 182, 780 (Faslodex), a steroidal estrogen antagonist, is the first in a new class of agent-an estrogen receptor downregulator. "( Faslodex (ICI 182, 780), a novel estrogen receptor downregulator--future possibilities in breast cancer.
Robertson, JF, 2001
)
1.75
"Tamoxifen is a candidate drug for prevention of breast cancer, although findings from trials have not been consistent. "( Tamoxifen for breast cancer among hysterectomised women.
Boyle, P; Maisonneuve, P; Rotmensz, N; Sacchini, V; Veronesi, U, 2002
)
3.2
"Tamoxifen is a widely utilized antiestrogen in the treatment and chemoprevention of breast cancer. "( Induction of cytochrome P450 3A4 in primary human hepatocytes and activation of the human pregnane X receptor by tamoxifen and 4-hydroxytamoxifen.
Buckley, AR; Buckley, DJ; Desai, PB; Goodwin, BJ; Moore, LB; Nallani, SC; Sane, RS, 2002
)
1.97
"Tamoxifen is an antiestrogenic drug that acts by binding to the estrogen receptor. "( [Toxic hepatitis associated with tamoxifen use. A case report and literature review].
Horga, JF; Lasso De La Vega, MC; Payá, A; Pérez-Mateo, M; Sola-Vera, J; Such, J; Zapater, P, 2002
)
2.04
"Tamoxifen is a major drug used for adjuvant chemotherapy of breast cancer; however, its use has been associated with a small but significant increase in risk of endometrial cancer. "( Bioactivation of tamoxifen by recombinant human cytochrome p450 enzymes.
De Wolf, CJ; Gillam, EM; Lancaster, RG; Notley, LM; Wunsch, RM, 2002
)
2.1
"Tamoxifen is a SERM that acts as an oestrogen antagonist in breast tissue and is currently being used for the treatment and prevention of breast cancer."( The search for the ideal SERM.
Anthony, M; Arun, B; Dunn, B, 2002
)
1.04
"Tamoxifen (TAM) is a well-tolerated compound in the treatment of breast cancer and is primarily considered to act by competition with estrogen receptors (ER). "( Effects of tamoxifen on human squamous cell carcinoma lines of the head and neck.
Balz, V; Bier, H; Bojar, H; Eckel, J; Friebe-Hoffmann, U; Hauser, U; Hoffmann, TK; van Lierop, A, 2002
)
2.15
"Tamoxifen is an antiestrogen used in the treatment of estrogen receptor-positive breast cancer in postmenopausal women. "( Genistein inhibits tamoxifen effects on cell proliferation and cell cycle arrest in T47D breast cancer cells.
Daley, BJ; Enderson, BL; Jones, JL; Karlstad, MD; Zhou, JR, 2002
)
2.09
"Tamoxifen is an estrogen receptor (ER)-antagonist that is widely used for the treatment of breast cancer, although it increases the risk of endometrial cancer. "( Estrogen receptor-mediated effects of tamoxifen on human endometrial cancer cells.
Ayabe, T; Eguchi, H; Hayashi, S; Mori, H; Omoto, Y; Sakamoto, T, 2002
)
2.03
"Tamoxifen is a synthetic nonsteroidal drug with antiestrogenic properties. "( Therapeutic use of tamoxifen in advanced breast cancer: correlation with biochemical parameters.
Beazley, RW; Hoth, D; Lippman, M; Macdonald, J; Morgan, LR; Posey, LE; Schein, PS; Woolley, PV, 1976
)
2.03
"Tamoxifen 1 is a triphenylethlene oestrogen antagonist which has partial oestrogen agonist activity in some species. "( Tamoxifen: a review of its pharmacological properties and therapeutic use in the treatment of breast cancer.
Avery, GS; Brogden, RN; Heel, RC; Speight, TM, 1978
)
3.14
"Tamoxifen is a specific estrogen antagonist used in the treatment of breast cancer. "( Ocular assessment of patients treated with tamoxifen.
Beck, M; Mills, PV,
)
1.84
"Tamoxifen is a useful agent for advanced breast cancer even in some patients with visceral disease."( Phase-II trial of tamoxifen in advanced breat cancer.
Green, L; Hoth, D; Macdonald, JS; Schein, PS; Smythe, T; Wiggans, RG; Woolley, PV, 1979
)
1.31
"Tamoxifen is a nonsteroidal antiestrogen employed frequently in the treatment of breast cancer. "( Tamoxifen and endometrial cancer.
Cohen, CJ; Deligdisch, L; Dottino, PR; Segna, RA, 1992
)
3.17
"Tamoxifen is a modifier of MDR, a role that warrants further clinical studies."( Intermittent high-dose tamoxifen as a potential modifier of multidrug resistance.
Cantwell, BM; Carmichael, J; Harris, AL; Lien, EA; Millward, MJ, 1992
)
1.32
"Tamoxifen citrate is an estrogen agonist/antagonist which protects the skeleton from osteopenia when ovarian hormones are depleted."( Tamoxifen in the rat prevents estrogen-deficiency bone loss elicited with the LHRH agonist buserelin.
Feng, W; Gold, E; Goulding, A, 1992
)
2.45
"Tamoxifen is a nonsteroidal antiestrogen that has found successful applications for each stage of breast cancer in the treatment of selected patients. "( The role of tamoxifen in the treatment and prevention of breast cancer.
Jordan, VC,
)
1.95
"Tamoxifen is a well-tolerated palliative and adjuvant treatment for human breast cancer and requires continuous, long-term administration for optimal therapeutic effectiveness. "( Tumor promotion as a target for estrogen/antiestrogen effects in rat hepatocarcinogenesis.
Dragan, YP; Pitot, HC; Xu, YD, 1991
)
1.72
"Tamoxifen is an important agent for the treatment of breast cancer. "( Endometrial carcinoma in tamoxifen-treated breast cancer patients.
Bardazzi, N; Citernesi, A; Curiel, P; Fontanarosa, M; Spinelli, G, 1991
)
2.03
"Tamoxifen is a nonsteroidal antiestrogen which has been reported by various investigators to have estrogen agonist and antagonist effects on rat bone. "( Dose-dependent effects of tamoxifen on long bones in growing rats: influence of ovarian status.
Moon, LY; Turner, RT; Wakley, GK, 1991
)
2.02
"Tamoxifen is a non-steroidal compound that has mixed agonist/antagonist actions in several biological models, but is commonly referred to as an 'antiestrogen'."( Effects of estrogen and tamoxifen on serum osteocalcin levels in ovariectomized rats.
Black, LJ; Paul, DC; Williams, DC, 1991
)
1.31
"Tamoxifen is a practical primary therapy of breast cancer in elderly and frail women obviating the need for surgery in a high proportion of cases."( A 10-year experience of tamoxifen as primary treatment of breast cancer in 100 elderly and frail patients.
Akhtar, SS; Allan, SG; Chetty, UD; Leonard, RC; Rodger, A; Smyth, JF, 1991
)
1.31
"Tamoxifen is a widely used drug in medical oncology, mainly for treatment of breast cancer, but also for second line treatment of endometrial cancer. "( Effects of tamoxifen on the female genital tract.
Fornander, T; Rutqvist, LE; Wilking, N, 1991
)
2.11
"Tamoxifen (ICI46,474) is a competitive inhibitor of estrogen action which has found ubiquitous application in the treatment of breast cancer. "( Long-term adjuvant tamoxifen therapy for breast cancer.
Jordan, VC, 1990
)
2.05
"Tamoxifen (TAM) is an antiestrogen that advances sexual puberty in cockerels, turkey toms, and Muscovy drakes. "( The effect of tamoxifen on semen fertilization capacity in White Leghorn male chicks.
Arnon, E; Robinzon, B; Rozenboim, I; Snapir, N, 1990
)
2.08
"Tamoxifen is a preferred agent for the treatment of breast cancer. "( Ocular toxicity of tamoxifen.
Gerner, EW, 1989
)
2.05
"Tamoxifen is a synthetic anti-oestrogen of low toxicity with proven anti-proliferative activity in endocrine sensitive breast cancer which makes it an attractive alternative for a trial of endocrine prevention."( Chemoprevention of breast cancer.
Ashley, SE; Cosgrove, D; Davey, JB; Dowsett, M; Hardy, JR; McKinna, A; Nash, AG; Powles, TJ; Rundle, SK; Sinnett, HD, 1989
)
1
"Tamoxifen is a well known and widely used drug."( The significance of estrogen receptors in tamoxifen and toremifene therapy.
Kangas, L; Valavaara, R, 1988
)
1.26
"Tamoxifen is an effective therapy for advanced breast cancer and is well tolerated. "( Anti-oestrogens in the treatment of breast and gynaecological cancers.
Furr, BJ, 1988
)
1.72
"Tamoxifen is a nonsteroidal antiestrogen whose mode of action is, as yet, unclear. "( Effect of tamoxifen on ultrastructure of endometrial carcinoma.
Amano, N; Kato, J; Ochiai, K; Terashima, Y; Tohtake, T, 1987
)
2.12
"Tamoxifen is an incomplete estrogen antagonist with partial estrogen agonist activity as well."( Response of advanced breast cancer to total endocrine ablation after exacerbation on tamoxifen: results in seven patients and possible mechanism of action.
Fletcher, WS; Hartley, JW; Wong, J, 1987
)
1.22
"Tamoxifen, which is a partial estrogen-agonist, did not alter tumor incidence, but it did reduce the total tumor burden under these same experimental conditions.(ABSTRACT TRUNCATED AT 250 WORDS)"( The interaction of dietary fat and antiestrogen treatment on DMBA-induced mammary tumors in the rat.
Brueggemann, G; King, MM; Magarian, RA; Pento, JT, 1985
)
0.99
"Tamoxifen is a potent anti-estrogen in the chicken oviduct [Sutherland, R., Mester, J., & Baulieu, E.E. "( Nuclear synthesis of egg white protein messenger ribonucleic acids in chick oviduct: effects of the anti-estrogen tamoxifen on estrogen-, progesterone-, and dexamethasone-induced synthesis.
Baulieu, EE; Cadepond-Vincent, F; Schweizer, G, 1985
)
1.92
"Tamoxifen is an estrogen agonist in mouse uterus, a partial estrogen agonist/antagonist in rat uterus, and a pure estrogen antagonist in chicken oviduct. "( Metabolism of tamoxifen and its uterotrophic activity.
Jordan, VC; Lyman, SD, 1985
)
2.07

Effects

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.

ExcerptReferenceRelevance
"Tamoxifen has a cytostatic effect on β-cells, independent of changes in glucose homeostasis, in mixed genetic background and also in C57Bl6 mice."( Tamoxifen suppresses pancreatic β-cell proliferation in mice.
Ahn, SH; Cox, AR; Granger, A; Kushner, JA; Lam, CJ; Rankin, MM, 2019
)
2.68
"Tamoxifen has a wide inter-variability. "( Genetic polymorphisms of 3'-untranslated region of SULT1A1 and their impact on tamoxifen metabolism and efficacy.
Dezentjé, VO; Gelderblom, H; Guchelaar, HJ; Moes, DJAR; Sanchez-Spitman, AB; Swen, JJ, 2018
)
2.15
"Tamoxifen (Tam) has a broad spectrum of anticancer activity, but is limited in clinical application. "( pH-responsive drug delivery of chitosan nanoparticles as Tamoxifen carriers for effective anti-tumor activity in breast cancer cells.
Kannan, S; Nipun Babu, V; Subramanian, KS; Thangam, R; Vivek, R, 2013
)
2.08
"Tamoxifen has a remarkable impact on the outcome of oestrogen receptor (ER)-positive breast cancer. "( Hormonal therapy for oestrogen receptor-negative breast cancer is associated with higher disease-specific mortality.
Bouchardy, C; Castiglione, M; Chappuis, PO; Fioretta, G; Merglen, A; Neyroud-Caspar, I; Rapiti, E; Verkooijen, HM; Vinh-Hung, V; Vlastos, G, 2009
)
1.8
"Tamoxifen has a key role in the management of women with hormone receptor (HR) positive breast cancer. "( Tamoxifen, cytochrome P450 genes and breast cancer clinical outcomes.
Francis, PA; Michael, M; Singh, MS, 2011
)
3.25
"Tamoxifen has a boneprotective effect when applied before exemestane treatment. "( Compliance, analgesic use and side-effect protection within a German cohort of the TEAM trial.
Becker, M; Bossart, M; Hadji, P; Hasenburg, A; Kieback, DG, 2012
)
1.82
"Tamoxifen has a good tolerability profile and moreover, unlike many other endocrine therapies, it is efficacious in both pre- and postmenopausal women."( Tamoxifen ("Nolvadex"): a review.
Clemons, M; Danson, S; Howell, A, 2002
)
2.48
"Tamoxifene has an atrophic effect but sometimes may induce an estrogenic stimulation of the endometrial mucosa through the alpha and beta estrogenic receptors."( [Effect of estrogens and antiestrogens on the endometrium].
Bergeron, C, 2002
)
1.04
"Tamoxifen has a valuable role as neo-adjuvant treatment in terms of breast conservation and survival."( Neo adjuvant Tamoxifen in post menopausal patients with operable breast cancer.
Asselain, B; Campana, F; Clough, KB; Languille, O; Magdalenat, H; Remvikos, Y; Salmon, RJ, 2003
)
1.41
"Tamoxifen has an antagonistic effect on the endometrium in premenopausal women and is associated with hot flushes and impaired sexual functioning."( [The effects of tamoxifen on the female genital tract].
de Vries, EG; Hollema, H; Mourits, MJ; van der Zee, AG; Willemse, PH, 2003
)
1.39
"Tamoxifen has a significant affect on hormone receptor expression and markers of apoptosis in endometrial polyps. "( Does tamoxifen therapy affect the hormone receptor expression and cell proliferation indices of endometrial polyps? An immunohistochemical comparison of endometrial polyps from postmenopausal women exposed and not exposed to tamoxifen.
Duffy, SR; McGurgan, P; O'Donovan, PJ; Taylor, LJ, 2006
)
2.29
"Tamoxifen has a lowering effect on serum lipids and is reported to decrease the risk of myocardial infarction but to increase the risk of thromboembolic events."( Cardiovascular health and aromatase inhibitors.
Abramson, BL; Pritchard, KI, 2006
)
1.06
"Tamoxifen treatment has a potential to stimulate the cell proliferation of endometrial glands and corpus luteum in tamoxifen-treated rats."( Immunohistochemical evaluation of cell proliferation and apoptosis markers in ovaries and uterus of tamoxifen-treated rats.
Akman, L; Cirpan, T; Kanit, L; Terek, MC; Ulukus, EC; Ulukus, M,
)
1.07
"Tamoxifen has a similar effect but to a much lesser extent than estradiol."( Anti-estrogens in fetal and newborn target tissues.
Gulino, A; Pasqualini, JR; Screpanti, I; Sumida, C, 1984
)
0.99
"Tamoxifen has a well established place in the adjuvant therapy of primary carcinoma of the breast. "( Hormonal manipulation and gynaecological cancer: the tamoxifen dilemma.
Ross, D; Whitehead, M, 1995
)
1.98
"Tamoxifen has an estrogen-like influence on the skeletal and cardiovascular systems, resulting in decreases in both postmenopausal bone loss and low density lipoprotein (LDL) levels."( A risk-benefit assessment of tamoxifen therapy.
Catherino, WH; Jordan, VC, 1993
)
1.3
"Tamoxifen has a wide range of systemic effects, possibly acting on every estrogen target tissue in the body."( Tamoxifen in postmenopausal women a safety perspective.
Kimmick, GG; Muss, HB; Robinson, E, 1996
)
2.46
"Tamoxifen has a particularly valuable role in developing countries in which the incidence of breast cancer is increasing as the average age of the population increases and in which control is substantially more difficult with mass mammography screening."( The control of breast cancer: the role of tamoxifen.
Forbes, JF, 1997
)
1.28
"Tamoxifen has a good tolerability profile and has demonstrated benefits for breast cancer patients in prolonging overall and disease-free survival and reducing the incidence of contralateral breast cancer."( Risks and benefits of tamoxifen therapy.
Assikis, VJ; Jordan, VC, 1997
)
1.33
"Tamoxifen has a beneficial effect on bone density presumably through its estrogen agonistic effects."( Tamoxifen effects on menopause--associated risk factors and symptoms.
Benshushan, A; Brzezinski, A, 1999
)
2.47
"Tamoxifen has a new role in chemoprevention in patients at high risk of breast cancer."( New drugs in breast cancer.
Iqbal, S; Miller, WR, 2001
)
1.03
"Tamoxifen has a complex effect on the female reproductive tract and several tamoxifen-associated changes have been described among tamoxifen users."( Tamoxifen and the female reproductive tract.
Eltabbakh, GH; Mount, SL, 2001
)
2.47
"Tamoxifen has an antiestrogenic action when opposed to 20 microgram of estradiol : this action is limited as soon as you give a dosis of 50 microgram on the uterus and it is nearly total with a dose of 1 mg ; we can notice it on the vaginal only from 200 microgram on."( [Action of an antiestrogen agent, tamoxifen on the uterus and vagina of the ovariectomized rat].
Marois, G; Marois, M, 1977
)
1.26
"(1) Tamoxifen has an E2 agonistic effect on histologically normal human endometrium. "( Tamoxifen increases plasma estrogen-binding equivalents and has an estradiol agonistic effect on histologically normal premenopausal and postmenopausal endometrium.
Beery, R; Geier, A; Gorodeski, GI; Lunenfeld, B, 1992
)
2.28
"Tamoxifen also has a potential role in other hormone-sensitive malignancies such as pancreatic carcinoma, and in treatment of benign breast disease."( Tamoxifen. A reappraisal of its pharmacodynamic and pharmacokinetic properties, and therapeutic use.
Buckley, MM; Goa, KL, 1989
)
2.44
"Tamoxifen has a 20-100-fold lower affinity than estradiol for the estrogen receptor."( Effects of tamoxifen and 4-hydroxytamoxifen on the pNR-1 and pNR-2 estrogen-regulated RNAs in human breast cancer cells.
May, FE; Westley, BR, 1987
)
1.38
"Tamoxifen (TAM) has a lower affinity to ER compared with one of its main metabolites, 4-OH-TAM."( Antiestrogen binding sites in human breast cancer biopsies. Measurement ligand-specificity and affinity, and correlation to estrogen and progesterone receptors.
Borg, A; Fernö, M,
)
0.85
"Tamoxifen has been shown to activate mitogen-activated protein kinase (MAPK) in an ERα-independent manner; therefore, we investigated its effects on the MAPK-mediated non-canonical activation of EphA2, a critical event regulating cell migration."( RSK-Mediated Non-canonical Activation of EphA2 by Tamoxifen.
Noguchi, M; Sakurai, H; Takahashi, JI; Tomihara, K; Yokoyama, S; Yonehara, K; Zhou, Y, 2022
)
1.7
"Tamoxifen has been associated with a plethora of ophthalmic adverse events, including macular holes, some of which are partial thickness subfoveal holes. "( Partial thickness subfoveal hole in a patient treated with tamoxifen: a case report and review of the literature.
Mantopoulos, D; Sanchez, G; Sohn, A, 2022
)
2.41
"Tamoxifen has been reported to cause pyometra in intact female dogs."( Stump pyometra in a spayed female dog secondary to tamoxifen.
Carvajal, J; Ehrhardt, C; Ham, K; Harris, AN; Odunayo, A; Pascutti, K, 2023
)
1.88
"Tamoxifen has been proven to be the first-line chemotherapy for several solid tumors in clinics, however, its therapeutic role in NAFLD has never been elucidated before."( Short-term tamoxifen administration improves hepatic steatosis and glucose intolerance through JNK/MAPK in mice.
Ding, J; Dou, K; Duan, J; Fang, Z; Li, Z; Liu, J; Ruan, B; Song, P; Wang, L; Xu, C; Xu, H, 2023
)
2.02
"Tamoxifen (TAM) has proven to be a therapeutic breakthrough to reduce mortality and recurrence in estrogen receptor-positive (ER+) breast cancer patients. "( ROS Generative Black Phosphorus-Tamoxifen Nanosheets for Targeted Endocrine-Sonodynamic Synergistic Breast Cancer Therapy.
Chen, W; Du, W; Hu, Y; Ilmer, M; Ma, X; Song, L; Wang, J; Zhang, H, 2023
)
2.64
"Tamoxifen (Tam) has been the first-line therapy for estrogen receptor-positive breast cancer since its FDA-approval in 1998. "( BRK confers tamoxifen-resistance in breast cancer via regulation of tyrosine phosphorylation of CDK1.
Baharani, A; Lukong, KE; Mandapati, A; Ning, Z, 2023
)
2.73
"Tamoxifen has not been assessed as a primary prevention agent in women with an inherited BRCA mutation."( Tamoxifen and the risk of breast cancer in women with a BRCA1 or BRCA2 mutation.
Aeilts, A; Bordeleau, L; Cullinane, CA; Eisen, A; Eng, C; Foulkes, WD; Fruscio, R; Gronwald, J; Huzarski, T; Karlan, B; Kotsopoulos, J; Lubinski, J; Metcalfe, K; Narod, SA; Neuhausen, SL; Olopade, O; Pal, T; Randall Armel, S; Singer, CF; Sun, P; Tung, N, 2023
)
3.07
"Tamoxifen has been tried successfully in adolescents with gynecomastia."( Gynecomastia.
Ayyavoo, A, 2023
)
1.63
"Tamoxifen (Tam) has long been a top treatment option for breast cancer patients, but the challenge of eliminating cancer recurrence remains. "( ELOVL2-AS1 suppresses tamoxifen resistance by sponging miR-1233-3p in breast cancer.
Baek, M; Jang, S; Jung, S; Kim, HW; Kim, SJ; Kwak, BS; Lee, H; Yang, SH, 2023
)
2.67
"Tamoxifen has been considered as the gold line therapy for estrogen receptor positive breast cancer."( Tamoxifen and Sulphoraphane for the breast cancer management: A synergistic nanomedicine approach.
Kohli, K; Mangla, B; Neupane, YR; Singh, A, 2019
)
2.68
"Tamoxifen has a cytostatic effect on β-cells, independent of changes in glucose homeostasis, in mixed genetic background and also in C57Bl6 mice."( Tamoxifen suppresses pancreatic β-cell proliferation in mice.
Ahn, SH; Cox, AR; Granger, A; Kushner, JA; Lam, CJ; Rankin, MM, 2019
)
2.68
"Tamoxifen has been clinically used in treating estrogen receptor (ER)-positive breast cancer for over 30 years. "( Elevated Hexokinase II Expression Confers Acquired Resistance to 4-Hydroxytamoxifen in Breast Cancer Cells.
Dai, X; Huang, M; Li, L; Liu, X; Miao, W; Wang, Y, 2019
)
2.19
"Tamoxifen has been the first-line adjuvant endocrine therapy in pre- and postmenopausal patients with ER + breast cancer for two decades."( Synergistic Cytotoxic and Apoptotic Effects of Local Probiotic Lactobacillus Brevis Isolated from Regional Dairy Products in Combination with Tamoxifen.
Akbari, N; Mirfazli, SS; Montazeri, H; Nasiri, Z; Tarighi, P, 2021
)
1.54
"Tamoxifen has been demonstrated to reduce breast cancer risk in high-risk, premenopausal women. "( Finding the five-year window: A qualitative study examining young women's decision-making and experience of using tamoxifen to reduce BRCA1/2 breast cancer risk.
Forbes Shepherd, R; Forrest, LE; James, PA; Keogh, LA; Young, MA, 2021
)
2.27
"Tamoxifen has been used for years for treating estrogen receptor-positive breast cancer; drug resistance, however, constitutes one of the main challenges for this therapy. "( ATF3 Modulates the Resistance of Breast Cancer Cells to Tamoxifen through an
Chen, Q; Dai, X; Li, L; Liu, X; Wang, Y; Yuan, J; Zhang, X, 2021
)
2.31
"Tamoxifen (TAM) therapy has been associated with fatty liver diseases. "( Luteolin mitigates tamoxifen-associated fatty liver and cognitive impairment in rats by modulating beta-catenin.
El-Asfar, RK; El-Demerdash, E; El-Derany, MO; El-Mesallamy, HO; Sallam, AM; Sayed, SA; Wahdan, SA, 2021
)
2.39
"Tamoxifen use has been associated with a variety of gynecologic problems."( Utilization of gynecologic services in women with breast cancer receiving hormonal therapy.
Accordino, M; Ananth, CV; Burke, WM; Chen, L; Desai, VB; Hershman, DL; Hou, JY; Neugut, AI; Tergas, AI; Wright, JD, 2017
)
1.18
"Tamoxifen has played a vital role in endocrine therapy for the treatment of estrogen receptor-positive breast cancer. "( The Effect of Tamoxifen on Thin Endometrium in Patients Undergoing Frozen-Thawed Embryo Transfer.
Chen, ZJ; Jiang, J; Ke, H; Qin, Y; Tang, R; Xia, M, 2018
)
2.28
"Tamoxifen (TAM) has been used in the treatment of breast cancers and is supplemented with erythropoietin (EPO) to alleviate the cancer-related anemia. "( Development of erythropoietin receptor-targeted drug delivery system against breast cancer using tamoxifen-loaded nanostructured lipid carriers.
Beh, CY; Foo, JB; Foong, JN; How, CW; Rasedee, A; Selvarajah, GT, 2017
)
2.12
"Tamoxifen has been reported to be associated with antagonism of estrogen-mediated cell growth signaling and activation of estrogen receptor-independent apoptosis events. "( Pyruvate kinase M2 interacts with mammalian sterile 20-like kinase 1 and inhibits tamoxifen-induced apoptosis in human breast cancer cells.
Chen, T; Guo, B; Huang, L; Huang, Y; Ji, F; Jiang, Y; Jin, Q; Liu, Y; Su, M; Wang, N; Wei, L; Yang, J; Zhang, Z; Zhong, C, 2017
)
2.12
"Tamoxifen has been used in women with hormone receptor-positive breast cancer and has been shown to successfully reduce both recurrence and mortality. "( Effects of tamoxifen on urinary incontinence: Case report and review of literature.
Altundag, K; Hasanov, E; Hasanov, M; Hasanov, R; Jonasch, E; Kuria, IM; Rzazade, R, 2017
)
2.29
"Tamoxifen has extraordinarily complex pharmacokinetics, with more than a dozen drug-metabolizing enzymes and transporters involved in its disposition."( The Underrated Risks of Tamoxifen Drug Interactions.
Hansten, PD, 2018
)
1.51
"Tamoxifen has been reported to ameliorate LPS-induced ALF via the induction of monocyte to macrophage differentiation-associated 2 (Mmd-2)."( Tamoxifen Prevents D-galactosamine/Lipopolysaccharide-Induced Murine Acute Hepatic Failure through Inhibition of Oxidative Stress and Mmd-2 Upregulation.
Cao, P; Gong, X; Lin, Y; Liu, L; Luo, M; Wu, T; Yang, Q; Zhou, L, 2018
)
2.64
"Tamoxifen (Tamo) has been clinically proven effective in a series of fibrotic diseases, such as PD-associated encapsulating peritoneal sclerosis (EPS), but the mechanisms underlying Tamoxifen's protective effects are yet to be defined."( Tamoxifen attenuates dialysate-induced peritoneal fibrosis by inhibiting GSK-3β/β-catenin axis activation.
Chen, X; Deng, H; Huang, H; Ji, S; Jin, W; Shen, J; Shen, Q; Tang, H; Yan, P; Zhang, J; Zhao, X, 2018
)
2.64
"Tamoxifen has a wide inter-variability. "( Genetic polymorphisms of 3'-untranslated region of SULT1A1 and their impact on tamoxifen metabolism and efficacy.
Dezentjé, VO; Gelderblom, H; Guchelaar, HJ; Moes, DJAR; Sanchez-Spitman, AB; Swen, JJ, 2018
)
2.15
"Tamoxifen has been used for many years to treat estrogen-positive breast cancer."( Tamoxifen mechanically reprograms the tumor microenvironment via HIF-1A and reduces cancer cell survival.
Cortes, E; Del Río Hernández, AE; Iwamoto, K; Lachowski, D; Lee, DA; Lieberthal, TJ; Okada-Hatakeyama, M; Robinson, B; Sarper, M; Teppo, JS; Thorpe, SD; Varjosalo, MT, 2019
)
2.68
"Tamoxifen has been used for many years to target estrogen receptor signalling in breast cancer cells. "( Tamoxifen mechanically deactivates hepatic stellate cells via the G protein-coupled estrogen receptor.
Cortes, E; Del Río Hernández, AE; Ghemtio, L; Lachowski, D; Lee, DA; Rice, A; Robinson, B; Rombouts, K; Thorpe, SD; Yeldag, G, 2019
)
3.4
"Tamoxifen has been used for over 40 years to treat estrogen receptor-positive breast cancers during both early stages of the disease and in the adjuvant setting."( Anticancer Drug Tamoxifen Affects Catecholamine Transmitter Release and Storage from Single Cells.
Ewing, AG; Larsson, A; Taleat, Z, 2019
)
1.58
"Tamoxifen has also shown a significant recurrence benefit and has become standard in the treatment of receptor-positive disease."( Ductal carcinoma in situ.
Bleicher, RJ, 2013
)
1.11
"Tamoxifen has been used in patients with estrogen-sensitive breast cancer, yet resistance to antiestrogens and recurrence will appear in some of the patients after its continued use."( 4-Hydroxytamoxifen-stimulated processing of cyclin E is mediated via G protein-coupled receptor 30 (GPR30) and accompanied by enhanced migration in MCF-7 breast cancer cells.
Chen, Y; Lei, TW; Li, Y; Liu, XH; Wan, L; Wang, XD; Yang, L; Zhu, ZX, 2013
)
1.53
"Tamoxifen (Tam) has a broad spectrum of anticancer activity, but is limited in clinical application. "( pH-responsive drug delivery of chitosan nanoparticles as Tamoxifen carriers for effective anti-tumor activity in breast cancer cells.
Kannan, S; Nipun Babu, V; Subramanian, KS; Thangam, R; Vivek, R, 2013
)
2.08
"Tamoxifen use has been associated with the development of vaginal myofibroblastoma."( Vaginal myofibroblastoma with prostatic glands: is there an association with tamoxifen use? A case report.
Cao, QJ; Harmanli, O; Jones, KA; Lorange, E,
)
1.08
"Tamoxifen (TAM) has both cytostatic and cytotoxic properties for breast cancer."( Vitamin C suppresses cell death in MCF-7 human breast cancer cells induced by tamoxifen.
Alitheen, NB; Aziz, SA; Ho, CL; Ho, WY; Omar, AR; Rahman, NM; Subramani, T; Yeap, SK, 2014
)
1.35
"Tamoxifen has been shown to significantly reduce the risk of tumour recurrence in women with receptor positive breast cancer and has been used for chemoprevention in women with both non-invasive cancer and those with a high risk of developing breast cancer. "( Uterine sarcoma after tamoxifen therapy for breast cancer.
O'Sullivan, R; Samuji, M; Shireen, R, 2013
)
2.15
"Tamoxifen has dramatically reduced the recurrence and mortality rate of estrogen receptor positive breast cancer. "( Hot flashes are not predictive for serum concentrations of tamoxifen and its metabolites.
Beijnen, JH; Huitema, AD; Jager, NG; Koornstra, RH; Korse, TM; Linn, SC; Schellens, JH; van Schaik, RH; Vincent, AD, 2013
)
2.08
"Tamoxifen has biologically active metabolites: 4-hydroxytamoxifen (4OHT) and endoxifen. "( Influence of the length and positioning of the antiestrogenic side chain of endoxifen and 4-hydroxytamoxifen on gene activation and growth of estrogen receptor positive cancer cells.
Curpan, RF; Fernandes, DJ; Jordan, VC; Maximov, PY; McDaniel, RE; Myers, CB, 2014
)
2.06
"Tamoxifen has anti-oestrogenic and anti-tumour activity in the breast, but is oestrogenic and carcinogenic in the endometrium. "( MGMT promoter hypermethylation and K-RAS, PTEN and TP53 mutations in tamoxifen-exposed and non-exposed endometrial cancer cases.
Gajjar, KB; Martin, FL; Martin-Hirsch, PL; Nagy, E; Patel, II; Phillips, DH; Stringfellow, HF; Taylor, S, 2014
)
2.08
"Tamoxifen has been a frontline treatment for estrogen receptor alpha (ERα)-positive breast tumors in premenopausal women. "( An epigenomic approach to therapy for tamoxifen-resistant breast cancer.
Bradner, J; Coarfa, C; Creighton, CJ; Feng, Q; Fu, X; He, B; Hilsenbeck, SG; Lanz, R; Mitsiades, CS; Mitsiades, N; Nardone, A; O'Malley, BW; Osborne, CK; Schiff, R; Shea, MJ; Song, Y; Wang, L; Zhang, Z, 2014
)
2.12
"Tamoxifen has long been used and still is the most commonly used endocrine therapy for treatment of both early and advanced estrogen receptor-positive breast cancer in pre- and post-menopause women. "( Combination treatment of tamoxifen with risperidone in breast cancer.
Chen, DR; Lin, HY; Wu, HM; Yeh, WL, 2014
)
2.15
"Tamoxifen has been used as an anti-estrogen for the prevention and treatment of breast cancer."( Tamoxifen ameliorates renal tubulointerstitial fibrosis by modulation of estrogen receptor α-mediated transforming growth factor-β1/Smad signaling pathway.
Jung, YJ; Kang, KP; Kim, D; Kim, W; Lee, AS; Lee, S; Park, SK; Yang, KH, 2014
)
2.57
"Tamoxifen has been used either alone or in- combination with other chemotherapeutic agents to treat melanoma."( Cholesterol depletion by methyl-β-cyclodextrin augments tamoxifen induced cell death by enhancing its uptake in melanoma.
Bhat, MK; Chaube, B; Kulkarni, MJ; Malvi, P; Meena, AS; Mohammad, N; Singh, SV; Vannuruswamy, G, 2014
)
1.37
"Tamoxifen has been US Food and Drug Administration-approved for primary prevention of breast cancer since 1998 but has not been widely adopted, in part because of increased risk of serious side effects. "( Risk-benefit profiles of women using tamoxifen for chemoprevention.
DeRoo, LA; Nichols, HB; Sandler, DP; Scharf, DR, 2015
)
2.13
"Tamoxifen also has pleiotropic and side effects."( Tamoxifen induces the development of hernia in mice by activating MMP-2 and MMP-13 expression.
Chen, Y; Duan, Y; Han, J; Li, X; Liu, M; Liu, Y; Ma, X; Wang, Q; Wei, Y; Xiang, R, 2015
)
2.58
"Tamoxifen has been used not only for the treatment or prevention of recurrence in patients with estrogen receptor positive breast cancers but also for recurrent breast cancer. "( Pharmacogenomics toward personalized tamoxifen therapy for breast cancer.
Zembutsu, H, 2015
)
2.13
"Tamoxifen may have been previously overestimated as a microvascular thrombotic risk factor. "( Tamoxifen (selective estrogen-receptor modulators) and aromatase inhibitors as potential perioperative thrombotic risk factors in free flap breast reconstruction.
Fischer, JP; Kanchwala, S; Kovach, SJ; Mirzabeigi, MN; Nelson, JA; Serletti, JM; Wu, LC, 2015
)
3.3
"Tamoxifen has been the basis of endocrine therapy for patients with ER(+) breast cancer for more than three decades."( Factors Promoting Tamoxifen Resistance in Breast Cancer via Stimulating Breast Cancer Stem Cell Expansion.
Bane, A; Lin, X; Liu, Y; Ojo, D; Tang, D; Wang, E; Wei, F; Wong, N; Zhang, H, 2015
)
1.47
"Tamoxifen has been used for the treatment of estrogen receptor (ER)-positive breast cancers and in women who are at an increased risk of breast cancer. "( Sensitization of estrogen receptor-positive breast cancer cell lines to 4-hydroxytamoxifen by isothiocyanates present in cruciferous plants.
Herman-Antosiewicz, A; Pawlik, A; Słomińska-Wojewódzka, M, 2016
)
2.1
"Tamoxifen has been reported to inhibit growth and induce cell death of glioma cells in vitro, in an estrogen-receptor-independent manner."( Tamoxifen-Induced Cell Death of Malignant Glioma Cells Is Brought About by Oxidative-Stress-Mediated Alterations in the Expression of BCL2 Family Members and Is Enhanced on miR-21 Inhibition.
Harmalkar, M; Kazi, S; Shirsat, NV; Upraity, S, 2015
)
2.58
"Tamoxifen has been shown to be particularly effective in preventing subsequent breast cancer in women with AH, with a more than 70% reduction in the P1 trial and a 60% reduction in IBIS-I."( Impact of preventive therapy on the risk of breast cancer among women with benign breast disease.
Cuzick, J; Sestak, I; Thorat, MA, 2015
)
1.14
"Tamoxifen (TX) has been extensively used as a selective oestrogen receptor modulator, although its neuroendocrine effects remain poorly understood."( Hypothalamic Effects of Tamoxifen on Oestrogen Regulation of Luteinising Hormone and Prolactin Secretion in Female Rats.
Aquino, NS; Araujo-Lopes, R; Batista, IA; Franci, CR; Henriques, PC; Poletini, MO; Reis, AM; Szawka, RE, 2016
)
1.46
"Tamoxifen for 5 years has been traditionally considered the standard endocrine therapy for premenopausal patients and this is still valid for many patients."( New insights on the role of luteinizing hormone releasing hormone agonists in premenopausal early breast cancer patients.
Del Mastro, L; Lambertini, M; Poggio, F; Pronzato, P; Rossi, G, 2016
)
1.16
"Tamoxifen has shown great success in the treatment of breast cancer; however, long-term treatment can lead to acquired tamoxifen (TOT) resistance and relapse. "( OCT-4: a novel estrogen receptor-α collaborator that promotes tamoxifen resistance in breast cancer cells.
Bhatt, S; Joshi, S; Katzenellenbogen, BS; Stender, JD; Wu, G, 2016
)
2.12
"Tamoxifen has been widely used to treat breast cancer as an endocrine therapy. "( Tamoxifen has a proliferative effect in endometrial carcinoma mediated via the GPER/EGFR/ERK/cyclin D1 pathway: A retrospective study and an in vitro study.
Lan, L; Li, Y; Liu, R; Qu, Q; Wen, K; Wu, Y; Zhang, L, 2016
)
3.32
"Tamoxifen has demonstrated some efficacy has a therapeutic for bipolar mania and is believed to exert these effects through inhibition of protein kinase C (PKC)."( Tamoxifen and amphetamine abuse: Are there therapeutic possibilities?
Gnegy, ME; Mardirossian, N; Mikelman, S, 2017
)
2.62
"Tamoxifen has been successfully used for treating breast cancer and preventing cancer recurrence. "( National Prociency Testing Result of CYP2D6*10 Genotyping for Adjuvant Tamoxifen Therapy in China.
Han, Y; Li, J; Lin, G; Xie, J; Yi, L; Zhang, K, 2016
)
2.11
"Tamoxifen has been used to prevent the recurrence of breast cancer. "( Feature of amenorrhea in postoperative tamoxifen users with breast cancer.
Choi, YM; Han, W; Kim, H; Kim, SH; Ku, SY; Suh, CS, 2017
)
2.17
"Tamoxifen (TAM) has been widely used for the treatment of estrogen receptor (ER)-positive breast cancer and its combination with other therapies is being actively investigated as a way to increase efficacy and decrease side effects. "( BreastDefend enhances effect of tamoxifen in estrogen receptor-positive human breast cancer in vitro and in vivo.
Alvarado, M; Castillo, V; Cheng, S; Eliaz, I; Sandusky, GE; Sliva, D; Temm, CJ; Welty, M, 2017
)
2.18
"Tamoxifen has been used as an antiestrogen in the treatment and prevention of breast cancer for many years."( Tamoxifen is effective in the treatment of Leishmania amazonensis infections in mice.
Miguel, DC; Uliana, SR; Yokoyama-Yasunaka, JK, 2008
)
2.51
"Tamoxifen has been reported to be oestrogenic on the lower genital tract. "( Ovulation induction with tamoxifen and alternate-day gonadotrophin in patients with thin endometrium.
Chen, CK; Horng, SG; Huang, HY; Lee, CL; Soong, YK; Wang, CW; Wang, HS, 2008
)
2.09
"Tamoxifen has efficacy as a breast cancer therapy and chemoprevention agent. "( Methylseleninic acid synergizes with tamoxifen to induce caspase-mediated apoptosis in breast cancer cells.
Carrier, L; Li, Z; Rowan, BG, 2008
)
2.06
"Tamoxifen has been the mainstay adjuvant hormonal treatment for breast cancer for many years. "( Impaired tamoxifen metabolism reduces survival in familial breast cancer patients.
Evans, DG; Hadfield, KD; Howell, S; Lalloo, F; Latif, A; McHague, C; Newman, WG; Roberts, SA; Shenton, A, 2008
)
2.21
"Tamoxifen has been the mainstay of endocrine therapy for estrogen receptor-positive breast cancer. "( Survivin plays as a resistant factor against tamoxifen-induced apoptosis in human breast cancer cells.
Kobayashi, D; Moriai, M; Moriai, R; Tsuji, N; Watanabe, N, 2009
)
2.06
"Tamoxifen has been used in patients with hepatocellular carcinoma (HCC). "( Tamoxifen inhibits proliferation and induces apoptosis in human hepatocellular carcinoma cell line HepG2 via down-regulation of survivin expression.
Ge, H; Guo, R; Huang, Z; Jin, S; Shu, Y, 2009
)
3.24
"Tamoxifen has a remarkable impact on the outcome of oestrogen receptor (ER)-positive breast cancer. "( Hormonal therapy for oestrogen receptor-negative breast cancer is associated with higher disease-specific mortality.
Bouchardy, C; Castiglione, M; Chappuis, PO; Fioretta, G; Merglen, A; Neyroud-Caspar, I; Rapiti, E; Verkooijen, HM; Vinh-Hung, V; Vlastos, G, 2009
)
1.8
"Tamoxifen has been used as adjuvant hormonal therapy for estrogen receptor positive breast cancer for over 30 years and is also widely used for the treatment of metastatic breast cancer. "( Clinical significance of CYP2D6 polymorphisms and tamoxifen in women with breast cancer.
Gaston, C; Kolesar, J, 2008
)
2.04
"Tamoxifen has been the most important therapeutic agent for the treatment of estrogen receptor (ER)-positive breast cancer for the past three decades. "( The tamoxifen metabolite, endoxifen, is a potent antiestrogen that targets estrogen receptor alpha for degradation in breast cancer cells.
Goetz, MP; Hawse, JR; Ingle, JN; Spelsberg, TC; Subramaniam, M; Wu, X, 2009
)
2.35
"Tamoxifen has been suggested to produce beneficial cardiovascular effects, although the mechanisms for these effects are not fully known. "( Assessment of vascular effects of tamoxifen and its metabolites on the rat perfused hindquarter vascular bed.
Desta, Z; Flockhart, DA; Gomes, VA; Montenegro, MF; Pessa, LR; Tanus-Santos, JE, 2009
)
2.07
"Tamoxifen has been found to be neuroprotective in both transient and permanent experimental ischemic stroke. "( Tamoxifen attenuates inflammatory-mediated damage and improves functional outcome after spinal cord injury in rats.
Liu, JL; Pan, DJ; Qu, WS; Tang, ZP; Tian, DS; Wang, W; Xie, MJ; Yu, ZY; Zhan, Y, 2009
)
3.24
"Tamoxifen has been the standard of adjuvant endocrine therapy in breast cancer for years, however only about half of relapses are prevented and there is an early occurrence of serious adverse events due to agonistic estrogenic activity of tamoxifen, such as an increase in the risk of endometrial hyperplasia and venous thromboembolism."( [Adjuvant endocrine therapy in breast cancer. Management of early-risk relapse].
Atallah, D; Chahine, G; Howayek, M,
)
0.85
"Tamoxifen has also shown significant potential in treating various dermatological disorders including psoriasis, characterized by hyperproliferation of epidermal keratinocytes."( Tamoxifen-encapsulated vesicular systems: cytotoxicity evaluation in human epidermal keratinocyte cell line.
Bhatia, A; Bhushan, S; Katare, OP; Singh, B, 2010
)
2.52
"Tamoxifen has been the standard adjuvant endocrine therapy for both pre- and post-menopausal women with hormone receptor-positive early breast cancer and remains the standard of care for premenopausal women."( Optimal adjuvant endocrine therapy for early breast cancer.
Davis, A; Stuart-Harris, R, 2010
)
1.08
"Tamoxifen has been a very effective treatment for breast cancer for several decades, however, at the same time increases the risk of endometrial cancer, especially after prolonged exposure. "( Genomic profile of endometrial tumors depends on morphological subtype, not on tamoxifen exposure.
de Leeuw-Mantel, G; Fles, R; Hollema, H; Hoogendoorn, WE; Mourits, MJ; Nederlof, PM; Platteel, I; Scheerman, CE; van Boven, HH; van Leeuwen, FE, 2010
)
2.03
"Tamoxifen use has been associated with increased risk of thromboembolic events (TEs) in women with breast cancer and women at high risk for the disease. "( Factor V Leiden mutation and thromboembolism risk in women receiving adjuvant tamoxifen for breast cancer.
Archer, L; Atkins, JN; Berliner, N; Dressler, L; Edge, S; Garber, JE; Halabi, S; Kaplan, E; Kimmick, G; Levine, E; Orcutt, J; Paskett, ED; Paskett, EM; Scalzo, A; Shahab, N; Shapiro, CL; Tolaney, SM; Winer, E, 2010
)
2.03
"Tamoxifen has been the standard adjuvant endocrine therapy for pre- and postmenopausal women with hormone receptor-positive breast cancer."( Clinical practice decisions in endocrine therapy.
Thomssen, C; Untch, M, 2010
)
1.08
"Tamoxifen has been shown to be a potent neuroprotectant against stroke in rodents. "( Tamoxifen as an effective neuroprotectant in an endovascular canine model of stroke.
Boulos, AS; Dalfino, JC; Deshaies, EM; Drazin, D; Feustel, PJ; Popp, AJ, 2011
)
3.25
"Tamoxifen has no negative effects on lipid peroxidation in an animal model."( Effects of tamoxifen on tissue nitrite/nitrate levels and plasma lipid peroxidation in female rats.
Akercan, F; Gharehbagni, M; Karadadas, N; Sendag, F; Sezer, E; Terek, MC; Zeybek, B, 2010
)
2.19
"Tamoxifen has been the most widely used hormonal therapy for more than two decades."( Tamoxifen for breast cancer.
Acharya, B; Bhandari, RB; Jha, AK; Karn, A; Poudel, S; Shrestha, S,
)
2.3
"Tamoxifen has a key role in the management of women with hormone receptor (HR) positive breast cancer. "( Tamoxifen, cytochrome P450 genes and breast cancer clinical outcomes.
Francis, PA; Michael, M; Singh, MS, 2011
)
3.25
"Tamoxifen has successfully been used in treating EPS; however, the mechanism of tamoxifen in treating EPS fibrosis disorders remains unclear."( Tamoxifen downregulates connective tissue growth factor to ameliorate peritoneal fibrosis.
Cheng, HT; Chiang, CK; Huang, JW; Hung, KY; Lien, YC; Tsai, TJ; Wu, HY; Yen, CJ, 2011
)
2.53
"Tamoxifen has been widely used for more than 30 years in breast cancer treatment and prevention."( Tamoxifen and its new derivatives in cancer research.
Camacho, J; Rivera-Guevara, C, 2011
)
2.53
"Tamoxifen has been used for the treatment or prevention of recurrence in patients with estrogen receptor-positive breast cancers. "( Should CYP2D6 inhibitors be administered in conjunction with tamoxifen?
Kiyotani, K; Mushiroda, T; Nakamura, Y; Sasa, M; Zembutsu, H, 2011
)
2.05
"Tamoxifen has been associated with an increased risk of stroke. "( Time dependent effects of adjuvant tamoxifen therapy on cerebrovascular disease: results from a randomised trial.
Bengtsson, NO; Carstensen, J; Fornander, T; Hatschek, T; Lindman, H; Malmström, PO; Nordenskjöld, B; Rosell, J; Stål, O; Wallgren, A, 2011
)
2.09
"Tamoxifen has been shown in vitro to inhibit protein kinase C through estrogen receptor-independent antineoplastic effects."( Phase I clinical trial assessing temozolomide and tamoxifen with concomitant radiotherapy for treatment of high-grade glioma.
Amin, P; Cheston, S; Dhople, A; DiBiase, S; Flannery, T; Meisenberg, B; Patel, A; Patel, S, 2012
)
1.35
"Tamoxifen has been shown to be atheroprotective."( Induction of macrophage scavenger receptor type BI expression by tamoxifen and 4-hydroxytamoxifen.
Chen, Y; Dong, P; Duan, Y; Han, J; Hu, W; Li, X; Xie, T; Zhou, X, 2011
)
1.33
"Tamoxifen has been associated with a reduction in the incidence of myocardial infarction. "( Effect of tamoxifen on the coronary vascular reactivity of spontaneously hypertensive female rats.
Abreu, GR; Bissoli, NS; Borgo, MV; Gouvêa, SA; Lopes, AB; Moyses, MR; Romero, WG, 2011
)
2.21
"Tamoxifen has been used extensively in the treatment of breast cancer and other neoplasms. "( Interaction of tamoxifen and noise-induced damage to the cochlea.
Pillai, JA; Siegel, JH, 2011
)
2.16
"Tamoxifen resistance has been largely attributed to genetic alterations in the epithelial tumor cells themselves, such as overexpression of HER-2/Neu. "( The tumor microenvironment modulates tamoxifen resistance in breast cancer: a role for soluble stromal factors and fibronectin through β1 integrin.
Bissell, MJ; Joffé, EB; Motter, A; Pontiggia, O; Raffo, D; Sampayo, R; Simian, M; Xu, R, 2012
)
2.09
"Tamoxifen has been widely used for the prevention of recurrence in patients with hormone receptor-positive breast cancer. "( Pharmacogenomics of tamoxifen: roles of drug metabolizing enzymes and transporters.
Kiyotani, K; Mushiroda, T; Nakamura, Y; Zembutsu, H, 2012
)
2.15
"Tamoxifen (TAM) has been shown to be active against the bicalutamide-induced breast events (BEs) gynecomastia, and breast pain in patients with prostate cancer (PC). "( A randomized trial comparing tamoxifen therapy vs. tamoxifen prophylaxis in bicalutamide-induced gynecomastia.
Allegro, R; Altieri, V; De Grande, G; Ferraù, F; Gebbia, V; Mazza, R; Melloni, D; Morgia, G; Nicolosi, F; Serretta, V, 2012
)
2.11
"Tamoxifen (TAM) has invariably demonstrated induction of pro-survival autophagy in numerous cancers."( Enhancement of apoptotic and autophagic induction by a novel synthetic C-1 analogue of 7-deoxypancratistatin in human breast adenocarcinoma and neuroblastoma cells with tamoxifen.
Collins, J; Hudlicky, T; Ma, D; Pandey, S, 2012
)
1.29
"Tamoxifen (TAM) has both cytostatic and cytotoxic properties for breast cancer. "( Tamoxifen regulates cell fate through mitochondrial estrogen receptor beta in breast cancer.
Fuqua, S; Jordan, VC; Levin, ER; Pedram, A; Razandi, M, 2013
)
3.28
"Tamoxifen has emerged as a potential management option for gynecomastia and breast pain due to non-steroidal antiandrogens, and it is considered an alternative to surgery or radiotherapy. "( Tamoxifen for the management of breast events induced by non-steroidal antiandrogens in patients with prostate cancer: a systematic review.
Antes, G; Keck, B; Kunath, F; Meerpohl, JJ; Wullich, B, 2012
)
3.26
"Tamoxifen has a boneprotective effect when applied before exemestane treatment. "( Compliance, analgesic use and side-effect protection within a German cohort of the TEAM trial.
Becker, M; Bossart, M; Hadji, P; Hasenburg, A; Kieback, DG, 2012
)
1.82
"Tamoxifen has been given for 8 months and the size of remnant thyroid decreased to 8 mm."( A misdiagnosed Riedel's thyroiditis successfully treated by thyroidectomy and tamoxifen.
Huang, SM; Lee, CT; Wang, CJ; Wu, TJ, 2012
)
1.33
"Tamoxifen (TAM) has been prescribed for decades and aromatase inhibitors (AIs) have been used since the early 2000s in preventing subsequent breast cancer. "( Effectiveness of aromatase inhibitors and tamoxifen in reducing subsequent breast cancer.
Ahmed, SA; Avila, CC; Craig Cheetham, T; Fisher, A; Guo, A; Haque, R; Schottinger, JE; Shi, J, 2012
)
2.09
"Both tamoxifen and the AIs have been shown to be active in the neoadjuvant treatment of breast cancer."( Evolving uses of hormonal agents for breast cancer therapy.
Cummings, FJ, 2002
)
0.77
"Tamoxifen has been used in the management of breast cancer for over 30 years. "( Tamoxifen ("Nolvadex"): a review.
Clemons, M; Danson, S; Howell, A, 2002
)
3.2
"Tamoxifen has also been shown to be a potent hepatocarcinogen in rats."( 4-Hydroxytamoxifen sulfation metabolism.
Chen, G; Maiti, S; Shao, X; Yin, S, 2002
)
1.45
"Tamoxifen has been the endocrine treatment of choice for patients with breast cancer. "( Aromatase inhibitors in breast cancer: an update.
Hudis, C; Lake, DE,
)
1.57
"Tamoxifen has served as a prototype for the development of selective estrogen receptor modulators at the laboratory-clinical interface. "( Update on clinical role of tamoxifen.
Benson, JR; Pitsinis, V, 2003
)
2.06
"Tamoxifen has adverse effects such as hot flashes, increased risk of uterine cancer in postmenopausal women, and rare occurrence of thromboembolic disease."( The role of aromatase inhibitors in early breast cancer.
Carlson, RW; Chung, CT, 2003
)
1.04
"Tamoxifen has been widely used for treatment, and more recently, for the prevention of breast cancer. "( Cell proliferation, apoptosis, and expression of cyclin D1 and cyclin E as potential biomarkers in tamoxifen-treated mammary tumors.
Christov, K; Green, A; Grubbs, C; Ikui, A; Lubet, R; Shilkaitis, A; Steele, V; Weinstein, IB; Yao, R; You, M, 2003
)
1.98
"Tamoxifen has been reported to enhance the antitumor activity of cisplatin in preclinical models by modulation of protein kinase C signal transduction and apoptosis-related pathways."( Phase I trial of high-dose tamoxifen in combination with cisplatin in patients with lung cancer and other advanced malignancies.
DeGregorio, M; Edelman, MJ; Gandara, DR; Lauder, IJ; O'Donnell, R; Perez, EA, 2003
)
2.06
"Tamoxifen has been tried in patients with hepatocellular carcinoma (HCC), however, its inhibitory mechanism remains unknown. "( [The effects of tamoxifen on human hepatocellular carcinoma cell proliferation and transforming growth factor-beta1 expression].
Choi, MH; Chung, YH; Kim, JA; Lee, HC; Lee, YJ; Lee, YS; Park, MI; Park, NH; Ryu, SH; Shin, JW; Suh, DJ; Yu, ES, 2003
)
2.11
"Tamoxifene has an atrophic effect but sometimes may induce an estrogenic stimulation of the endometrial mucosa through the alpha and beta estrogenic receptors."( [Effect of estrogens and antiestrogens on the endometrium].
Bergeron, C, 2002
)
1.04
"Tamoxifen treatment has also been associated with improvement of retroperitoneal fibrosis and desmoid tumors, conditions also associated with abnormal fibroblast proliferation."( Open label trial of tamoxifen in scleroderma.
Fessler, BJ; Hoffman, GS; Thomas-Golbanov, CK; Wilke, WS,
)
1.18
"Tamoxifen has been registered for breast cancer prevention for high risk individuals in the United States."( [Breakthrough in breast cancer chemoprevention].
Kahán, Z; Thurzó, L, 2003
)
1.04
"Tamoxifen has been the gold standard adjuvant therapeutic agent for postmenopausal women with hormone-sensitive breast cancer for > 25 years. "( Anastrozole as adjuvant therapy for early-stage breast cancer: implications of the ATAC trial.
Buzdar, A, 2003
)
1.76
"Tamoxifen has been successfully used worldwide as adjuvant therapy in the treatment of women with breast cancer."( Tamoxifen: is it safe? Comparison of activation and detoxication mechanisms in rodents and in humans.
White, IN, 2003
)
2.48
"Tamoxifen, which has been related to increased incidence of endometrial carcinoma in women, dramatically increased IGF-I mRNA levels in rat uterus."( Effects of SERM (selective estrogen receptor modulator) treatment on growth and proliferation in the rat uterus.
Eriksson, B; Eriksson, H; Muravitskaya, N; Sahlin, L; Stygar, D, 2003
)
1.04
"Tamoxifen has been reported to show an efficacy in the treatment of breast cancer. "( Biochemical studies of apoptosis induced by tamoxifen in estrogen receptor positive and negative breast cancer cell lines.
Karami-Tehrani, F; Salami, S, 2003
)
2.02
"Tamoxifen has long been an established adjuvant treatment in the management of advanced breast cancer. "( Tamoxifen's impact as a preventive agent in clinical practice and an update on the STAR trial.
Wickerham, DL, 2003
)
3.2
"Tamoxifen has been used in the treatment of patients with metastatic malignant melanoma either as a single agent or, more commonly, in combination with other chemotherapeutic agents. "( Use of tamoxifen in the treatment of malignant melanoma.
Husain, AF; Lens, MB; Reiman, T, 2003
)
2.22
"Tamoxifene has also been approved for use in reducing the incidence of breast cancer amongst high risk women."( Ocular side-effects in breast cancer patients treated with tamoxifen and toremifene: a randomized follow-up study.
Holli, K; Paakkala, AM; Parkkari, M; Salminen, L, 2003
)
1.28
"Tamoxifen has been the principal adjuvant hormonal therapy in pre- and postmenopausal women with hormone receptor-positive breast cancer for nearly 20 years."( Sequential hormonal therapy for metastatic breast cancer after adjuvant tamoxifen or anastrozole.
Carlson, RW; Henderson, IC, 2003
)
1.27
"Tamoxifen has also been evaluated as a risk-reducing agent among patients at a high risk for the development of breast cancer and found to be effective, although it is associated with untoward adverse events (ie, stroke, venous thrombosis, and endometrial cancer)."( A review of selective estrogen receptor modulators and national surgical adjuvant breast and bowel project clinical trials.
Smith, RE, 2003
)
1.04
"Tamoxifen has been reported to protect against the progression of coronary artery diseases in human and different atherosclerosis animal models by blocking the appearance of the atheromatous plaque."( Tamoxifen is a potent inhibitor of cholesterol esterification and prevents the formation of foam cells.
Bernad, J; Bosser, I; de Medina, P; Favre, G; Faye, JC; Payré, BL; Pipy, B; Poirot, M; Silvente-Poirot, S, 2004
)
2.49
"Tamoxifen has a valuable role as neo-adjuvant treatment in terms of breast conservation and survival."( Neo adjuvant Tamoxifen in post menopausal patients with operable breast cancer.
Asselain, B; Campana, F; Clough, KB; Languille, O; Magdalenat, H; Remvikos, Y; Salmon, RJ, 2003
)
1.41
"Tamoxifen has been reported to cause retinal changes as side effects."( Kinetics of inhibition of glutamate uptake by antioestrogens.
Mäenpää, H; Saransaari, P; Tähti, H, 2003
)
1.04
"Tamoxifen has been used in some previous studies with variety of responses to therapy in patients with unresectable recurrent brain tumors."( Encouraging result of tamoxifen in a retinoblastoma patient with central nervous system metastasis.
Ekinci, C; Günalp, I; Gündüz, K; Taçyildiz, N; Unal, E; Yavuz, G, 2003
)
1.35
"Tamoxifen has clearly been shown to significantly decrease the risk of recurrence and improve survival in women of all ages who have estrogen (ER) or progesterone receptor (PR) positive invasive breast cancer, including those 70 years and older."( Adjuvant therapy for older women with breast cancer.
Muss, HB, 2003
)
1.04
"Tamoxifen has both agonistic and antagonistic effects on the female genital tract, depending on the ambient oestradiol concentration and the menopausal status of the patient. "( [The effects of tamoxifen on the female genital tract].
de Vries, EG; Hollema, H; Mourits, MJ; van der Zee, AG; Willemse, PH, 2003
)
2.11
"Tamoxifen has been widely used in breast cancer treatment. "( High-grade endometrial stromal sarcoma after treatment with tamoxifen in a patient treated for breast cancer.
Kohno, T; Ohwada, M; Saga, Y; Suzuki, M; Takayashiki, N,
)
1.82
"Tamoxifen has been shown in numerous prevention studies to decrease the incidence of breast cancer in high-risk women."( Endocrine prevention of breast cancer using selective oestrogen receptor modulators (SORMs).
Lo, SS; Vogel, VG, 2004
)
1.04
"Tamoxifen has been successfully used in the treatment of patients with fibrosing diseases, mainly retroperitoneal fibrosis."( Clinical experience with tamoxifen in peritoneal fibrosing syndromes.
Aguilera, A; Bajo, MA; Castro, MJ; Costero, O; del Peso, G; Gil, F; Ros, S; Selgas, R, 2003
)
1.34
"Tamoxifen has become the standard of care in relation to hormonal therapy for women with hormone-sensitive tumors. "( New developments in endocrine therapy: role of adjuvant therapy for early breast cancer.
Grana, G, 2003
)
1.76
"Tamoxifen has dramatically eliminated HHT-related bleeding in two cases."( Hormonal and antihormonal therapy for epistaxis in hereditary hemorrhagic telangiectasia.
Cave, DR; Jameson, JJ, 2004
)
1.04
"Tamoxifen has been the chosen endocrine therapy for postmenopausal, hormone-sensitive, ABC for over 20 years."( Tamoxifen--what next?
Gradishar, WJ, 2004
)
2.49
"Tamoxifen has been shown to stimulate arachidonic acid release from rat liver cells."( Tamoxifen and the Rafoxifene analog LY117018: their effects on arachidonic acid release from cells in culture and on prostaglandin I2 production by rat liver cells.
Levine, L, 2004
)
2.49
"Tamoxifen has emerged from recent Breast Cancer Prevention Trials, conducted to evaluate risk reduction, as an effective preventive agent."( Tamoxifen: an emerging preventive.
Schwartz, J, 2004
)
2.49
"Tamoxifen has been the mainstay of endocrine treatment for postmenopausal patients with early and advanced breast cancer for many years. "( Shifting paradigms in hormonal therapy for breast cancer.
Grana, G, 2004
)
1.77
"Tamoxifen metabolites have been previously shown to possess enhanced bioactivity, and consistent with this observation, tamoxifen metabolites but not tamoxifen modestly increased platelet aggregation."( The effects of tamoxifen and its metabolites on platelet function and release of reactive oxygen intermediates.
Flockhart, DA; Freedman, JE; Jin, Y; Varghese, S; Vitseva, O, 2005
)
1.4
"Tamoxifen has multiple metabolic effects, including reducing oxidative damage, while vitamin E primarily has this property."( Tamoxifen and vitamin E treatments delay symptoms in the mouse model of Niemann-Pick C.
Bascuñan-Castillo, EC; Erickson, RP; Gillies, RJ; Heidenreich, RH; Hicks, C; Howison, CM; Hunter, RJ; Trouard, TP, 2004
)
2.49
"Tamoxifen has been shown to inhibit ERalpha-mediated cyclin D1 transcription, and acquired resistance to tamoxifen is associated with a shift to ERalpha-independent cyclin D1 up-regulation. "( Histone deacetylase inhibitor trichostatin A represses estrogen receptor alpha-dependent transcription and promotes proteasomal degradation of cyclin D1 in human breast carcinoma cell lines.
Alao, JP; Ali, S; Bordogna, W; Buluwela, L; Coombes, RC; Lam, EW; Lockey, P; Stavropoulou, AV; Varshochi, R; Vigushin, DM, 2004
)
1.77
"Tamoxifen has long been the endocrine treatment of choice for women with breast cancer and is now employed for prophylactic use in women at high risk from breast cancer. "( Gene expression changes induced by estrogen and selective estrogen receptor modulators in primary-cultured human endometrial cells: signals that distinguish the human carcinogen tamoxifen.
Carmichael, PL; Gold, LI; Huby, R; Orton, T; Pole, JC, 2005
)
1.96
"Tamoxifen has been reported to directly activate large conductance calcium-activated potassium (KCa) channels through the KCa beta1 subunit, suggesting a cardio-protective role of this compound. "( Dual effect of tamoxifen on arterial KCa channels does not depend on the presence of the beta1 subunit.
Pérez, GJ, 2005
)
2.12
"Tamoxifen has been the standard adjuvant therapy for patients with breast cancer for the last several decades. "( A practical overview of aromatase inhibitors in postmenopausal women with hormone receptor-positive breast cancer.
Vandenberg, TA; Younus, J, 2005
)
1.77
"Tamoxifen has been the definitive standard of hormonal therapies for the last 30 years because of its documented efficacy and reasonable safety profile."( Aromatase inhibitors as adjuvant therapy for postmenopausal patients with early stage breast cancer.
Kudachadkar, R; O'Regan, RM,
)
0.85
"Tamoxifen has been a mainstay of adjuvant therapy for breast cancer for many years. "( Association of genetic variation in tamoxifen-metabolizing enzymes with overall survival and recurrence of disease in breast cancer patients.
Ahn, J; Ambrosone, CB; Kadlubar, FF; MacLeod, SL; Nowell, SA; Rae, JM; Scheys, JO; Sweeney, C; Trovato, A, 2005
)
2.05
"Tamoxifen has been available for over 20 years and remains the most commonly recognized endocrine therapy. "( Selective oestrogen receptor modulators, aromatase inhibitors and the female breast.
Howell, A, 2005
)
1.77
"Tamoxifen has been the standard of care for adjuvant endocrine therapy of early breast cancer. "( Adjuvant endocrine therapy in postmenopausal women with early breast cancer: where are we now?
Baum, M, 2005
)
1.77
"Tamoxifen has been the standard adjuvant therapy for patients with breast cancer for several decades. "( A practical overview of aromatase inhibitors.
Vandenberg, TA; Younus, J,
)
1.57
"Tamoxifen has been the standard adjuvant treatment for postmenopausal women with hormone-responsive early breast cancer for more than 20 years. "( Switching of postmenopausal women with endocrine-responsive early breast cancer to anastrozole after 2 years' adjuvant tamoxifen: combined results of ABCSG trial 8 and ARNO 95 trial.
Gademann, G; Gnant, M; Greil, R; Hilfrich, J; Jakesz, R; Jonat, W; Kaufmann, M; Kwasny, W; Menzel, C; Mittlboeck, M; Samonigg, H; Seifert, M; Tausch, C; Wolfgang, J,
)
1.78
"Tamoxifen has been known to be an effective agent in regression of desmoid tumors which include similar mesenchymal elements to those seen in RF."( Tamoxifen in the treatment of idiopathic retroperitoneal fibrosis.
Canbakan, B; Ekmekci, Y; Erbay, B; Ergun, I; Keven, K, 2005
)
2.49
"Tamoxifen has been the endocrine agent of choice for adjuvant hormonal therapy for early breast cancer since approval in 1986. "( Adjuvant endocrine therapy in postmenopausal breast cancer patients.
Köberle, D; Thürlimann, B, 2005
)
1.77
"Tamoxifen has been shown to reduce the incidence of invasive breast cancer in women at higher risk. "( How should we inform women at higher risk of breast cancer about tamoxifen? An approach with a decision guide.
Latosinsky, S; Martin, W; McKay, A, 2005
)
2.01
"Tamoxifen has been shown to be more effective and safe than RT in this setting."( Gynecomastia and breast pain induced by adjuvant therapy with bicalutamide after radical prostatectomy in patients with prostate cancer: the role of tamoxifen and radiotherapy.
Autorino, R; D'Armiento, M; Damiano, R; De Placido, S; De Sio, M; Di Lorenzo, G; Gallo, A; Gallo, L; Perdonà, S; Pingitore, D, 2005
)
1.25
"Tamoxifen has shown to be species, tissue, and cell-type specific."( Susceptibility of human breast epithelial cells in vitro to hormones and drugs.
Calaf, GM, 2006
)
1.06
"Tamoxifen has a significant affect on hormone receptor expression and markers of apoptosis in endometrial polyps. "( Does tamoxifen therapy affect the hormone receptor expression and cell proliferation indices of endometrial polyps? An immunohistochemical comparison of endometrial polyps from postmenopausal women exposed and not exposed to tamoxifen.
Duffy, SR; McGurgan, P; O'Donovan, PJ; Taylor, LJ, 2006
)
2.29
"Tamoxifen (TMX) has been related with the development of uterine sarcomas. "( Uterine sarcomas in breast cancer patients treated with tamoxifen.
Arenas, M; Biete, A; Hernández, V; Jorcano, S; Mellado, B; Ordi, J; Rovirosa, A,
)
1.82
"Tamoxifen has been approved for breast cancer risk reduction in high-risk women, but how raloxifene compares with tamoxifen is unknown."( Patient-reported symptoms and quality of life during treatment with tamoxifen or raloxifene for breast cancer prevention: the NSABP Study of Tamoxifen and Raloxifene (STAR) P-2 trial.
Costantino, JP; Dakhil, S; Ganz, PA; Land, SR; Lee, M; Lockhart, JB; Pajon, ER; Ritter, MW; Vogel, VG; Wade, JL; Wickerham, DL; Wolmark, N, 2006
)
2.01
"Tamoxifen has been the standard therapy for reducing risk of recurrence, although more than 50% of relapses and deaths occur after completion of tamoxifen."( Extended adjuvant therapy with letrozole: reducing the risk of recurrence.
Dixon, JM, 2006
)
1.06
"Tamoxifen has dual estrogenic and antiestrogenic effects; the estrogenic effects have been associated with ovulation induction in premenopausal women. "( Villous papyraceous: an unusual cause of tamoxifen-induced postmenopausal bleeding.
Mathew, J; Oladipo, A, 2006
)
2.04
"Tamoxifen has long been studied as a drug to treat breast cancer and now for its preventive effect. "( Modeling the effect of tamoxifen chemoprevention on long-term mortality in white women at high risk of breast cancer.
Maucort-Boulch, D; Roy, P, 2006
)
2.09
"Tamoxifen has long been the drug of choice in adjuvant endocrine therapy of steroid hormone receptor-positive breast cancer, and it still remains important due to its well-documented beneficial effect. "( High progesterone receptor expression correlates to the effect of adjuvant tamoxifen in premenopausal breast cancer patients.
Jirström, K; Jönsson, PE; Landberg, G; Nordenskjöld, B; Rydén, L; Stendahl, M, 2006
)
2.01
"Tamoxifen has provided the mainstay of endocrine therapy for more than 20 years. "( Aromatase inhibitors: changing the face of endocrine therapy for breast cancer.
Buzdar, AU,
)
1.57
"Tamoxifen has a lowering effect on serum lipids and is reported to decrease the risk of myocardial infarction but to increase the risk of thromboembolic events."( Cardiovascular health and aromatase inhibitors.
Abramson, BL; Pritchard, KI, 2006
)
1.06
"Tamoxifen has been a standard therapy for breast cancer, but its use is complicated by serious events, including endometrial cancer and thromboembolism. "( Adjuvant trials: Aromatase inhibitors in early breast cancer--are they alike?
Monnier, A, 2006
)
1.78
"Tamoxifen (TAM) has been the drug widely used until the recent emergence of the aromatase inhibitors (AIs)."( Side effects of aromatase inhibitors versus tamoxifen: the patients' perspective.
Delamelena, T; Garreau, JR; Johnson, N; Karamlou, K; Walts, D, 2006
)
1.32
"Tamoxifen has been reported to potentiate the anticoagulant effect of warfarin and also to increase the plasma level of phenytoin, which are mainly metabolized by CYP2C9. "( Tamoxifen inhibits cytochrome P450 2C9 activity in breast cancer patients.
Babaoglu, MO; Boruban, MC; Bozkurt, A; Sencan, O; Yasar, U, 2006
)
3.22
"Tamoxifen (TAM) has been used since early '70s as antitumor agent in the adjuvant therapy of breast carcinoma. "( Tamoxifen (TAM): the dispute goes on.
Grilli, S, 2006
)
3.22
"Tamoxifen has traditionally been the hormone therapy of choice for patients unable to undergo surgery, but development of resistance is a common feature."( Neoadjuvant use of hormonal therapy in elderly patients with early or locally advanced hormone receptor-positive breast cancer.
Dixon, JM; Macaskill, EJ; Renshaw, L,
)
0.85
"Tamoxifen has been the most important form of adjuvant endocrine therapy over the last 25 years."( Adjuvant endocrine therapy for early breast cancer.
Andreetta, C; Smith, I, 2007
)
1.06
"Tamoxifen has been a standard first-line endocrine therapy for post-menopausal women with hormone-responsive advanced breast cancer, but more than half of patients fail to respond and time to progression is less than 12 months in responders. "( Letrozole in advanced breast cancer: the PO25 trial.
Mouridsen, HT, 2007
)
1.78
"Tamoxifen has antiestrogenic effects in the breast tissue and is the standard endocrine treatment for women with breast cancer."( Estradiol affects liver mitochondrial function in ovariectomized and tamoxifen-treated ovariectomized female rats.
Custódio, JB; Moreira, PI; Moreno, A; Nunes, E; Oliveira, CR; Santos, MS; Seiça, R, 2007
)
1.3
"Tamoxifen has remained the antihormonal therapy of choice for the treatment of ER positive breast cancer for the last 30 years."( SERMs for the treatment and prevention of breast cancer.
Jordan, VC; Sharma, CG; Swaby, RF, 2007
)
1.06
"Tamoxifen treatment has a potential to stimulate the cell proliferation of endometrial glands and corpus luteum in tamoxifen-treated rats."( Immunohistochemical evaluation of cell proliferation and apoptosis markers in ovaries and uterus of tamoxifen-treated rats.
Akman, L; Cirpan, T; Kanit, L; Terek, MC; Ulukus, EC; Ulukus, M,
)
1.07
"Tamoxifen has been shown to be metabolized by CYP2D6 to the more potent metabolite endoxifen."( CYP2D6 polymorphisms and the impact on tamoxifen therapy.
Beverage, JN; Danesi, R; Figg, WD; Sion, AM; Sissung, TM, 2007
)
1.33
"Tamoxifen has been used and shown good results in non-HIV peritoneal dialysis patients with EPS."( First use of tamoxifen in an HIV patient with encapsulating peritoneal sclerosis.
Dratwa, M; Guillaume, MP; Mesquita, M, 2007
)
1.43
"Tamoxifen has been used as adjuvant therapy for early breast cancer for many years, and safety data have been well documented, but a poor risk:benefit profile limits treatment duration to 5 years."( Safety profiles of tamoxifen and the aromatase inhibitors in adjuvant therapy of hormone-responsive early breast cancer.
Perez, EA, 2007
)
1.39
"Tamoxifen has been found to be safe and effective in gynecological cancer patients with normal renal function. "( Tamoxifen is safe and effective in gynecological cancer patients with renal dysfunction.
Gershenson, DM; Jaishuen, A; Kavanagh, JJ; Li, Y; Sirisabya, N; Zheng, HG,
)
3.02
"Tamoxifen has been in the center of management of hormone-sensitive breast cancer. "( Tamoxifen induced-thrombocytopenia: it does occur.
Abali, H; Nasiroğlu, N; Oksüzoğlu, B; Pamukçuoğlu, M; Uner, A; Zengin, N, 2007
)
3.23
"Tamoxifen has significantly improved mortality of both pre- and postmenopausal women with hormone receptor-positive breast cancer. "( [Clinical benefit of antiestrogens for breast cancer].
Iino, Y; Koibuchi, Y, 2008
)
1.79
"Tamoxifen has antiestrogenic effects in the breast and estrogenlike activity in the skeletons of postmenopausal women. "( Prevention of bone loss after withdrawal of tamoxifen.
Brown, IN; Cohen, A; Fleischer, JB; Hershman, DL; Joe, AK; Johnson, MK; McMahon, DJ; Silverberg, SJ, 2008
)
2.05
"Tamoxifen (Tam) has been used experimentally to treat boys with gynecomastia and girls with McCune-Albright syndrome. "( Tamoxifen impairs both longitudinal and cortical bone growth in young male rats.
Chagin, AS; Gjerde, J; Heino, T; Karimian, E; Lien, EA; Ohlsson, C; Sävendahl, L, 2008
)
3.23
"Tamoxifen has been shown to reduce the incidence of estrogen receptor-positive invasive breast cancer in women with a high risk of developing this condition by nearly 50%, and studies in osteoporosis have revealed a similar protective effect of raloxifene in postmenopausal women."( Chemoprevention of breast cancer.
Castrellon, AB; Glück, S, 2008
)
1.07
"Tamoxifen has been the standard first-line adjuvant treatment for postmenopausal women with early breast cancer for over 3 decades. "( Translating trial data into patients benefits: making the right choice.
Chlebowski, RT, 2008
)
1.79
"Tamoxifen has been associated with increased risk of endometrial carcinoma, although the exact mechanism of action is unknown."( Clinicopathological and molecular analysis of endometrial carcinoma associated with tamoxifen.
Dahiya, S; Hardisson, D; Moreno-Bueno, G; Oliva, E; Palacios, J; Prat, J; Sánchez-Estevez, C; Turbiner, J, 2008
)
1.29
"Tamoxifen has been used in the management of receptor-positive breast cancer for >20 years. "( Quantifiable mRNA transcripts for tamoxifen-metabolising enzymes in human endometrium.
Abdo, KR; Ashton, KM; Martin, FL; Martin-Hirsch, PL; Paraskevaidis, E; Phillips, DH; Singh, MN; Stringfellow, HF; Walsh, MJ, 2008
)
2.07
"Tamoxifen has been shown to be an unusually safe and well-tolerated drug."( Antiestrogen therapy of breast cancer.
Lippman, ME, 1983
)
0.99
"Tamoxifen has a similar effect but to a much lesser extent than estradiol."( Anti-estrogens in fetal and newborn target tissues.
Gulino, A; Pasqualini, JR; Screpanti, I; Sumida, C, 1984
)
0.99
"Tamoxifen has been given to Chick embryos between the 3rd and 7th day at doses of 0.2-2 mg/egg. "( [Changes in the female gonads of the chick embryo after tamoxifen].
Baulieu, EE; Reyss-Brion, M; Salzgeber, B, 1981
)
1.95
"Tamoxifen has recently been shown to suppress the growth and secretion of prolactin (PRL)-secreting pituitary tumors in rats. "( The effect of tamoxifen on GH and PRL secretion by human pituitary tumors.
de Quijada, M; Klijn, JG; Lamberts, SW,
)
1.93
"But tamoxifen has no effect on the growth rate (growth constant of R27 under control condition, 0.071 +/- 0.007 day-1; tamoxifen-treated cells, 0.073 +/- 0.011 day-1) and minimal effects on thymidine incorporation in R27, whereas tamoxifen has a strongly suppressive effect on the growth rate and thymidine incorporation in MCF-7."( Isolation and characterization of a tamoxifen-resistant cell line derived from MCF-7 human breast cancer cells.
Bronzert, D; Lippman, ME; Nawata, H, 1981
)
1.02
"Tamoxifen citrate has been administered continuously at various dosages to 31 males with evaluable advanced breast cancer in 16 different centers. "( Use of tamoxifen in advanced male breast cancer.
Bach, BK; Battersby, LA; Patterson, JS,
)
2.03
"Tamoxifen (TAM) has been reported to enhance cisplatin (CDDP) cytotoxicity in experimental and clinical melanoma studies. "( A phase II study of tamoxifen combined with cisplatin-interleukin 2 and alpha-interferon in metastatic melanoma.
Antoine, EC; Auclerc, G; Benhammouda, A; Borel, C; Franks, C; Ghironzi, GC; Mularoni, E; Rixe, O; Soubrane, C; Vuillemin, E, 1995
)
2.06
"Tamoxifen has been used as adjuvant treatment in advanced and early-stage breast cancer for the past decade. "( Sensory perceptions of women receiving tamoxifen for breast cancer.
Hanson, BM; McDaniel, RW; Nelson, RA; Rhodes, VA, 1995
)
2
"Tamoxifen, however, has been promoted as a modulator in some drug regimens."( Activity of platinum drugs against melanoma cell lines: is it modulated in vitro in the presence of tamoxifen?
Mohammed, MQ; Photiou, A; Retsas, S; Shah, P,
)
1.07
"Tamoxifen has no efficacy in the treatment of patients with advanced hepatocellular carcinoma."( Treatment of hepatocellular carcinoma with tamoxifen: a double-blind placebo-controlled trial in 120 patients.
Ayuso, C; Boix, L; Brú, C; Bruix, J; Castells, A; Roca, M; Rodés, J; Vilana, R, 1995
)
2
"Tamoxifen has been shown to be effective in the treatment of desmoid tumors, and we present a patient with retroperitoneal fibrosis who was treated successfully with this anti-estrogen."( Retroperitoneal fibrosis treated with tamoxifen.
Cance, WG; Huth, JF; Owens, LV, 1995
)
1.28
"Tamoxifen has a well established place in the adjuvant therapy of primary carcinoma of the breast. "( Hormonal manipulation and gynaecological cancer: the tamoxifen dilemma.
Ross, D; Whitehead, M, 1995
)
1.98
"Tamoxifen has been shown to inhibit the proliferation of human gliomas in vitro. "( A comparison of the relative chemosensitivity of human gliomas to tamoxifen and n-desmethyltamoxifen in vitro.
Kristofik, MP; Randall, MS; Rehn, T; Selker, RG; Vertosick, FT, 1994
)
1.97
"Tamoxifen has found extensive use in the treatment of all stages of human breast cancer. "( Tamoxifen induces hepatic aneuploidy and mitotic spindle disruption after a single in vivo administration to female Sprague-Dawley rats.
Bahnub, N; Dragan, YP; Jordan, VC; Pitot, HC; Sargent, LM; Sattler, CA; Sattler, GL; Schroeder, P; Wiley, JE, 1994
)
3.17
"Tamoxifen has estrogen-like effects on bone metabolism that result in an increase and stabilization of bone mineral density in the axial skeleton and a stabilization of bone mineral content in the appendicular skeleton."( Tamoxifen and bone metabolism in postmenopausal low-risk breast cancer patients: a randomized study.
Dalgaard, P; Ejlertsen, B; Holmegaard, SN; Kristensen, B; Larsen, L; Mouridsen, HT; Transbøl, I, 1994
)
3.17
"Tamoxifen has been an effective antiestrogen in suppressing breast cancer growth which is estrogen-responsive or dependent. "( Absence of transforming growth factor-beta responsiveness in the tamoxifen growth-inhibited human breast cancer cell line CAMA-1.
Ji, H; Leung, BS; Leung, HT; Stout, LE; Zhang, Q; Zhang, R, 1994
)
1.97
"Tamoxifen has been found to be metabolized by liver primarily into three metabolites, tamoxifen-N-oxide, formed by the flavin-containing monooxygenase, and N-desmethyl- and 4-hydroxytamoxifen, formed by cytochrome P450. "( Induction of tamoxifen-4-hydroxylation by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), beta-naphthoflavone (beta NF), and phenobarbital (PB) in avian liver: identification of P450 TCDDAA as catalyst of 4-hydroxylation induced by TCDD and beta NF.
Kupfer, D; Lee, CA; Mani, C; Rifkind, AB, 1994
)
2.1
"Tamoxifen has been found to be a safe and effective treatment for all stages of breast cancer. "( Fourteenth Gaddum Memorial Lecture. A current view of tamoxifen for the treatment and prevention of breast cancer.
Jordan, VC, 1993
)
1.98
"Tamoxifen has anti-estrogenic effects not only on breast cancer cells but also on liver metabolism and bone, with concomitant decreases in risk factors for chronic skeletal and vascular system diseases."( Tamoxifen therapy in breast cancer control worldwide.
Koroltchouk, V; Love, RR, 1993
)
2.45
"Tamoxifen has very little or no effect, 4-hydroxytamoxifen has an intermediate effect and ICI 164,384 is active in the enzyme inhibition, particularly with MDA-MB-231 cells."( Effect of promegestone, tamoxifen, 4-hydroxytamoxifen and ICI 164,384 on the oestrone sulphatase activity of human breast cancer cells.
Chetrite, G; Delalonde, L; Pasqualini, JR; Varin, C,
)
1.16
"Tamoxifen (Nolvadex) has been in use for over 20 years and currently is probably the most prescribed anti-cancer medication in the world. "( The role of tamoxifen in the prevention and treatment of benign and malignant breast lesions: a chemopreventive.
Leis, HP,
)
1.95
"Tamoxifen has been used in the adjuvant treatment of breast cancer because of its antiestrogenic effects. "( Intestinal and pelvic endometriosis presenting as a tumor and associated with tamoxifen therapy: report of a case.
Hajjar, LR; Kim, W; Nolan, GH; Raju, UR; Turner, S, 1993
)
1.96
"Tamoxifen has an estrogen-like influence on the skeletal and cardiovascular systems, resulting in decreases in both postmenopausal bone loss and low density lipoprotein (LDL) levels."( A risk-benefit assessment of tamoxifen therapy.
Catherino, WH; Jordan, VC, 1993
)
1.3
"Tamoxifen has produced a small increase in the response rate when added to the present combination and schedule of chemotherapy."( The addition of tamoxifen to dacarbazine and cisplatin in metastatic malignant melanoma. A phase II trial of the Southwest Oncology Group, (SWOG-8921).
Flaherty, LE; Fletcher, WS; Goodwin, JW; Liu, PY; Mitchell, MS; Sondak, VK; Stephens, RL; Walker, MJ, 1996
)
1.36
"Tamoxifen has been used extensively as adjuvant therapy in the treatment of pre- and post-menopausal patients with breast cancer. "( Thrombosis of tibial arteries in a patient receiving tamoxifen therapy.
Deshmukh, N; Tripathi, SP, 1995
)
1.98
"Tamoxifen has been shown to improve survival among subsets of patients with breast cancer in all stages."( Endometrial cancer. Management of high risk and recurrence including the tamoxifen controversy.
Cohen, CJ; Rahaman, J, 1995
)
1.24
"Tamoxifen (Tx) has been used in breast cancer treatment and prophylaxis because of its antiestrogenic activity; however, Tx may also have beneficial cardiovascular effects and other actions mediated by mechanisms other than estrogen receptors. "( Tamoxifen (estrogen antagonist) inhibits voltage-gated calcium current and contractility in vascular smooth muscle from rats.
Gappy, S; Joshi, D; Ram, JL; Song, J; Sowers, JR; Standley, PR; Zhang, F, 1996
)
3.18
"Tamoxifen has been noted for its reportedly low incidence of side effects."( [Tamoxifen and endometrial cancer. A case report].
Lindal, S; Mortensen, E; Orbo, A, 1996
)
1.93
"Tamoxifen has previously been shown to prolong the survival of patients with advanced stages of hepatocellular carcinoma and it has been suggested that it inhibits the growth of hepatoma cells through an estrogen receptor-dependent mechanism. "( Tamoxifen inhibits hepatoma cell growth through an estrogen receptor independent mechanism.
Jiang, SY; Jordan, VC; Shyu, RY; Yeh, MY, 1995
)
3.18
"Tamoxifen has been widely used in the treatment of breast cancer. "( Tamoxifen and the uterus: an old drug tested by new modalities.
Achiron, R; Golan-Porat, N; Grisaru, D; Lipitz, S, 1996
)
3.18
"Tamoxifen, which has estrogenic effects on bone resorption, and transforming growth factor-beta 1 (TGF-beta), whose production by osteoblasts is increased by estrogen, had similar effects in vitro."( Estrogen promotes apoptosis of murine osteoclasts mediated by TGF-beta.
Boyce, BF; Dai, A; Hughes, DE; Li, HH; Mundy, GR; Tiffee, JC, 1996
)
1.02
"Tamoxifen has been the endocrine treatment of choice for all stages of breast cancer for nearly a decade. "( A realistic clinical perspective of tamoxifen and endometrial carcinogenesis.
Assikis, VJ; Jordan, VC; Neven, P; Vergote, I, 1996
)
2.01
"Tamoxifen has a wide range of systemic effects, possibly acting on every estrogen target tissue in the body."( Tamoxifen in postmenopausal women a safety perspective.
Kimmick, GG; Muss, HB; Robinson, E, 1996
)
2.46
"Tamoxifen (TAM) has been shown to circumvent multidrug resistance in P-glycoprotein-expressing cell lines."( Tamoxifen circumvents the multidrug resistance in fresh human gastrointestinal cancer cells.
Arii, K; Hotta, T; Iwahashi, M; Mizobata, S; Noguchi, K; Tamai, M; Tani, M; Tanimura, H; Terasawa, H; Tsunoda, T; Yamaue, H, 1996
)
2.46
"Tamoxifen has not been previously used in the treatment of Riedel's thyroiditis."( Riedel's thyroiditis: treatment with tamoxifen.
Angelos, P; Few, J; Giordano, T; Reeve, T; Simeone, D; Thompson, NW, 1996
)
1.29
"Tamoxifen has proved to be the most effective drug therapy available for managing Riedel's thyroiditis. "( Riedel's thyroiditis: treatment with tamoxifen.
Angelos, P; Few, J; Giordano, T; Reeve, T; Simeone, D; Thompson, NW, 1996
)
2.01
"Tamoxifen has a particularly valuable role in developing countries in which the incidence of breast cancer is increasing as the average age of the population increases and in which control is substantially more difficult with mass mammography screening."( The control of breast cancer: the role of tamoxifen.
Forbes, JF, 1997
)
1.28
"Tamoxifen has been used most commonly to treat breast and endometrial cancer, two malignancies in which the antiestrogenic properties of tamoxifen have substantial therapeutic benefit. "( Tamoxifen for the treatment of malignancies other than breast and endometrial carcinoma.
Gelmann, EP, 1997
)
3.18
"Tamoxifen has been demonstrated to be hepatocarcinogenic in some but not all strains of the laboratory rat and is not a carcinogen in the mouse. "( Comparative metabolism of tamoxifen and DNA adduct formation and in vitro studies on genotoxicity.
Tannenbaum, SR, 1997
)
2.04
"Tamoxifen has both antiestrogenic and estrogenic activity."( Risks and benefits of tamoxifen therapy.
Assikis, VJ; Jordan, VC, 1997
)
1.33
"Tamoxifen has well-documented activity in reducing breast cancer mortality. "( Interaction of tamoxifen's impact on overall net mortality and quality of life.
Ragaz, J, 1997
)
2.09
"Tamoxifen citrate has been prescribed to millions of women with breast cancer and has been one of the most important advances in breast cancer treatment over the past 25 years. "( Tamoxifen's impact on the management of breast cancer: patient perspectives.
Reichman, BS, 1997
)
3.18
"Tamoxifen has been shown to be useful in the treatment of desmoid tumors and idiopathic retroperitoneal fibrosis."( Sclerosing mesenteritis: an unusual cause of abdominal pain in an HIV-positive patient.
Behling, CA; Lyche, KD; Venkataramani, A, 1997
)
1.02
"Tamoxifen has primarily estrogen-antagonistic effects on epicardial coronary artery dilator responses in atherosclerotic monkeys. "( Contrasting effects of conjugated estrogens and tamoxifen on dilator responses of atherosclerotic epicardial coronary arteries in nonhuman primates.
Adams, MR; Honoré, EK; Williams, JK, 1997
)
2
"Tamoxifen has been associated with maintenance of bone mineral density, a reduction in cardiac events, and a slightly increased risk of endometrial cancer."( Tamoxifen and toremifene in breast cancer: comparison of safety and efficacy.
Buzdar, AU; Hortobagyi, GN, 1998
)
2.46
"Tamoxifen has been shown to decrease the recurrence rate of breast cancer. "( The use of transvaginal ultrasound and saline infusion sonohysterography for the evaluation of asymptomatic postmenopausal breast cancer patients on tamoxifen.
Goldstein, SR; Horan, C; Nachtigall, LE; Porges, RF; Schwartz, LB; Snyder, J, 1998
)
1.94
"Tamoxifen (TAM) has been found to be effective in inhibiting proliferation of glioblastoma cells in vitro, but clinical studies have been disappointing. "( Antagonist effect of insulin-like growth factor I on protein kinase inhibitor-mediated apoptosis in human glioblastoma cells in association with bcl-2 and bcl-xL.
Barna, BP; Barnett, GH; Casey, G; Haqqi, T; Hercbergs, A; Iwasaki, K; Kondo, S; Liu, J; Toms, SA, 1998
)
1.74
"Tamoxifen has been shown to potentiate in vivo anti-tumour activity of IL-2, and because of its non-toxic behaviour it was included in both groups."( Survival in renal cell carcinoma-a randomized evaluation of tamoxifen vs interleukin 2, alpha-interferon (leucocyte) and tamoxifen.
Colleen, S; Engman, K; Helsing, M; Henriksson, R; Nilsson, S; Wersäll, P; Zimmerman, R, 1998
)
1.26
"Tamoxifen has few adverse effects and severe complications are very uncommon."( [Monitoring women on tamoxifen ].
Diouf, A; Lansac, J, 1998
)
1.34
"Tamoxifen (Tam) has been shown to inhibit dexamethasone (Dex)-mediated effects on bone formation in vitro. "( Tamoxifen attenuates the effects of exogenous glucocorticoid on bone formation and growth in piglets.
Atkinson, SA; Fritz, PC; Tenenbaum, HC; Ward, WE, 1998
)
3.19
"Tamoxifen (TAM) has moderate PKC-inhibiting activity, blocking DNA synthesis and cellular proliferation in human glioma cells at concentrations that can be achieved therapeutically."( Tamoxifen modulation of carboplatin cytotoxicity in a human U-138 glioma cell line.
Farah, JO; Mastronardi, L; Puzzilli, F; Ruggeri, A, 1998
)
2.46
"Tamoxifen has been used as an adjuvant therapy for breast cancer for nearly two decades. "( Gynecologic effects of tamoxifen and the association with endometrial carcinoma.
Assikis, VJ; Jordan, VC, 1995
)
2.04
"Tamoxifen (TAM) has recently been shown to inhibit the growth rate of established and low-passage human glioma cell lines."( Tamoxifen as a potential treatment of glioma.
Mastronardi, L; Puzzilli, F; Ruggeri, A, 1998
)
2.46
"Tamoxifen has been shown to promote the growth of human endometrial tumors implanted in athymic mice, and it has been associated with a twofold to threefold increase in endometrial cancer. "( Effects of the antiestrogens tamoxifen, toremifene, and ICI 182,780 on endometrial cancer growth.
Assikis, VJ; Bilimoria, MM; Chatterton, R; Cisneros, A; Dragan, YP; England, GM; Jordan, VC; MacGregor, JI; Muenzner, HD; O'Regan, RM; Piette, M; Pitot, HC, 1998
)
2.03
"Tamoxifen, which has been used extensively in the treatment of breast cancer over the last 20 years has recently been shown to inhibit the proliferation of fibroblasts cultured from keloid biopsies."( Topical tamoxifen--a potential therapeutic regime in treating excessive dermal scarring?
Cherry, GW; Hu, D; Hughes, MA, 1998
)
1.46
"Tamoxifen therapy has been associated with the development of endometrial polyps, hyperplasia and adenocarcinoma possibly mediated through its agonistic estrogenic properties."( Tamoxifen-induced endometrial polyp. A case report and review of the literature.
Elemenoglou, J; Nomikos, IN; Papatheophanis, J, 1998
)
2.46
"Tamoxifen has some weak estrogenic activity."( [Severe hypertriglyceridemia induced by tamoxifen].
Komiya, I; Taira, M; Takasu, N, 1998
)
1.29
"Tamoxifen has been used for a long time as an adjuvant hormonal treatment in breast cancer patients. "( Changes in serum lipid and lipoprotein levels in postmenopausal patients with node-positive breast cancer treated with tamoxifen.
Belev, B; Plestina, S; Reiner, Z; Vrbanec, D,
)
1.78
"Tamoxifen has been shown to be a potent liver carcinogen in rats, and generates covalent DNA adducts. "( Tamoxifen metabolism in rat liver microsomes: identification of a dimeric metabolite derived from free radical intermediates by liquid chromatography/mass spectrometry.
Jones, RM; Lim, CK; Yuan, ZX, 1999
)
3.19
"Tamoxifen has a beneficial effect on bone density presumably through its estrogen agonistic effects."( Tamoxifen effects on menopause--associated risk factors and symptoms.
Benshushan, A; Brzezinski, A, 1999
)
2.47
"Tamoxifen has been reported to have numerous physiological effects that are independent of the estrogen receptor, including sensitization of resistant tumor cells to many chemotherapeutic agents. "( Tamoxifen inhibits acidification in cells independent of the estrogen receptor.
Altan, N; Chen, Y; Schindler, M; Simon, SM, 1999
)
3.19
"Tamoxifen has become one of the most widely used drugs in the treatment of breast cancer, and concerns about its long-term safety and efficacy are being raised. "( The association between tamoxifen and the development of hepatocellular carcinoma: case report and literature review.
Law, CH; Tandan, VR, 1999
)
2.05
"Tamoxifen has been reported to inhibit acidification of cytoplasmic organelles in mammalian cells. "( A mechanism for tamoxifen-mediated inhibition of acidification.
Chen, Y; Schindler, M; Simon, SM, 1999
)
2.09
"Tamoxifen has been used for the treatment of human HCC."( Regulation of transforming growth factor-beta1 gene expression and cell proliferation in human hepatocellular carcinoma cells (PLC/PRF/5) by tamoxifen.
Gong, Y; Minuk, GY; Zhang, M, 1999
)
1.23
"Tamoxifen has been widely used for almost 20 years as adjuvant therapy for breast cancer."( Tamoxifen and malignant epithelial-nonepithelial tumours of the endometrium: report of six cases and review of the literature.
Bailly, C; Clement-Chassagne, C; Guastalla, P; Mignotte, H; Treilleux, T, 1999
)
2.47
"Tamoxifen (TAM) has been shown to induce apoptosis in breast cancer cells. "( Tamoxifen-induced apoptosis in breast cancer cells relates to down-regulation of bcl-2, but not bax and bcl-X(L), without alteration of p53 protein levels.
Abe, R; Kanno, M; Kimijima, I; Onda, M; Sato, H; Takenoshita, S; Tsuchiya, A; Watanabe, T; Zhang, GJ, 1999
)
3.19
"Tamoxifen has been linked to an increased risk for the development of endometrial adenocarcinoma. "( Detection of endometrial adenocarcinoma in two asymptomatic postmenopausal women receiving tamoxifen. A report of two cases.
Eastlund, M; Look, K; Sanders, B; Sutton, G, 1999
)
1.97
"Tamoxifen has been used as adjuvant therapy for the treatment of breast cancer. "( Uterine pleomorphic rhabdomyosarcoma in a patient receiving tamoxifen therapy.
Okada, DH; Petrovic, LM; Rowland, JB, 1999
)
1.99
"Tamoxifen has been used traditionally as adjuvant therapy for breast cancer, but new data indicate that it is effective in the primary prevention of breast cancer in women at increased risk."( Selective estrogen receptor modulators and postmenopausal health.
Arnaud, CD; Chiu, KM; Roe, EB, 2000
)
1.03
"Tamoxifen has no efficacy in the treatment of patients with advanced HCC and response to treatment was not affected by the expression of hormone receptors."( Treatment of advanced hepatocellular carcinoma with tamoxifen and the correlation with expression of hormone receptors: a prospective randomized study.
Fan, ST; Liu, CL; Lo, CM; Ng, IO; Poon, RT; Wong, J, 2000
)
2
"Oral tamoxifen has been proposed on the basis of beneficial results in some trials."( Controlled clinical trial of doxorubicin and tamoxifen versus tamoxifen monotherapy in hepatocellular carcinoma.
Lochs, H; Plauth, M; Schachschal, G, 2000
)
1.02
"Tamoxifen has partial agonist effects with ERalpha but not with ERbeta."( Estrogen receptors alpha and beta: prevalence of estrogen receptor beta mRNA in human vascular smooth muscle and transcriptional effects.
Graham, JD; Hodges, YK; Horwitz, KB; Horwitz, LD; Tung, L; Yan, XD, 2000
)
1.03
"Tamoxifen has been used for the treatment of breast cancer since the 1970s, but is considered a carcinogen because it has been linked to liver cancer in rats and an increased risk of endometrial cancer in patients. "( Genotoxic effects of the novel mixed antiestrogen FC-1271a in comparison to tamoxifen and toremifene.
DeGregorio, MW; Hellmann-Blumberg, U; Taras, TL; Wurz, GT, 2000
)
1.98
"Yet tamoxifen has been shown to be equipotent in both sexes."( Sex differences in the activation of tamoxifen to DNA binding species in rat liver in vivo and in rat hepatocytes in vitro: role of sulfotransferase induction.
Davis, W; Glatt, H; Hewer, A; Meinl, W; Phillips, DH; Rajkowski, KM, 2000
)
1.06
"Tamoxifen has multiple influence on the rate of growth of cancer cells: depends on estrogen receptor (ER), conducts reduction of proliferation rate; depends on ER and other mechanisms conducts to suppressions of Bcl-2 protein expression and induction of cell death through apoptotic pathway."( Influence of estrogen, antiestrogen and UV-light on the balance between proliferation and apoptosis in MCF-7 breast adenocarcinoma cells culture.
Anchim, T; Dabrowska, M; Dziecioł, J; Pietruczuk, M; Swiatecka, J; Wołczyński, S, 2000
)
1.03
"Tamoxifen has been shown to decrease the risk of invasive breast cancer and decrease breast density."( Effect of tamoxifen on mammographic density.
Chow, CK; Jones, EC; O'Shaughnessy, J; Premkumar, A; Venzon, D; Zujewski, J, 2000
)
1.43
"Tamoxifen therapy has limited efficacy in refractory ovarian carcinoma."( Tamoxifen in the treatment of recurrent ovarian carcinoma.
Kaern, J; Marth, C; Tropé, C, 2000
)
2.47
"Tamoxifen has been approved by the U.S."( Breast cancer risk reduction: what do we know and where should we go?
Prout, MN,
)
0.85
"Tamoxifen has both agonist and antagonist activities, which are manifested in a tissue-specific pattern."( Thoughts on tamoxifen resistant breast cancer. Are coregulators the answer or just a red herring?
Bain, DL; Graham, JD; Horwitz, KB; Jackson, TA; Richer, JK; Tung, L, 2000
)
1.41
"Tamoxifen has been reported as variously active or inactive with or without previous systemic therapy."( Tamoxifen in the treatment of advanced or recurrent endometrial carcinoma: a Gynecologic Oncology Group study.
Bell, J; Brady, MF; Homesley, HD; Soper, JT; Thigpen, T, 2001
)
2.47
"Tamoxifen has recently been shown to reduce the incidence of noninvasive breast cancer in high-risk women, but the molecular mechanism of tamoxifen chemoprevention in mammary epithelial tissue that does not overexpress the estrogen receptor is poorly understood."( Human papillomavirus type 16 E6 inactivation of p53 in normal human mammary epithelial cells promotes tamoxifen-mediated apoptosis.
Caldwell, LE; Dietze, EC; Mrózek, K; Parker, M; Seewaldt, VL, 2001
)
1.25
"Tamoxifen has several potential mechanisms of action including inhibition of the release of excitatory amino acids (EAA) and nitric oxide synthase (NOS) activity."( Tamoxifen inhibits nitrotyrosine formation after reversible middle cerebral artery occlusion in the rat.
Feustel, PJ; Kimelberg, HK; Mongin, AA; Osuka, K; Tranmer, BI, 2001
)
2.47
"Tamoxifen has been shown to inhibit volume activated chloride currents in many cell types. "( Volume--activated chloride currents in HeLa cells are blocked by tamoxifen but not by a membrane impermeant quaternary analogue.
Allen, MC; Hardy, SP; Hunter, AC; Lloyd, AW; Sahebgharani, M, 2001
)
1.99
"Tamoxifen, which has both estrogen-mimetic and estrogen-antagonist properties, has been widely used to improve the prognosis of breast cancer patients."( Novel tumor-promoting property of tamoxifen.
Abbas, T; Barile, N; Chatakondu, K; Foster, DA; Hornia, A; Kaplan, P; Lu, Z; Zhong, M, 2001
)
1.31
"Tamoxifen has the potential for perturbing the rate of OM since it can function as a calcium antagonist by binding to calmodulin and inhibiting the formation of a calcium-calmodulin complex which is needed for activating calmodulin-dependent cAMP phosphodiesterase and initiating OM."( Tamoxifen-induced alterations in meiotic maturation and cytogenetic abnormalities in mouse oocytes and 1-cell zygotes.
London, SN; Mailhes, JB, 2001
)
2.47
"Tamoxifen citrate has shown promise in the treatment of keloids."( Effect of tamoxifen on transforming growth factor beta1 production by keloid and fetal fibroblasts.
Hanasono, MM; Kadleck, JM; Kita, M; Koch, RJ; Lum, J; Mikulec, AA,
)
1.26
"Tamoxifen (TMX) has proven to be an effective palliative treatment for advanced breast cancer with low reported incidence of side effects. "( On the promoting action of tamoxifen in a model of hepatocarcinogenesis induced by p-dimethylaminoazobenzene in CF1 mice.
Batlle, A; Caballero, F; Falcoff, N; Gerez, E; Oliveri, L; Vazquez, E, 2001
)
2.05
"Tamoxifen (Nolvadex) has long been established as "standard" adjuvant therapy for receptor-positive, early-stage breast cancer. "( Adjuvant exemestane therapy after 5 years of tamoxifen: rationale for the NSABP B-33 trial.
Mamounas, EP, 2001
)
2.01
"Tamoxifen has been an epoch-making drug during the late 20th century."( [Developments of hormonal agents for breast cancer].
Tominaga, T, 2001
)
1.03
"Tamoxifen has proven to be effective in improving relapse-free and overall survival in both pre- and postmenopausal women with ER(+) early-stage breast cancer."( Role of adjuvant endocrine therapy in early-stage breast cancer.
Muss, HB, 2001
)
1.03
"Tamoxifen has mixed estrogen agonist and antagonist properties in estrogen-regulated tissues. "( Tamoxifen is not detrimental to endothelial function in postmenopausal women with breast cancer.
Collins, P; Coombes, RC; Graham, HA; Hayward, CS; Linardou, H; Ong, PJ; Savage, P, 2001
)
3.2
"Tamoxifen has a new role in chemoprevention in patients at high risk of breast cancer."( New drugs in breast cancer.
Iqbal, S; Miller, WR, 2001
)
1.03
"Tamoxifen has a complex effect on the female reproductive tract and several tamoxifen-associated changes have been described among tamoxifen users."( Tamoxifen and the female reproductive tract.
Eltabbakh, GH; Mount, SL, 2001
)
2.47
"Only tamoxifen has been approved by the US Food and Drug Administration to reduce the incidence of breast cancer in high-risk women."( Selective estrogen-receptor modulators in 2001.
Gradishar, WJ; O'Regan, RM, 2001
)
0.77
"Tamoxifen (TAM) has been used in the treatment of breast cancer for over a decade. "( Mechanisms of tamoxifen-induced apoptosis.
Kong, AN; Mandlekar, S, 2001
)
2.11
"Tamoxifen has been used for the systemic treatment of patients with breast cancer for nearly three decades. "( Tamoxifen resistance in breast cancer: elucidating mechanisms.
Beex, LV; Berns, EM; Brinkman, A; Dorssers, LC; Foekens, JA; Klijn, JG; van Agthoven, T; Van der Flier, S; Veldscholte, J, 2001
)
3.2
"Tamoxifen has proved efficacious in all settings of breast cancer."( The effect of SERMs on the endometrium.
Goldstein, SR, 2001
)
1.03
"Tamoxifen has not only proved to be a valuable treatment for estrogen receptor (ER)-positive breast cancer, but is also a pioneering medicine for chemoprevention in high-risk pre- and postmenopausal women. "( Selective estrogen receptor modulators (SERMS) and their roles in breast cancer prevention.
Jordan, VC; Park, WC, 2002
)
1.76
"Tamoxifen has been shown to increase cytoplasmic free Ca2+ levels [Ca2+]i in renal tubular cells and bladder cancer cells, and to after Ca2+ signaling in MCF-7 breast cancer cells. "( Tamoxifen-induced increases in cytoplasmic free Ca2+ levels in human breast cancer cells.
Chang, HT; Chen, WC; Cheng, JS; Chou, KJ; Huang, JK; Jan, CR; Law, YP; Lee, KC; Liu, CP; Lo, YK; Su, W; Wang, JL, 2002
)
3.2
"Tamoxifen has been shown to be genotoxic in several studies."( Toxicity of antiestrogens.
Aaltonen, A; Hirsimäki, P; Mäntylä, E,
)
0.85
"Tamoxifen has been shown to induce apoptosis in multiple myeloma cell lines and primary myeloma cells. "( Tamoxifen-based treatment induces clinically meaningful responses in multiple myeloma patients with relapsing disease after autotransplantation.
Bolaños-Meade, J; Cottler-Fox, M; Fassas, AB; Rapoport, AP; Shanholtz, C; Tricot, G,
)
3.02
"Tamoxifen has favorable effects on the serum lipid profile. "( Are the effects of tamoxifen on the serum lipid profile modified by apolipoprotein E phenotypes?
Bairaktari, E; Elisaf, M; Karabina, SA; Liberopoulos, E; Nicolaides, C; Pavlidis, N; Tselepis, A, 2002
)
2.09
"Tamoxifen has been shown to decrease the risk of invasive breast cancer by 49% and noninvasive breast cancer by 50%. "( Selective estrogen receptor modulators (SERMs) and retinoids in breast cancer chemoprevention.
Zujewski, J, 2002
)
1.76
"Tamoxifen treatment has been demonstrated to decrease the function of fibroblasts derived from Dupuytren's affected fascia and downregulated TGF(beta2) production in these same fibroblasts."( Tamoxifen decreases fibroblast function and downregulates TGF(beta2) in dupuytren's affected palmar fascia.
Ko, F; Kuhn, MA; Payne, WG; Robson, MC; Wang, X, 2002
)
2.48
"Tamoxifen has dominated endocrine treatment of breast cancer for over two decades. "( Tamoxifen resistant and refractory breast cancer: the value of aromatase inhibitors.
Goss, PE; Strasser, K, 2002
)
3.2
"Tamoxifen has been shown previously to be metabolized to reactive products that have the potential to form protein and DNA adducts."( Bioactivation of tamoxifen by recombinant human cytochrome p450 enzymes.
De Wolf, CJ; Gillam, EM; Lancaster, RG; Notley, LM; Wunsch, RM, 2002
)
1.38
"Tamoxifen has been used for a long time as a hormonal treatment in breast cancer. "( Tamoxifen therapy and hepatic steatosis.
Coskun, U; Günel, N; Törüner, FB, 2002
)
3.2
"Tamoxifen has mixed agonist/antagonist activities, leading to tissue-specific estrogen-like actions and endometrial cancer. "( Regulation of estrogen target genes and growth by selective estrogen-receptor modulators in endometrial cancer cells.
Chen, B; Dardes, RC; Jordan, VC; Osipo, C; Pearce, ST; Schafer, JM, 2002
)
1.76
"Tamoxifen has more or less strong estrogen influence according to the targets : a light one on the uterus (1 mg being much less strong than 0.25 microgram of estradiol), a dynamic one on the vagina (50 microgram of tamoxifen make the vagina open in as short a time as 0.25 microgram of estradiol do but the keratinisation is still not completed even with 1 mg of tamoxifen). "( [Action of an antiestrogen agent, tamoxifen on the uterus and vagina of the ovariectomized rat].
Marois, G; Marois, M, 1977
)
1.98
"Tamoxifen (ICI 46,474) has been shown to possess anti-tumour properties in the dimethylbenz(a)anthracene (DMBA)-induced rat mammary carcinoma model. "( Tamoxifen as an anti-tumour agent: effect on oestrogen binding.
Dowse, LJ; Jordan, VC, 1976
)
3.14
"Tamoxifen has been used as a chemotherapeutic agent with no serious side effects noted. "( Tamoxifen retinopathy.
Kaiser-Kupfer, MI; Lippman, ME, 1978
)
3.14
"Tamoxifen has been implicated as a risk factor for venous thrombosis in advanced breast cancer although the evidence for increased arterial or venous thrombosis with tamoxifen in early breast cancer is less clear. "( Haemostatic changes and thromboembolic risk during tamoxifen therapy in normal women.
Ashley, SE; Burman, JF; Chung, HI; Jones, AL; Nicolson, MC; Powles, TJ; Treleaven, JG, 1992
)
1.98
"Tamoxifen has some estrogen-like activities in postmenopausal women and causes a preservation of bone in the lumbar spine and a decrease in circulating cholesterol."( The role of tamoxifen in the treatment and prevention of breast cancer.
Jordan, VC,
)
1.23
"Tamoxifen has no effect on secreted proteins from the AL-1 cells, whereas ICI 164,384 has a complete estrogen antagonistic effect on secreted proteins, indicating that the mechanisms by which estrogens and antiestrogens influence cell proliferation may be via up and down regulation of secreted proteins with growth regulatory functions."( Effect of estrogen and antiestrogens on cell proliferation and synthesis of secreted proteins in the human breast cancer cell line MCF-7 and a tamoxifen resistant variant subline, AL-1.
Lykkesfeldt, AE; Sørensen, EK, 1992
)
1.21
"Tamoxifen has both antiestrogen and estrogen-agonistic activity, which depends on the target tissue involved owing its systemic distribution."( [Cancer of the endometrium caused by antiestrogens].
Dauplat, J; Le Bouëdec, G, 1992
)
1
"Tamoxifen has become the endocrine treatment of choice for all stages of breast cancer. "( The strategic use of antiestrogens to control the development and growth of breast cancer.
Jordan, VC, 1992
)
1.73
"(1) Tamoxifen has an E2 agonistic effect on histologically normal human endometrium. "( Tamoxifen increases plasma estrogen-binding equivalents and has an estradiol agonistic effect on histologically normal premenopausal and postmenopausal endometrium.
Beery, R; Geier, A; Gorodeski, GI; Lunenfeld, B, 1992
)
2.28
"Tamoxifen has antiestrogenic properties and may thus theoretically decrease bone mineral density, particularly after long-term treatment."( Long-term adjuvant tamoxifen in early breast cancer: effect on bone mineral density in postmenopausal women.
Blomqvist, L; Fornander, T; Glas, U; Mattsson, A; Rutqvist, LE; Sjöberg, HE, 1990
)
1.33
"Tamoxifen citrate has recently been shown to be effective palliative therapy in advanced endometrial carcinoma. "( Tamoxifen flare in advanced endometrial carcinoma.
Brooks, BJ; Lippman, ME, 1985
)
3.15
"Tamoxifen also has a potential role in other hormone-sensitive malignancies such as pancreatic carcinoma, and in treatment of benign breast disease."( Tamoxifen. A reappraisal of its pharmacodynamic and pharmacokinetic properties, and therapeutic use.
Buckley, MM; Goa, KL, 1989
)
2.44
"Tamoxifen has become the most commonly used endocrine therapy for advanced breast cancer due to its few side effects and an overall response rate of 35%."( Endocrine management of advanced breast cancer.
Mouridsen, HT; Rose, C, 1989
)
1
"Tamoxifen has a 20-100-fold lower affinity than estradiol for the estrogen receptor."( Effects of tamoxifen and 4-hydroxytamoxifen on the pNR-1 and pNR-2 estrogen-regulated RNAs in human breast cancer cells.
May, FE; Westley, BR, 1987
)
1.38
"Tamoxifen has become the most commonly used endocrine therapy of advanced breast cancer due to its few side effects and an overall response rate of 35%, which has been obtained in randomized trials of tamoxifen compared with either ablative, additive or inhibitive treatment approaches."( Endocrine therapy of advanced breast cancer.
Mouridsen, HT; Rose, C, 1988
)
1
"Tamoxifen has probably been the most widely studied endocrine therapy for breast cancer and the subject of some of the longest and best controlled studies."( Anti-oestrogens in the treatment of breast and gynaecological cancers.
Furr, BJ, 1988
)
1
"Tamoxifen has not been as useful as adjuvant treatment in premenopausal women, for whom combination chemotherapy is the treatment of choice."( Tamoxifen in the treatment of breast cancer.
Legha, SS, 1988
)
2.44
"Tamoxifen has recently been suggested as treatment for endometriosis. "( Endometriosis developing during tamoxifen therapy.
Ford, MR; Soutter, WP; Turner, MJ; Wood, C, 1988
)
2
"Tamoxifen (TAM) has previously been shown to inhibit growth of the Dunning R3327 rat prostate adenocarcinoma and to elevate serum prolactin levels. "( Role of prolactin in modulating the effects of tamoxifen on growth of the Dunning R3327 rat prostate adenocarcinoma.
Ip, MM; Sylvester, PW, 1987
)
1.97
"Tamoxifen (TAM) has a lower affinity to ER compared with one of its main metabolites, 4-OH-TAM."( Antiestrogen binding sites in human breast cancer biopsies. Measurement ligand-specificity and affinity, and correlation to estrogen and progesterone receptors.
Borg, A; Fernö, M,
)
0.85

Actions

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.

ExcerptReferenceRelevance
"Tamoxifen did not enhance vorinostat-induced HIV transcription (between-arm ratio, 0.8; 95% confidence interval [CI], .2-2.4)."( Impact of Tamoxifen on Vorinostat-Induced Human Immunodeficiency Virus Expression in Women on Antiretroviral Therapy: AIDS Clinical Trials Group A5366, The MOXIE Trial.
Aga, E; Archin, N; Bosch, RJ; Chomont, N; Connick, E; Coxen, K; Deeks, S; Dobrowolski, C; Ehui, L; Gandhi, M; Gandhi, RT; Giguel, F; Godfrey, C; Hosey, L; Howell, BJ; Karn, J; Kuritzkes, DR; Ma, Q; Morse, GD; Scully, EP; Sieg, SF; Squires, KE; Starr, K; Tsibris, A; Wu, G, 2022
)
1.85
"Tamoxifen may produce a toxic maculopathy which may progress despite discontinuation of the medication."( Tamoxifen maculopathy: The importance of screening and long follow-up.
Borroni, D; España Contreras, M; Rachwani Anil, R; Rocha-de-Lossada, C; Rodriguez Calvo de Mora, M; Zamorano Martín, F, 2020
)
2.72
"Tamoxifen may cause proliferative effects in the endometrium. "( Asymptomatic Atypical Hyperplasia and Endometriosis Following Treatment with Tamoxifen: A Case Report and Review of the Literature.
Alghamdi, S; Boutross-Tadross, O; Grisdale, M; Luketic, L, 2021
)
2.29
"Tamoxifen may cause hormone disturbance leading to the development of disorders in the pachychoroid spectrum."( Pachychoroid Pigment Epitheliopathy Associated With Tamoxifen.
Arf, S; Ersoz, MG; Hocaoglu, M; Karacorlu, M; Muslubas, IS, 2017
)
1.43
"Tamoxifen plays a critical role in the treatment of hormone receptor-positive breast cancer. "( Lobular breast cancer metastasis to uterus during adjuvant tamoxifen treatment: A case report and review of the literature.
Aytekin, A; Benekli, M; Bilgetekin, I; Ciltas, A; Coskun, U; Ogut, B,
)
1.82
"Tamoxifen acts to inhibit the intracellular action of protein kinase C, which is also an action of well-established treatments such as lithium and valproate."( Tamoxifen for bipolar disorder: Systematic review and meta-analysis.
Palacios, J; Taylor, MJ; Yildiz, A; Young, AH, 2019
)
2.68
"Tamoxifen promotes the survival of FOX-3+ neurons in the injured area and a recovery in the amplitude of electrocorticogram waves."( Tamoxifen favoured the rat sensorial cortex regeneration after a penetrating brain injury.
De la Torre Valdovinos, B; Dueñas Jiménez, JM; Dueñas Jiménez, SH; Franco Rodríguez, NE; Hernández Hernández, L; López Ruiz, JR, 2013
)
2.55
"Tamoxifen therapy may cause hepatic injury."( Protective role of thymoquinone against liver damage induced by tamoxifen in female rats.
Suddek, GM, 2014
)
1.36
"The tamoxifen users had lower risks for overall fractures with hazard ratios (HRs) of 0.52 and 0.59 in the crude and adjusted models (95 % CI = 0.45-0.61 and 0.51-0.69), respectively."( 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
)
2.34
"Tamoxifen was found to increase HER2/neu 1.5-fold to threefold in breast cancer cell lines that were HER2/neu non-amplified."( NK cell-mediated antibody-dependent cellular cytotoxicity is enhanced by tamoxifen in HER2/neu non-amplified, but not HER2/neu-amplified, breast cancer cells.
Albers, AJ; Richards, JO; Smith, TS; Tjoe, JA, 2016
)
1.39
"Tamoxifen seems to inhibit the process of hepatic fibrosis dose-dependently by suppressing the transcription of TGF-beta1 and TGF-beta RI in an experimental model of periportal hepatic fibrosis."( Antifibrogenic effects of tamoxifen in a rat model of periportal hepatic fibrosis.
Chung, YH; Jang, MK; Kim, JA; Lee, HC; Lee, JK; Lee, YS; Park, NH; Ryu, SH; Shin, JW; Suh, DJ, 2009
)
2.1
"Tamoxifen reversed this increase as well as inhibited nuclear translocation of angiogenin."( Angiogenin regulation by estradiol in breast tissue: tamoxifen inhibits angiogenin nuclear translocation and antiangiogenin therapy reduces breast cancer growth in vivo.
Abrahamsson, A; Dabrosin, C; Nilsson, UW, 2010
)
1.33
"Tamoxifen was seen to suppress carrageenan-induced inflammation significantly. "( Role of adrenal gland hormones in the anti-inflammatory effect mechanism of tamoxifen, a partial antagonist for oestrogen receptors, and relation with COX levels.
Alp, HH; Borekci, B; Cadirci, E; Karaca, M; Kumbasar, S; Kumtepe, Y; Salman, S; Suleyman, H; Yildirim, K, 2011
)
2.04
"Tamoxifen did not inhibit cell-free C6-GC synthesis in the P-gp/off or P-gp/on homogenates."( Expression of P-glycoprotein in HeLa cells confers resistance to ceramide cytotoxicity.
Cabot, MC; Chapman, JV; Gouazé-Andersson, V, 2010
)
1.08
"Tamoxifen effects to increase uterine weight, decrease serum IGF-I, increase pituitary prolactin, and increase bone mineral density could be fully blocked by fulvestrant, indicating mediation by ERα/ERβ."( Tamoxifen regulation of bone growth and endocrine function in the ovariectomized rat: discrimination of responses involving estrogen receptor α/estrogen receptor β, G protein-coupled estrogen receptor, or estrogen-related receptor γ using fulvestrant (ICI
Fitts, JM; Klein, RM; Powers, CA, 2011
)
2.53
"Tamoxifen may increase diabetes incidence through its estrogen-inhibiting effects."( Association between tamoxifen treatment and diabetes: a population-based study.
Anderson, GM; Austin, P; Fischer, HD; Gruneir, A; Lipscombe, LL; Paszat, L; Rochon, PA; Yun, L, 2012
)
1.42
"Tamoxifen may increase the risk of microvascular flap complications. "( Tamoxifen increases the risk of microvascular flap complications in patients undergoing microvascular breast reconstruction.
Kelley, BP; Kronowitz, SJ; Valero, V; Yi, M, 2012
)
3.26
"Tamoxifen was able to blunt the rise in Gh mRNA in response to estradiol in females."( Sexual dimorphism of growth hormone in the hypothalamus: regulation by estradiol.
Addison, ML; Rissman, EF, 2012
)
1.1
"Tamoxifen could inhibit the contraction of fibroblast-populated collagen lattices, indicating that tamoxifen may have potential effect on abnormal scar contraction in vivo."( [The inhibitory effect of tamoxifen on human dermal fibroblast-populated collagen lattices].
Chen, B; George, WC; Hu, D; Margaret, AH; Xu, M; Zhu, X, 2002
)
2.06
"Tamoxifen may cause malignant transformation of endometriosis through atypical endometriosis even in the postmenopausal state. "( Ovarian endometrioid adenocarcinoma arising from an endometriotic cyst in a postmenopausal woman under tamoxifen therapy for breast cancer: a case report.
Hirakawa, T; Kaku, T; Nakano, H; Ogawa, S; Okugawa, K, 2002
)
1.97
"Tamoxifen actually activate the AP-1 transcription factor."( Possible interaction between activator protein-1 and proto-oncogene B-cell lymphoma gene 6 in breast cancer patients resistant to tamoxifen.
Altundag, K; Altundag, O; Arun, B; Gunduz, M, 2004
)
1.25
"Tamoxifen alone did not increase urogenital tumors or affect arsenic-induced neoplasia but did increase arsenic-induced uroepithelial proliferative lesions."( Urogenital carcinogenesis in female CD1 mice induced by in utero arsenic exposure is exacerbated by postnatal diethylstilbestrol treatment.
Diwan, BA; Liu, J; Powell, DA; Waalkes, MP; Ward, JM, 2006
)
1.06
"Tamoxifen may enhance risk for other neoplasias, especially endometrial cancer."( The role of flavin-containing monooxygenase (FMO) in the metabolism of tamoxifen and other tertiary amines.
Hines, RN; Krueger, SK; Vandyke, JE; Williams, DE, 2006
)
1.29
"Tamoxifen may increase mortality in women at the lower end of the "high-risk" range for breast cancer. "( Chemoprevention: drug pricing and mortality: the case of tamoxifen.
Barnato, A; Birch, S; Helms, LJ; Kuenneth, C; Kuppermann, M; Melnikow, J; Nuovo, J, 2006
)
2.02
"Tamoxifen did not inhibit oestrogen-induced polysome aggregation."( Tamoxifen-induced changes in the polyribosomes and associated mRNA of rat uterus.
Knowler, JT; Wakeling, AE; Waters, AP, 1983
)
2.43
"Tamoxifen produced a slower rise in nuclear estrogen receptor levels and never reached the levels achieved by estradiol or monohydroxytamoxifen."( Modulation of rat uterine steroid hormone receptors by estrogen and antiestrogen.
Dix, CJ; Jordan, VC, 1980
)
0.98
"The tamoxifen-induced increase in IGFBP-1 plasma levels may be an important mechanism modulating IGF-I action at the tissue level."( Plasma insulin-like growth factor I and its binding proteins 1 and 3 in postmenopausal patients with breast cancer receiving long term tamoxifen.
Knip, M; Laatikainen, TJ; Lahti, EI, 1994
)
1.05
"Tamoxifen plays a major role in the management of breast cancer in women and is currently used to a lesser extent in other neoplasias. "( Tamoxifen inhibition of ocular melanoma cell attachment to matrix proteins.
MacNeil, S; Rennie, IG; Wagner, M, 1994
)
3.17
"Tamoxifen is known to inhibit the growth of some human mammary carcinoma cells; this effect is accompanied by a decrease in the proportion of cells synthesizing DNA. "( Cell cycle kinetic effects of tamoxifen on human breast cancer cells. Flow cytometric analyses of DNA content, BrdU labeling, Ki-67, PCNA, and statin expression.
Danova, M; Gibelli, N; Giordano, M; Mangiarotti, R; Mazzini, G; Pellicciari, C; Riccardi, A; Wang, E; Zibera, C, 1993
)
2.02
"Tamoxifen is known to lower serum cholesterol levels, and the findings reported here indicate that the drug might also protect heart cell membranes against peroxidative damage."( Tamoxifen inhibits lipid peroxidation in cardiac microsomes. Comparison with liver microsomes and potential relevance to the cardiovascular benefits associated with cancer prevention and treatment by tamoxifen.
Arnstein, HR; Cannon, M; Halliwell, B; Wiseman, H, 1993
)
2.45
"Tamoxifen was found to inhibit the proliferation of three of five leiomyoma-derived cell lines (ELT cell lines) in vitro, including an estrogen receptor-negative cell line."( Presence of an insulin-like growth factor I autocrine loop predicts uterine fibroid responsiveness to tamoxifen.
Ethier, SP; Howe, SR; Matthews, WJ; Pass, HI; Walker, C, 1996
)
1.23
"Tamoxifen can produce a sonographic image of the endometrium that resembles endometrial neoplasia. "( Ultrasonographic appearance of endometrium in postmenopausal breast cancer patients receiving tamoxifen.
Arvas, M; Beşe, N; Beşe, T; Demirkiran, F; Kösebay, D; Mandel, N, 1996
)
1.96
"Tamoxifen may cause tumor stimulation due to deregulation of [Ca2+]i or its consequences such as activity of protein kinase C, calmodulin and related protein kinases."( Tamoxifen induces deregulation of [Ca2+] in human breast cancer cells.
Jain, PT; Trump, BF,
)
2.3
"Tamoxifen did not increase necrosis (which significantly decreased in treated tumours once they had regressed (p < 0.01)."( Tamoxifen induced apoptosis in ZR-75 breast cancer xenografts antedates tumour regression.
Anderson, TJ; Cameron, DA; Langdon, S; Miller, WR; Ritchie, AA, 1997
)
2.46
"Thus tamoxifen is shown to cause an oestrogen-reversible decrease of es nucleoside transporters in MCF-7 cells."( Reduction of equilibrative nitrobenzylthioinosine-sensitive nucleoside transporter in tamoxifen-treated MCF-7 cells: an oestrogen-reversible phenomenon.
Goh, LB; Lee, CW, 1997
)
0.98
"Tamoxifen also did not inhibit GH trends to increase tibia bone mineral density."( Comparison of tamoxifen effects on the actions of triiodothyronine or growth hormone in the ovariectomized-hypothyroid rat.
Fitts, JM; Klein, RM; Powers, CA, 1998
)
1.38
"Tamoxifen may, however, cause adverse effects at the uterine level."( Tamoxifen-induced uterine abnormalities: the role of imaging.
Ascher, SM; Imaoka, I; Lage, JM, 2000
)
2.47
"Tamoxifen caused an increase in %ED-FMD maximal at 28 days in the CAD group (2.1+/-0.3% to 7.5+/-0.7%; P<0.0001) and the NCA group (3.8+/-0.4% to 7.9+/-1.0%; P<0.0001), with no significant change in the untreated group."( Tamoxifen effects on endothelial function and cardiovascular risk factors in men with advanced atherosclerosis.
Clarke, SC; Grace, AA; Kirschenlohr, HL; Metcalfe, JC; Schofield, PM, 2001
)
2.47
"Tamoxifen alone did not produce side effects."( Effect of endocrine treatment on sexuality in premenopausal breast cancer patients: a prospective randomized study.
Berglund, G; Bolund, C; Nystedt, M; Rutquist, LE; Sjödén, PO, 2001
)
1.03
"2. Tamoxifen was found to inhibit this in vitro-induced change."( Tamoxifen inhibition of an in vitro oestradiol-induced surface coat change on mouse blastocysts.
Bloxham, PA; Pugh, DM, 1977
)
2.21
"Tamoxifen did not enhance the toxicity of vinblastine."( High-dose oral tamoxifen, a potential multidrug-resistance-reversal agent: phase I trial in combination with vinblastine.
Ellis, PG; Fine, RL; Jordan, VC; Panella, TJ; Rogers, MP; Schold, SC; Smith, DC; Trump, DL; Winer, EP, 1992
)
1.36
"The Tamoxifen did not produce any significant change in the metabolic clearance rate, the plasma concentration or the calculated blood production rate of testosterone."( Effects of tamoxifen on testosterone metabolism in postmenopausal women with breast cancer.
Bird, CE; Clark, AF; Masters, V; Sterns, EE, 1985
)
1.14
"Tamoxifen does not inhibit the Ca2+- and phospholipid-independent phosphorylation of protamine sulfate by protein kinase C, indicating that the drug does not interact with the active site of the enzyme."( Inhibition of protein kinase C by tamoxifen.
Liskamp, RM; O'Brian, CA; Solomon, DH; Weinstein, IB, 1985
)
1.27
"Tamoxifen did not cause tumor growth."( Estradiol-stimulated growth of MCF-7 tumors implanted in athymic mice: a model to study the tumoristatic action of tamoxifen.
Gottardis, MM; Jordan, VC; Robinson, SP, 1988
)
1.21
"Tamoxifen citrate did cause regression of the breasts."( Virginal hypertrophy.
Pernoll, ML; Ryan, RF, 1985
)
0.99
"Tamoxifen (TAM) has a lower affinity to ER compared with one of its main metabolites, 4-OH-TAM."( Antiestrogen binding sites in human breast cancer biopsies. Measurement ligand-specificity and affinity, and correlation to estrogen and progesterone receptors.
Borg, A; Fernö, M,
)
0.85

Treatment

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.

ExcerptReferenceRelevance
"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."( Untargeted Metabolomics of Breast Cancer Cells MCF-7 and SkBr3 Treated With Tamoxifen/Trastuzumab.
Al-Hroub, HM; Almehdi, A; Alniss, H; El-Awady, R; Giddey, AD; Mousa, M; Semreen, MH; Sharaf, BM; Soares, NC,
)
1.8
"Tamoxifen-treated, but not aromatase-treated patients had a poor survival when BCL3 scores were high."( BCL3 expression is strongly associated with the occurrence of breast cancer relapse under tamoxifen treatment in a retrospective cohort study.
Cornelius, M; Czapiewski, P; Dittmer, A; Dittmer, J; Hartig, R; Haybaeck, J; Ignatov, A; Kalinski, T; Nass, N, 2022
)
1.66
"Tamoxifen treatment may induce dysregulation of estrogen homeostasis, leading to the occurrence of related adverse reactions. "( The inhibition of tamoxifen on UGT2B gene expression and enzyme activity in rat liver contribute to the estrogen homeostasis dysregulation.
Hao, Z; He, S; Liu, Z; Wang, Z; Xu, J; Yin, X; Zhang, B; Zhao, H; Zhou, W; Zhou, X, 2022
)
2.5
"Tamoxifen-treated patients can develop mild and transient thyroid dysfunction within the first 12 months, yet further significant changes in thyroid function beyond one year of tamoxifen treatment have been reported in a single study. "( Influence of the anti-oestrogens tamoxifen and letrozole on thyroid function in women with early and advanced breast cancer: A systematic review.
Andersson, M; Buch-Larsen, K; Gillberg, L; Marina, D; Rasmussen, ÅK; Schwarz, P, 2023
)
2.63
"tamoxifen vs. no added treatment affects hormonal composition and size of stimulated ovarian follicles."( Hormone concentrations of dominant follicles in the TALES randomized controlled trial comparing letrozole with tamoxifen.
Abel, MK; Juarez-Hernandez, F; Letourneau, JM; Mok-Lin, E; Rosen, MP; Wang, A, 2022
)
1.65
"Tamoxifen treatment."( Risk of Endometrial Polyps, Hyperplasia, Carcinoma, and Uterine Cancer After Tamoxifen Treatment in Premenopausal Women With Breast Cancer.
Jeong, HG; Kim, MS; Kim, T; Lee, JY; Nam, S; Park, H; Ryu, KJ, 2022
)
2.39
"Tamoxifen treatment ameliorated high glucose-induced MMT of HPMCs, improved ultrafiltration rate, and decreased PSTR of mouse peritoneum."( Tamoxifen exerts anti-peritoneal fibrosis effects by inhibiting H19-activated VEGFA transcription.
Guo, Z; Lai, X; Li, S; Liu, L; Lu, H; Sun, Z; Yuan, JH; Zhao, T, 2023
)
3.07
"Tamoxifen treatment significantly facilitated functional restoration of working memory impairment in mice after white matter injury, thus indicating a translational potential for this estrogen receptor modulator given its clinical safety and applicability for WMLs, which lack of currently available treatments."( Tamoxifen promotes white matter recovery and cognitive functions in male mice after chronic hypoperfusion.
Chen, Y; Fang, Y; Huang, Q; Pan, D; Tian, H; Tian, Y; Wan, Y; Wang, W; Xie, M, 2019
)
2.68
"Tamoxifen treatment increased the weight of the uterus and the level of UCA1, while decreasing the expression of miR‑144."( Metformin alleviates endometrial hyperplasia through the UCA1/miR‑144/TGF‑β1/AKT signaling pathway.
Guo, M; Huang, W; Zhou, JJ, 2020
)
1.28
"Tamoxifen- treated patients with recurrence or non-recurrence were selected using a matched case-control design."( Evaluation of SPP1/osteopontin expression as predictor of recurrence in tamoxifen treated breast cancer.
Andersson, G; Göthlin Eremo, A; Lagergren, K; Montgomery, S; Othman, L; Tina, E, 2020
)
1.51
"Tamoxifen treatment was associated with improved DFS for MBC patients."( Survival benefit of tamoxifen in male breast cancer: prospective cohort analysis.
Brucker, C; Costa, SD; Eggemann, H; Flock, F; Ignatov, A; Reinisch, M; Schrauder, M; Thill, M, 2020
)
2.32
"Tamoxifen-treated mice were compared to corn oil (vehicle)-treated mice."( Effects of tamoxifen on tendon homeostasis and healing: Considerations for the use of tamoxifen-inducible mouse models.
Ackerman, JE; Awad, HA; Best, KT; Cobb, J; Knapp, E; Loiselle, AE; Myers, M; Nichols, AEC; Studentsova, V, 2021
)
1.73
"Tamoxifen treatment causes down-regulation, mutation, or loss in estrogen receptors."( COVID-19 infection can cause chemotherapy resistance development in patients with breast cancer and tamoxifen may cause susceptibility to COVID-19 infection.
Cumhur Cure, M; Cure, E; Kadiyoran, C; Vatansev, H, 2020
)
1.5
"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
)
2.79
"Tamoxifen treatment median duration was 1.4 years IQR[0.4-3.2]."( Tamoxifen. A treatment for meningioma?
Champeaux-Depond, C; Weller, J, 2021
)
2.79
"Tamoxifen treatment is associated with decreased relapse rate (RR = 0.70, p value < 0.001); however, it did not effect on HER2 positive ones (RR = 1, p value = 0.99)."( Evaluating human epidermal growth factor receptor 2 roles in the efficacy of Tamoxifen treatment in breast cancer, a systematic review.
Farahmand, L; Ghahremanlou, M; Majidzadeh-A, K; Mansouri, S; Mokhtari-Hesari, P; Moradi-Kalbolandi, S; Naghavi-Al-Hosseini, F; Seyednejad, SA, 2021
)
1.57
"Tamoxifen-treated patients retained motor and respiratory function, compared with a significant deterioration of age-matched historical control patients receiving corticosteroids only."( Safety and clinical outcome of tamoxifen in Duchenne muscular dystrophy.
Avrahami, R; Ben-Sasson, S; Dor, T; Eliav, O; Lavi, E; Simchovitz, E; Tsabari, R, 2021
)
1.63
"Tamoxifen treatment was applied to corroborate the estrogenic effect."( Estrogen induces CXCR4 overexpression and CXCR4/CXL12 pathway activation in lung adenocarcinoma cells in vitro.
Cerbón Cervantes, MA; Ignacio, GS; Rodriguez-Lara, V, 2017
)
1.18
"Tamoxifen treatment inhibited the CXCR4 overexpression observed in estrogen-treated groups, demonstrating that estrogen strongly influences CXCR4 expression in lung adenocarcinoma cells."( Estrogen induces CXCR4 overexpression and CXCR4/CXL12 pathway activation in lung adenocarcinoma cells in vitro.
Cerbón Cervantes, MA; Ignacio, GS; Rodriguez-Lara, V, 2017
)
1.18
"Tamoxifen treatment in breast cancer patients is associated with increased risk of endometrial malignancies. "( Tamoxifen-Dependent Induction of AGR2 Is Associated with Increased Aggressiveness of Endometrial Cancer Cells.
Bouchal, P; Durech, M; Faktor, J; Hrstka, R; Nenutil, R; Obacz, J; Podhorec, J; Skoupilova, H; Sommerova, L; Vojtesek, B, 2017
)
3.34
"Tamoxifen treatment was associated with elevated incidence of carcinosarcoma among women with uterine sarcoma, but was not found to be associated with prognosis or with co-morbidities."( High Incidence of Carcinosarcoma among Patients Previously Treated with Tamoxifen.
Arnon, E; Auslender, R; Gemer, O; Goldberg, Y; Kaldawy, A; Lavie, O; Segev, Y; Siegler, E, 2017
)
2.13
"In tamoxifen-treated patients, DKK-1 levels were reduced by 35% (p < 0.01) one year after surgery but remained unaltered in patients treated with aromatase inhibitors."( Adjuvant tamoxifen but not aromatase inhibitor therapy decreases serum levels of the Wnt inhibitor dickkopf-1 while not affecting sclerostin in breast cancer patients.
Browne, AJ; Göbel, A; Hofbauer, LC; Kuhlmann, JD; Link, T; Rachner, TD; Rauner, M; Wimberger, P, 2017
)
1.39
"Tamoxifen-treated, 70-gene low- and high-risk patients had 20-year BCSS of 90 and 83%, as compared to 80 and 65% for untreated patients, respectively (log-rank p < 0.0001). "( Tamoxifen therapy benefit for patients with 70-gene signature high and low risk.
Benz, CC; Esserman, LJ; Fornander, T; Lindström, LS; Nordenskjöld, B; Stål, O; van 't Veer, LJ; Yau, C; Yu, NY, 2017
)
3.34
"Tamoxifen treatment does not seem to accentuate structural changes in patients with MacTel type 2. "( Potential Effects of Hormone Therapy in Type 2 Idiopathic Macular Telangiectasia.
Bird, AC; Chew, EY; Clemons, TE; Leung, I; Peto, T; Sallo, FB; Wolf-Schnurrbusch, UEK, 2018
)
1.92
"Tamoxifen-pretreated inguinal fat showed beige fat features, with smaller adipocyte size, up-regulated uncoupling protein 1 expression, and improved vascularization. "( Tamoxifen-Prefabricated Beige Adipose Tissue Improves Fat Graft Survival in Mice.
Cai, J; Li, B; Liao, Y; Liu, K; Lu, F; Wang, J; Zhang, Y, 2018
)
3.37
"Tamoxifen treatment before fat grafting resulted in prefabricated vascularized beige fat with small adipocytes, which greatly improve fat graft survival. "( Tamoxifen-Prefabricated Beige Adipose Tissue Improves Fat Graft Survival in Mice.
Cai, J; Li, B; Liao, Y; Liu, K; Lu, F; Wang, J; Zhang, Y, 2018
)
3.37
"Tamoxifen treatment of estrogen receptor (ER)-positive breast cancer reduces mortality by 31%. "( Association of tamoxifen resistance and lipid reprogramming in breast cancer.
Hultsch, S; Ikonen, E; Kallioniemi, O; Kangaspeska, S; Kankainen, M; Kovanen, RM; Paavolainen, L; Pietiäinen, V, 2018
)
2.28
"Tamoxifen treatment ameliorated UUO-induced renal fibrosis as shown by decreased expression of α-smooth muscle actin (SMA), fibronectin and connective tissue growth factor (CTGF). "( Tamoxifen ameliorates obstructive nephropathy through Src and the PI3K/Akt/mTOR pathway.
Bae, EH; Choi, JS; Kim, CS; Kim, IJ; Kim, SW; Ma, SK, 2019
)
3.4
"Tamoxifen treatment greatly reduces a woman's risk of developing a second primary breast cancer. "( CYP2D6 phenotype, tamoxifen, and risk of contralateral breast cancer in the WECARE Study.
Bernstein, JL; Bernstein, L; Brooks, JD; Comen, EA; Doody, DR; John, EM; Knight, JA; Leong, SF; Liang, X; Lynch, CF; Malone, KE; Mellemkjær, L; Orlow, I; Reiner, AS; Woods, M, 2018
)
2.26
"Tamoxifen treatment is important assistant for estrogen-receptor-positive breast cancer (BRCA) after resection. "( Tamoxifen therapy benefit predictive signature combining with prognostic signature in surgical-only ER-positive breast cancer.
Jin, WH; Lv, F; Sun, AJ; Wang, ZR; Zhang, XL, 2019
)
3.4
"Tamoxifen treatment of ER-positive cells inhibited ERα and LINC00472 expression and increased p65 and IκBα phosphorylation."( ERα upregulates the expression of long non-coding RNA LINC00472 which suppresses the phosphorylation of NF-κB in breast cancer.
Biglia, N; Chu, WM; Deng, X; Fei, P; Fu, Y; Jia, W; Katsaros, D; Lin, H; Loo, L; Ni, Y; Qian, B; Shen, Y; Wang, Z; Yu, H; Yu, X, 2019
)
1.24
"Upon tamoxifen treatment, reporter protein mEGFP was observed in the junctional zone (JZ) and chorionic plate (CP)."( The platelet-derived growth factor receptor alpha promoter-directed expression of cre recombinase in mouse placenta.
Lee, S; Natale, DRC; Qiao, L; Shao, J; Wattez, JS, 2019
)
0.97
"Tamoxifen-treated patients with ER+ tumors (n = 310) who consumed two or more cups/day had significantly decreased risk for early events compared to patients with low consumption, adjusted HR 0.40 (0.19-0.83)."( Coffee prevents early events in tamoxifen-treated breast cancer patients and modulates hormone receptor status.
Henningson, M; Hjertberg, M; Ingvar, C; Jernström, H; Rose, C; Simonsson, M; Söderlind, V, 2013
)
1.39
"Tamoxifen treatment is associated with a reduction in mammographic density and an improved survival. "( Mammographic density reduction is a prognostic marker of response to adjuvant tamoxifen therapy in postmenopausal patients with breast cancer.
Czene, K; Edgren, G; Eriksson, L; Hall, P; Humphreys, K; Li, J, 2013
)
2.06
"Tamoxifen-treatment preserved the fibrinolytic capacity of MCs treated with TGF-β1 and decreased their migration capacity."( Tamoxifen ameliorates peritoneal membrane damage by blocking mesothelial to mesenchymal transition in peritoneal dialysis.
Aguilera, AI; Bajo, MA; del Peso, G; Fernández-Millara, V; Gónzalez-Mateo, G; Guerra-Azcona, G; López-Cabrera, M; Loureiro, J; Sánchez-Tomero, JA; Sandoval, P; Santamaria, B; Selgas, R, 2013
)
2.55
"Tamoxifen treatment induced efficient recombination of PTHrP-floxed alleles and decreased PTHrP expression in vascular and visceral smooth muscle cells of PTHrPSM-/- mice."( Knockdown of parathyroid hormone related protein in smooth muscle cells alters renal hemodynamics but not blood pressure.
Barthelmebs, M; Chambon, P; Coquard, C; Helwig, JJ; Hochane, M; Karaplis, AC; Massfelder, T; Metzger, D; Moulin, B; Raison, D; Steger, J, 2013
)
1.11
"In tamoxifen-treated patients Low-MKS/Low-ERS cancers had continuously increasing risk of relapse that was higher after 5 years than Low-MKS/High-ERS cancers [0 to 10 year, HR 3.36; p = 0.013]."( Proliferation and estrogen signaling can distinguish patients at risk for early versus late relapse among estrogen receptor positive breast cancers.
Becker, S; Bianchini, G; Del Conte, G; Fasolo, A; Gianni, L; Haibe-Kains, B; Holtrich, U; Iwamoto, T; Karn, T; Kelly, C; Müller, V; Pusztai, L; Qi, Y; Rody, A; Santarpia, L; Schmidt, S; Sotiriou, C; Symmans, WF; Zambetti, M, 2013
)
0.9
"In tamoxifen-treated breast cancer patients the occurrence of hot flashes may be associated with effective estrogen receptor antagonism dependent on genetic variations of metabolic enzymes and the estrogen receptor. "( CYP2D6 genotype in relation to hot flashes as tamoxifen side effect in a Dutch cohort of the tamoxifen exemestane adjuvant multinational (TEAM) trial.
Berns, EM; Dezentjé, VO; Gelderblom, H; Guchelaar, HJ; Kranenbarg, EM; Nortier, JW; Putter, H; Seynaeve, C; Van de Velde, CJ; Van der Straaten, T; Van Schaik, RH; Vletter-Bogaartz, JM; Wessels, JA, 2014
)
1.28
"Tamoxifen treatment increased aromatase promoter activity through an enhanced recruitment of c-fos/c-jun complex to AP-1 responsive elements located within the promoter region."( Tamoxifen through GPER upregulates aromatase expression: a novel mechanism sustaining tamoxifen-resistant breast cancer cell growth.
Andò, S; Barone, I; Bonofiglio, D; Catalano, S; Chemi, F; Fuqua, SA; Giordano, C; Lanzino, M; Maggiolini, M; Panza, S; Rizza, P; Romeo, F, 2014
)
2.57
"Tamoxifen treatment of the first cancer has been associated with a reduction in the risk of a subsequent contralateral cancer."( Duration of tamoxifen use and the risk of contralateral breast cancer in BRCA1 and BRCA2 mutation carriers.
Ainsworth, P; Demsky, R; Eisen, A; Eng, C; Foulkes, WD; Gilchrist, DM; Ginsburg, O; Gronwald, J; Huzarski, T; Kim-Sing, C; Lubinski, J; Lynch, HT; Manoukian, S; Moller, P; Narod, SA; Neuhausen, SL; Olopade, O; Robidoux, A; Saal, H; Senter, L; Singer, CF; Sun, P; Tung, N; Weitzel, J, 2014
)
1.5
"Tamoxifen treatment was continued for 14 days after UUO operation."( Tamoxifen ameliorates renal tubulointerstitial fibrosis by modulation of estrogen receptor α-mediated transforming growth factor-β1/Smad signaling pathway.
Jung, YJ; Kang, KP; Kim, D; Kim, W; Lee, AS; Lee, S; Park, SK; Yang, KH, 2014
)
2.57
"Tamoxifen treatment significantly decreased UUO-induced renal tubular injury and fibrosis."( Tamoxifen ameliorates renal tubulointerstitial fibrosis by modulation of estrogen receptor α-mediated transforming growth factor-β1/Smad signaling pathway.
Jung, YJ; Kang, KP; Kim, D; Kim, W; Lee, AS; Lee, S; Park, SK; Yang, KH, 2014
)
2.57
"In tamoxifen-treated cases, ERK1/2 expression was an independent prognostic marker of longer survival."( ERK1/2 is related to oestrogen receptor and predicts outcome in hormone-treated breast cancer.
Abduljabbar, R; Alabdullah, M; Alkaabi, M; Ellis, IO; Green, AR; Jerjees, DA; Muftah, A; Nolan, C; Rakha, EA, 2014
)
0.92
"Tamoxifen treatment after and/or before induction of silicosis decreased lung fibrosis score with blood TGF-β levels. "( Tamoxifen citrate: a glimmer of hope for silicosis.
Akbiyik, F; Akin, T; Alici, IO; Bilgin, BC; Karaca, N; Karaca, T; Simsek, GG; Uzdogan, A; Yilmaz, OH; Yoldas, O; Yoldas, S, 2015
)
3.3
"Tamoxifen treatment in these mice strongly reduced connexin 40 mRNA and protein expression in the kidneys."( Inducible deletion of connexin 40 in adult mice causes hypertension and disrupts pressure control of renin secretion.
Gerl, M; Kurt, B; Kurtz, A; van Veen, TA; Vöckl, J; Wagner, C, 2015
)
1.14
"In tamoxifen-treated patients, tumours with high PKD1 mRNA levels (n = 77, 50.66%) were significantly associated with less metastasis-free survival than tumours with low PKD1 mRNA expression (n = 75, 49.34%; P = 0.031)."( Protein kinase D1 regulates ERα-positive breast cancer cell growth response to 17β-estradiol and contributes to poor prognosis in patients.
Auclair, C; Bièche, I; Karam, M; Legay, C; Ricort, JM; Vacher, S, 2014
)
0.92
"Tamoxifen treatment of high MD tissue in SCID mice led to a decrease in stromal (p = 0.009), and an increase in adipose (p = 0.023) percent areas, compared to placebo-treated mice."( Effects of Tamoxifen and oestrogen on histology and radiographic density in high and low mammographic density human breast tissues maintained in murine tissue engineering chambers.
Blick, T; Britt, K; Cawson, J; Chew, GL; Frazer, H; Haviv, I; Henderson, MA; Hill, P; Hopper, JL; Huang, D; Huo, CW; Southey, MC; Thompson, EW, 2014
)
1.51
"With tamoxifen treatment (n=6) (68)Ga-AMBA uptake plateaued after 1week and decreased after 2weeks, with a significant reduction compared to controls (n=4)."( (68)Ga-AMBA and (18)F-FDG for preclinical PET imaging of breast cancer: effect of tamoxifen treatment on tracer uptake by tumor.
Cagnolini, A; Gruaz-Guyon, A; Lantry, LE; Montravers, F; Nataf, V; Nunn, AD; Prignon, A; Provost, C; Talbot, JN, 2015
)
1.1
"Tamoxifen is a major treatment modality for estrogen receptor positive breast cancer, but the occurrence of resistance remains a problem. "( Synergy of leptin/STAT3 with HER2 receptor induces tamoxifen resistance in breast cancer cells through regulation of apoptosis-related genes.
Dubos, S; Palianopoulou, M; Papanikolaou, V; Papathanasiou, I; Stefanou, N; Tsezou, A; Valiakou, V, 2015
)
2.11
"Tamoxifen treatment and radiotherapy improve both local tumor control and patient survival."( Altered radiation responses of breast cancer cells resistant to hormonal therapy.
Kovalchuk, O; Luzhna, L; Lykkesfeldt, AE, 2015
)
1.14
"In tamoxifen-treated patients, breast cancer recurrence differs according to CYP2D6 genotype and endoxifen steady-state concentrations (Endx Css). "( Evaluation of CYP2D6 enzyme activity using a 13C-dextromethorphan breath test in women receiving adjuvant tamoxifen.
Ames, MM; Black, JL; Buhrow, SA; Gilbert, JA; Goetz, MP; Ingle, JN; Kosel, ML; Modak, AS; Northfelt, DW; Reid, JM; Rosen, D; Safgren, SL; Suman, VJ, 2015
)
1.25
"Tamoxifen-treated SMMHC-Cre(ERT2)/Myocd(F/F) conditional mutant mice die within 6 mo of Myocd gene deletion, exhibiting profound derangements in the structure of great arteries as well as the gastrointestinal and genitourinary tracts."( Myocardin is required for maintenance of vascular and visceral smooth muscle homeostasis during postnatal development.
Huang, J; Li, L; Parmacek, MS; Small, A; Wang, T; Wright, AC; Yang, J; Zhou, S, 2015
)
1.14
"Tamoxifen treatment significantly accelerated Twist1 degradation in multiple cell lines including HEK293 human kidney cells, 4T1 and 168FARN mouse mammary tumor cells with either ectopically or endogenously expressed Twist1."( Tamoxifen inhibits ER-negative breast cancer cell invasion and metastasis by accelerating Twist1 degradation.
He, J; Lonard, DM; Ma, G; Martinez, J; Xu, J; Xu, Y; Yu, X; Yu, Y, 2015
)
2.58
"Tamoxifen treatment coupled with miR-21 inhibition could therefore be an effective strategy for the treatment of malignant gliomas."( Tamoxifen-Induced Cell Death of Malignant Glioma Cells Is Brought About by Oxidative-Stress-Mediated Alterations in the Expression of BCL2 Family Members and Is Enhanced on miR-21 Inhibition.
Harmalkar, M; Kazi, S; Shirsat, NV; Upraity, S, 2015
)
2.58
"Tamoxifen is the treatment of choice in estrogen receptor alpha breast cancer patients that are eligible for adjuvant endocrine therapy. "( Tamoxifen induces a pluripotency signature in breast cancer cells and human tumors.
Alexakis, K; Askoxilakis, J; Castanas, E; Kampa, M; Laliotis, A; Notas, G; Pelekanou, V; Sfakianakis, S; Tsapis, A; Tsentelierou, E; Tzardi, M, 2015
)
3.3
"Tamoxifen treatment effects on body composition, energy homeostasis, parameters of AT biology, glucose and lipid metabolism were investigated up to an age of 18 weeks."( Tamoxifen affects glucose and lipid metabolism parameters, causes browning of subcutaneous adipose tissue and transient body composition changes in C57BL/6NTac mice.
Berger, C; Blüher, M; Gericke, M; Hesselbarth, N; Klöting, N; Kunath, A; Pettinelli, C; Stumvoll, M, 2015
)
2.58
"Tamoxifen, used for treatment and chemoprevention of breast cancer, is converted to 4-hydroxy-tamoxifen and other metabolites by cytochrome P450 (CYP) enzymes. "( Does purified Swedish pollen extract, a nonhormonal treatment for vasomotor symptoms, inhibit the CYP2D6 enzyme system?
Druckmann, R; Espié, M; Goldstein, SR, 2015
)
1.86
"Thus tamoxifen treatment could potentially effect pubertal bone development."( The effect of tamoxifen on pubertal bone development in adolescents with pubertal gynecomastia.
Akgül, S; Derman, O; Kanbur, N, 2016
)
1.25
"For tamoxifen- treated patients, no statistically significant difference in rate of recurrence observed between CYP2D6 metabolic variants in stage 3 and post-menopausal patients."( CYP2D6 Genotype and Risk of Recurrence in Tamoxifen Treated Breast Cancer Patients.
Gholi-Nataj, M; Nazari, T; Neamatzadeh, H; Rafieian, S; Sheikhha, MH; Yazdi, MF, 2015
)
1.16
"Tamoxifen treatment reduced FeCl2-induced brain edema in male mice."( Effects of Gender and Estrogen Receptors on Iron-Induced Brain Edema Formation.
Hua, Y; Keep, RF; Xi, G; Xie, Q, 2016
)
1.16
"Tamoxifen treatment decreased BALF neutrophil counts (65.3 ± 19.38% before treatment; 7.6 ± 4.5% 2 days post-treatment,; and 13.6 ± 9.3% 5 days post-treatment). "( Tamoxifen as a new therapeutic tool for neutrophilic lung inflammation.
Folch, H; Galesio, JS; Henriquez, C; Morales, N; Morán, G; Perez, B; Sarmiento, J; Uberti, B, 2016
)
3.32
"Tamoxifen treatment in horses with induced acute pulmonary inflammation promoted early apoptosis of blood and BALF neutrophils, reduction in BALF neutrophils and improvement in the animals' clinical status."( Tamoxifen as a new therapeutic tool for neutrophilic lung inflammation.
Folch, H; Galesio, JS; Henriquez, C; Morales, N; Morán, G; Perez, B; Sarmiento, J; Uberti, B, 2016
)
3.32
"Tamoxifen treatment reduced ovarian weight independently from effects on antral follicle populations, as there was no difference in visible antral follicle numbers on the day of collection."( Prepubertal tamoxifen treatment affects development of heifer reproductive tissues and related signaling pathways.
Akers, RM; Al Naib, A; Bartol, FF; Keisler, DH; Rhoads, ML; Rhoads, RP; Tucker, HLM; Xie, G, 2016
)
1.53
"Tamoxifen treatment repressed the expression of cyclins by MPM cells, resulting in cell-cycle arrest and caspase-3-coupled apoptosis signaling."( Tamoxifen Suppresses the Growth of Malignant Pleural Mesothelioma Cells.
Dahlan, IM; Harvey, BJ; Jennings, CJ; Kay, EW; Thomas, W; Zainal, N, 2016
)
2.6
"Tamoxifen treatment produced a rapid and near complete loss of Foxd3 mRNA and protein."( Regulation of embryonic stem cell self-renewal and pluripotency by Foxd3.
Labosky, PA; Liu, Y, 2008
)
1.07
"Tamoxifen treatment significantly reduced methylation at Igf2-H19 ICR in epididymal sperm. "( Effect of tamoxifen treatment on global and insulin-like growth factor 2-H19 locus-specific DNA methylation in rat spermatozoa and its association with embryo loss.
Balasinor, N; D'Souza, R; Gill-Sharma, M; Kedia-Mokashi, N; Maitra, A; Parte, P; Pathak, S; Saxena, M, 2009
)
2.2
"Tamoxifen treatment reduced the induction of major histocompatibility complex II by lipopolysaccharide stimulated dendritic cells and decreased their ability to activate myelin specific T-cells."( Treatment with selective estrogen receptor modulators regulates myelin specific T-cells and suppresses experimental autoimmune encephalomyelitis.
Bebo, BF; Dehghani, B; Foster, S; Kurniawan, A; Lopez, FJ; Sherman, LS, 2009
)
1.07
"Tamoxifen treatment resulted in a 0.5% increase from baseline in BMD at the spine, which was maintained at 12 months."( Effects of exemestane and tamoxifen on bone health within the Tamoxifen Exemestane Adjuvant Multicentre (TEAM) trial: results of a German, 12-month, prospective, randomised substudy.
Dornoff, W; Hadji, P; Hasenburg, A; Kieback, DG; Kuck, J; Melchert, F; Menschik, T; Tessen, HW; Ziller, M, 2009
)
1.37
"Tamoxifen treatment primarily induces cytostasis (growth arrest) and the surviving breast cancer cells commonly acquire tamoxifen resistance."( Autophagy facilitates the progression of ERalpha-positive breast cancer cells to antiestrogen resistance.
Barrett, JT; Jackson, WH; Periyasamy-Thandavan, S; Samaddar, JS; Schoenlein, PV, 2009
)
1.07
"When tamoxifen-treated patients were selected, an absence of stromal Cav-1 was a strong predictor of poor clinical outcome, suggestive of tamoxifen resistance."( An absence of stromal caveolin-1 expression predicts early tumor recurrence and poor clinical outcome in human breast cancers.
Brody, JR; Dasgupta, A; Kleer, CG; Lisanti, MP; Mercier, I; Pestell, RG; Sabel, M; Sotgia, F; Witkiewicz, AK, 2009
)
0.81
"Tamoxifen-treated women (n=297) were genotyped for CYP2D6 variants and assigned a 'score' based on predicted allele activities from 0 (no activity) to 2 (high activity)."( Cytochrome P450 2D6 activity predicts discontinuation of tamoxifen therapy in breast cancer patients.
Desta, Z; Flockhart, DA; Hayes, DF; Henry, NL; Kim, S; Li, L; Nguyen, AT; Oesterreich, S; Rae, JM; Sikora, MJ; Skaar, TC; Stearns, V; Storniolo, AM, 2009
)
1.32
"Tamoxifen treatment of HER-2/neu transgenic mice combined to anti-HER-2/neu cell vaccine did not hamper the efficacy of cancer immunoprevention, and caused a significantly increased production of interferon-gamma."( Tamoxifen combined to anti-HER-2/neu cell vaccine does not hamper cancer immunopreventive efficacy.
Antognoli, A; Croci, S; De Giovanni, C; Grosso, V; Ianzano, ML; Iezzi, M; Landuzzi, L; Lollini, PL; Murgo, A; Musiani, P; Nanni, P; Nicoletti, G; Palladini, A; Stivani, V, 2009
)
2.52
"Tamoxifen treatment for breast cancer does not appear to increase the risk of ovarian cancer in BRCA1 mutation carriers."( Tamoxifen and the risk of ovarian cancer in BRCA1 mutation carriers.
Domchek, S; Isaacs, C; Kauff, ND; Lubinski, J; Lynch, HT; Narod, SA; Rosen, B; Sun, P; Tung, N; Vicus, D, 2009
)
3.24
"Tamoxifen treatment significantly increased RFS in patients with estrogen receptor-positive/progesterone receptor-positive (ER(+)/PR(+)) tumors with low EPOR expression (P = 0.001) but had no effect on RFS in patients with tumors with high EPOR expression (P = 0.98)."( Erythropoietin receptor expression and correlation to tamoxifen response and prognosis in breast cancer.
Fredlund, E; Jirström, K; Landberg, G; Larsson, AM; Nilsson, S; Påhlman, S; Rydén, L, 2009
)
1.32
"Tamoxifen, an effective treatment of breast cancer, has been shown to cause ocular toxic effects. "( Retinal function in patients treated with tamoxifen.
Berezovsky, A; Gebrim, LH; Motono, M; Pereira, JM; Sacai, PY; Sallum, JM; Salomão, SR; Watanabe, SE, 2010
)
2.07
"Tamoxifen treatment induced cell death in the hippocampus formation of the prenatal and postnatal rat. "( Effects of tamoxifen on morphological and ultrastructural aspects of developing hippocampus of rat.
Kordestani Shargh, B; Najafzadeh, N; Nobakht, M, 2009
)
2.19
"In tamoxifen-treated patients, LRR was significantly associated with RS risk groups (P < .001). "( Association between the 21-gene recurrence score assay and risk of locoregional recurrence in node-negative, estrogen receptor-positive breast cancer: results from NSABP B-14 and NSABP B-20.
Costantino, JP; Fisher, B; Geyer, CE; Mamounas, EP; Paik, S; Shak, S; Tang, G; Watson, D; Wickerham, DL; Wolmark, N, 2010
)
0.98
"Upon tamoxifen treatment, these mice showed genomic recombination in the tissues where endogenous Sall1 is expressed."( A mouse line expressing Sall1-driven inducible Cre recombinase in the kidney mesenchyme.
Fujimura, S; Inoue, M; Inoue, S; Nishinakamura, R, 2010
)
0.82
"Tamoxifen treatments may be associated with an increased rate of PD; however these effects act after four years, are of limited duration, and the adverse effect is overwhelmed by the protection against breast recurrence conferred by tamoxifen therapy."( Risk of Parkinson's disease after tamoxifen treatment.
Destefano, AL; Dybdahl, M; Lash, TL; Latourelle, JC; Myers, RH, 2010
)
1.36
"Tamoxifen treatment in EPS patients is associated with lower mortality and shows a trend to an increased multivariate-adjusted survival. "( Tamoxifen is associated with lower mortality of encapsulating peritoneal sclerosis: results of the Dutch Multicentre EPS Study.
Betjes, MG; Fieren, MW; Korte, MR; Lingsma, HF; Sampimon, DE; Weimar, W, 2011
)
3.25
"Tamoxifen-treated patients with estrogen receptor-positive tumors expressing none or low levels of HOXB13 had a clear benefit from tamoxifen in terms of longer distant recurrence-free survival (DRFS) (hazard ratio = 0.38, 95% confidence interval = 0.23 to 0.60, P = 0.000048). "( Predictive relevance of HOXB13 protein expression for tamoxifen benefit in breast cancer.
Fornander, T; Jansson, A; Jerevall, PL; Nordenskjöld, B; Skoog, L; Stål, O, 2010
)
2.05
"Tamoxifen treatment induced almost complete recombination in white adipose tissue of the AdipoqCreER(T)² mouse line (97%-99%), while no recombination was seen in vehicle-treated animals."( Tamoxifen-inducible Cre-mediated recombination in adipocytes.
Offermanns, S; Sassmann, A; Wettschureck, N, 2010
)
2.52
"In tamoxifen treated patients, there was weak evidence that the poor-metaboliser variant, CYP2D6*6 (MAF = 0.01), was associated with decreased BCSS (P = 0.02; HR = 1.95; 95% CI = 1.12-3.40). "( CYP2D6 gene variants: association with breast cancer specific survival in a cohort of breast cancer patients from the United Kingdom treated with adjuvant tamoxifen.
Abraham, JE; Baynes, C; Caldas, C; Driver, KE; Dunning, AM; Earl, HM; Greenberg, D; Ingle, S; Kalmyrzaev, B; Luccarini, C; Maranian, MJ; Pharoah, PD; Platte, R; Shah, M, 2010
)
1.18
"In tamoxifen-treated animals, the mean infarct volume reduction was 40% (p < 0.05) and the mean CSS was significantly less than vehicle-treated animals (p < 0.001)."( Tamoxifen as an effective neuroprotectant in an endovascular canine model of stroke.
Boulos, AS; Dalfino, JC; Deshaies, EM; Drazin, D; Feustel, PJ; Popp, AJ, 2011
)
2.33
"Tamoxifen treatment of MDA-435 breast cancer cells enhanced the CD44(+) /CD176(+) phenotype."( Expression of CD176 (Thomsen-Friedenreich antigen) on lung, breast and liver cancer-initiating cells.
Cao, Y; Cheng, RC; Goletz, S; Karsten, U; Lin, WM, 2011
)
1.09
"In tamoxifen-treated cohorts, the 23 gene ER expression signature predicted clinical outcome (HR = 2.20, P = 0.00035)."( Minimising immunohistochemical false negative ER classification using a complementary 23 gene expression signature of ER status.
Eklund, AC; Haibe-Kains, B; Juul, N; Li, Q; Richardson, AL; Swanton, C; Szallasi, Z; Workman, CT, 2010
)
0.87
"Tamoxifen treatment (vs no treatment) saved 29 QALYs in a population of 1000 postmenopausal women aged <55 years with an additional cost of $333,000 over the population's lifetime (average cost-effectiveness ratio, $11,530 per QALY). "( Cost-effectiveness of chemoprevention of breast cancer using tamoxifen in a postmenopausal US population.
Alperin, P; Dinh, TA; Green, LE; Noah-Vanhoucke, J; Smith, RA, 2011
)
2.05
"Tamoxifen used in the treatment of breast cancer is reported to cause hepatic steatosis. "( Incidence and risk factors for non-alcoholic steatohepatitis in females treated with tamoxifen for breast cancer.
Akhondi-Meybodi, M; Hashemian, Z; Moaiedi, M; Mortazavy-Zadah, MR, 2011
)
2.04
"The tamoxifen-treated mice developed a severe peripheral neuropathy that was associated with dramatic alterations in peripheral nerve structure and function."( Sox10 is required for Schwann-cell homeostasis and myelin maintenance in the adult peripheral nerve.
Bremer, M; Fröb, F; Kichko, T; Reeh, P; Suter, U; Tamm, ER; Wegner, M, 2011
)
0.85
"Tamoxifen (Tam) treatment is a first-line endocrine therapy for estrogen receptor-α-positive breast cancer patients. "( Farnesoid X receptor inhibits tamoxifen-resistant MCF-7 breast cancer cell growth through downregulation of HER2 expression.
Andò, S; Barone, I; Bonofiglio, D; Catalano, S; Fuqua, SA; Gelsomino, L; Giordano, C; Panza, S; Rizza, P; Vizza, D, 2011
)
2.1
"Tamoxifen treatment for 6 months did not result in a significantly greater concentration of E2 or in any of the other analytes in DLF of pre- or postmenopausal women."( Breast ductal lavage for assessment of breast cancer biomarkers.
Bryk, M; Chatterton, RT; Habe-Evans, M; Khan, SA; Parker, NP; Scholtens, DM, 2010
)
1.08
"Tamoxifen treatment strongly reduced the production of the T."( A helminth cestode parasite express an estrogen-binding protein resembling a classic nuclear estrogen receptor.
Ambrosio, JR; Escobedo, G; Fonseca-Liñán, R; García-Varela, M; Hernández, ME; Hernández-Bello, R; Ibarra-Coronado, EG; Jesús Ramses, CR; Morales-Montor, J; Nava-Castro, K; Ortega-Pierres, G; Pavón, L; Reynoso-Ducoing, O,
)
0.85
"Tamoxifen treatment of FAK(loxP/loxP)//γGT-Cre-ER(T2) mice caused renal-specific fak recombination (FAK(ΔloxP/ΔloxP)) and reduction of FAK expression in proximal tubules."( Focal adhesion kinase signaling mediates acute renal injury induced by ischemia/reperfusion.
Alderliesten, MC; Bonventre, JV; de Graauw, M; de Heer, E; Ichimura, T; Pennekamp, P; Price, LS; Qin, Y; Stokman, G; van de Water, B, 2011
)
1.09
"Tamoxifen treatment resulted in increases from baseline in SHBG and PTH-intact, whereas levels of testosterone and FSH decreased and DHEAS levels did not change."( Effects of exemestane and tamoxifen on hormone levels within the Tamoxifen Exemestane Adjuvant Multicentre (TEAM) trial: results of a German substudy.
Bauer, T; Hadji, P; Hasenburg, A; Kauka, A; Kieback, DG; Tams, J, 2012
)
1.4
"In tamoxifen treatment of idiopathic oligozoospermia, NNT was 3.9, and in antioxidant supplementation, it was 7.8."( Comparing the effectiveness of infertility treatments by numbers needed to treat (NNT).
Comhaire, F; Decleer, W, 2012
)
0.89
"Tamoxifen-treated xenografts also had reduced levels of IGF1R, and dalotuzumab did not enhance the effect of tamoxifen."( Acquired resistance to tamoxifen is associated with loss of the type I insulin-like growth factor receptor: implications for breast cancer treatment.
Fagan, DH; Sachdev, D; Uselman, RR; Yee, D, 2012
)
1.41
"Tamoxifen-treated breast cancer patients were included in this prospective study between February 2009 and June 2010. "( Evaluation of endometrium by transvaginal ultrasonography and Doppler in tamoxifen-treated women with breast cancer.
Baloglu, A; Bezircioglu, I; Oziz, E; Tarhan, MO; Yigit, S, 2012
)
2.05
"Tamoxifen treatment both in vivo and in vitro results in efficient recombination of loci marked by LoxP sites."( Generation of CD4CreER(T²) transgenic mice to study development of peripheral CD4-T-cells.
Aghajani, K; Gounari, F; Keerthivasan, S; Yu, Y, 2012
)
1.1
"Tamoxifen-treated patients reported significantly more dyspareunia (31.3%; P < 0.05) but resembled controls in all other concerns."( Sexual dysfunction in women on adjuvant endocrine therapy after breast cancer.
Baumgart, J; Evers, AS; Kallak, TK; Nilsson, K; Poromaa, IS, 2013
)
1.11
"Tamoxifen treatment was initiated for SEP after surgery."( Sclerosing encapsulating peritonitis after living donor liver transplantation: a case successfully treated with tamoxifen: report of a case.
Asonuma, K; Inomata, Y; Lee, KJ; Narita, Y; Takeichi, T; Yamamoto, H, 2013
)
1.32
"Tamoxifen pretreatment also significantly upregulated MxA expression in Imiquimod-treated PBMCs (P = 0.0011**), an effect not ascribed to ER blocking nor to an upregulation in TLR7 expression because Tamoxifen showed no potentiating effect on the expression of the receptor."( Tamoxifen alleviates hepatitis C virus-induced inhibition of both toll-like receptor 7 and JAK-STAT signalling pathways in PBMCs of infected Egyptian females.
Abdelaziz, AI; Ahmed, R; Esmat, G; Fawzy, IO; Hamdi, N; Negm, M, 2012
)
2.54
"Oral tamoxifen treatment from 3 weeks of age for 15 months at a dose of 10 mg/kg/day stabilized myofiber membranes, normalized whole body force, and increased force production and resistance to repeated contractions of the triceps muscle above normal values."( The anticancer drug tamoxifen counteracts the pathology in a mouse model of duchenne muscular dystrophy.
Comyn, SA; Dahmane, E; Décosterd, LA; Dorchies, OM; Gayi, E; Handa, RJ; Ismail, HM; Patthey- Vuadens, O; Petermann, O; Piacenza, T; Reutenauer-Patte, J; Ruegg, UT, 2013
)
1.17
"Tamoxifen treatment to the fry (yolk sac absorbed stage) of Oreochromis niloticus in the dose of 200 microg l(-1) for 60 days produced 90% males and 1% intersex population."( Effect of a non steroidal tamoxifen on the gonad and sex differentiation in Nile tilapia, Oreochromis niloticus.
Singh, AK; Singh, R; Tripathi, M, 2012
)
1.4
"Tamoxifen treatment did not alter phosphodiesterase activity."( Estrogen receptor, calcium mobilization and rat sperm motility.
Balasinor, N; Choudhary, J; Juneja, HS; Saberwal, GS; Sharma, MK, 2002
)
1.04
"A tamoxifen or raloxifene treatment of 2 weeks increased uterine weights by 35 and 15%, respectively, but significantly less than estradiol treatment."( Estrogenic properties of raloxifene, but not tamoxifen, on D2 and D3 dopamine receptors in the rat forebrain.
Di Paolo, T; Landry, M; Lévesque, D, 2002
)
1.13
"Tamoxifen treatment was started."( Solitary esophageal metastasis of breast cancer after 11 years: a case report.
Aydingöz, U; Ayhan, A; Erman, M; Güler, N; Karaoğlu, A; Oksüzoğlu, B, 2002
)
1.04
"Tamoxifen treatment significantly reduced autoantibody production directed against either NE or DNA. "( Beneficial effects of the anti-oestrogen tamoxifen on systemic lupus erythematosus of (NZBxNZW)F1 female mice are associated with specific reduction of IgG3 autoantibodies.
Mozes, E; Sthoeger, ZM; Zinger, H, 2003
)
2.03
"Tamoxifen treatment has also been associated with improvement of retroperitoneal fibrosis and desmoid tumors, conditions also associated with abnormal fibroblast proliferation."( Open label trial of tamoxifen in scleroderma.
Fessler, BJ; Hoffman, GS; Thomas-Golbanov, CK; Wilke, WS,
)
1.18
"Tamoxifen treatment reduced recurrence, and recurrent tumors had higher PKC activity."( Estrogen-dependent rapid activation of protein kinase C in estrogen receptor-positive MCF-7 breast cancer cells and estrogen receptor-negative HCC38 cells is membrane-mediated and inhibited by tamoxifen.
Boyan, BD; Dean, DD; Dietl, J; Frambach, T; Lohmann, CH; Schwartz, Z; Sylvia, VL, 2003
)
1.23
"Tamoxifen treatment produced a transient but significant increase in circulating gonadotropins, at Day 90 of treatment schedule, corresponding to 60 days of treatment."( Effect of oral tamoxifen on semen characteristics and serum hormone profile in male bonnet monkeys.
Aleem, M; Balasinor, N; Choudhuri, J; D'Souza, S; Gill-Sharma, MK; Juneja, HS; Majramkar, DD; Parte, P, 2003
)
1.39
"Tamoxifen treatment was associated with pathological response in 15 of 24 (63%) tumours."( Pathological features of breast cancer response following neoadjuvant treatment with either letrozole or tamoxifen.
Anderson, TJ; Cameron, D; Dixon, JM; Macfarlane, L; Miller, WR, 2003
)
1.25
"Tamoxifen treated animals had fewer complications of skin wound healing than controls (4.5% vs. "( Neoadjuvant antiangiogenic therapy with tamoxifen does not impair gastrointestinal anastomotic repair in the rat.
Bouchier-Hayes, DJ; Kay, E; McNamara, DA; Walsh, TN, 2003
)
2.03
"Tamoxifen treatment did not alter the protein profile in the cauda sperms, epididymal fluid and tissues."( Effect of tamoxifen treatment on motility related proteins in rat spermatozoa.
Balasinor, N; Choudhary, J; Gill-Sharma, MK; Juneja, HS; Sethi-Saberwal, G, 2003
)
1.44
"Tamoxifen treatment of precocious puberty in MAS results in a reduction of vaginal bleeding and significant improvements in growth velocity and rate of skeletal maturation."( Tamoxifen treatment for precocious puberty in McCune-Albright syndrome: a multicenter trial.
Eugster, EA; Jou, HC; Pescovitz, OH; Plourde, P; Reiter, EO; Rubin, SD, 2003
)
3.2
"Tamoxifen treatment significantly increased rhodamine 123 fluorescent dye uptake by sperm mitochondria, reflecting an altered mitochondrial membrane potential."( Tamoxifen, protein kinase C and rat sperm mitochondria.
Balasinor, N; Choudhary, J; Gill-Sharma, MK; Juneja, HS; Padwal, V; Saberwal, GS, 2003
)
2.48
"In tamoxifen-treated women, sonohysterography provides a significant improvement in sensitivity for diagnosis of endometrial polyps compared with endometrial biopsy."( Sonohysterography compared with endometrial biopsy for evaluation of the endometrium in tamoxifen-treated women.
Bach, AM; Barakat, R; Choi, PH; Gonen, M; Hann, LE; Kim, CM, 2003
)
1.16
"More tamoxifen-treated (21.9%; 7/32) rats had irregular cycling than did control (9%; 3/23) rats. "( Estrous cycle and ovarian changes in a rat mammary carcinogenesis model after irradiation, tamoxifen chemoprevention, and aging.
Christian, A; Dicello, JF; Eyabi, PO; Huso, DL; Karim, BO; Khan, KA; Landolfi, JA; Mann, JF; McAlonis, M; Qiu, W; Ricart-Arbona, R, 2003
)
1.05
"Tamoxifen treatment is relatively non-toxic, may be beneficial and we think it should be considered for pubertal gynecomastia."( Tamoxifen treatment for pubertal gynecomastia.
Derman, O; Kanbur, NO; Kutluk, T,
)
2.3
"Tamoxifen pre-treatment reduced brain weight loss from 21.5+/-4.0% in vehicle pups (n=27) to 2.6+/-2.5% in the treated pups (n=22, P<0.05)."( Treatment with tamoxifen reduces hypoxic-ischemic brain injury in neonatal rats.
Feng, Y; Fratkins, JD; LeBlanc, MH, 2004
)
1.4
"With tamoxifen treatment, ER alpha remained in the nucleus, but ER beta was lost."( Estrogen receptors ER alpha and ER beta in proliferation in the rodent mammary gland.
Cheng, G; Gustafsson, JA; Warner, M; Weihua, Z, 2004
)
0.78
"Tamoxifen treatment additionally increased the level of vascular endothelial growth factor."( PC cell-derived growth factor mediates tamoxifen resistance and promotes tumor growth of human breast cancer cells.
Hayashi, J; Serrero, G; Tangkeangsirisin, W, 2004
)
1.31
"Tamoxifen treatment was associated with reduction in breast density, most of which occurred during the first 18 months of treatment."( Tamoxifen and breast density in women at increased risk of breast cancer.
Cuzick, J; Duffy, SW; Pinney, E; Warren, RM; Warwick, J, 2004
)
3.21
"Tamoxifen treatment slows the progression of atherosclerosis in postmenopausal women with breast cancer as assessed by changes in carotid IMT. "( Tamoxifen improves endothelial function and reduces carotid intima-media thickness in postmenopausal women.
Aznaouridis, K; Kumar, S; Lekakis, JP; Papaioannou, TG; Papamichael, CM; Poulakaki, NA; Protogerou, AD; Stamatelopoulos, KS; Stamatelopoulos, SF; Venetsanou, K, 2004
)
3.21
"Tamoxifen treatment led to increased bone mineral density (BMD) and hyperplastic uteri."( Effects of the antiestrogen tamoxifen and the aromatase inhibitor letrozole on serum hormones and bone characteristics in a preclinical tumor model for breast cancer.
Barrett, JC; Berrigan, D; Brodie, A; Hursting, SD; Jelovac, D; Macedo, L; Núñez, NP; Perkins, SN, 2004
)
1.34
"Tamoxifen treatment inhibited breast cancer cell growth and increased BMD but caused uterine hypertrophy in this preclinical model of postmenopausal breast cancer. "( Effects of the antiestrogen tamoxifen and the aromatase inhibitor letrozole on serum hormones and bone characteristics in a preclinical tumor model for breast cancer.
Barrett, JC; Berrigan, D; Brodie, A; Hursting, SD; Jelovac, D; Macedo, L; Núñez, NP; Perkins, SN, 2004
)
2.06
"Tamoxifen treatment substantially improves the 10-year survival of women with estrogen-receptor (ER)-alpha-positive tumors. "( Reduced PTEN expression predicts relapse in patients with breast carcinoma treated by tamoxifen.
Bickis, MG; Chibbar, R; Klassen, S; McFadden, A; Shoman, N; Torlakovic, E, 2005
)
1.99
"Tamoxifen-treated animals showed increases in measures of anxiety, compared with ERT-treated animals, suggesting that this SERM may be anxiogenic."( Tamoxifen fails to affect central serotonergic tone but increases indices of anxiety in female rhesus macaques.
Felger, J; Graves, F; Mook, D; Wallen, K; Wilson, ME, 2005
)
2.49
"Tamoxifen treatment by itself significantly delayed weight loss (an endpoint of neurodegeneration) in male and female mice compared to untreated controls."( Tamoxifen and vitamin E treatments delay symptoms in the mouse model of Niemann-Pick C.
Bascuñan-Castillo, EC; Erickson, RP; Gillies, RJ; Heidenreich, RH; Hicks, C; Howison, CM; Hunter, RJ; Trouard, TP, 2004
)
2.49
"Tamoxifen-treated rats showed a significant reduction of body weight gain, food intake, adipose tissue weight and leptin concentration (p < 0.001). "( Plasma leptin concentration in tamoxifen-treated ovariectomized rats.
Hakamata, Y; Hozumi, Y; Nagai, H, 2005
)
2.06
"Tamoxifen treatment of Bcl-2-overexpressing clones was found to result in activation of c-Jun N-terminal kinase (JNK) and p38 kinase."( Activated JNK brings about accelerated apoptosis of Bcl-2-overexpressing C6 glioma cells on treatment with tamoxifen.
Moodbidri, MS; Shirsat, NV, 2005
)
1.26
"Tamoxifen treatment significantly increased RFS in patients with hormone receptor-positive (oestrogen receptor-positive (ER+) and/or progesterone receptor-positive (PR+)) tumours (Relative Risk (RR) 0.65; 95% Confidence Interval (CI): 0.48-0.89, P=0.006), and the beneficial effect of tamoxifen was extended to patients with indicators of poor prognosis, such as young age and nodal-positivity."( Two years of adjuvant tamoxifen in premenopausal patients with breast cancer: a randomised, controlled trial with long-term follow-up.
Chebil, G; Dufmats, M; Fernö, M; Jirström, K; Jönsson, PE; Källström, AC; Landberg, G; Nordenskjöld, B; Rydén, L; Stål, O; Thorstenson, S, 2005
)
1.36
"The tamoxifen-treated group's aortas had a five-fold increase in catalase mRNA expression (P = .02) on day 7 and an eight-fold increase in catalase protein on day 14 (P = .04)."( Tamoxifen up-regulates catalase production, inhibits vessel wall neutrophil infiltration, and attenuates development of experimental abdominal aortic aneurysms.
Ailawadi, G; Cho, BS; Deatrick, KB; Eagleton, MJ; Grigoryants, V; Hannawa, KK; Henke, PK; Pearce, CG; Roelofs, KJ; Sinha, I; Stanley, JC; Upchurch, GR; Woodrum, DT, 2005
)
2.25
"In tamoxifen-treated mice fed the soy meal, casein, or high-dose isoflavone enriched diets, the majority (>80%) showed no tumor formation by 60 weeks of age."( Low-dose dietary phytoestrogen abrogates tamoxifen-associated mammary tumor prevention.
Alvarez, K; Edgerton, S; Kim, A; Liu, B; Liu, N; Mason, T; McKimmey, C; Ordonez-Ercan, D; Thor, A; Yang, X, 2005
)
1.11
"Tamoxifen treatment of breast cancer is associated with an increased risk of endometrial cancer, but tamoxifen-related risks of endometrial cancer are unclear in premenopausal women, in long-term users of tamoxifen, and in women for whom several years have passed since ending treatment. "( Tamoxifen treatment for breast cancer and risk of endometrial cancer: a case-control study.
Jones, ME; Swerdlow, AJ, 2005
)
3.21
"Tamoxifen treatment for breast cancer does not appear to increase or decrease MI risk, although radiation therapy appears to increase MI risk."( Myocardial infarction risk and tamoxifen therapy for breast cancer.
Bernstein, L; Chen, W; Geiger, AM, 2005
)
1.34
"Tamoxifen treatment yielded polymerase-blocking DNA adducts at multiple nucleotide positions along the cII transgene."( Investigating DNA adduct-targeted mutagenicity of tamoxifen: preferential formation of tamoxifen-DNA adducts in the human p53 gene in SV40 immortalized hepatocytes but not endometrial carcinoma cells.
Besaratinia, A; Pfeifer, GP, 2005
)
1.3
"Tamoxifen-treated patients with UGT2B15 high activity genotypes had increased risk of recurrence and poorer survival."( Association of genetic variation in tamoxifen-metabolizing enzymes with overall survival and recurrence of disease in breast cancer patients.
Ahn, J; Ambrosone, CB; Kadlubar, FF; MacLeod, SL; Nowell, SA; Rae, JM; Scheys, JO; Sweeney, C; Trovato, A, 2005
)
1.32
"Tamoxifen treatment is effective in resolving the mass and compression in Riedel's thyroiditis."( A case of Riedel's thyroiditis treated with tamoxifen: another successful outcome.
Jung, YJ; Muehlenbein, SJ; Rhodes, R; Rich, FA; Schaub, CR,
)
1.84
"Tamoxifen-treated rats had significantly improved neurobehavioral deficit scores when evaluated daily throughout the 1 week or 2 week periods and showed significantly reduced median infarct volumes measured after 1 week and 2 weeks."( Behavioral and histological neuroprotection by tamoxifen after reversible focal cerebral ischemia.
Behr, MJ; Feustel, PJ; Jin, Y; Kimelberg, HK; Morrison, JP; Zhang, Y, 2005
)
1.31
"Tamoxifen treatment results in a doubling of the risk of endometrial cancer after 1-2 years of treatment and a quadrupling after 5 years. "( The ATAC ('Arimidex', Tamoxifen, Alone or in Combination) adjuvant breast cancer trial: first results of the endometrial sub-protocol following 2 years of treatment.
Bianco, AR; Clack, G; Coibion, M; Duffy, S; Jackson, TL; Lansdown, M; Philips, K; Pollard, S; Wells, M, 2006
)
2.09
"Tamoxifen treatment for breast cancer increases proliferation of the endometrium, resulting in an enhanced prevalence of endometrial pathologies, including endometrial cancer. "( Tamoxifen treatment for breast cancer enforces a distinct gene-expression profile on the human endometrium: an exploratory study.
Blok, LJ; Burger, CW; Ewing, PC; Gielen, SC; Kühne, LC, 2005
)
3.21
"In tamoxifen-treated patients, women with the CYP2D6 *4/*4 genotype tend to have a higher risk of disease relapse and a lower incidence of hot flashes, which is consistent with our previous observation that CYP2D6 is responsible for the metabolic activation of tamoxifen to endoxifen."( Pharmacogenetics of tamoxifen biotransformation is associated with clinical outcomes of efficacy and hot flashes.
Ames, MM; Couch, FJ; Desta, Z; Flockhart, DA; Goetz, MP; Ingle, JN; Lingle, WL; Perez, EA; Rae, JM; Reynolds, C; Safgren, SL; Suman, VJ; Visscher, DW, 2005
)
1.27
"The tamoxifen treatment effect could be studied in subgroups of breast cancer and pure prognostic information could be scrutinized for untreated control patients."( Hypoxia inducible factor-1alpha is a prognostic marker in premenopausal patients with intermediate to highly differentiated breast cancer but not a predictive marker for tamoxifen response.
Jirström, K; Kronblad, A; Landberg, G; Nordenskjöld, B; Rydén, L, 2006
)
1.01
"Tamoxifen treatment and menopausal status correlated significantly with the changes in lumbar spine BMD (P < .0001). "( Tamoxifen treatment after adjuvant chemotherapy has opposite effects on bone mineral density in premenopausal patients depending on menstrual status.
Blomqvist, C; Elomaa, I; Saarto, T; Vehmanen, L, 2006
)
3.22
"Tamoxifen treatment significantly improved the mitochondrial respiratory function and enhanced superoxide-scavenging activity of mitochondria."( Tamoxifen protects against acute tumor necrosis factor alpha-induced cardiac injury via improving mitochondrial functions.
Chaiswing, L; Lien, YC; Lin, SM; Mattson, MP; Oberley, TD; St Clair, D; Wang, LM; Yen, HC; Zhao, Y, 2006
)
2.5
"The tamoxifen-treated TG mouse hearts also exhibited better functional recovery from ex vivo I/R, as well as significantly reduced necrosis and apoptosis."( Endoplasmic reticulum stress gene induction and protection from ischemia/reperfusion injury in the hearts of transgenic mice with a tamoxifen-regulated form of ATF6.
Fernandez, R; Glembotski, CC; Gude, N; Martindale, JJ; Sussman, MA; Thuerauf, D; Whittaker, R, 2006
)
1.02
"Tamoxifen treatment was associated with a decrease in ERalpha, but an increase was the most frequent change (17 out of 33) in ERbeta, and no consistent change was evident in staining of the ERbeta2/betacx variant."( Oestrogen receptor beta and neoadjuvant therapy with tamoxifen: prediction of response and effects of treatment.
Anderson, TJ; Dixon, JM; Miller, WR; Saunders, PT, 2006
)
1.3
"Tamoxifen treatment allows MerCreMer fusion recombinase to localize to the nucleus where MerCreMer can excise a floxed inhibitory DNA segment, thereby activating the expression of a downstream gene. "( Floxed reporter genes: Flow-cytometric selection of clonable cells expressing high levels of a target gene after tamoxifen-regulated Cre-loxP recombination.
Schreiber, H; Spiotto, MT, 2006
)
1.99
"Tamoxifen treatment of Lpl(flox/flox) mice did not cause a significant increase in triglyceride levels."( Acute lipoprotein lipase deletion in adult mice leads to dyslipidemia and cardiac dysfunction.
Goldberg, IJ; Homma, S; Molkentin, JD; Noh, HL; Okajima, K, 2006
)
1.06
"In tamoxifen-treated patients, endometrial cytology was reliable for detection of endometrial pathology, and was well accepted by the patients."( Endometrial brush cytology in the surveillance of post-menopausal patients under tamoxifen: a prospective longitudinal study.
Annane, K; Bellocq, JP; Brettes, JP; Mathelin, C; Walter, P; Youssef, C, 2007
)
1.19
"Tamoxifen-treated rats had significantly improved neurobehavioral deficit scores after 24 h and showed approximately 75% reduced infarct volumes."( Neuroprotection by tamoxifen in focal cerebral ischemia is not mediated by an agonist action at estrogen receptors but is associated with antioxidant activity.
Aschner, M; Feustel, PJ; Kimelberg, HK; Milatovic, D; Zhang, Y, 2007
)
1.39
"Tamoxifen treatment significantly decreased sperm concentration and motility in seminal and epididymal sperm. "( Effect of tamoxifen treatment on the semen quality and fertility of the male rat.
Motrich, RD; Ponce, AA; Rivero, VE, 2007
)
2.18
"Tamoxifen treatment significantly altered sperm quality in seminal and epididymal sperm. "( Effect of tamoxifen treatment on the semen quality and fertility of the male rat.
Motrich, RD; Ponce, AA; Rivero, VE, 2007
)
2.18
"Tamoxifen treatment was stopped at 10-(7/12) years, and growth velocity and skeletal maturation rate returned to normal."( Tamoxifen treatment in a patient with blepharophimosis-ptosis-epicanthus inversus syndrome and peripheral precocious puberty.
Carrascosa, A; González-Niño, C; Yeste, D, 2007
)
2.5
"Tamoxifen treatment has a potential to stimulate the cell proliferation of endometrial glands and corpus luteum in tamoxifen-treated rats."( Immunohistochemical evaluation of cell proliferation and apoptosis markers in ovaries and uterus of tamoxifen-treated rats.
Akman, L; Cirpan, T; Kanit, L; Terek, MC; Ulukus, EC; Ulukus, M,
)
1.07
"Tamoxifen treatment was accompanied by an uncoupling of the regulation of PRA and PRB expression without effect on ER expression."( Effect of tamoxifen on endometrial histology, hormone receptors, and cervical cytology: a prospective study with follow-up.
Leslie, KK; Singh, M; Stephens, JK; Thompson, C; Torkko, K; Walter, SA, 2007
)
1.46
"Tamoxifen-treated patients carrying the CYP2D6 alleles *4, *5, *10, *41-all associated with impaired formation of antiestrogenic metabolites-had significantly more recurrences of breast cancer, shorter relapse-free periods (hazard ratio [HR], 2.24; 95% CI, 1.16 to 4.33; P = .02), and worse event-free survival rates (HR, 1.89; 95% CI, 1.10 to 3.25; P = .02) compared with carriers of functional alleles. "( Breast cancer treatment outcome with adjuvant tamoxifen relative to patient CYP2D6 and CYP2C19 genotypes.
Antoniadou, L; Brauch, H; Eichelbaum, M; Fritz, P; Muerdter, T; Schroth, W; Schwab, M; Simon, W; Zanger, UM, 2007
)
2.04
"Tamoxifen treatment of estrogen-dependent breast cancer ultimately loses its effectiveness due to the development of resistance. "( Fibroblast growth factor receptor 4 predicts failure on tamoxifen therapy in patients with recurrent breast cancer.
Dorssers, LC; Foekens, JA; Look, MP; Meijer, D; Sieuwerts, AM; van Agthoven, T, 2008
)
2.03
"tamoxifen treatment modified 17-beta estradiol production in females, whereas serum testosterone was not affected."( Tamoxifen treatment induces protection in murine cysticercosis.
De León-Nava, MA; Escobedo, G; Larralde, C; Morales-Montor, J; Vargas-Villavicencio, JA, 2007
)
2.5
"In tamoxifen-treated patients, women with the CYP2D6 *10 T/T genotype have a lower 4OHtam level in the serum and a worse clinical outcome."( Association between CYP2D6 *10 genotype and survival of breast cancer patients receiving tamoxifen treatment.
Fan, T; Fan, Z; He, L; Li, J; Li, P; Lin, B; Ouyang, T; Shi, L; Sun, Y; Wang, T; Wu, Y; Xie, Y; Xu, Y; Yao, L, 2008
)
1.19
"Tamoxifen treatment of wild-type islets did not affect their cell survival, Preproinsulin gene expression, and glucose stimulus-secretion coupling."( Effects of c-MYC activation on glucose stimulus-secretion coupling events in mouse pancreatic islets.
Guiot, Y; Jonas, JC; Khan, M; Pascal, SM; Pelengaris, S, 2008
)
1.07
"Tamoxifen citrate treatment of female rats had no effect on hepatic, pulmonary, or intestinal microsomal aryl hydrocarbon hydroxylase or 7-ethoxycoumarin O-de-ethylase activities or hepatic cytochrome P-450 content."( Effect of tamoxifen treatment on liver, lung and intestinal mixed-function oxidases in male and female rats.
Al-Turk, WA; Roche, EB; Stohs, SJ,
)
1.26
"Tamoxifen treatment caused a reduction in plasma LH and FSH concentrations within 6 h."( Effects of tamoxifen on concentrations of luteinizing hormone and follicle-stimulating hormone in the plasma of ovariectomized ewes.
Clarke, IJ, 1983
)
1.38
"In tamoxifen-treated animals only 7% (8/111) of hormone-dependent tumours showed progressive growth, compared to 60% in controls."( Antioestrogenic and antitumour activities of a series of non-steroidal antioestrogens.
Valcaccia, B; Wakeling, AE, 1983
)
0.78
"Such tamoxifen-treated rats were used to study the acute effect of oestrogens on testosterone secretion, both in vivo and in vitro."( The acute effect of oestrogens on testosterone production appears not to be mediated by testicular oestrogen receptors.
Bergh, A; Daehlin, L; Damber, JE; Ekholm, C; Selstam, G; Södergård, R, 1983
)
0.72
"Tamoxifen treatment (20 mg/day) did not affect the gonadotropin levels, but it temporarily increased prolactin, induced sex hormone-binding globulin production, and suppressed peripheral serum progesterone, 17-hydroxyprogesterone, androstenedione, testosterone, and 5 alpha-dihydrotestosterone concentrations."( Rapid endocrine effects of tamoxifen and testolactone in prostatic carcinoma patients.
Bolton, NJ; Kontturi, M; Leinonen, P; Vihko, R, 1982
)
1.28
"Tamoxifen treatment or castration allowed tumors to remain hormone responsive, whereas initial estrogen treatment prevented response to subsequent therapy and led to an autonomous change."( Development of androgen-stimulated transplants of Nb rat carcinoma of the dorsal prostate and their response to sex hormones and tamoxifen.
Noble, RL, 1980
)
1.19
"Tamoxifen treatment lowered levels of serum cholesterol by (mean +/- SE) 12 +/- 2%, low density lipoprotein cholesterol by 19 +/- 3%, and fibrinogen by 18 +/- 4% (P < 0.0001 vs."( The effect of the anti-estrogen tamoxifen on cardiovascular risk factors in normal postmenopausal women.
Evans, MC; Grey, AB; Reid, IR; Stapleton, JP, 1995
)
1.3
"Tamoxifen treatment had no effect on the 16/6 Id induced autoantibody production. "( The beneficial effect of the estrogen antagonist, tamoxifen, on experimental systemic lupus erythematosus.
Bentwich, Z; Mozes, E; Sthoeger, ZM; Zinger, H, 1994
)
1.98
"Tamoxifen treatment decreased the PI of the luminal epithelial cells and of the stroma as much as ovariectomy."( PCNA-immunoreactivity in the uterus of rats after treatment with the antiestrogen tamoxifen.
Kühnel, W; Michna, H; Rumpel, E, 1995
)
1.24
"Tamoxifen treatment inhibited the growth of FTC133 xenografts in nude mice by 52% compared to that in placebo-treated controls (P < 0.002)."( Tamoxifen inhibits growth, migration, and invasion of human follicular and papillary thyroid cancer cells in vitro and in vivo.
Clark, OH; Duh, QY; Hoelting, T; Siperstein, AE, 1995
)
2.46
"b) Tamoxifen treatment is probably associated with an increased incidence of endometrial cancer; however, this association appears to be linked to higher tamoxifen doses (40 mg/d)."( What do we know and what don't we know about tamoxifen in the human uterus.
Friedl, A; Jordan, VC, 1994
)
1.06
"Tamoxifen treatment produces changes in the cellular and circulating levels of growth factors that could influence both receptor negative or receptor positive tumor growth and the metastatic potential of a tumor."( Molecular mechanisms of antiestrogen action in breast cancer.
Jordan, VC, 1994
)
1.01
"Tamoxifen treatment appears to be associated with an increased incidence of endometrial carcinoma in humans and hepatocellular carcinoma in rats."( Involvement of cytochrome P4503A in catalysis of tamoxifen activation and covalent binding to rat and human liver microsomes.
Kupfer, D; Mani, C; Parkinson, A; Pearce, R, 1994
)
1.26
"Tamoxifen treatment resulted in the induction of aneuploidy in approximately 70% of the examined hepatocytes at the doses used."( Tamoxifen induces hepatic aneuploidy and mitotic spindle disruption after a single in vivo administration to female Sprague-Dawley rats.
Bahnub, N; Dragan, YP; Jordan, VC; Pitot, HC; Sargent, LM; Sattler, CA; Sattler, GL; Schroeder, P; Wiley, JE, 1994
)
2.45
"Tamoxifen treatment resulted in diminished expression, but incomplete inhibition of the protooncogene mRNAs."( Protooncogene, growth factor, growth factor receptor, and estrogen and progesterone receptor gene expression in the immature rat uterus after treatment with estrogen and tamoxifen.
Anderson, WA; Bhattacharyya, N; Eatman, E; Hollis, VW; Ramsammy, R, 1994
)
1.2
"Tamoxifen treatment was associated with a significant (P < 0.05) decrease in plasma insulin-like growth factor-I concentrations."( Estrogen receptor blockade with tamoxifen diminishes growth hormone secretion in boys: evidence for a stimulatory role of endogenous estrogens during male adolescence.
Kerrigan, JR; Metzger, DL, 1994
)
1.29
"Four tamoxifen-treated women died of uterine cancer."( Endometrial cancer in tamoxifen-treated breast cancer patients: findings from the National Surgical Adjuvant Breast and Bowel Project (NSABP) B-14.
Costantino, JP; Cronin, WM; Fisher, B; Fisher, ER; Redmond, CK; Wickerham, DL, 1994
)
1.06
"Tamoxifen treatment for breast cancer should continue. "( Endometrial cancer in tamoxifen-treated breast cancer patients: findings from the National Surgical Adjuvant Breast and Bowel Project (NSABP) B-14.
Costantino, JP; Cronin, WM; Fisher, B; Fisher, ER; Redmond, CK; Wickerham, DL, 1994
)
2.05
"Tamoxifen treatment alone or in combination with verapamil did not affect the activity of protein kinase C, an enzyme implicated in the anti-tumor activity of tamoxifen."( Potentiation of tamoxifen activity by verapamil in a human breast cancer cell line.
Gupta, V; Kamath, N; Singh, SV; Tkalcevic, GT, 1994
)
1.36
"Tamoxifen treatment did not significantly affect liver weight at 24 h but by 48 h there was a highly significant reduction in liver remnant weight (TAM, 5.41 +/- 0.85 g; vehicle, 7.31 +/- 1.43 g; P < 0.001)."( Role of the oestrogen receptor in liver regeneration in the male rat.
Farrell, GC; Liddle, C,
)
0.85
"Tamoxifen treatment (20 mg/day orally for 3 weeks), produced a significant increase in plasma estradiol (p = 0.0018) without simultaneous changes in plasma luteinizing hormone, follicle stimulating hormone, prolactin or progesterone."( Effects of tamoxifen on endometrial estrogen and progesterone receptor concentrations in women with fibrocystic disease of the breast.
Blasco Comenge, C; Pérez-López, FR, 1993
)
1.4
"Tamoxifen-treated and control cells were inoculated into opposite flanks of nine nude mice, where they produced measurable tumors in every case."( Tamoxifen stimulates in vivo growth of drug-resistant estrogen receptor-negative breast cancer.
DeGregorio, M; Emshoff, V; Koester, S; Maenpaa, J; Seymour, R; Sipila, P; Wiebe, V; Wurz, G, 1993
)
2.45
"Tamoxifen-treated patients had a median Ki67 LI of 5.6% in the first biopsy falling to 3.0% in the second biopsy (P < 0.001 by Wilcoxon's matched pairs test), whereas placebo-treated patients had a median Ki67 LI of 5.4% in the first biopsy and 5.75% in the second (no significant difference)."( Effect of tamoxifen on Ki67 labelling index in human breast tumours and its relationship to oestrogen and progesterone receptor status.
Anderson, E; Clarke, RB; Howell, A; Jones, LJ; Laidlaw, IJ, 1993
)
1.41
"Tamoxifen treatment did not alter the number of lung metastases, whereas MPA or ovariectomy produced a significant reduction in the number of lung metastases."( The EnDA endometrial adenocarcinoma: an oestrogen-sensitive, metastasizing, in vivo tumour model of the rat.
Deerberg, F; Horn, DW; Schneider, MR; Vollmer, G, 1993
)
1.01
"Tamoxifen pretreatment also enhanced testosterone imprinting of the adult androgen responsiveness of testosterone 2 alpha- and 6 beta-hydroxylase and steroid 5 alpha-reductase activities."( Impact of tamoxifen on peripubertal androgen imprinting of rat hepatic cytochrome P450 2C11, cytochrome P450 3A2, and steroid 5 alpha-reductase.
Bandiera, SM; Bellward, GD; Chan, MM; Chang, TK; Holsmer, SL, 1996
)
1.42
"Tamoxifen treatment is associated with an increased incidence of proliferative and neoplastic changes in the endometrium, with a 1.3 to 7.5 relative risk of developing endometrial carcinoma."( The effects of tamoxifen treatment on the endometrium.
Bar-Am, A; Daniel, Y; Inbar, M; Lessing, JB; Peyser, MR, 1996
)
2.09
"Tamoxifen treatment during postmastectomy radiotherapy enhances the risk of radiation-induced lung fibrosis."( Radiotherapy-related lung fibrosis enhanced by tamoxifen.
Bentzen, SM; Overgaard, J; Overgaard, M; Skoczylas, JZ, 1996
)
1.99
"Tamoxifen treatment on days 9 to 11 resulted in significant reduction of decidual weight (35.1% on day 12 of pregnancy, P < 0.001)."( The effects of the antihormones RU486 and tamoxifen on fetoplacental development and placental bed vascularisation in the rat: a model for intrauterine fetal growth retardation.
Bell, SC; Sadek, S, 1996
)
1.28
"Tamoxifen treatment for 9 and 14 days induced ovarian regression but not incubation behavior."( Changes in pituitary somatotrophs and lactotrophs associated with ovarian regression in the turkey hen (Meleagris gallopavo).
Kuenzel, WJ; Proudman, JA; Ramesh, R, 1995
)
1.01
"Tamoxifen-treated patients who remained disease free after 5 years of therapy were then reassigned to receive either another 5 years of tamoxifen (n = 322) or 5 years of placebo (n = 321)."( Five versus more than five years of tamoxifen therapy for breast cancer patients with negative lymph nodes and estrogen receptor-positive tumors.
Bowman, DM; Bryant, J; Costantino, J; DeCillis, A; Deschênes, L; Dignam, J; Dimitrov, NV; Evans, J; Farrar, W; Feldman, MI; Fisher, B; Fisher, ER; Lickley, HL; Margolese, RG; Paterson, AH; Redmond, C; Robidoux, A; Shibata, H; Terz, J; Wickerham, DL; Wolmark, N, 1996
)
1.29
"Tamoxifen (TAM) treatment following isolated locoregional recurrence of breast cancer significantly increases 5-year disease-free survival rates compared with observation alone in potentially hormone-responsive patients [J Clin Oncol 1994, 12, 2071-2077]. "( Possible deleterious effect of tamoxifen in premenopausal women with locoregional recurrence of breast cancer.
Bacchi, M; Borner, MM; Castiglione, M, 1996
)
2.02
"In tamoxifen treated cells, IFN-beta and IFN-gamma readily activated transcription factors ISGF-3 and GAF, respectively."( Tamoxifen enhances interferon-regulated gene expression in breast cancer cells.
Borden, EC; Kalvakolanu, DV; Kolla, V; Lindner, DJ, 1997
)
2.25
"Tamoxifen treatment increased the secretion of TGF-beta activity into serum-free cell medium and the cellular content of affinity cross-linked type I and III TGF-beta receptors in both cell lines."( Blockade of transforming growth factor-beta signaling does not abrogate antiestrogen-induced growth inhibition of human breast carcinoma cells.
Arteaga, CL; Brattain, MG; Dugger, TC; Ko, Y; Koli, KM; Ramsey, TT, 1997
)
1.02
"Tamoxifen treatment (40mg/day) for 1 month in eight patients increased oestradiol values (62.2 +/- 77.0 vs."( Oestradiol and testosterone blood levels in patients with viral cirrhosis and hepatocellular carcinoma.
Daniele, B; Esposito, G; Fiore, F; Galati, MG; Pergola, M; Pignata, S; Ricchi, P; Vallone, P, 1997
)
1.02
"Tamoxifen treatment is a proven therapy for breast cancer that produces a survival advantage when used as an adjuvant, and reduces the incidence of recurrences and controlateral tumor evolution. "( Acute leukaemia during tamoxifen therapy.
Demiroğlu, H; Güllü, I; Tekuzman, G; Yalçin, S, 1997
)
2.05
"Tamoxifen treatment had no effect on oxytocinase activity."( Metabolism of oxytocin in rat uterus and placenta in late gestation.
Fang, X; Mitchell, BF; Wong, S, 1997
)
1.02
"Tamoxifen treatment, on the other hand, produced an increase in both the number and crowding of the endometrial glands and a mild atrophy of the myometrial layer."( Comparative effects of 28-day treatment with the new anti-estrogen EM-800 and tamoxifen on estrogen-sensitive parameters in intact mice.
Belanger, A; Gauthier, S; Labrie, C; Labrie, F; Luo, S; Martel, C; Mérand, Y; Sourla, A, 1997
)
1.25
"Tamoxifen treatment increased hypoxia in the tumors, as measured by EF5 binding (P = 0.01 by Mann-Whitney test)."( Tamoxifen induces hypoxia in MCF-7 xenografts.
Evans, SM; Jenkins, WT; Koch, CJ; Laughlin, KM; Van Winkle, T; Wilson, DF, 1997
)
2.46
"Tamoxifen treatment suppressed plasma levels of FT3 and FT4 (p < 0.005 for both) and elevated plasma concentrations of TBG (p < 0.005 and TG (p < 0.025)."( Thyroid function in postmenopausal breast cancer patients treated with tamoxifen.
Aakvaag, A; Anker, GB; Lien, EA; Lønning, PE, 1998
)
1.25
"Tamoxifen treatment was well tolerated by the patients."( Tamoxifen does not improve survival of patients with advanced hepatocellular carcinoma.
de la Mata, M; Delgado, M; Diaz, G; González, N; Miño-Fugarolas, G; Riestra, S; Rodrigo, L; Rodriguez, M; Suárez, A, 1998
)
2.46
"Tamoxifen (1 mg/kg/day) treated diabetic rats showed tumour regression in 67% of NMU-induced mammary tumours versus 53% in controls (NS)."( An experimental model of diabetes and cancer in rats.
Bergoc, RM; Cocca, C; Cricco, G; Croci, M; Davio, C; Fitzsimons, C; Gutierrez, A; Lemos, B; Levin, E; Levin, R; Martin, G; Rivera, E, 1998
)
1.02
"Tamoxifen treated patients showed nonsignificant increase in molybdenum, after 3 months, significant increase after 6 months and significant increase in xanthine oxidase and riboflavin levels."( Molybdenum, xanthine oxidase and riboflavin levels in tamoxifen treated postmenopausal women with breast cancer.
Kamble, SM; Kamlakar, PL; Vaidya, SM, 1998
)
1.27
"Tamoxifen treatment increases the incidence of ovarian cysts and the significantly higher 17beta-estradiol serum levels in premenopausal breast cancer patients."( Ovarian overstimulation and cystic formation in premenopausal tamoxifen exposure: comparison between tamoxifen-treated and nontreated breast cancer patients.
Altaras, MM; Beyth, Y; Cohen, I; Figer, A; Shapira, J; Tepper, R; Yigael, D, 1999
)
1.99
"Tamoxifen-treated patients were less likely to have ovarian cancer, 0 of 53 patients (95% confidence interval (CI): 0.0%, 6.7%) compared with 10 of 99 patients (95% CI: 5.0%, 17.8%) patients not receiving tamoxifen (P = 0.015)."( Ovarian histopathology in breast cancer patients receiving tamoxifen.
McGonigle, KF; Odom-Maryon, T; Simpson, JF; Vasilev, SA, 1999
)
1.27
"Tamoxifen-treated postmenopausal patients show a significantly better prognosis than premenopausal patients, favoring the hypothesis of a more pronounced effect of tamoxifen in the older age groups."( Randomized trial of low-dose chemotherapy added to tamoxifen in patients with receptor-positive and lymph node-positive breast cancer.
Fridrik, M; Gnant, M; Haider, K; Hausmaninger, H; Jakesz, R; Kolb, R; Kubista, E; Manfreda, D; Mittlböck, M; Mlineritsch, B; Samonigg, H; Steger, G; Steindorfer, P; Stierer, M; Tschurtschenthaler, G, 1999
)
1.28
"Tamoxifen treatment significantly reduced TPH protein compared to EE and ovariectomized control animals."( Steroid regulation of tryptophan hydroxylase protein in the dorsal raphe of macaques.
Adams, MR; Bethea, CL; Mirkes, SJ; Shively, CA, 2000
)
1.03
"In tamoxifen-treated patients, total cholesterol (TC), free cholesterol (FC), phospholipids (PL), free fatty acids (FFA), low density lipoprotein cholesterol (LDL) levels were decreased and the triglycerides (TG), ester cholesterol (EC), high density lipoprotein cholesterol (HDL) and very low density lipoprotein cholesterol (VLDL) levels were increased."( Salubrious effect of vitamin C and vitamin E on tamoxifen-treated women in breast cancer with reference to plasma lipid and lipoprotein levels.
Arumugam, G; Babu, JR; Deepa, N; Renuka, R; Sachdanandam, P; Sundravel, S, 2000
)
1.08
"In tamoxifen-treated hepatocytes and after a single dose of tamoxifen in vivo, DNA adduct formation in male cells was significantly lower than in female cells, 11- and 6-fold, respectively."( Sex differences in the activation of tamoxifen to DNA binding species in rat liver in vivo and in rat hepatocytes in vitro: role of sulfotransferase induction.
Davis, W; Glatt, H; Hewer, A; Meinl, W; Phillips, DH; Rajkowski, KM, 2000
)
1.09
"Tamoxifen treatment was significantly associated with higher circulating and platelet-derived VEGF levels."( Vascular endothelial growth factor (VEGF) in breast cancer: comparison of plasma, serum, and tissue VEGF and microvessel density and effects of tamoxifen.
Adams, J; Allgar, V; Banks, RE; Bicknell, R; Cairnduff, F; Carder, PJ; Downey, S; Forbes, MA; Hallam, S; Kaufman, S; Lansdown, M; MacLennan, K; Perren, TJ; Selby, PJ; Walker, JJ, 2000
)
1.23
"Tamoxifen-treated breast carcinoma survivors are at elevated risk of endometrial carcinoma. "( Surveillance for uterine abnormalities in tamoxifen-treated breast carcinoma survivors: a community based study.
Althuis, MD; Bush, TL; Khoo, L; Langenberg, P; Magaziner, J; Sexton, M; Tkaczuk, K, 2000
)
2.01
"Tamoxifen pretreatment reduced the total protein of the cytosolic fraction by 50% and reduced the formation of doxorubicinol both in vitro and in vivo. "( Effect of tamoxifen pretreatment on the pharmacokinetics, metabolism and cardiotoxicity of doxorubicin in female rats.
Boroujerdi, M; Vaidyanathan, S, 2000
)
2.15
"In tamoxifen-treated patients, TVS offered a high false-positive rate, even with a cutoff value of 10 mm for endometrial thickness and repeated TVS scans. "( Effects of adjuvant tamoxifen on the endometrium in postmenopausal women with breast cancer: a prospective long-term study using transvaginal ultrasound.
Friese, K; Gerber, B; Krause, A; Külz, T; Kundt, G; Makovitzky, J; Müller, H; Reimer, T, 2000
)
1.25
"Tamoxifen-treated patients displayed greater levels of endometrial dysplasia and glandular hyperplasia, in addition to a statistically significant (P<0.0001) elevation in gland-associated TGFbeta1 protein."( Modulation of endometrial transforming growth factor beta (TGFbeta) by tamoxifen.
Carmichael, PL; Neven, P; Pole, JC, 2000
)
1.26
"Tamoxifen treatment can therefore be used successfully to manipulate several components of the female reproductive phenotype (egg composition, intraclutch egg-size variation) to further explore the fitness consequences of these traits."( Experimental (tamoxifen-induced) manipulation of female reproduction in zebra finches (Taeniopygia guttata).
Williams, TD,
)
1.21
"Tamoxifen treatment of women leads to a small increase in the incidence of endometrial cancers."( Anti-oestrogenic drugs and endometrial cancers.
White, IN, 2001
)
1.03
"Tamoxifen treatment resulted in a modest, but significant (p < 0.05), increase in oocytes with PCS."( Tamoxifen-induced alterations in meiotic maturation and cytogenetic abnormalities in mouse oocytes and 1-cell zygotes.
London, SN; Mailhes, JB, 2001
)
2.47
"Tamoxifen treatment significantly increased IGF-BP1 after 18 and 27 months (baseline: mean, 21.6 ng/ml; SD, 16.6; 18 months: mean, 52.0 ng/ml; SD, 41.8; p = 0.019; 27 months: mean, 40.7 ng/ml; SD, 24.9; p = 0.043) and IGF-BP3 after nine, 18, and 27 months (baseline: mean, 3119 ng/ml; SD, 507; nine months: mean, 3673 ng/ml; SD, 476; p = 0.004; 18 months: mean, 3445 ng/ml; SD, 634; p = 0.034; 27 months: 3409 ng/ml; SD, 501; p = 0.043) when compared with baseline values."( IGF status is altered by tamoxifen in patients with breast cancer.
Campbell, MJ; Leathem, AJ; Secker-Walker, J; Titcomb, A; Woodside, JV, 2001
)
1.34
"Tamoxifen treatment, however, increased the expression of both proteins whereas progesterone had no effect."( Function of the exon 7 deletion variant estrogen receptor alpha protein in an estradiol-resistant, tamoxifen-sensitive human endometrial adenocarcinoma grown in nude mice.
Helou, K; Henriksson, M; Horvath, G; Leser, G, 2002
)
1.25
"Tamoxifen treatment has been demonstrated to decrease the function of fibroblasts derived from Dupuytren's affected fascia and downregulated TGF(beta2) production in these same fibroblasts."( Tamoxifen decreases fibroblast function and downregulates TGF(beta2) in dupuytren's affected palmar fascia.
Ko, F; Kuhn, MA; Payne, WG; Robson, MC; Wang, X, 2002
)
2.48
"The tamoxifen-treated patients were subdivided in premenopausal (Group IB = 72 patients) and in postmenopausal (Group IIB = 262 patients) groups."( Indication of hysteroscopy in tamoxifen treated breast cancer patients.
Artini, PG; Curcio, C; Fasciani, A; Fornaciari, G; Genazzani, AR; Giuntini, A; Petraglia, F; Taponeco, F, 2002
)
1.08
"Tamoxifen treatment of women with advanced breast cancer has previously been reported to reduce plasma insulin-like growth factor-type I (IGF-I) concentrations. "( The effect of endocrine therapy with medroxyprogesterone acetate, 4-hydroxyandrostenedione or tamoxifen on plasma concentrations of insulin-like growth factor (IGF)-I, IGF-II and IGFBP-1 in women with advanced breast cancer.
Christodoulides, A; Ghilchik, MW; Koistinen, R; Reed, MJ; Seppälä, M; Teale, JD, 1992
)
1.95
"Tamoxifen treatment resulted in a dose-duration increase in ADP-ribosylation."( Elevation of ADP-ribosylation as an indicator of mononuclear leucocyte responsiveness in breast cancer patients treated with tamoxifen.
Killander, F; Olsson, H; Pero, RW; Troll, W, 1992
)
1.21
"Tamoxifen treatment should still be regarded as the gold standard for postmenopausal ER positive patients."( Chemotherapy versus tamoxifen versus chemotherapy plus tamoxifen in node-positive, oestrogen-receptor positive breast cancer patients. An update at 7 years of the 1st GROCTA (Breast Cancer Adjuvant Chemo-Hormone Therapy Cooperative Group) trial.
Amoroso, D; Boccardo, F; Castagnetta, L; Farris, A; Genta, F; Nenci, I; Piffanelli, A; Rubagotti, A; Sismondi, P; Traina, A, 1992
)
1.33
"Tamoxifen treated ovariectomized mice did not develop any decrease either in the bone density or in calcium and phosphate content of the femora which were observed in ovariectomized mice."( Tamoxifen prevents bone loss in ovariectomized mice.
Broulik, PD, 1991
)
2.45
"Tamoxifen treatment prevented the decrease in BV/TV after OVX, although the highest dose of tamoxifen resulted in a small decrease in BV/TV in intact female rats."( Dose-dependent effects of tamoxifen on long bones in growing rats: influence of ovarian status.
Moon, LY; Turner, RT; Wakley, GK, 1991
)
1.3
"Tamoxifen treatment did not significantly influence the growth of the transplanted carcinomas in the rat model."( Effects of sex steroid hormones on pancreatic cancer in the rat.
Longnecker, DS; Sumi, C,
)
0.85
"The tamoxifen or placebo treatment continued to death or to 10 months after accrual into the trial was stopped."( Tamoxifen therapy in unresectable adenocarcinoma of the pancreas and the papilla of Vater.
Arnesjø, B; Bakkevold, KE; Espehaug, B; Pettersen, A, 1990
)
2.2
"When tamoxifen treatment was withdrawn, recurrence of endometrial implants was observed."( Disparate effect of tamoxifen in rats with experimentally induced endometriosis.
Kadaba, R; Simpson, CW, 1990
)
1.06
"Tamoxifen treatment did not influence ER and PR levels."( Steroid hormone receptors in carcinoma of the cervix: lack of response to an antiestrogen.
Baiocchi, G; Battaglia, F; Ferrandina, G; Greggi, S; Mancuso, S; Panici, PB; Scambia, G, 1990
)
1
"Tamoxifen treatment resulted in decreased cell proliferation and decrease of estrogen receptor content and of total protein synthesis."( Effect of alpha-interferon, 17 beta-estradiol, and tamoxifen on estrogen receptor concentration and cell cycle kinetics of MCF 7 cells.
Bezwoda, WR; Meyer, K, 1990
)
1.25
"Tamoxifen treatment induced a PR of 6 months, with normalization of serum bilirubin, reduction of alfa-fetoprotein level and improvement of PS, and was free of toxicity."( [Hepatocellular carcinoma (HCC): the long-term response to tamoxifen. A clinical case report and review of the literature].
Belli, L; Morgante, A; Passalacqua, G; Rabitti, G; Recchia, F; Rodorigo, C, 1989
)
1.24
"Tamoxifen treatment is justified in patients who meet the eligibility criteria of the present study and who refuse to participate in those trials."( A randomized clinical trial evaluating tamoxifen in the treatment of patients with node-negative breast cancer who have estrogen-receptor-positive tumors.
Bowman, D; Costantino, J; Couture, J; Dimitrov, NV; Fisher, B; Fisher, ER; Poisson, R; Redmond, C; Wickerham, DL; Wolmark, N, 1989
)
1.27
"Tamoxifen pretreated women had a GH peak after GHRH of 35.6 +/- 9.7 ng/ml, not significant versus control test."( Growth hormone and prolactin secretion after growth hormone-releasing hormone administration, in anorexia nervosa patients, normal controls and tamoxifen-pretreated volunteers.
Borras, CG; Burguera, B; Casanueva, FF; Devesa, J; Lima, L; Muruais, C; Tresguerres, JA, 1987
)
1.19
"Tamoxifen-bromocryptine-treated groups displayed a 2-fold increase in latency of tumor appearance as compared to vehicle-treated controls; however, this long latency was not reduced when these rats were fed a high fat diet."( Effects of high dietary fat on the growth and development of ovarian-independent carcinogen-induced mammary tumors in rats.
Ip, C; Ip, MM; Sylvester, PW, 1986
)
0.99
"Tamoxifen treatment induced tumor regression but the percentage of regressing, static or growing tumors was no different in the presence or absence of DFMO."( Effect of tamoxifen and D,L-2-difluoromethylornithine on the growth, ornithine decarboxylase activity and polyamine content of mammary carcinomas induced by 1-methyl-1-nitrosourea.
Meeker, LD; Ritacco, KA; Ronan, AM; Thompson, HJ, 1986
)
1.39
"Tamoxifen treatment, however, did not modify significantly the reactivity of the testes towards high doses of hCG (10 i.u.), administered either 2 h before sacrifice or for 9 days."( Influence of a prolonged tamoxifen administration on steroidogenesis by incubated rat testes.
Eechaute, W; Lacroix, E; Leusen, I; Vanderstichele, H, 1987
)
1.3
"Tamoxifen treatment caused a transient tumour growth inhibition during weeks 1-5 with subsequent re-growth of mammary tumours."( Therapeutic effect of the arotinoid Ro 15-0778 on chemically induced rat mammary carcinoma.
Bollag, W; Teelmann, K, 1988
)
1
"Tamoxifen treatment significantly reduced the loss of trabecular bone, restoring resorbing surface length to the control (sham-operated) animal levels."( The effects of tamoxifen on the osteopenia induced by sciatic neurotomy in the rat: a histomorphometric study.
Baum, BL; Hannon, KS; Turner, RT; Wakley, GK, 1988
)
1.35
"Tamoxifen-treated women had been postmenopausal for more years (p = 0.012)."( Bone mineral density in women with breast cancer treated with adjuvant tamoxifen for at least two years.
Barden, HS; Jordan, VC; Love, RR; Mazess, RB; Newcomb, PA; Tormey, DC, 1988
)
1.23
"Tamoxifen treatment of cockerels results in dose- and time-dependent decreases in serum free and esterified cholesterol, and in phospholipids and triglycerides."( Interactions of tamoxifen in the chicken.
Lazier, CB, 1987
)
1.34
"Tamoxifen-treated animals did not develop kidney tumors and did not show any detectable DNA damage."( Inhibition of estrogen-induced renal carcinogenesis in male Syrian hamsters by tamoxifen without decrease in DNA adduct levels.
Jurka, E; Liehr, JG; Randerath, E; Randerath, K; Sirbasku, DA, 1988
)
1.22
"Tamoxifen treatment (1.0 and 10.0 mg/kg/day for 14 days) had no significant effect on the delta rate."( Effect of in vivo antiestrogen pretreatment on rabbit atrial chronotropic response to histamine.
Baksi, SN; Hughes, MJ, 1986
)
0.99
"Tamoxifen treatment was not associated with changes in mean hormone levels, although there was a tendency toward reductions in the magnitude of episodic LH and testosterone secretion."( Evidence that estrogen regulation of testosterone secretion in adult rams is mediated by both indirect (gonadotropin dependent) and direct (gonadotropin independent) means.
Sanford, LM,
)
0.85
"Tamoxifen treatment resulted in structural and cytoskeletal changes similar to those observed in estrogen stimulated cells."( Estrogen and tamoxifen induced cytoskeletal changes in breast cancer cells.
Bussolati, G; Guidoni, L; Marchisio, PC; Sapino, A, 1985
)
1.36
"Tamoxifen-treated rabbits had less incorporation of radioactivity."( A possible mechanism in arterial wall for mediation of sex difference in atherosclerosis.
Bashey, RI; Fischer, GM; Lyttle, CR; Rosenbaum, H, 1985
)
0.99
"Cotreatment with tamoxifen, an estrogen receptor inhibitor, increased the sensitivity to doxorubicin, which decreased the colony formation of P53(+) U2OS cells."( Suppression of Estrogen Receptor Alpha Inhibits Cell Proliferation, Differentiation and Enhances the Chemosensitivity of P53-Positive U2OS Osteosarcoma Cell.
Chen, CF; Chen, CM; Chen, WM; Wang, JY; Wu, PK, 2021
)
0.95
"Treatment with tamoxifen can be as effective as GnRH agonist for endometrial preparation in FET."( Comparison of tamoxifen and hormone replacement cycle (HRT) in frozen embryo transfer. A randomized controlled trial.
Ebrahimi, R; Khadem, N; Mahmoudinia, M; Rastaghi, S; Sadeghi, T; Souizi, B, 2023
)
1.62
"Mice treated with tamoxifen for 1 week and left untreated for an additional week before infection showed similar parasitaemia levels and signs of cerebral malaria as control untreated mice."( Tamoxifen activity against Plasmodium in vitro and in mice.
Fisher, E; Gallego-Delgado, J; Gomes, C; Gonzalez, S; Nikain, C; Rodriguez, A; Sherman, J; Weinstock, A, 2019
)
2.28
"Treatment with tamoxifen decreased viability of MKN-45 cells in a dose-dependent manner. "( Tamoxifen Downregulates the Expression of Notch1 and DLL1 Genes in MKN-45 Gastric Cancer Cells.
Akrami, H; Khanipouyani, F, 2021
)
2.42
"Treatment with tamoxifen decreased TP mRNA and protein levels through AKT inactivation."( Tamoxifen enhances erlotinib-induced cytotoxicity through down-regulating AKT-mediated thymidine phosphorylase expression in human non-small-cell lung cancer cells.
Chen, CY; Chiu, HC; Huang, YJ; Jian, YJ; Jian, YT; Ko, JC; Lin, YW; Syu, JJ; Wo, TY, 2014
)
2.18
"Rats treated with Tamoxifen recovered some locomotor activity at 21 and 28 DPI, which could be related to the antioxidant protection seen at these time points."( Tamoxifen and estradiol improved locomotor function and increased spared tissue in rats after spinal cord injury: their antioxidant effect and role of estrogen receptor alpha.
Colón, JM; Meléndez, M; Miranda, JD; Mosquera, L; Rodríguez-Orengo, JF; Santiago, JM; Segarra, AC; Torrado, AI, 2014
)
2.17
"When treatment with tamoxifen was considered, STAT1 gene expression was nearly predictive of distant metastasis-free survival (DMFS, log-rank p = 0.067), while STAT3 gene expression was predictive of DMFS (log-rank p<0.0001)."( Increased STAT1 signaling in endocrine-resistant breast cancer.
Faratian, D; Harrison, DJ; Huang, R; Langdon, SP; Sims, AH; Thomas, JS; Wilson, D, 2014
)
0.72
"Treatment with tamoxifen significantly controlled dyslipidemia, hypertension, bradycardia, oxidative stress and reduced serum cardiac markers."( Beneficial role of tamoxifen in experimentally induced cardiac hypertrophy.
Desai, VJ; Patel, BM, 2014
)
1.07
"Treatment with tamoxifen significantly controlled dyslipidemia, hypertension, bradycardia, oxidative stress, and reduced serum cardiac markers."( Beneficial role of tamoxifen in isoproterenol-induced myocardial infarction.
Patel, BM; Rayabarapu, N, 2014
)
1.07
"Treatment with tamoxifen for 6 months after chemotherapy significantly reduced the plasma levels of NT-proBNP and did not change LVEF in women with breast cancer."( Hormone therapy with tamoxifen reduces plasma levels of NT-B-type natriuretic peptide but does not change ventricular ejection fraction after chemotherapy in women with breast cancer.
Abreu, GR; Amorim, MH; Borgo, MV; Carvalho, AL; Gouvea, SA; Romero, WG; Silva, FB, 2015
)
1.08
"Pretreatment with tamoxifen/l-NAME/Hb blocked the BPA-induced increase of nitrite levels."( Bisphenol A depresses monosynaptic and polysynaptic reflexes in neonatal rat spinal cord in vitro involving estrogen receptor-dependent NO-mediated mechanisms.
Deshpande, SB; Pandey, AK, 2015
)
0.74
"Treatment with tamoxifen for at least 5 years has been for a long time the standard of care, as it is associated with overall positive clinical outcomes."( Endocrine therapy in premenopausal women with breast cancer: a critical appraisal of current evidence.
De Laurentiis, M; Del Mastro, L; Montemurro, F; Puglisi, F, 2016
)
0.77
"Treatment with tamoxifen for 28 days caused hepatic PLD in rats."( Arachidonic acid-containing phosphatidylcholine characterized by consolidated plasma and liver lipidomics as an early onset marker for tamoxifen-induced hepatic phospholipidosis.
Goda, K; Kobayashi, A; Maekawa, K; Saito, K; Saito, Y; Sugai, S; Yamada, N, 2017
)
1
"Pre-treatment with tamoxifen for 2-5 years may reduce the clinical significance of the adverse bone effects associated with aromatase inhibitors, particularly if this leads to a shortening in the duration of exposure to an aromatase inhibitor."( Guidance for the management of breast cancer treatment-induced bone loss: a consensus position statement from a UK Expert Group.
Coleman, RE; Doughty, J; Eastell, R; Heys, SD; Howell, A; McCloskey, EV; Powles, T; Reid, DM; Selby, P, 2008
)
0.66
"Treatment with tamoxifen of breast cancer patients led to a decrease of E2 sensitivity, whereas growth potential was not affected significantly."( The growth-promoting action of individual women's sera on mammary carcinoma cells.
Auer, D; Daxenbichler, G; Fleischer, M; Hubalek, M; Roessler, J,
)
0.47
"Cotreatment with tamoxifen or the chemokine interferon-inducible protein-10 (IP-10) suppressed the action estrogen on VEGF expression."( Antitumor/antiestrogenic effect of the chemokine interferon inducible protein 10 (IP-10) involves suppression of VEGF expression in mammary tissue.
Aronica, SM; Hanzly, M; Kisela, C; Raiber, L, 2009
)
0.68
"Treatment with tamoxifen reduced the responses to acetylcholine (pD(2) = 2.2 +/- 0.06 and 1.9 +/- 0.05 after vehicle and tamoxifen, respectively; P < 0.05), while its metabolites improved these responses (pD(2) = 2.5 +/- 0.04 after N-desmethyl-tamoxifen, 2.5 +/- 0.03 after 4-hydroxy-tamoxifen, and 2.6 +/- 0.08 after endoxifen; P < 0.01)."( Assessment of vascular effects of tamoxifen and its metabolites on the rat perfused hindquarter vascular bed.
Desta, Z; Flockhart, DA; Gomes, VA; Montenegro, MF; Pessa, LR; Tanus-Santos, JE, 2009
)
0.97
"Treatment with tamoxifen did not inhibit this hyperplasia; instead, such treatment exaggerated hyperplasia with an enhanced degree of alteration, indicative of hypersensitivity to tamoxifen."( Extranuclear coactivator signaling confers insensitivity to tamoxifen.
Holm, C; Kumar, R; Landberg, G; Rayala, SK; Vadlamudi, RK; Zhang, H, 2009
)
0.93
"Treatment with tamoxifen should be recommended to patients with estrogen receptor positive tumors who have been treated with conservative surgery."( Current perspectives of treatment of ductal carcinoma in situ.
Alvarez, I; Estévez, LG; Lluch, A; Margelí, M; Miró, C; Muñoz, M; Rubio, C; Seguí, MÁ; Tusquets, I, 2010
)
0.7
"The treatment with Tamoxifen was done in 11 patients with high values of Progesterone and Estrogen Receptors (PR, ER)."( [Breast cancer in the male].
Bostaca, T; Coşman, C; Diaconu, C; Dogaru, C; Florea, I; Livadariu, R; Miron, L; Scarlat, V,
)
0.45
"Treatment with tamoxifen (TAM) increases the risk of developing endometrial cancer in women. "( Anti-breast cancer potential of SS5020, a novel benzopyran antiestrogen.
Chen, JJ; Kim, HJ; Laxmi, YR; Liu, X; Okamoto, K; Okamoto, Y; Shibutani, S; Suzuki, N; Zhang, G, 2011
)
0.72
"Co-treatment with tamoxifen decreased GPx and catalase levels; did not completely inhibit E2-mediated oxidative DNA damage and estrogen-responsive genes monoamine oxygenase B1 (MaoB1) and cell death inducing DFF45 like effector C (Cidec) but differentially affected the levels of tamoxifen metabolizing enzymes."( Partial inhibition of estrogen-induced mammary carcinogenesis in rats by tamoxifen: balance between oxidant stress and estrogen responsiveness.
Bhat, HK; Bhat, NK; Singh, B, 2011
)
0.92
"Treatment of tamoxifen significantly reduced the estrogen-induced MCF-7 tumor prevalence and tumor size."( Low-dose dietary genistein negates the therapeutic effect of tamoxifen in athymic nude mice.
Cooke, PS; Doerge, DR; Du, M; Hartman, JA; Helferich, WG; Ju, YH; Yang, X, 2012
)
0.97
"Treatment with tamoxifen and letrozole (200mg/kg feed) to fingerlings of C."( Introduction of modern endocrine techniques for the production of monosex population of fishes.
Singh, AK, 2013
)
0.73
"Pretreatment with Tamoxifen reversed the suppressive effect of E2 on the JAK-STAT pathway in IFNα-treated PBMCs as indicated by a significant increase in MxA expression (P = 0.05*)."( Tamoxifen alleviates hepatitis C virus-induced inhibition of both toll-like receptor 7 and JAK-STAT signalling pathways in PBMCs of infected Egyptian females.
Abdelaziz, AI; Ahmed, R; Esmat, G; Fawzy, IO; Hamdi, N; Negm, M, 2012
)
2.15
"Treatment with tamoxifen, a selective estrogen receptor blocker, has been shown to effectively reduce the disc size and is generally considered for treatment when the disc diameter is > 3-4 cm."( The histopathological effects of tamoxifen in the treatment of pubertal gynecomastia.
Akgül, S; Derman, O; Güçer, S; Kanbur, N; Safak, T, 2012
)
1
"Treatment with tamoxifen led to a significant subjective improvement and objective changes, confirmed by regular clinical examinations, ultrasonography, and computed tomography of the neck."( Riedel's thyroiditis treated with tamoxifen.
Dabelic, N; Jukic, T; Kusic, Z; Labar, Z; Matesa, N; Novosel, SA, 2003
)
0.94
"Treatment with tamoxifen had effects similar to those of estrogen."( Effects of long-term HRT and tamoxifen on the expression of progesterone receptors A and B in breast tissue from surgically postmenopausal cynomolgus macaques.
Cline, JM; Isaksson, E; Sahlin, L; von Schoultz, B; von Schoultz, E; Wang, H, 2003
)
0.95
"Treatment with tamoxifen citrate and testosterone undecanoate improved sperm variables and led to a higher incidence of pregnancy in couples with subfertility related to idiopathic oligozoospermia."( Effectiveness of combined tamoxifen citrate and testosterone undecanoate treatment in men with idiopathic oligozoospermia.
Adamopoulos, DA; Billa, E; Koukkou, E; Michopoulos, J; Nicopoulou, S; Pappa, A, 2003
)
0.97
"The treatment with tamoxifen at doses of 2 mg/kg/24 h and 4 mg/kg/24 h significantly increased BMC and BMD in comparison with ovariectomized control."( Effect of tamoxifen on bone mineral density and blood lipids in ovariectomized rats.
Czerny, B; Juzyszyn, Z; Myśliwiec, Z; Pawlik, A,
)
0.85
"Treatment with tamoxifen may still be useful upon subsequent progression."( Anastrozole ('Arimidex') versus tamoxifen as first-line therapy in postmenopausal women with advanced breast cancer: results of the double-blind cross-over SAKK trial 21/95--a sub-study of the TARGET (Tamoxifen or 'Arimidex' Randomized Group Efficacy and
Aebi, S; Ballabeni, P; Goldhirsch, A; Hess, D; Köberle, D; Pagani, O; Perey, L; Rochlitz, C; Senn, I; Thürlimann, B, 2004
)
0.95
"The treatment with tamoxifen significantly increased the total number of lymphocytes in the follicles, PALS (periarterial lymph sheath) and red pulp relative to all other groups."( Response of T- and B-lymphocytes in the spleen of mammary tumor-bearing rats to treatment with tamoxifen and soluble tumor-associated antigens.
Ben-Hur, H; Elhayany, A; Geva, D; Kossoy, G; Sanko, H; Shumlin, N; Zusman, I, 2004
)
0.86
"Ever treatment with tamoxifen was associated with a much greater risk of Mullerian and mesodermal mixed endometrial tumors (OR = 13.5, 95% CI = 4.1 to 44.5) than of adenocarcinoma (OR = 2.1, 95% CI = 1.6 to 2.7) or clear cell and papillary serous tumors (OR = 3.1, 95% CI = 0.8 to 17.9)."( Tamoxifen treatment for breast cancer and risk of endometrial cancer: a case-control study.
Jones, ME; Swerdlow, AJ, 2005
)
2.09
"Treatment with tamoxifen (or vehicle) started on day 4 after implantation."( Effect of tamoxifen in an experimental model of breast tumor studied by dynamic contrast-enhanced magnetic resonance imaging and different contrast agents.
Calderan, L; Cavagna, F; Crescimanno, C; Grotti, A; Lorusso, V; Lovati, E; Marzola, P; Merigo, F; Nicolato, E; Osculati, F; Ramponi, S; Sandri, M; Sbarbati, A; Vultaggio, S, 2005
)
1.07
"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,
)
0.73
"Treatment with tamoxifen alone or in combination with sTAA significantly increased the number of primordial follicles and atretic follicles in the ovaries, and promoted the formation of small follicular cysts."( Effects of tamoxifen and soluble tumor-associated antigens on ovarian structure in mammary tumor-bearing rats.
Ben-Hur, H; Elhayany, A; Kossoy, G; Kossoy, N; Schneider, DF; Zusman, I, 2005
)
1.06
"Treatment with tamoxifen for more than five years appears detrimental rather than beneficial and, therefore, tamoxifen is not indicated for use beyond the initial five years."( Extended breast cancer treatment with an aromatase inhibitor (Letrozole) after tamoxifen: why, who and how long?
Kaufmann, M; Rody, A, 2006
)
0.9
"Treatment with tamoxifen, raloxifene, or the pure antiestrogen ICI 182,780 inhibited proliferation of 5637 cells in vitro. "( Efficacy of selective estrogen receptor modulators in nude mice bearing human transitional cell carcinoma.
Jian, W; Lerner, SP; Okuno, N; Shen, SS; Smith, CL; Sonpavde, G; Weiss, H; Younes, M; Yu, J, 2007
)
0.69
"Treatment with tamoxifen, or its metabolite 4-hydroxytamoxifen (4OHT), has cytostatic and cytotoxic effects on breast cancer cells in vivo and in culture. "( Regulation of intracellular calcium release and PP1alpha in a mechanism for 4-hydroxytamoxifen-induced cytotoxicity.
Bollig, A; Kuo, TH; Liao, JD; Thakur, A; Wu, J; Xu, L, 2007
)
0.92
"Treatment with tamoxifen or identical placebo tablets for up to 3 weeks. "( Protein kinase C inhibition in the treatment of mania: a double-blind, placebo-controlled trial of tamoxifen.
Ankerst, DP; Guleryuz, S; Ongür, D; Renshaw, PF; Yildiz, A, 2008
)
0.92
"Treatment with tamoxifen resulted in significantly elevated levels of cortisol throughout the period of treatment; this effect was probably solely due to an increase in transcortin levels."( Effects of tamoxifen on the serum levels of oestrogens and adrenocortical steroids in postmenopausal breast cancer patients.
Carlström, K; Sköldefors, H; Theve, NO; Wallgren, A; Wilking, N, 1982
)
0.99
"Pre-treatment with tamoxifen prevented the acute anti-gonadotropic effect of NET and GnRH administration to NET treated rats resulted in an abolishment of the pituitary responsiveness in terms of LH."( Estrogen-like effects of norethisterone on the hypothalamic pituitary unit of ovariectomized rats.
Larrea, F; Moctezuma, O; Pérez-Palacios, G, 1984
)
0.59
"Treatment with tamoxifen over a 4-day period also augmented pituitary responsiveness but only at the lowest dose (0.5 mg/kg); no effect on serum LH concentrations was observed."( Effects of chronic treatment with oestrogen, an oestrogen antagonist and a potent luteinizing hormone releasing hormone agonist analogue on pituitary responsiveness to luteinizing hormone releasing hormone in the rat.
Hall, JM; Whitehead, SA, 1983
)
0.61
"Treatment with Tamoxifen did not decrease serum prolactin in the luteectomized rats but lactose synthetase was reduced to values similar to that obtained in ovariectomized rats."( Effect of estrogen and placental lactogen on lactogenesis in pregnant rats.
Bussmann, LE; Deis, RP; Koninckx, A, 1983
)
0.61
"Treatment with tamoxifen revealed no side effects regarding sexual behaviour, development of gynecomastia or nipple pains."( Results of treatment with tamoxifen in oligozoospermic men.
Danner, Ch; Frick, J; Maier, F, 1983
)
0.91
"Treatment with Tamoxifen for 66 days beginning 33 days after carcinogen treatment reduced (p less than 0.05) the incidence of mammary carcinomas by 65%; CB-154 treatment, during the same time period, did not significantly effect the final yield of mammary carcinomas."( 2-bromo-alpha-ergocryptine (CB-154) and tamoxifen (ICI 46,474) induced suppression of the genesis of mammary carcinomas in female rats treated with 7,12-dimethylbenzanthracene (DMBA): a comparison.
Brown, CK; Goodrich-Smith, M; Johnson, D; Mackie, D; Welsch, CW, 1982
)
0.87
"Pretreatment with tamoxifen resulted in a dose-dependent decrease in the proportion of rapidly cycling cells and an increase in the proportion of cells with slow G1 transit times."( Cell proliferation kinetics of MCF-7 human mammary carcinoma cells in culture and effects of tamoxifen on exponentially growing and plateau-phase cells.
Hall, RE; Sutherland, RL; Taylor, IW, 1983
)
0.81
"Rats treated with tamoxifen for 3 months but not promoted with phenobarbital also developed liver tumors over a longer period of time."( Tamoxifen induces short-term cumulative DNA damage and liver tumors in rats: promotion by phenobarbital.
Carthew, P; De Matteis, F; Dorman, BM; Edwards, RE; Heydon, RT; Martin, EA; Smith, LL; White, IN, 1995
)
2.06
"Treatment with tamoxifen, an anti-calmodulin drug, suppressed tumor takes in the recipient mice with tamoxifen-dose-dependent fashion."( A murine model for bone marrow metastasis established by an i.v. injection of C-1300 neuroblastoma in A/J mice.
Ando, K; Chen, YJ; Iwakawa, M; Koike, S; Ohkawa, H, 1994
)
0.63
"Treatment with tamoxifen on days 3 and 4, or given daily from day 17 onwards did not modify prolactin concentrations but diminished serum GH concentrations at 08.00 on day 5 and on days 19-22, with the exception of a peak on day 22 (08.00 h)."( Correlation of growth hormone secretion during pregnancy with circulating prolactin in rats.
Deis, RP; Jahn, GA; Rastrilla, AM, 1993
)
0.63
"Treatment with tamoxifen alone also caused a reduction in tumor volume, but had no effect on final incidence or number of mammary tumors."( Effect of conjoint administration of tamoxifen and high-dose radiation on the development of mammary carcinoma.
Furmanski, P; Kantorowitz, DA; Thompson, HJ, 1993
)
0.9
"Treatment with tamoxifen resulted in uterine luminal and glandular epithelial hypertrophy and basally located nuclei by 36 h."( Tamoxifen-induced proto-oncogene expression persists in uterine endometrial epithelium.
Khan, SA; Nephew, KP; Polek, TC, 1996
)
2.08
"Treatment with tamoxifen reversed the E2-inhibition of expression of the message."( Estrogen regulation of JE/MCP-1 mRNA expression in fibroblasts.
Dy, PW; Faunce, DE; Frazier-Jessen, MR; Kovacs, EJ; Mott, FJ; Ramer-Quinn, DS, 1996
)
0.63
"Untreated or tamoxifen-treated ovariectomised mice were injected with FGF-transfected cells, treated with AGM-1470 or PPS, and tumour growth and metastasis analysed."( Effects of AGM-1470 and pentosan polysulphate on tumorigenicity and metastasis of FGF-transfected MCF-7 cells.
Gottardis, MM; Kern, FG; Kharbanda, S; Lippman, ME; Liu, Y; McLeskey, SW; Trock, BJ; Zhang, L, 1996
)
0.65
"Treatment with tamoxifen (40 mg/day) did not induce clinical manifestations of sex hormone imbalance."( Oestradiol and testosterone blood levels in patients with viral cirrhosis and hepatocellular carcinoma.
Daniele, B; Esposito, G; Fiore, F; Galati, MG; Pergola, M; Pignata, S; Ricchi, P; Vallone, P, 1997
)
0.64
"Treatment with tamoxifen led to a significant reduction in the PE to PE+PC peak amplitude ratio in the tumors under consideration."( Hormonally induced modulation in the phosphate metabolites of breast cancer: analysis of in vivo 31P MRS signals with a modified prony method.
Barone, P; Degani, H; Furman, E; Guidoni, L; Ragona, R; Viti, V, 1997
)
0.64
"The treatment of tamoxifen, widely used as adjuvant chemotherapy for breast cancer, increases significantly the risk of developing endometrial cancer. "( Miscoding potential of tamoxifen-derived DNA adducts: alpha-(N2-deoxyguanosinyl)tamoxifen.
Dasaradhi, L; Shibutani, S, 1997
)
0.95
"Pre-treatment with tamoxifen (1-20 microM) inhibits 3H-AA release stimulated by both these agents and again the presence of excess estradiol does not reverse this effect."( Tamoxifen inhibits the release of arachidonic acid stimulated by thapsigargin in estrogen receptor-negative A549 cells.
Choudhury, Q; Croxtall, JD; Flower, RJ; White, JO, 1997
)
2.06
"Treatment with tamoxifen is associated with reduced incidence of myocardial infarction. "( Tamoxifen reduces plasma homocysteine levels in healthy women.
Baglietto, L; Bettega, D; Cattaneo, M; Costa, A; Decensi, A; Mannucci, PM; Robertson, C; Zighetti, ML, 1998
)
2.1
"Treatment with tamoxifen alone had no effect on either gene expression or the density of binding sites."( Effects of tamoxifen on serotonin transporter and 5-hydroxytryptamine(2A) receptor binding sites and mRNA levels in the brain of ovariectomized rats with or without acute estradiol replacement.
Fink, G; Fritzemeier, KH; Grant, KE; Hegele-Hartung, C; Rosie, R; Sumner, BE, 1999
)
1.03
"Treatment with tamoxifen resulted in an improvement in outcome (EFS: RR = 0.81; 95% CI, 0.61 to 1.07, OS: RR = 0.74; 95% CI, 0.55 to 1.0) although it proved not significant."( Randomized 2 x 2 trial evaluating hormonal treatment and the duration of chemotherapy in node-positive breast cancer patients: an update based on 10 years' follow-up. German Breast Cancer Study Group.
Bastert, G; Beyerle, C; Bojar, H; Neumann, RL; Sauerbrei, W; Schmoor, C; Schumacher, M, 2000
)
0.65
"Treatment with tamoxifen increased the risk of endometrial cancers in breast cancer patients and women participating in the chemoprevention study. "( Identification of tamoxifen-DNA adducts induced by alpha-acetoxy-N-desmethyltamoxifen.
Kitagawa, M; Ravindernath, A; Rieger, R; Shibutani, S; Suzuki, N; Terashima, I; Umemoto, A, 2000
)
0.99
"Treatment with tamoxifen or raloxifene analog LY 326315 reduced leiomyoma incidence by 40-60% and reduced the size of remaining tumors."( Preclinical evidence for therapeutic efficacy of selective estrogen receptor modulators for uterine leiomyoma.
Burroughs, KD; Davis, B; Everitt, JI; Fuchs-Young, R; Sowell, K; Walker, CL,
)
0.47
"Pretreatment with tamoxifen alone had no effect on arteriolar diameter but inhibited estrogen-induced vasodilation (P < 0.001)."( Effects of estrogen on cerebral blood flow and pial microvasculature in rabbits.
Agnew, DM; Hurn, PD; Littleton-Kearney, MT; Traystman, RJ, 2000
)
0.63
"Treatment with tamoxifen or ICI 182,780 of 3-week BDL rats inhibited cholangiocyte proliferation and induced overexpression of Fas antigen and apoptosis in cholangiocytes."( Estrogens stimulate proliferation of intrahepatic biliary epithelium in rats.
Alpini, G; Alvaro, D; Baiocchi, L; Folli, F; Franchitto, A; Gaudio, E; Glaser, SS; Le Sage, G; Onori, P; Perego, L; Svegliata Baroni, G, 2000
)
0.65
"Treatment with tamoxifen, known in restoration of tumor suppressor function and on induction of programmed cell death (apoptosis), after OTA administration, had no significant inhibition effect on the incidence of apoptotic bodies in liver."( Significance of apoptosis and its relationship to antioxidants after ochratoxin A administration in mice.
Ali-Vehmas, T; Atroshi, F; Biese, I; Rizzo, A; Saari, S; Saloniemi, H; Veijalainen, P,
)
0.47
"Treatment with tamoxifen added only marginal benefit while causing unacceptable side effects. "( The role of tamoxifen in the treatment of symptomatic uterine leiomyomata -- a pilot study.
Debby, A; Ginath, S; Glezerman, M; Rotmensch, S; Sadan, O; Sofer, D; Zakut, H, 2001
)
1.04
"Pretreatment with tamoxifen (TAM) 10 micromol/L, an inhibitor of estrogen receptor, did not block the effect of E2 on CBA."( 17 beta-Estradiol inhibits carotid sinus baroreceptor activity in anesthetized male rats.
Fan, ZZ; He, RR; Wang, S, 2001
)
0.63
"Treatment with tamoxifen inhibited tumor growth and their malignance: the number of rats without malignant tumors significantly increased compared to controls, 27.3% and 5.6%, respectively."( Soluble low-molecular-mass tumor-associated antigens promote the suppression of rat mammary tumors by tamoxifen and prevent its toxic effect.
Ben-Hur, H; Kossoy, G; Zusman, I, 2002
)
0.87
"Treatment with Tamoxifen for 2 weeks resulted in a small, but significant, decrease in IGF-I levels, but increase in the plasma concentration of IGFBP-I."( The effect of endocrine therapy with medroxyprogesterone acetate, 4-hydroxyandrostenedione or tamoxifen on plasma concentrations of insulin-like growth factor (IGF)-I, IGF-II and IGFBP-1 in women with advanced breast cancer.
Christodoulides, A; Ghilchik, MW; Koistinen, R; Reed, MJ; Seppälä, M; Teale, JD, 1992
)
0.84
"Treatment with tamoxifen in order to raise the serum AAT level only resulted in an insufficient increase."( A new variant of alpha-1-antitrypsin deficiency (Siiyama) associated with pulmonary emphysema.
Ichioka, M; Marumo, F; Miyahara, Y; Miyake, K; Nouchi, T; Nukiwa, T; Seyama, K; Shinada, H; Takabe, K; Tsukimoto, K, 1992
)
0.62
"Treatment with tamoxifen (TM), alone or in combination with cyclophosphamide, methotrexate, and fluorouracil (CMF), was used as an adjuvant to surgery in 433 patients with stage I, II, or III(T3a) breast cancer. "( Adjuvant therapy with tamoxifen in operable breast cancer. 10 year results of the Naples (GUN) study.
Bianco, AR; D'Istria, M; De Placido, S; Delrio, G; Gallo, C; Marinelli, A; Pagliarulo, C; Petrella, G, 1988
)
0.94
"Treatment with tamoxifen was associated with lower concentrations of plasma IGF-I (0.48 +/- 0.3 unit/ml in treated versus 1.03 +/- 0.6 units/ml in nontreated patients, P less than 0.01)."( Effect of tamoxifen on plasma insulin-like growth factor I in patients with breast cancer.
Colletti, RB; Copeland, KC; Devlin, JT; Roberts, JD, 1989
)
1.02
"Treatment with tamoxifen did not alter serum levels of testosterone in male rats during the perinatal period, but it inhibited development and differentiation of the SDN-POA."( Pre- and postnatal influence of an estrogen antagonist and an androgen antagonist on differentiation of the sexually dimorphic nucleus of the preoptic area in male and female rats.
Coquelin, A; Davis, F; Döhler, KD; Gorski, RA; Hines, M; Jarzab, B; Shryne, JE; Sickmöller, PM, 1986
)
0.61
"Treatment with tamoxifen resulted in a dose-dependent reduction in cancer incidence, and the number of cancers induced and significantly prolonged the median cancer-free time."( Effect of D,L-2-difluoromethylornithine and endocrine manipulation on the induction of mammary carcinogenesis by 1-methyl-1-nitrosourea.
Ronan, AM; Thompson, HJ, 1986
)
0.61
"Treatment with tamoxifen before or during the period of gland genesis also reduced uterine responsiveness to a single dose of E2 as measured by both uterine weight gain (after a 24-h exposure on days 14, 19, 22, and 26) and the pattern of E2-induced ODC activity in 26-day-old rats."( Inhibition of rat uterine gland genesis by tamoxifen.
Branham, WS; Medlock, KL; Nelson, CJ; Ridlon, E; Sheehan, DM; Zehr, DR, 1985
)
0.87

Toxicity

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.

ExcerptReferenceRelevance
" The 58-day ip LD50 of TCDD was reduced from 330 to 185 micrograms/kg by sc administration of 1 mg/kg/day tamoxifen."( 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
)
0.73
" An exogenous P-450-dependent hepatic biotransforming (catechol-generating) system failed to alter either the incidence of observed toxic effects or measured growth parameters."( Embryotoxicity induced by diethylstilbestrol in vitro.
Beyer, BK; Fantel, AG; Greenaway, JC; Juchau, MR, 1987
)
0.27
" Adverse effects were experienced in 3 (5."( [Efficacy and safety of high dose NK 622 (toremifene citrate) in tamoxifen failed patients with breast cancer].
Abe, O; Asaishi, K; Izuo, M; Nomura, Y; Tominaga, T, 1993
)
0.52
"Long-term tamoxifen has generally only few and usually mild adverse side effects."( Long-term toxicity of tamoxifen.
Rutqvist, LE, 1993
)
1
" However, tamoxifen alone caused significant toxic effects to TSGH-8301 at > or = 40 microM and to HTB9 at > or = 30 microM."( Combined cytotoxic effects of tamoxifen and chemotherapeutic agents on bladder cancer cells: a potential use in intravesical chemotherapy.
Cheng, AL; Hsieh, CY; Hsieh, TS; Lai, MK; Pu, YS; Su, IJ; Tsai, TC; Tseng, NF, 1996
)
0.98
"Tamoxifen enhanced the cytotoxicity of chemotherapeutic agents largely through its toxic effects on the bladder cancer cells."( Combined cytotoxic effects of tamoxifen and chemotherapeutic agents on bladder cancer cells: a potential use in intravesical chemotherapy.
Cheng, AL; Hsieh, CY; Hsieh, TS; Lai, MK; Pu, YS; Su, IJ; Tsai, TC; Tseng, NF, 1996
)
2.03
" In these experiments, a 24-h pretreatment with 15 and 50 nM 17 beta-estradiol significantly reduced cellular lactate dehydrogenase (LDH) release from primary cortical neurons, indicating that neurons treated with 17 beta-estradiol were protected from a toxic glutamate exposure."( Estrogen protects primary cortical neurons from glutamate toxicity.
Dorsa, DM; Rogers, KL; Singer, CA; Strickland, TM, 1996
)
0.29
"The main adverse effects of tamoxifen, aspirin, oral contraceptives (OCs) and retinoids used as chemopreventive agents in humans are reviewed and quantified here."( Adverse effects of preventive therapy in humans.
Garattini, S; La Vecchia, C; Tavani, A, 1996
)
0.59
" Most patients treated with tamoxifen have minimal adverse effects."( Tamoxifen in postmenopausal women a safety perspective.
Kimmick, GG; Muss, HB; Robinson, E, 1996
)
2.03
" Most of the adverse effects of toremifene are related to its activity at estrogen receptors and include hot flashes, vaginal discharge and nausea."( Toremifene in postmenopausal breast cancer. Efficacy, safety and cost.
Ala-Fossi, SL; Mäenpää, JU, 1997
)
0.3
" It is generally well tolerated, apart from certain well-documented adverse effects concerning mainly the reproductive organs, the most worrying being its carcinogenicity for the endometrium."( Tamoxifen and ocular toxicity.
Ah-Song, R; Sasco, AJ, 1997
)
1.74
" These results provide support for the toxic fragment hypothesis whereby cleavage of atrophin-1 by caspases may be an important step in the pathogenesis of DRPLA."( Cleavage of atrophin-1 at caspase site aspartic acid 109 modulates cytotoxicity.
Andrusiak, RL; Bredesen, DE; Ellerby, LM; Hackam, AS; Hayden, MR; Margolis, RL; Propp, SS; Ross, CA; Salvesen, GS; Sharp, AH; Wellington, CL; Wood, JD, 1999
)
0.3
" The guinea pig is the most susceptible mammal known, with an LD50 in the range 1-2 micrograms TCDD/kg, whereas the hamster is the most resistant species with an LD50 greater than 3000 micrograms/kg."( Interspecies differences in cancer susceptibility and toxicity.
Hengstler, JG; Oesch, F; Steinberg, P; Van der Burg, B, 1999
)
0.3
"Prompt reporting of symptoms and yearly ophthalmic examinations are mandatory in patients on tamoxifen to detect toxic effects while these are still reversible."( Ocular toxicity in low-dose tamoxifen: a prospective study.
Bashshur, Z; Khalil, A; Noureddin, BN; Salem, Z; Seoud, M; Shamseddin, A, 1999
)
0.82
" Adverse drug effects were suspected due to the presence of yellow-white dots in the paramacular region and the fovea and by modifications of the retinal epithelial pigments."( [Birdshot chorioretinopathy associated with tamoxifen retinal toxicity].
Badet, JC; Naoun-Hubert, I; Rozot, P; Sommer, S; Zaoui, M, 2000
)
0.57
" However, the use of potentially toxic genes, such as tumor suppressor genes or apoptotic genes, needs controllable transgene activation."( Improved safety through tamoxifen-regulated induction of cytotoxic genes delivered by Ad vectors for cancer gene therapy.
Crespo, F; Esche, H; Pützer, BM; Stiewe, T, 2000
)
0.61
" The levels of this toxic metabolite and its corresponding biliary rate constant were reduced by approximately 50%."( Effect of tamoxifen pretreatment on the pharmacokinetics, metabolism and cardiotoxicity of doxorubicin in female rats.
Boroujerdi, M; Vaidyanathan, S, 2000
)
0.71
" The subjective side-effect profile was similar in both treatment groups."( Safety and efficacy results of a randomized trial comparing adjuvant toremifene and tamoxifen in postmenopausal patients with node-positive breast cancer. Finnish Breast Cancer Group.
Blanco, G; Flander, M; Hietanen, P; Holli, K; Joensuu, H; Kataja, V; Pukkala, E; Valavaara, R, 2000
)
0.53
"The side-effect profile of toremifene resembles that of tamoxifen."( Safety and efficacy results of a randomized trial comparing adjuvant toremifene and tamoxifen in postmenopausal patients with node-positive breast cancer. Finnish Breast Cancer Group.
Blanco, G; Flander, M; Hietanen, P; Holli, K; Joensuu, H; Kataja, V; Pukkala, E; Valavaara, R, 2000
)
0.78
" The 4-HPR and safingol combination was cytotoxic in low-oxygen conditions and was minimally toxic to normal fibroblasts and bone marrow myeloid progenitor cells."( Synergistic cytotoxicity in solid tumor cell lines between N-(4-hydroxyphenyl)retinamide and modulators of ceramide metabolism.
Billups, C; Cabot, MC; Maurer, BJ; Melton, L; Reynolds, CP, 2000
)
0.31
" The most frequently reported side effect was hot flushes, and the most worrisome gynecologic side effect was a two- to three-fold increased risk of endometrial cancer in postmenopausal women."( Tamoxifen treatment and gynecologic side effects: a review.
De Vries, EG; Hollema, H; Mourits, MJ; Ten Hoor, KA; Van der Zee, AG; Willemse, PH, 2001
)
1.75
" One patient experienced a life-threatening adverse reaction within minutes of receiving the first dose."( Pegylated liposomal doxorubicin: tolerability and toxicity.
Goram, AL; Richmond, PL, 2001
)
0.31
"Determination of potential drug toxicity and side effect in early stages of drug development is important in reducing the cost and time of drug discovery."( Prediction of potential toxicity and side effect protein targets of a small molecule by a ligand-protein inverse docking approach.
Chen, YZ; Ung, CY, 2001
)
0.31
" Serum protected the cells from the toxic effects of the drugs."( 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
)
0.31
" Five micrograms per kilogram per day represented the No Observed Adverse Effect Level (NOAEL) in males and the No Observed Effect Level (NOEL) in females."( Tamoxifen: 28-day oral toxicity study in the rat based on the Enhanced OECD Test Guideline 407 to detect endocrine effects.
Barale-Thomas, E; Bars, R; Espuña, G; Kennel, P; Pallen, C, 2003
)
1.76
" Although published information about the side effects of AIs is scarce, it is likely that they will have adverse effects on bone and possibly also on lipid metabolism."( Safety issues surrounding the use of aromatase inhibitors in breast cancer.
Dixon, JM; Jackson, J; Miller, WR, 2003
)
0.32
" Among the side effects of therapy that were observed in metastatic trials, AIs have shown less vascular and uterine adverse events than tamoxifen."( Origin and characteristics of adverse events in aromatase inhibition therapy for breast cancer.
Dowsett, M, 2003
)
0.52
" No significant adverse events related to the study drug were observed clinically or biochemically."( Activity and safety of the antiestrogen EM-800, the orally active precursor of acolbifene, in tamoxifen-resistant breast cancer.
Candas, B; Champagne, P; Cusan, L; Diamond, P; Drolet, Y; Dufresne, J; Jolivet, J; L'Espérance, B; Labrie, C; Labrie, F; Latreille, J; Laverdière, J; Panasci, L; Pollak, M; Potvin, M; Provencher, L; Robert, J; Roy, J; Samson, B; Yelle, L, 2004
)
0.54
" Our results support the view that metabolic activation of tamoxifen in liver cells may proceed via CYP450-mediated metabolism and subsequent sulfotransferase-mediated activation and point to the role of CYP3A4 and dehydroepiandrosterone sulfotransferase in adverse tamoxifen effects."( Tamoxifen cytotoxicity in hepatoblastoma cells stably transfected with human CYP3A4.
Braszko, JJ; Holownia, A, 2004
)
2.01
" Results of the analysis showed that women who experienced at least one TAM-related side effect had significantly higher levels of TAM than women not experiencing any TAM-related side effects."( Association of tamoxifen (TAM) and TAM metabolite concentrations with self-reported side effects of TAM in women with breast cancer.
Danton, M; Flaws, JA; Gallicchio, L; Lewis, LM; Lim, CK; Lord, G; Tkaczuk, K, 2004
)
0.68
" The incidence and severity of adverse events were assessed by physical examination and patient reporting."( Pilot study evaluating the pharmacokinetics, pharmacodynamics, and safety of the combination of exemestane and tamoxifen.
Asnis, AG; Duncan, B; Francis, D; Hortobagyi, GN; Rivera, E; Schaaf, LJ; Valero, V, 2004
)
0.54
" All drug-related adverse events were grades 1 or 2; none was unexpected."( Pilot study evaluating the pharmacokinetics, pharmacodynamics, and safety of the combination of exemestane and tamoxifen.
Asnis, AG; Duncan, B; Francis, D; Hortobagyi, GN; Rivera, E; Schaaf, LJ; Valero, V, 2004
)
0.54
" Our current study suggests that adjuvant tamoxifen therapy reverses the adverse effects of chemotherapy-induced ovarian failure on total and LDL cholesterol and even lowers their serum levels below the baseline."( Tamoxifen treatment reverses the adverse effects of chemotherapy-induced ovarian failure on serum lipids.
Blomqvist, C; Elomaa, I; Saarto, T; Taskinen, MR; Vehmanen, L, 2004
)
2.03
" In the present study, estrogenic and toxic effects of PCBs on embryonic chicken ovarian development were evaluated by a germ-somatic cell co-culture system."( Estrogenic and toxic effects of polychlorinated biphenyls on cultured ovarian germ cells of embryonic chickens.
Xie, M; Zhang, C, 2004
)
0.32
"In vitro assays involving primary cells are used routinely to evaluate organ-specific toxic effects, for instance, the use of primary hepatocytes to evaluate hepatotoxicity."( A novel in vitro system, the integrated discrete multiple organ cell culture (IdMOC) system, for the evaluation of human drug toxicity: comparative cytotoxicity of tamoxifen towards normal human cells from five major organs and MCF-7 adenocarcinoma breast
Bode, C; Li, AP; Sakai, Y, 2004
)
0.52
" Clinical trials have begun to define the role of these agents and their unique side-effect profiles."( Advances in endocrine therapy for breast cancer: considering efficacy, safety, and quality of life.
Harwood, KV, 2004
)
0.32
" The AIs have differing pharmacological profiles, which may translate into dissimilar adverse event profiles in the adjuvant treatment setting, but patient follow-up in most trials is relatively short to make a valid comparison."( Safety considerations of adjuvant therapy in early breast cancer in postmenopausal women.
Gradishar, WJ, 2005
)
0.33
"Many adverse drug reactions are caused by the cytochrome P450 (CYP) dependent activation of drugs into reactive metabolites."( An in vitro approach to detect metabolite toxicity due to CYP3A4-dependent bioactivation of xenobiotics.
Grossi, P; Kanter, Rd; Monaci, S; Monshouwer, M; Turlizzi, E; Vignati, L, 2005
)
0.33
"Ocular toxicity during adjuvant therapy is a common side effect mainly represented by irritative symptoms due to chemotherapy."( Ocular toxicity during adjuvant chemoendocrine therapy for early breast cancer: results from International Breast Cancer Study Group trials.
Castiglione-Gertsch, M; Coates, AS; Collins, J; Crivellari, D; Gelber, RD; Gianni, L; Goldhirsch, A; Holmberg, SB; Li, S; Panzini, I; Ravaioli, A, 2006
)
0.33
" Thirty-six patients have dropped out of the study, 17 because of adverse events and 19 for various other reasons."( Preliminary results on safety and activity of a randomized, double-blind, 2 x 2 trial of low-dose tamoxifen and fenretinide for breast cancer prevention in premenopausal women.
Bonanni, B; Cazzaniga, M; Decensi, A; Formelli, F; Franchi, D; Guerrieri-Gonzaga, A; Gulisano, M; Intra, M; Johansson, H; Johnson, K; Latronico, A; Mora, S; Pelosi, G; Robertson, C; Serrano, D, 2006
)
0.55
"The combination of low-dose tamoxifen and fenretinide is safe but not synergistic in lowering IGF-I levels in premenopausal women."( Preliminary results on safety and activity of a randomized, double-blind, 2 x 2 trial of low-dose tamoxifen and fenretinide for breast cancer prevention in premenopausal women.
Bonanni, B; Cazzaniga, M; Decensi, A; Formelli, F; Franchi, D; Guerrieri-Gonzaga, A; Gulisano, M; Intra, M; Johansson, H; Johnson, K; Latronico, A; Mora, S; Pelosi, G; Robertson, C; Serrano, D, 2006
)
0.84
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
"One of the most attractive approaches to disease prevention involves the use of natural antioxidants to protect tissue against toxic injury."( Attenuation of tamoxifen-induced hepatotoxicity by taurine in mice.
Banerjee, BD; Parvez, S; Raisuddin, S; Rehman, H; Tabassum, H, 2006
)
0.69
" This paper summarizes the adverse events reported in third-generation AI trials and comments on the appropriate management of these drug-induced adverse events in patients."( Incidence and management of side effects associated with aromatase inhibitors in the adjuvant treatment of breast cancer in postmenopausal women.
Mouridsen, HT, 2006
)
0.33
"The most commonly reported adverse events associated with adjuvant AI therapy include hot flushes and musculoskeletal complaints/arthralgia."( Incidence and management of side effects associated with aromatase inhibitors in the adjuvant treatment of breast cancer in postmenopausal women.
Mouridsen, HT, 2006
)
0.33
" We calculated a risk-benefit analysis using the two global indices for the Women's Health Initiative and for Disease-Free Survival and Serious Adverse Events."( Comprehensive side-effect profile of anastrozole and tamoxifen as adjuvant treatment for early-stage breast cancer: long-term safety analysis of the ATAC trial.
Buzdar, A; Cuzick, J; Distler, W; Hoctin-Boes, G; Houghton, J; Howell, A; Locker, GY; Nabholtz, JM; Wale, C, 2006
)
0.58
"At median follow-up of 68 months (range 1-93), treatment-related adverse events occurred significantly less often with anastrozole than with tamoxifen (1884 [61%] vs 2117 [68%]; p<0."( Comprehensive side-effect profile of anastrozole and tamoxifen as adjuvant treatment for early-stage breast cancer: long-term safety analysis of the ATAC trial.
Buzdar, A; Cuzick, J; Distler, W; Hoctin-Boes, G; Houghton, J; Howell, A; Locker, GY; Nabholtz, JM; Wale, C, 2006
)
0.78
"Anastrozole is tolerated better than tamoxifen by postmenopausal women with early-stage breast cancer, and results in fewer serious adverse events."( Comprehensive side-effect profile of anastrozole and tamoxifen as adjuvant treatment for early-stage breast cancer: long-term safety analysis of the ATAC trial.
Buzdar, A; Cuzick, J; Distler, W; Hoctin-Boes, G; Houghton, J; Howell, A; Locker, GY; Nabholtz, JM; Wale, C, 2006
)
0.86
" Given this known side effect associated with tamoxifen therapy, newer endocrine therapies such as the third-generation aromatase inhibitors have been compared to tamoxifen also in terms of their uterine effects."( Endometrial safety of third generation aromatase inhibitors versus tamoxifen in breast cancer patients.
Morales, L; Neven, P; Paridaens, R; Timmerman, D, 2006
)
0.83
"Bone loss may be a potential side effect of implementing aromatase inhibitors in the adjuvant setting."( Bone safety of aromatase inhibitors versus tamoxifen.
Lønning, PE, 2006
)
0.6
" Three other patients had ocular toxic effects, with two cases of refractile retinal crystals and one case of keratopathy."( Multifocal electroretinography, color discrimination and ocular toxicity in tamoxifen use.
Berezovsky, A; Motono, M; Salomão, SR; Watanabe, SE, 2007
)
0.57
" Some degree of color vision loss and ocular toxic effects were found in a few cases of this cohort suggesting that women using tamoxifen should receive an eye exam at least as often as recommended for middle-aged people."( Multifocal electroretinography, color discrimination and ocular toxicity in tamoxifen use.
Berezovsky, A; Motono, M; Salomão, SR; Watanabe, SE, 2007
)
0.77
"The optic nerve is quite vulnerable to the toxic effect of drugs."( [Toxicity of recent and less recent drugs on the optic nerve. Does Viagra cause blindness?].
Cordonnier, M, 2007
)
0.34
"We reviewed the most recent systemic drugs used in Belgium causing toxic corneal side effects."( [Toxic effects of medications on the cornea].
Ravet, O, 2007
)
0.34
" In published clinical trials and in clinical practice, adverse events (AEs) constitute the main reason for nonadherence to endocrine treatment."( Recognition and management of treatment-related side effects for breast cancer patients receiving adjuvant endocrine therapy.
Cella, D; Fallowfield, LJ, 2008
)
0.35
" As AIs lack estrogenic activity, they are not associated with these serious adverse events."( Safety profiles of tamoxifen and the aromatase inhibitors in adjuvant therapy of hormone-responsive early breast cancer.
Perez, EA, 2007
)
0.67
"Tamoxifen has been found to be safe and effective in gynecological cancer patients with normal renal function."( Tamoxifen is safe and effective in gynecological cancer patients with renal dysfunction.
Gershenson, DM; Jaishuen, A; Kavanagh, JJ; Li, Y; Sirisabya, N; Zheng, HG,
)
3.02
" Generally, adverse events with AIs are predictable and manageable, whereas tamoxifen may be associated with life-threatening events in a minority of patients."( Safety of aromatase inhibitors in the adjuvant setting.
Perez, EA, 2007
)
0.57
"Previous analyses of adjuvant studies of aromatase inhibitors versus tamoxifen, including the Breast International Group (BIG) 1-98 study, have suggested a small numerical excess of cardiac adverse events (AEs) on aromatase inhibitors, a reduction in the incidence of hypercholesterolemia on tamoxifen, and significantly higher incidence of thromboembolic AEs on tamoxifen."( Cardiovascular adverse events during adjuvant endocrine therapy for early breast cancer using letrozole or tamoxifen: safety analysis of BIG 1-98 trial.
Castiglione-Gertsch, M; Coates, AS; Colleoni, M; Forbes, JF; Gelber, RD; Goldhirsch, A; Keshaviah, A; Mauriac, L; Mouridsen, H; Paridaens, R; Price, KN; Rabaglio, M; Smith, I; Sun, Z; Thürlimann, B, 2007
)
0.79
" The rates of severe taxane-related toxic effects and thrombocytopenia, although low overall, are significantly increased with the dose-dense sequential regimen."( Postoperative dose-dense sequential chemotherapy with epirubicin, paclitaxel and CMF in patients with high-risk breast cancer: safety analysis of the Hellenic Cooperative Oncology Group randomized phase III trial HE 10/00.
Bafaloukos, D; Briasoulis, E; Dafni, U; Dimitrakakis, K; Dimopoulos, AM; Fountzilas, G; Gogas, H; Kalofonos, HP; Karanikiotis, C; Karina, M; Linardou, H; Makrantonakis, P; Markopoulos, C; Papadimitriou, C; Papakostas, P; Pectasides, D; Pisanidis, N; Polichronis, A; Samantas, E; Skarlos, D; Stathopoulos, GP; Tzorakoeleftherakis, E; Varthalitis, I; Xiros, N, 2008
)
0.35
" Moreover, patients who were positive for COX-2 predicted adverse effects of tamoxifen (P=0."( Cyclooxygenase-2 predicts adverse effects of tamoxifen: a possible mechanism of role for nuclear HER2 in breast cancer patients.
Crotty, TB; Dillon, MF; Hill, AD; Kelly, G; McDermott, E; McIlroy, M; Redmond, AM; Stafford, AT; Young, LS, 2008
)
0.83
"To experimentally test whether using pictographs (image matrices), incremental risk formats, and varied risk denominators would influence perceptions and comprehension of side effect risks in an online decision aid about prophylactic use of tamoxifen to prevent primary breast cancers."( Communicating side effect risks in a tamoxifen prophylaxis decision aid: the debiasing influence of pictographs.
Derry, HA; Fagerlin, A; McClure, JB; Pitsch, RK; Smith, DM; Stark, A; Ubel, PA; Zikmund-Fisher, BJ, 2008
)
0.8
" However, the adverse events associated with AIs are different from those associated with SERMs."( Safety profiles of aromatase inhibitors and selective estrogen-receptor modulators in the treatment of early breast cancer.
Iwase, H; Yamamoto, Y, 2008
)
0.35
"Results of the Arimidex, Tamoxifen, Alone or in Combination (ATAC) trial have shown that tamoxifen is associated with a significantly higher incidence of gynecologic adverse events than anastrozole."( A lower incidence of gynecologic adverse events and interventions with anastrozole than with tamoxifen in the ATAC trial.
Baum, M; Cuzick, J; Distler, W; Duffy, SR; Howell, A, 2009
)
0.88
"This was a retrospective analysis of all gynecologic adverse events and interventions conducted in patients receiving anastrozole or tamoxifen in the main ATAC trial database."( A lower incidence of gynecologic adverse events and interventions with anastrozole than with tamoxifen in the ATAC trial.
Baum, M; Cuzick, J; Distler, W; Duffy, SR; Howell, A, 2009
)
0.78
"Women taking tamoxifen experienced significantly more gynecologic adverse events than those taking anastrozole (34."( A lower incidence of gynecologic adverse events and interventions with anastrozole than with tamoxifen in the ATAC trial.
Baum, M; Cuzick, J; Distler, W; Duffy, SR; Howell, A, 2009
)
0.94
"The lower incidence of gynecologic adverse events and interventions with anastrozole and the early occurrence of these events provide further support for using anastrozole as the initial adjuvant treatment for early hormone receptor-positive breast cancer."( A lower incidence of gynecologic adverse events and interventions with anastrozole than with tamoxifen in the ATAC trial.
Baum, M; Cuzick, J; Distler, W; Duffy, SR; Howell, A, 2009
)
0.57
" Adverse effects of TAM include hepatotoxicity."( Caffeic acid phenethyl ester protects against tamoxifen-induced hepatotoxicity in rats.
Abdel-Naim, AB; Albukhari, AA; El-Beshbishy, HA; Gashlan, HM; Nagy, AA, 2009
)
0.61
" A UK government regulatory publication recommends providing medicine side effect risk information in a combined format, using verbal descriptors accompanied by numerical information."( Communicating the risk of side effects to patients: an evaluation of UK regulatory recommendations.
Carrigan, N; Gardner, PH; Knapp, P; McMillan, B; Raynor, DK; Woolf, E, 2009
)
0.35
"This study, with users of an existing popular patient information website, investigates the effectiveness of presenting medicine side effect risk information in different forms."( Communicating the risk of side effects to patients: an evaluation of UK regulatory recommendations.
Carrigan, N; Gardner, PH; Knapp, P; McMillan, B; Raynor, DK; Woolf, E, 2009
)
0.35
" They were also more accurate at estimating the likelihood of themselves or the average person having any side effect from taking tamoxifen."( Communicating the risk of side effects to patients: an evaluation of UK regulatory recommendations.
Carrigan, N; Gardner, PH; Knapp, P; McMillan, B; Raynor, DK; Woolf, E, 2009
)
0.56
" They also add weight to the growing body of research highlighting the deficiencies in using verbal descriptors for conveying side effect risk, and the strength of using absolute frequency descriptors."( Communicating the risk of side effects to patients: an evaluation of UK regulatory recommendations.
Carrigan, N; Gardner, PH; Knapp, P; McMillan, B; Raynor, DK; Woolf, E, 2009
)
0.35
" Our results confirmed that longterm postoperative therapy with UFT alone was feasible, provided that early adverse events are carefully monitored."( [Safety and compliance with UFT (tegafur and uracil) alone and in combination with hormone therapy in patients with breast cancer].
Noguchi, S; Taguchi, T, 2009
)
0.35
"Tamoxifen is generally considered a safe drug for Indian women with breast cancer."( Tamoxifen use in Indian women--adverse effects revisited.
Alam, N; Ashraf, M; Biswas, J; Gupta, S; Majumdar, S; Mukherjee, KK; Nayak, S,
)
3.02
"To investigate the effectiveness of presenting medicine side effect risk information in different forms, including that proposed by UK guidelines [[1] Medicines and Healthcare products Regulatory Agency."( Perceived risk of tamoxifen side effects: a study of the use of absolute frequencies or frequency bands, with or without verbal descriptors.
Gardner, PH; Knapp, P; McMillan, B; Raynor, DK; Woolf, E, 2010
)
0.69
"Those presented with absolute frequencies demonstrated greater accuracy in estimating 2 of 4 side effects, and of any side effect occurring, than those presented with frequency bands."( Perceived risk of tamoxifen side effects: a study of the use of absolute frequencies or frequency bands, with or without verbal descriptors.
Gardner, PH; Knapp, P; McMillan, B; Raynor, DK; Woolf, E, 2010
)
0.69
"Absolute frequencies outperform frequency bands when presenting side effect risk information."( Perceived risk of tamoxifen side effects: a study of the use of absolute frequencies or frequency bands, with or without verbal descriptors.
Gardner, PH; Knapp, P; McMillan, B; Raynor, DK; Woolf, E, 2010
)
0.69
" Phase 3 clinical data have shown that bazedoxifene is effective in preventing and treating postmenopausal osteoporosis, without adverse effects on the endometrium or breast."( Endometrial safety: a key hurdle for selective estrogen receptor modulators in development.
Goldstein, SR; Pinkerton, JV,
)
0.13
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36
" 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
" The aim of this study was to evaluate the adverse effects when exposing healthy female dogs to tamoxifen."( Evaluation of adverse effects in tamoxifen exposed healthy female dogs.
Bertagnolli, AC; Carneiro, RA; Cassali, GD; Cavalcanti, GA; Figueiredo, MS; Lavalle, GE; Melo, MM; Paes, PR; Souza, AG; Tavares, WL; Viana, FA, 2010
)
0.86
" This meta-analysis suggested that toremifene was as effective as tamoxifen in the adjuvant setting for both perimenopausal and postmenopausal breast cancer patients with similar severe adverse effects to tamoxifen."( Toremifene is an effective and safe alternative to tamoxifen in adjuvant endocrine therapy for breast cancer: results of four randomized trials.
Chen, L; Ding, Q; Liu, XA; Wang, S; Zhou, WB, 2011
)
0.86
" Odds ratios (ORs), 95% confidence intervals (CIs), absolute risks, and the number needed to harm associated with one adverse event were computed for prespecified serious adverse events including cardiovascular disease, cerebrovascular disease, bone fractures, thromboembolic events, endometrial carcinoma and other second cancers not including new breast cancer."( Toxicity of adjuvant endocrine therapy in postmenopausal breast cancer patients: a systematic review and meta-analysis.
Amir, E; Carlsson, L; Niraula, S; Ocaña, A; Seruga, B, 2011
)
0.37
" It is well tolerated with mild adverse effects."( Gynecomastia during imatinib mesylate treatment for gastrointestinal stromal tumor: a rare adverse event.
Liao, G; Liu, H; Yan, Z, 2011
)
0.37
"Health-related quality of life (HRQOL), symptoms of depression, and adverse events (AEs) were compared between Japanese postmenopausal patients with hormone-sensitive breast cancer (BC) who received adjuvant tamoxifen, exemestane, or anastrozole in an open-labeled, randomized, multicenter trial designated as the National Surgical Adjuvant Study of Breast Cancer (N-SAS BC) 04 substudy of the Tamoxifen Exemestane Adjuvant Multinational (TEAM) trial."( Health-related quality of life, psychological distress, and adverse events in postmenopausal women with breast cancer who receive tamoxifen, exemestane, or anastrozole as adjuvant endocrine therapy: National Surgical Adjuvant Study of Breast Cancer 04 (N-
Hozumi, Y; Ohashi, Y; Ohsumi, S; Shimozuma, K; Suemasu, K; Takehara, M; Takei, H, 2012
)
0.77
"Toremifene may be a valid and safe alternative to tamoxifen in premenopausal women with endocrine-responsive breast cancer."( A comparison of survival outcomes and side effects of toremifene or tamoxifen therapy in premenopausal estrogen and progesterone receptor positive breast cancer patients: a retrospective cohort study.
Chen, K; Chen, L; Gu, R; Hu, Y; Jia, W; Jin, L; Li, S; Long, M; Rao, N; Song, E; Su, F; Wu, J; Wu, M; Xiao, Q; Zeng, Y, 2012
)
0.87
" AFB was selective toxic towards the human hepatocytes and relatively noncytotoxic towards 3T3 cells both in the presence and absence of the hepatocytes."( Definition of metabolism-dependent xenobiotic toxicity with co-cultures of human hepatocytes and mouse 3T3 fibroblasts in the novel integrated discrete multiple organ co-culture (IdMOC) experimental system: results with model toxicants aflatoxin B1, cyclo
LaForge, YS; Li, AP; Uzgare, A, 2012
)
0.38
"10), but no differences in hysterectomy rates or other serious adverse event rates were observed."( A double-blind placebo-controlled study to evaluate endometrial safety and gynaecological symptoms in women treated for up to 5 years with tamoxifen or placebo - a substudy for IBIS I Breast Cancer Prevention Trial.
Cuzick, J; Holli, K; Koivisto, AM; Palva, T; Pylkkänen, L; Ranta, H, 2013
)
0.59
" With its very low chronic skin toxicity rates and outstanding long-term results regarding toxicity and local control, IORT with 50 kV X-rays is a safe and effective method for treatment of selected breast cancer patients."( Late radiation toxicity after intraoperative radiotherapy (IORT) for breast cancer: results from the randomized phase III trial TARGIT A.
Gerhardt, A; Keller, A; Kraus-Tiefenbacher, U; Sperk, E; Sütterlin, M; Welzel, G; Wenz, F, 2012
)
0.38
" However, the use of both anastrozole and letrozole appears to be safe with concomitant RT, without increasing the risk of pulmonary fibrosis."( Comparison of the effects of aromatase inhibitors and tamoxifen on radiation-induced lung toxicity: results of an experimental study.
Acar, H; Ata, O; Toy, H; Yavas, C; Yavas, G; Yuce, D, 2013
)
0.64
" Safety assessments included adverse events, cervical Papanicolaou tests, endometrial histology, endometrial thickness, gynecological examination, breast palpation, mammography, physical examination, and clinical safety laboratory assessments."( One-year long-term safety extension study of ospemifene for the treatment of vulvar and vaginal atrophy in postmenopausal women with a uterus.
Bachmann, GA; Lin, VH; Radovich, C; Simon, JA, 2013
)
0.39
"No clinically significant adverse changes in safety assessments were observed in any treatment group."( One-year long-term safety extension study of ospemifene for the treatment of vulvar and vaginal atrophy in postmenopausal women with a uterus.
Bachmann, GA; Lin, VH; Radovich, C; Simon, JA, 2013
)
0.39
"Daily doses of ospemifene 30 mg and ospemifene 60 mg yielded few treatment-emergent adverse events and demonstrated no significant endometrial changes during the 1-year treatment of vulvar and vaginal atrophy in postmenopausal women with a uterus."( One-year long-term safety extension study of ospemifene for the treatment of vulvar and vaginal atrophy in postmenopausal women with a uterus.
Bachmann, GA; Lin, VH; Radovich, C; Simon, JA, 2013
)
0.39
"Tamoxifen is a safe and viable therapeutic option in the treatment of iRPF."( Long-term safety and efficacy of a tamoxifen-based treatment strategy for idiopathic retroperitoneal fibrosis.
Hendriksz, TR; Pelkmans, LG; van Bommel, EF; van Damme, H, 2013
)
2.11
"030) between the numbers of Ultrarapid Metabolizer patients (UM; high activity) with two or more adverse drug reactions to tamoxifen (7/9; 77."( Side effects associated with ultrarapid cytochrome P450 2D6 genotype among women with early stage breast cancer treated with tamoxifen.
Agostino, FD; Alabiso, O; Bellomo, G; Borra, G; Fanello, MR; Forti, L; Meola, S; Nicolotti, C; Pollarolo, P; Rolla, R; Rossi, V; Saggia, C; Stratica, F; Vidali, M, 2012
)
0.79
"Acitretin is a synthetic retinoid used for severe extensive psoriasis and it has been shown to be an effective and a safe therapeutic drug for other diseases including cancer when used in combination with other agents."( Acitretin affects bioenergetics of liver mitochondria and promotes mitochondrial permeability transition: potential mechanisms of hepatotoxicity.
Custódio, JB; Ribeiro, MP; Rocha-Pereira, P; Santos, MS; Santos-Silva, A; Silva, FS, 2013
)
0.39
"The study evaluated the interpretation of, and preferences for, numerical information on side-effect incidence when presented in three different formats."( Evaluating a combined (frequency and percentage) risk expression to communicate information on medicine side effects to patients.
Gardner, P; Knapp, P; McMillan, B; Raynor, DK; Woolf, E, 2013
)
0.39
" They then interpreted information on tamoxifen and its effect on health, and estimates of side-effect frequency, and then stated a preference from the three risk expression formats."( Evaluating a combined (frequency and percentage) risk expression to communicate information on medicine side effects to patients.
Gardner, P; Knapp, P; McMillan, B; Raynor, DK; Woolf, E, 2013
)
0.66
"The results showed that the three formats did not influence participants' ratings of the information or their side-effect estimates."( Evaluating a combined (frequency and percentage) risk expression to communicate information on medicine side effects to patients.
Gardner, P; Knapp, P; McMillan, B; Raynor, DK; Woolf, E, 2013
)
0.39
" Physiopathologic mechanisms associated with these toxic effects are yet unclear and, besides discontinuation of the drug, when possible, there is no current validated treatment once visual loss is present."( [Ocular toxicity of drugs].
Audo, I, 2013
)
0.39
" We conducted a larger self-report evaluation of endocrine therapy discontinuation associated with patient characteristics and therapy-related adverse effects."( Patient-reported discontinuation of endocrine therapy and related adverse effects among women with early-stage breast cancer.
Aiello Bowles, EJ; Boudreau, DM; Buist, DS; Chestnut, J; Chubak, J; Fujii, M; Yu, O, 2012
)
0.38
" Women reported adverse effects and reasons for discontinuation via mailed survey; tumor characteristics were obtained via registry linkage."( Patient-reported discontinuation of endocrine therapy and related adverse effects among women with early-stage breast cancer.
Aiello Bowles, EJ; Boudreau, DM; Buist, DS; Chestnut, J; Chubak, J; Fujii, M; Yu, O, 2012
)
0.38
" Almost all women (94%) experienced adverse effects."( Patient-reported discontinuation of endocrine therapy and related adverse effects among women with early-stage breast cancer.
Aiello Bowles, EJ; Boudreau, DM; Buist, DS; Chestnut, J; Chubak, J; Fujii, M; Yu, O, 2012
)
0.38
"Few individual adverse effects or patient characteristics were significantly associated with endocrine therapy discontinuation, yet adverse effects were prevalent and were the most common reason women reported for discontinuing therapy."( Patient-reported discontinuation of endocrine therapy and related adverse effects among women with early-stage breast cancer.
Aiello Bowles, EJ; Boudreau, DM; Buist, DS; Chestnut, J; Chubak, J; Fujii, M; Yu, O, 2012
)
0.38
"Specific adverse events (AEs) associated with endocrine therapy and related to depletion or blocking of circulating estrogens may be related to treatment efficacy."( Specific adverse events predict survival benefit in patients treated with tamoxifen or aromatase inhibitors: an international tamoxifen exemestane adjuvant multinational trial analysis.
Bartlett, JM; Fontein, DB; Hadji, P; Hasenburg, A; Hille, ET; Hozumi, Y; Jones, SE; Kranenbarg, EM; Markopoulos, C; Nortier, JW; Paridaens, RJ; Putter, H; Rea, DW; Seynaeve, C; van de Velde, CJ; van de Water, W; Vannetzel, JM, 2013
)
0.62
"It is increasingly apparent that treatment with a variety of anticancer agents often is associated with adverse neurological consequences."( MEK1/2 inhibition suppresses tamoxifen toxicity on CNS glial progenitor cells.
Chen, HY; Han, R; Noble, M; Yang, YM, 2013
)
0.68
" Regarding serious adverse events (AEs), there are data indicating an increase in cardiovascular AEs and bone fractures but a lower incidence of thromboembolic phenomena and endometrial cancer with AIs vis-à-vis tamoxifen."( Postmenopausal women with hormone receptor-positive breast cancer: balancing benefit and toxicity from aromatase inhibitors.
Ingle, JN, 2013
)
0.58
"00001), treatment emergent adverse event, discontinuations due to adverse event, and serious adverse event indicated that ospemifene was generally safe."( The efficacy and safety of ospemifene in treating dyspareunia associated with postmenopausal vulvar and vaginal atrophy: a systematic review and meta-analysis.
Cui, Y; Li, N; Yan, H; Zhang, Y; Zong, H, 2014
)
0.4
"This meta-analysis indicates that ospemifene to be an effective and safe treatment for dyspareunia associated with postmenopausal vulvar and vaginal atrophy."( The efficacy and safety of ospemifene in treating dyspareunia associated with postmenopausal vulvar and vaginal atrophy: a systematic review and meta-analysis.
Cui, Y; Li, N; Yan, H; Zhang, Y; Zong, H, 2014
)
0.4
" CYP2D6 genotypes and phenotypes were related to the occurrence of hot flashes as adverse event during the first year of tamoxifen use (primary aim) and the time to the occurrence of hot flashes as AE during the complete time on tamoxifen (secondary aim)."( CYP2D6 genotype in relation to hot flashes as tamoxifen side effect in a Dutch cohort of the tamoxifen exemestane adjuvant multinational (TEAM) trial.
Berns, EM; Dezentjé, VO; Gelderblom, H; Guchelaar, HJ; Kranenbarg, EM; Nortier, JW; Putter, H; Seynaeve, C; Van de Velde, CJ; Van der Straaten, T; Van Schaik, RH; Vletter-Bogaartz, JM; Wessels, JA, 2014
)
0.87
"Safety assessments included adverse events, laboratory studies, physical and gynecologic examination, vital signs, breast palpation, and mammography."( Long-term safety of ospemifene (52-week extension) in the treatment of vulvar and vaginal atrophy in hysterectomized postmenopausal women.
Mabey, RG; Portman, D; Simon, J, 2014
)
0.4
"Most treatment-emergent adverse events (TEAEs) during the extension study were mild or moderate in severity."( Long-term safety of ospemifene (52-week extension) in the treatment of vulvar and vaginal atrophy in hysterectomized postmenopausal women.
Mabey, RG; Portman, D; Simon, J, 2014
)
0.4
"Ospemifene is clinically safe and generally well tolerated in postmenopausal patients with dyspareunia, a symptom of VVA."( Long-term safety of ospemifene (52-week extension) in the treatment of vulvar and vaginal atrophy in hysterectomized postmenopausal women.
Mabey, RG; Portman, D; Simon, J, 2014
)
0.4
" However, tamoxifen produces adverse effects that could be due to its ability to induce cellular DNA damage."( Comparison of cytotoxicity and genotoxicity of 4-hydroxytamoxifen in combination with Tualang honey in MCF-7 and MCF-10A cells.
Ismail, NF; Yaacob, NS, 2014
)
1.05
"The findings indicate that TH could afford protection of non-cancerous cells from the toxic effects of tamoxifen by increasing the efficiency of DNA repair mechanism in these cells."( Comparison of cytotoxicity and genotoxicity of 4-hydroxytamoxifen in combination with Tualang honey in MCF-7 and MCF-10A cells.
Ismail, NF; Yaacob, NS, 2014
)
0.86
" The most commonly reported adverse events were 'reproductive system disorders' in the tamoxifen group (17."( A prospective, randomized study on hepatotoxicity of anastrozole compared with tamoxifen in women with breast cancer.
Chen, D; Deng, Y; Feng, G; He, P; Hu, R; Huang, T; Li, E; Li, L; Li, Y; Liang, Z; Lin, Y; Liu, J; Lu, Y; Ma, R; Su, F; Sun, S; Tong, Z; Wang, S; Wang, X; Wu, Y; Xu, Z; Zhang, H; Zhang, X; Zhang, Y; Zhao, Y, 2014
)
0.85
"These clinical trial data indicate that up to 52 weeks of treatment with oral ospemifene 60 mg/day was safe for the endometrium."( Endometrial safety of ospemifene: results of the phase 2/3 clinical development program.
Archer, DF; Constantine, GD; Goldstein, SR, 2015
)
0.42
"Besides the well-known adverse effects on joints and bone and the vasomotor system, more neglected and latent toxicity like cognitive problems and vulvovaginal atrophy will be discussed."( Safety of aromatase inhibitor therapy in breast cancer.
Lintermans, A; Neven, P, 2015
)
0.42
"Placebo-controlled long-term studies carefully monitoring these adverse events, together with more extensive research in the etiologies, are warranted."( Safety of aromatase inhibitor therapy in breast cancer.
Lintermans, A; Neven, P, 2015
)
0.42
" A preliminary assessment of their acute aquatic toxicity at two trophic levels by means of quantitative structure-activity relationship models showed that the identified byproducts were up to 110-fold more toxic than the parent compounds."( Transformation of tamoxifen and its major metabolites during water chlorination: Identification and in silico toxicity assessment of their disinfection byproducts.
Barceló, D; López de Alda, M; Negreira, N; Regueiro, J, 2015
)
0.75
" Whether such tamoxifen dose escalation is effective and safe in view of long-term toxic effects is uncertain and needs to be explored."( CYP2D6 genotype- and endoxifen-guided tamoxifen dose escalation increases endoxifen serum concentrations without increasing side effects.
Dezentjé, VO; Dieudonné, AS; Gelderblom, H; Guchelaar, HJ; Hartigh den, J; Maartense, E; Neven, P; Nortier, JW; Opdam, FL; Putter, H; Smorenburg, CH; Van de Velde, CJ; Van der Straaten, T; Vree, R, 2015
)
1.05
" In a cellular model, tamoxifen resistance was associated with increased sensitivity towards toxic dicarbonyls and reduced free sulfhydryl group content."( Oxidative stress and glyoxalase I activity mediate dicarbonyl toxicity in MCF-7 mamma carcinoma cells and a tamoxifen resistant derivative.
Ignatov, A; Kalinski, T; Nass, N; Roessner, A; Sel, S, 2016
)
0.96
" This systematic review of seven randomized controlled studies comparing TAM and AI, and one study comparing extended therapy with an AI with placebo after about 5 years of tamoxifen, aims to assess long-term clinical efficacy and adverse events."( Aromatase inhibitors alone or sequentially combined with tamoxifen in postmenopausal early breast cancer compared with tamoxifen or placebo - Meta-analyses on efficacy and adverse events based on randomized clinical trials.
Ahlgren, J; Heibert Arnlind, M; Höistad, M; Rydén, L; Vitols, S, 2016
)
0.87
" We reviewed the adverse events (AEs) reported in studies of men prescribed tamoxifen for these conditions to better understand its side-effect profile."( Tamoxifen in men: a review of adverse events.
Hollis, N; Pollock, PA; Wassersug, RJ; Wibowo, E, 2016
)
2.11
"Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites."( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016
)
0.43
" Because many BCSs decide not take OET as recommended because of adverse effects, understanding BCSs' decisional supports and needs is foundational to supporting quality OET decision making about whether to adhere to OET."( Oral Endocrine Therapy Nonadherence, Adverse Effects, Decisional Support, and Decisional Needs in Women With Breast Cancer.
Carpenter, JS; Milata, JL; Otte, JL,
)
0.13
"The aim of this study was to examine literature pertaining to OET nonadherence and adverse effects using the Ottawa Decision Support Framework categories of decisional supports and decisional needs because these factors potentially influence OET use."( Oral Endocrine Therapy Nonadherence, Adverse Effects, Decisional Support, and Decisional Needs in Women With Breast Cancer.
Carpenter, JS; Milata, JL; Otte, JL,
)
0.13
"Findings identified the impact of adverse effects on OET nonadherence, an absence of decisional supports provided to or available for BCSs who are experiencing OET adverse effects, and the likelihood of unmet decisional needs related to OET."( Oral Endocrine Therapy Nonadherence, Adverse Effects, Decisional Support, and Decisional Needs in Women With Breast Cancer.
Carpenter, JS; Milata, JL; Otte, JL,
)
0.13
" This review serves as a call to action for providers to provide support to BCSs experiencing OET adverse effects and facing decisions related to nonadherence."( Oral Endocrine Therapy Nonadherence, Adverse Effects, Decisional Support, and Decisional Needs in Women With Breast Cancer.
Carpenter, JS; Milata, JL; Otte, JL,
)
0.13
"Findings suggest BCSs prescribed OET have unmet decisional needs, and more decisional supports are needed for BCSs experiencing OET adverse effects."( Oral Endocrine Therapy Nonadherence, Adverse Effects, Decisional Support, and Decisional Needs in Women With Breast Cancer.
Carpenter, JS; Milata, JL; Otte, JL,
)
0.13
"This paper focuses primarily on adverse effects of aromatase inhibitors which can lead to non-compliance or to discontinuation of treatment."( [Treatment with Aromatase Inhibitors in Postmenopausal Women with Breast Cancer and the Possibility of Influencing Side Effects].
Krásenská, M, 2016
)
0.43
" On the other hand as aromatase inhibitors lack estrogenic activity, they are not associated with serious adverse events typical for tamoxifen, such as endometrial cancer and thromboembolic disease."( [Treatment with Aromatase Inhibitors in Postmenopausal Women with Breast Cancer and the Possibility of Influencing Side Effects].
Krásenská, M, 2016
)
0.64
" Safety information in a long-term safety trial was used to assess the potential changes in risk of adverse events with ospemifene-exposure increase."( Population pharmacokinetics of ospemifene and safety evaluation of pharmacokinetic alterations caused by intrinsic and extrinsic factors
.
Kubota, R; Matsumoto, S; Wajima, T, 2017
)
0.46
" The drug appears safe to use in renal impairment, moderate hepatic impairment, and when coadministered with ketoconazole."( Population pharmacokinetics of ospemifene and safety evaluation of pharmacokinetic alterations caused by intrinsic and extrinsic factors
.
Kubota, R; Matsumoto, S; Wajima, T, 2017
)
0.46
" The main outcome measures included disease-free survival (DFS), recurrence-free survival (RFS), overall survival (OS), overall response rate (ORR), and adverse events."( A meta-analysis of randomized controlled trials comparing the efficacy and safety of anastrozole versus tamoxifen for breast cancer.
Pan, W; Sun, X; Tang, X; Wu, S; Yang, Y, 2017
)
0.67
" It is widely used for treatment of breast cancer; however, analogous with many antineoplastic agents, tamoxifen is associated with numerous adverse effects, most prominently nausea."( Mechanism of Off-Target Interactions and Toxicity of Tamoxifen and Its Metabolites.
Alisaraie, L; Flynn, M; Heale, KA, 2017
)
0.92
" Secondary outcomes were adverse events."( Efficacy and safety of endocrine monotherapy as first-line treatment for hormone-sensitive advanced breast cancer: A network meta-analysis.
He, Y; Huang, Y; Wang, C; Wu, K; Zhang, J; Zheng, S, 2017
)
0.46
" We directly compared adverse events and found that tamoxifen produced more hot flash events than fulvestrant 250 mg."( Efficacy and safety of endocrine monotherapy as first-line treatment for hormone-sensitive advanced breast cancer: A network meta-analysis.
He, Y; Huang, Y; Wang, C; Wu, K; Zhang, J; Zheng, S, 2017
)
0.71
" We found that a single dose of tamoxifen less than 10% of the mean dose used for recombination induction, caused adverse effects to the testis and to the reproductive endocrine system that persisted long-term."( Low-dose tamoxifen treatment in juvenile males has long-term adverse effects on the reproductive system: implications for inducible transgenics.
Atanassova, N; Curley, MK; Darbey, AL; Gannon, AL; O'Hara, L; Patel, SH; Rebourcet, D; Sharpe, RM; Smith, LB; Smith, SE, 2017
)
1.16
"We found 19 cases of serious adverse events possibly related to tamoxifen (thrombi, uterine malignancies)."( Tamoxifen Pharmacovigilance: Implications for Safe Use in the Future.
Antimisiaris, D; Bae, KG; Gully, Z; Morton, L, 2017
)
2.14
"Some studies direct the important pharmacovigilance toward prevention of thrombi, uterine malignancies, and hypercalcemia; however, it is not easy to identify recommendations for frequency or focus of monitoring to prevent adverse events for individual older adults based on existing recommendations."( Tamoxifen Pharmacovigilance: Implications for Safe Use in the Future.
Antimisiaris, D; Bae, KG; Gully, Z; Morton, L, 2017
)
1.9
"Post hoc analysis of safety data (treatment-emergent adverse events [TEAEs]) pooled from six phase 2 and 3 randomized, double-blind, multicenter placebo-controlled studies, evaluating the effects of ospemifene 60 mg on the breast, cardiovascular system, and bone in postmenopausal women."( Overall Safety of Ospemifene in Postmenopausal Women from Placebo-Controlled Phase 2 and 3 Trials.
Altomare, C; Cort, S; Jiang, W; Pinkerton, JV; Simon, JA, 2018
)
0.48
" Most women discontinued treatment due to adverse events (AEs): hot flushes, muscle spasms, headache, and vaginal discharge."( Overall Safety of Ospemifene in Postmenopausal Women from Placebo-Controlled Phase 2 and 3 Trials.
Altomare, C; Cort, S; Jiang, W; Pinkerton, JV; Simon, JA, 2018
)
0.48
"This study was designed to evaluate the effect of CYP2D6 and ABCB1 polymorphisms and co-medication on the outcomes and adverse events (AEs) of tamoxifen therapy."( Impact of ABCB1 and CYP2D6 polymorphisms on tamoxifen treatment outcomes and adverse events in breast cancer patients.
Argalacsova, S; Bakhouche, H; Pertuzelka, L; Slanar, O,
)
0.59
"Antimalarial drugs including chloroquine, its less toxic quinolone-derivative hydroxychloroquine (HCQ), and quinacrine have become cornerstones in the treatment of autoimmune diseases including systemic lupus, rheumatoid arthritis, sarcoidosis, and Sjogren syndrome; cutaneous disorders, antiphospholipid syndrome, and have recently been employed at higher dioses in oncology."( Hydroxychloroquine: balancing the need to maintain therapeutic levels with ocular safety: an update.
Abdulaziz, N; McCune, WJ; Shah, AR, 2018
)
0.48
"BCS and ET without RT seem to be a safe treatment option in women ≥ 65 years with early breast cancer and favorable histopathology."( Omitting radiotherapy in women ≥ 65 years with low-risk early breast cancer after breast-conserving surgery and adjuvant endocrine therapy is safe.
Ahlgren, J; Bjöhle, J; Blomqvist, C; Carlberg, M; Killander, F; Liljegren, G; Lindman, H; Villman, K; Wickberg, Å, 2018
)
0.48
" Nevertheless, endocrine therapy is also linked with adverse effects that impact quality of life, social function, and adherence to treatment."( Managing side effects in adjuvant endocrine therapy for breast cancer.
Condorelli, R; Vaz-Luis, I, 2018
)
0.48
" Two groups of outcomes were selected: 1) side-effects, including hot flushes, urinary tract infection (UTI), headache, deep venous thrombosis (DVT), coronary heart disease (CHD), cardiovascular event (CVE), discontinuation due to side-effects, serious adverse event (SAE); 2) Safety, in relation to endometrial thickness, vaginal bleeding, breast tenderness, breast and endometrial cancer."( Ospemifene for the treatment of vulvar and vaginal atrophy: A meta-analysis of randomized trials. Part II: Evaluation of tolerability and safety.
Benedetti Panici, P; D'oria, O; Di Donato, V; Iacobelli, V; Kontopantelis, E; Muzii, L; Schiavi, MC; Simoncini, T, 2019
)
0.51
" Safety was assessed by treatment-emergent adverse events (TEAEs) and endometrial biopsies."( Efficacy and safety of ospemifene in postmenopausal women with moderate-to-severe vaginal dryness: a phase 3, randomized, double-blind, placebo-controlled, multicenter trial.
Altomare, C; Archer, DF; Goldstein, SR; Schaffer, S; Simon, JA; Soulban, G; Sussman, SA; Waldbaum, AS; Yoshida, Y; Zhu, J, 2019
)
0.51
"To clarify the profile of adverse events from endocrine therapies in older patients."( Characteristics of adverse events of endocrine therapies among older patients with breast cancer.
Akiyama, F; Honma, N; Horii, R; Iwase, T; Makita, M; Mikami, T; Ogata, H; Ohno, S; Saji, S, 2019
)
0.51
"Among patients ≥ 70 years old, many symptoms were significantly more frequent/severe with AIs than with SERMs, compared with those aged 56-69, which suggests a difference in the profile of adverse events according to the type of endocrine therapy and the patient's age."( Characteristics of adverse events of endocrine therapies among older patients with breast cancer.
Akiyama, F; Honma, N; Horii, R; Iwase, T; Makita, M; Mikami, T; Ogata, H; Ohno, S; Saji, S, 2019
)
0.51
"Taselisib combined with tamoxifen was generally well tolerated, with treatment-emergent adverse events as expected for this class of drugs, including diarrhea (13 patients, 43%), mucositis (10 patients, 33%), and hyperglycemia (8 patients, 27%)."( POSEIDON Trial Phase 1b Results: Safety, Efficacy and Circulating Tumor DNA Response of the Beta Isoform-Sparing PI3K Inhibitor Taselisib (GDC-0032) Combined with Tamoxifen in Hormone Receptor Positive Metastatic Breast Cancer Patients.
Baird, RD; Beddowes, E; Beelen, K; Bernards, R; Caldas, C; Callari, M; Cortès, J; de Vries Schultink, A; Dougall, G; Gallagher, W; Gao, M; Garcia-Corbacho, J; Kumar, S; Linn, SC; Linossi, C; Mandjes, IAM; Nederlof, P; Oliveira, M; Perez-Garcia, JM; Platte, E; Rosing, H; Saura, C; Schot, M; Schrier, M; Vallier, AL; van Rossum, AGJ; van Tinteren, H; van Werkhoven, E, 2019
)
1.02
" Endoxifen, which is toxic to aquatic animals, has been detected in wastewater treatment plant (WWTP) effluent."( Photodegradation of (E)- and (Z)-Endoxifen in water by ultraviolet light: Efficiency, kinetics, by-products, and toxicity assessment.
Delorme, A; Khan, E; Martin, MA; McEvoy, J; Sivaguru, J; Sonthiphand, P, 2020
)
0.56
" While the efficacy is comparable with that of estrogenic treatments, ospemifene is not only well tolerated and safe but also reduces bone turnover in postmenopausal women, and available data indicate no safety concerns for breast tissue."( Ospemifene efficacy and safety data in women with vulvovaginal atrophy.
Pup, LD; Sánchez-Borrego, R, 2020
)
0.56
" Lipid metabolism disorder was the most common adverse event (69."( Safety and efficacy of sirolimus combined with endocrine therapy in patients with advanced hormone receptor-positive breast cancer and the exploration of biomarkers.
Guan, X; Li, C; Li, H; Li, L; Liu, B; Ma, F; Qian, H; Rong, G; Sun, X; Wang, W; Xu, B; Yi, Z; Zhai, J, 2020
)
0.56
" Differences in the toxicity profiles of these drugs are described; however, little is known about whether the risk of adverse events changes over time."( Evolution in the risk of adverse events of adjuvant endocrine therapy in postmenopausal women with early-stage breast cancer.
Amir, E; Desnoyers, A; Goldvaser, H; Moore, A; Reinhorn, D; Saleh, RR; Yerushalmi, R, 2020
)
0.56
" Data on pre-specified adverse events were extracted including cardiovascular events, bone fractures, cerebrovascular disease, endometrial cancer, secondary malignancies excluding breast cancer, venous thrombosis and death without recurrence."( Evolution in the risk of adverse events of adjuvant endocrine therapy in postmenopausal women with early-stage breast cancer.
Amir, E; Desnoyers, A; Goldvaser, H; Moore, A; Reinhorn, D; Saleh, RR; Yerushalmi, R, 2020
)
0.56
" We also evaluated the power and sensitivity of the method for detecting toxic effects of drugs by conducting a set of experiments using known toxicants and other methods of screening for cytotoxic effects."( Quantifying drug-induced structural toxicity in hepatocytes and cardiomyocytes derived from hiPSCs using a deep learning method.
Dame, K; Grafton, F; Loewke, K; Maddah, M; Mandegar, MA; Ribeiro, AJS, 2020
)
0.56
" Lifestyle changes and complementary therapies can be important tools for side effect management."( How patients experience endocrine therapy for breast cancer: an online survey of side effects, adherence, and medical team support.
Attai, DJ; Baker, JL; Berkowitz, JS; Berkowitz, MJ; DiNome, ML; Lee, MK; Streja, E; Thompson, CK; Wenziger, CM; Zibecchi, LT, 2021
)
0.62
"Women randomised to tamoxifen in the IBIS-I trial and for whom side effect status was known at the 6-month follow-up visit were included in this analysis."( Tamoxifen related side effects and their impact on breast cancer incidence: A retrospective analysis of the randomised IBIS-I trial.
Cuzick, J; Dowsett, M; Hale, MJ; Howell, A; Sestak, I, 2020
)
2.32
" Ospemifene therapy was however superior to laser and vaginal estrogen therapies in ameliorating sexual function, however, it presents a high risk of developing adverse events and endometrial hyperplasia."( Efficacy and safety of current therapies for genitourinary syndrome of menopause: A Bayesian network analysis of 29 randomized trials and 8311 patients.
Chang, Y; Duan, H; Li, B; Wang, S, 2021
)
0.62
" The incidence of bone-related adverse events was around 5% in both groups."( A follow-up study of a randomized controlled study evaluating safety and efficacy of leuprorelin acetate every-3-month depot for 2 versus 3 or more years with tamoxifen for 5 years as adjuvant treatment in premenopausal patients with endocrine-responsive
Fujii, T; Kurebayashi, J; Matsumoto, H; Nomizu, T; Ohashi, Y; Ohtake, T; Okazaki, M; Shiba, E; Toyama, T, 2021
)
0.82
"By reviewing the recent articles regarding the ocular side effect of tamoxifen when treating breast cancer and glioma, this article summarized the incidence and the potential mechanism of the side effects of tamoxifen, and the specific ocular toxicity including keratopathy, cataract, retinopathy, optic neuropathy."( [Ocular toxicity induced by tamoxifen: an overview].
Ma, J; Wang, M; Zhong, Y, 2021
)
1.15
" The adverse events induced by tamoxifen were assessed using both World Health Organization-Uppsala Monitoring Centre (WHO-UMC) causality categories and the Naranjo probability scale."( Traditional Korean medicine treatment for tamoxifen associated adverse events of breast cancer patient: A CARE - Compliant case report.
Jo, HG; Lee, D; Seo, J, 2021
)
1.17
"This case report suggests that traditional Korean medicine interventions might have improved the adverse events of tamoxifen in breast cancer patients."( Traditional Korean medicine treatment for tamoxifen associated adverse events of breast cancer patient: A CARE - Compliant case report.
Jo, HG; Lee, D; Seo, J, 2021
)
1.1
"Patients having Duchenne muscular dystrophy (DMD) are currently being treated with corticosteroids, which slow down disease progression at the expense of serious adverse effects."( Safety and clinical outcome of tamoxifen in Duchenne muscular dystrophy.
Avrahami, R; Ben-Sasson, S; Dor, T; Eliav, O; Lavi, E; Simchovitz, E; Tsabari, R, 2021
)
0.91
"Graphical displays and data visualization are essential components of statistical analysis that can lead to improved understanding of clinical trial adverse event (AE) data."( Visualizing adverse events in clinical trials using correspondence analysis with R-package visae.
Diniz, MA; Ganz, PA; Gresham, G; Henry, NL; Kim, S; Luu, M; Rogatko, A; Tighiouart, M; Yothers, G, 2021
)
0.62
" We defined five levels of refinement for the analysis based on data derived from the Common Terminology Criteria for Adverse Events (CTCAE) grades, domains, terms and their combinations."( Visualizing adverse events in clinical trials using correspondence analysis with R-package visae.
Diniz, MA; Ganz, PA; Gresham, G; Henry, NL; Kim, S; Luu, M; Rogatko, A; Tighiouart, M; Yothers, G, 2021
)
0.62
" The data analytical platform Molecular Health Effect was utilized to map population ADR data from the US Food and Drug Administration (FDA) Adverse Event Reporting System to chemical and biological databases (such as UniProt and Reactome), for hypothesis generation regarding the underlying molecular mechanisms causing cardiotoxicity."( A case study of a patient-centered reverse translational systems-based approach to understand adverse event profiles in drug development.
Jackson, DB; Kim, S; Lahu, G; Lesko, LJ; Soldatos, TG; Trame, MN; Vakilynejad, M, 2022
)
0.72
"The overall response rate of the research group was statistically higher than that of the control group, and the incidence of adverse reactions was significantly lower."( Efficacy, Safety, and Prognosis of Sequential Therapy with Tamoxifen and Letrozole versus Letrozole Monotherapy for Breast Carcinoma.
Lu, X; Qian, C, 2022
)
0.96
"LTZ alone or in sequence with TAM is effective and safe for the treatment of BC, which can significantly improve the prognosis and blood lipid indices of BC patients."( Efficacy, Safety, and Prognosis of Sequential Therapy with Tamoxifen and Letrozole versus Letrozole Monotherapy for Breast Carcinoma.
Lu, X; Qian, C, 2022
)
0.96
" Although much has been published on adverse events related to taxanes, data on ocular outcomes with these very important drugs are scant."( Risk of Ocular Adverse Events With Taxane-Based Chemotherapy.
Etminan, M; Maberley, D; Mikelberg, F; Sodhi, M; Yeung, SN, 2022
)
0.72
"To quantify the risk of 3 mutually exclusive ocular adverse events of epiphora, cystoid macular edema (CME), and optic neuropathy with taxane-based chemotherapy agents by undertaking a large pharmacoepidemiologic study."( Risk of Ocular Adverse Events With Taxane-Based Chemotherapy.
Etminan, M; Maberley, D; Mikelberg, F; Sodhi, M; Yeung, SN, 2022
)
0.72
" Ophthalmologists and oncologists should be aware of these adverse events in women with breast cancer who receive these drugs."( Risk of Ocular Adverse Events With Taxane-Based Chemotherapy.
Etminan, M; Maberley, D; Mikelberg, F; Sodhi, M; Yeung, SN, 2022
)
0.72
"Tamoxifen-induced hepatotoxicity is an inevitable side effect during breast cancer treatment."( Nrf2 and NF-қB interplay in tamoxifen-induced hepatic toxicity: A promising therapeutic approach of sildenafil and low-dose γ radiation.
Galal, SM; Karam, HM; Lotfy, DM, 2023
)
2.65
" These findings highlight the importance of fostering side effect awareness and applying appropriate interventions to assist with disease management throughout BC survivorship care."( Treatment-related side effects among Hispanic and non-Hispanic white long-term breast cancer survivors by tamoxifen use and duration.
Baumgartner, KB; Baumgartner, RN; Boone, SD; Connor, AE; Dibble, KE, 2023
)
1.12
" All adverse events were of mild or moderate severity and distributed similarly among active and placebo groups."( Pharmacokinetics, safety and preliminary pharmacodynamic evaluation of DARE-VVA1: a soft gelatin capsule containing tamoxifen for the treatment of vulvovaginal atrophy.
Friend, D; Hatheway, J; Hull, L; Mauck, C; Stuckey, B; Thurman, A; Zack, N, 2023
)
1.12
"DARE-VVA1 is safe and results in minimal systemic exposure to tamoxifen."( Pharmacokinetics, safety and preliminary pharmacodynamic evaluation of DARE-VVA1: a soft gelatin capsule containing tamoxifen for the treatment of vulvovaginal atrophy.
Friend, D; Hatheway, J; Hull, L; Mauck, C; Stuckey, B; Thurman, A; Zack, N, 2023
)
1.36
"Ospemifene is an efficacious, well-tolerated, and safe therapeutic option for postmenopausal women with moderate to severe symptoms of VVA."( Efficacy, tolerability, and endometrial safety of ospemifene compared with current therapies for the treatment of vulvovaginal atrophy: a systematic literature review and network meta-analysis.
Beauchemin, C; Black, D; Castonguay, A; Ferenczy, A; Marouf, R; Royer, C; Simon, JA, 2023
)
0.91

Pharmacokinetics

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.

ExcerptReferenceRelevance
" By deconvolution analysis, elderly men had a significant decrease in FSH secretory burst duration, and an increase in FSH half-life and FSH secretory burst amplitude compared with younger men."( Modulation of immunoradiometric and bioactive follicle stimulating hormone secretion and clearance in young and elderly men during treatment with tamoxifen or flutamide.
Dahl, KD; Lippert, MC; Urban, RJ; Veldhuis, JD,
)
0.33
"A multicenter phase I pharmacokinetic study of a new triphenylethylene antiestrogen, toremifene, was examined in 70 patients with advanced breast cancer."( Pharmacokinetics of toremifene and its metabolites in patients with advanced breast cancer.
Benz, CC; Cadman, TB; DeGregorio, MW; Shemano, I; Wiebe, VJ, 1990
)
0.28
" The half-life was found to be 5 days, and at three weeks following discontinuation of treatment concentrations greater than 24 ng/ml were detected."( Phase I study of the tolerance and pharmacokinetics of toremifene in patients with cancer.
DeGregorio, MW; Hamm, JT; Kohler, PC; Shemano, I; Tormey, DC; Wiebe, VJ, 1990
)
0.28
" After three widely separated single doses, a reversible increase in elimination half-life occurred."( Studies on the metabolism and pharmacokinetics of tamoxifen in normal volunteers.
Adam, HK; Kemp, JV; Patterson, JS,
)
0.38
" We conclude that 124I-labelled idoxifene combined with PET imaging would facilitate human in vivo pharmacokinetic studies of this new anticancer drug and provide an opportunity to investigate relationships between drug uptake and tumour response."( Biodistribution and kinetics of radiolabelled pyrrolidino-4-iodo-tamoxifen: prospects for pharmacokinetic studies using PET.
Carnochan, P; Eccles, S; Haynes, B; Ott, R; Potter, G; Trivedi, M; Young, H, 1994
)
0.53
" Pharmacokinetic parameters were not significantly different between premenopausal and postmenopausal patients."( 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
" In addition, this study compiled pharmacokinetic parameters for the current 30 mg regimen in postmenopausal women, the target population of tamoxifen therapy."( Pharmacokinetics and bioavailability of tamoxifen in postmenopausal healthy women.
Fuchs, WS; Gay, S; Leary, WP; van der Meer, MJ; von Nieciecki, A; Witschital, K, 1996
)
0.76
" As to the dose escalation, pharmacokinetic studies were carried out at doses of 24, 48 and 96 mg in two volunteers, and 120 mg in one volunteer."( Pharmacokinetics of panomifene in healthy volunteers at phase I/a study.
Bojti, E; Csörgo, M; Drabant, S; Erdélyi-Tóth, V; Gyergyay, F; Klebovich, I; Kralovánszky, J; Pap, E; Számel, I, 1997
)
0.3
"To determine whether tamoxifen plasma concentrations capable of blocking P-glycoprotein (Pgp) in vitro can be safely achieved in dogs and whether doxorubicin pharmacokinetic alterations occur when tamoxifen is coadministered."( Phase I and pharmacokinetic analysis of high-dose tamoxifen and chemotherapy in normal and tumor-bearing dogs.
Case, BC; Fine, RL; Frazier, D; Page, RL; Trogdon, ML; Tyczkowska, K; Waddle, JR, 1999
)
0.88
"This study examined whether the addition of tamoxifen to the treatment regimen of patients with advanced breast cancer being treated with the aromatase inhibitor letrozole led to any pharmacokinetic or pharmacodynamic interaction."( Impact of tamoxifen on the pharmacokinetics and endocrine effects of the aromatase inhibitor letrozole in postmenopausal women with breast cancer.
Dowsett, M; Gundacker, H; Houston, SJ; Johnston, SR; Miles, DW; Pfister, C; Sioufi, A; Smith, IE; Verbeek, JA, 1999
)
0.97
" The pharmacokinetic parameters of VP-16, such as area under curve (AUC), free AUC and protein binding, were determined from drug plasma concentrations at 1 and 4 h after VP-16 administration on the first day (day -1) and at the end of the chemotherapy cycle (day -21) for VP-16 alone and VP-16+TAM, respectively."( Pharmacokinetic interaction between etoposide and tamoxifen in patients with hepatocellular carcinoma.
Aita, P; Bearz, A; Boiocchi, M; Colussi, AM; Corona, G; Sartor, F; Sorio, R; Toffoli, G, 1999
)
0.56
" Standard pharmacokinetic parameters were assessed."( Pharmacokinetics of (deaminohydroxy)toremifene in humans: a new, selective estrogen-receptor modulator.
DeGregorio, MW; Erkkola, RU; Halonen, KH; Huupponen, RK; Taras, TL; Wurz, GT, 2000
)
0.31
" Patients included in the pharmacokinetic (PK) sub-protocol had been in ATAC for > or =3 months, taking their medication in the morning and were 100% compliant for the preceding 14 days."( Pharmacokinetics of anastrozole and tamoxifen alone, and in combination, during adjuvant endocrine therapy for early breast cancer in postmenopausal women: a sub-protocol of the 'Arimidex and tamoxifen alone or in combination' (ATAC) trial.
Cuzick, J; Dowsett, M; Howell, A; Jackson, I, 2001
)
0.59
" A pharmacokinetic interaction has been established between letrozole and tamoxifen, whereby reduced circulating levels of letrozole are found with combined application."( Comparative clinical pharmacology and pharmacokinetic interactions of aromatase inhibitors.
Boeddinghaus, IM; Dowsett, M, 2001
)
0.54
" Treatment started 2 to 3 weeks before surgery and blood was taken at various times up to 12 weeks after fulvestrant administration to assess pharmacokinetic variables."( 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
"A total of 200 patients entered the trial, of whom 58 took part in the pharmacokinetic analysis (50 mg, n = 20; 125 mg, n = 16; 250 mg, n = 22)."( 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
" Tipifarnib pharmacokinetic and pharmacodynamic variables were similar in the presence and absence of tamoxifen."( A phase I trial and pharmacokinetic study of tipifarnib, a farnesyltransferase inhibitor, and tamoxifen in metastatic breast cancer.
Balis, FM; Chow, C; Clark, G; Eng-Wong, J; Gantz, SB; Jayaprakash, N; Lebowitz, PF; Venzon, D; Widemann, BC; Zujewski, J, 2005
)
0.76
"The simultaneous curve fitting of plasma data with urine and bile data with the help of the related pharmacokinetic equations provided the calculated parameters and constants."( Investigation of the influence of modulation of P-glycoprotein by a multiple dosing regimen of tamoxifen on the pharmacokinetics and toxicodynamics of doxorubicin.
Boroujerdi, M; Darvari, R, 2005
)
0.55
" Pharmacokinetic and safety assessments were conducted throughout the trial."( A phase I study to determine the effect of tamoxifen on the pharmacokinetics of a single 250 mg oral dose of gefitinib (IRESSA) in healthy male volunteers.
Bailey, CJ; Cantarini, MV; Macpherson, MP; Marshall, AL; Robinson, AV, 2005
)
0.59
" The presence of tamoxifen did not have a clinically significant effect on the primary variables AUC and Cmax of gefitinib, nor on the secondary variables AUC(0-t), tmax, t1/2, and lambdaz."( A phase I study to determine the effect of tamoxifen on the pharmacokinetics of a single 250 mg oral dose of gefitinib (IRESSA) in healthy male volunteers.
Bailey, CJ; Cantarini, MV; Macpherson, MP; Marshall, AL; Robinson, AV, 2005
)
0.93
" Clinical trials combining tamoxifen with letrozole or anastrazole have shown minor pharmacokinetic drug interactions."( Effect of exemestane on tamoxifen pharmacokinetics in postmenopausal women treated for breast cancer.
Cleary, JF; Havighurst, TC; Hutson, PR; Love, RR; Rogers, E, 2005
)
0.93
" Blood was collected for pharmacokinetic analysis after at least 4 months of receiving 20 mg tamoxifen daily."( Effect of exemestane on tamoxifen pharmacokinetics in postmenopausal women treated for breast cancer.
Cleary, JF; Havighurst, TC; Hutson, PR; Love, RR; Rogers, E, 2005
)
0.85
"There is no pharmacokinetic interaction between tamoxifen and exemestane."( Effect of exemestane on tamoxifen pharmacokinetics in postmenopausal women treated for breast cancer.
Cleary, JF; Havighurst, TC; Hutson, PR; Love, RR; Rogers, E, 2005
)
0.89
" The TC-loaded TSSLN was administered to the rats intravenously and the pharmacokinetic parameters in the plasma were determined."( Tamoxifen citrate loaded solid lipid nanoparticles (SLN): preparation, characterization, in vitro drug release, and pharmacokinetic evaluation.
Bakshi, N; Murthy, RS; Reddy, LH; Vivek, K, 2006
)
1.78
" 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
" The presence of kaempferol did not alter the pharmacokinetic parameters of a metabolite of tamoxifen, 4-hydroxytamoxifen."( 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
)
0.81
" The purpose of this study was to report the pharmacokinetic interaction between tamoxifen and ondansetron in rats."( Pharmacokinetic interaction between tamoxifen and ondansetron in rats: non-competitive (hepatic) and competitive (intestinal) inhibition of tamoxifen metabolism by ondansetron via CYP2D subfamily and 3A1/2.
Lee, MG; Suh, JH; Yang, SH, 2010
)
0.86
" Pharmacokinetic parameters of tamoxifen and 4-hydroxytamoxifen were determined in rats after oral (10 mg/kg) and intravenous (2 mg/kg) administration of tamoxifen in the presence and absence of myricetin (0."( 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
)
0.87
" Pharmacokinetic parameters of tamoxifen and 4-hydroxytamoxifen were determined in rats after an oral administration of tamoxifen (10 mg/kg) to rats in the presence and absence of baicalein (0."( 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
)
0.91
" This study was conducted to investigate the pharmacokinetic interactions between ondansetron and tamoxifen after intravenous and oral administration of ondansetron (both 8 mg/kg) and/or tamoxifen (2 and 10 mg/kg for intravenous and oral administration, respectively), in rats bearing 7,12-dimethylbenz[a]anthracene (DMBA)-induced mammarian tumors (DMBA rats), used as an animal model of human breast cancer."( Pharmacokinetic drug interactions between ondansetron and tamoxifen in female Sprague-Dawley rats with DMBA-induced mammary tumor.
Kim, SH; Lee, MG; Suh, JH; Yang, SH, 2013
)
0.85
"The clinical pharmacokinetic findings and in vitro data suggest that CYP3A4 is important for ospemifene metabolism, but other CYP isoforms and metabolic pathways also contribute."( Effects of cytochrome P450 inhibitors and inducers on the metabolism and pharmacokinetics of ospemifene.
Lammintausta, R; Lehtinen, T; Pelkonen, O; Scheinin, M; Tolonen, A; Turpeinen, M; Uusitalo, J; Vuorinen, J, 2013
)
0.39
" Three single-dose, open-label, parallel-group pharmacokinetic studies examined the pharmacokinetics of ospemifene in postmenopausal women with (1) mild hepatic impairment (n = 7), (2) moderate hepatic impairment (n = 8), and (3) severe renal impairment (n = 8) compared with a similar number of matched healthy controls."( The effect of renal and hepatic impairment on the pharmacokinetics of ospemifene, a tissue-selective estrogen agonist/antagonist.
Graham, S; Marbury, TC; Preston, RA; Wajima, T,
)
0.13
"Population pharmacokinetic models were developed for dextromethorphan, tamoxifen and their metabolites."( Population pharmacokinetic modelling to assess the impact of CYP2D6 and CYP3A metabolic phenotypes on the pharmacokinetics of tamoxifen and endoxifen.
Beijnen, JH; Binkhorst, L; de Bruijn, P; de Graan, AJ; Huitema, AD; Mathijssen, RH; ter Heine, R, 2014
)
0.84
"This phase I study assessed the pharmacokinetic (PK), tolerability, safety and preliminary clinical activity of tamoxifen (T) and lapatinib (L) in patients with metastatic breast cancer (MBC)."( A phase I pharmacokinetics study of lapatinib and tamoxifen in metastatic breast cancer (EORTC 10053 Lapatam study).
Awada, A; Bogaerts, J; Brain, E; Cardoso, F; Fumoleau, P; Hayward, L; Koch, KM; Lokiec, F; Marréaud, S; Rezai, K; Werutsky, G, 2014
)
0.87
" Period 1, day 1, subjects were administered tamoxifen 40 mg followed by 23 days of blood sampling for pharmacokinetic analyses."( Open-label, 2-period sequential drug interaction study to evaluate the effect of a 100-mg dose of desvenlafaxine on the pharmacokinetics of tamoxifen when coadministered in healthy postmenopausal female subjects.
Braley, G; Liang, Y; Lubaczewski, S; Matschke, K; Nichols, AI; Ramey, T, 2014
)
0.86
" Therapeutic drug monitoring is a valid tool to determine the pharmacokinetic of a drug and individualized drug therapy, adjusting patient's dose requirement through the measurement and interpretation of drug concentrations."( [Clinical application, limits and perspectives of pharmacogenetic and pharmacokinetic analysis of anticancer drugs].
Chantry, AS; Ciccolini, J; Lacarelle, B; Quaranta, S,
)
0.13
" For each CYP enzyme, the influence of polymorphisms on pharmacokinetic and pharmacodynamic outcome measures is described throughout this review."( Effects of Pharmacogenetics on the Pharmacokinetics and Pharmacodynamics of Tamoxifen.
Beijnen, JH; de Vries Schultink, AH; Huitema, AD; Linn, SC; Zwart, W, 2015
)
0.65
" In conclusion, our results describe important molecular events that occur during combination breast cancer therapies and might modulate pharmacokinetic DOX resistance and/or behaviour."( Pharmacokinetic interactions of breast cancer chemotherapeutics with human doxorubicin reductases.
Havrankova, J; Hofman, J; Skarka, A; Wsol, V, 2015
)
0.42
"The anti-estrogen tamoxifen is characterized by a large variability in response, partly due to pharmacokinetic differences."( 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
)
1.06
" The compounds were designed with the objective of improving pharmacokinetic properties."( Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
Abdelghany, TM; Bayoumi, SA; Disouky, AM; El-Morsy, A; Elshafeey, A; Mancy, AS; Mayhoub, AS; Mohammad, H; Seleem, MA; Seleem, MN, 2016
)
0.43
" The efficacy was evaluated by in vitro MTT studies, safety by erythrocyte compatibility, and biodistribution by in vivo pharmacokinetic studies."( Chitosan-Stearic Acid Based Polymeric Micelles for the Effective Delivery of Tamoxifen: Cytotoxic and Pharmacokinetic Evaluation.
Bhushan, S; Dadarwal, M; Guru, SK; Katare, OP; Kumar, P; Raza, K; Sharma, G; Thotakura, N, 2017
)
0.68
"To develop a population pharmacokinetic (PPK) model to assess factors influencing ospemifene pharmacokinetics and to assess safety for pharmacokinetic alteration observed in drug development."( Population pharmacokinetics of ospemifene and safety evaluation of pharmacokinetic alterations caused by intrinsic and extrinsic factors
.
Kubota, R; Matsumoto, S; Wajima, T, 2017
)
0.46
" Interestingly, pharmacokinetic outcomes of the conjugate were superior and the area under the curve was enhanced by approximately three-times, whereas the drug clearance was reduced by around five-times, after single intravenous injection."( Glycinated fullerenes for tamoxifen intracellular delivery with improved anticancer activity and pharmacokinetics.
Katare, OP; Kumar, M; Kumar, R; Misra, C; Raza, K; Sharma, G; Singh, B, 2017
)
0.76
"The pharmacokinetic-pharmacodynamic model was established by integrating a four compartments pharmacokinetics model and a pharmacodynamic model, the first one include central compartment and peripheral compartment both of which contain tamoxifen and endoxifen."( A Pharmacokinetic-Pharmacodynamic Model of Tamoxifen and Endoxifen to Predict Their Distribution and Effects on Inhibition of Tumor Growth.
Chen, Y; Liao, J; Sun, Q; Yuan, S, 2017
)
0.9
" The parameters of the pharmacodynamic model, which characterized the tumor growth, revealed the patterns of tamoxifen's anti-tumor functions."( A Pharmacokinetic-Pharmacodynamic Model of Tamoxifen and Endoxifen to Predict Their Distribution and Effects on Inhibition of Tumor Growth.
Chen, Y; Liao, J; Sun, Q; Yuan, S, 2017
)
0.93
" This work describes the optimization of the pharmacokinetic properties of a previously published family of triazine lead compounds."( Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives.
Augustyns, K; Baán, A; Caljon, G; Kiekens, F; Maes, L; Matheeussen, A; Salado, IG; Van der Veken, P; Verdeyen, T, 2018
)
0.48
" This phase I study assessed the safety and pharmacokinetic (PK) profiles of olaparib combined with tamoxifen, anastrozole or letrozole in patients with advanced solid tumours."( Pharmacokinetic Effects and Safety of Olaparib Administered with Endocrine Therapy: A Phase I Study in Patients with Advanced Solid Tumours.
Bailey, C; Birkett, J; De Grève, J; De Vos, FYFL; Dean, E; Dirix, L; Goessl, C; Grundtvig-Sørensen, P; Italiano, A; Jerusalem, G; Learoyd, M; Leunen, K; Molife, LR; Plummer, R; Rolfo, C; Rottey, S; Spencer, S; Spicer, J; Verheul, HM, 2018
)
0.7
" The physiologically based pharmacokinetic (PBPK) models were developed to investigate the influence of different triazoles on tamoxifen pharmacokinetics in this paper."( Predicting the Effects of Different Triazole Antifungal Agents on the Pharmacokinetics of Tamoxifen.
Chen, L; Li, M; Li, N; Qi, F; Wang, N; Zhu, L, 2019
)
0.94
" We developed a population pharmacokinetic (PopPK) model for tamoxifen and six metabolites to determine clinically relevant factors of ENDO exposure."( Model-Based Quantification of Impact of Genetic Polymorphisms and Co-Medications on Pharmacokinetics of Tamoxifen and Six Metabolites in Breast Cancer.
Arellano, C; Bernard-Marty, C; Boyer, JC; Chatelut, E; Dalenc, F; Debled, M; Delmas, C; Dohollou, N; Evrard, A; Filleron, T; Jacot, W; Laharie-Mineur, H; Le Morvan, V; Puszkiel, A; Robert, J; Roché, H; Thomas, F; Vachoux, C; Venat-Bouvet, L; White-Koning, M, 2021
)
1.08
"The purpose of this study was to develop and validate a population pharmacokinetic model for Z-endoxifen in patients with advanced solid tumors and to identify clinical variables that influence pharmacokinetic parameters."( 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
" 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

Compound-Compound Interactions

Tamoxifen (TMX) combined with coenzyme Q10 (CoQ10) can significantly improve sperm concentration, motility and morphology in patients with idiopathic oligoasthenospermia.

ExcerptReferenceRelevance
"A comparative study of 5'-DFUR 600 mg/day alone (C-arm) or in combination with TAM 30 mg/day (A-arm) or MPA 600 mg/day (B-arm) was carried out."( [A comparative study with 5'-DFUR alone or in combination with tamoxifen (TAM) or medroxyprogesterone acetate (MPA) for advanced or recurrent breast cancer].
Aikawa, T; Hirai, T; Kotsuma, Y; Maeura, Y; Miyauchi, K; Takatsuka, Y; Yayoi, E, 1992
)
0.52
"The effect of Lonidamine (LND) alone or combined with the antiestrogen Tamoxifen (TAM) or Medroxyprogesterone acetate (MPA) on cell proliferation and steroid hormone receptor content of a human estrogen sensitive breast cancer cell line was investigated."( Antitumor effect of lonidamine alone or combined with tamoxifen or medroxyprogesterone acetate in breast cancer cells.
Angelucći, C; Della Cuna, GR; Iacopino, F; Lama, G; Marchetti, P; Sica, G,
)
0.61
" Synergistic activities were produced with TAM combined with either cisplatin or doxorubicin."( The effects of estrogen, progesterone, and tamoxifen alone and in combination with cytotoxic agents against human ovarian carcinoma in vitro.
Berens, ME; Duckett, Y; Geisinger, KR; Kute, TE; Morgan, TM; Welander, CE, 1990
)
0.54
" The majority of patients with this subtype t-AML had prior cytotoxic therapy with topoisomerase II-reactive drugs including anthracyclines, epipodophyllotoxins, or actinomycin D, combined with either an alkylating agent or cisplatin."( Implication of prior treatment with drug combinations including inhibitors of topoisomerase II in therapy-related monocytic leukemia with a 9;11 translocation.
Albain, KS; Le Beau, MM; Schumacher, H; Ullirsch, R, 1990
)
0.28
" The radiation therapy was given with high-voltage techniques and included the chest wall and regional nodes."( Randomized trial of adjuvant tamoxifen combined with postoperative radiation therapy or adjuvant chemotherapy in postmenopausal breast cancer.
Askergren, J; Cedermark, B; Glas, U; Johansson, H; Rotstein, S; Rutqvist, LE; Skoog, L; Somell, A; Theve, T; Wilking, N, 1990
)
0.57
"Serum concentrations of growth hormone (GH) and somatomedin C were monitored in 14 women during post-menopausal replacement therapy with oestrogen alone and in combination with a specific antioestrogen."( Growth hormone and somatomedin C during post-menopausal replacement therapy with oestrogen alone and in combination with an antioestrogen.
Fröhlander, N; von Schoultz, B, 1988
)
0.27
" Our results indicate that HHNs are hormone-dependent and that malignant transformation can be inhibited by tamoxifen alone or in combination with estradiol-17 beta."( Tamoxifen alone or in combination with estradiol-17 beta inhibits the growth and malignant transformation of hepatic hyperplastic nodules.
Farber, E; Ho, R; Mishkin, S; Mishkin, SY; Mulay, S, 1985
)
1.92
" Our results indicated that HHNs are hormone-dependent and that malignant transformation can be inhibited by tamoxifen alone or in combination with estradiol-17 beta."( Tamoxifen alone or in combination with estradiol-17 beta inhibits the growth and malignant transformation of hepatic hyperplastic nodules.
Farber, E; Ho, R; Mishkin, S; Mishkin, SY; Mulay, S, 1985
)
1.92
" After addition and in combination with tamoxifen this LHRH-agonist treatment caused an objective response in about half (8/17) of the patients."( Long-term LHRH-agonist treatment in metastatic breast cancer as a single treatment and in combination with other additive endocrine treatments.
Klijn, JG, 1984
)
0.54
" for 7 days) in combination with a fixed dose of DNR (50 mg/m2 intravenously on days 5, 6 and 7) in patients with advanced leukemia to determine whether this combination could be given safely and whether plasma levels of 10 microM, the effective in vitro MDR modulator concentration, could be achieved."( Phase I trial of high-dose tamoxifen as a modulator of drug resistance in combination with daunorubicin in patients with relapsed or refractory acute leukemia.
Berman, E; Lin, S; McBride, M; Menedez-Botet, C; Tong, W, 1995
)
0.59
" Based on our previous experience with sequential cisplatin-interleukin-2 (IL2)-interferon (IFN), we performed a phase II study of TAM combined with our original CDDP-IL2-IFN regimen in 22 pretreated metastatic melanoma patients."( A phase II study of tamoxifen combined with cisplatin-interleukin 2 and alpha-interferon in metastatic melanoma.
Antoine, EC; Auclerc, G; Benhammouda, A; Borel, C; Franks, C; Ghironzi, GC; Mularoni, E; Rixe, O; Soubrane, C; Vuillemin, E, 1995
)
0.61
"A total of 39 patients with breast cancer of stages I and II received breast-conservation treatment (BCT) combined with tamoxifen and systemic chemotherapy (CAF) from August 1989 to March 1993."( Early experiences of breast-conservation treatment combined with tamoxifen and CAF chemotherapy for breast cancer of stages I and II.
Araki, K; Hamada, N; Inomata, T; Kumon, M; Nishioka, A; Ogawa, Y; Ogoshi, S; Tanaka, Y; Terashima, M; Yoshida, S,
)
0.58
" For suppression of carcinogenesis in vivo, 9cRA was much more potent than all-trans-retinoic acid, both as a single agent or in combination with TAM, although both retinoids had equivalent inhibitory effects on DNA synthesis in cultured human breast cancer cell lines."( Prevention of breast cancer in the rat with 9-cis-retinoic acid as a single agent and in combination with tamoxifen.
Anzano, MA; Brown, CC; Byers, SW; Mullen, LT; Peer, CW; Roberts, AB; Smith, JM; Sporn, MB, 1994
)
0.5
"The purpose of this study was to determine the maximal tolerable dose (MTD) of epirubicin and ADR-529 given in combination with cyclophosphamide, 5-fluorouracil, and tamoxifen."( The cardioprotector ADR-529 and high-dose epirubicin given in combination with cyclophosphamide, 5-fluorouracil, and tamoxifen: a phase I study in metastatic breast cancer.
Bastholt, L; Gjedde, SB; Jakobsen, P; Mirza, MR; Mouridsen, HT; Rose, C; Sørensen, B, 1994
)
0.69
"The effects of RU 486 combined with tamoxifen and tamoxifen alone on hormonal parameters and endometrial development at the time of implantation were studied."( 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
)
0.96
" In this study, we investigated the effect of the antiestrogen tamoxifen and the antiandrogen cyproterone acetate in combination with the LH-RH agonist buserelin in 9 patients with unresectable pancreatic adenocarcinoma."( Tamoxifen or cyproterone acetate in combination with buserelin are ineffective in patients with pancreatic adenocarcinoma.
Arnold, R; Havemann, K; Swarovsky, B; Wolf, M,
)
1.81
"In a prospective and randomized study comprising 540 primary endometrial carcinoma patients the influence of adjuvant hormone therapy by Oxyprogesterone caproate (OPC) and by its combination with Tamoxifen on the corrected survival rates after surgical and combined (surgical and irradiation) therapy was investigated."( Favourable influence of adjuvant hormone therapy by oxyprogesterone caproate (OPC) and by its combination with tamoxifen on 5-year survival rate of surgical and combined treatment of primary endometrial carcinoma patients.
Loutfi, G; Vishnevsky, AS, 1993
)
0.69
" If treatment with DPPE was begun from the day after tumor inoculation, the inhibitory effect of DPPE was further enhanced, especially when combined with CDDP."( Growth-inhibitory effects of N,N-diethyl-2-[4-(phenylmethyl)phenoxy]-ethanamine-HCl combined with cisplatin on human ovarian cancer cells inoculated into nude mice.
Hiramatsu, H; Kikuchi, Y; Kita, T; Kudoh, K; Nagata, I; Tode, T, 1997
)
0.3
"One hundred thirty-five eligible postmenopausal women with metastatic breast carcinoma were randomized to TAM (10 mg twice daily) alone or combined with octreotide 150 microg (administered subcutaneously thrice daily)."( A randomized trial of tamoxifen alone or combined with octreotide in the treatment of women with metastatic breast carcinoma.
Conover, CA; Dalton, RJ; Hartmann, LC; Ingle, JN; Kardinal, CG; Krook, JE; Loprinzi, CL; Mailliard, JA; Pollak, MN; Suman, VJ; Veeder, MH, 1999
)
0.62
"The toxicity of DFMO in combination with TAM was evaluated in female Beagle dogs following 13 weeks of daily oral administration by capsule."( Thirteen-week oral toxicity study of difluoromethylornithine in combination with tamoxifen citrate in female dogs.
Brown, AP; Crowell, JA; Levine, BS; Morrissey, RL, 1999
)
0.53
"The toxicity of DFMO in combination with TAM was evaluated in female rats following 13 weeks of daily administration by gavage."( Difluoromethylornithine in combination with tamoxifen in female rats: 13-week oral toxicity study.
Brown, AP; Crowell, JA; Levine, BS; Morrissey, RL, 1999
)
0.56
"The reversal effects of quinine (Quin) in combination with cyclosporin A (CsA), dipyridamole (DPM) or tamoxifen (Tam), respectively on the drug resistance of K562/HHT were studied by MTT, flow cytometry and median-effect principle."( [Synergistic reversal effect of quinine in combination with modulators on multidrug resistant cell line K562/HHT].
Bian, S; Feng, M; Luo, M, 1998
)
0.52
" Quin combined with CsA increased intracellular DNR accumulation significantly as compared with either of them alone."( [Synergistic reversal effect of quinine in combination with modulators on multidrug resistant cell line K562/HHT].
Bian, S; Feng, M; Luo, M, 1998
)
0.3
" Hyperthermia in combination with radiotherapy or chemotherapy for breast cancer may produce a remarkable effect as in the present case, and may become one choice for medical treatment of locally advanced or recurrent breast cancer."( [A case of locally advanced breast cancer treated with hyperthermia in combination with radiotherapy].
Kawasaki, K; Kishibuchi, M; Nishi, T; Nishide, T; Ostapenko, V; Yagyu, T; Yamasaki, M; Yayoi, E, 2001
)
0.31
"To compare the effects of one year treatment of estrogen and tamoxifen, either alone or combined with fluoride on bone metabolism in ovariectomized rats."( [One year observation on effects of estrogen, tamoxifen combined with or without fluoride on preventing bone loss in ovariectomized rats].
Liu, H; Liu, J; Peng, H, 2002
)
0.81
" Further studies should be conducted to determine whether tamoxifen combined with mifepristone for emergency contraception is more effective as compared with mifepristone alone."( A randomized comparative study on mifepristone alone and in combination with tamoxifen for emergency contraception.
Bingshun, W; Changhai, H; Ersheng, G; Exiang, Z; Jie, Y; Mauck, C; Youlun, G, 2002
)
0.79
"We conducted a phase I study of high-dose oral tamoxifen in combination with intravenous cisplatin, with two objectives: 1) to determine tolerability, and 2) to determine the daily tamoxifen dose required to achieve serum levels equivalent to in vitro concentrations reported to enhance cisplatin cytotoxicity in preclinical models."( Phase I trial of high-dose tamoxifen in combination with cisplatin in patients with lung cancer and other advanced malignancies.
DeGregorio, M; Edelman, MJ; Gandara, DR; Lauder, IJ; O'Donnell, R; Perez, EA, 2003
)
0.87
" Classic dose-limiting toxicity was not observed; the trial was closed to further accrual after documentation that targeted tamoxifen levels (around 5 microM) were achieved with daily tamoxifen doses > or = 160 mg/m2 in combination with cisplatin."( Phase I trial of high-dose tamoxifen in combination with cisplatin in patients with lung cancer and other advanced malignancies.
DeGregorio, M; Edelman, MJ; Gandara, DR; Lauder, IJ; O'Donnell, R; Perez, EA, 2003
)
0.82
"This regimen of high-dose tamoxifen in combination with cisplatin can be safely administered."( Phase I trial of high-dose tamoxifen in combination with cisplatin in patients with lung cancer and other advanced malignancies.
DeGregorio, M; Edelman, MJ; Gandara, DR; Lauder, IJ; O'Donnell, R; Perez, EA, 2003
)
0.92
"In this phase I/II clinical trial the antitumor activity of high-dose tamoxifen when administered in combination with vinblastine was assessed and the toxicity profile of this combination characterized."( A phase I/II study of high-dose tamoxifen in combination with vinblastine in patients with androgen-independent prostate cancer.
Brawley, O; Dahut, W; Davis, P; Duray, P; Figg, WD; Hamilton, M; Kohler, D; Lakhani, N; Liewehr, DJ; Reed, E; Steinberg, SM; Wells-Jones, T, 2003
)
0.84
"To evaluate the effect of tamoxifen (TAM) combined with a somatostatin analogue, octretide (OCT) on advanced liver cancer and whether tamoxifen combined with OCT is superior to regular chemotherapeutic agents 5-Fu and mitomycin C (MMC)."( Tamoxifen combined with octreotide or regular chemotherapeutic agents in treatment of primary liver cancer: a randomized controlled trial.
Chen, JW; Huo, YC; Pan, DY; Qiao, JG; Shi, HA; Zhou, YK, 2003
)
2.06
"To study the correlation of the reversal effect of tetrandrine (Tet) in combination with droloxifene (DRL) on multidrug resistant cell line K562/A02 and induction apoptosis, the apoptosis of K562 cells and K562/A02 cells after the treatment of Tet and DRL alone or their combination was detected by flow cytometry (FCM)."( [Reversal effect of tetrandrine in combination with droloxifene on cell line K562/A02 and its correlation with inducted apoptosis].
Chen, BA; Cheng, J; Dong, Y; Gao, F; Sheng, M; Wang, T; Zhang, P; Zhou, Y, 2004
)
0.32
"To observe the effect of Tetrandrine (tet) combined with Droloxifen (DRL) on the expression of bcr/abl mRNA and P(210) BCR/ABL protein of K562 cell line, after K562 cells were cultured in the medium containing Tet (1 micromol/L), DRL (5 micromol/L) separately or in their combination for some time, the changes of bcr/abl mRNA and protein expression were detected by RT-PCR and Western blot respectively."( [Effect of tetrandrine combined with Droloxifen on the expression of bcr/abl of K562 at both mRNA and protein levels].
Chen, BA; Cheng, J; Gao, F; Qian, XJ, 2005
)
0.33
"The Immediate Preoperative Anastrozole, Tamoxifen, or Combined With Tamoxifen (IMPACT) trial was designed to test the hypothesis that the clinical and/or biologic effects of neoadjuvant tamoxifen compared with anastrozole and with the combination of tamoxifen and anastrozole before surgery in postmenopausal women with estrogen receptor (ER) -positive, invasive, nonmetastatic breast cancer might predict for outcome in the Arimidex, Tamoxifen Alone or in Combination (ATAC) adjuvant therapy trial."( Neoadjuvant treatment of postmenopausal breast cancer with anastrozole, tamoxifen, or both in combination: the Immediate Preoperative Anastrozole, Tamoxifen, or Combined with Tamoxifen (IMPACT) multicenter double-blind randomized trial.
Ashley, SE; Blohmer, JU; Boeddinghaus, I; Dixon, JM; Dowsett, M; Ebbs, SR; Francis, S; Skene, A; Smith, IE; Walsh, G, 2005
)
0.83
"The aim of this study was to investigate the mechanism to reverse the drug resistance of leukemia cells in tetrandrine (Tet) alone or in combination with droloxifen (Drol) by using protein chips and to lay the theoretical basis for the clinical applications."( [Using protein chips to study mechanism underlying reversion of drug resistance in leukemia cells in tetrandrine alone or in combination with droloxifene].
Chen, BA; Cheng, J; Du, J; Gao, F; Lu, ZH; Zhang, CX, 2005
)
0.33
"The purpose of this study was to evaluate the effect of tamoxifen (TAM) when used in combination with cisplatin on oral squamous cell carcinoma (OSCC)."( The role of tamoxifen in combination with cisplatin on oral squamous cell carcinoma cell lines.
Kim, MJ; Kim, YK; Lee, JH; Myoung, H; Yun, PY, 2007
)
0.96
"Postmenopausal women with early stage breast cancer that was known to be estrogen receptor (ER) positive were randomized to treatment with Tam (20 mg per day orally for 5 years) alone or combined with Flu (10 mg orally twice per day for 1 year)."( Randomized trial of tamoxifen alone or combined with fluoxymesterone as adjuvant therapy in postmenopausal women with resected estrogen receptor positive breast cancer. North Central Cancer Treatment Group Trial 89-30-52.
Donohue, JH; Goetz, MP; Ingle, JN; Krook, JE; Kugler, JW; Mailliard, JA; Michalak, JC; Perez, EA; Pisansky, TM; Suman, VJ; Wold, LE, 2006
)
0.66
" This study was to evaluate the chemopreventive effect of tamoxifen combined with celecoxib, a COX-2 selective inhibitor, on 7,12-dimethylbenz anthracene (DMBA)-induced breast cancer in rats."( [Chemopreventive effect of tamoxifen combined with celecoxib on DMBA-induced breast cancer in rats].
Dai, ZJ; Kang, HF; Liu, XX; Wang, XJ; Xue, FJ; Xue, XH, 2006
)
0.88
" Our objective was to determine the effects of liarozole alone or in combination with tamoxifen on the N-methyl-N-nitrosourea (MNU)-induced rat mammary carcinoma model, as well as on the uterus in ovariectomized immature rats."( Effects of liarozole fumarate (R85246) in combination with tamoxifen on N-methyl-N-nitrosourea (MNU)-induced mammary carcinoma and uterus in the rat model.
Goss, PE; Hu, H; Qi, S; Strasser-Weippl, K, 2007
)
0.81
" In combination with tamoxifen, liarozole had neither an additive nor an antagonistic effect."( Effects of liarozole fumarate (R85246) in combination with tamoxifen on N-methyl-N-nitrosourea (MNU)-induced mammary carcinoma and uterus in the rat model.
Goss, PE; Hu, H; Qi, S; Strasser-Weippl, K, 2007
)
0.9
"Liarozole's antitumor effects on ER positive mammary tumors and its protective effect on the uterus merit further studies to confirm its clinical value in combination with tamoxifen in ER positive postmenopausal breast cancer."( Effects of liarozole fumarate (R85246) in combination with tamoxifen on N-methyl-N-nitrosourea (MNU)-induced mammary carcinoma and uterus in the rat model.
Goss, PE; Hu, H; Qi, S; Strasser-Weippl, K, 2007
)
0.78
" This study determined whether the effect of FS, alone or in combination with TAM, is dose dependent, and it explored the potential mechanism of action."( Flaxseed alone or in combination with tamoxifen inhibits MCF-7 breast tumor growth in ovariectomized athymic mice with high circulating levels of estrogen.
Chen, J; Cheng, A; Mann, J; Power, KA; Thompson, LU, 2007
)
0.61
" We therefore investigated the efficacy of the farnesyltransferase inhibitor (FTI) R115777 (tipifarnib) in combination with tamoxifen in MCF-7 human breast cancer models both in vitro and in vivo."( The farnesyltransferase inhibitor R115777 (tipifarnib) in combination with tamoxifen acts synergistically to inhibit MCF-7 breast cancer cell proliferation and cell cycle progression in vitro and in vivo.
Detre, S; Dowsett, M; Head, JE; Howes, A; Johnston, SR; Kaye, S; Martin, LA; Pancholi, S; Quinn, E; Salter, J, 2007
)
0.78
" The results demonstrate that tamoxifen at realistic doses (75 mug kg(-1)) can suppress the growth of ER-negative breast cancer when combined with EGCG."( A new role for tamoxifen in oestrogen receptor-negative breast cancer when it is combined with epigallocatechin gallate.
Menzies, AR; Rosengren, RJ; Scandlyn, MJ; Somers-Edgar, TJ; Stuart, EC, 2008
)
0.99
"To study the effect of tetrandrine (Tet) in combination with droloxifen (DRL) on the expression of nuclear factor kappa B (NF-kappaB) in K562 and K562/A02 cell lines and its reversal mechanism."( [Effect of tetrandrine in combination with droloxifen on the expression of NF-kappaB protein in K562 and K562/A02 cell lines].
Chen, BA; Chen, NN; Cheng, HY; Cheng, J; Ding, JH; Gao, C; Gao, F; Huang, CY; Shen, HL; Su, AL; Sun, XC; Sun, YY; Wang, J; Xu, WL; Zhao, G; Zhao, HH, 2008
)
0.35
" Rats bearing DMBA- or NMU-induced mammary tumors were treated with ON or MEG either alone or in combination with TAM for four weeks."( Potentiation of the antitumor effect of tamoxifen by combination with the antiprogestin onapristone.
Hirtreiter, C; Ishibashi, K; Nishino, T; Nishino, Y, 2009
)
0.62
" Tegafur and Uracil (UFT) have been widely used for the postoperative chemotherapy of breast cancer, and often combined with hormonal agents."( [Safety and compliance with UFT (tegafur and uracil) alone and in combination with hormone therapy in patients with breast cancer].
Noguchi, S; Taguchi, T, 2009
)
0.35
"The effects of retinoids combined with trastuzumab or tamoxifen were examined in two human breast cancer cell lines in culture, BT474 and SKBR3."( Anti-tumor effects of retinoids combined with trastuzumab or tamoxifen in breast cancer cells: induction of apoptosis by retinoid/trastuzumab combinations.
DiGiovanna, MP; Harris, LN; Koay, DC; Narayan, M; Zerillo, C, 2010
)
0.85
" BT474 and HER2-overexpressing/ER-negative SKBR3 cells were treated with a panel of retinoids (atRA, 9-cis-retinoic acid, 13-cis-retinoic acid, or N-(4-hydroxyphenyl) retinamide (fenretinide) (4-HPR)) combined with trastuzumab."( Anti-tumor effects of retinoids combined with trastuzumab or tamoxifen in breast cancer cells: induction of apoptosis by retinoid/trastuzumab combinations.
DiGiovanna, MP; Harris, LN; Koay, DC; Narayan, M; Zerillo, C, 2010
)
0.6
"We conducted a double-blinded, placebo-controlled pilot trial to test the effectiveness of adjuvant tocotrienol therapy in combination with tamoxifen for five years in women with early breast cancer."( Effectiveness of tocotrienol-rich fraction combined with tamoxifen in the management of women with early breast cancer: a pilot clinical trial.
Abdul Razak, G; Gomez, PA; Nesaretnam, K; Selvaduray, KR; Veerasenan, SD, 2010
)
0.81
" Interestingly, TAM affected all tested cell lines, irrespective of their ER-a status, and in combination with ROSC it enhanced G1 or G2 arrest."( Effect of anti-estrogen combined with roscovitine, a selective CDK inhibitor, on human breast cancer cells differing in expression of ER.
Maurer, M; Wesierska-Gadek, J; Zulehner, N, 2011
)
0.37
" Due to the potential for drug-drug interactions, the ability of toremifene and its primary circulating metabolite N-desmethyltoremifene (NDMT) to inhibit nine human cytochrome P450 (CYP) enzymes was determined using human liver microsomes."( Drug interaction potential of toremifene and N-desmethyltoremifene with multiple cytochrome P450 isoforms.
Dalton, JT; Johanning, KM; Kim, J; Peraire, C; Solà, J; Veverka, KA, 2011
)
0.37
"To investigate the effects of tamoxifen (TMX) combined with coenzyme Q10 (CoQ10) on idiopathic oligoasthenospermia."( [Tamoxifen combined with coenzyme Q10 for idiopathic oligoasthenospermia].
Liu, RZ; Tang, KF; Wang, XY; Wu, CY; Xing, JP; Xing, Y, 2011
)
1.57
"Tamoxifen combined with CoQ10 can significantly improve sperm concentration, motility and morphology in patients with idiopathic oligoasthenospermia."( [Tamoxifen combined with coenzyme Q10 for idiopathic oligoasthenospermia].
Liu, RZ; Tang, KF; Wang, XY; Wu, CY; Xing, JP; Xing, Y, 2011
)
2.72
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38
" This analysis evaluated efficacy and safety of everolimus in combination with tamoxifen in patients with mBC resistant to aromatase inhibitors (AIs)."( Randomized phase II trial of everolimus in combination with tamoxifen in patients with hormone receptor-positive, human epidermal growth factor receptor 2-negative metastatic breast cancer with prior exposure to aromatase inhibitors: a GINECO study.
Abadie-Lacourtoisie, S; Allouache, D; Bachelot, T; Bourgier, C; Cropet, C; Debled, M; El Kouri, C; Eymard, JC; Ferrero, JM; Freyer, G; Legouffe, E; Pujade-Lauraine, E; Ray-Coquard, I; Spaëth, D, 2012
)
0.85
" We developed a mouse model for ER+ breast cancer bone metastasis and evaluated the effect of RANKL inhibition on tumor-induced osteolysis and skeletal tumor growth both alone and in combination with tamoxifen."( RANKL inhibition combined with tamoxifen treatment increases anti-tumor efficacy and prevents tumor-induced bone destruction in an estrogen receptor-positive breast cancer bone metastasis model.
Branstetter, DG; Bryant, R; Canon, J; Dougall, WC; Roudier, M, 2012
)
0.85
"BC cell lines expressing aromatase (AROM) and modeling endocrine-sensitive (MCF7-AROM1) and human epidermal growth factor receptor 2 (HER2)-dependent de novo resistant disease (BT474-AROM3) and long-term estrogen-deprived (LTED) MCF7 cells that had acquired resistance associated with HER2 overexpression were treated in vitro and as subcutaneous xenografts with everolimus (RAD001-mTORC1 inhibitor), in combination with tamoxifen or letrozole."( Effectiveness and molecular interactions of the clinically active mTORC1 inhibitor everolimus in combination with tamoxifen or letrozole in vitro and in vivo.
A'Hern, R; Dowsett, M; Evans, DB; Farmer, I; Ghazoui, Z; Guest, S; Johnston, SR; Lane, HA; Martin, LA; Pancholi, S; Ribas, R; Thornhill, AM; Weigel, MT, 2012
)
0.75
"To study the demethylation effect of arsenic trioxide (As2O3) on ERα-negative human breast cancer MDA-MB-435s cells and its possible mechanisms, and to observe its treatment efficacy in combination with tamoxifen (TAM) after ERα re-expression."( [Arsenic trioxide restores ERα expression in ERα-negative human breast cancer cells and its treatment efficacy in combination with tamoxifen in xenografts in nude mice].
Fan, QX; Wang, F; Wang, LX; Wang, R; Wu, XA; Xu, DF; Zhang, WJ, 2012
)
0.77
"MTT assay was used to examine the inhibitory effect of As2O3 treatment alone or in combination with TAM on cell proliferation."( [Arsenic trioxide restores ERα expression in ERα-negative human breast cancer cells and its treatment efficacy in combination with tamoxifen in xenografts in nude mice].
Fan, QX; Wang, F; Wang, LX; Wang, R; Wu, XA; Xu, DF; Zhang, WJ, 2012
)
0.58
"The level of proliferation of the MDA-MB-435s cells was significantly suppressed after treatment with different concentration of As2O3 alone or As2O3 combined with TAM, and the 4 µmol/L As2O3 + TAM treatment for 72 h showed the highest inhibition rate (62."( [Arsenic trioxide restores ERα expression in ERα-negative human breast cancer cells and its treatment efficacy in combination with tamoxifen in xenografts in nude mice].
Fan, QX; Wang, F; Wang, LX; Wang, R; Wu, XA; Xu, DF; Zhang, WJ, 2012
)
0.58
" As2O3 combined with TAM may provide a new therapeutic approach for patients with ERα-negative breast cancer in the clinic."( [Arsenic trioxide restores ERα expression in ERα-negative human breast cancer cells and its treatment efficacy in combination with tamoxifen in xenografts in nude mice].
Fan, QX; Wang, F; Wang, LX; Wang, R; Wu, XA; Xu, DF; Zhang, WJ, 2012
)
0.58
"Leukemia, breast and cervical cancer cell lines were exposed to D3CLP-alone or in combination with imatinib, tamoxifen or cisplatin, respectively."( Synergistic anticancer activity of Thiazolo[5,4-b]quinoline derivative D3CLP in combination with cisplatin in human cervical cancer cells.
Cerbón, MA; Coronel-Cruz, C; González-Sánchez, I; Lira-Rocha, A; Loza-Mejía, MA; Mendoza-Rodríguez, CA; Navarrete, A, 2012
)
0.59
"Antiproliferative activity results indicate that D3CLP in combination with antineoplastic drugs induced a synergistic effect, at 3:1 and 1:1 ratios for D3CLP plus imatinib in K-562 leukemia cells, and at a 3:1 ratio for D3CLP with cisplatin in HeLa cells, as determined by their combination index."( Synergistic anticancer activity of Thiazolo[5,4-b]quinoline derivative D3CLP in combination with cisplatin in human cervical cancer cells.
Cerbón, MA; Coronel-Cruz, C; González-Sánchez, I; Lira-Rocha, A; Loza-Mejía, MA; Mendoza-Rodríguez, CA; Navarrete, A, 2012
)
0.38
" This work evaluated the effects of RA alone and in combination with the antiestrogen endoxifen (EDX) on liver mitochondria."( Effects of all-trans-retinoic acid on the permeability transition and bioenergetic functions of rat liver mitochondria in combination with endoxifen.
Custódio, JB; Ribeiro, MP; Santos, AE; Santos, MS, 2013
)
0.39
"RA-induced hepatotoxicity may be related with induction of MPT and alterations in bioenergetic parameters; the combination with EDX, which reduces mitochondrial dysfunction and synergistically potentiates the anticancer activity, may provide a safer therapeutic strategy."( Effects of all-trans-retinoic acid on the permeability transition and bioenergetic functions of rat liver mitochondria in combination with endoxifen.
Custódio, JB; Ribeiro, MP; Santos, AE; Santos, MS, 2013
)
0.39
"The role of aromatase inhibitors combined with gonadotropin-releasing hormone analog in metastatic male breast cancer patients remains unknown."( Letrozole combined with gonadotropin-releasing hormone analog for metastatic male breast cancer.
Barba, M; Del Medico, P; Di Lauro, L; Giannarelli, D; Laudadio, L; Maugeri-Saccà, M; Pizzuti, L; Sergi, D; Tomao, S; Vici, P, 2013
)
0.39
" Drugs were selected based not only on the knowledge that the 6-hydroxylation of exogenous melatonin, its principal pathway of metabolism, is mainly mediated by hepatic CYP1A2, but also on the likelihood of the drug being concurrently administered with melatonin."( Potential drug interactions with melatonin.
Ioannides, C; Papagiannidou, E; Skene, DJ, 2014
)
0.4
" During period 2, subjects received desvenlafaxine 100 mg/d for 28 days; a single dose of tamoxifen 40 mg was administered with desvenlafaxine 100 mg on day 7, followed by 23 days of blood sampling."( Open-label, 2-period sequential drug interaction study to evaluate the effect of a 100-mg dose of desvenlafaxine on the pharmacokinetics of tamoxifen when coadministered in healthy postmenopausal female subjects.
Braley, G; Liang, Y; Lubaczewski, S; Matschke, K; Nichols, AI; Ramey, T, 2014
)
0.83
" 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
"Considering the ability of SCS to also promote the activity of the antiestrogen, tamoxifen, we further examined the effect of SCS in modulating cell cycle progression and related proteins in MCF-7 and MDA-MB-231 cells alone and in combination with tamoxifen."( Cell Cycle Modulation of MCF-7 and MDA-MB-231 by a Sub- Fraction of Strobilanthes crispus and its Combination with Tamoxifen.
Nik Mohamed Kamal, NN; Norazmi, MN; Wong, KK; Yaacob, NS, 2015
)
0.85
" In combination with tamoxifen, the anticancer effects involved downregulation of ERα protein in MCF-7 cells but appeared independent of an ER-mediated mechanism in MDA-MB-231 cells."( Cell Cycle Modulation of MCF-7 and MDA-MB-231 by a Sub- Fraction of Strobilanthes crispus and its Combination with Tamoxifen.
Nik Mohamed Kamal, NN; Norazmi, MN; Wong, KK; Yaacob, NS, 2015
)
0.95
"Although radiotherapy and tamoxifen have been extensively used to treat estrogen receptor α (ERα)-positive breast cancers, it is still questionable when tamoxifen should be started to maximize clinical benefits in combination with radiotherapy."( Determination of the optimal time for tamoxifen treatment in combination with radiotherapy.
Baek, J; Jang, H; Kim, S; Nam, KS, 2016
)
1.01
" Antidepressants (ADs), which are often coprescribed to patients receiving tamoxifen, are also metabolized by CYP2D6 and evidence suggests that a drug-drug interaction between these agents adversely affects the outcome of tamoxifen therapy by inhibiting endoxifen formation."( Application of Mice Humanized for CYP2D6 to the Study of Tamoxifen Metabolism and Drug-Drug Interaction with Antidepressants.
Henderson, CJ; MacLeod, AK; McLaughlin, LA; Wolf, CR, 2017
)
0.93
"To determine the impact on antitumor activity when active hexose correlated compound (AHCC) in combination with anticancer hormonal agents in orthotopic mouse models of human estrogen receptor positive breast cancer and evaluate impact of AHCC on aromatase activity."( Evaluation of Active Hexose Correlated Compound (AHCC) in Combination With Anticancer Hormones in Orthotopic Breast Cancer Models.
Gaikwad, A; Gonzalez, A; Mathew, L; Nugent, EK; Smith, JA, 2017
)
0.46
"We conducted an open-label, randomized controlled trial evaluating the appropriate treatment duration of leuprorelin acetate 3-month depot, TAP-144-SR (3M), administered postsurgically every 3 months for 2 years versus 3 or more (up to 5) years, in combination with tamoxifen, for 5 years in premenopausal endocrine-responsive breast cancer patients and reported similar survival benefit in the two treatment groups."( Comparison of quality of life between 2-year and 3-or-more-year administration of leuprorelin acetate every-3-months depot in combination with tamoxifen as adjuvant endocrine treatment in premenopausal patients with endocrine-responsive breast cancer: a r
Fujimoto, T; Iwase, H; Kurebayashi, J; Noguchi, S; Ohashi, Y; Shiba, E; Yamashita, H; Yoshida, M, 2018
)
0.86
"Improved activity was observed with UPF or FVF in combination with tamoxifen in both the MCF-7 and ZR-75D breast cancer mouse models."( Evaluation Fucoidan Extracts From Undaria pinnatifida and Fucus vesiculosus in Combination With Anticancer Drugs in Human Cancer Orthotopic Mouse Models.
Burney, M; Gaikwad, A; Gonzalez, AO; Mathew, L; Nugent, EK; Smith, JA, 2018
)
0.72
"This study did confirm that UPF/FVF in combination with tamoxifen did not decrease tamoxifen activity in both breast and ovarian cancer, with some potential to improve activity compared to tamoxifen alone in breast cancers."( Evaluation Fucoidan Extracts From Undaria pinnatifida and Fucus vesiculosus in Combination With Anticancer Drugs in Human Cancer Orthotopic Mouse Models.
Burney, M; Gaikwad, A; Gonzalez, AO; Mathew, L; Nugent, EK; Smith, JA, 2018
)
0.73
" The present work determines if AE-PG alone or in combination with the selective serotonin reuptake inhibitor, citalopram, has antidepressant-like effects."( Aqueous Extract of Pomegranate Alone or in Combination with Citalopram Produces Antidepressant-Like Effects in an Animal Model of Menopause: Participation of Estrogen Receptors.
Estrada-Camarena, E; García-Viguera, C; González-Trujano, ME; López-Rubalcava, C; Valdés-Sustaita, B, 2017
)
0.46
" In addition to drug-drug interactions (DDI) involving CYP2D6, there is growing evidence that enzyme inducers can substantially alter the disposition of endoxifen, reducing tamoxifen efficacy."( The Underrated Risks of Tamoxifen Drug Interactions.
Hansten, PD, 2018
)
0.98
"To investigate the effect of alpha-lipoic acid (α-LA) combined with tamoxifen citrate (TC) in the treatment of oligoasthenospermia."( [Efficacy of alpha-lipoic acid combined with tamoxifen citrate in the treatment of oligoasthenospermia].
Chang, XL; Li, JD; Li, W; Teng, ZH; Wang, YX; Yang, SW; Zhang, H; Zhang, YP, 2017
)
0.95
"Alpha-lipoic acid combined with tamoxifen citrate can evidently improve semen parameters in oligoasthenospermia patients by relieving oxidative stress injury."( [Efficacy of alpha-lipoic acid combined with tamoxifen citrate in the treatment of oligoasthenospermia].
Chang, XL; Li, JD; Li, W; Teng, ZH; Wang, YX; Yang, SW; Zhang, H; Zhang, YP, 2017
)
1
"To explore the feasibility, safety and clinical effect of mid-frequency transcutaneous electrical acupoint stimulation (TEAS) combined with oral tamoxifen (TAM) in the treatment of oligoasthenozoospermia."( [Mid-frequency transcutaneous electrical acupoint stimulation combined with tamoxifen for the treatment of oligoasthenozoospermia].
Li, H; Li, T; Tan, Y; Wang, WR; Xie, S; Xie, ZP, 2017
)
0.89
"Mid-frequency TEAS combined with tamoxifen can significantly improve semen quality and increase sex hormone levels in patients with idiopathic oligoasthenozoospermia."( [Mid-frequency transcutaneous electrical acupoint stimulation combined with tamoxifen for the treatment of oligoasthenozoospermia].
Li, H; Li, T; Tan, Y; Wang, WR; Xie, S; Xie, ZP, 2017
)
0.97
"The PARP inhibitor olaparib is efficacious as monotherapy and has potential application in combination with endocrine therapy for the treatment of breast cancer."( Pharmacokinetic Effects and Safety of Olaparib Administered with Endocrine Therapy: A Phase I Study in Patients with Advanced Solid Tumours.
Bailey, C; Birkett, J; De Grève, J; De Vos, FYFL; Dean, E; Dirix, L; Goessl, C; Grundtvig-Sørensen, P; Italiano, A; Jerusalem, G; Learoyd, M; Leunen, K; Molife, LR; Plummer, R; Rolfo, C; Rottey, S; Spencer, S; Spicer, J; Verheul, HM, 2018
)
0.48
"The in vitro results suggest that mistletoe preparations can be used in combination with tamoxifen without the risk of HDIs."( Absence of herb-drug interactions of mistletoe with the tamoxifen metabolite (E/Z)-endoxifen and cytochrome P450 3A4/5 and 2D6 in vitro.
Baumgartner, S; Hamburger, M; Kunz, M; Oufir, M; Regueiro, U; Urech, K; Wang, JT; Weissenstein, U, 2019
)
0.98
" Therefore, this study attempted to demonstrate the in vitro anti-cancer activity of high-dose vitamin C in combination with conventional treatment in breast cancer."( Effect of High-dose Vitamin C Combined With Anti-cancer Treatment on Breast Cancer Cells.
Chae, YS; Jeong, JH; Jung, JH; Lee, DH; Lee, IH; Lee, J; Lee, SJ; Park, HY, 2019
)
0.51
"30 patients with ER-positive, metastatic breast cancer who had failed prior endocrine therapy were treated with escalating doses of taselisib (2 or 4 mg in an intermittent or continuous schedule) combined with tamoxifen 20 mg once daily in this phase 1b study using a "rolling six" design."( POSEIDON Trial Phase 1b Results: Safety, Efficacy and Circulating Tumor DNA Response of the Beta Isoform-Sparing PI3K Inhibitor Taselisib (GDC-0032) Combined with Tamoxifen in Hormone Receptor Positive Metastatic Breast Cancer Patients.
Baird, RD; Beddowes, E; Beelen, K; Bernards, R; Caldas, C; Callari, M; Cortès, J; de Vries Schultink, A; Dougall, G; Gallagher, W; Gao, M; Garcia-Corbacho, J; Kumar, S; Linn, SC; Linossi, C; Mandjes, IAM; Nederlof, P; Oliveira, M; Perez-Garcia, JM; Platte, E; Rosing, H; Saura, C; Schot, M; Schrier, M; Vallier, AL; van Rossum, AGJ; van Tinteren, H; van Werkhoven, E, 2019
)
0.9
"Taselisib combined with tamoxifen was generally well tolerated, with treatment-emergent adverse events as expected for this class of drugs, including diarrhea (13 patients, 43%), mucositis (10 patients, 33%), and hyperglycemia (8 patients, 27%)."( POSEIDON Trial Phase 1b Results: Safety, Efficacy and Circulating Tumor DNA Response of the Beta Isoform-Sparing PI3K Inhibitor Taselisib (GDC-0032) Combined with Tamoxifen in Hormone Receptor Positive Metastatic Breast Cancer Patients.
Baird, RD; Beddowes, E; Beelen, K; Bernards, R; Caldas, C; Callari, M; Cortès, J; de Vries Schultink, A; Dougall, G; Gallagher, W; Gao, M; Garcia-Corbacho, J; Kumar, S; Linn, SC; Linossi, C; Mandjes, IAM; Nederlof, P; Oliveira, M; Perez-Garcia, JM; Platte, E; Rosing, H; Saura, C; Schot, M; Schrier, M; Vallier, AL; van Rossum, AGJ; van Tinteren, H; van Werkhoven, E, 2019
)
1.02
"Taselisib can be safely combined with tamoxifen at the recommended phase 2 dose of 4 mg given once daily on a continuous schedule."( POSEIDON Trial Phase 1b Results: Safety, Efficacy and Circulating Tumor DNA Response of the Beta Isoform-Sparing PI3K Inhibitor Taselisib (GDC-0032) Combined with Tamoxifen in Hormone Receptor Positive Metastatic Breast Cancer Patients.
Baird, RD; Beddowes, E; Beelen, K; Bernards, R; Caldas, C; Callari, M; Cortès, J; de Vries Schultink, A; Dougall, G; Gallagher, W; Gao, M; Garcia-Corbacho, J; Kumar, S; Linn, SC; Linossi, C; Mandjes, IAM; Nederlof, P; Oliveira, M; Perez-Garcia, JM; Platte, E; Rosing, H; Saura, C; Schot, M; Schrier, M; Vallier, AL; van Rossum, AGJ; van Tinteren, H; van Werkhoven, E, 2019
)
0.98
" Therefore we investigated whether there is a drug-drug interaction between tamoxifen and SRIs resulting in a prolonged QTc-interval."( The Risk of QTc-Interval Prolongation in Breast Cancer Patients Treated with Tamoxifen in Combination with Serotonin Reuptake Inhibitors.
Berger, FA; Binkhorst, L; de Groot, NMS; Hussaarts, KGAM; Mathijssen, RHJ; Mathijssen-van Stein, D; Oomen-de Hoop, E; van Alphen, RJ; van Gelder, T; van Leeuwen, RWF, 2019
)
0.97
" Proliferation of MCF-7, a breast cancer cell line, was investigated after treatment with Lactobacillus Brevis supernatant (LBS) solely, and in combination with Tamoxifen."( Synergistic Cytotoxic and Apoptotic Effects of Local Probiotic Lactobacillus Brevis Isolated from Regional Dairy Products in Combination with Tamoxifen.
Akbari, N; Mirfazli, SS; Montazeri, H; Nasiri, Z; Tarighi, P, 2021
)
1.02
" The RP2D of alpelisib and buparlisib in combination with tamoxifen and goserelin were 350 mg and 100 mg, respectively."( A Phase Ib Study of Alpelisib or Buparlisib Combined with Tamoxifen Plus Goserelin in Premenopausal Women with HR-Positive HER2-Negative Advanced Breast Cancer.
Chang, YC; Chao, TY; Chen, SC; Chitapanarux, I; Gao, M; Jung, KH; Kim, JH; Lee, KS; Liu, CT; Lu, YS; Park, YH; Shotelersuk, K; Slader, C; Sohn, J; Tseng, LM; Valenti, R; Yang, Y, 2021
)
1.11
"To explore the efficacy and safety of everolimus combined with endocrine therapy in patients with hormone receptor (HR)-positive/human epidermal growth factor receptor 2 (HER-2)-negative advanced breast cancer."( Efficacy of everolimus combined with endocrine therapy in HR-positive/HER-2-negativeadvanced breast cancer.
Chen, C; Kong, F; Lu, J; Shan, H; Song, X; Wang, L; Yuan, H,
)
0.13
" Of them, 54 patients were treated with everolimus combined with endocrine drugs (Everolimus group), while the other 54 patients underwent endocrine monotherapy (Control group)."( Efficacy of everolimus combined with endocrine therapy in HR-positive/HER-2-negativeadvanced breast cancer.
Chen, C; Kong, F; Lu, J; Shan, H; Song, X; Wang, L; Yuan, H,
)
0.13
"Everolimus combined with endocrine therapy has significant clinical efficacy in patients with HR-positive/HER-2-negative advanced breast cancer, and can effectively improve the survival of patients with tolerable adverse reactions."( Efficacy of everolimus combined with endocrine therapy in HR-positive/HER-2-negativeadvanced breast cancer.
Chen, C; Kong, F; Lu, J; Shan, H; Song, X; Wang, L; Yuan, H,
)
0.13
" Our study is aimed at exploring the interactive antitumour effects of celastrol combined with tamoxifen and the potential underlying anticancer mechanisms in MCF-7 cells."( The Synergistic Effects of Celastrol in combination with Tamoxifen on Apoptosis and Autophagy in MCF-7 Cells.
Liu, C; Shu, Y; Tang, L; Wang, L; Yao, C, 2021
)
1.09
" Participants received standard care - amphotericin combined with fluconazole for the first 2 weeks - or standard care plus tamoxifen 300 mg/day."( An open label randomized controlled trial of tamoxifen combined with amphotericin B and fluconazole for cryptococcal meningitis.
Beardsley, J; Binh, TQ; Chau, NVV; Day, JN; Geskus, R; Hope, W; Hung, LQ; Kestelyn, E; Krysan, D; Lalloo, DG; Lan, NPH; Mai, NTH; Ngan, NTT; Phu, NH; Tai, LTH; Thanh Hoang Le, N; Thwaites, GE; Trieu, PH; Tung, NLN; Van Anh, D; Van, NTT; Vi Vi, NN; White, NJ, 2021
)
1.09
"nextMONARCH is an open-label, controlled, randomized, Phase 2 study of abemaciclib alone or in combination with tamoxifen in women with endocrine-refractory HR + , HER2- MBC previously treated with chemotherapy."( nextMONARCH Phase 2 randomized clinical trial: overall survival analysis of abemaciclib monotherapy or in combination with tamoxifen in patients with endocrine-refractory HR + , HER2- metastatic breast cancer.
Chen, SC; Chen, Y; Cortes, J; Hamilton, E; Hegg, R; Huober, J; Jerusalem, G; Manikhas, A; Martin, M; Ozyilkan, O; Petrakova, K; Zhang, W, 2022
)
1.14
"To examine whether potential drug-drug interactions (PDDI) with tamoxifen or aromatase inhibitor were associated with adherence to ET in patients with early and advanced breast cancer."( Association of Adherence to Endocrine Therapy Among Patients With Breast Cancer and Potential Drug-Drug Interactions.
André, F; Bardet, A; Bougacha, O; Delaloge, S; Gantzer, L; Lekens, B; Michiels, S; Pistilli, B; Rassy, E, 2022
)
0.96
" Our data are favorable to ERβ1 being a marker of responsiveness and ERβ2 being a marker of resistance of MCF7 cells to antiestrogens alone and in combination with ATRA."( ERβ1 Sensitizes and ERβ2 Desensitizes ERα-Positive Breast Cancer Cells to the Inhibitory Effects of Tamoxifen, Fulvestrant and Their Combination with All-Trans Retinoic Acid.
Alexis, MN; Chatziioannou, A; Ganou, V; Gkotsi, EF; Meligova, AK; Mitsiou, DJ; Papadodima, O; Pilalis, E; Siakouli, D; Stasinopoulou, S; Xenopoulou, DS; Zoumpouli, M, 2023
)
1.13
" The 3-drug combination targets ERα in combination with PI3Kα and cyclin-dependent kinase inhibitor 1 (p21)."( Network-informed discovery of multidrug combinations for ERα+/HER2-/PI3Kα-mutant breast cancer.
Bhattacharya, K; Hany, D; Nowak-Sliwinska, P; Picard, D; Zoetemelk, M, 2023
)
0.91
"To investigate the effects of two protocols (hormone replacement therapy (HRT) alone or in combination with tamoxifen) on the endometrium and pregnancy outcome of patients with thin endometrium in frozen-thawed embryo transfer (FET) cycles."( Hormone replacement therapy alone or in combination with tamoxifen in women with thin endometrium undergoing frozen-thawed embryo transfer: A retrospective study.
Huang, C; Kong, N; Li, Y; Liu, J; Lu, F; Mei, J; Shen, X; Shi, Q; Sun, H; Sun, Y; Yan, G, 2023
)
1.37
"Although tamoxifen when used in combination with hormone replacement therapy can significantly increase endometrial thickness, it may not have a role in improving the pregnancy outcomes of patients with thin endometrium undergoing FET cycles."( Hormone replacement therapy alone or in combination with tamoxifen in women with thin endometrium undergoing frozen-thawed embryo transfer: A retrospective study.
Huang, C; Kong, N; Li, Y; Liu, J; Lu, F; Mei, J; Shen, X; Shi, Q; Sun, H; Sun, Y; Yan, G, 2023
)
1.57

Bioavailability

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.

ExcerptReferenceRelevance
" 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

Dosage Studied

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.

ExcerptRelevanceReference
"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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (8)

RoleDescription
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
estrogen receptor antagonistAn antagonist at the estrogen receptor.
bone density conservation agentAn 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 modulatorA 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 antagonistA compound which inhibits or antagonises the biosynthesis or actions of estrogens.
angiogenesis inhibitorAn agent and endogenous substances that antagonize or inhibit the development of new blood vessels.
EC 2.7.11.13 (protein kinase C) inhibitorAn 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) inhibitorAn 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]

Drug Classes (2)

ClassDescription
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
stilbenoidAny 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]

Pathways (9)

PathwayProteinsCompounds
Metabolism14961108
Biological oxidations150276
Phase I - Functionalization of compounds69175
FMO oxidises nucleophiles313
Tamoxifen Action Pathway1027
Tamoxifen Metabolism Pathway1027
Female steroid hormones in cardiomyocyte energy metabolism73
Integrated breast cancer pathway9818
Tamoxifen metabolism013

Protein Targets (205)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency5.01190.044717.8581100.0000AID485294
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency44.66840.631035.7641100.0000AID504339
Chain A, Ferritin light chainEquus caballus (horse)Potency25.28555.623417.292931.6228AID485281
acetylcholinesteraseHomo sapiens (human)Potency62.95940.002541.796015,848.9004AID1347397; AID1347398
phosphopantetheinyl transferaseBacillus subtilisPotency51.02040.141337.9142100.0000AID1490; AID2701
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency45.90793.189029.884159.4836AID1224846; AID1224894
RAR-related orphan receptor gammaMus musculus (house mouse)Potency29.36180.006038.004119,952.5996AID1159521; AID1159523
SMAD family member 2Homo sapiens (human)Potency59.35360.173734.304761.8120AID1346859; AID1346924; AID1347035
Fumarate hydrataseHomo sapiens (human)Potency35.48130.00308.794948.0869AID1347053
USP1 protein, partialHomo sapiens (human)Potency59.66490.031637.5844354.8130AID504865
PPM1D proteinHomo sapiens (human)Potency30.08830.00529.466132.9993AID1347411
SMAD family member 3Homo sapiens (human)Potency59.35360.173734.304761.8120AID1346859; AID1346924; AID1347035
TDP1 proteinHomo sapiens (human)Potency24.20490.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency20.84080.000714.592883.7951AID1259369; AID1259392
Microtubule-associated protein tauHomo sapiens (human)Potency18.85410.180013.557439.8107AID1460
AR proteinHomo sapiens (human)Potency40.82030.000221.22318,912.5098AID1259243; AID1259247; AID743035; AID743036; AID743053; AID743063
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency35.48130.707912.194339.8107AID720542
DNA polymerase III, partialBacillus subtilisPotency29.93491.062114.152826.6795AID485295
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency44.30170.013326.981070.7614AID1346978
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency54.29180.000657.913322,387.1992AID1259377; AID1259378; AID1259394
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency68.69430.001022.650876.6163AID1224838; AID1224839; AID1224893
progesterone receptorHomo sapiens (human)Potency68.91040.000417.946075.1148AID1346784; AID1346795; AID1347036
regulator of G-protein signaling 4Homo sapiens (human)Potency11.01800.531815.435837.6858AID504845
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency27.98140.000214.376460.0339AID720691; AID720692; AID720719
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency50.19100.003041.611522,387.1992AID1159552; AID1159553; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency38.60970.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency34.65280.001530.607315,848.9004AID1224819; AID1224820; AID1224821; AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency49.59240.375827.485161.6524AID743217; AID743220; AID743239
pregnane X nuclear receptorHomo sapiens (human)Potency12.02150.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency21.15710.000229.305416,493.5996AID1259244; AID1259248; AID1259383; AID743069; AID743075; AID743077; AID743078; AID743079; AID743080; AID743091
polyproteinZika virusPotency35.48130.00308.794948.0869AID1347053
67.9K proteinVaccinia virusPotency8.91250.00018.4406100.0000AID720580
glucocerebrosidaseHomo sapiens (human)Potency24.70280.01268.156944.6684AID2101
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency35.48130.707936.904389.1251AID504333
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency54.94100.001024.504861.6448AID743212; AID743227
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency58.93210.001019.414170.9645AID743094; AID743140; AID743191
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency61.64480.023723.228263.5986AID743222; AID743241
arylsulfatase AHomo sapiens (human)Potency5.35821.069113.955137.9330AID720538
caspase-3Homo sapiens (human)Potency44.30170.013326.981070.7614AID1346978
IDH1Homo sapiens (human)Potency16.36010.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency14.81490.035520.977089.1251AID504332
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency6.02500.001723.839378.1014AID743083
thyroid stimulating hormone receptorHomo sapiens (human)Potency64.08750.001628.015177.1139AID1259385; AID1259395
activating transcription factor 6Homo sapiens (human)Potency44.05380.143427.612159.8106AID1159516; AID1159519
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency27.31850.154917.870243.6557AID1346877; AID1346891
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency26.706319.739145.978464.9432AID1159509; AID1159518
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency20.51880.057821.109761.2679AID1159526; AID1159528
Histone H2A.xCricetulus griseus (Chinese hamster)Potency46.08760.039147.5451146.8240AID1224845; AID1224896
Caspase-7Cricetulus griseus (Chinese hamster)Potency39.48390.006723.496068.5896AID1346980
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency31.62280.00207.533739.8107AID891
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency58.04790.01262.451825.0177AID485313
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency31.62280.316212.443531.6228AID902; AID924
D(1A) dopamine receptorHomo sapiens (human)Potency6.02000.02245.944922.3872AID488981; AID488982
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency46.48520.354828.065989.1251AID504847
chromobox protein homolog 1Homo sapiens (human)Potency37.64600.006026.168889.1251AID488953; AID540317
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency11.22020.794321.275750.1187AID624246
caspase-3Cricetulus griseus (Chinese hamster)Potency39.48390.006723.496068.5896AID1346980
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency12.12590.000323.4451159.6830AID743065; AID743066; AID743067
heat shock protein beta-1Homo sapiens (human)Potency54.94100.042027.378961.6448AID743210; AID743228
ras-related protein Rab-9AHomo sapiens (human)Potency91.99970.00022.621531.4954AID485297
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency18.49820.00378.618923.2809AID2660; AID2666; AID2667; AID2668
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency35.61840.000627.21521,122.0200AID743202; AID743219
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency23.73590.00798.23321,122.0200AID2546; AID2551
gemininHomo sapiens (human)Potency7.14740.004611.374133.4983AID624296; AID624297
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency31.62280.031610.279239.8107AID884; AID885
M-phase phosphoprotein 8Homo sapiens (human)Potency21.19230.177824.735279.4328AID488949
lethal factor (plasmid)Bacillus anthracis str. A2012Potency31.62280.020010.786931.6228AID912
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency6.30960.316212.765731.6228AID881
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency4.43020.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency30.08830.00339.158239.8107AID1347411
Cellular tumor antigen p53Homo sapiens (human)Potency61.91490.002319.595674.0614AID651631; AID720552
Integrin beta-3Homo sapiens (human)Potency31.62280.316211.415731.6228AID924
Integrin alpha-IIbHomo sapiens (human)Potency31.62280.316211.415731.6228AID924
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency4.43020.001551.739315,848.9004AID1259244
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Alpha-synucleinHomo sapiens (human)Potency18.35640.56239.398525.1189AID652106
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency6.30960.00638.235039.8107AID881
D(1A) dopamine receptorSus scrofa (pig)Potency14.68920.00378.108123.2809AID2667
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency61.31720.011917.942071.5630AID651632
Ataxin-2Homo sapiens (human)Potency48.34050.011912.222168.7989AID588378; AID651632
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, CES1 proteinHomo sapiens (human)Ki15.200015.200015.200015.2000AID977610
ubiquitin-conjugating enzyme E2 NHomo sapiens (human)IC50 (µMol)20.00000.873010.721978.4000AID493155
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC50 (µMol)0.46000.00011.00768.7800AID625218
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.24100.00000.887110.0000AID625218
Serine/threonine-protein kinase D3Homo sapiens (human)IC50 (µMol)10.50000.00011.170110.0000AID1323681; AID1323683
Bile salt export pumpHomo sapiens (human)IC50 (µMol)63.34000.11007.190310.0000AID1443980; AID1449628; AID1473738; AID681139; AID681155
Epidermal growth factor receptorHomo sapiens (human)IC50 (µMol)3.55300.00000.536910.0000AID625184
Estrogen receptorHomo sapiens (human)IC50 (µMol)1.17960.00000.723732.7000AID103082; 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 receptorHomo sapiens (human)Ki0.05860.00000.42297.9070AID497602; AID68902; AID68906; AID68910
Receptor tyrosine-protein kinase erbB-2Homo sapiens (human)IC50 (µMol)2.94900.00010.545310.0000AID625186
Protein kinase C gamma typeHomo sapiens (human)IC50 (µMol)10.50000.00011.035410.0000AID1323681; AID1323683
Protein kinase C alpha typeRattus norvegicus (Norway rat)IC50 (µMol)75.00000.00000.21931.0000AID1323682
Protein kinase C beta typeHomo sapiens (human)IC50 (µMol)10.50000.00010.554210.0000AID1323681; AID1323683
Tyrosine-protein kinase LckHomo sapiens (human)IC50 (µMol)8.03300.00021.317310.0000AID625187
Tyrosine-protein kinase FynHomo sapiens (human)IC50 (µMol)1.19500.00021.67898.6800AID625185
Progesterone receptorHomo sapiens (human)IC50 (µMol)50.06440.00000.580710.0000AID1251782; AID1251783
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC50 (µMol)1.47200.00041.877310.0000AID625207
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki1.45900.00322.28879.3160AID625207
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC50 (µMol)7.79300.00001.23267.7930AID625152
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki2.77100.00000.690210.0000AID625152
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC50 (µMol)4.81700.00001.15467.5858AID625154
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.67200.00000.79519.1201AID625154
ATP-dependent translocase ABCB1Homo sapiens (human)IC50 (µMol)19.72500.00022.318510.0000AID679077; AID681126; AID681127; AID681131
ATP-dependent translocase ABCB1Homo sapiens (human)Ki0.10000.02002.35948.5900AID150616
Beta-1 adrenergic receptorHomo sapiens (human)IC50 (µMol)17.28900.00021.46819.0000AID625204
Beta-1 adrenergic receptorHomo sapiens (human)Ki9.98400.00011.33919.9840AID625204
Cytochrome P450 3A4Homo sapiens (human)Ki0.20000.00011.41629.9000AID589145
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC50 (µMol)2.58500.00010.99178.0000AID625155
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki1.85700.00000.72926.9183AID625155
Alpha-2A adrenergic receptorHomo sapiens (human)IC50 (µMol)1.93500.00001.44217.3470AID625201
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.72600.00010.807410.0000AID625201
Protein kinase C delta typeRattus norvegicus (Norway rat)IC50 (µMol)75.00000.00000.25851.0000AID1323682
Protein kinase C epsilon typeRattus norvegicus (Norway rat)IC50 (µMol)75.00000.00000.25851.0000AID1323682
Protein kinase C zeta typeRattus norvegicus (Norway rat)IC50 (µMol)75.00000.00000.25851.0000AID1323682
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)Ki0.08450.00010.03040.1570AID68902; AID68906
Adenosine receptor A3Homo sapiens (human)IC50 (µMol)3.70100.00001.89408.5470AID625196
Adenosine receptor A3Homo sapiens (human)Ki2.09200.00000.930610.0000AID625196
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC50 (µMol)2.82900.00001.403910.0000AID625151
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.68100.00000.59729.1201AID625151
Steroid hormone receptor ERR1Homo sapiens (human)IC50 (µMol)0.20000.00201.16639.6400AID728186
Transcriptional activator protein LuxRAliivibrio fischeriIC50 (µMol)40.00001.36003.25337.0000AID493958
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC50 (µMol)0.96700.00001.612910.0000AID625171
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki0.79220.00042.03378.6606AID625171
Beta-3 adrenergic receptorHomo sapiens (human)IC50 (µMol)7.70300.00233.24158.0600AID625206
Beta-3 adrenergic receptorHomo sapiens (human)Ki5.77800.00302.30986.0450AID625206
D(2) dopamine receptorHomo sapiens (human)IC50 (µMol)13.88500.00000.74728.0000AID625253
D(2) dopamine receptorHomo sapiens (human)Ki4.62800.00000.651810.0000AID625253
Androgen receptorRattus norvegicus (Norway rat)IC50 (µMol)17.34230.00101.979414.1600AID255211; AID625228
Androgen receptorRattus norvegicus (Norway rat)Ki15.10800.00031.21858.9270AID625228
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)3.70100.00021.874210.0000AID625196
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki2.09200.00010.949010.0000AID625196
Protein kinase C alpha typeHomo sapiens (human)IC50 (µMol)10.50000.00010.972010.0000AID1323681; AID1323683
Alpha-2B adrenergic receptorHomo sapiens (human)IC50 (µMol)3.51800.00001.23808.1590AID625202
Alpha-2B adrenergic receptorHomo sapiens (human)Ki1.60600.00020.725710.0000AID625202
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)12.16000.00031.38338.4000AID625190
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki6.94900.00010.739610.0000AID625190
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC50 (µMol)2.97400.00011.01049.9280AID625153
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.63000.00000.54057.7600AID625153
Cytochrome P450 2B6Homo sapiens (human)Ki0.90000.00041.416010.0000AID589238
Substance-K receptorHomo sapiens (human)IC50 (µMol)3.67000.00013.12109.5530AID625227
Substance-K receptorHomo sapiens (human)Ki1.22300.00011.92429.7930AID625227
D(1A) dopamine receptorHomo sapiens (human)IC50 (µMol)8.50200.00031.84739.2250AID625252
D(1A) dopamine receptorHomo sapiens (human)Ki4.25100.00010.836310.0000AID625252
D(4) dopamine receptorHomo sapiens (human)IC50 (µMol)11.16100.00011.14239.3280AID625255
D(4) dopamine receptorHomo sapiens (human)Ki3.91300.00000.436210.0000AID625255
Prostaglandin G/H synthase 1Homo sapiens (human)IC50 (µMol)4.39100.00021.557410.0000AID625243
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC50 (µMol)1.47200.00081.541620.0000AID625207
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki1.45900.00031.465610.0000AID625207
Thromboxane-A synthase Homo sapiens (human)IC50 (µMol)0.91600.00091.230410.0000AID625229
Protein kinase C eta typeHomo sapiens (human)IC50 (µMol)10.50000.00010.797110.0000AID1323681; AID1323683
Histamine H2 receptorHomo sapiens (human)IC50 (µMol)9.39600.02202.298710.0000AID625270
Histamine H2 receptorHomo sapiens (human)Ki9.24000.00062.197310.0000AID625270
Alpha-1D adrenergic receptorHomo sapiens (human)IC50 (µMol)4.98200.00020.75688.8970AID625200
Alpha-1D adrenergic receptorHomo sapiens (human)Ki2.44900.00000.360910.0000AID625200
Substance-P receptorHomo sapiens (human)IC50 (µMol)15.65600.00000.09526.8130AID625226
Substance-P receptorHomo sapiens (human)Ki8.54000.00000.79368.7470AID625226
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC50 (µMol)4.80100.00010.88018.8500AID625192
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki1.37200.00000.385510.0000AID625192
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)0.46000.00011.03029.0000AID625218
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.24100.00010.954910.0000AID625218
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC50 (µMol)12.16000.00051.48357.8000AID625190
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki6.94900.00031.29679.2440AID625190
Adenosine receptor A2aHomo sapiens (human)IC50 (µMol)7.09900.00071.559410.0000AID625195
Adenosine receptor A2aHomo sapiens (human)Ki3.98500.00001.06099.7920AID625195
B2 bradykinin receptorHomo sapiens (human)IC50 (µMol)20.35600.00040.02120.2800AID625213
B2 bradykinin receptorHomo sapiens (human)Ki12.04800.00000.70577.6740AID625213
Adenosine receptor A1Homo sapiens (human)IC50 (µMol)23.76700.00020.68187.7010AID625194
Adenosine receptor A1Homo sapiens (human)Ki13.86400.00020.931610.0000AID625194
Sodium-dependent serotonin transporterHomo sapiens (human)IC50 (µMol)2.33400.00010.86458.7096AID625222
Sodium-dependent serotonin transporterHomo sapiens (human)Ki1.24000.00000.70488.1930AID625222
Melanocortin receptor 4Homo sapiens (human)IC50 (µMol)30.48100.00020.64136.1900AID625148
Melanocortin receptor 4Homo sapiens (human)Ki29.30800.00000.30864.8860AID625148
C-8 sterol isomeraseSaccharomyces cerevisiae S288CKi1.50000.00000.90487.1500AID239296
Melanocortin receptor 5Homo sapiens (human)IC50 (µMol)26.52900.00091.25669.5180AID625149
Melanocortin receptor 5Homo sapiens (human)Ki24.88600.00053.52658.9290AID625149
Mu-type opioid receptorHomo sapiens (human)IC50 (µMol)17.59400.00010.813310.0000AID625163
Mu-type opioid receptorHomo sapiens (human)Ki7.14200.00000.419710.0000AID625163
D(3) dopamine receptorHomo sapiens (human)IC50 (µMol)1.07200.00011.01788.7960AID625254
D(3) dopamine receptorHomo sapiens (human)Ki0.36400.00000.602010.0000AID625254
Delta-type opioid receptorHomo sapiens (human)IC50 (µMol)13.33900.00020.75218.0140AID625161
Delta-type opioid receptorHomo sapiens (human)Ki4.70200.00000.59789.9300AID625161
Kappa-type opioid receptorHomo sapiens (human)IC50 (µMol)15.62900.00001.201110.0000AID625162
Kappa-type opioid receptorHomo sapiens (human)Ki6.25200.00000.362410.0000AID625162
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC50 (µMol)2.08400.00011.18738.9125AID625217
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki1.32600.00030.769310.0000AID625217
Protein kinase C iota typeHomo sapiens (human)IC50 (µMol)10.50000.00012.037810.0000AID1323681; AID1323683
Melanocortin receptor 3Homo sapiens (human)IC50 (µMol)19.85600.00120.01660.0832AID625147
Melanocortin receptor 3Homo sapiens (human)Ki17.32900.00010.24522.8650AID625147
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)3.70100.00001.819410.0000AID625196
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki2.09200.00000.965010.0000AID625196
5-hydroxytryptamine receptor 6Homo sapiens (human)IC50 (µMol)2.67900.00170.83815.4200AID625221
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki1.14250.00020.522910.0000AID625221; AID691260
Estrogen-related receptor gammaHomo sapiens (human)IC50 (µMol)0.06220.00200.22732.0000AID1464223
Protein kinase C gamma typeRattus norvegicus (Norway rat)IC50 (µMol)75.00000.00000.26401.1000AID1323682
Protein kinase C beta typeRattus norvegicus (Norway rat)IC50 (µMol)75.00000.00000.21641.1000AID1323682
Phospholipase D1 Rattus norvegicus (Norway rat)IC50 (µMol)20.00000.01100.34381.0000AID498481
Sodium-dependent dopamine transporter Homo sapiens (human)IC50 (µMol)1.84100.00071.841946.0000AID625256
Sodium-dependent dopamine transporter Homo sapiens (human)Ki1.46200.00021.11158.0280AID625256
Protein kinase C epsilon typeHomo sapiens (human)IC50 (µMol)10.50000.00010.802910.0000AID1323681; AID1323683
Protein kinase C theta typeHomo sapiens (human)IC50 (µMol)10.50000.00010.989710.0000AID1323681; AID1323683
Protein kinase C zeta typeHomo sapiens (human)IC50 (µMol)10.50000.00012.445310.0000AID1323681; AID1323683
Protein kinase C delta typeHomo sapiens (human)IC50 (µMol)10.50000.00010.844810.0000AID1323681; AID1323683
Serine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)IC50 (µMol)30.57300.01480.09890.1830AID625183
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)1.27590.00091.901410.0000AID576612; AID625171
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki0.79220.00211.840710.0000AID625171
Platelet-activating factor acetylhydrolaseHomo sapiens (human)IC50 (µMol)0.90400.00000.38373.9000AID103918
Phospholipase D1Homo sapiens (human)IC50 (µMol)20.00000.00101.06568.5000AID1799396
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)IC50 (µMol)0.01200.01200.01200.0120AID38614
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)Ki0.00500.00040.54906.7000AID239597
Serine/threonine-protein kinase D1Homo sapiens (human)IC50 (µMol)10.50000.00011.231910.0000AID1323681; AID1323683
Protein kinase C eta typeRattus norvegicus (Norway rat)IC50 (µMol)75.00000.00000.25851.0000AID1323682
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC50 (µMol)0.96700.10482.83988.3173AID625171
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki0.79220.08582.95428.6606AID625171
Estrogen receptor betaHomo sapiens (human)IC50 (µMol)1.27900.00010.529432.7000AID103082; AID103918; AID106081; AID1170538; AID1170542; AID1284374; AID1387888; AID1387894; AID1387906; AID1464222; AID1464227; AID1666650; AID1666655; AID242704; AID248083; AID248163; AID344798; AID482348; AID677850; AID68744; AID70030; AID70337
Estrogen receptor betaHomo sapiens (human)Ki0.05100.00000.12512.8760AID669589; AID68902; AID68906; AID68910
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC50 (µMol)0.02100.00030.70285.3660AID625223
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.02190.00000.490110.0000AID239347; AID625223
Emopamil-binding protein-likeHomo sapiens (human)Ki0.00280.00280.00330.0039AID723649
7-dehydrocholesterol reductaseHomo sapiens (human)IC50 (µMol)0.01200.01200.01200.0120AID38614
Protein kinase C theta typeRattus norvegicus (Norway rat)IC50 (µMol)75.00000.00000.25851.0000AID1323682
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Spike glycoproteinBetacoronavirus England 1EC50 (µMol)51.49500.00304.57559.8200AID1804127
Replicase polyprotein 1abBetacoronavirus England 1EC50 (µMol)51.49500.00304.57559.8200AID1804127
streptokinase A precursorStreptococcus pyogenes M1 GASEC50 (µMol)78.08600.06008.9128130.5170AID1902; AID1914
Transmembrane protease serine 2Homo sapiens (human)EC50 (µMol)51.49500.00304.51689.8200AID1804127
Estrogen receptorHomo sapiens (human)EC50 (µMol)1.15680.00000.53054.4000AID1797989; AID1797992; AID747466
Lysosomal acid glucosylceramidaseHomo sapiens (human)EC50 (µMol)2.50002.50002.50002.5000AID1646801
Estrogen receptorRattus norvegicus (Norway rat)EC50 (µMol)150.00000.006022.3670130.5170AID1914
Procathepsin LHomo sapiens (human)EC50 (µMol)51.49500.00304.48749.8200AID1804127
ATP-dependent translocase ABCB1Homo sapiens (human)EC50 (µMol)56.50000.01600.67863.1000AID407205
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusEC50 (µMol)51.49500.00304.61369.8200AID1804127
Replicase polyprotein 1abHuman coronavirus 229EEC50 (µMol)51.49500.00304.61369.8200AID1804127
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusEC50 (µMol)51.49500.00304.45549.8200AID1804127
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC50 (µMol)51.49500.00304.11059.8200AID1804127
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusEC50 (µMol)51.49500.00304.57559.8200AID1804127
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)Kd0.00100.00100.00100.0010AID38728
Estrogen receptor betaRattus norvegicus (Norway rat)EC50 (µMol)150.00000.006022.3670130.5170AID1914
Estrogen receptor betaHomo sapiens (human)EC50 (µMol)0.98080.00000.47954.8900AID1797989; AID1797992; AID747465
Angiotensin-converting enzyme 2 Homo sapiens (human)EC50 (µMol)51.49500.00304.57559.8200AID1804127
7-dehydrocholesterol reductaseHomo sapiens (human)Kd0.00100.00100.00100.0010AID38728
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
interferon gamma precursorHomo sapiens (human)AC5035.24000.128015.173038.6100AID1259418
Estrogen receptorHomo sapiens (human)DC500.09100.00010.03040.0910AID1768139
Estrogen receptorRattus norvegicus (Norway rat)A500.02000.02000.02000.0200AID69358
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km32.00007.00007.00007.0000AID624633
Estrogen receptor betaRattus norvegicus (Norway rat)A500.02000.02000.02000.0200AID69358
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (1281)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
viral translationTransmembrane protease serine 2Homo sapiens (human)
proteolysisTransmembrane protease serine 2Homo sapiens (human)
protein autoprocessingTransmembrane protease serine 2Homo sapiens (human)
positive regulation of viral entry into host cellTransmembrane protease serine 2Homo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase D3Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwaySerine/threonine-protein kinase D3Homo sapiens (human)
sphingolipid biosynthetic processSerine/threonine-protein kinase D3Homo sapiens (human)
intracellular signal transductionSerine/threonine-protein kinase D3Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySerine/threonine-protein kinase D3Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
MAPK cascadeEpidermal growth factor receptorHomo sapiens (human)
ossificationEpidermal growth factor receptorHomo sapiens (human)
embryonic placenta developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein phosphorylationEpidermal growth factor receptorHomo sapiens (human)
hair follicle developmentEpidermal growth factor receptorHomo sapiens (human)
translationEpidermal growth factor receptorHomo sapiens (human)
signal transductionEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
activation of phospholipase C activityEpidermal growth factor receptorHomo sapiens (human)
salivary gland morphogenesisEpidermal growth factor receptorHomo sapiens (human)
midgut developmentEpidermal growth factor receptorHomo sapiens (human)
learning or memoryEpidermal growth factor receptorHomo sapiens (human)
circadian rhythmEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
diterpenoid metabolic processEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
cerebral cortex cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell growthEpidermal growth factor receptorHomo sapiens (human)
lung developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of superoxide anion generationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
response to cobalaminEpidermal growth factor receptorHomo sapiens (human)
response to hydroxyisoflavoneEpidermal growth factor receptorHomo sapiens (human)
cellular response to reactive oxygen speciesEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
ERBB2-EGFR signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of protein catabolic processEpidermal growth factor receptorHomo sapiens (human)
vasodilationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphorylationEpidermal growth factor receptorHomo sapiens (human)
ovulation cycleEpidermal growth factor receptorHomo sapiens (human)
hydrogen peroxide metabolic processEpidermal growth factor receptorHomo sapiens (human)
negative regulation of apoptotic processEpidermal growth factor receptorHomo sapiens (human)
positive regulation of MAP kinase activityEpidermal growth factor receptorHomo sapiens (human)
tongue developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA repairEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA replicationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of bone resorptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of vasoconstrictionEpidermal growth factor receptorHomo sapiens (human)
negative regulation of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEpidermal growth factor receptorHomo sapiens (human)
regulation of JNK cascadeEpidermal growth factor receptorHomo sapiens (human)
symbiont entry into host cellEpidermal growth factor receptorHomo sapiens (human)
protein autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
astrocyte activationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of fibroblast proliferationEpidermal growth factor receptorHomo sapiens (human)
digestive tract morphogenesisEpidermal growth factor receptorHomo sapiens (human)
positive regulation of smooth muscle cell proliferationEpidermal growth factor receptorHomo sapiens (human)
neuron projection morphogenesisEpidermal growth factor receptorHomo sapiens (human)
epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
protein insertion into membraneEpidermal growth factor receptorHomo sapiens (human)
response to calcium ionEpidermal growth factor receptorHomo sapiens (human)
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicEpidermal growth factor receptorHomo sapiens (human)
positive regulation of glial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
morphogenesis of an epithelial foldEpidermal growth factor receptorHomo sapiens (human)
eyelid development in camera-type eyeEpidermal growth factor receptorHomo sapiens (human)
response to UV-AEpidermal growth factor receptorHomo sapiens (human)
positive regulation of mucus secretionEpidermal growth factor receptorHomo sapiens (human)
regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
cellular response to amino acid stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to mechanical stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to cadmium ionEpidermal growth factor receptorHomo sapiens (human)
cellular response to epidermal growth factor stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to estradiol stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to xenobiotic stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to dexamethasone stimulusEpidermal growth factor receptorHomo sapiens (human)
positive regulation of canonical Wnt signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
liver regenerationEpidermal growth factor receptorHomo sapiens (human)
cell-cell adhesionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein kinase C activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of prolactin secretionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of miRNA transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein localization to plasma membraneEpidermal growth factor receptorHomo sapiens (human)
negative regulation of cardiocyte differentiationEpidermal growth factor receptorHomo sapiens (human)
neurogenesisEpidermal growth factor receptorHomo sapiens (human)
multicellular organism developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of kinase activityEpidermal growth factor receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
antral ovarian follicle growthEstrogen receptorHomo sapiens (human)
epithelial cell developmentEstrogen receptorHomo sapiens (human)
chromatin remodelingEstrogen receptorHomo sapiens (human)
regulation of DNA-templated transcriptionEstrogen receptorHomo sapiens (human)
signal transductionEstrogen receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayEstrogen receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationEstrogen receptorHomo sapiens (human)
androgen metabolic processEstrogen receptorHomo sapiens (human)
male gonad developmentEstrogen receptorHomo sapiens (human)
negative regulation of gene expressionEstrogen receptorHomo sapiens (human)
positive regulation of phospholipase C activityEstrogen receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayEstrogen receptorHomo sapiens (human)
intracellular estrogen receptor signaling pathwayEstrogen receptorHomo sapiens (human)
response to estradiolEstrogen receptorHomo sapiens (human)
regulation of toll-like receptor signaling pathwayEstrogen receptorHomo sapiens (human)
negative regulation of smooth muscle cell apoptotic processEstrogen receptorHomo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionEstrogen receptorHomo sapiens (human)
negative regulation of DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
response to estrogenEstrogen receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionEstrogen receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
fibroblast proliferationEstrogen receptorHomo sapiens (human)
positive regulation of fibroblast proliferationEstrogen receptorHomo sapiens (human)
stem cell differentiationEstrogen receptorHomo sapiens (human)
regulation of inflammatory responseEstrogen receptorHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
RNA polymerase II preinitiation complex assemblyEstrogen receptorHomo sapiens (human)
uterus developmentEstrogen receptorHomo sapiens (human)
vagina developmentEstrogen receptorHomo sapiens (human)
prostate epithelial cord elongationEstrogen receptorHomo sapiens (human)
prostate epithelial cord arborization involved in prostate glandular acinus morphogenesisEstrogen receptorHomo sapiens (human)
regulation of branching involved in prostate gland morphogenesisEstrogen receptorHomo sapiens (human)
mammary gland branching involved in pregnancyEstrogen receptorHomo sapiens (human)
mammary gland alveolus developmentEstrogen receptorHomo sapiens (human)
epithelial cell proliferation involved in mammary gland duct elongationEstrogen receptorHomo sapiens (human)
protein localization to chromatinEstrogen receptorHomo sapiens (human)
cellular response to estradiol stimulusEstrogen receptorHomo sapiens (human)
negative regulation of miRNA transcriptionEstrogen receptorHomo sapiens (human)
regulation of epithelial cell apoptotic processEstrogen receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
cellular response to estrogen stimulusEstrogen receptorHomo sapiens (human)
mitochondrion organizationLysosomal acid glucosylceramidaseHomo sapiens (human)
neuron projection developmentLysosomal acid glucosylceramidaseHomo sapiens (human)
glucosylceramide catabolic processLysosomal acid glucosylceramidaseHomo sapiens (human)
autophagyLysosomal acid glucosylceramidaseHomo sapiens (human)
lysosome organizationLysosomal acid glucosylceramidaseHomo sapiens (human)
cholesterol metabolic processLysosomal acid glucosylceramidaseHomo sapiens (human)
determination of adult lifespanLysosomal acid glucosylceramidaseHomo sapiens (human)
cellular response to starvationLysosomal acid glucosylceramidaseHomo sapiens (human)
response to pHLysosomal acid glucosylceramidaseHomo sapiens (human)
microglia differentiationLysosomal acid glucosylceramidaseHomo sapiens (human)
regulation of macroautophagyLysosomal acid glucosylceramidaseHomo sapiens (human)
antigen processing and presentationLysosomal acid glucosylceramidaseHomo sapiens (human)
lipid storageLysosomal acid glucosylceramidaseHomo sapiens (human)
cerebellar Purkinje cell layer formationLysosomal acid glucosylceramidaseHomo sapiens (human)
pyramidal neuron differentiationLysosomal acid glucosylceramidaseHomo sapiens (human)
respiratory electron transport chainLysosomal acid glucosylceramidaseHomo sapiens (human)
termination of signal transductionLysosomal acid glucosylceramidaseHomo sapiens (human)
lipid glycosylationLysosomal acid glucosylceramidaseHomo sapiens (human)
negative regulation of protein-containing complex assemblyLysosomal acid glucosylceramidaseHomo sapiens (human)
regulation of TOR signalingLysosomal acid glucosylceramidaseHomo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processLysosomal acid glucosylceramidaseHomo sapiens (human)
negative regulation of interleukin-6 productionLysosomal acid glucosylceramidaseHomo sapiens (human)
T cell differentiation in thymusLysosomal acid glucosylceramidaseHomo sapiens (human)
response to testosteroneLysosomal acid glucosylceramidaseHomo sapiens (human)
positive regulation of protein dephosphorylationLysosomal acid glucosylceramidaseHomo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processLysosomal acid glucosylceramidaseHomo sapiens (human)
positive regulation of protein-containing complex disassemblyLysosomal acid glucosylceramidaseHomo sapiens (human)
negative regulation of MAP kinase activityLysosomal acid glucosylceramidaseHomo sapiens (human)
negative regulation of neuron apoptotic processLysosomal acid glucosylceramidaseHomo sapiens (human)
response to estrogenLysosomal acid glucosylceramidaseHomo sapiens (human)
sphingosine biosynthetic processLysosomal acid glucosylceramidaseHomo sapiens (human)
ceramide biosynthetic processLysosomal acid glucosylceramidaseHomo sapiens (human)
cell maturationLysosomal acid glucosylceramidaseHomo sapiens (human)
brain morphogenesisLysosomal acid glucosylceramidaseHomo sapiens (human)
homeostasis of number of cellsLysosomal acid glucosylceramidaseHomo sapiens (human)
negative regulation of inflammatory responseLysosomal acid glucosylceramidaseHomo sapiens (human)
neuromuscular processLysosomal acid glucosylceramidaseHomo sapiens (human)
neuron apoptotic processLysosomal acid glucosylceramidaseHomo sapiens (human)
establishment of skin barrierLysosomal acid glucosylceramidaseHomo sapiens (human)
microglial cell proliferationLysosomal acid glucosylceramidaseHomo sapiens (human)
motor behaviorLysosomal acid glucosylceramidaseHomo sapiens (human)
cellular response to tumor necrosis factorLysosomal acid glucosylceramidaseHomo sapiens (human)
hematopoietic stem cell proliferationLysosomal acid glucosylceramidaseHomo sapiens (human)
response to dexamethasoneLysosomal acid glucosylceramidaseHomo sapiens (human)
lymphocyte migrationLysosomal acid glucosylceramidaseHomo sapiens (human)
response to thyroid hormoneLysosomal acid glucosylceramidaseHomo sapiens (human)
beta-glucoside catabolic processLysosomal acid glucosylceramidaseHomo sapiens (human)
positive regulation of protein lipidationLysosomal acid glucosylceramidaseHomo sapiens (human)
positive regulation of neuronal action potentialLysosomal acid glucosylceramidaseHomo sapiens (human)
positive regulation of autophagy of mitochondrion in response to mitochondrial depolarizationLysosomal acid glucosylceramidaseHomo sapiens (human)
autophagosome organizationLysosomal acid glucosylceramidaseHomo sapiens (human)
regulation of lysosomal protein catabolic processLysosomal acid glucosylceramidaseHomo sapiens (human)
cell surface receptor signaling pathwayReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of protein phosphorylationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
protein phosphorylationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
signal transductionReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
enzyme-linked receptor protein signaling pathwayReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
heart developmentReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
neuromuscular junction developmentReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
motor neuron axon guidanceReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
Schwann cell developmentReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
peptidyl-tyrosine phosphorylationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of cell growthReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
regulation of microtubule-based processReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
immature T cell proliferation in thymusReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
negative regulation of immature T cell proliferation in thymusReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of Rho protein signal transductionReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
intracellular signal transductionReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
ERBB2-ERBB3 signaling pathwayReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
ERBB2-EGFR signaling pathwayReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
ERBB2-ERBB4 signaling pathwayReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
wound healingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
myelinationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of MAP kinase activityReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of translationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
regulation of angiogenesisReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of cell adhesionReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
oligodendrocyte differentiationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of epithelial cell proliferationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
regulation of ERK1 and ERK2 cascadeReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
cellular response to growth factor stimulusReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
cellular response to epidermal growth factor stimulusReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
semaphorin-plexin signaling pathwayReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of protein targeting to membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
neurotransmitter receptor localization to postsynaptic specialization membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
neurogenesisReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of MAPK cascadeReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
negative regulation of apoptotic processReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of kinase activityReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
multicellular organism developmentReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of cell population proliferationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
neuron differentiationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
negative regulation of low-density lipoprotein receptor activityIntegrin beta-3Homo sapiens (human)
positive regulation of protein phosphorylationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
cell-substrate junction assemblyIntegrin beta-3Homo sapiens (human)
cell adhesionIntegrin beta-3Homo sapiens (human)
cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
embryo implantationIntegrin beta-3Homo sapiens (human)
blood coagulationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of gene expressionIntegrin beta-3Homo sapiens (human)
negative regulation of macrophage derived foam cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast migrationIntegrin beta-3Homo sapiens (human)
negative regulation of lipid storageIntegrin beta-3Homo sapiens (human)
response to activityIntegrin beta-3Homo sapiens (human)
smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
platelet activationIntegrin beta-3Homo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
cell-substrate adhesionIntegrin beta-3Homo sapiens (human)
activation of protein kinase activityIntegrin beta-3Homo sapiens (human)
negative regulation of lipid transportIntegrin beta-3Homo sapiens (human)
regulation of protein localizationIntegrin beta-3Homo sapiens (human)
regulation of actin cytoskeleton organizationIntegrin beta-3Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of osteoblast proliferationIntegrin beta-3Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin beta-3Homo sapiens (human)
substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
tube developmentIntegrin beta-3Homo sapiens (human)
wound healing, spreading of epidermal cellsIntegrin beta-3Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusIntegrin beta-3Homo sapiens (human)
apolipoprotein A-I-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
wound healingIntegrin beta-3Homo sapiens (human)
apoptotic cell clearanceIntegrin beta-3Homo sapiens (human)
regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
positive regulation of angiogenesisIntegrin beta-3Homo sapiens (human)
positive regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
symbiont entry into host cellIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast proliferationIntegrin beta-3Homo sapiens (human)
mesodermal cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationIntegrin beta-3Homo sapiens (human)
negative regulation of lipoprotein metabolic processIntegrin beta-3Homo sapiens (human)
negative chemotaxisIntegrin beta-3Homo sapiens (human)
regulation of release of sequestered calcium ion into cytosolIntegrin beta-3Homo sapiens (human)
regulation of serotonin uptakeIntegrin beta-3Homo sapiens (human)
angiogenesis involved in wound healingIntegrin beta-3Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeIntegrin beta-3Homo sapiens (human)
platelet aggregationIntegrin beta-3Homo sapiens (human)
cellular response to mechanical stimulusIntegrin beta-3Homo sapiens (human)
cellular response to xenobiotic stimulusIntegrin beta-3Homo sapiens (human)
positive regulation of glomerular mesangial cell proliferationIntegrin beta-3Homo sapiens (human)
blood coagulation, fibrin clot formationIntegrin beta-3Homo sapiens (human)
maintenance of postsynaptic specialization structureIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor diffusion trappingIntegrin beta-3Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
positive regulation of adenylate cyclase-inhibiting opioid receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
regulation of trophoblast cell migrationIntegrin beta-3Homo sapiens (human)
regulation of extracellular matrix organizationIntegrin beta-3Homo sapiens (human)
cellular response to insulin-like growth factor stimulusIntegrin beta-3Homo sapiens (human)
negative regulation of endothelial cell apoptotic processIntegrin beta-3Homo sapiens (human)
positive regulation of T cell migrationIntegrin beta-3Homo sapiens (human)
cell migrationIntegrin beta-3Homo sapiens (human)
protein phosphorylationProtein kinase C gamma typeHomo sapiens (human)
chemical synaptic transmissionProtein kinase C gamma typeHomo sapiens (human)
learning or memoryProtein kinase C gamma typeHomo sapiens (human)
chemosensory behaviorProtein kinase C gamma typeHomo sapiens (human)
response to toxic substanceProtein kinase C gamma typeHomo sapiens (human)
phosphorylationProtein kinase C gamma typeHomo sapiens (human)
negative regulation of protein ubiquitinationProtein kinase C gamma typeHomo sapiens (human)
regulation of response to foodProtein kinase C gamma typeHomo sapiens (human)
positive regulation of mismatch repairProtein kinase C gamma typeHomo sapiens (human)
negative regulation of protein catabolic processProtein kinase C gamma typeHomo sapiens (human)
regulation of circadian rhythmProtein kinase C gamma typeHomo sapiens (human)
response to morphineProtein kinase C gamma typeHomo sapiens (human)
negative regulation of neuron apoptotic processProtein kinase C gamma typeHomo sapiens (human)
response to painProtein kinase C gamma typeHomo sapiens (human)
rhythmic processProtein kinase C gamma typeHomo sapiens (human)
regulation of phagocytosisProtein kinase C gamma typeHomo sapiens (human)
long-term synaptic potentiationProtein kinase C gamma typeHomo sapiens (human)
innervationProtein kinase C gamma typeHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionProtein kinase C gamma typeHomo sapiens (human)
negative regulation of proteasomal protein catabolic processProtein kinase C gamma typeHomo sapiens (human)
response to psychosocial stressProtein kinase C gamma typeHomo sapiens (human)
regulation of synaptic vesicle exocytosisProtein kinase C gamma typeHomo sapiens (human)
intracellular signal transductionProtein kinase C gamma typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C gamma typeHomo sapiens (human)
adaptive immune responseProtein kinase C beta typeHomo sapiens (human)
chromatin remodelingProtein kinase C beta typeHomo sapiens (human)
regulation of transcription by RNA polymerase IIProtein kinase C beta typeHomo sapiens (human)
protein phosphorylationProtein kinase C beta typeHomo sapiens (human)
calcium ion transportProtein kinase C beta typeHomo sapiens (human)
intracellular calcium ion homeostasisProtein kinase C beta typeHomo sapiens (human)
apoptotic processProtein kinase C beta typeHomo sapiens (human)
mitotic nuclear membrane disassemblyProtein kinase C beta typeHomo sapiens (human)
signal transductionProtein kinase C beta typeHomo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayProtein kinase C beta typeHomo sapiens (human)
response to xenobiotic stimulusProtein kinase C beta typeHomo sapiens (human)
response to glucoseProtein kinase C beta typeHomo sapiens (human)
regulation of glucose transmembrane transportProtein kinase C beta typeHomo sapiens (human)
negative regulation of glucose transmembrane transportProtein kinase C beta typeHomo sapiens (human)
regulation of dopamine secretionProtein kinase C beta typeHomo sapiens (human)
dibenzo-p-dioxin metabolic processProtein kinase C beta typeHomo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwayProtein kinase C beta typeHomo sapiens (human)
positive regulation of insulin secretionProtein kinase C beta typeHomo sapiens (human)
response to vitamin DProtein kinase C beta typeHomo sapiens (human)
regulation of growthProtein kinase C beta typeHomo sapiens (human)
B cell activationProtein kinase C beta typeHomo sapiens (human)
positive regulation of odontogenesis of dentin-containing toothProtein kinase C beta typeHomo sapiens (human)
lipoprotein transportProtein kinase C beta typeHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionProtein kinase C beta typeHomo sapiens (human)
post-translational protein modificationProtein kinase C beta typeHomo sapiens (human)
response to ethanolProtein kinase C beta typeHomo sapiens (human)
positive regulation of angiogenesisProtein kinase C beta typeHomo sapiens (human)
positive regulation of DNA-templated transcriptionProtein kinase C beta typeHomo sapiens (human)
negative regulation of insulin receptor signaling pathwayProtein kinase C beta typeHomo sapiens (human)
B cell receptor signaling pathwayProtein kinase C beta typeHomo sapiens (human)
positive regulation of B cell receptor signaling pathwayProtein kinase C beta typeHomo sapiens (human)
cellular response to carbohydrate stimulusProtein kinase C beta typeHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionProtein kinase C beta typeHomo sapiens (human)
regulation of synaptic vesicle exocytosisProtein kinase C beta typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C beta typeHomo sapiens (human)
intracellular signal transductionProtein kinase C beta typeHomo sapiens (human)
protein phosphorylationTyrosine-protein kinase LckHomo sapiens (human)
intracellular zinc ion homeostasisTyrosine-protein kinase LckHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processTyrosine-protein kinase LckHomo sapiens (human)
response to xenobiotic stimulusTyrosine-protein kinase LckHomo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase LckHomo sapiens (human)
hemopoiesisTyrosine-protein kinase LckHomo sapiens (human)
platelet activationTyrosine-protein kinase LckHomo sapiens (human)
T cell differentiationTyrosine-protein kinase LckHomo sapiens (human)
T cell costimulationTyrosine-protein kinase LckHomo sapiens (human)
positive regulation of heterotypic cell-cell adhesionTyrosine-protein kinase LckHomo sapiens (human)
intracellular signal transductionTyrosine-protein kinase LckHomo sapiens (human)
peptidyl-tyrosine autophosphorylationTyrosine-protein kinase LckHomo sapiens (human)
Fc-gamma receptor signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
T cell receptor signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
positive regulation of T cell receptor signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
positive regulation of T cell activationTyrosine-protein kinase LckHomo sapiens (human)
leukocyte migrationTyrosine-protein kinase LckHomo sapiens (human)
release of sequestered calcium ion into cytosolTyrosine-protein kinase LckHomo sapiens (human)
regulation of lymphocyte activationTyrosine-protein kinase LckHomo sapiens (human)
positive regulation of leukocyte cell-cell adhesionTyrosine-protein kinase LckHomo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
innate immune responseTyrosine-protein kinase LckHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
B cell receptor signaling pathwayTyrosine-protein kinase LckHomo sapiens (human)
response to singlet oxygenTyrosine-protein kinase FynHomo sapiens (human)
neuron migrationTyrosine-protein kinase FynHomo sapiens (human)
stimulatory C-type lectin receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
adaptive immune responseTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusTyrosine-protein kinase FynHomo sapiens (human)
heart processTyrosine-protein kinase FynHomo sapiens (human)
protein phosphorylationTyrosine-protein kinase FynHomo sapiens (human)
calcium ion transportTyrosine-protein kinase FynHomo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
axon guidanceTyrosine-protein kinase FynHomo sapiens (human)
learningTyrosine-protein kinase FynHomo sapiens (human)
feeding behaviorTyrosine-protein kinase FynHomo sapiens (human)
regulation of cell shapeTyrosine-protein kinase FynHomo sapiens (human)
gene expressionTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of gene expressionTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of hydrogen peroxide biosynthetic processTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of neuron projection developmentTyrosine-protein kinase FynHomo sapiens (human)
protein ubiquitinationTyrosine-protein kinase FynHomo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase FynHomo sapiens (human)
protein catabolic processTyrosine-protein kinase FynHomo sapiens (human)
forebrain developmentTyrosine-protein kinase FynHomo sapiens (human)
T cell costimulationTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of protein ubiquitinationTyrosine-protein kinase FynHomo sapiens (human)
intracellular signal transductionTyrosine-protein kinase FynHomo sapiens (human)
cellular response to platelet-derived growth factor stimulusTyrosine-protein kinase FynHomo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of protein catabolic processTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinTyrosine-protein kinase FynHomo sapiens (human)
response to ethanolTyrosine-protein kinase FynHomo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
ephrin receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
dendrite morphogenesisTyrosine-protein kinase FynHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationTyrosine-protein kinase FynHomo sapiens (human)
activated T cell proliferationTyrosine-protein kinase FynHomo sapiens (human)
modulation of chemical synaptic transmissionTyrosine-protein kinase FynHomo sapiens (human)
T cell receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
leukocyte migrationTyrosine-protein kinase FynHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painTyrosine-protein kinase FynHomo sapiens (human)
cellular response to hydrogen peroxideTyrosine-protein kinase FynHomo sapiens (human)
cellular response to transforming growth factor beta stimulusTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of protein targeting to membraneTyrosine-protein kinase FynHomo sapiens (human)
dendritic spine maintenanceTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of protein localization to nucleusTyrosine-protein kinase FynHomo sapiens (human)
regulation of glutamate receptor signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of oxidative stress-induced intrinsic apoptotic signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
negative regulation of dendritic spine maintenanceTyrosine-protein kinase FynHomo sapiens (human)
response to amyloid-betaTyrosine-protein kinase FynHomo sapiens (human)
cellular response to amyloid-betaTyrosine-protein kinase FynHomo sapiens (human)
cellular response to L-glutamateTyrosine-protein kinase FynHomo sapiens (human)
cellular response to glycineTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of protein localization to membraneTyrosine-protein kinase FynHomo sapiens (human)
regulation of calcium ion import across plasma membraneTyrosine-protein kinase FynHomo sapiens (human)
positive regulation of cysteine-type endopeptidase activityTyrosine-protein kinase FynHomo sapiens (human)
innate immune responseTyrosine-protein kinase FynHomo sapiens (human)
cell differentiationTyrosine-protein kinase FynHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayTyrosine-protein kinase FynHomo sapiens (human)
ovulation from ovarian follicleProgesterone receptorHomo sapiens (human)
glandular epithelial cell maturationProgesterone receptorHomo sapiens (human)
regulation of DNA-templated transcriptionProgesterone receptorHomo sapiens (human)
signal transductionProgesterone receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayProgesterone receptorHomo sapiens (human)
cell-cell signalingProgesterone receptorHomo sapiens (human)
positive regulation of gene expressionProgesterone receptorHomo sapiens (human)
negative regulation of gene expressionProgesterone receptorHomo sapiens (human)
paracrine signalingProgesterone receptorHomo sapiens (human)
negative regulation of phosphorylationProgesterone receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIProgesterone receptorHomo sapiens (human)
lung alveolus developmentProgesterone receptorHomo sapiens (human)
regulation of epithelial cell proliferationProgesterone receptorHomo sapiens (human)
progesterone receptor signaling pathwayProgesterone receptorHomo sapiens (human)
maintenance of protein location in nucleusProgesterone receptorHomo sapiens (human)
tertiary branching involved in mammary gland duct morphogenesisProgesterone receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIProgesterone receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayProgesterone receptorHomo sapiens (human)
adaptive immune responseProcathepsin LHomo sapiens (human)
proteolysisProcathepsin LHomo sapiens (human)
protein autoprocessingProcathepsin LHomo sapiens (human)
fusion of virus membrane with host plasma membraneProcathepsin LHomo sapiens (human)
receptor-mediated endocytosis of virus by host cellProcathepsin LHomo sapiens (human)
antigen processing and presentationProcathepsin LHomo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class IIProcathepsin LHomo sapiens (human)
collagen catabolic processProcathepsin LHomo sapiens (human)
zymogen activationProcathepsin LHomo sapiens (human)
enkephalin processingProcathepsin LHomo sapiens (human)
fusion of virus membrane with host endosome membraneProcathepsin LHomo sapiens (human)
CD4-positive, alpha-beta T cell lineage commitmentProcathepsin LHomo sapiens (human)
symbiont entry into host cellProcathepsin LHomo sapiens (human)
antigen processing and presentation of peptide antigenProcathepsin LHomo sapiens (human)
proteolysis involved in protein catabolic processProcathepsin LHomo sapiens (human)
elastin catabolic processProcathepsin LHomo sapiens (human)
macrophage apoptotic processProcathepsin LHomo sapiens (human)
cellular response to thyroid hormone stimulusProcathepsin LHomo sapiens (human)
positive regulation of apoptotic signaling pathwayProcathepsin LHomo sapiens (human)
positive regulation of peptidase activityProcathepsin LHomo sapiens (human)
immune responseProcathepsin LHomo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of heart contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
response to virusMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M2Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M4Homo sapiens (human)
cell surface receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M4Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M4Homo sapiens (human)
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of leukocyte migrationIntegrin alpha-IIbHomo sapiens (human)
cell-matrix adhesionIntegrin alpha-IIbHomo sapiens (human)
integrin-mediated signaling pathwayIntegrin alpha-IIbHomo sapiens (human)
angiogenesisIntegrin alpha-IIbHomo sapiens (human)
cell-cell adhesionIntegrin alpha-IIbHomo sapiens (human)
cell adhesion mediated by integrinIntegrin alpha-IIbHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
response to coldBeta-1 adrenergic receptorHomo sapiens (human)
heat generationBeta-1 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-1 adrenergic receptorHomo sapiens (human)
fear responseBeta-1 adrenergic receptorHomo sapiens (human)
regulation of circadian sleep/wake cycle, sleepBeta-1 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-1 adrenergic receptorHomo sapiens (human)
regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-1 adrenergic receptorHomo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
gastric acid secretionMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
dopamine transportMuscarinic acetylcholine receptor M5Homo sapiens (human)
transmission of nerve impulseMuscarinic acetylcholine receptor M5Homo sapiens (human)
regulation of phosphatidylinositol dephosphorylationMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M5Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M5Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of endothelial cell proliferationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukocyte chemotaxis involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukocyte migration involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene production involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene metabolic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
humoral immune responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of angiogenesisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
positive regulation of bone mineralizationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
dendritic cell migrationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
glucose homeostasisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
long-chain fatty acid biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of fat cell differentiationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of insulin secretionPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of vascular wound healingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of wound healingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of inflammatory response to woundingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of cytokine production involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of cellular response to oxidative stressPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene A4 biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of reactive oxygen species biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of response to endoplasmic reticulum stressPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of sprouting angiogenesisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
positive regulation of leukocyte adhesion to arterial endothelial cellPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipoxin biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
symbiont-mediated perturbation of host ubiquitin-like protein modificationReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
symbiont-mediated perturbation of host ubiquitin-like protein modificationReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
inflammatory responseAdenosine receptor A3Homo sapiens (human)
signal transductionAdenosine receptor A3Homo sapiens (human)
activation of adenylate cyclase activityAdenosine receptor A3Homo sapiens (human)
regulation of heart contractionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A3Homo sapiens (human)
response to woundingAdenosine receptor A3Homo sapiens (human)
regulation of norepinephrine secretionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell migrationAdenosine receptor A3Homo sapiens (human)
negative regulation of NF-kappaB transcription factor activityAdenosine receptor A3Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A3Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A3Homo sapiens (human)
positive regulation of monoatomic ion transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
neuromuscular synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M1Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M1Homo sapiens (human)
cognitionMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of postsynaptic membrane potentialMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of glial cell proliferationMuscarinic acetylcholine receptor M1Homo sapiens (human)
positive regulation of intracellular protein transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of DNA-templated transcriptionSteroid hormone receptor ERR1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IISteroid hormone receptor ERR1Homo sapiens (human)
intracellular steroid hormone receptor signaling pathwaySteroid hormone receptor ERR1Homo sapiens (human)
regulation of transcription by RNA polymerase IISteroid hormone receptor ERR1Homo sapiens (human)
receptor-mediated endocytosisBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
carbohydrate metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
generation of precursor metabolites and energyBeta-3 adrenergic receptorHomo sapiens (human)
energy reserve metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
response to coldBeta-3 adrenergic receptorHomo sapiens (human)
heat generationBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-3 adrenergic receptorHomo sapiens (human)
eating behaviorBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-3 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-3 adrenergic receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
angiogenesisProtein kinase C alpha typeHomo sapiens (human)
positive regulation of endothelial cell proliferationProtein kinase C alpha typeHomo sapiens (human)
desmosome assemblyProtein kinase C alpha typeHomo sapiens (human)
chromatin remodelingProtein kinase C alpha typeHomo sapiens (human)
protein phosphorylationProtein kinase C alpha typeHomo sapiens (human)
mitotic nuclear membrane disassemblyProtein kinase C alpha typeHomo sapiens (human)
cell adhesionProtein kinase C alpha typeHomo sapiens (human)
positive regulation of endothelial cell migrationProtein kinase C alpha typeHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyProtein kinase C alpha typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C alpha typeHomo sapiens (human)
peptidyl-threonine phosphorylationProtein kinase C alpha typeHomo sapiens (human)
positive regulation of cell migrationProtein kinase C alpha typeHomo sapiens (human)
positive regulation of lipopolysaccharide-mediated signaling pathwayProtein kinase C alpha typeHomo sapiens (human)
negative regulation of glial cell apoptotic processProtein kinase C alpha typeHomo sapiens (human)
regulation of mRNA stabilityProtein kinase C alpha typeHomo sapiens (human)
positive regulation of blood vessel endothelial cell migrationProtein kinase C alpha typeHomo sapiens (human)
post-translational protein modificationProtein kinase C alpha typeHomo sapiens (human)
positive regulation of macrophage differentiationProtein kinase C alpha typeHomo sapiens (human)
positive regulation of angiogenesisProtein kinase C alpha typeHomo sapiens (human)
positive regulation of bone resorptionProtein kinase C alpha typeHomo sapiens (human)
positive regulation of cell adhesionProtein kinase C alpha typeHomo sapiens (human)
positive regulation of mitotic cell cycleProtein kinase C alpha typeHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeProtein kinase C alpha typeHomo sapiens (human)
response to interleukin-1Protein kinase C alpha typeHomo sapiens (human)
regulation of platelet aggregationProtein kinase C alpha typeHomo sapiens (human)
apoptotic signaling pathwayProtein kinase C alpha typeHomo sapiens (human)
positive regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwayProtein kinase C alpha typeHomo sapiens (human)
positive regulation of angiotensin-activated signaling pathwayProtein kinase C alpha typeHomo sapiens (human)
positive regulation of dense core granule biogenesisProtein kinase C alpha typeHomo sapiens (human)
intracellular signal transductionProtein kinase C alpha typeHomo sapiens (human)
positive regulation of insulin secretionProtein kinase C alpha typeHomo sapiens (human)
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
calcium-mediated signalingMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of monoatomic ion transmembrane transporter activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
synaptic transmission, cholinergicMuscarinic acetylcholine receptor M3Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of insulin secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein modification processMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ion channel modulating, G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ligand-gated ion channel signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M3Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M3Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2B6Homo sapiens (human)
steroid metabolic processCytochrome P450 2B6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2B6Homo sapiens (human)
cellular ketone metabolic processCytochrome P450 2B6Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2B6Homo sapiens (human)
muscle contractionSubstance-K receptorHomo sapiens (human)
tachykinin receptor signaling pathwaySubstance-K receptorHomo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmissionSubstance-K receptorHomo sapiens (human)
intestine smooth muscle contractionSubstance-K receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionSubstance-K receptorHomo sapiens (human)
operant conditioningSubstance-K receptorHomo sapiens (human)
positive regulation of vascular permeabilitySubstance-K receptorHomo sapiens (human)
positive regulation of monoatomic ion transportSubstance-K receptorHomo sapiens (human)
positive regulation of smooth muscle contractionSubstance-K receptorHomo sapiens (human)
response to electrical stimulusSubstance-K receptorHomo sapiens (human)
prolactin secretionSubstance-K receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionSubstance-K receptorHomo sapiens (human)
positive regulation of flagellated sperm motilitySubstance-K receptorHomo sapiens (human)
temperature homeostasisD(1A) dopamine receptorHomo sapiens (human)
conditioned taste aversionD(1A) dopamine receptorHomo sapiens (human)
behavioral fear responseD(1A) dopamine receptorHomo sapiens (human)
regulation of protein phosphorylationD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(1A) dopamine receptorHomo sapiens (human)
response to amphetamineD(1A) dopamine receptorHomo sapiens (human)
protein import into nucleusD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
activation of adenylate cyclase activityD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
synapse assemblyD(1A) dopamine receptorHomo sapiens (human)
memoryD(1A) dopamine receptorHomo sapiens (human)
mating behaviorD(1A) dopamine receptorHomo sapiens (human)
grooming behaviorD(1A) dopamine receptorHomo sapiens (human)
adult walking behaviorD(1A) dopamine receptorHomo sapiens (human)
visual learningD(1A) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(1A) dopamine receptorHomo sapiens (human)
astrocyte developmentD(1A) dopamine receptorHomo sapiens (human)
dopamine transportD(1A) dopamine receptorHomo sapiens (human)
transmission of nerve impulseD(1A) dopamine receptorHomo sapiens (human)
neuronal action potentialD(1A) dopamine receptorHomo sapiens (human)
dentate gyrus developmentD(1A) dopamine receptorHomo sapiens (human)
striatum developmentD(1A) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of cell migrationD(1A) dopamine receptorHomo sapiens (human)
peristalsisD(1A) dopamine receptorHomo sapiens (human)
operant conditioningD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
vasodilationD(1A) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
maternal behaviorD(1A) dopamine receptorHomo sapiens (human)
positive regulation of potassium ion transportD(1A) dopamine receptorHomo sapiens (human)
glucose importD(1A) dopamine receptorHomo sapiens (human)
habituationD(1A) dopamine receptorHomo sapiens (human)
sensitizationD(1A) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(1A) dopamine receptorHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(1A) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic potentiationD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic depressionD(1A) dopamine receptorHomo sapiens (human)
cellular response to catecholamine stimulusD(1A) dopamine receptorHomo sapiens (human)
modification of postsynaptic structureD(1A) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of neuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral fear responseD(4) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(4) dopamine receptorHomo sapiens (human)
response to amphetamineD(4) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
adult locomotory behaviorD(4) dopamine receptorHomo sapiens (human)
positive regulation of sodium:proton antiporter activityD(4) dopamine receptorHomo sapiens (human)
positive regulation of kinase activityD(4) dopamine receptorHomo sapiens (human)
response to histamineD(4) dopamine receptorHomo sapiens (human)
social behaviorD(4) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
fear responseD(4) dopamine receptorHomo sapiens (human)
regulation of circadian rhythmD(4) dopamine receptorHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(4) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(4) dopamine receptorHomo sapiens (human)
rhythmic processD(4) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(4) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(4) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
inhibitory postsynaptic potentialD(4) dopamine receptorHomo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationD(4) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(4) dopamine receptorHomo sapiens (human)
chemical synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
bilirubin conjugationUDP-glucuronosyltransferase 1A4Homo sapiens (human)
heme catabolic processUDP-glucuronosyltransferase 1A4Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A4Homo sapiens (human)
vitamin D3 metabolic processUDP-glucuronosyltransferase 1A4Homo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 1Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 1Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 1Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 1Homo sapiens (human)
regulation of cell population proliferationProstaglandin G/H synthase 1Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 1Homo sapiens (human)
monoamine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent noradrenaline transporter Homo sapiens (human)
chemical synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent noradrenaline transporter Homo sapiens (human)
response to painSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent noradrenaline transporter Homo sapiens (human)
neuron cellular homeostasisSodium-dependent noradrenaline transporter Homo sapiens (human)
amino acid transportSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent noradrenaline transporter Homo sapiens (human)
prostaglandin biosynthetic processThromboxane-A synthase Homo sapiens (human)
icosanoid metabolic processThromboxane-A synthase Homo sapiens (human)
cyclooxygenase pathwayThromboxane-A synthase Homo sapiens (human)
intracellular chloride ion homeostasisThromboxane-A synthase Homo sapiens (human)
response to ethanolThromboxane-A synthase Homo sapiens (human)
positive regulation of vasoconstrictionThromboxane-A synthase Homo sapiens (human)
response to fatty acidThromboxane-A synthase Homo sapiens (human)
protein phosphorylationProtein kinase C eta typeHomo sapiens (human)
signal transductionProtein kinase C eta typeHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationProtein kinase C eta typeHomo sapiens (human)
cell differentiationProtein kinase C eta typeHomo sapiens (human)
negative regulation of glial cell apoptotic processProtein kinase C eta typeHomo sapiens (human)
positive regulation of keratinocyte differentiationProtein kinase C eta typeHomo sapiens (human)
positive regulation of B cell receptor signaling pathwayProtein kinase C eta typeHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityProtein kinase C eta typeHomo sapiens (human)
positive regulation of glial cell proliferationProtein kinase C eta typeHomo sapiens (human)
protein kinase C signalingProtein kinase C eta typeHomo sapiens (human)
positive regulation of protein localization to plasma membraneProtein kinase C eta typeHomo sapiens (human)
regulation of bicellular tight junction assemblyProtein kinase C eta typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C eta typeHomo sapiens (human)
intracellular signal transductionProtein kinase C eta typeHomo sapiens (human)
gastric acid secretionHistamine H2 receptorHomo sapiens (human)
immune responseHistamine H2 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H2 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
aggressive behaviorSubstance-P receptorHomo sapiens (human)
positive regulation of leukocyte migrationSubstance-P receptorHomo sapiens (human)
angiotensin-mediated drinking behaviorSubstance-P receptorHomo sapiens (human)
inflammatory responseSubstance-P receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySubstance-P receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationSubstance-P receptorHomo sapiens (human)
tachykinin receptor signaling pathwaySubstance-P receptorHomo sapiens (human)
long-term memorySubstance-P receptorHomo sapiens (human)
associative learningSubstance-P receptorHomo sapiens (human)
detection of abiotic stimulusSubstance-P receptorHomo sapiens (human)
response to ozoneSubstance-P receptorHomo sapiens (human)
positive regulation of epithelial cell migrationSubstance-P receptorHomo sapiens (human)
response to auditory stimulusSubstance-P receptorHomo sapiens (human)
regulation of smooth muscle cell migrationSubstance-P receptorHomo sapiens (human)
positive regulation of synaptic transmission, cholinergicSubstance-P receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicSubstance-P receptorHomo sapiens (human)
response to estradiolSubstance-P receptorHomo sapiens (human)
response to progesteroneSubstance-P receptorHomo sapiens (human)
response to nicotineSubstance-P receptorHomo sapiens (human)
operant conditioningSubstance-P receptorHomo sapiens (human)
sperm ejaculationSubstance-P receptorHomo sapiens (human)
eating behaviorSubstance-P receptorHomo sapiens (human)
positive regulation of vascular permeabilitySubstance-P receptorHomo sapiens (human)
response to ethanolSubstance-P receptorHomo sapiens (human)
positive regulation of action potentialSubstance-P receptorHomo sapiens (human)
positive regulation of blood pressureSubstance-P receptorHomo sapiens (human)
positive regulation of ossificationSubstance-P receptorHomo sapiens (human)
positive regulation of vasoconstrictionSubstance-P receptorHomo sapiens (human)
positive regulation of hormone secretionSubstance-P receptorHomo sapiens (human)
behavioral response to painSubstance-P receptorHomo sapiens (human)
regulation of smooth muscle cell proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of lymphocyte proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of epithelial cell proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of stress fiber assemblySubstance-P receptorHomo sapiens (human)
response to electrical stimulusSubstance-P receptorHomo sapiens (human)
smooth muscle contraction involved in micturitionSubstance-P receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionSubstance-P receptorHomo sapiens (human)
positive regulation of flagellated sperm motilitySubstance-P receptorHomo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
synaptic transmission, dopaminergicAdenosine receptor A2aHomo sapiens (human)
response to amphetamineAdenosine receptor A2aHomo sapiens (human)
regulation of DNA-templated transcriptionAdenosine receptor A2aHomo sapiens (human)
phagocytosisAdenosine receptor A2aHomo sapiens (human)
apoptotic processAdenosine receptor A2aHomo sapiens (human)
inflammatory responseAdenosine receptor A2aHomo sapiens (human)
cellular defense responseAdenosine receptor A2aHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
cell-cell signalingAdenosine receptor A2aHomo sapiens (human)
synaptic transmission, cholinergicAdenosine receptor A2aHomo sapiens (human)
central nervous system developmentAdenosine receptor A2aHomo sapiens (human)
blood coagulationAdenosine receptor A2aHomo sapiens (human)
sensory perceptionAdenosine receptor A2aHomo sapiens (human)
locomotory behaviorAdenosine receptor A2aHomo sapiens (human)
blood circulationAdenosine receptor A2aHomo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A2aHomo sapiens (human)
response to xenobiotic stimulusAdenosine receptor A2aHomo sapiens (human)
response to inorganic substanceAdenosine receptor A2aHomo sapiens (human)
positive regulation of glutamate secretionAdenosine receptor A2aHomo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmissionAdenosine receptor A2aHomo sapiens (human)
regulation of norepinephrine secretionAdenosine receptor A2aHomo sapiens (human)
response to purine-containing compoundAdenosine receptor A2aHomo sapiens (human)
response to caffeineAdenosine receptor A2aHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAdenosine receptor A2aHomo sapiens (human)
synaptic transmission, glutamatergicAdenosine receptor A2aHomo sapiens (human)
positive regulation of urine volumeAdenosine receptor A2aHomo sapiens (human)
vasodilationAdenosine receptor A2aHomo sapiens (human)
eating behaviorAdenosine receptor A2aHomo sapiens (human)
negative regulation of vascular permeabilityAdenosine receptor A2aHomo sapiens (human)
negative regulation of neuron apoptotic processAdenosine receptor A2aHomo sapiens (human)
positive regulation of circadian sleep/wake cycle, sleepAdenosine receptor A2aHomo sapiens (human)
negative regulation of alpha-beta T cell activationAdenosine receptor A2aHomo sapiens (human)
astrocyte activationAdenosine receptor A2aHomo sapiens (human)
neuron projection morphogenesisAdenosine receptor A2aHomo sapiens (human)
positive regulation of protein secretionAdenosine receptor A2aHomo sapiens (human)
negative regulation of inflammatory responseAdenosine receptor A2aHomo sapiens (human)
regulation of mitochondrial membrane potentialAdenosine receptor A2aHomo sapiens (human)
membrane depolarizationAdenosine receptor A2aHomo sapiens (human)
regulation of calcium ion transportAdenosine receptor A2aHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicAdenosine receptor A2aHomo sapiens (human)
excitatory postsynaptic potentialAdenosine receptor A2aHomo sapiens (human)
inhibitory postsynaptic potentialAdenosine receptor A2aHomo sapiens (human)
prepulse inhibitionAdenosine receptor A2aHomo sapiens (human)
apoptotic signaling pathwayAdenosine receptor A2aHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A2aHomo sapiens (human)
positive regulation of long-term synaptic potentiationAdenosine receptor A2aHomo sapiens (human)
positive regulation of apoptotic signaling pathwayAdenosine receptor A2aHomo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
smooth muscle contractionB2 bradykinin receptorHomo sapiens (human)
inflammatory responseB2 bradykinin receptorHomo sapiens (human)
cell surface receptor signaling pathwayB2 bradykinin receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayB2 bradykinin receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationB2 bradykinin receptorHomo sapiens (human)
blood circulationB2 bradykinin receptorHomo sapiens (human)
response to salt stressB2 bradykinin receptorHomo sapiens (human)
regulation of vasoconstrictionB2 bradykinin receptorHomo sapiens (human)
negative regulation of peptidyl-serine phosphorylationB2 bradykinin receptorHomo sapiens (human)
vasoconstrictionB2 bradykinin receptorHomo sapiens (human)
vasodilationB2 bradykinin receptorHomo sapiens (human)
regulation of vascular permeabilityB2 bradykinin receptorHomo sapiens (human)
arachidonic acid secretionB2 bradykinin receptorHomo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stress by p53 class mediatorB2 bradykinin receptorHomo sapiens (human)
intrinsic apoptotic signaling pathway in response to osmotic stress by p53 class mediatorB2 bradykinin receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayB2 bradykinin receptorHomo sapiens (human)
temperature homeostasisAdenosine receptor A1Homo sapiens (human)
response to hypoxiaAdenosine receptor A1Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
regulation of respiratory gaseous exchange by nervous system processAdenosine receptor A1Homo sapiens (human)
negative regulation of acute inflammatory responseAdenosine receptor A1Homo sapiens (human)
negative regulation of leukocyte migrationAdenosine receptor A1Homo sapiens (human)
positive regulation of peptide secretionAdenosine receptor A1Homo sapiens (human)
positive regulation of systemic arterial blood pressureAdenosine receptor A1Homo sapiens (human)
negative regulation of systemic arterial blood pressureAdenosine receptor A1Homo sapiens (human)
regulation of glomerular filtrationAdenosine receptor A1Homo sapiens (human)
protein targeting to membraneAdenosine receptor A1Homo sapiens (human)
phagocytosisAdenosine receptor A1Homo sapiens (human)
inflammatory responseAdenosine receptor A1Homo sapiens (human)
signal transductionAdenosine receptor A1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
cell-cell signalingAdenosine receptor A1Homo sapiens (human)
nervous system developmentAdenosine receptor A1Homo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A1Homo sapiens (human)
response to inorganic substanceAdenosine receptor A1Homo sapiens (human)
negative regulation of glutamate secretionAdenosine receptor A1Homo sapiens (human)
response to purine-containing compoundAdenosine receptor A1Homo sapiens (human)
lipid catabolic processAdenosine receptor A1Homo sapiens (human)
negative regulation of synaptic transmission, GABAergicAdenosine receptor A1Homo sapiens (human)
positive regulation of nucleoside transportAdenosine receptor A1Homo sapiens (human)
negative regulation of neurotrophin productionAdenosine receptor A1Homo sapiens (human)
positive regulation of protein dephosphorylationAdenosine receptor A1Homo sapiens (human)
vasodilationAdenosine receptor A1Homo sapiens (human)
negative regulation of circadian sleep/wake cycle, non-REM sleepAdenosine receptor A1Homo sapiens (human)
negative regulation of apoptotic processAdenosine receptor A1Homo sapiens (human)
positive regulation of potassium ion transportAdenosine receptor A1Homo sapiens (human)
positive regulation of MAPK cascadeAdenosine receptor A1Homo sapiens (human)
negative regulation of hormone secretionAdenosine receptor A1Homo sapiens (human)
cognitionAdenosine receptor A1Homo sapiens (human)
leukocyte migrationAdenosine receptor A1Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of painAdenosine receptor A1Homo sapiens (human)
negative regulation of lipid catabolic processAdenosine receptor A1Homo sapiens (human)
positive regulation of lipid catabolic processAdenosine receptor A1Homo sapiens (human)
regulation of sensory perception of painAdenosine receptor A1Homo sapiens (human)
negative regulation of synaptic transmission, glutamatergicAdenosine receptor A1Homo sapiens (human)
fatty acid homeostasisAdenosine receptor A1Homo sapiens (human)
excitatory postsynaptic potentialAdenosine receptor A1Homo sapiens (human)
long-term synaptic depressionAdenosine receptor A1Homo sapiens (human)
mucus secretionAdenosine receptor A1Homo sapiens (human)
negative regulation of mucus secretionAdenosine receptor A1Homo sapiens (human)
triglyceride homeostasisAdenosine receptor A1Homo sapiens (human)
regulation of cardiac muscle cell contractionAdenosine receptor A1Homo sapiens (human)
apoptotic signaling pathwayAdenosine receptor A1Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentrationAdenosine receptor A1Homo sapiens (human)
negative regulation of long-term synaptic potentiationAdenosine receptor A1Homo sapiens (human)
negative regulation of long-term synaptic depressionAdenosine receptor A1Homo sapiens (human)
G protein-coupled receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
monoamine transportSodium-dependent serotonin transporterHomo sapiens (human)
response to hypoxiaSodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transportSodium-dependent serotonin transporterHomo sapiens (human)
response to nutrientSodium-dependent serotonin transporterHomo sapiens (human)
memorySodium-dependent serotonin transporterHomo sapiens (human)
circadian rhythmSodium-dependent serotonin transporterHomo sapiens (human)
response to xenobiotic stimulusSodium-dependent serotonin transporterHomo sapiens (human)
response to toxic substanceSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of gene expressionSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of serotonin secretionSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of cerebellar granule cell precursor proliferationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of synaptic transmission, dopaminergicSodium-dependent serotonin transporterHomo sapiens (human)
response to estradiolSodium-dependent serotonin transporterHomo sapiens (human)
social behaviorSodium-dependent serotonin transporterHomo sapiens (human)
vasoconstrictionSodium-dependent serotonin transporterHomo sapiens (human)
sperm ejaculationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of neuron differentiationSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of cell cycleSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of organ growthSodium-dependent serotonin transporterHomo sapiens (human)
behavioral response to cocaineSodium-dependent serotonin transporterHomo sapiens (human)
enteric nervous system developmentSodium-dependent serotonin transporterHomo sapiens (human)
brain morphogenesisSodium-dependent serotonin transporterHomo sapiens (human)
serotonin uptakeSodium-dependent serotonin transporterHomo sapiens (human)
membrane depolarizationSodium-dependent serotonin transporterHomo sapiens (human)
platelet aggregationSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to retinoic acidSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to cGMPSodium-dependent serotonin transporterHomo sapiens (human)
regulation of thalamus sizeSodium-dependent serotonin transporterHomo sapiens (human)
conditioned place preferenceSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion transmembrane transportSodium-dependent serotonin transporterHomo sapiens (human)
amino acid transportSodium-dependent serotonin transporterHomo sapiens (human)
diet induced thermogenesisMelanocortin receptor 4Homo sapiens (human)
energy reserve metabolic processMelanocortin receptor 4Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMelanocortin receptor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 4Homo sapiens (human)
feeding behaviorMelanocortin receptor 4Homo sapiens (human)
insulin secretionMelanocortin receptor 4Homo sapiens (human)
response to insulinMelanocortin receptor 4Homo sapiens (human)
positive regulation of bone resorptionMelanocortin receptor 4Homo sapiens (human)
regulation of eating behaviorMelanocortin receptor 4Homo sapiens (human)
response to melanocyte-stimulating hormoneMelanocortin receptor 4Homo sapiens (human)
negative regulation of feeding behaviorMelanocortin receptor 4Homo sapiens (human)
regulation of grooming behaviorMelanocortin receptor 4Homo sapiens (human)
regulation of metabolic processMelanocortin receptor 4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelanocortin receptor 5Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 5Homo sapiens (human)
regulation of metabolic processMelanocortin receptor 5Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMu-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
sensory perceptionMu-type opioid receptorHomo sapiens (human)
negative regulation of cell population proliferationMu-type opioid receptorHomo sapiens (human)
sensory perception of painMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
behavioral response to ethanolMu-type opioid receptorHomo sapiens (human)
positive regulation of neurogenesisMu-type opioid receptorHomo sapiens (human)
negative regulation of Wnt protein secretionMu-type opioid receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeMu-type opioid receptorHomo sapiens (human)
calcium ion transmembrane transportMu-type opioid receptorHomo sapiens (human)
cellular response to morphineMu-type opioid receptorHomo sapiens (human)
regulation of cellular response to stressMu-type opioid receptorHomo sapiens (human)
regulation of NMDA receptor activityMu-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayMu-type opioid receptorHomo sapiens (human)
response to ethanolD(3) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(3) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
learning or memoryD(3) dopamine receptorHomo sapiens (human)
learningD(3) dopamine receptorHomo sapiens (human)
locomotory behaviorD(3) dopamine receptorHomo sapiens (human)
visual learningD(3) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(3) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(3) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(3) dopamine receptorHomo sapiens (human)
response to histamineD(3) dopamine receptorHomo sapiens (human)
social behaviorD(3) dopamine receptorHomo sapiens (human)
response to cocaineD(3) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(3) dopamine receptorHomo sapiens (human)
response to morphineD(3) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(3) dopamine receptorHomo sapiens (human)
positive regulation of mitotic nuclear divisionD(3) dopamine receptorHomo sapiens (human)
acid secretionD(3) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(3) dopamine receptorHomo sapiens (human)
negative regulation of oligodendrocyte differentiationD(3) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(3) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(3) dopamine receptorHomo sapiens (human)
musculoskeletal movement, spinal reflex actionD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(3) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(3) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(3) dopamine receptorHomo sapiens (human)
positive regulation of dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(3) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(3) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(3) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(3) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(3) dopamine receptorHomo sapiens (human)
calcium ion homeostasisAlpha-synucleinHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIAlpha-synucleinHomo sapiens (human)
microglial cell activationAlpha-synucleinHomo sapiens (human)
positive regulation of receptor recyclingAlpha-synucleinHomo sapiens (human)
positive regulation of neurotransmitter secretionAlpha-synucleinHomo sapiens (human)
negative regulation of protein kinase activityAlpha-synucleinHomo sapiens (human)
fatty acid metabolic processAlpha-synucleinHomo sapiens (human)
neutral lipid metabolic processAlpha-synucleinHomo sapiens (human)
phospholipid metabolic processAlpha-synucleinHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
mitochondrial membrane organizationAlpha-synucleinHomo sapiens (human)
adult locomotory behaviorAlpha-synucleinHomo sapiens (human)
response to xenobiotic stimulusAlpha-synucleinHomo sapiens (human)
response to iron(II) ionAlpha-synucleinHomo sapiens (human)
regulation of phospholipase activityAlpha-synucleinHomo sapiens (human)
negative regulation of platelet-derived growth factor receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
regulation of glutamate secretionAlpha-synucleinHomo sapiens (human)
regulation of dopamine secretionAlpha-synucleinHomo sapiens (human)
synaptic vesicle exocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle primingAlpha-synucleinHomo sapiens (human)
regulation of transmembrane transporter activityAlpha-synucleinHomo sapiens (human)
negative regulation of microtubule polymerizationAlpha-synucleinHomo sapiens (human)
receptor internalizationAlpha-synucleinHomo sapiens (human)
protein destabilizationAlpha-synucleinHomo sapiens (human)
response to magnesium ionAlpha-synucleinHomo sapiens (human)
negative regulation of transporter activityAlpha-synucleinHomo sapiens (human)
response to lipopolysaccharideAlpha-synucleinHomo sapiens (human)
negative regulation of monooxygenase activityAlpha-synucleinHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationAlpha-synucleinHomo sapiens (human)
response to type II interferonAlpha-synucleinHomo sapiens (human)
cellular response to oxidative stressAlpha-synucleinHomo sapiens (human)
SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
positive regulation of SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
regulation of locomotionAlpha-synucleinHomo sapiens (human)
dopamine biosynthetic processAlpha-synucleinHomo sapiens (human)
mitochondrial ATP synthesis coupled electron transportAlpha-synucleinHomo sapiens (human)
regulation of macrophage activationAlpha-synucleinHomo sapiens (human)
positive regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of neuron apoptotic processAlpha-synucleinHomo sapiens (human)
positive regulation of endocytosisAlpha-synucleinHomo sapiens (human)
negative regulation of exocytosisAlpha-synucleinHomo sapiens (human)
positive regulation of exocytosisAlpha-synucleinHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityAlpha-synucleinHomo sapiens (human)
synaptic vesicle endocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle transportAlpha-synucleinHomo sapiens (human)
positive regulation of inflammatory responseAlpha-synucleinHomo sapiens (human)
regulation of acyl-CoA biosynthetic processAlpha-synucleinHomo sapiens (human)
protein tetramerizationAlpha-synucleinHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolAlpha-synucleinHomo sapiens (human)
neuron apoptotic processAlpha-synucleinHomo sapiens (human)
dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of serotonin uptakeAlpha-synucleinHomo sapiens (human)
regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
negative regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
excitatory postsynaptic potentialAlpha-synucleinHomo sapiens (human)
long-term synaptic potentiationAlpha-synucleinHomo sapiens (human)
positive regulation of inositol phosphate biosynthetic processAlpha-synucleinHomo sapiens (human)
negative regulation of thrombin-activated receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
response to interleukin-1Alpha-synucleinHomo sapiens (human)
cellular response to copper ionAlpha-synucleinHomo sapiens (human)
cellular response to epinephrine stimulusAlpha-synucleinHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityAlpha-synucleinHomo sapiens (human)
supramolecular fiber organizationAlpha-synucleinHomo sapiens (human)
negative regulation of mitochondrial electron transport, NADH to ubiquinoneAlpha-synucleinHomo sapiens (human)
positive regulation of glutathione peroxidase activityAlpha-synucleinHomo sapiens (human)
positive regulation of hydrogen peroxide catabolic processAlpha-synucleinHomo sapiens (human)
regulation of synaptic vesicle recyclingAlpha-synucleinHomo sapiens (human)
regulation of reactive oxygen species biosynthetic processAlpha-synucleinHomo sapiens (human)
positive regulation of protein localization to cell peripheryAlpha-synucleinHomo sapiens (human)
negative regulation of chaperone-mediated autophagyAlpha-synucleinHomo sapiens (human)
regulation of presynapse assemblyAlpha-synucleinHomo sapiens (human)
amyloid fibril formationAlpha-synucleinHomo sapiens (human)
synapse organizationAlpha-synucleinHomo sapiens (human)
chemical synaptic transmissionAlpha-synucleinHomo sapiens (human)
immune responseDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerDelta-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
adult locomotory behaviorDelta-type opioid receptorHomo sapiens (human)
negative regulation of gene expressionDelta-type opioid receptorHomo sapiens (human)
negative regulation of protein-containing complex assemblyDelta-type opioid receptorHomo sapiens (human)
positive regulation of CREB transcription factor activityDelta-type opioid receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationDelta-type opioid receptorHomo sapiens (human)
response to nicotineDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
eating behaviorDelta-type opioid receptorHomo sapiens (human)
regulation of mitochondrial membrane potentialDelta-type opioid receptorHomo sapiens (human)
regulation of calcium ion transportDelta-type opioid receptorHomo sapiens (human)
cellular response to growth factor stimulusDelta-type opioid receptorHomo sapiens (human)
cellular response to hypoxiaDelta-type opioid receptorHomo sapiens (human)
cellular response to toxic substanceDelta-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayDelta-type opioid receptorHomo sapiens (human)
immune responseKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
chemical synaptic transmissionKappa-type opioid receptorHomo sapiens (human)
sensory perceptionKappa-type opioid receptorHomo sapiens (human)
locomotory behaviorKappa-type opioid receptorHomo sapiens (human)
sensory perception of painKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
response to insulinKappa-type opioid receptorHomo sapiens (human)
positive regulation of dopamine secretionKappa-type opioid receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionKappa-type opioid receptorHomo sapiens (human)
response to nicotineKappa-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
maternal behaviorKappa-type opioid receptorHomo sapiens (human)
eating behaviorKappa-type opioid receptorHomo sapiens (human)
response to estrogenKappa-type opioid receptorHomo sapiens (human)
estrous cycleKappa-type opioid receptorHomo sapiens (human)
response to ethanolKappa-type opioid receptorHomo sapiens (human)
regulation of saliva secretionKappa-type opioid receptorHomo sapiens (human)
behavioral response to cocaineKappa-type opioid receptorHomo sapiens (human)
sensory perception of temperature stimulusKappa-type opioid receptorHomo sapiens (human)
defense response to virusKappa-type opioid receptorHomo sapiens (human)
cellular response to lipopolysaccharideKappa-type opioid receptorHomo sapiens (human)
cellular response to glucose stimulusKappa-type opioid receptorHomo sapiens (human)
positive regulation of p38MAPK cascadeKappa-type opioid receptorHomo sapiens (human)
positive regulation of potassium ion transmembrane transportKappa-type opioid receptorHomo sapiens (human)
response to acrylamideKappa-type opioid receptorHomo sapiens (human)
positive regulation of eating behaviorKappa-type opioid receptorHomo sapiens (human)
conditioned place preferenceKappa-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayKappa-type opioid receptorHomo sapiens (human)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein phosphorylationProtein kinase C iota typeHomo sapiens (human)
protein targeting to membraneProtein kinase C iota typeHomo sapiens (human)
cytoskeleton organizationProtein kinase C iota typeHomo sapiens (human)
actin filament organizationProtein kinase C iota typeHomo sapiens (human)
positive regulation of neuron projection developmentProtein kinase C iota typeHomo sapiens (human)
vesicle-mediated transportProtein kinase C iota typeHomo sapiens (human)
cell migrationProtein kinase C iota typeHomo sapiens (human)
cellular response to insulin stimulusProtein kinase C iota typeHomo sapiens (human)
negative regulation of glial cell apoptotic processProtein kinase C iota typeHomo sapiens (human)
establishment of apical/basal cell polarityProtein kinase C iota typeHomo sapiens (human)
eye photoreceptor cell developmentProtein kinase C iota typeHomo sapiens (human)
negative regulation of apoptotic processProtein kinase C iota typeHomo sapiens (human)
negative regulation of neuron apoptotic processProtein kinase C iota typeHomo sapiens (human)
establishment or maintenance of epithelial cell apical/basal polarityProtein kinase C iota typeHomo sapiens (human)
cell-cell junction organizationProtein kinase C iota typeHomo sapiens (human)
positive regulation of Notch signaling pathwayProtein kinase C iota typeHomo sapiens (human)
positive regulation of glucose importProtein kinase C iota typeHomo sapiens (human)
secretionProtein kinase C iota typeHomo sapiens (human)
Golgi vesicle buddingProtein kinase C iota typeHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityProtein kinase C iota typeHomo sapiens (human)
positive regulation of glial cell proliferationProtein kinase C iota typeHomo sapiens (human)
membrane organizationProtein kinase C iota typeHomo sapiens (human)
cellular response to chemical stressProtein kinase C iota typeHomo sapiens (human)
response to interleukin-1Protein kinase C iota typeHomo sapiens (human)
regulation of postsynaptic membrane neurotransmitter receptor levelsProtein kinase C iota typeHomo sapiens (human)
positive regulation of protein localization to plasma membraneProtein kinase C iota typeHomo sapiens (human)
positive regulation of endothelial cell apoptotic processProtein kinase C iota typeHomo sapiens (human)
intracellular signal transductionProtein kinase C iota typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C iota typeHomo sapiens (human)
regulation of heart rateMelanocortin receptor 3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelanocortin receptor 3Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 3Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 3Homo sapiens (human)
regulation of blood pressureMelanocortin receptor 3Homo sapiens (human)
circadian regulation of gene expressionMelanocortin receptor 3Homo sapiens (human)
homoiothermyMelanocortin receptor 3Homo sapiens (human)
locomotor rhythmMelanocortin receptor 3Homo sapiens (human)
sodium ion homeostasisMelanocortin receptor 3Homo sapiens (human)
regulation of feeding behaviorMelanocortin receptor 3Homo sapiens (human)
regulation of metabolic processMelanocortin receptor 3Homo sapiens (human)
cerebral cortex cell migration5-hydroxytryptamine receptor 6Homo sapiens (human)
positive regulation of TOR signaling5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 6Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 6Homo sapiens (human)
regulation of DNA-templated transcriptionEstrogen-related receptor gammaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEstrogen-related receptor gammaHomo sapiens (human)
retinoic acid receptor signaling pathwayEstrogen-related receptor gammaHomo sapiens (human)
positive regulation of cold-induced thermogenesisEstrogen-related receptor gammaHomo sapiens (human)
regulation of transcription by RNA polymerase IIEstrogen-related receptor gammaHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayEstrogen-related receptor gammaHomo sapiens (human)
monoamine transportSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent dopamine transporter Homo sapiens (human)
lactationSodium-dependent dopamine transporter Homo sapiens (human)
sensory perception of smellSodium-dependent dopamine transporter Homo sapiens (human)
locomotory behaviorSodium-dependent dopamine transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent dopamine transporter Homo sapiens (human)
response to iron ionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine transportSodium-dependent dopamine transporter Homo sapiens (human)
adenohypophysis developmentSodium-dependent dopamine transporter Homo sapiens (human)
response to nicotineSodium-dependent dopamine transporter Homo sapiens (human)
positive regulation of multicellular organism growthSodium-dependent dopamine transporter Homo sapiens (human)
regulation of dopamine metabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to cocaineSodium-dependent dopamine transporter Homo sapiens (human)
dopamine biosynthetic processSodium-dependent dopamine transporter Homo sapiens (human)
dopamine catabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to ethanolSodium-dependent dopamine transporter Homo sapiens (human)
cognitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent dopamine transporter Homo sapiens (human)
response to cAMPSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
prepulse inhibitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
hyaloid vascular plexus regressionSodium-dependent dopamine transporter Homo sapiens (human)
amino acid transportSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine transportSodium-dependent dopamine transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent dopamine transporter Homo sapiens (human)
MAPK cascadeProtein kinase C epsilon typeHomo sapiens (human)
macrophage activation involved in immune responseProtein kinase C epsilon typeHomo sapiens (human)
protein phosphorylationProtein kinase C epsilon typeHomo sapiens (human)
apoptotic processProtein kinase C epsilon typeHomo sapiens (human)
signal transductionProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of epithelial cell migrationProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of fibroblast migrationProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of cell-substrate adhesionProtein kinase C epsilon typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C epsilon typeHomo sapiens (human)
insulin secretionProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of actin filament polymerizationProtein kinase C epsilon typeHomo sapiens (human)
negative regulation of protein ubiquitinationProtein kinase C epsilon typeHomo sapiens (human)
cell-substrate adhesionProtein kinase C epsilon typeHomo sapiens (human)
lipopolysaccharide-mediated signaling pathwayProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of insulin secretionProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of cytokinesisProtein kinase C epsilon typeHomo sapiens (human)
locomotory exploration behaviorProtein kinase C epsilon typeHomo sapiens (human)
TRAM-dependent toll-like receptor 4 signaling pathwayProtein kinase C epsilon typeHomo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionProtein kinase C epsilon typeHomo sapiens (human)
response to morphineProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of MAPK cascadeProtein kinase C epsilon typeHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of lipid catabolic processProtein kinase C epsilon typeHomo sapiens (human)
regulation of release of sequestered calcium ion into cytosolProtein kinase C epsilon typeHomo sapiens (human)
cell divisionProtein kinase C epsilon typeHomo sapiens (human)
establishment of localization in cellProtein kinase C epsilon typeHomo sapiens (human)
synaptic transmission, GABAergicProtein kinase C epsilon typeHomo sapiens (human)
regulation of insulin secretion involved in cellular response to glucose stimulusProtein kinase C epsilon typeHomo sapiens (human)
mucus secretionProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of mucus secretionProtein kinase C epsilon typeHomo sapiens (human)
cellular response to ethanolProtein kinase C epsilon typeHomo sapiens (human)
cellular response to prostaglandin E stimulusProtein kinase C epsilon typeHomo sapiens (human)
cellular response to hypoxiaProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of wound healingProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of protein localization to plasma membraneProtein kinase C epsilon typeHomo sapiens (human)
negative regulation of sodium ion transmembrane transporter activityProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of cellular glucuronidationProtein kinase C epsilon typeHomo sapiens (human)
intracellular signal transductionProtein kinase C epsilon typeHomo sapiens (human)
regulation of cell growthProtein kinase C theta typeHomo sapiens (human)
regulation of DNA-templated transcriptionProtein kinase C theta typeHomo sapiens (human)
protein phosphorylationProtein kinase C theta typeHomo sapiens (human)
membrane protein ectodomain proteolysisProtein kinase C theta typeHomo sapiens (human)
inflammatory responseProtein kinase C theta typeHomo sapiens (human)
axon guidanceProtein kinase C theta typeHomo sapiens (human)
positive regulation of telomere maintenance via telomeraseProtein kinase C theta typeHomo sapiens (human)
positive regulation of interleukin-17 productionProtein kinase C theta typeHomo sapiens (human)
positive regulation of interleukin-2 productionProtein kinase C theta typeHomo sapiens (human)
positive regulation of interleukin-4 productionProtein kinase C theta typeHomo sapiens (human)
intracellular signal transductionProtein kinase C theta typeHomo sapiens (human)
CD4-positive, alpha-beta T cell proliferationProtein kinase C theta typeHomo sapiens (human)
Fc-epsilon receptor signaling pathwayProtein kinase C theta typeHomo sapiens (human)
negative regulation of insulin receptor signaling pathwayProtein kinase C theta typeHomo sapiens (human)
positive regulation of T cell activationProtein kinase C theta typeHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityProtein kinase C theta typeHomo sapiens (human)
positive regulation of telomerase activityProtein kinase C theta typeHomo sapiens (human)
cell chemotaxisProtein kinase C theta typeHomo sapiens (human)
negative regulation of T cell apoptotic processProtein kinase C theta typeHomo sapiens (human)
regulation of platelet aggregationProtein kinase C theta typeHomo sapiens (human)
positive regulation of telomere cappingProtein kinase C theta typeHomo sapiens (human)
positive regulation of T-helper 17 type immune responseProtein kinase C theta typeHomo sapiens (human)
positive regulation of CD4-positive, alpha-beta T cell proliferationProtein kinase C theta typeHomo sapiens (human)
positive regulation of T-helper 2 cell activationProtein kinase C theta typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C theta typeHomo sapiens (human)
microtubule cytoskeleton organizationProtein kinase C zeta typeHomo sapiens (human)
positive regulation of cell-matrix adhesionProtein kinase C zeta typeHomo sapiens (human)
protein phosphorylationProtein kinase C zeta typeHomo sapiens (human)
inflammatory responseProtein kinase C zeta typeHomo sapiens (human)
signal transductionProtein kinase C zeta typeHomo sapiens (human)
cell surface receptor signaling pathwayProtein kinase C zeta typeHomo sapiens (human)
long-term memoryProtein kinase C zeta typeHomo sapiens (human)
positive regulation of cell population proliferationProtein kinase C zeta typeHomo sapiens (human)
cell migrationProtein kinase C zeta typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C zeta typeHomo sapiens (human)
establishment of cell polarityProtein kinase C zeta typeHomo sapiens (human)
negative regulation of protein-containing complex assemblyProtein kinase C zeta typeHomo sapiens (human)
positive regulation of interleukin-10 productionProtein kinase C zeta typeHomo sapiens (human)
positive regulation of interleukin-13 productionProtein kinase C zeta typeHomo sapiens (human)
positive regulation of interleukin-4 productionProtein kinase C zeta typeHomo sapiens (human)
positive regulation of interleukin-5 productionProtein kinase C zeta typeHomo sapiens (human)
cellular response to insulin stimulusProtein kinase C zeta typeHomo sapiens (human)
negative regulation of apoptotic processProtein kinase C zeta typeHomo sapiens (human)
establishment or maintenance of epithelial cell apical/basal polarityProtein kinase C zeta typeHomo sapiens (human)
positive regulation of T-helper 2 cell differentiationProtein kinase C zeta typeHomo sapiens (human)
negative regulation of insulin receptor signaling pathwayProtein kinase C zeta typeHomo sapiens (human)
positive regulation of insulin receptor signaling pathwayProtein kinase C zeta typeHomo sapiens (human)
vesicle transport along microtubuleProtein kinase C zeta typeHomo sapiens (human)
negative regulation of peptidyl-tyrosine phosphorylationProtein kinase C zeta typeHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityProtein kinase C zeta typeHomo sapiens (human)
positive regulation of protein transportProtein kinase C zeta typeHomo sapiens (human)
membrane depolarizationProtein kinase C zeta typeHomo sapiens (human)
membrane hyperpolarizationProtein kinase C zeta typeHomo sapiens (human)
long-term synaptic potentiationProtein kinase C zeta typeHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeProtein kinase C zeta typeHomo sapiens (human)
protein kinase C signalingProtein kinase C zeta typeHomo sapiens (human)
protein localization to plasma membraneProtein kinase C zeta typeHomo sapiens (human)
regulation of neurotransmitter receptor localization to postsynaptic specialization membraneProtein kinase C zeta typeHomo sapiens (human)
neuron projection extensionProtein kinase C zeta typeHomo sapiens (human)
positive regulation of excitatory postsynaptic potentialProtein kinase C zeta typeHomo sapiens (human)
positive regulation of T-helper 2 cell cytokine productionProtein kinase C zeta typeHomo sapiens (human)
intracellular signal transductionProtein kinase C zeta typeHomo sapiens (human)
protein phosphorylationProtein kinase C delta typeHomo sapiens (human)
apoptotic processProtein kinase C delta typeHomo sapiens (human)
DNA damage responseProtein kinase C delta typeHomo sapiens (human)
signal transductionProtein kinase C delta typeHomo sapiens (human)
intrinsic apoptotic signaling pathway in response to oxidative stressProtein kinase C delta typeHomo sapiens (human)
regulation of signaling receptor activityProtein kinase C delta typeHomo sapiens (human)
immunoglobulin mediated immune responseProtein kinase C delta typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C delta typeHomo sapiens (human)
peptidyl-threonine phosphorylationProtein kinase C delta typeHomo sapiens (human)
termination of signal transductionProtein kinase C delta typeHomo sapiens (human)
negative regulation of actin filament polymerizationProtein kinase C delta typeHomo sapiens (human)
positive regulation of endodeoxyribonuclease activityProtein kinase C delta typeHomo sapiens (human)
negative regulation of protein bindingProtein kinase C delta typeHomo sapiens (human)
activation of protein kinase activityProtein kinase C delta typeHomo sapiens (human)
positive regulation of superoxide anion generationProtein kinase C delta typeHomo sapiens (human)
regulation of actin cytoskeleton organizationProtein kinase C delta typeHomo sapiens (human)
negative regulation of glial cell apoptotic processProtein kinase C delta typeHomo sapiens (human)
cellular response to UVProtein kinase C delta typeHomo sapiens (human)
positive regulation of protein dephosphorylationProtein kinase C delta typeHomo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisProtein kinase C delta typeHomo sapiens (human)
B cell proliferationProtein kinase C delta typeHomo sapiens (human)
neutrophil activationProtein kinase C delta typeHomo sapiens (human)
positive regulation of protein import into nucleusProtein kinase C delta typeHomo sapiens (human)
defense response to bacteriumProtein kinase C delta typeHomo sapiens (human)
negative regulation of MAP kinase activityProtein kinase C delta typeHomo sapiens (human)
regulation of mRNA stabilityProtein kinase C delta typeHomo sapiens (human)
post-translational protein modificationProtein kinase C delta typeHomo sapiens (human)
negative regulation of insulin receptor signaling pathwayProtein kinase C delta typeHomo sapiens (human)
negative regulation of inflammatory responseProtein kinase C delta typeHomo sapiens (human)
negative regulation of peptidyl-tyrosine phosphorylationProtein kinase C delta typeHomo sapiens (human)
protein stabilizationProtein kinase C delta typeHomo sapiens (human)
negative regulation of filopodium assemblyProtein kinase C delta typeHomo sapiens (human)
cell chemotaxisProtein kinase C delta typeHomo sapiens (human)
cellular response to hydrogen peroxideProtein kinase C delta typeHomo sapiens (human)
cellular response to hydroperoxideProtein kinase C delta typeHomo sapiens (human)
negative regulation of platelet aggregationProtein kinase C delta typeHomo sapiens (human)
cellular senescenceProtein kinase C delta typeHomo sapiens (human)
positive regulation of phospholipid scramblase activityProtein kinase C delta typeHomo sapiens (human)
cellular response to angiotensinProtein kinase C delta typeHomo sapiens (human)
regulation of ceramide biosynthetic processProtein kinase C delta typeHomo sapiens (human)
positive regulation of ceramide biosynthetic processProtein kinase C delta typeHomo sapiens (human)
positive regulation of glucosylceramide catabolic processProtein kinase C delta typeHomo sapiens (human)
positive regulation of sphingomyelin catabolic processProtein kinase C delta typeHomo sapiens (human)
positive regulation of apoptotic signaling pathwayProtein kinase C delta typeHomo sapiens (human)
intracellular signal transductionProtein kinase C delta typeHomo sapiens (human)
G1/S transition of mitotic cell cycleSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
response to amphetamineSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
protein dephosphorylationSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
protein import into nucleusSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
calcium ion transportSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
epidermis developmentSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of gene expressionSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of gene expressionSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
transition between fast and slow fiberSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
cardiac muscle hypertrophy in response to stressSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
dephosphorylationSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of signalingSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
keratinocyte differentiationSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of cell migrationSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
calcineurin-NFAT signaling cascadeSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
multicellular organismal response to stressSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
wound healingSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of activated T cell proliferationSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
T cell activationSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
skeletal muscle tissue regenerationSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of osteoblast differentiationSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of osteoclast differentiationSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of cell adhesionSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of endocytosisSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of transcription by RNA polymerase IISerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of insulin secretionSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of saliva secretionSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
skeletal muscle fiber developmentSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
dendrite morphogenesisSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of dendrite morphogenesisSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
modulation of chemical synaptic transmissionSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
response to calcium ionSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
excitatory postsynaptic potentialSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
regulation of cell proliferation involved in kidney morphogenesisSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
peptidyl-serine dephosphorylationSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of calcineurin-NFAT signaling cascadeSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
cellular response to glucose stimulusSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of glomerulus developmentSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
renal filtrationSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
calcineurin-mediated signalingSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of angiotensin-activated signaling pathwaySerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of cardiac muscle hypertrophy in response to stressSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of connective tissue replacementSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of calcium ion import across plasma membraneSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of calcium ion import across plasma membraneSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
peptide hormone processingPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
low-density lipoprotein particle remodelingPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
lipid oxidationPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
plasma lipoprotein particle oxidationPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
phosphatidylcholine catabolic processPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
platelet activating factor metabolic processPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
positive regulation of inflammatory responsePlatelet-activating factor acetylhydrolaseHomo sapiens (human)
platelet activating factor catabolic processPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
positive regulation of monocyte chemotaxisPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
phosphatidic acid biosynthetic processPhospholipase D1Homo sapiens (human)
chemotaxisPhospholipase D1Homo sapiens (human)
small GTPase-mediated signal transductionPhospholipase D1Homo sapiens (human)
Ras protein signal transductionPhospholipase D1Homo sapiens (human)
cellular response to nutrientPhospholipase D1Homo sapiens (human)
regulation of microvillus assemblyPhospholipase D1Homo sapiens (human)
positive regulation of translationPhospholipase D1Homo sapiens (human)
regulation of synaptic vesicle cyclePhospholipase D1Homo sapiens (human)
phospholipid catabolic processPhospholipase D1Homo sapiens (human)
regulation of vesicle-mediated transportPhospholipase D1Homo sapiens (human)
cholesterol biosynthetic process3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
cholesterol metabolic process3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
hemopoiesis3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
cholesterol biosynthetic process via desmosterol3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
cholesterol biosynthetic process via lathosterol3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
ossification involved in bone maturation3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
peptidyl-threonine phosphorylationSerine/threonine-protein kinase D1Homo sapiens (human)
angiogenesisSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of endothelial cell proliferationSerine/threonine-protein kinase D1Homo sapiens (human)
apoptotic processSerine/threonine-protein kinase D1Homo sapiens (human)
inflammatory responseSerine/threonine-protein kinase D1Homo sapiens (human)
Golgi organizationSerine/threonine-protein kinase D1Homo sapiens (human)
signal transductionSerine/threonine-protein kinase D1Homo sapiens (human)
integrin-mediated signaling pathwaySerine/threonine-protein kinase D1Homo sapiens (human)
nervous system developmentSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of autophagySerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of endothelial cell migrationSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of gene expressionSerine/threonine-protein kinase D1Homo sapiens (human)
regulation of keratinocyte proliferationSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of neuron projection developmentSerine/threonine-protein kinase D1Homo sapiens (human)
regulation of skeletal muscle contraction by modulation of calcium ion sensitivity of myofibrilSerine/threonine-protein kinase D1Homo sapiens (human)
peptidyl-serine phosphorylationSerine/threonine-protein kinase D1Homo sapiens (human)
peptidyl-threonine phosphorylationSerine/threonine-protein kinase D1Homo sapiens (human)
sphingolipid biosynthetic processSerine/threonine-protein kinase D1Homo sapiens (human)
cell differentiationSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to amino acid starvationSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to oxidative stressSerine/threonine-protein kinase D1Homo sapiens (human)
intracellular signal transductionSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of protein import into nucleusSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationSerine/threonine-protein kinase D1Homo sapiens (human)
innate immune responseSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of osteoblast differentiationSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of angiogenesisSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of cell sizeSerine/threonine-protein kinase D1Homo sapiens (human)
negative regulation of endocytosisSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IISerine/threonine-protein kinase D1Homo sapiens (human)
protein autophosphorylationSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of protein export from nucleusSerine/threonine-protein kinase D1Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwaySerine/threonine-protein kinase D1Homo sapiens (human)
Golgi vesicle transportSerine/threonine-protein kinase D1Homo sapiens (human)
defense response to Gram-negative bacteriumSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activitySerine/threonine-protein kinase D1Homo sapiens (human)
regulation of release of sequestered calcium ion into cytosolSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of sarcomere organizationSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to hydroperoxideSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to norepinephrine stimulusSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of peptide hormone secretionSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of NLRP3 inflammasome complex assemblySerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to angiotensinSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to phorbol 13-acetate 12-myristateSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to endothelinSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of endothelial cell chemotaxisSerine/threonine-protein kinase D1Homo sapiens (human)
regulation of integrin-mediated signaling pathwaySerine/threonine-protein kinase D1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySerine/threonine-protein kinase D1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIEstrogen receptor betaHomo sapiens (human)
regulation of DNA-templated transcriptionEstrogen receptor betaHomo sapiens (human)
signal transductionEstrogen receptor betaHomo sapiens (human)
cell-cell signalingEstrogen receptor betaHomo sapiens (human)
negative regulation of cell growthEstrogen receptor betaHomo sapiens (human)
intracellular estrogen receptor signaling pathwayEstrogen receptor betaHomo sapiens (human)
positive regulation of DNA-templated transcriptionEstrogen receptor betaHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityEstrogen receptor betaHomo sapiens (human)
cellular response to estradiol stimulusEstrogen receptor betaHomo sapiens (human)
regulation of transcription by RNA polymerase IIEstrogen receptor betaHomo sapiens (human)
cellular response to estrogen stimulusEstrogen receptor betaHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
lipid transportSigma non-opioid intracellular receptor 1Homo sapiens (human)
nervous system developmentSigma non-opioid intracellular receptor 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwaySigma non-opioid intracellular receptor 1Homo sapiens (human)
regulation of neuron apoptotic processSigma non-opioid intracellular receptor 1Homo sapiens (human)
protein homotrimerizationSigma non-opioid intracellular receptor 1Homo sapiens (human)
sterol metabolic processEmopamil-binding protein-likeHomo sapiens (human)
negative regulation of signaling receptor activityAngiotensin-converting enzyme 2 Homo sapiens (human)
symbiont entry into host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of cytokine productionAngiotensin-converting enzyme 2 Homo sapiens (human)
angiotensin maturationAngiotensin-converting enzyme 2 Homo sapiens (human)
angiotensin-mediated drinking behaviorAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of systemic arterial blood pressure by renin-angiotensinAngiotensin-converting enzyme 2 Homo sapiens (human)
tryptophan transportAngiotensin-converting enzyme 2 Homo sapiens (human)
viral life cycleAngiotensin-converting enzyme 2 Homo sapiens (human)
receptor-mediated endocytosis of virus by host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of vasoconstrictionAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of transmembrane transporter activityAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of cell population proliferationAngiotensin-converting enzyme 2 Homo sapiens (human)
symbiont entry into host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
receptor-mediated virion attachment to host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
negative regulation of smooth muscle cell proliferationAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of inflammatory responseAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of amino acid transportAngiotensin-converting enzyme 2 Homo sapiens (human)
maternal process involved in female pregnancyAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of cardiac muscle contractionAngiotensin-converting enzyme 2 Homo sapiens (human)
membrane fusionAngiotensin-converting enzyme 2 Homo sapiens (human)
negative regulation of ERK1 and ERK2 cascadeAngiotensin-converting enzyme 2 Homo sapiens (human)
blood vessel diameter maintenanceAngiotensin-converting enzyme 2 Homo sapiens (human)
entry receptor-mediated virion attachment to host cellAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of gap junction assemblyAngiotensin-converting enzyme 2 Homo sapiens (human)
regulation of cardiac conductionAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of L-proline import across plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processAngiotensin-converting enzyme 2 Homo sapiens (human)
cholesterol biosynthetic process7-dehydrocholesterol reductaseHomo sapiens (human)
cholesterol biosynthetic process via desmosterol7-dehydrocholesterol reductaseHomo sapiens (human)
cholesterol biosynthetic process via lathosterol7-dehydrocholesterol reductaseHomo sapiens (human)
brassinosteroid biosynthetic process7-dehydrocholesterol reductaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (349)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
serine-type endopeptidase activityTransmembrane protease serine 2Homo sapiens (human)
protein bindingTransmembrane protease serine 2Homo sapiens (human)
serine-type peptidase activityTransmembrane protease serine 2Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activitySerine/threonine-protein kinase D3Homo sapiens (human)
protein bindingSerine/threonine-protein kinase D3Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase D3Homo sapiens (human)
kinase activitySerine/threonine-protein kinase D3Homo sapiens (human)
metal ion bindingSerine/threonine-protein kinase D3Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase D3Homo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase D3Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
virus receptor activityEpidermal growth factor receptorHomo sapiens (human)
chromatin bindingEpidermal growth factor receptorHomo sapiens (human)
double-stranded DNA bindingEpidermal growth factor receptorHomo sapiens (human)
MAP kinase kinase kinase activityEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane signaling receptor activityEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
integrin bindingEpidermal growth factor receptorHomo sapiens (human)
protein bindingEpidermal growth factor receptorHomo sapiens (human)
calmodulin bindingEpidermal growth factor receptorHomo sapiens (human)
ATP bindingEpidermal growth factor receptorHomo sapiens (human)
enzyme bindingEpidermal growth factor receptorHomo sapiens (human)
kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein phosphatase bindingEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
ubiquitin protein ligase bindingEpidermal growth factor receptorHomo sapiens (human)
identical protein bindingEpidermal growth factor receptorHomo sapiens (human)
cadherin bindingEpidermal growth factor receptorHomo sapiens (human)
actin filament bindingEpidermal growth factor receptorHomo sapiens (human)
ATPase bindingEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor bindingEpidermal growth factor receptorHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificEstrogen receptorHomo sapiens (human)
TFIIB-class transcription factor bindingEstrogen receptorHomo sapiens (human)
transcription coregulator bindingEstrogen receptorHomo sapiens (human)
transcription corepressor bindingEstrogen receptorHomo sapiens (human)
transcription coactivator bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificEstrogen receptorHomo sapiens (human)
chromatin bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
nuclear receptor activityEstrogen receptorHomo sapiens (human)
steroid bindingEstrogen receptorHomo sapiens (human)
protein bindingEstrogen receptorHomo sapiens (human)
calmodulin bindingEstrogen receptorHomo sapiens (human)
beta-catenin bindingEstrogen receptorHomo sapiens (human)
zinc ion bindingEstrogen receptorHomo sapiens (human)
TBP-class protein bindingEstrogen receptorHomo sapiens (human)
enzyme bindingEstrogen receptorHomo sapiens (human)
protein kinase bindingEstrogen receptorHomo sapiens (human)
nitric-oxide synthase regulator activityEstrogen receptorHomo sapiens (human)
nuclear estrogen receptor activityEstrogen receptorHomo sapiens (human)
nuclear estrogen receptor bindingEstrogen receptorHomo sapiens (human)
estrogen response element bindingEstrogen receptorHomo sapiens (human)
identical protein bindingEstrogen receptorHomo sapiens (human)
ATPase bindingEstrogen receptorHomo sapiens (human)
14-3-3 protein bindingEstrogen receptorHomo sapiens (human)
sequence-specific double-stranded DNA bindingEstrogen receptorHomo sapiens (human)
galactosylceramidase activityLysosomal acid glucosylceramidaseHomo sapiens (human)
glucosylceramidase activityLysosomal acid glucosylceramidaseHomo sapiens (human)
signaling receptor bindingLysosomal acid glucosylceramidaseHomo sapiens (human)
scavenger receptor bindingLysosomal acid glucosylceramidaseHomo sapiens (human)
protein bindingLysosomal acid glucosylceramidaseHomo sapiens (human)
glucosyltransferase activityLysosomal acid glucosylceramidaseHomo sapiens (human)
steryl-beta-glucosidase activityLysosomal acid glucosylceramidaseHomo sapiens (human)
growth factor bindingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
RNA polymerase I core bindingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
protein tyrosine kinase activityReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activityReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
transmembrane signaling receptor activityReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
signaling receptor bindingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
protein bindingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
ATP bindingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
coreceptor activityReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
receptor tyrosine kinase bindingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
identical protein bindingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
ErbB-3 class receptor bindingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
protein heterodimerization activityReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
fibroblast growth factor bindingIntegrin beta-3Homo sapiens (human)
C-X3-C chemokine bindingIntegrin beta-3Homo sapiens (human)
insulin-like growth factor I bindingIntegrin beta-3Homo sapiens (human)
neuregulin bindingIntegrin beta-3Homo sapiens (human)
virus receptor activityIntegrin beta-3Homo sapiens (human)
fibronectin bindingIntegrin beta-3Homo sapiens (human)
protease bindingIntegrin beta-3Homo sapiens (human)
protein disulfide isomerase activityIntegrin beta-3Homo sapiens (human)
protein kinase C bindingIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor bindingIntegrin beta-3Homo sapiens (human)
integrin bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin beta-3Homo sapiens (human)
coreceptor activityIntegrin beta-3Homo sapiens (human)
enzyme bindingIntegrin beta-3Homo sapiens (human)
identical protein bindingIntegrin beta-3Homo sapiens (human)
vascular endothelial growth factor receptor 2 bindingIntegrin beta-3Homo sapiens (human)
metal ion bindingIntegrin beta-3Homo sapiens (human)
cell adhesion molecule bindingIntegrin beta-3Homo sapiens (human)
extracellular matrix bindingIntegrin beta-3Homo sapiens (human)
fibrinogen bindingIntegrin beta-3Homo sapiens (human)
protein kinase activityProtein kinase C gamma typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C gamma typeHomo sapiens (human)
calcium,diacylglycerol-dependent serine/threonine kinase activityProtein kinase C gamma typeHomo sapiens (human)
protein serine/threonine/tyrosine kinase activityProtein kinase C gamma typeHomo sapiens (human)
protein bindingProtein kinase C gamma typeHomo sapiens (human)
ATP bindingProtein kinase C gamma typeHomo sapiens (human)
zinc ion bindingProtein kinase C gamma typeHomo sapiens (human)
protein serine kinase activityProtein kinase C gamma typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C gamma typeHomo sapiens (human)
chromatin bindingProtein kinase C beta typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C beta typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C beta typeHomo sapiens (human)
protein kinase C bindingProtein kinase C beta typeHomo sapiens (human)
calcium channel regulator activityProtein kinase C beta typeHomo sapiens (human)
protein bindingProtein kinase C beta typeHomo sapiens (human)
ATP bindingProtein kinase C beta typeHomo sapiens (human)
zinc ion bindingProtein kinase C beta typeHomo sapiens (human)
nuclear receptor coactivator activityProtein kinase C beta typeHomo sapiens (human)
histone H3T6 kinase activityProtein kinase C beta typeHomo sapiens (human)
histone bindingProtein kinase C beta typeHomo sapiens (human)
nuclear androgen receptor bindingProtein kinase C beta typeHomo sapiens (human)
protein serine kinase activityProtein kinase C beta typeHomo sapiens (human)
phosphotyrosine residue bindingTyrosine-protein kinase LckHomo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase LckHomo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase LckHomo sapiens (human)
protein serine/threonine phosphatase activityTyrosine-protein kinase LckHomo sapiens (human)
protein bindingTyrosine-protein kinase LckHomo sapiens (human)
ATP bindingTyrosine-protein kinase LckHomo sapiens (human)
phospholipase activator activityTyrosine-protein kinase LckHomo sapiens (human)
protein kinase bindingTyrosine-protein kinase LckHomo sapiens (human)
protein phosphatase bindingTyrosine-protein kinase LckHomo sapiens (human)
SH2 domain bindingTyrosine-protein kinase LckHomo sapiens (human)
T cell receptor bindingTyrosine-protein kinase LckHomo sapiens (human)
CD4 receptor bindingTyrosine-protein kinase LckHomo sapiens (human)
CD8 receptor bindingTyrosine-protein kinase LckHomo sapiens (human)
identical protein bindingTyrosine-protein kinase LckHomo sapiens (human)
phospholipase bindingTyrosine-protein kinase LckHomo sapiens (human)
phosphatidylinositol 3-kinase bindingTyrosine-protein kinase LckHomo sapiens (human)
ATPase bindingTyrosine-protein kinase LckHomo sapiens (human)
signaling receptor bindingTyrosine-protein kinase LckHomo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase FynHomo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase FynHomo sapiens (human)
protein bindingTyrosine-protein kinase FynHomo sapiens (human)
ATP bindingTyrosine-protein kinase FynHomo sapiens (human)
phospholipase activator activityTyrosine-protein kinase FynHomo sapiens (human)
enzyme bindingTyrosine-protein kinase FynHomo sapiens (human)
type 5 metabotropic glutamate receptor bindingTyrosine-protein kinase FynHomo sapiens (human)
identical protein bindingTyrosine-protein kinase FynHomo sapiens (human)
alpha-tubulin bindingTyrosine-protein kinase FynHomo sapiens (human)
phospholipase bindingTyrosine-protein kinase FynHomo sapiens (human)
transmembrane transporter bindingTyrosine-protein kinase FynHomo sapiens (human)
metal ion bindingTyrosine-protein kinase FynHomo sapiens (human)
ephrin receptor bindingTyrosine-protein kinase FynHomo sapiens (human)
tau protein bindingTyrosine-protein kinase FynHomo sapiens (human)
tau-protein kinase activityTyrosine-protein kinase FynHomo sapiens (human)
growth factor receptor bindingTyrosine-protein kinase FynHomo sapiens (human)
scaffold protein bindingTyrosine-protein kinase FynHomo sapiens (human)
disordered domain specific bindingTyrosine-protein kinase FynHomo sapiens (human)
signaling receptor bindingTyrosine-protein kinase FynHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingProgesterone receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificProgesterone receptorHomo sapiens (human)
transcription coactivator bindingProgesterone receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificProgesterone receptorHomo sapiens (human)
DNA bindingProgesterone receptorHomo sapiens (human)
nuclear steroid receptor activityProgesterone receptorHomo sapiens (human)
G protein-coupled receptor activityProgesterone receptorHomo sapiens (human)
steroid bindingProgesterone receptorHomo sapiens (human)
protein bindingProgesterone receptorHomo sapiens (human)
zinc ion bindingProgesterone receptorHomo sapiens (human)
enzyme bindingProgesterone receptorHomo sapiens (human)
identical protein bindingProgesterone receptorHomo sapiens (human)
ATPase bindingProgesterone receptorHomo sapiens (human)
estrogen response element bindingProgesterone receptorHomo sapiens (human)
nuclear receptor activityProgesterone receptorHomo sapiens (human)
fibronectin bindingProcathepsin LHomo sapiens (human)
cysteine-type endopeptidase activityProcathepsin LHomo sapiens (human)
protein bindingProcathepsin LHomo sapiens (human)
collagen bindingProcathepsin LHomo sapiens (human)
cysteine-type peptidase activityProcathepsin LHomo sapiens (human)
histone bindingProcathepsin LHomo sapiens (human)
proteoglycan bindingProcathepsin LHomo sapiens (human)
serpin family protein bindingProcathepsin LHomo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic processProcathepsin LHomo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
arrestin family protein bindingMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
protein bindingIntegrin alpha-IIbHomo sapiens (human)
identical protein bindingIntegrin alpha-IIbHomo sapiens (human)
metal ion bindingIntegrin alpha-IIbHomo sapiens (human)
extracellular matrix bindingIntegrin alpha-IIbHomo sapiens (human)
molecular adaptor activityIntegrin alpha-IIbHomo sapiens (human)
fibrinogen bindingIntegrin alpha-IIbHomo sapiens (human)
integrin bindingIntegrin alpha-IIbHomo sapiens (human)
beta-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
beta1-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
protein bindingBeta-1 adrenergic receptorHomo sapiens (human)
PDZ domain bindingBeta-1 adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingBeta-1 adrenergic receptorHomo sapiens (human)
protein heterodimerization activityBeta-1 adrenergic receptorHomo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C delta typeRattus norvegicus (Norway rat)
arachidonate 5-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonate 12(S)-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
iron ion bindingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
protein bindingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
hydrolase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
RNA-dependent RNA polymerase activityReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
cysteine-type endopeptidase activityReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
K63-linked deubiquitinase activityReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
K48-linked deubiquitinase activityReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
3'-5'-RNA exonuclease activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
RNA-dependent RNA polymerase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
cysteine-type endopeptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
mRNA 5'-cap (guanine-N7-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
mRNA (nucleoside-2'-O-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
5'-3' RNA helicase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
K63-linked deubiquitinase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
K48-linked deubiquitinase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
G protein-coupled adenosine receptor activityAdenosine receptor A3Homo sapiens (human)
3'-5'-RNA exonuclease activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA-dependent RNA polymerase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
cysteine-type endopeptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA 5'-cap (guanine-N7-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA (nucleoside-2'-O-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA endonuclease activity, producing 3'-phosphomonoestersReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
ISG15-specific peptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
5'-3' RNA helicase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
protein guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificSteroid hormone receptor ERR1Homo sapiens (human)
DNA-binding transcription factor activitySteroid hormone receptor ERR1Homo sapiens (human)
nuclear steroid receptor activitySteroid hormone receptor ERR1Homo sapiens (human)
steroid bindingSteroid hormone receptor ERR1Homo sapiens (human)
protein bindingSteroid hormone receptor ERR1Homo sapiens (human)
zinc ion bindingSteroid hormone receptor ERR1Homo sapiens (human)
protein domain specific bindingSteroid hormone receptor ERR1Homo sapiens (human)
sequence-specific DNA bindingSteroid hormone receptor ERR1Homo sapiens (human)
sequence-specific double-stranded DNA bindingSteroid hormone receptor ERR1Homo sapiens (human)
estrogen response element bindingSteroid hormone receptor ERR1Homo sapiens (human)
nuclear receptor activitySteroid hormone receptor ERR1Homo sapiens (human)
norepinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
protein bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta3-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
beta-3 adrenergic receptor bindingBeta-3 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-3 adrenergic receptorHomo sapiens (human)
epinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
protein kinase activityProtein kinase C alpha typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C alpha typeHomo sapiens (human)
calcium,diacylglycerol-dependent serine/threonine kinase activityProtein kinase C alpha typeHomo sapiens (human)
integrin bindingProtein kinase C alpha typeHomo sapiens (human)
protein bindingProtein kinase C alpha typeHomo sapiens (human)
ATP bindingProtein kinase C alpha typeHomo sapiens (human)
zinc ion bindingProtein kinase C alpha typeHomo sapiens (human)
enzyme bindingProtein kinase C alpha typeHomo sapiens (human)
histone H3T6 kinase activityProtein kinase C alpha typeHomo sapiens (human)
protein serine kinase activityProtein kinase C alpha typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C alpha typeHomo sapiens (human)
diacylglycerol bindingProtein kinase C alpha typeHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
signaling receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
monooxygenase activityCytochrome P450 2B6Homo sapiens (human)
iron ion bindingCytochrome P450 2B6Homo sapiens (human)
testosterone 16-alpha-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
heme bindingCytochrome P450 2B6Homo sapiens (human)
testosterone 16-beta-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2B6Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2B6Homo sapiens (human)
tachykinin receptor activitySubstance-K receptorHomo sapiens (human)
protein bindingSubstance-K receptorHomo sapiens (human)
substance K receptor activitySubstance-K receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via GsD(1A) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(1A) dopamine receptorHomo sapiens (human)
protein bindingD(1A) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine bindingD(1A) dopamine receptorHomo sapiens (human)
arrestin family protein bindingD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(1A) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(4) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
protein bindingD(4) dopamine receptorHomo sapiens (human)
potassium channel regulator activityD(4) dopamine receptorHomo sapiens (human)
SH3 domain bindingD(4) dopamine receptorHomo sapiens (human)
dopamine bindingD(4) dopamine receptorHomo sapiens (human)
identical protein bindingD(4) dopamine receptorHomo sapiens (human)
metal ion bindingD(4) dopamine receptorHomo sapiens (human)
epinephrine bindingD(4) dopamine receptorHomo sapiens (human)
norepinephrine bindingD(4) dopamine receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityD(4) dopamine receptorHomo sapiens (human)
neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
serotonin bindingD(4) dopamine receptorHomo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A4Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A4Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 1Homo sapiens (human)
protein bindingProstaglandin G/H synthase 1Homo sapiens (human)
heme bindingProstaglandin G/H synthase 1Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 1Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 1Homo sapiens (human)
actin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
alpha-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
metal ion bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
beta-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monooxygenase activityThromboxane-A synthase Homo sapiens (human)
thromboxane-A synthase activityThromboxane-A synthase Homo sapiens (human)
iron ion bindingThromboxane-A synthase Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygenThromboxane-A synthase Homo sapiens (human)
heme bindingThromboxane-A synthase Homo sapiens (human)
12-hydroxyheptadecatrienoic acid synthase activityThromboxane-A synthase Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityThromboxane-A synthase Homo sapiens (human)
protein kinase activityProtein kinase C eta typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C eta typeHomo sapiens (human)
diacylglycerol-dependent, calcium-independent serine/threonine kinase activityProtein kinase C eta typeHomo sapiens (human)
protein bindingProtein kinase C eta typeHomo sapiens (human)
ATP bindingProtein kinase C eta typeHomo sapiens (human)
enzyme bindingProtein kinase C eta typeHomo sapiens (human)
small GTPase bindingProtein kinase C eta typeHomo sapiens (human)
metal ion bindingProtein kinase C eta typeHomo sapiens (human)
protein serine kinase activityProtein kinase C eta typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C eta typeHomo sapiens (human)
histamine receptor activityHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H2 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H2 receptorHomo sapiens (human)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
tachykinin receptor activitySubstance-P receptorHomo sapiens (human)
protein bindingSubstance-P receptorHomo sapiens (human)
substance P receptor activitySubstance-P receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2aHomo sapiens (human)
protein bindingAdenosine receptor A2aHomo sapiens (human)
calmodulin bindingAdenosine receptor A2aHomo sapiens (human)
lipid bindingAdenosine receptor A2aHomo sapiens (human)
enzyme bindingAdenosine receptor A2aHomo sapiens (human)
type 5 metabotropic glutamate receptor bindingAdenosine receptor A2aHomo sapiens (human)
identical protein bindingAdenosine receptor A2aHomo sapiens (human)
protein-containing complex bindingAdenosine receptor A2aHomo sapiens (human)
alpha-actinin bindingAdenosine receptor A2aHomo sapiens (human)
protease bindingB2 bradykinin receptorHomo sapiens (human)
phosphatidylinositol phospholipase C activityB2 bradykinin receptorHomo sapiens (human)
bradykinin receptor activityB2 bradykinin receptorHomo sapiens (human)
protein bindingB2 bradykinin receptorHomo sapiens (human)
type 1 angiotensin receptor bindingB2 bradykinin receptorHomo sapiens (human)
protein heterodimerization activityB2 bradykinin receptorHomo sapiens (human)
G protein-coupled receptor bindingAdenosine receptor A1Homo sapiens (human)
purine nucleoside bindingAdenosine receptor A1Homo sapiens (human)
protein bindingAdenosine receptor A1Homo sapiens (human)
heat shock protein bindingAdenosine receptor A1Homo sapiens (human)
G-protein beta/gamma-subunit complex bindingAdenosine receptor A1Homo sapiens (human)
heterotrimeric G-protein bindingAdenosine receptor A1Homo sapiens (human)
protein heterodimerization activityAdenosine receptor A1Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A1Homo sapiens (human)
integrin bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoatomic cation channel activitySodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
serotonin:sodium:chloride symporter activitySodium-dependent serotonin transporterHomo sapiens (human)
protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
antiporter activitySodium-dependent serotonin transporterHomo sapiens (human)
syntaxin-1 bindingSodium-dependent serotonin transporterHomo sapiens (human)
cocaine bindingSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion bindingSodium-dependent serotonin transporterHomo sapiens (human)
identical protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
nitric-oxide synthase bindingSodium-dependent serotonin transporterHomo sapiens (human)
actin filament bindingSodium-dependent serotonin transporterHomo sapiens (human)
serotonin bindingSodium-dependent serotonin transporterHomo sapiens (human)
melanocortin receptor activityMelanocortin receptor 4Homo sapiens (human)
melanocyte-stimulating hormone receptor activityMelanocortin receptor 4Homo sapiens (human)
protein bindingMelanocortin receptor 4Homo sapiens (human)
peptide hormone bindingMelanocortin receptor 4Homo sapiens (human)
ubiquitin protein ligase bindingMelanocortin receptor 4Homo sapiens (human)
neuropeptide bindingMelanocortin receptor 4Homo sapiens (human)
protein bindingMelanocortin receptor 5Homo sapiens (human)
hormone bindingMelanocortin receptor 5Homo sapiens (human)
melanocortin receptor activityMelanocortin receptor 5Homo sapiens (human)
G-protein alpha-subunit bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled receptor activityMu-type opioid receptorHomo sapiens (human)
beta-endorphin receptor activityMu-type opioid receptorHomo sapiens (human)
voltage-gated calcium channel activityMu-type opioid receptorHomo sapiens (human)
protein bindingMu-type opioid receptorHomo sapiens (human)
morphine receptor activityMu-type opioid receptorHomo sapiens (human)
G-protein beta-subunit bindingMu-type opioid receptorHomo sapiens (human)
neuropeptide bindingMu-type opioid receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(3) dopamine receptorHomo sapiens (human)
protein bindingD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(3) dopamine receptorHomo sapiens (human)
fatty acid bindingAlpha-synucleinHomo sapiens (human)
phospholipase D inhibitor activityAlpha-synucleinHomo sapiens (human)
SNARE bindingAlpha-synucleinHomo sapiens (human)
magnesium ion bindingAlpha-synucleinHomo sapiens (human)
transcription cis-regulatory region bindingAlpha-synucleinHomo sapiens (human)
actin bindingAlpha-synucleinHomo sapiens (human)
protein kinase inhibitor activityAlpha-synucleinHomo sapiens (human)
copper ion bindingAlpha-synucleinHomo sapiens (human)
calcium ion bindingAlpha-synucleinHomo sapiens (human)
protein bindingAlpha-synucleinHomo sapiens (human)
phospholipid bindingAlpha-synucleinHomo sapiens (human)
ferrous iron bindingAlpha-synucleinHomo sapiens (human)
zinc ion bindingAlpha-synucleinHomo sapiens (human)
lipid bindingAlpha-synucleinHomo sapiens (human)
oxidoreductase activityAlpha-synucleinHomo sapiens (human)
kinesin bindingAlpha-synucleinHomo sapiens (human)
Hsp70 protein bindingAlpha-synucleinHomo sapiens (human)
histone bindingAlpha-synucleinHomo sapiens (human)
identical protein bindingAlpha-synucleinHomo sapiens (human)
alpha-tubulin bindingAlpha-synucleinHomo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
tau protein bindingAlpha-synucleinHomo sapiens (human)
phosphoprotein bindingAlpha-synucleinHomo sapiens (human)
molecular adaptor activityAlpha-synucleinHomo sapiens (human)
dynein complex bindingAlpha-synucleinHomo sapiens (human)
cuprous ion bindingAlpha-synucleinHomo sapiens (human)
G protein-coupled opioid receptor activityDelta-type opioid receptorHomo sapiens (human)
protein bindingDelta-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled enkephalin receptor activityDelta-type opioid receptorHomo sapiens (human)
neuropeptide bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor activityKappa-type opioid receptorHomo sapiens (human)
protein bindingKappa-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingKappa-type opioid receptorHomo sapiens (human)
dynorphin receptor activityKappa-type opioid receptorHomo sapiens (human)
neuropeptide bindingKappa-type opioid receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase activityProtein kinase C iota typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C iota typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C iota typeHomo sapiens (human)
protein bindingProtein kinase C iota typeHomo sapiens (human)
ATP bindingProtein kinase C iota typeHomo sapiens (human)
phospholipid bindingProtein kinase C iota typeHomo sapiens (human)
metal ion bindingProtein kinase C iota typeHomo sapiens (human)
protein serine kinase activityProtein kinase C iota typeHomo sapiens (human)
melanocortin receptor activityMelanocortin receptor 3Homo sapiens (human)
melanocyte-stimulating hormone receptor activityMelanocortin receptor 3Homo sapiens (human)
protein bindingMelanocortin receptor 3Homo sapiens (human)
neuropeptide bindingMelanocortin receptor 3Homo sapiens (human)
peptide hormone bindingMelanocortin receptor 3Homo sapiens (human)
histamine receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 6Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificEstrogen-related receptor gammaHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificEstrogen-related receptor gammaHomo sapiens (human)
nuclear steroid receptor activityEstrogen-related receptor gammaHomo sapiens (human)
steroid bindingEstrogen-related receptor gammaHomo sapiens (human)
protein bindingEstrogen-related receptor gammaHomo sapiens (human)
zinc ion bindingEstrogen-related receptor gammaHomo sapiens (human)
AF-2 domain bindingEstrogen-related receptor gammaHomo sapiens (human)
sequence-specific double-stranded DNA bindingEstrogen-related receptor gammaHomo sapiens (human)
estrogen response element bindingEstrogen-related receptor gammaHomo sapiens (human)
nuclear receptor activityEstrogen-related receptor gammaHomo sapiens (human)
protease bindingSodium-dependent dopamine transporter Homo sapiens (human)
signaling receptor bindingSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
protein bindingSodium-dependent dopamine transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine bindingSodium-dependent dopamine transporter Homo sapiens (human)
amine bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein-containing complex bindingSodium-dependent dopamine transporter Homo sapiens (human)
metal ion bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein phosphatase 2A bindingSodium-dependent dopamine transporter Homo sapiens (human)
heterocyclic compound bindingSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
actin monomer bindingProtein kinase C epsilon typeHomo sapiens (human)
protein kinase activityProtein kinase C epsilon typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C epsilon typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C epsilon typeHomo sapiens (human)
diacylglycerol-dependent, calcium-independent serine/threonine kinase activityProtein kinase C epsilon typeHomo sapiens (human)
protein bindingProtein kinase C epsilon typeHomo sapiens (human)
ATP bindingProtein kinase C epsilon typeHomo sapiens (human)
enzyme activator activityProtein kinase C epsilon typeHomo sapiens (human)
enzyme bindingProtein kinase C epsilon typeHomo sapiens (human)
signaling receptor activator activityProtein kinase C epsilon typeHomo sapiens (human)
ethanol bindingProtein kinase C epsilon typeHomo sapiens (human)
metal ion bindingProtein kinase C epsilon typeHomo sapiens (human)
14-3-3 protein bindingProtein kinase C epsilon typeHomo sapiens (human)
protein serine kinase activityProtein kinase C epsilon typeHomo sapiens (human)
protein kinase activityProtein kinase C theta typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C theta typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C theta typeHomo sapiens (human)
protein bindingProtein kinase C theta typeHomo sapiens (human)
ATP bindingProtein kinase C theta typeHomo sapiens (human)
metal ion bindingProtein kinase C theta typeHomo sapiens (human)
protein serine kinase activityProtein kinase C theta typeHomo sapiens (human)
protein kinase activityProtein kinase C zeta typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C zeta typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C zeta typeHomo sapiens (human)
protein bindingProtein kinase C zeta typeHomo sapiens (human)
ATP bindingProtein kinase C zeta typeHomo sapiens (human)
potassium channel regulator activityProtein kinase C zeta typeHomo sapiens (human)
protein kinase bindingProtein kinase C zeta typeHomo sapiens (human)
phospholipase bindingProtein kinase C zeta typeHomo sapiens (human)
insulin receptor substrate bindingProtein kinase C zeta typeHomo sapiens (human)
protein-containing complex bindingProtein kinase C zeta typeHomo sapiens (human)
metal ion bindingProtein kinase C zeta typeHomo sapiens (human)
14-3-3 protein bindingProtein kinase C zeta typeHomo sapiens (human)
protein serine kinase activityProtein kinase C zeta typeHomo sapiens (human)
protein kinase activityProtein kinase C delta typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C delta typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C delta typeHomo sapiens (human)
diacylglycerol-dependent, calcium-independent serine/threonine kinase activityProtein kinase C delta typeHomo sapiens (human)
non-membrane spanning protein tyrosine kinase activityProtein kinase C delta typeHomo sapiens (human)
protein bindingProtein kinase C delta typeHomo sapiens (human)
ATP bindingProtein kinase C delta typeHomo sapiens (human)
enzyme activator activityProtein kinase C delta typeHomo sapiens (human)
enzyme bindingProtein kinase C delta typeHomo sapiens (human)
protein kinase bindingProtein kinase C delta typeHomo sapiens (human)
insulin receptor substrate bindingProtein kinase C delta typeHomo sapiens (human)
metal ion bindingProtein kinase C delta typeHomo sapiens (human)
protein serine kinase activityProtein kinase C delta typeHomo sapiens (human)
protein serine/threonine phosphatase activitySerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
calcium ion bindingSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
protein bindingSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
calmodulin bindingSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
cyclosporin A bindingSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
myosin phosphatase activitySerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
enzyme bindingSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
calmodulin-dependent protein phosphatase activitySerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
protein-containing complex bindingSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
protein dimerization activitySerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
ATPase bindingSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
1-alkyl-2-acetylglycerophosphocholine esterase activityPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
phospholipid bindingPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
hydrolase activity, acting on ester bondsPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
calcium-independent phospholipase A2 activityPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
phospholipase D activityPhospholipase D1Homo sapiens (human)
protein bindingPhospholipase D1Homo sapiens (human)
phosphatidylinositol bindingPhospholipase D1Homo sapiens (human)
N-acylphosphatidylethanolamine-specific phospholipase D activityPhospholipase D1Homo sapiens (human)
C-8 sterol isomerase activity3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
steroid delta-isomerase activity3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
protein binding3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
identical protein binding3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
cholestenol delta-isomerase activity3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase D1Homo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activitySerine/threonine-protein kinase D1Homo sapiens (human)
protein kinase C bindingSerine/threonine-protein kinase D1Homo sapiens (human)
protein bindingSerine/threonine-protein kinase D1Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase D1Homo sapiens (human)
kinase activitySerine/threonine-protein kinase D1Homo sapiens (human)
heat shock protein bindingSerine/threonine-protein kinase D1Homo sapiens (human)
identical protein bindingSerine/threonine-protein kinase D1Homo sapiens (human)
metal ion bindingSerine/threonine-protein kinase D1Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase D1Homo sapiens (human)
phosphatidylinositol 3-kinase activator activitySerine/threonine-protein kinase D1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingEstrogen receptor betaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificEstrogen receptor betaHomo sapiens (human)
DNA bindingEstrogen receptor betaHomo sapiens (human)
nuclear steroid receptor activityEstrogen receptor betaHomo sapiens (human)
nuclear receptor activityEstrogen receptor betaHomo sapiens (human)
steroid bindingEstrogen receptor betaHomo sapiens (human)
protein bindingEstrogen receptor betaHomo sapiens (human)
zinc ion bindingEstrogen receptor betaHomo sapiens (human)
enzyme bindingEstrogen receptor betaHomo sapiens (human)
nuclear estrogen receptor activityEstrogen receptor betaHomo sapiens (human)
estrogen response element bindingEstrogen receptor betaHomo sapiens (human)
receptor antagonist activityEstrogen receptor betaHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
cholestenol delta-isomerase activityEmopamil-binding protein-likeHomo sapiens (human)
virus receptor activityAngiotensin-converting enzyme 2 Homo sapiens (human)
endopeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
carboxypeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
metallocarboxypeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
protein bindingAngiotensin-converting enzyme 2 Homo sapiens (human)
metallopeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
peptidyl-dipeptidase activityAngiotensin-converting enzyme 2 Homo sapiens (human)
zinc ion bindingAngiotensin-converting enzyme 2 Homo sapiens (human)
identical protein bindingAngiotensin-converting enzyme 2 Homo sapiens (human)
protein binding7-dehydrocholesterol reductaseHomo sapiens (human)
7-dehydrocholesterol reductase activity7-dehydrocholesterol reductaseHomo sapiens (human)
NADP binding7-dehydrocholesterol reductaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (210)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular regionTransmembrane protease serine 2Homo sapiens (human)
nucleoplasmTransmembrane protease serine 2Homo sapiens (human)
plasma membraneTransmembrane protease serine 2Homo sapiens (human)
extracellular exosomeTransmembrane protease serine 2Homo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
nucleoplasmSerine/threonine-protein kinase D3Homo sapiens (human)
cytosolSerine/threonine-protein kinase D3Homo sapiens (human)
plasma membraneSerine/threonine-protein kinase D3Homo sapiens (human)
cytosolSerine/threonine-protein kinase D3Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
endosomeEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
ruffle membraneEpidermal growth factor receptorHomo sapiens (human)
Golgi membraneEpidermal growth factor receptorHomo sapiens (human)
extracellular spaceEpidermal growth factor receptorHomo sapiens (human)
nucleusEpidermal growth factor receptorHomo sapiens (human)
cytoplasmEpidermal growth factor receptorHomo sapiens (human)
endosomeEpidermal growth factor receptorHomo sapiens (human)
endoplasmic reticulum membraneEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
focal adhesionEpidermal growth factor receptorHomo sapiens (human)
cell surfaceEpidermal growth factor receptorHomo sapiens (human)
endosome membraneEpidermal growth factor receptorHomo sapiens (human)
membraneEpidermal growth factor receptorHomo sapiens (human)
basolateral plasma membraneEpidermal growth factor receptorHomo sapiens (human)
apical plasma membraneEpidermal growth factor receptorHomo sapiens (human)
cell junctionEpidermal growth factor receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneEpidermal growth factor receptorHomo sapiens (human)
early endosome membraneEpidermal growth factor receptorHomo sapiens (human)
nuclear membraneEpidermal growth factor receptorHomo sapiens (human)
membrane raftEpidermal growth factor receptorHomo sapiens (human)
perinuclear region of cytoplasmEpidermal growth factor receptorHomo sapiens (human)
multivesicular body, internal vesicle lumenEpidermal growth factor receptorHomo sapiens (human)
intracellular vesicleEpidermal growth factor receptorHomo sapiens (human)
protein-containing complexEpidermal growth factor receptorHomo sapiens (human)
receptor complexEpidermal growth factor receptorHomo sapiens (human)
Shc-EGFR complexEpidermal growth factor receptorHomo sapiens (human)
basal plasma membraneEpidermal growth factor receptorHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
nucleusEstrogen receptorHomo sapiens (human)
nucleoplasmEstrogen receptorHomo sapiens (human)
transcription regulator complexEstrogen receptorHomo sapiens (human)
cytoplasmEstrogen receptorHomo sapiens (human)
Golgi apparatusEstrogen receptorHomo sapiens (human)
cytosolEstrogen receptorHomo sapiens (human)
plasma membraneEstrogen receptorHomo sapiens (human)
membraneEstrogen receptorHomo sapiens (human)
chromatinEstrogen receptorHomo sapiens (human)
euchromatinEstrogen receptorHomo sapiens (human)
protein-containing complexEstrogen receptorHomo sapiens (human)
nucleusEstrogen receptorHomo sapiens (human)
lysosomeLysosomal acid glucosylceramidaseHomo sapiens (human)
lysosomal membraneLysosomal acid glucosylceramidaseHomo sapiens (human)
endoplasmic reticulumLysosomal acid glucosylceramidaseHomo sapiens (human)
Golgi apparatusLysosomal acid glucosylceramidaseHomo sapiens (human)
trans-Golgi networkLysosomal acid glucosylceramidaseHomo sapiens (human)
lysosomal lumenLysosomal acid glucosylceramidaseHomo sapiens (human)
extracellular exosomeLysosomal acid glucosylceramidaseHomo sapiens (human)
semaphorin receptor complexReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
nucleusReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
nucleoplasmReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
early endosomeReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
cytosolReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
plasma membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
endosome membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
basolateral plasma membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
apical plasma membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
neuromuscular junctionReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
ruffle membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
presynaptic membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
myelin sheathReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
perinuclear region of cytoplasmReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
ERBB3:ERBB2 complexReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
receptor complexReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
plasma membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
basal plasma membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
glutamatergic synapseIntegrin beta-3Homo sapiens (human)
nucleusIntegrin beta-3Homo sapiens (human)
nucleoplasmIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin beta-3Homo sapiens (human)
cell-cell junctionIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
external side of plasma membraneIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
apical plasma membraneIntegrin beta-3Homo sapiens (human)
platelet alpha granule membraneIntegrin beta-3Homo sapiens (human)
lamellipodium membraneIntegrin beta-3Homo sapiens (human)
filopodium membraneIntegrin beta-3Homo sapiens (human)
microvillus membraneIntegrin beta-3Homo sapiens (human)
ruffle membraneIntegrin beta-3Homo sapiens (human)
integrin alphav-beta3 complexIntegrin beta-3Homo sapiens (human)
melanosomeIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
postsynaptic membraneIntegrin beta-3Homo sapiens (human)
extracellular exosomeIntegrin beta-3Homo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin beta-3Homo sapiens (human)
glycinergic synapseIntegrin beta-3Homo sapiens (human)
integrin complexIntegrin beta-3Homo sapiens (human)
protein-containing complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-PKCalpha complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-IGF-1-IGF1R complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-HMGB1 complexIntegrin beta-3Homo sapiens (human)
receptor complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-vitronectin complexIntegrin beta-3Homo sapiens (human)
alpha9-beta1 integrin-ADAM8 complexIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
nucleusProtein kinase C gamma typeHomo sapiens (human)
cytosolProtein kinase C gamma typeHomo sapiens (human)
plasma membraneProtein kinase C gamma typeHomo sapiens (human)
cell-cell junctionProtein kinase C gamma typeHomo sapiens (human)
postsynaptic densityProtein kinase C gamma typeHomo sapiens (human)
dendriteProtein kinase C gamma typeHomo sapiens (human)
calyx of HeldProtein kinase C gamma typeHomo sapiens (human)
perinuclear region of cytoplasmProtein kinase C gamma typeHomo sapiens (human)
synaptic membraneProtein kinase C gamma typeHomo sapiens (human)
presynaptic cytosolProtein kinase C gamma typeHomo sapiens (human)
postsynaptic cytosolProtein kinase C gamma typeHomo sapiens (human)
nucleusProtein kinase C beta typeHomo sapiens (human)
nucleoplasmProtein kinase C beta typeHomo sapiens (human)
cytoplasmProtein kinase C beta typeHomo sapiens (human)
centrosomeProtein kinase C beta typeHomo sapiens (human)
cytosolProtein kinase C beta typeHomo sapiens (human)
plasma membraneProtein kinase C beta typeHomo sapiens (human)
brush border membraneProtein kinase C beta typeHomo sapiens (human)
calyx of HeldProtein kinase C beta typeHomo sapiens (human)
extracellular exosomeProtein kinase C beta typeHomo sapiens (human)
presynaptic cytosolProtein kinase C beta typeHomo sapiens (human)
spectrinProtein kinase C beta typeHomo sapiens (human)
pericentriolar materialTyrosine-protein kinase LckHomo sapiens (human)
immunological synapseTyrosine-protein kinase LckHomo sapiens (human)
cytosolTyrosine-protein kinase LckHomo sapiens (human)
plasma membraneTyrosine-protein kinase LckHomo sapiens (human)
membrane raftTyrosine-protein kinase LckHomo sapiens (human)
extracellular exosomeTyrosine-protein kinase LckHomo sapiens (human)
plasma membraneTyrosine-protein kinase LckHomo sapiens (human)
membrane raftTyrosine-protein kinase FynHomo sapiens (human)
dendriteTyrosine-protein kinase FynHomo sapiens (human)
nucleusTyrosine-protein kinase FynHomo sapiens (human)
mitochondrionTyrosine-protein kinase FynHomo sapiens (human)
endosomeTyrosine-protein kinase FynHomo sapiens (human)
cytosolTyrosine-protein kinase FynHomo sapiens (human)
actin filamentTyrosine-protein kinase FynHomo sapiens (human)
plasma membraneTyrosine-protein kinase FynHomo sapiens (human)
postsynaptic densityTyrosine-protein kinase FynHomo sapiens (human)
dendriteTyrosine-protein kinase FynHomo sapiens (human)
perikaryonTyrosine-protein kinase FynHomo sapiens (human)
cell bodyTyrosine-protein kinase FynHomo sapiens (human)
membrane raftTyrosine-protein kinase FynHomo sapiens (human)
perinuclear region of cytoplasmTyrosine-protein kinase FynHomo sapiens (human)
perinuclear endoplasmic reticulumTyrosine-protein kinase FynHomo sapiens (human)
glial cell projectionTyrosine-protein kinase FynHomo sapiens (human)
Schaffer collateral - CA1 synapseTyrosine-protein kinase FynHomo sapiens (human)
plasma membraneTyrosine-protein kinase FynHomo sapiens (human)
plasma membraneProgesterone receptorHomo sapiens (human)
nucleoplasmProgesterone receptorHomo sapiens (human)
mitochondrial outer membraneProgesterone receptorHomo sapiens (human)
cytosolProgesterone receptorHomo sapiens (human)
chromatinProgesterone receptorHomo sapiens (human)
nucleusProgesterone receptorHomo sapiens (human)
extracellular regionProcathepsin LHomo sapiens (human)
extracellular spaceProcathepsin LHomo sapiens (human)
nucleusProcathepsin LHomo sapiens (human)
lysosomeProcathepsin LHomo sapiens (human)
multivesicular bodyProcathepsin LHomo sapiens (human)
Golgi apparatusProcathepsin LHomo sapiens (human)
plasma membraneProcathepsin LHomo sapiens (human)
apical plasma membraneProcathepsin LHomo sapiens (human)
endolysosome lumenProcathepsin LHomo sapiens (human)
chromaffin granuleProcathepsin LHomo sapiens (human)
lysosomal lumenProcathepsin LHomo sapiens (human)
intracellular membrane-bounded organelleProcathepsin LHomo sapiens (human)
collagen-containing extracellular matrixProcathepsin LHomo sapiens (human)
extracellular exosomeProcathepsin LHomo sapiens (human)
endocytic vesicle lumenProcathepsin LHomo sapiens (human)
extracellular spaceProcathepsin LHomo sapiens (human)
lysosomeProcathepsin LHomo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
clathrin-coated endocytic vesicle membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
asymmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
symmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
neuronal cell bodyMuscarinic acetylcholine receptor M2Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M2Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M4Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M4Homo sapiens (human)
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneIntegrin alpha-IIbHomo sapiens (human)
focal adhesionIntegrin alpha-IIbHomo sapiens (human)
cell surfaceIntegrin alpha-IIbHomo sapiens (human)
platelet alpha granule membraneIntegrin alpha-IIbHomo sapiens (human)
extracellular exosomeIntegrin alpha-IIbHomo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin alpha-IIbHomo sapiens (human)
blood microparticleIntegrin alpha-IIbHomo sapiens (human)
integrin complexIntegrin alpha-IIbHomo sapiens (human)
external side of plasma membraneIntegrin alpha-IIbHomo sapiens (human)
early endosomeBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
Schaffer collateral - CA1 synapseBeta-1 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M5Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M5Homo sapiens (human)
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
cytosolProtein kinase C delta typeRattus norvegicus (Norway rat)
cytosolProtein kinase C zeta typeRattus norvegicus (Norway rat)
extracellular regionPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
extracellular spacePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelopePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelope lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nucleoplasmPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
cytosolPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear matrixPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear membranePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
secretory granule lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
perinuclear region of cytoplasmPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
ficolin-1-rich granule lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelopePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
double membrane vesicle viral factory outer membraneReplicase polyprotein 1aSevere acute respiratory syndrome-related coronavirus
double membrane vesicle viral factory outer membraneReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
plasma membraneAdenosine receptor A3Homo sapiens (human)
presynaptic membraneAdenosine receptor A3Homo sapiens (human)
Schaffer collateral - CA1 synapseAdenosine receptor A3Homo sapiens (human)
dendriteAdenosine receptor A3Homo sapiens (human)
plasma membraneAdenosine receptor A3Homo sapiens (human)
synapseAdenosine receptor A3Homo sapiens (human)
double membrane vesicle viral factory outer membraneReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M1Homo sapiens (human)
Schaffer collateral - CA1 synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic density membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M1Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
fibrillar centerSteroid hormone receptor ERR1Homo sapiens (human)
nucleusSteroid hormone receptor ERR1Homo sapiens (human)
nucleoplasmSteroid hormone receptor ERR1Homo sapiens (human)
cytoplasmSteroid hormone receptor ERR1Homo sapiens (human)
microtubule cytoskeletonSteroid hormone receptor ERR1Homo sapiens (human)
intercellular bridgeSteroid hormone receptor ERR1Homo sapiens (human)
chromatinSteroid hormone receptor ERR1Homo sapiens (human)
nucleusSteroid hormone receptor ERR1Homo sapiens (human)
plasma membraneBeta-3 adrenergic receptorHomo sapiens (human)
receptor complexBeta-3 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-3 adrenergic receptorHomo sapiens (human)
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliary basal bodyProtein kinase C alpha typeHomo sapiens (human)
nucleoplasmProtein kinase C alpha typeHomo sapiens (human)
cytoplasmProtein kinase C alpha typeHomo sapiens (human)
mitochondrionProtein kinase C alpha typeHomo sapiens (human)
endoplasmic reticulumProtein kinase C alpha typeHomo sapiens (human)
cytosolProtein kinase C alpha typeHomo sapiens (human)
plasma membraneProtein kinase C alpha typeHomo sapiens (human)
mitochondrial membraneProtein kinase C alpha typeHomo sapiens (human)
perinuclear region of cytoplasmProtein kinase C alpha typeHomo sapiens (human)
extracellular exosomeProtein kinase C alpha typeHomo sapiens (human)
alphav-beta3 integrin-PKCalpha complexProtein kinase C alpha typeHomo sapiens (human)
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basal plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basolateral plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M3Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2B6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2B6Homo sapiens (human)
cytoplasmCytochrome P450 2B6Homo sapiens (human)
plasma membraneSubstance-K receptorHomo sapiens (human)
sperm flagellumSubstance-K receptorHomo sapiens (human)
sperm headSubstance-K receptorHomo sapiens (human)
sperm midpieceSubstance-K receptorHomo sapiens (human)
sperm midpieceSubstance-K receptorHomo sapiens (human)
plasma membraneSubstance-K receptorHomo sapiens (human)
nucleusD(1A) dopamine receptorHomo sapiens (human)
endoplasmic reticulum membraneD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
ciliumD(1A) dopamine receptorHomo sapiens (human)
presynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
dendritic spineD(1A) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
ciliary membraneD(1A) dopamine receptorHomo sapiens (human)
non-motile ciliumD(1A) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(1A) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
centrosomeD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
membraneD(4) dopamine receptorHomo sapiens (human)
postsynapseD(4) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
dendriteD(4) dopamine receptorHomo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A4Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A4Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A4Homo sapiens (human)
photoreceptor outer segmentProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 1Homo sapiens (human)
Golgi apparatusProstaglandin G/H synthase 1Homo sapiens (human)
intracellular membrane-bounded organelleProstaglandin G/H synthase 1Homo sapiens (human)
extracellular exosomeProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 1Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
cell surfaceSodium-dependent noradrenaline transporter Homo sapiens (human)
membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
presynaptic membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
axonSodium-dependent noradrenaline transporter Homo sapiens (human)
endoplasmic reticulumThromboxane-A synthase Homo sapiens (human)
endoplasmic reticulum membraneThromboxane-A synthase Homo sapiens (human)
cytosolThromboxane-A synthase Homo sapiens (human)
cytoplasmProtein kinase C eta typeHomo sapiens (human)
cytosolProtein kinase C eta typeHomo sapiens (human)
plasma membraneProtein kinase C eta typeHomo sapiens (human)
cell-cell junctionProtein kinase C eta typeHomo sapiens (human)
extracellular exosomeProtein kinase C eta typeHomo sapiens (human)
plasma membraneHistamine H2 receptorHomo sapiens (human)
synapseHistamine H2 receptorHomo sapiens (human)
plasma membraneHistamine H2 receptorHomo sapiens (human)
dendriteHistamine H2 receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneSubstance-P receptorHomo sapiens (human)
cell surfaceSubstance-P receptorHomo sapiens (human)
dendriteSubstance-P receptorHomo sapiens (human)
sperm flagellumSubstance-P receptorHomo sapiens (human)
cell bodySubstance-P receptorHomo sapiens (human)
sperm headSubstance-P receptorHomo sapiens (human)
sperm midpieceSubstance-P receptorHomo sapiens (human)
plasma membraneSubstance-P receptorHomo sapiens (human)
sperm midpieceSubstance-P receptorHomo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membraneAdenosine receptor A2aHomo sapiens (human)
intermediate filamentAdenosine receptor A2aHomo sapiens (human)
plasma membraneAdenosine receptor A2aHomo sapiens (human)
membraneAdenosine receptor A2aHomo sapiens (human)
dendriteAdenosine receptor A2aHomo sapiens (human)
axolemmaAdenosine receptor A2aHomo sapiens (human)
asymmetric synapseAdenosine receptor A2aHomo sapiens (human)
presynaptic membraneAdenosine receptor A2aHomo sapiens (human)
neuronal cell bodyAdenosine receptor A2aHomo sapiens (human)
postsynaptic membraneAdenosine receptor A2aHomo sapiens (human)
presynaptic active zoneAdenosine receptor A2aHomo sapiens (human)
glutamatergic synapseAdenosine receptor A2aHomo sapiens (human)
endosomeB2 bradykinin receptorHomo sapiens (human)
Golgi apparatusB2 bradykinin receptorHomo sapiens (human)
plasma membraneB2 bradykinin receptorHomo sapiens (human)
intracellular membrane-bounded organelleB2 bradykinin receptorHomo sapiens (human)
plasma membraneB2 bradykinin receptorHomo sapiens (human)
plasma membraneAdenosine receptor A1Homo sapiens (human)
plasma membraneAdenosine receptor A1Homo sapiens (human)
basolateral plasma membraneAdenosine receptor A1Homo sapiens (human)
axolemmaAdenosine receptor A1Homo sapiens (human)
asymmetric synapseAdenosine receptor A1Homo sapiens (human)
presynaptic membraneAdenosine receptor A1Homo sapiens (human)
neuronal cell bodyAdenosine receptor A1Homo sapiens (human)
terminal boutonAdenosine receptor A1Homo sapiens (human)
dendritic spineAdenosine receptor A1Homo sapiens (human)
calyx of HeldAdenosine receptor A1Homo sapiens (human)
postsynaptic membraneAdenosine receptor A1Homo sapiens (human)
presynaptic active zoneAdenosine receptor A1Homo sapiens (human)
synapseAdenosine receptor A1Homo sapiens (human)
dendriteAdenosine receptor A1Homo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
focal adhesionSodium-dependent serotonin transporterHomo sapiens (human)
endosome membraneSodium-dependent serotonin transporterHomo sapiens (human)
endomembrane systemSodium-dependent serotonin transporterHomo sapiens (human)
presynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
membrane raftSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
postsynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
serotonergic synapseSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
neuron projectionSodium-dependent serotonin transporterHomo sapiens (human)
plasma membraneMelanocortin receptor 4Homo sapiens (human)
membraneMelanocortin receptor 4Homo sapiens (human)
plasma membraneMelanocortin receptor 4Homo sapiens (human)
cytoplasmMelanocortin receptor 4Homo sapiens (human)
plasma membraneMelanocortin receptor 5Homo sapiens (human)
plasma membraneMelanocortin receptor 5Homo sapiens (human)
cytoplasmMelanocortin receptor 5Homo sapiens (human)
endosomeMu-type opioid receptorHomo sapiens (human)
endoplasmic reticulumMu-type opioid receptorHomo sapiens (human)
Golgi apparatusMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
axonMu-type opioid receptorHomo sapiens (human)
dendriteMu-type opioid receptorHomo sapiens (human)
perikaryonMu-type opioid receptorHomo sapiens (human)
synapseMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
neuron projectionMu-type opioid receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
synapseD(3) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
platelet alpha granule membraneAlpha-synucleinHomo sapiens (human)
extracellular regionAlpha-synucleinHomo sapiens (human)
extracellular spaceAlpha-synucleinHomo sapiens (human)
nucleusAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
mitochondrionAlpha-synucleinHomo sapiens (human)
lysosomeAlpha-synucleinHomo sapiens (human)
cytosolAlpha-synucleinHomo sapiens (human)
plasma membraneAlpha-synucleinHomo sapiens (human)
cell cortexAlpha-synucleinHomo sapiens (human)
actin cytoskeletonAlpha-synucleinHomo sapiens (human)
membraneAlpha-synucleinHomo sapiens (human)
inclusion bodyAlpha-synucleinHomo sapiens (human)
axonAlpha-synucleinHomo sapiens (human)
growth coneAlpha-synucleinHomo sapiens (human)
synaptic vesicle membraneAlpha-synucleinHomo sapiens (human)
perinuclear region of cytoplasmAlpha-synucleinHomo sapiens (human)
postsynapseAlpha-synucleinHomo sapiens (human)
supramolecular fiberAlpha-synucleinHomo sapiens (human)
protein-containing complexAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
axon terminusAlpha-synucleinHomo sapiens (human)
neuronal cell bodyAlpha-synucleinHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneDelta-type opioid receptorHomo sapiens (human)
dendrite membraneDelta-type opioid receptorHomo sapiens (human)
presynaptic membraneDelta-type opioid receptorHomo sapiens (human)
axon terminusDelta-type opioid receptorHomo sapiens (human)
spine apparatusDelta-type opioid receptorHomo sapiens (human)
postsynaptic density membraneDelta-type opioid receptorHomo sapiens (human)
neuronal dense core vesicleDelta-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
neuron projectionDelta-type opioid receptorHomo sapiens (human)
nucleoplasmKappa-type opioid receptorHomo sapiens (human)
mitochondrionKappa-type opioid receptorHomo sapiens (human)
cytosolKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
membraneKappa-type opioid receptorHomo sapiens (human)
sarcoplasmic reticulumKappa-type opioid receptorHomo sapiens (human)
T-tubuleKappa-type opioid receptorHomo sapiens (human)
dendriteKappa-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneKappa-type opioid receptorHomo sapiens (human)
presynaptic membraneKappa-type opioid receptorHomo sapiens (human)
perikaryonKappa-type opioid receptorHomo sapiens (human)
axon terminusKappa-type opioid receptorHomo sapiens (human)
postsynaptic membraneKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
neuron projectionKappa-type opioid receptorHomo sapiens (human)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
Golgi membraneProtein kinase C iota typeHomo sapiens (human)
nucleusProtein kinase C iota typeHomo sapiens (human)
nucleoplasmProtein kinase C iota typeHomo sapiens (human)
endosomeProtein kinase C iota typeHomo sapiens (human)
cytosolProtein kinase C iota typeHomo sapiens (human)
plasma membraneProtein kinase C iota typeHomo sapiens (human)
brush borderProtein kinase C iota typeHomo sapiens (human)
bicellular tight junctionProtein kinase C iota typeHomo sapiens (human)
microtubule cytoskeletonProtein kinase C iota typeHomo sapiens (human)
apical plasma membraneProtein kinase C iota typeHomo sapiens (human)
cell leading edgeProtein kinase C iota typeHomo sapiens (human)
Schmidt-Lanterman incisureProtein kinase C iota typeHomo sapiens (human)
intercellular bridgeProtein kinase C iota typeHomo sapiens (human)
extracellular exosomeProtein kinase C iota typeHomo sapiens (human)
tight junctionProtein kinase C iota typeHomo sapiens (human)
Schaffer collateral - CA1 synapseProtein kinase C iota typeHomo sapiens (human)
glutamatergic synapseProtein kinase C iota typeHomo sapiens (human)
PAR polarity complexProtein kinase C iota typeHomo sapiens (human)
plasma membraneMelanocortin receptor 3Homo sapiens (human)
cytoplasmMelanocortin receptor 3Homo sapiens (human)
plasma membraneMelanocortin receptor 3Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
cilium5-hydroxytryptamine receptor 6Homo sapiens (human)
synapse5-hydroxytryptamine receptor 6Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 6Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
nucleoplasmEstrogen-related receptor gammaHomo sapiens (human)
chromatinEstrogen-related receptor gammaHomo sapiens (human)
nucleusEstrogen-related receptor gammaHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
cytoplasmSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
cell surfaceSodium-dependent dopamine transporter Homo sapiens (human)
membraneSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
neuron projectionSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell bodySodium-dependent dopamine transporter Homo sapiens (human)
axon terminusSodium-dependent dopamine transporter Homo sapiens (human)
membrane raftSodium-dependent dopamine transporter Homo sapiens (human)
postsynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
dopaminergic synapseSodium-dependent dopamine transporter Homo sapiens (human)
flotillin complexSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
presynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent dopamine transporter Homo sapiens (human)
Golgi apparatusProtein kinase C epsilon typeHomo sapiens (human)
nucleusProtein kinase C epsilon typeHomo sapiens (human)
cytoplasmProtein kinase C epsilon typeHomo sapiens (human)
mitochondrionProtein kinase C epsilon typeHomo sapiens (human)
endoplasmic reticulumProtein kinase C epsilon typeHomo sapiens (human)
cytosolProtein kinase C epsilon typeHomo sapiens (human)
plasma membraneProtein kinase C epsilon typeHomo sapiens (human)
intracellular membrane-bounded organelleProtein kinase C epsilon typeHomo sapiens (human)
intermediate filament cytoskeletonProtein kinase C epsilon typeHomo sapiens (human)
synapseProtein kinase C epsilon typeHomo sapiens (human)
perinuclear region of cytoplasmProtein kinase C epsilon typeHomo sapiens (human)
cell peripheryProtein kinase C epsilon typeHomo sapiens (human)
immunological synapseProtein kinase C theta typeHomo sapiens (human)
cytosolProtein kinase C theta typeHomo sapiens (human)
plasma membraneProtein kinase C theta typeHomo sapiens (human)
aggresomeProtein kinase C theta typeHomo sapiens (human)
centriolar satelliteProtein kinase C theta typeHomo sapiens (human)
stress fiberProtein kinase C zeta typeHomo sapiens (human)
nuclear envelopeProtein kinase C zeta typeHomo sapiens (human)
cytoplasmProtein kinase C zeta typeHomo sapiens (human)
endosomeProtein kinase C zeta typeHomo sapiens (human)
microtubule organizing centerProtein kinase C zeta typeHomo sapiens (human)
cytosolProtein kinase C zeta typeHomo sapiens (human)
plasma membraneProtein kinase C zeta typeHomo sapiens (human)
cell-cell junctionProtein kinase C zeta typeHomo sapiens (human)
bicellular tight junctionProtein kinase C zeta typeHomo sapiens (human)
postsynaptic densityProtein kinase C zeta typeHomo sapiens (human)
membraneProtein kinase C zeta typeHomo sapiens (human)
apical plasma membraneProtein kinase C zeta typeHomo sapiens (human)
nuclear matrixProtein kinase C zeta typeHomo sapiens (human)
cell junctionProtein kinase C zeta typeHomo sapiens (human)
cell leading edgeProtein kinase C zeta typeHomo sapiens (human)
vesicleProtein kinase C zeta typeHomo sapiens (human)
myelin sheath abaxonal regionProtein kinase C zeta typeHomo sapiens (human)
axon hillockProtein kinase C zeta typeHomo sapiens (human)
apical cortexProtein kinase C zeta typeHomo sapiens (human)
perinuclear region of cytoplasmProtein kinase C zeta typeHomo sapiens (human)
extracellular exosomeProtein kinase C zeta typeHomo sapiens (human)
tight junctionProtein kinase C zeta typeHomo sapiens (human)
Schaffer collateral - CA1 synapseProtein kinase C zeta typeHomo sapiens (human)
glutamatergic synapseProtein kinase C zeta typeHomo sapiens (human)
PAR polarity complexProtein kinase C zeta typeHomo sapiens (human)
extracellular regionProtein kinase C delta typeHomo sapiens (human)
nucleusProtein kinase C delta typeHomo sapiens (human)
nucleoplasmProtein kinase C delta typeHomo sapiens (human)
cytoplasmProtein kinase C delta typeHomo sapiens (human)
mitochondrionProtein kinase C delta typeHomo sapiens (human)
endoplasmic reticulumProtein kinase C delta typeHomo sapiens (human)
cytosolProtein kinase C delta typeHomo sapiens (human)
plasma membraneProtein kinase C delta typeHomo sapiens (human)
cell-cell junctionProtein kinase C delta typeHomo sapiens (human)
nuclear matrixProtein kinase C delta typeHomo sapiens (human)
azurophil granule lumenProtein kinase C delta typeHomo sapiens (human)
endolysosomeProtein kinase C delta typeHomo sapiens (human)
perinuclear region of cytoplasmProtein kinase C delta typeHomo sapiens (human)
extracellular exosomeProtein kinase C delta typeHomo sapiens (human)
cytoplasmic side of plasma membraneSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
nucleoplasmSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
cytoplasmSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
mitochondrionSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
cytosolSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
plasma membraneSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
calcineurin complexSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
protein serine/threonine phosphatase complexSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
extrinsic component of plasma membraneSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
Z discSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
slit diaphragmSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
sarcolemmaSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
dendritic spineSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
Schaffer collateral - CA1 synapseSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
glutamatergic synapseSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
cytosolSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
cytoplasmSerine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
extracellular regionPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
low-density lipoprotein particlePlatelet-activating factor acetylhydrolaseHomo sapiens (human)
high-density lipoprotein particlePlatelet-activating factor acetylhydrolaseHomo sapiens (human)
cholinergic synapsePhospholipase D1Homo sapiens (human)
Golgi membranePhospholipase D1Homo sapiens (human)
lysosomal membranePhospholipase D1Homo sapiens (human)
endosomePhospholipase D1Homo sapiens (human)
endoplasmic reticulum membranePhospholipase D1Homo sapiens (human)
Golgi apparatusPhospholipase D1Homo sapiens (human)
plasma membranePhospholipase D1Homo sapiens (human)
membranePhospholipase D1Homo sapiens (human)
apical plasma membranePhospholipase D1Homo sapiens (human)
endocytic vesiclePhospholipase D1Homo sapiens (human)
late endosome membranePhospholipase D1Homo sapiens (human)
specific granule membranePhospholipase D1Homo sapiens (human)
perinuclear region of cytoplasmPhospholipase D1Homo sapiens (human)
tertiary granule membranePhospholipase D1Homo sapiens (human)
intracellular membrane-bounded organellePhospholipase D1Homo sapiens (human)
plasma membrane regionPhospholipase D1Homo sapiens (human)
nuclear envelope3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
endoplasmic reticulum3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
endoplasmic reticulum membrane3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
cytoplasmic vesicle3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
nuclear membrane3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
endoplasmic reticulum3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
autophagosome membraneSerine/threonine-protein kinase D1Homo sapiens (human)
nucleusSerine/threonine-protein kinase D1Homo sapiens (human)
trans-Golgi networkSerine/threonine-protein kinase D1Homo sapiens (human)
cytosolSerine/threonine-protein kinase D1Homo sapiens (human)
plasma membraneSerine/threonine-protein kinase D1Homo sapiens (human)
cell-cell junctionSerine/threonine-protein kinase D1Homo sapiens (human)
cell cortexSerine/threonine-protein kinase D1Homo sapiens (human)
Z discSerine/threonine-protein kinase D1Homo sapiens (human)
perinuclear region of cytoplasmSerine/threonine-protein kinase D1Homo sapiens (human)
Golgi apparatusSerine/threonine-protein kinase D1Homo sapiens (human)
cytosolSerine/threonine-protein kinase D1Homo sapiens (human)
nucleusEstrogen receptor betaHomo sapiens (human)
nucleoplasmEstrogen receptor betaHomo sapiens (human)
mitochondrionEstrogen receptor betaHomo sapiens (human)
intracellular membrane-bounded organelleEstrogen receptor betaHomo sapiens (human)
chromatinEstrogen receptor betaHomo sapiens (human)
nucleusEstrogen receptor betaHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
nuclear envelopeSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear inner membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear outer membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulum membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
lipid dropletSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytosolSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic densitySigma non-opioid intracellular receptor 1Homo sapiens (human)
membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
growth coneSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytoplasmic vesicleSigma non-opioid intracellular receptor 1Homo sapiens (human)
anchoring junctionSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic density membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumEmopamil-binding protein-likeHomo sapiens (human)
endoplasmic reticulum membraneEmopamil-binding protein-likeHomo sapiens (human)
endoplasmic reticulumEmopamil-binding protein-likeHomo sapiens (human)
plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular regionAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular spaceAngiotensin-converting enzyme 2 Homo sapiens (human)
endoplasmic reticulum lumenAngiotensin-converting enzyme 2 Homo sapiens (human)
plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
ciliumAngiotensin-converting enzyme 2 Homo sapiens (human)
cell surfaceAngiotensin-converting enzyme 2 Homo sapiens (human)
membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
apical plasma membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
endocytic vesicle membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
brush border membraneAngiotensin-converting enzyme 2 Homo sapiens (human)
membrane raftAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular exosomeAngiotensin-converting enzyme 2 Homo sapiens (human)
extracellular spaceAngiotensin-converting enzyme 2 Homo sapiens (human)
nuclear outer membrane7-dehydrocholesterol reductaseHomo sapiens (human)
endoplasmic reticulum7-dehydrocholesterol reductaseHomo sapiens (human)
endoplasmic reticulum membrane7-dehydrocholesterol reductaseHomo sapiens (human)
membrane7-dehydrocholesterol reductaseHomo sapiens (human)
endoplasmic reticulum membrane7-dehydrocholesterol reductaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (1247)

Assay IDTitleYearJournalArticle
AID1346880Human Estrogen receptor-beta (3A. Estrogen receptors)1997Endocrinology, Mar, Volume: 138, Issue:3
Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
AID1345880Human GPER (G protein-coupled estrogen receptor)2005Endocrinology, Feb, Volume: 146, Issue:2
Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells.
AID1346845Human Estrogen receptor-alpha (3A. Estrogen receptors)1997Endocrinology, Mar, Volume: 138, Issue:3
Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS 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.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The 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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1768143Intrinsic clearance in human hepatocytes measured up to 60 mins by LC/MS/MS analysis
AID677850Antagonist activity at ERbeta receptor LBD expressed in yeast AH109 cells assessed as inhibition of interaction with SRC1 after 24 hrs by alpha-galactosidase assay2012European journal of medicinal chemistry, Aug, Volume: 54Discovery and structure-activity analysis of selective estrogen receptor modulators via similarity-based virtual screening.
AID678713Inhibition 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 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1284678Cytotoxicity against human MOLT4 cells assessed as growth inhibition after 48 hrs by SRB assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
AID131085Uterotrophic effect in BDF1 mouse measured as([weight of uterus (mg)/body weight (g)] *100)1988Journal 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.
AID1567372Cytotoxicity against human SiHa cells2019European journal of medicinal chemistry, Sep-15, Volume: 178Tetrazole hybrids with potential anticancer activity.
AID1164493Antiproliferative activity human MIAPaCa2 cells after 2 days by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of new estradiol-cationic lipid hybrids: ten-carbon twin chain cationic lipid is a more suitable partner for estradiol to elicit better anticancer activity.
AID759309Cytotoxicity against african green monkey Vero cells assessed as growth inhibition after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.
AID324585Increase in long-lived protein degradation in human H4 cells after 24 hrs relative to control2007Proceedings 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.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current 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.
AID1471123Displacement of fluoromone from full length recombinant human estrogen receptor alpha expressed in Spodoptera frugiperda measured after 2 hrs by fluorescence polarization assay relative to estradiol2017Bioorganic & 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.
AID1217708Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system2011Drug 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.
AID1310519Induction 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%)2016European journal of medicinal chemistry, Aug-08, Volume: 1184-(1,2-diarylbut-1-en-1-yl)isobutyranilide derivatives as inhibitors of topoisomerase II.
AID1366609Induction of necrosis in human MCF7 cells after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.51 +/- 0.21%)2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Syntheses of conformationally restricted benzopyran based triarylethylenes as growth inhibitors of carcinoma cells.
AID1705310Antiproliferative activity against human K562 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1302506Inhibition 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 analysis2016Journal 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.
AID1327718Anticancer activity against human DLD1 cells measured after 48 hrs by SRB assay2016Bioorganic & 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.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID567405Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and in vitro anti-tumor activity of new oxadiazole thioglycosides.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current 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.
AID597269Antiproliferative 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 NuSerum2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Biomimetic syntheses and antiproliferative activities of racemic, natural (-), and unnnatural (+) glyceollin I.
AID561040Antifungal activity against Cryptococcus neoformans NYS2 assessed as disruption of cell wall integrity-associated adenylate kinase release at 64 ug/ml by hemocytometry2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID1284726Cytotoxicity against human UO31 cells assessed as growth inhibition after 48 hrs by SRB assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
AID101920Effect on [3H]-thymidine incorporation into estrogen receptor positive MCF-7 human breast carcinoma cells at 10e-6 M (exp 1)1987Journal 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.
AID191588The compound was tested for serum prolactin level in rats at 10 mg/kg dose after peroral administration1984Journal 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
AID106453Cell growth inhibition of MXT-ER+ breast cancer cells at a dose of 8 mg1988Journal 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.
AID1312680Displacement of fluorescein-labeled estrogen ligand from recombinant ER-alpha (unknown origin) incubated for 2 hrs by fluorescence polarization assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents.
AID1395719Cytotoxicity against human A549 cells preincubated for 4 hrs followed by incubation in compound free media for 24 hrs by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Antiproliferative efficacy of curcumin mimics through microtubule destabilization.
AID498480Stimulation of human PLD1 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins by exogenous substrate assay2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID1559016Antitumor activity against human MCF7:TAM1 cells xenografted in athymic nude mouse assessed as tumor regression at 100 mg/kg, po measured after 4 weeks2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Design and Synthesis of Basic Selective Estrogen Receptor Degraders for Endocrine Therapy Resistant Breast Cancer.
AID70499Displacement of radioligand from Estrogen receptor alpha2002Bioorganic & medicinal chemistry letters, May-06, Volume: 12, Issue:9
Synthesis of a novel fluorescent probe for estrogen receptor.
AID1371164Aqueous solubility of the compound in PBS after 2 hrs by turbidimetric method2017Journal 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).
AID184113Minimum effective dose at which significant increase in uterine weight/body weight in rat was determined (in vivo); expressed as % increase relative to ovariectomized (OVX) controls1997Journal 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.
AID503305Antiproliferative activity against human PC3 cells at 500 nM after 120 hrs by MTT assay relative to DMSO2006Nature chemical biology, Jun, Volume: 2, Issue:6
Identifying off-target effects and hidden phenotypes of drugs in human cells.
AID1209454Inactivation 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 NADPH2012Drug 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.
AID597266Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Biomimetic syntheses and antiproliferative activities of racemic, natural (-), and unnnatural (+) glyceollin I.
AID1287599Cytotoxicity against human MRC5 cells assessed as cell viability after 4 to 7 days by Alamar Blue staining based fluorometric analysis2016European journal of medicinal chemistry, May-04, Volume: 113In vitro screening of 2-(1H-imidazol-1-yl)-1-phenylethanol derivatives as antiprotozoal agents and docking studies on Trypanosoma cruzi CYP51.
AID344797Displacement of fluorescein labeled estradiol from human recombinant ERalpha expressed in baculovirus infected insect cells by fluorescence polarization assay2008Bioorganic & 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.
AID134510In vivo inhibition of hormone-dependent MXT mammary tumor in mice1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
2-Alkyl-substituted 1,1-bis(4-acetoxyphenyl)-2-phenylethenes. Estrogen receptor affinity, estrogenic and antiestrogenic properties, and mammary tumor inhibiting activity.
AID1686037Cytotoxicity in human HepG2 cells assessed as induction of cell necrosis incubated for 4 hrs by LDH release assay2016Journal 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.
AID691260Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Chemocentric informatics approach to drug discovery: identification and experimental validation of selective estrogen receptor modulators as ligands of 5-hydroxytryptamine-6 receptors and as potential cognition enhancers.
AID1705368Antiproliferative activity against human CNS cancer cells2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1387891Selectivity index, ratio of IC50 for human recombinant full-length estrogen receptor beta to IC50 for human recombinant full-length estrogen receptor alpha2018Journal 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.
AID306820Cell viability of estrogen receptor negative MDA-MB-231 cells at 5 uM after 48 hrs by MTT assay relative to DMSO2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Identification of a series of tetrahydroisoquinoline derivatives as potential therapeutic agents for breast cancer.
AID164973Percent stimulation or inhibition of protein kinase C with [Ca2+] for phosphatidylserine and diolein(PS+DO)1992Journal 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.
AID1464228Agonist activity at full length ERbeta (unknown origin) expressed in human HeLa cells incubated for 24 hrs by ERE-driven luciferase reporter gene assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Design and synthesis of benzoacridines as estrogenic and anti-estrogenic agents.
AID1065303Cytotoxicity against human A549 cells after 48 hrs by MTT assay2013European journal of medicinal chemistry, Aug, Volume: 66Diversity-oriented synthesis of α-aminophosphonates: a new class of potential anticancer agents.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID1327720Anticancer activity against human DU145 cells measured after 48 hrs by SRB assay2016Bioorganic & 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.
AID1705359Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1705320Antiproliferative activity against human NCI-H460 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1662874Cytotoxicity against human Chang cells2020Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13
Design and synthesis of amphiphilic 2-hydroxybenzylphosphonium salts with antimicrobial and antitumor dual action.
AID1779058Antiproliferative activity against human Ishikawa cells assessed as reduction in cell growth incubated for 48 hrs by CCK8 assay2021European journal of medicinal chemistry, Oct-05, Volume: 221Design and synthesis of novel benzothiophene analogs as selective estrogen receptor covalent antagonists against breast cancer.
AID270143Cytotoxicity against human SK-BR-3 cells expressing HER2 and lacking ER2006Journal 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.
AID1602669Mitochondrial toxicity in human HepG2 cells assessed as reduction in cell viability after 24 hrs in presence of galactose by CellTiter-Glo assay2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
A Cinchona Alkaloid Antibiotic That Appears To Target ATP Synthase in Streptococcus pneumoniae.
AID482992Antiproliferative activity against human MDA-MB-231 cells by MTT assay2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Synthesis of new cis-fused tetrahydrochromeno[4,3-b]quinolines and their antiproliferative activity studies against MDA-MB-231 and MCF-7 breast cancer cell lines.
AID1464644Cytotoxicity against human MCF7 cells after 72 hrs by resazurin based fluorescence assay2017Bioorganic & medicinal chemistry letters, 10-15, Volume: 27, Issue:20
Synthesis and evaluation of the NSCLC anti-cancer activity and physical properties of 4-aryl-N-phenylpyrimidin-2-amines.
AID1768146Apparent permeability in MDCK cells across apical to basolateral side at 10 uM incubated for 3 hrs by LC-MS/MS analysis
AID191693Uterotrophic effect in rats uterine at 50 ug/day dose1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent.
AID1688050Antiproliferative activity against human MCF-7 cells assessed as inhibition of cell growth measured after 48 hrs by SRB assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition.
AID589238Mechanism based inhibition of human cytochrome P450 2B6 measured by 7-EFC O-deethylation2005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID397944Antiproliferative activity against human estrogen receptor deficient MDA-MB-231 cells after 48 hrs by MTT assay2009Bioorganic & 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.
AID1323683Inhibition of PKC in human neutrophil assessed as inhibition of PMA-stimulated chemiluminescence preincubated for 5 mins followed by PMA stimulation by luciferase reporter gene assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Design and synthesis of triarylacrylonitrile analogues of tamoxifen with improved binding selectivity to protein kinase C.
AID69513Relative binding affinity(RBA) against Estrogen receptor in rat liver1992Journal 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.
AID1705367Antiproliferative activity against human colon cancer cells2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1866706Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Rational 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.
AID306818Enhancement of growth of estrogen receptor positive MCF7 cells at 5 uM after 48 hrs by MTT assay relative to DMSO2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Identification of a series of tetrahydroisoquinoline derivatives as potential therapeutic agents for breast cancer.
AID470166Antiestrogenic activity in human T47D 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 assay2009Journal of natural products, Nov, Volume: 72, Issue:11
Antiestrogenic constituents of the Thai medicinal plants Capparis flavicans and Vitex glabrata.
AID677849Antagonist activity at ERalpha receptor LBD expressed in yeast AH109 cells assessed as inhibition of interaction with SRC1 after 24 hrs by alpha-galactosidase assay2012European journal of medicinal chemistry, Aug, Volume: 54Discovery and structure-activity analysis of selective estrogen receptor modulators via similarity-based virtual screening.
AID344791Antiproliferative activity against estrogen receptor dependent human MCF7 cells after 72 hrs by MTT assay2008Bioorganic & 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.
AID1755842Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay2021European journal of medicinal chemistry, Jan-15, Volume: 210Metronidazole-conjugates: A comprehensive review of recent developments towards synthesis and medicinal perspective.
AID127060Ability to antagonize uterine weight gain in immature mice, at a dose of 30 ug; Activity is expressed as anti-uterotrophic % reduction1991Journal 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.
AID248173Antiproliferative activity in MDA-MB 231 human breast cancer cells2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Antitumor-active cobalt-alkyne complexes derived from acetylsalicylic acid: studies on the mode of drug action.
AID101931Inhibition of estrogen receptor positive MCF-7 cell proliferation as percent treated/control cell number after 10 days at 10e-6 M1981Journal 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.
AID1529804Cytotoxicity against HEK293 cells after 24 hrs by resazurin dye-based fluorescence analysis2018European journal of medicinal chemistry, Dec-05, Volume: 160Norbornane-based cationic antimicrobial peptidomimetics targeting the bacterial membrane.
AID1502305Displacement of fluorescent estrogen ligand from recombinant human ERalpha expressed in insect cells incubated for 2 hrs by polarization2017European journal of medicinal chemistry, Nov-10, Volume: 140Novel 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.
AID1073742Aqueous solubility of compound in phosphate buffer assessed as solubility limit after 2 hrs by turbidity analysis2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Discovery and characterization of potent thiazoles versus methicillin- and vancomycin-resistant Staphylococcus aureus.
AID493961Induction of of LuxR-dependent quorum sensing in Vibrio fischeri assessed as induction of bioluminescence intensity up to 200 uM2010Bioorganic & 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.
AID38728Binding affinity towards antiestrogen binding site AEBS2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 1. Receptor interactions.
AID1418619Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay2018Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
Synthesis, computational studies and antiproliferative activities of coumarin-tagged 1,3,4-oxadiazole conjugates against MDA-MB-231 and MCF-7 human breast cancer cells.
AID1705331Antiproliferative activity against human SNB-19 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID589123Mechanism based inhibition of human cytochrome P450 3A4 measured by midazolam 1'-hydroxylation2005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID561226Antifungal activity against Candida parapsilosis R058-G12 after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID1415056Aqueous solubility of the compound in PBS buffer at pH 7.4 after 2 hrs2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.
AID497605Antagonist activity at human ERalpha expressed in human HeLa cells coexpressing ERE-E1b-Luc assessed as inhibition of estradiol-induced transcriptional activation at 1 uM after 48 hrs by luciferase reporter gene assay2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha.
AID1170537Displacement of fluorescein-labeled estrogen from human recombinant ERalpha by fluorescence polarization based competitive binding affinity assay2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
β-Lactam estrogen receptor antagonists and a dual-targeting estrogen receptor/tubulin ligand.
AID1387887Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length estrogen receptor alpha after 2 hrs by fluorescence polarization assay2018Journal 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.
AID69358Displacement of [3H]E2 specific binding to estrogen receptor1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent.
AID1364333Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin based assay2017Journal of natural products, 04-28, Volume: 80, Issue:4
Antibacterial Nerol Cinnamates from the Australian Plant Eremophila longifolia.
AID597272Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Biomimetic syntheses and antiproliferative activities of racemic, natural (-), and unnnatural (+) glyceollin I.
AID1705318Antiproliferative activity against human NCI-H23 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1209444Cytotoxicity against human hepatocytes assessed as reduction in cell viability after 4 hrs by ATP detection based assay2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
In vitro hepatotoxicity and cytochrome P450 induction and inhibition characteristics of carnosic acid, a dietary supplement with antiadipogenic properties.
AID91597Concentration of compound required to induce 50 % of the maximum stimulation of alkaline phosphatase activity in Ishikawa cells1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
3-[4-(1,2-Diphenylbut-1-enyl)phenyl]acrylic acid: a non-steroidal estrogen with functional selectivity for bone over uterus in rats.
AID1356856In-vivo agonist activity at ERalpha in CD-IGS rat assessed as increase in uterine wet weight at 60 mg/kg, po dosed daily for 3 days by gavage and measured 24 hrs after last dose by immature rat uterine wet weight assay2018Journal 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.
AID324582Increase in long-lived protein degradation in human H4 cells after 1 hr relative to control2007Proceedings 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.
AID1254846Antiproliferative activity against human GBM3 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method2015European journal of medicinal chemistry, Oct-20, Volume: 103Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID756453Antiproliferative activity against human MSTO-211H cells after 72 hrs by trypan blue assay2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and biological evaluation of novel tamoxifen analogues.
AID1705333Antiproliferative activity against human U251 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1366618Induction of ROS accumulation in human MCF7 cells assessed as mean fluorescence intensity after 24 hrs by H2DCF-DA staining based flow cytometry (Rvb = 62.46 +/- 2.26 No_unit)2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Syntheses of conformationally restricted benzopyran based triarylethylenes as growth inhibitors of carcinoma cells.
AID302179Growth inhibition of human HL60 cells after 4 hrs by MTT assay2007Bioorganic & 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.
AID1705339Antiproliferative activity against human SK-MEL-28 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID597268Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Biomimetic syntheses and antiproliferative activities of racemic, natural (-), and unnnatural (+) glyceollin I.
AID191697Uterotrophic effect in rats uterine at 50 ug/day dose in the presence of 0.05 ug hexestrol1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent.
AID1284682Cytotoxicity against human EKVX cells assessed as growth inhibition after 48 hrs by SRB assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
AID1217707Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system2011Drug 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.
AID1283249Inhibition of delta 8-7 isomerase in Dhcr7-deficient mouse Neuro2a cells assessed as increase in zymosterol levels at 1 uM by LC-MS/GC-MS analysis2016Journal 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.
AID106081Anti-estrogenicity for 50% inhibition of the MVLN cell luciferase activity due to 0.1 nM E2 (estradiol)1997Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
Cytotoxicity and antiestrogenicity of a novel series of basic diphenylethylenes.
AID103080Agonistic effect on estrogen receptor mediated transcriptional activation in MCF-7-2a cells at 1 uM compared to 10e-8 M estradiol2003Journal 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.
AID103376Inhibitory concentration against MCF-7 breast tumor cells using MCF-7 assay.2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.
AID124179Uterine weight after 9 day treatment at 4.2 ug by oral gavage to ovariectomised mice with estrone1997Journal 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.
AID497601Cellular uptake in human HeLa cells assessed as retention time at 2 uM after 48 hrs by HPLC-MS analysis2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha.
AID1684751Cytotoxicity against human MCF-10A cells after 48 hrs by MTT assay2021Bioorganic & medicinal chemistry letters, 02-01, Volume: 33Synthesis of mitochondria-targeted coumarin-3-carboxamide fluorescent derivatives: Inhibiting mitochondrial TrxR2 and cell proliferation on breast cancer cells.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID498481Inhibition of N-terminally truncated rat PLD1 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins by exogenous substrate assay2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID1533115Inhibition of P-gp-mediated Rho-123 efflux in human Lucena 1 cells at 12.5 uM preincubated for 1 hr followed by Rho-123 addition measured after 1 hr by flow cytometry2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors.
AID1705369Antiproliferative activity against human Melanoma cells2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID677864Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 24 hrs by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54Discovery and structure-activity analysis of selective estrogen receptor modulators via similarity-based virtual screening.
AID678556Cytotoxicity against human U937 cells after 72 hrs by WST1 assay in presence of 20% FBS2012Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
Synthesis and cytotoxic activity of non-naturally substituted 4-oxycoumarin derivatives.
AID324469Increase in light chain 3-GFP+ autophagosome vesicle area per cell in human H4 cells at 4.4 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings 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.
AID756563Cytotoxicity against human Caco2 cells after 1 hr by Alamar Blue assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Design, synthesis, and biological evaluation of (E)-N-aryl-2-arylethenesulfonamide analogues as potent and orally bioavailable microtubule-targeted anticancer agents.
AID493959Inhibition of LuxR-dependent quorum sensing in Vibrio fischeri assessed as reduction of 3-oxo-C6-HSL-induced bioluminescence intensity at 20 uM2010Bioorganic & 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.
AID1688052Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 48 hrs by SRB assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition.
AID172430Change in DMBA-induced mammary tumor area in rats after 28 day therapy at 3 mg dose (experiment-1)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity.
AID1469717Induction of selective estrogen receptor alpha degradation in human MCF7 cells harboring TK-ERE-Luc assessed as reduction in estradiol-induced transcriptional activity after 24 hrs by luciferase reporter gene assay2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.
AID270139Cytotoxicity against human MCF7 cells expressing ER2006Journal 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.
AID1312682Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents.
AID781330pKa (acid-base dissociation constant) as determined by potentiometric titration2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID374713Cytotoxicity against human MCF7 cells expressing estrogen receptor after 72 hrs by SRB assay2009Journal 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.
AID604744Displacement of radiolabeled dansylsarcosine from fatty acid containing human serum albumin site 2 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions.
AID183959Eosinophil peroxidase activity expressed as Vmax was determined in rat (in vivo) Eosinophil peroxidase activity expressed as Vmax was determined in rat (in vivo)1997Journal 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.
AID103918Inhibition of 17-beta-estradiol (10e-11 M) mediated MCF-7 cell proliferation1999Bioorganic & medicinal chemistry letters, Apr-19, Volume: 9, Issue:8
Synthesis and biological activity of trans-2,3-dihydroraloxifene.
AID1364837Inhibition of estradiol-induced proliferation in human MCF7 cells after 72 hrs by Cell-titer-Glo assay2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Functional evaluation of synthetic flavonoids and chalcones for potential antiviral and anticancer properties.
AID1401997Inhibition of PKC in rat brain soluble fraction at 3 uM using calf thymus H1 histone, phosphatidylserine and [gamma-32P]ATP by liquid scintillation counting method2018European journal of medicinal chemistry, Jan-01, Volume: 143Tamoxifen a pioneering drug: An update on the therapeutic potential of tamoxifen derivatives.
AID482351Antagonist activity at ERalpha expressed in yeast assessed as inhibition of E2-induced alpha-galactosidase activity2010Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14
Discovery of potent ligands for estrogen receptor beta by structure-based virtual screening.
AID624633Drug glucuronidation reaction catalyzed by human recombinant UGT1A42005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID723539Cytotoxicity against drug-resistant human MDA-MB-231 cells assessed as change in cell viability at 5 uM after 48 hrs by MTT assay2013European journal of medicinal chemistry, Feb, Volume: 60Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent.
AID1500968Effect on AIM2 mRNA expression in human MCF7 cells at 2 uM by RT-PCR method2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel 2-methoxyestradiol analogs as dual selective estrogen receptor modulators (SERMs) and antiangiogenic agents.
AID561224Antifungal activity against Candida albicans ATCC 90028 after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID103754Cytostatic activity against MCF-7 cell proliferation.1992Journal 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.
AID1366608Cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase at 10 uM after 24 to 48 hrs by propidium iodide staining based flow cytometry2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Syntheses of conformationally restricted benzopyran based triarylethylenes as growth inhibitors of carcinoma cells.
AID576612Inhibition of human ERG2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.
AID677855Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability at 100 uM after 24 hrs by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54Discovery and structure-activity analysis of selective estrogen receptor modulators via similarity-based virtual screening.
AID1217710Covalent binding in human liver microsomes measured per mg of protein using radiolabelled compound at 10 uM after 1 hr incubation by liquid scintillation counting2011Drug 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.
AID1570846Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
A Bioreductive Prodrug of Cucurbitacin B Significantly Inhibits Tumor Growth in the 4T1 Xenograft Mice Model.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID498477Inhibition of PLD1 in human Calu-1 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID276684Antagonist activity at ER receptor assessed as inhibition of 17-alpha-ethynylestradiol-induced increase in uterine weight of Sprague-Dawley rat at 3 mg/kg/day, po2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
Rapid synthesis of 4-benzylidene and 4-[bis-(4-methoxyphenyl)-methylene-2-substituted phenyl-benzopyrans as potential selective estrogen receptor modulators (SERMs) using McMurry coupling reaction.
AID1395720Cytotoxicity against human A431 cells preincubated for 4 hrs followed by incubation in compound free media for 24 hrs by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Antiproliferative efficacy of curcumin mimics through microtubule destabilization.
AID673825Growth inhibition of human MCF7 cells at 10'-6 M after 5 days relative to control2012ACS medicinal chemistry letters, Apr-06, Volume: 3, Issue:5
Boron-Based 4-Hydroxytamoxifen Bioisosteres for Treatment of de Novo Tamoxifen Resistant Breast Cancer.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1210949Ratio of Kinact to Ki for CYP3A4 (unknown origin)2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Inactivation of cytochrome P450 (P450) 3A4 but not P450 3A5 by OSI-930, a thiophene-containing anticancer drug.
AID324417Increase in light chain 3-GFP+ autophagosome vesicle number per cell in human H4 cells at 4.4 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings 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.
AID474293Inhibition of PKC at 0.2 mM after 90 mins by ELISA2010Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
Endoxifen is a new potent inhibitor of PKC: a potential therapeutic agent for bipolar disorder.
AID176791In vivo inhibition of estrogen-stimulated uterine weight gain in immature rats on subcutaneous administration; ND=not determined1997Journal 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.
AID1387903Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 5 days by SRB assay2018Journal 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.
AID1705365Antiproliferative activity against human leukemia cells2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1233703Cytotoxicity against African green monkey Vero cells assessed as cell viability by MTT assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Synthesis and cancer cell growth inhibitory activity of icaritin derivatives.
AID491955Cytotoxicity against human HT-29 cells after 24 hrs by CellTiter-BlueCell viability assay2010Journal of natural products, Jul-23, Volume: 73, Issue:7
Mayamycin, a cytotoxic polyketide from a Streptomyces strain isolated from the marine sponge Halichondria panicea.
AID102765Percentage [3H]thymidine incorporation treated/control in hormone sensitive MCF-7 cell proliferation assay at 10e-5 M or 10e-6 M1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity.
AID620850Binding affinity to bovine serum albumin at pH 7.4 by fluorescence spectroscopy2011European 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.
AID1676127Antiviral activity against pseudotyped Marburgvirus-Musoke infected in human A549 cells assessed as reduction in viral infection incubated for 48 hrs by luciferase reporter gene assay2020Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors.
AID1210013Inhibition of recombinant CYP2J2 (unknown origin)-mediated terfenadine hydroxylation assessed as remaining activity at 30 uM after 5 mins by LC-MS analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID103427Cytotoxicity against MCF-7 cells in the absence of 1 uM E2 (estradiol)1997Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
Cytotoxicity and antiestrogenicity of a novel series of basic diphenylethylenes.
AID1284374Displacement of [3H]-E2 from human ER-beta incubated for 16 to 20 hrs by liquid scintillation counting analysis2016European journal of medicinal chemistry, Apr-13, Volume: 112Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
AID124171Uterine weight after 9 day treatment at 1.4 ug by oral gavage to ovariectomised mice with estrone1997Journal 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.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID681131TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID588215FDA HLAED, alkaline phosphatase increase2004Current 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.
AID1065290Cytotoxicity against human Jurkat cells after 48 hrs by MTT assay2013European journal of medicinal chemistry, Aug, Volume: 66Diversity-oriented synthesis of α-aminophosphonates: a new class of potential anticancer agents.
AID514395Cytostatic activity against human MCF7 cells at 5 uM after 3 days by microtiter assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
2-phenyl-1-[4-(2-piperidine-1-yl-ethoxy)benzyl]-1H-benzimidazoles as ligands for the estrogen receptor: synthesis and pharmacological evaluation.
AID69229Relative binding affinity against Estrogen receptor in immature mouse.1986Journal 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.
AID1395722Cytotoxicity against human MCF7 cells preincubated for 4 hrs followed by incubation in compound free media for 24 hrs by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Antiproliferative efficacy of curcumin mimics through microtubule destabilization.
AID282039Decrease doxorubicin-saliform uptake in MDA-MB-435 cells at 10 uM after 1 hr relative to DOX-TEG-TAM2004Journal 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.
AID187052The compound was tested for uterotropic activity in immature rats(Dosage 100 ug)1984Journal 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
AID324578Effect on FYVE-RFP+ vesicle intensity per cell in human H4 cells after 8 hrs relative to control2007Proceedings 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.
AID723649Binding affinity to emopamil binding protein (unknown origin)2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Synthesis and biological evaluation of ¹⁸F labeled fluoro-oligo-ethoxylated 4-benzylpiperazine derivatives for sigma-1 receptor imaging.
AID179336Percent uterotrophic effect at 10 ug/day dose compared to estradiol1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent.
AID1283250Inhibition of delta 8-7 isomerase in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in cholesterol levels at 1 uM by LC-MS/GC-MS analysis2016Journal 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.
AID1853584Cytotoxicity against human HEK293 cells reduction in cell viability at 74 ug/ml incubated for 24 hrs by resazurin cell viability assay2021RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
Design, synthesis, and antibacterial activity of
AID102756Effect on [3H]-thymidine incorporation into MCF-7 human breast cancer cells at 1x10E-5 M1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Indolo[2,1-a]isoquinolines. Syntheses, steroid hormone receptor binding affinities, and cytostatic activity.
AID344801Selectivity ratio of IC50 for human recombinant ERalpha to IC50 for human recombinant ERbeta2008Bioorganic & 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.
AID1158148Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Synthesis and anticancer activity of γ-(triazolyl ethylidene)butenolides and polyfunctional pyrrolinones.
AID1602139Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay2019European journal of medicinal chemistry, Mar-15, Volume: 166Structure-based drug design, synthesis, In vitro, and In vivo biological evaluation of indole-based biomimetic analogs targeting estrogen receptor-α inhibition.
AID1242128Anti-proliferative activity against human A549 cells incubated for 48 hrs by SRB assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Design, synthesis and anticancer properties of novel oxa/azaspiro[4,5]trienones as potent apoptosis inducers through mitochondrial disruption.
AID723807Antiproliferative activity against human T47D cells after 48 hrs by MTT assay2013European journal of medicinal chemistry, Feb, Volume: 60Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent.
AID1438379Cytotoxicity against human SKBR3 cells assessed as growth inhibition after 120 hrs by MTT assay2017European journal of medicinal chemistry, Mar-10, Volume: 128Synthesis and biological evaluation of fluorinated N-benzoyl and N-phenylacetoyl derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as steroid sulfatase inhibitors.
AID1646802Chaperone activity at GCase in wild-type human fibroblasts assessed as increase in GPN-induced reduction of calcium release using Fluo-8AM based fluorescence assay relative to control2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells.
AID176788In vivo inhibition of estrogen-stimulated uterine weight gain in immature rats on peroral administration1997Journal 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.
AID1705317Antiproliferative activity against human NCI-H226 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID102432Effect on the growth of MCF-7 cells at a concentration of,10 e-7 M, percentage of control value being 841985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Hydroxy derivatives of tamoxifen.
AID1193495Thermodynamic equilibrium solubility, log S of the compound in simulated intestinal fluid at pH 6.8 at RT after 4 hrs by 96 well plate method2015Bioorganic & 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.
AID1365723Solubility of compound in Middlebrook 7H9 broth media at pH 6.4 at 200 uM after 90 mins by UV-VIS spectrophotometric method2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID1469736Downregulation of progesterone receptor mRNA level in NOD SCID gamma mouse xenografted with human MCF7 cells at 60 mg/kg, po 5 days per week for 48 days post tumor implantation measured 7 hrs post last dose by RT-PCR method2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.
AID103539Inhibition of MCF-7 cell proliferation at 10000 nM1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Carboxylic acid analogues of tamoxifen: (Z)-2-[p-(1, 2-diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine. Estrogen receptor affinity and estrogen antagonist effects in MCF-7 cells.
AID1310513Cytotoxicity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by trypan blue assay2016European journal of medicinal chemistry, Aug-08, Volume: 1184-(1,2-diarylbut-1-en-1-yl)isobutyranilide derivatives as inhibitors of topoisomerase II.
AID179144Partial remission of DMBA-induced mammary tumors in rats at 3 mg dose1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity.
AID1533102Inhibition of P-gp-mediated doxorubicin efflux in human Lucena 1 cells assessed as ratio of doxorubicin fluorescence intensity in presence of compound to doxorubicin fluorescence intensity in absence of compound at 6.25 uM preincubated for 1 hr followed b2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors.
AID467756Cytotoxicity against human adriamycin- resistant MCF7 cells by WST-1 assay2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Cytotoxic and PTP1B inhibitory activities from Erythrina abyssinica.
AID1364335Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin based assay2017Journal of natural products, 04-28, Volume: 80, Issue:4
Antibacterial Nerol Cinnamates from the Australian Plant Eremophila longifolia.
AID1502304Displacement of fluorescent estrogen ligand from recombinant human ERalpha expressed in insect cells at 10 uM incubated for 2 hrs by polarization2017European journal of medicinal chemistry, Nov-10, Volume: 140Novel 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.
AID407204Inhibition of P-glycoprotein-mediated rhodamine 123 absorption in guinea-pig ileum2008Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
Effect of some P-glycoprotein modulators on Rhodamine-123 absorption in guinea-pig ileum.
AID514396Cytostatic activity against human MDA-MB-231 cells after 3 days by microtiter assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
2-phenyl-1-[4-(2-piperidine-1-yl-ethoxy)benzyl]-1H-benzimidazoles as ligands for the estrogen receptor: synthesis and pharmacological evaluation.
AID1422687Cytotoxicity against HEK293 cells after 24 hrs by resazurin dye-based fluorescence analysis2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Antifungal benzo[b]thiophene 1,1-dioxide IMPDH inhibitors exhibit pan-assay interference (PAINS) profiles.
AID736609Growth inhibition of estrogen-dependent human MCF7 cells2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Synthesis and growth inhibition activity of fluorinated derivatives of tamoxifen.
AID1161689Cytotoxicity against human HeLa cells assessed as reduction in cell viability in presence of 10 mM NAC after 48 hrs by WST8 assay2014Journal of natural products, Sep-26, Volume: 77, Issue:9
Bioactive dihydronaphthoquinone derivatives from Fusarium solani.
AID124174Uterine weight after 9 day treatment at 14 ug by oral gavage to ovariectomised mice without estrone1997Journal 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.
AID1694960Cytotoxicity against human PC-3 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2020RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2
Development of potent CPP6-gemcitabine conjugates against human prostate cancer cell line (PC-3).
AID1291379Cytotoxicity against human ER-negative MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay2016Bioorganic & 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.
AID69051Displacement of [3H]17-beta-estradiol from estrogen receptor of MCF-7 cell lysate as relative binding affinity1999Bioorganic & medicinal chemistry letters, Apr-19, Volume: 9, Issue:8
Synthesis and biological activity of trans-2,3-dihydroraloxifene.
AID1065300Cytotoxicity against human NCI-H23 cells after 48 hrs by MTT assay2013European journal of medicinal chemistry, Aug, Volume: 66Diversity-oriented synthesis of α-aminophosphonates: a new class of potential anticancer agents.
AID103056Inhibition of hormone-sensitive MCF-7 mammary tumor cell proliferation at 1*10e-5 M1992Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19
6-Alkyl-12-formylindolo[2,1-a]isoquinolines. Syntheses, estrogen receptor binding affinities, and stereospecific cytostatic activity.
AID1217727Intrinsic clearance for reactive metabolites formation per mg of protein in human liver microsomes based on [3H]GSH adduct formation rate at 100 uM by [3H]GSH trapping assay2011Drug 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.
AID1754978Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Design, synthesis and broad spectrum antibreast cancer activity of diarylindoles via induction of apoptosis in aggressive breast cancer cells.
AID1158149Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Synthesis and anticancer activity of γ-(triazolyl ethylidene)butenolides and polyfunctional pyrrolinones.
AID1297990Antiparasitic activity against amastigote stage of Leishmania chagasi MHOM/BR/1972/LD infected in golden hamster assessed as golden hamster survival rate at 20 mg/kg, ip after 18 weeks by limiting dillution method2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Repurposing strategies for tropical disease drug discovery.
AID1389791Antiproliferative activity against human Ishikawa cells at >40 uM after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6
Synthesis and biological evaluation of 4,6-diaryl-2-pyrimidinamine derivatives as anti-breast cancer agents.
AID614553Antiproliferative activity against human HEK293 cells after 48 hrs by MTT assay2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Design and synthesis of 1,3-biarylsulfanyl derivatives as new anti-breast cancer agents.
AID1530766Displacement of fluorescent estrogen ligand from recombinant human full length untagged ERalpha expressed in Spodoptera frugiperda insect cells at 20 uM measured after 2 hrs by fluorescence polarization assay relative to control2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2.
AID451835Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2009Bioorganic & 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.
AID1705343Antiproliferative activity against human IGROV-1 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID756455Antiproliferative activity against human MCF7 cells after 72 hrs by trypan blue assay2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and biological evaluation of novel tamoxifen analogues.
AID173698Percent decrease in serum cholesterol relative to OVX controls, at 0.01 mg/Kg compound dose1998Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
Synthesis and pharmacology of conformationally restricted raloxifene analogues: highly potent selective estrogen receptor modulators.
AID444841Induction of human MCF7 cell differentiation assessed as lipid accumulation in intracytoplasmic vesicle at 5 uM after 48 hrs by oil red O staining-based light microscopy2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis of new alkylaminooxysterols with potent cell differentiating activities: identification of leads for the treatment of cancer and neurodegenerative diseases.
AID103222Antiproliferative activity against Human MCF-7 Breast cancer cell line in vitro.2001Journal of medicinal chemistry, Mar-29, Volume: 44, Issue:7
Flexible estrogen receptor modulators: design, synthesis, and antagonistic effects in human MCF-7 breast cancer cells.
AID69212Relative binding affinity (RBA) for Estrogen receptor compared to [3H]-estradiol1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Estrogenic affinity labels: synthesis, irreversible receptor binding, and bioactivity of aziridine-substituted hexestrol derivatives.
AID514397Cytostatic activity against human MCF7 cells at 10 uM after 3 days by microtiter assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
2-phenyl-1-[4-(2-piperidine-1-yl-ethoxy)benzyl]-1H-benzimidazoles as ligands for the estrogen receptor: synthesis and pharmacological evaluation.
AID103893Anti-proliferative activity against estrogen-responsive human breast cancer cell line MCF-7 in the presence of ER at a 10e-4 uM concentration of estradiol1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Novel 5-aminoflavone derivatives as specific antitumor agents in breast cancer.
AID471242Agonist activity at estrogen receptor in human MCF7 cells assessed as 17-beta-estradiol-induced cell proliferation at 10 uM after 24 hrs by [14C]thymidine incorporation assay2009Journal 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.
AID1533100Inhibition of P-gp-mediated doxorubicin efflux in human Lucena 1 cells assessed as ratio of doxorubicin fluorescence intensity in presence of compound to doxorubicin fluorescence intensity in absence of compound at 25 uM preincubated for 1 hr followed by 2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1356938Binding affinity to untagged human recombinant full length ERalpha expressed in insect cells 0.1 to 10000 uM by Fluormone ES2 Green displacement based assay2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
AID1536994In vivo agonist activity at ERalpha in CD-IGS rat assessed as increase in uterine weight at 60 mg/kg, po for 3 consecutive days measured at 24 hrs post last dose2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Maximizing ER-α Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927.
AID1057862Inhibition of RML prion protein infected in mouse dividing ScN2a-cl3 cells expressing full length mouse PrP assessed as reduction of PrPsc level after 5 days by ELISA2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Antiprion compounds that reduce PrP(Sc) levels in dividing and stationary-phase cells.
AID620854Effect on secondary structure of bovine serum albumin assessed as random coil content at 0.5 uM at pH 7.4 by circular dichroism method (Rvb = 6 %)2011European 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.
AID1546178Growth inhibition of human PANC1 cells2019European journal of medicinal chemistry, Dec-15, Volume: 184Current scenario of tetrazole hybrids for antibacterial activity.
AID723808Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2013European journal of medicinal chemistry, Feb, Volume: 60Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent.
AID1628320Antiestrogenic activity in human T47D cells assessed as compound concentration required to decrease 100 pM E2-induced cell proliferation to equivalent levels induced by 50 pM E2 after 96 hrs by alamar blue assay2016Journal of natural products, 05-27, Volume: 79, Issue:5
Furofuran Lignan Glucosides with Estrogen-Inhibitory Properties from the Bangladeshi Medicinal Plant Terminalia citrina.
AID1233702Cytotoxicity against human A549 cells assessed as cell viability by MTT assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Synthesis and cancer cell growth inhibitory activity of icaritin derivatives.
AID1312683Antiproliferative activity against human Ishikawa cells incubated for 48 hrs by MTT assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents.
AID1768139Induction of estrogen receptor degradation in human MCF7 cells incubated for 4 hrs by Alexafluor -488 conjugate anti-mouse IgG staining based fluorescence method
AID1284706Cytotoxicity against human MDA-MB-435 cells assessed as growth inhibition after 48 hrs by SRB assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
AID444843Induction of human MCF7 cell differentiation assessed as stimulation of milk fat globulin expression at 5 uM after 48 hrs by immunocytochemistry2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis of new alkylaminooxysterols with potent cell differentiating activities: identification of leads for the treatment of cancer and neurodegenerative diseases.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1705372Antiproliferative activity against human prostate cancer cells2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1693875Cytotoxicity against ER-negative human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Synthesis, antitumor activity and structure-activity studies of novel pyridoxine-based bioisosteric analogs of estradiol.
AID1364836Inhibition of estradiol-induced proliferation in human Ishikawa cells after 72 hrs by Cell-titer-Glo assay2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Functional evaluation of synthetic flavonoids and chalcones for potential antiviral and anticancer properties.
AID1768144Intrinsic clearance in rat hepatocytes measured up to 60 mins by LC/MS/MS analysis
AID1518643Cytotoxicity against human Chang cells assessed as reduction in cell viability by fluorescence based viable cell counting method2019European journal of medicinal chemistry, Dec-15, Volume: 184New 2,6-diaminopyridines containing a sterically hindered benzylphosphonate moiety in the aromatic core as potential antioxidant and anti-cancer drugs.
AID38614Displacement of [3H]tamoxifen from antiestrogen binding site (AEBS)1989Journal of medicinal chemistry, Jan, Volume: 32, Issue:1
Phenolic metabolites of clomiphene: [(E,Z)-2-[4-(1,2-diphenyl-2-chlorovinyl)phenoxy]ethyl]diethylamine. Preparation, electrophilicity, and effects in MCF 7 breast cancer cells.
AID191695Uterotrophic effect in rats uterine at 50 ug/day dose in the presence of 0.2 ug estradiol1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent.
AID1662877Selectivity index, ratio of IC50 for human Chang cells to IC50 for human HepG2 cells2020Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13
Design and synthesis of amphiphilic 2-hydroxybenzylphosphonium salts with antimicrobial and antitumor dual action.
AID1193497Thermodynamic equilibrium solubility, log S of the compound PBS at pH 7.4 at RT after 24 hrs by shake-flask method2015Bioorganic & 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.
AID681127TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID1705342Antiproliferative activity against human UACC-62 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID102275Inhibition of [3H]thymidine incorporation into hormone sensitive MCF-7 human breast cancer cells at 10e-5 M1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity.
AID103517Incorporation of [3H]thymidine into estrogen-responsive MCF-7 human breast tumor cells at 10e-8 M concentration with hexestrol; dpm/dish1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
N,N'-Dialkyl-1,2-bis(hydroxyphenyl)ethylenediamines and N,N-dialkyl-4,5-bis(4-hydroxyphenyl)imidazolidines: syntheses and evaluation of their mammary tumor inhibiting activity.
AID1209427Cytotoxicity against human hepatocytes assessed as reduction in cell viability after 4 hrs by LDH release assay2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
In vitro hepatotoxicity and cytochrome P450 induction and inhibition characteristics of carnosic acid, a dietary supplement with antiadipogenic properties.
AID105054Inhibition of estrogen receptor negative MDA-MB-453 breast cancer cell proliferation with 10e-4 M estradiol1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Novel 5-aminoflavone derivatives as specific antitumor agents in breast cancer.
AID101642Cytostatic effect on hormone-independent MDA-MB 231 human breast cancer cell proliferation at 1x10E-5 M1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Indolo[2,1-a]isoquinolines. Syntheses, steroid hormone receptor binding affinities, and cytostatic activity.
AID1170536Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
β-Lactam estrogen receptor antagonists and a dual-targeting estrogen receptor/tubulin ligand.
AID1209974Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1666650Displacement of fluorescent estrogen ligand from recombinant human full length untagged ERbeta expressed in baculovirus infected insect cells incubated in dark for 2 hrs by Beacon single-tube fluorescent polarization assay2020Bioorganic & 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.
AID1705308Antiproliferative activity against human CCRF-CEM cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID378639Displacement of [3H]estradiol from estrogen receptor relative to estradiol2000Journal of natural products, Dec, Volume: 63, Issue:12
Three new arylobenzofurans from Onobrychis ebenoides and evaluation of their binding affinity for the estrogen receptor.
AID1283273Decrease in cholesterol levels in human SLOS fibroblasts at 10 nM after 5 days by LC-MS/GC-MS analysis2016Journal 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.
AID102764Percentage cell number change as treated/control in hormone sensitive MCF-7 cell proliferation assay at 10e-6 M or 10e-5 M1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity.
AID302175Antiproliferative activity against human HL60 cells assessed as cell viability at 1 ug/ml after 4 hrs by MTT assay2007Bioorganic & 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.
AID1530772Antiproliferative activity against human Ishikawa cells after 48 hrs by MTT assay2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2.
AID68902Binding affinity for estrogen receptor2001Journal of medicinal chemistry, Mar-29, Volume: 44, Issue:7
Flexible estrogen receptor modulators: design, synthesis, and antagonistic effects in human MCF-7 breast cancer cells.
AID1310520Induction of apoptosis in human HeLa cells assessed as dead cells at 50 uM after 28 hrs by annexin V/FITC/propidium iodide staining-based flow cytometry (Rvb = 1%)2016European journal of medicinal chemistry, Aug-08, Volume: 1184-(1,2-diarylbut-1-en-1-yl)isobutyranilide derivatives as inhibitors of topoisomerase II.
AID71122Relative binding affinity against estrogen receptors in calf uterine cytosol.1989Journal of medicinal chemistry, Dec, Volume: 32, Issue:12
Derivatives of tamoxifen. Dependence of antiestrogenicity on the 4-substituent.
AID1624367Cytotoxicity against human MRC5 cells after 24 hrs by resazurin dye based assay2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Amino acid based prodrugs of a fosmidomycin surrogate as antimalarial and antitubercular agents.
AID68743Antiestrogenic activity in MCF-7-2a cells as concentration required to reduce estradiol effect by 50%2002Journal 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.
AID537735Binding affinity to Candida albicans CaMdr1p expressed in yeast AD1-8u2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID1693881Cytotoxicity against human HSF cells assessed as reduction in colony formation incubated for 7 days by crystal violet staining based assay2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Synthesis, antitumor activity and structure-activity studies of novel pyridoxine-based bioisosteric analogs of estradiol.
AID1069845Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Synthesis of neolignans as microtubule stabilisers.
AID1570855Antitumor activity against mouse 4T1 cells implanted in BALB/c mouse assessed as tumor growth inhibition at 5 mg/kg/day, ip for 2 weeks measured daily during compound dosing by digital caliper method relative to control2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
A Bioreductive Prodrug of Cucurbitacin B Significantly Inhibits Tumor Growth in the 4T1 Xenograft Mice Model.
AID127064Ability to antagonize uterine weight gain in immature mice, at a dose of 750 ug; Activity is expressed as anti-uterotrophic % reduction1991Journal 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.
AID102602In vitro inhibition of MCF-7 cell proliferation compared to 0.1 nM [3H]-estradiol.1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Effect of triphenylacrylonitrile derivatives on estradiol-receptor binding and on human breast cancer cell growth.
AID561220Antifungal activity against Saccharomyces cerevisiae BY4741 at 8 ug/ml by alexa fluor-phalloidin staining2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID136218In vivo inhibition of hormone-dependent MXT mammary tumor in mice1986Journal 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.
AID1480298Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Computer-Aided Discovery and Characterization of Novel Ebola Virus Inhibitors.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current 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.
AID781326pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID344798Displacement of fluorescein labeled estradiol from human recombinant ERbeta expressed in baculovirus infected insect cells by fluorescence polarization assay2008Bioorganic & 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.
AID29139Calculated dissociation constant (pKa, calculated with ACD/pKa)2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID1684753Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay2021Bioorganic & medicinal chemistry letters, 02-01, Volume: 33Synthesis of mitochondria-targeted coumarin-3-carboxamide fluorescent derivatives: Inhibiting mitochondrial TrxR2 and cell proliferation on breast cancer cells.
AID1688069Antiproliferative activity against human MCF-7 cells assessed as inhibition of colony formation measured after 3 weeks by crystal violet staining based soft agar colony formation assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition.
AID1502323Inhibition of ERalpha in human MCF7 cells assessed as reduction in 10 nM estrogen-induced progesterone receptor expression at 1 uM incubated for 24 hrs by Western blot method2017European journal of medicinal chemistry, Nov-10, Volume: 140Novel 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.
AID1866711Selectivity index, ratio of IC50 for human recombinant ERbeta to human recombinant ERalpha2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Rational 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.
AID1705341Antiproliferative activity against human UACC-257 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID324521Increase in light chain 3-GFP+ autophagosome vesicle intensity per cell in human H4 cells at 4.4 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings 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.
AID1705323Antiproliferative activity against human HCC 2998 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID614556Estrogenic activity in Sprague-Dawley rat assessed as increase in uterine weight administered as po daily once for 3 days relative to control2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Design and synthesis of 1,3-biarylsulfanyl derivatives as new anti-breast cancer agents.
AID1465914Inhibition of ERalpha in human MCF7 cells assessed as downregulation of 17beta-estradiol-mediated pS2 mRNA expression at 1 uM preincubated for 4 hrs followed by 17beta-estradiol addition measured after 16 hrs by quantitative RT-PCR analysis2017Journal 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.
AID1312953Aqueous solubility of the compound in PBS after 2 hrs by turbidity assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID1604321Antiparasitic activity against Toxoplasma gondii2019European journal of medicinal chemistry, Dec-01, Volume: 183Recent progress on anti-Toxoplasma drugs discovery: Design, synthesis and screening.
AID501535Antagonist activity at human wild type ERbeta expressed in human HeLa cells co-expressing ERE assessed as inhibition of transactivation activity by luciferase reporter gene assay2010Bioorganic & 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.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID101932Inhibition of estrogen receptor positive MCF-7 cell proliferation as percent treated/control cell number after 10 days at 10e-7 M1981Journal 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.
AID171779Uterotrophic and anti-uterotrophic activities in immature rats at 0.05 mg/kg dose as %agonist:%antagonist = 33:351983Journal 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.
AID673837Cytotoxicity against human MDA-MB-231 cells assessed as cell survival at 10'-7 M relative to vehicle-treated control2012ACS medicinal chemistry letters, Apr-06, Volume: 3, Issue:5
Boron-Based 4-Hydroxytamoxifen Bioisosteres for Treatment of de Novo Tamoxifen Resistant Breast Cancer.
AID1688122Inhibition of bovine brain tubulin polymerisation measured by turbidometric method2020European journal of medicinal chemistry, Feb-15, Volume: 188Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition.
AID1705315Antiproliferative activity against human HOP-62 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID324576Effect on FYVE-RFP+ vesicle intensity per cell in human H4 cells after 2 hrs relative to control2007Proceedings 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.
AID1464223Binding affinity to human ERRgamma2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Design and synthesis of benzoacridines as estrogenic and anti-estrogenic agents.
AID1209426Cytotoxicity against human hepatocytes assessed as reduction in cell viability after 24 hrs by LDH release assay2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
In vitro hepatotoxicity and cytochrome P450 induction and inhibition characteristics of carnosic acid, a dietary supplement with antiadipogenic properties.
AID127057Ability to antagonize uterine weight gain in immature mice, at a dose of 150 ug; Activity is expressed as anti-uterotrophic % reduction1991Journal 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.
AID1533101Inhibition of P-gp-mediated doxorubicin efflux in human Lucena 1 cells assessed as ratio of doxorubicin fluorescence intensity in presence of compound to doxorubicin fluorescence intensity in absence of compound at 12.5 uM preincubated for 1 hr followed b2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors.
AID614548Antiproliferative activity against human Ishikawa cells expressing estrogen receptor after 48 hrs by MTT assay2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Design and synthesis of 1,3-biarylsulfanyl derivatives as new anti-breast cancer agents.
AID1755841Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay2021European journal of medicinal chemistry, Jan-15, Volume: 210Metronidazole-conjugates: A comprehensive review of recent developments towards synthesis and medicinal perspective.
AID1217716Time dependent inhibition of CYP2C8 (unknown origin) at 10 uM by LC/MS system2011Drug 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.
AID1158151Antiproliferative activity against human HCT116 cells after 24 hrs by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Synthesis and anticancer activity of γ-(triazolyl ethylidene)butenolides and polyfunctional pyrrolinones.
AID124182Uterine weight after 9 day treatment at 42 ug by oral gavage to ovariectomised mice without estrone1997Journal 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.
AID493958Inhibition of LuxR-dependent quorum sensing in Vibrio fischeri assessed as reduction of 3-oxo-C6-HSL-induced bioluminescence intensity2010Bioorganic & 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.
AID302176Antiproliferative activity against human HL60 cells assessed as cell viability at 5 ug/ml after 4 hrs by MTT assay2007Bioorganic & 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.
AID723804Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2013European journal of medicinal chemistry, Feb, Volume: 60Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent.
AID1705350Antiproliferative activity against human A498 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological 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.
AID102623Percent of inhibitory activity against proliferation of MCF-7 cells in presence of 10e-6 M concentration of [3H]estradiol (E2).1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Effect of triphenylacrylonitrile derivatives on estradiol-receptor binding and on human breast cancer cell growth.
AID451834Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2009Bioorganic & 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.
AID1327719Anticancer activity against human A549 cells measured after 48 hrs by SRB assay2016Bioorganic & 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.
AID158737Inhibition of calmodulin-dependent Phosphodiesterase1995Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2
Rationally designed analogues of tamoxifen with improved calmodulin antagonism.
AID597271Antiproliferative activity against human MCF7 cells expressing estrogen receptor incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Biomimetic syntheses and antiproliferative activities of racemic, natural (-), and unnnatural (+) glyceollin I.
AID1728101Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs2021European journal of medicinal chemistry, Jan-15, Volume: 210Potent antiproliferative activity of bradykinin B2 receptor selective agonist FR-190997 and analogue structures thereof: A paradox resolved?
AID1387888Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length estrogen receptor beta after 2 hrs by fluorescence polarization assay2018Journal 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.
AID101818Inhibitory concentration against MDA-MB-231 (ER-) cell line using SRB assay2003Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3
A facile synthesis of C(2)-symmetric 17 beta-estradiol dimers.
AID1752648Antiproliferative activity against ER-negative human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay2021Bioorganic & medicinal chemistry, 10-01, Volume: 47Benzothiophene derivatives as selective estrogen receptor covalent antagonists: Design, synthesis and anti-ERα activities.
AID548940Growth inhibition of human MCF7 cells at 25 ug/ml after 24 hrs by MTT colorimetric assay2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Isochaihulactone analogues: synthesis and anti-proliferative activity of novel dibenzylbutyrolactones.
AID604747Aqueous solubility of the compound in phosphate buffer solution of pH 7.4 after 24 hrs by LC-UV analysis2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions.
AID678557Cytotoxicity against mouse Neuro2a cells after 72 hrs by WST1 assay in presence of 20% FBS2012Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
Synthesis and cytotoxic activity of non-naturally substituted 4-oxycoumarin derivatives.
AID1217705Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system2011Drug 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.
AID736610Growth inhibition of estrogen-independent human MDA-MB-231 cells2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Synthesis and growth inhibition activity of fluorinated derivatives of tamoxifen.
AID102754Effect on hormone-dependent MCF-7 human breast cancer cell proliferation at 1x10E-5 M1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Indolo[2,1-a]isoquinolines. Syntheses, steroid hormone receptor binding affinities, and cytostatic activity.
AID242704Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor beta; ERE assay2005Journal 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.
AID1193498Thermodynamic equilibrium solubility, log S of the compound simulated gastric fluid at pH 1.2 at RT after 24 hrs by shake-flask method2015Bioorganic & 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.
AID311934Dissociation constant, pKa of the compound2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID1283262Inhibition of DR24 in human SLOS fibroblasts assessed as decrease in 7-DHC levels at 10 nM after 5 days by LC-MS/GC-MS analysis2016Journal 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.
AID1210017Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1254843Selectivity index, ratio of IC50 for normal human astrocytes to IC50 for human GBM1 cells2015European journal of medicinal chemistry, Oct-20, Volume: 103Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID1217704Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system2011Drug 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.
AID101930Effect on [3H]thymidine incorporation into estrogen receptor positive MCF-7 human breast carcinoma cells at 10e-6 M (ex 2)1987Journal 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.
AID1227984Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated at 37 degC for 3 days by resazurin microplate assay2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Eremophilane Sesquiterpenes and Diphenyl Thioethers from the Soil Fungus Penicillium copticola PSU-RSPG138.
AID764644Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of novel triaryl (Z)-olefins as tamoxifen analogues.
AID1705316Antiproliferative activity against human HOP-92 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1415057Aqueous solubility of the compound in simulated intestinal fluid2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.
AID471241Agonist activity at estrogen receptor in human Ishikawa cells assessed as 17-beta-estradiol-induced alkaline phosphatase activity at 10 uM after 3 days by chemiluminescence assay2009Journal 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.
AID135693Anti-uterotrophic effect in hormone-dependent transplant MXT bearing mice as relative uterine weight in treated and control mice at 8.8 mg (control=100+/-24)1991Journal 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.
AID1193496Thermodynamic equilibrium solubility, log S of the compound in water at RT after 24 hrs by shake-flask method2015Bioorganic & 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.
AID1310526Inhibition of human recombinant topoisomerase 2 alpha-mediated relaxation of supercoiled pBR322 plasmid DNA at 50 to 100 uM after 60 mins by electrophoretic analysis2016European journal of medicinal chemistry, Aug-08, Volume: 1184-(1,2-diarylbut-1-en-1-yl)isobutyranilide derivatives as inhibitors of topoisomerase II.
AID191704Uterotrophic effect as uterine weight gain in rats at 1 mg/kg/day oral dose for 4 days2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
4-(4-alkylpiperazin-1-yl)phenyl group: a novel class of basic side chains for selective estrogen receptor modulators.
AID1310521Induction of mitochondrial membrane depolarization in human HeLa cells after 28 hrs by JC-1 staining-based flow cytometric analysis2016European journal of medicinal chemistry, Aug-08, Volume: 1184-(1,2-diarylbut-1-en-1-yl)isobutyranilide derivatives as inhibitors of topoisomerase II.
AID1164490Antiproliferative activity human ER-positive MCF7 cells after 2 days by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of new estradiol-cationic lipid hybrids: ten-carbon twin chain cationic lipid is a more suitable partner for estradiol to elicit better anticancer activity.
AID1385440Antitumor activity against human MCF7 cells xenografted in nude Balb/c mouse assessed as tumor growth inhibition at 25 mg/kg, po administered once every 2 days via gavage measured on day 272018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Novel Hybrid Conjugates with Dual Suppression of Estrogenic and Inflammatory Activities Display Significantly Improved Potency against Breast Cancer.
AID1387893Estrogenic activity at estrogen receptor alpha/beta in human Ishikawa cells at 1 uM after 72 hrs by alkaline phosphatase assay relative to estradiol2018Journal 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.
AID185420Percent inhibition of estradiol stimulated uterine growth in rats1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans.
AID561041Antifungal activity against Candida albicans SC5314 infected in BALB/c mouse assessed as fungal count per gram of kidney at 200 mg/kg, po administered for 7 days prior to fungal infection2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID1191565Antiproliferative activity against human MCF7 cells after 5 days by WST-8 assay2015Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
Structure-activity relationship study of diphenylamine-based estrogen receptor (ER) antagonists.
AID723801Antiproliferative activity against mouse NIH/3T3 cells after 48 hrs by MTT assay2013European journal of medicinal chemistry, Feb, Volume: 60Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent.
AID1705325Antiproliferative activity against human HCT-15 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1065297Cytotoxicity against human COLO320DM cells after 48 hrs by MTT assay2013European journal of medicinal chemistry, Aug, Volume: 66Diversity-oriented synthesis of α-aminophosphonates: a new class of potential anticancer agents.
AID1705351Antiproliferative activity against human ACHN cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal 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.
AID1061211Inhibition 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 control2014European journal of medicinal chemistry, Jan, Volume: 71A novel tamoxifen derivative, ridaifen-F, is a nonpeptidic small-molecule proteasome inhibitor.
AID1866707Cytotoxicity against human HEK293 cells assessed as cell viability after 24 hrs by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Rational 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.
AID1443552Induction of ERalpha degradation in human MCF7 cells assessed as remaining ERalpha protein level at 10 uM after 18 to 24 hrs by Western blot analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer.
AID1705363Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1768147Oral bioavailability in Sprague-Dawley rat at 5 mg/kg measured after 0.083 to 24 hrs by LC/MS/MS analysis
AID1688067Antiproliferative activity against human MCF-7 cells assessed as proportion of dead cells at 5.39 ug/ml measured after 3 weeks by crystal violet staining based soft agar colony formation assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition.
AID270145Cytotoxicity against human SW620 cells2006Journal 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.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current 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.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID268618Displacement of [6,7-3H]17 beta-estradiol from human recombinant ERalpha relative to estradiol2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
m-Carborane bisphenol structure as a pharmacophore for selective estrogen receptor modulators.
AID1197745Inhibition of human OATP1B3-mediated [3H]CCK-8 at 100 uM after 5 mins relative to control2015European journal of medicinal chemistry, Mar-06, Volume: 92Interaction of human organic anion transporter polypeptides 1B1 and 1B3 with antineoplastic compounds.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1217706Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system2011Drug 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.
AID1242126Anti-proliferative activity against human MCF7 cells incubated for 48 hrs by SRB assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Design, synthesis and anticancer properties of novel oxa/azaspiro[4,5]trienones as potent apoptosis inducers through mitochondrial disruption.
AID620855Binding affinity to bovine serum albumin at pH 7.4 by Stern-Volmer plot2011European 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.
AID501536Agonist activity at human wild type ERbeta expressed in human HeLa cells co-expressing AP-1 assessed as transactivation activity by luciferase reporter gene assay2010Bioorganic & 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.
AID103542Inhibition of MCF-7 cell proliferation at 10 nM1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Carboxylic acid analogues of tamoxifen: (Z)-2-[p-(1, 2-diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine. Estrogen receptor affinity and estrogen antagonist effects in MCF-7 cells.
AID1161695Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 96 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents.
AID69235Displacement of [3H]tamoxifen from AEBS of EL4 cells1992Journal 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.
AID1693878Therapeutic index, ratio of CC50 for human HSF cells to IC50 for ER and PR-positive human MCF7 cells2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Synthesis, antitumor activity and structure-activity studies of novel pyridoxine-based bioisosteric analogs of estradiol.
AID588214FDA HLAED, liver enzyme composite activity2004Current 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.
AID695957Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
New prenylated isoflavonoids as protein tyrosine phosphatase 1B (PTP1B) inhibitors from Erythrina addisoniae.
AID179471Percentage progressive DMBA-induced mammary tumors in rats at 3 mg dose (experiment-1)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity.
AID561219Antifungal activity against Saccharomyces cerevisiae BY4741 assessed as appearance of unbudded cells with more than one nucleus at 8 ug/ml2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID324583Increase in long-lived protein degradation in human H4 cells after 2 hrs relative to control2007Proceedings 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.
AID1533116Inhibition of P-gp-mediated Rho-123 efflux in human Lucena 1 cells at 25 uM preincubated for 1 hr followed by Rho-123 addition measured after 1 hr by flow cytometry2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors.
AID115227Inhibition of estradiol-induced uterine weight gain in ovariectomized BALB/c mice at 3 ug dose twice daily; nonsignificant1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Synthesis and biological activity of new halo-steroidal antiestrogens.
AID1562213Antiproliferative activity against human A2058 cells assessed as cell viability at 50 uM measured after 24 hrs by celltiter-blue assay relative to control2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Nitric Oxide-Releasing Selective Estrogen Receptor Modulators: A Bifunctional Approach to Improve the Therapeutic Index.
AID135914Uterotrophic effect in BDF1 mouse at a dose of 8 mg1988Journal 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.
AID101644Cytostatic effect on hormone-independent MDA-MB 231 human breast cancer cell proliferation at 1x10E-6M1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Indolo[2,1-a]isoquinolines. Syntheses, steroid hormone receptor binding affinities, and cytostatic activity.
AID1646798Chaperone activity at GCase L444P GBA gene mutant in human fibroblasts derived from Gaucher patient assessed as increase in GPN-induced reduction of calcium release using Fluo-8AM based fluorescence assay relative to control2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells.
AID103394Growth inhibitory activity against MCF-7 human breast tumor cell line at a concentration of 10e-8 M in vitro.1989Journal of medicinal chemistry, Dec, Volume: 32, Issue:12
Derivatives of tamoxifen. Dependence of antiestrogenicity on the 4-substituent.
AID134511In vivo inhibition of uterine growth in hormone-dependent MXT mammary tumor bearing mice1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
2-Alkyl-substituted 1,1-bis(4-acetoxyphenyl)-2-phenylethenes. Estrogen receptor affinity, estrogenic and antiestrogenic properties, and mammary tumor inhibiting activity.
AID1366600Selectivity index, ratio of IC50 for HEK293 cells to IC50 for human MDA-MB-231 cells2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Syntheses of conformationally restricted benzopyran based triarylethylenes as growth inhibitors of carcinoma cells.
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID103600Agonistic activity in MCF-7 cell proliferation.1992Journal 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.
AID101929Effect on [3H]thymidine incorporation into estrogen receptor positive MCF-7 human breast carcinoma cells at 10e-7 M1987Journal 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.
AID1283264Inhibition of delta 8-7 isomerase in human SLOS fibroblasts assessed as decrease in 7-DHC levels at 10 nM after 5 days by LC-MS/GC-MS analysis2016Journal 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.
AID191973The compound was tested for the growth of mammary tumors in rats at 10 mg/kg dose after peroral administration at the end of the exp-21984Journal 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
AID1628319Antiestrogenic activity in human MCF7 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 assay2016Journal of natural products, 05-27, Volume: 79, Issue:5
Furofuran Lignan Glucosides with Estrogen-Inhibitory Properties from the Bangladeshi Medicinal Plant Terminalia citrina.
AID1705371Antiproliferative activity against human renal cancer cells2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID15714CLog P was determined2003Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3
A facile synthesis of C(2)-symmetric 17 beta-estradiol dimers.
AID1500964Inhibition of estrogen receptor in human MCF7 cells assessed as inhibition of estradiol-induced PgR mRNA expression at 2 uM by RT-PCR method relative to control2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel 2-methoxyestradiol analogs as dual selective estrogen receptor modulators (SERMs) and antiangiogenic agents.
AID184865Minimum effective dose at which significant increase in uterine weight/body weight in rat was determined (in vivo)1997Journal 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.
AID1705327Antiproliferative activity against human KM12 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1395069Displacement of Fluormone ES2 Green from full length human ER-alpha expressed in insect cells after 2 hrs by fluorescence polarization assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ERα/VEGFR-2 ligands with anti-breast cancer activity.
AID1705356Antiproliferative activity against human PC-3 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID191694Uterotrophic effect in rats uterine at 50 ug/day dose in the presence of 0.1 ug estradiol1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent.
AID1464646Cytotoxicity against human MCF7 cells at 10 ug/ml after 72 hrs by resazurin based fluorescence assay2017Bioorganic & medicinal chemistry letters, 10-15, Volume: 27, Issue:20
Synthesis and evaluation of the NSCLC anti-cancer activity and physical properties of 4-aryl-N-phenylpyrimidin-2-amines.
AID1210015Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID677854Selectivity ratio of IC50 for ERalpha receptor LBD expressed in yeast AH109 cells to IC50 for ERbeta receptor LBD expressed in yeast AH109 cells2012European journal of medicinal chemistry, Aug, Volume: 54Discovery and structure-activity analysis of selective estrogen receptor modulators via similarity-based virtual screening.
AID1401996Cytostatic activity against human MCF7 cells2018European journal of medicinal chemistry, Jan-01, Volume: 143Tamoxifen a pioneering drug: An update on the therapeutic potential of tamoxifen derivatives.
AID102435Effective dose for [3H]- estradiol against proliferation of MCF-7 cells1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Effect of triphenylacrylonitrile derivatives on estradiol-receptor binding and on human breast cancer cell growth.
AID186921The compound was tested for uterotropic activity in immature rats(Dosage 1000 ug)1984Journal 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
AID1530773Effect on progesterone receptor mRNA expression in non-stimulated human MCF7 cells at 1 uM by SYBR green dye based RT-PCR analysis2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2.
AID250368Percent agonist activity against human breast adenocarcinoma (MCF-7) cell proliferation2005Journal 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.
AID1283247Inhibition of delta 8-7 isomerase in mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis2016Journal 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.
AID1284373Displacement of [3H]-E2 from human ER-alpha incubated for 16 to 20 hrs by liquid scintillation counting analysis2016European journal of medicinal chemistry, Apr-13, Volume: 112Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
AID756454Antiproliferative activity against human HeLa cells after 72 hrs by trypan blue assay2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and biological evaluation of novel tamoxifen analogues.
AID1465899Cytotoxicity against human MCF7 cells assessed as cell viability up to 100 uM after 24 hrs by MTT assay2017Journal 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.
AID1693874Cytotoxicity against ER and PR-positive human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Synthesis, antitumor activity and structure-activity studies of novel pyridoxine-based bioisosteric analogs of estradiol.
AID1578361Selectivity index, ratio of CC50 for mouse RAW264.7 cells to MIC90 for antimycobacterial activity against Mycobacterium tuberculosis H37Rv2020European journal of medicinal chemistry, Jan-01, Volume: 185Novel thiazolidinedione-hydroxamates as inhibitors of Mycobacterium tuberculosis virulence factor Zmp1.
AID1688061Antiproliferative activity against human MCF-7 cells assessed as proportion of live cells at 26.95 ug/ml measured after 3 weeks by crystal violet staining based soft agar colony formation assay (Rvb = 100%)2020European journal of medicinal chemistry, Feb-15, Volume: 188Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition.
AID1443579Antitumor activity against human MCF7 cells xenografted in 17-beta estradiol release pellet implanted immunocompromised nude mouse assessed as tumor growth inhibition at 60 mg/kg, po administered 5 times per week measured on day 108 relative to control2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer.
AID1387882Cytotoxicity against human MCF7 cells assessed as reduction in cell viability at 10 uM by CytoTox 96 non-radioactive LDH cytotoxicity assay2018Journal 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.
AID482348Antagonist activity at ERbeta expressed in yeast assessed as inhibition of E2-induced alpha-galactosidase activity2010Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14
Discovery of potent ligands for estrogen receptor beta by structure-based virtual screening.
AID1754372Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by cell-titer 96 aqueous one solution cell proliferation assay2021Bioorganic & medicinal chemistry, 07-01, Volume: 41Iodinated 1,2-diacylhydrazines, benzohydrazide-hydrazones and their analogues as dual antimicrobial and cytotoxic agents.
AID397943Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 48 hrs by MTT assay2009Bioorganic & 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.
AID102416Effect of compound on the growth of MCF-7 cells at a concentration of,10 e-6 M, percentage of control value being 631985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Hydroxy derivatives of tamoxifen.
AID71135Relative binding affinity for estrogen receptor of calf uterine cytosol1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Synthesis, conformational considerations, and estrogen receptor binding of diastereoisomers and enantiomers of 1-[4-[2-(dimethylamino)ethoxy]phenyl]-1,2-diphenylbutane (dihydrotamoxifen).
AID499834Antiestrogenic activity in human MCF7 cells xenografted in ovariectomized Nu/Nu mouse assessed as decrease of estradiol-induced tumor volume at 50 mg/kg, daily once for 21 days2010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Effects of 7-O substitutions on estrogenic and anti-estrogenic activities of daidzein analogues in MCF-7 breast cancer cells.
AID1636395Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 25.3 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of N2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID69837Relative binding affinity to the estrogen receptor in lamb uterus cytosol1997Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
Cytotoxicity and antiestrogenicity of a novel series of basic diphenylethylenes.
AID679077TP_TRANSPORTER: transepithelial transport of Rhodamine 123 (basal to apical) in Caco-2 cells2004Biopharmaceutics & drug disposition, Oct, Volume: 25, Issue:7
Interactions of tamoxifen, N-desmethyltamoxifen and 4-hydroxytamoxifen with P-glycoprotein and CYP3A.
AID38611Relative binding affinity for antiestrogen binding site (AEBS) of calf uterus cytosol1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Effect of triphenylacrylonitrile derivatives on estradiol-receptor binding and on human breast cancer cell growth.
AID1628318Antiestrogenic activity in human MCF7 cells assessed as compound concentration required to decrease 100 pM E2-induced cell proliferation to equivalent levels induced by 10 pM E2 after 96 hrs by alamar blue assay2016Journal of natural products, 05-27, Volume: 79, Issue:5
Furofuran Lignan Glucosides with Estrogen-Inhibitory Properties from the Bangladeshi Medicinal Plant Terminalia citrina.
AID134363Antiestrogenic effect in immature mouse at a dose of 1 ug.1986Journal 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.
AID103380Percent agonistic activity in MCF-7 breast tumor cells using MCF-7 assay2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.
AID276692Antagonist activity at ER receptor assessed as inhibition of increase in uterine weight of Sprague-Dawley rat at 3 mg/kg/day, po relative to 17-alpha-ethynylestradiol2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
Rapid synthesis of 4-benzylidene and 4-[bis-(4-methoxyphenyl)-methylene-2-substituted phenyl-benzopyrans as potential selective estrogen receptor modulators (SERMs) using McMurry coupling reaction.
AID1576204Antiproliferative activity against human M-HeLa cells assessed as reduction in cell viability after 24 hrs by DAPI/propidium iodide staining based assay2019MedChemComm, Aug-01, Volume: 10, Issue:8
Synthesis and anti-cancer activities of glycosides and glycoconjugates of diterpenoid isosteviol.
AID604743Displacement of radiolabeled warfarin from fatty acid containing human serum albumin site 1 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions.
AID230360Relative binding affinity as ratio of molar concentrations of E/Z-4-OHT to compound required to displace 50% [3H]E2 from MCF-7 cell lysates2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Design, synthesis, and biological evaluation of doxorubicin-formaldehyde conjugates targeted to breast cancer cells.
AID1705309Antiproliferative activity against human HL-60(TB) cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1754979Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Design, synthesis and broad spectrum antibreast cancer activity of diarylindoles via induction of apoptosis in aggressive breast cancer cells.
AID69397Displacement of [3H]estradiol from estrogen receptor in rat uterine cytosol1982Journal of medicinal chemistry, Feb, Volume: 25, Issue:2
Antiestrogen basicity--activity relationships: a comparison of the estrogen receptor binding and antiuterotrophic potencies of several analogues of (Z)-1,2-diphenyl-1-[4-[2-(dimethylamino)ethoxy]phenyl]-1-butene (tamoxifen, Nolvadex) having altered basici
AID1422688Cytotoxicity against human HepG2 cells after 24 hrs by resazurin dye-based fluorescence analysis2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Antifungal benzo[b]thiophene 1,1-dioxide IMPDH inhibitors exhibit pan-assay interference (PAINS) profiles.
AID589145Mechanism based inhibition of human cytochrome P450 3A4 measured by testosterone 6-beta hydroxylation2005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1415060Apparent permeability across basolateral to apical side in human Caco2 cells at pH 6.5 to 7.5 after 2 hrs by LC/MS/MS analysis2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.
AID497606Cytotoxicity against human MCF7 cells assessed as reduction of cell proliferation at 1 nM to 1 uM after 96 hrs by MTT assay2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha.
AID248055Antiproliferative activity in MCF-7 human breast cancer cells2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Antitumor-active cobalt-alkyne complexes derived from acetylsalicylic acid: studies on the mode of drug action.
AID1553349Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 72 hrs by resazurin dye-based fluorimetric analysis2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors (Part 2).
AID1693879Cytotoxicity against ER and PR-positive human MCF7 cells assessed as reduction in colony formation incubated for 7 days by crystal violet staining based assay2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Synthesis, antitumor activity and structure-activity studies of novel pyridoxine-based bioisosteric analogs of estradiol.
AID1438380Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 120 hrs by MTT assay2017European journal of medicinal chemistry, Mar-10, Volume: 128Synthesis and biological evaluation of fluorinated N-benzoyl and N-phenylacetoyl derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as steroid sulfatase inhibitors.
AID718399Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Synthesis and docking studies of novel antitumor benzimidazoles.
AID667234Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel (E) stilbene-based antitumor agents.
AID1703747Aqueous solubility of compound in phosphate-buffered saline at pH 7.4 incubated for 2 hrs by turbidometric analysis2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID604742Displacement of radiolabeled dansylsarcosine from fatty acid-free human serum albumin site 2 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions.
AID173693Percent decrease in serum cholesterol relative to OVX control at 1 mg/kg in rat1997Journal 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.
AID1415061Half life in human liver microsomes in presence of NADPH by LC-MS/MS analysis2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.
AID124183Uterine weight after 9 day treatment at 42 ug by oral gavage to ovariectomised mice with estrone1997Journal 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.
AID276685Agonist activity at ER receptor assessed as increase in uterine weight of Sprague-Dawley rat at 3 mg/kg/day, po2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
Rapid synthesis of 4-benzylidene and 4-[bis-(4-methoxyphenyl)-methylene-2-substituted phenyl-benzopyrans as potential selective estrogen receptor modulators (SERMs) using McMurry coupling reaction.
AID625276FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID1395368Cytotoxicity against human MRC5 SV2 cells after 72 hrs by resazurin dye-based fluorimetric analysis2018European journal of medicinal chemistry, May-10, Volume: 151Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives.
AID667228Cytotoxicity against human A253 cells after 96 hrs by SRB assay2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel (E) stilbene-based antitumor agents.
AID1546176Growth inhibition of human SiHa cells2019European journal of medicinal chemistry, Dec-15, Volume: 184Current scenario of tetrazole hybrids for antibacterial activity.
AID69688Relative binding affinity against estrogen receptor(ER)1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans.
AID1684752Cytotoxicity against human SK-BR-3 cells after 48 hrs by MTT assay2021Bioorganic & medicinal chemistry letters, 02-01, Volume: 33Synthesis of mitochondria-targeted coumarin-3-carboxamide fluorescent derivatives: Inhibiting mitochondrial TrxR2 and cell proliferation on breast cancer cells.
AID471243Uterotropic activity in rat assessed as inhibition of estrone-stimulated uterine weight at 1 mg/kg, po QD after 3 days2009Journal 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.
AID302758Solubility by shake flask method2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Poorly soluble marketed drugs display solvation limited solubility.
AID561231Antifungal activity against Cryptococcus neoformans KN99alpha after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID1471125Antiproliferative activity against ER positive human MCF7 cells after 48 hrs by MTT assay2017Bioorganic & 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.
AID302177Antiproliferative activity against human HL60 cells assessed as cell viability at 10 ug/ml after 4 hrs by MTT assay2007Bioorganic & 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.
AID103057Inhibition of hormone-sensitive MCF-7 mammary tumor cell proliferation at 1*10e-6 M1992Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19
6-Alkyl-12-formylindolo[2,1-a]isoquinolines. Syntheses, estrogen receptor binding affinities, and stereospecific cytostatic activity.
AID1705370Antiproliferative activity against human ovarian cancer cells2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1911288Antitumor activity against tamoxifen-resistant human LCC2 cells xenografted in BALB/C mouse assessed as tumor growth inhibition at 20 mg/kg, po measured every 2 days for 22 days2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Discovery of Novel Bicyclic Phenylselenyl-Containing Hybrids: An Orally Bioavailable, Potential, and Multiacting Class of Estrogen Receptor Modulators against Endocrine-Resistant Breast Cancer.
AID101928Effect on [3H]-thymidine incorporation into estrogen receptor positive MCF-7 human breast carcinoma cells at 10e-6 M1987Journal 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.
AID1666651Selectivity ratio of IC50 for displacement of fluorescent estrogen ligand from recombinant human full length untagged ERbeta expressed in baculovirus infected insect cells to IC50 for displacement of fluorescent estrogen ligand from recombinant human full2020Bioorganic & 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.
AID482357Antiproliferative activity against human MCF7 cells assessed as viable cells at 100 uM after 24 hrs by MTT assay2010Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14
Discovery of potent ligands for estrogen receptor beta by structure-based virtual screening.
AID69365Relative binding affinity against estrogen receptor in cytosol assay1986Journal 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.
AID1705319Antiproliferative activity against human NCI-H322M cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1732431Cytotoxicity against HEK293 cells assessed as cell viability after 20 hrs by fluorescence assay2021Bioorganic & medicinal chemistry letters, 05-01, Volume: 39Design, synthesis and bioactivity evaluation of novel pyrazole linked phenylthiazole derivatives in context of antibacterial activity.
AID101938Inhibition of estrogen receptor positive MCF-7 cell proliferation as percent treated/control cell number after 10 days at 10e-8 M1981Journal 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.
AID1609742Cytotoxicity against human MCF7 cells assessed as reduction in cell viability at 0.1 to 100 uM incubated for 24 hrs by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Single-molecule chemiluminescent photosensitizer for a self-activating and tumor-selective photodynamic therapy of cancer.
AID1469733Antitumor activity against human MCF7 cells xenografted in NOD SCID gamma mouse assessed as change in tumor volume at 60 mg/kg, po 5 days per week for 48 days post tumor implantation measured 7 hrs post last dose2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.
AID1705364Antiproliferative activity against human OVCAR-8 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1401995Displacement of [3H]E2 from human recombinant ERalpha assessed as receptor binding after 45 mins by scintillation counting method2018European journal of medicinal chemistry, Jan-01, Volume: 143Tamoxifen a pioneering drug: An update on the therapeutic potential of tamoxifen derivatives.
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1389793Effect on PgR mRNA expression in human MCF7 cells at 1 uM by SYBR Green dye based RT-PCR analysis2018Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6
Synthesis and biological evaluation of 4,6-diaryl-2-pyrimidinamine derivatives as anti-breast cancer agents.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1705348Antiproliferative activity against human SK-OV-3 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID306819Cell viability of estrogen receptor positive MCF7 cells at 5 uM after 48 hrs by MTT assay relative to DMSO2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Identification of a series of tetrahydroisoquinoline derivatives as potential therapeutic agents for breast cancer.
AID102759Effect on [3H]thymidine incorporation into MCF-7 human breast cancer cells at 1x10E-6M1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Indolo[2,1-a]isoquinolines. Syntheses, steroid hormone receptor binding affinities, and cytostatic activity.
AID470167Antiestrogenic activity in human T47D cells assessed as drug level causing inhibition of 100 pM E2-enhanced cell proliferation to level equivalent to 10 pM E2 after 96 hrs by alamar blue assay2009Journal of natural products, Nov, Volume: 72, Issue:11
Antiestrogenic constituents of the Thai medicinal plants Capparis flavicans and Vitex glabrata.
AID1652345Antitumor activity against human MCF7:TAM1 cells xenografted in ovariectomized athymic Nude-Foxn1 mouse assessed as tumor growth inhibition at 50 mg/kg/day, po administered via gavage for 4 weeks2020Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.
AID678721Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID102274Inhibition of [3H]thymidine incorporation into hormone sensitive MCF-7 human breast cancer cells at 10e-6 M1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity.
AID1768140Induction of estrogen receptor degradation in human MCF7 cells at 0.0002 to 100 nM incubated for 4 hrs by Alexafluor-488 conjugate anti-mouse IgG staining based fluorescence method relative to control
AID676725Antimicrobial activity against Bacillus subtilis DSM 347 incubated for 5 hrs by resazurin dye based assay2012Journal of natural products, Jul-27, Volume: 75, Issue:7
Geranylphenazinediol, an acetylcholinesterase inhibitor produced by a Streptomyces species.
AID1602140Antiproliferative activity against human T47D cells after 24 hrs by MTT assay2019European journal of medicinal chemistry, Mar-15, Volume: 166Structure-based drug design, synthesis, In vitro, and In vivo biological evaluation of indole-based biomimetic analogs targeting estrogen receptor-α inhibition.
AID597275Antiproliferative activity against androgen receptor-deficient human PC3 cells incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Biomimetic syntheses and antiproliferative activities of racemic, natural (-), and unnnatural (+) glyceollin I.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1705330Antiproliferative activity against human SF-539 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1688054Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth measured after 48 hrs by SRB assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition.
AID184864Minimum effective dose at which significant increase in uterine eosinophil peroxidase (EPO) activity in rat was determined (in vivo)1997Journal 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.
AID1193492Thermodynamic equilibrium solubility, log S of the compound in water at RT after 4 hrs by 96 well plate method2015Bioorganic & 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.
AID1310514Cytotoxicity against human A2780 cells assessed as cell growth inhibition after 72 hrs by MTS assay2016European journal of medicinal chemistry, Aug-08, Volume: 1184-(1,2-diarylbut-1-en-1-yl)isobutyranilide derivatives as inhibitors of topoisomerase II.
AID561230Antifungal activity against Cryptococcus neoformans NYS3-81 after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID765190Antiproliferative activity against human K562 cells after 48 hrs by MTT assay2013Bioorganic & 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.
AID103428Cytotoxicity against MCF-7 cells in presence of 1 uM E2 (estradiol)1997Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
Cytotoxicity and antiestrogenicity of a novel series of basic diphenylethylenes.
AID451831Estrogenic agonistic activity in bilaterally ovariectomized Sprague-Dawley rat assessed as uterine weight gain at 10 mg/kg, po once daily for three days measured on day 31 of age2009Bioorganic & 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.
AID1705307Antiproliferative activity against human SR cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID101760Percent inhibition of estrogen receptor positive MCF-7 human breast cancer cell proliferation at 10e-7 M1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
Molecular structures and conformational studies of triarylcyclopropyl and related nonsteroidal antiestrogens.
AID71140Relative binding affinity for the calf uterine estrogen receptor.1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Platinum complexes with binding affinity for the estrogen receptor.
AID1763180Cytotoxicity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 05-15, Volume: 38Design, synthesis and molecular docking studies of thymol based 1,2,3-triazole hybrids as thymidylate synthase inhibitors and apoptosis inducers against breast cancer cells.
AID471238Displacement of radiolabeled estrogen from estrogen receptor alpha by scintillation counting2009Journal 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.
AID1217728Intrinsic clearance for reactive metabolites formation per mg of protein based on cytochrome P450 (unknown origin) inactivation rate by TDI assay2011Drug 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.
AID681155TP_TRANSPORTER: increase in bodipy intracellular accumulation (Bodipy: 0.2 uM) in SK-E2 cells (expressing BSEP)2003Pharmaceutical research, Apr, Volume: 20, Issue:4
Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites.
AID1387905Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length untagged estrogen receptor alpha expressed in Spodoptera frugiperda by fluorescence polarization assay2018Journal 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.
AID1830575Displacement of fluorescent labeled-ligand from ERalpha (unknown origin) by competitive binding assay2021Bioorganic & medicinal chemistry letters, 11-15, Volume: 52Searching for an ideal SERM: Mining tamoxifen structure-activity relationships.
AID1576203Cytotoxicity against human Chang liver cells assessed as reduction in cell viability after 24 hrs by DAPI/propidium iodide staining based assay2019MedChemComm, Aug-01, Volume: 10, Issue:8
Synthesis and anti-cancer activities of glycosides and glycoconjugates of diterpenoid isosteviol.
AID1079933Acute 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
AID1705328Antiproliferative activity against human SW-620 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1284693Cytotoxicity against human HCT15 cells assessed as growth inhibition after 48 hrs by SRB assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
AID188606The compound was tested for no of tumors without change at 10 mg/kg dose after peroral administration (experiment-2)1984Journal 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
AID1546177Growth inhibition of human MDA-MB-231 cells2019European journal of medicinal chemistry, Dec-15, Volume: 184Current scenario of tetrazole hybrids for antibacterial activity.
AID480628Displacement of [3H]estradiol from human ERalpha expressed in african green monkey COS1 cells assessed as relative binding affinity after 2 hrs by liquid scintillation counting relative to estradiol2010Bioorganic & 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.
AID188600The compound was tested for no of tumors with complete remission at 10 mg/kg dose after peroral administration (experiment-2)1984Journal 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
AID747465Antagonist activity at human estrogen receptor-beta by yeast two-hybrid assay in presence of SRC12013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Discovery of natural estrogen receptor modulators with structure-based virtual screening.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug 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.
AID765188Antiproliferative activity against human Bel7402 cells after 48 hrs by MTT assay2013Bioorganic & 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.
AID1705314Antiproliferative activity against human EKVX cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID676726Toxicity against human KIF5 cells incubated for 24 hrs by CellTiter Blue cell viability assay2012Journal of natural products, Jul-27, Volume: 75, Issue:7
Geranylphenazinediol, an acetylcholinesterase inhibitor produced by a Streptomyces species.
AID615401Cytotoxicity activity against human MCF7 cells by MTS assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Design, synthesis and bioevaluation of novel candidate selective estrogen receptor modulators.
AID1705337Antiproliferative activity against human MDA-MB-435 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID136774Percentage reduction in estradiol-stimulated uterotrophic effect of immature mice at 150 ug1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
Molecular structures and conformational studies of triarylcyclopropyl and related nonsteroidal antiestrogens.
AID42278Inhibitory activity against proliferation of BT-20 cells in presence of TPE at 10e-5 M concentration.1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Effect of triphenylacrylonitrile derivatives on estradiol-receptor binding and on human breast cancer cell growth.
AID679347TP_TRANSPORTER: transepithelial transport in Caco-2 cells2004Biopharmaceutics & drug disposition, Oct, Volume: 25, Issue:7
Interactions of tamoxifen, N-desmethyltamoxifen and 4-hydroxytamoxifen with P-glycoprotein and CYP3A.
AID276682Displacement of [3H]estradiol from ER in rat uterus at 3 mg/kg/day relative to estradiol2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
Rapid synthesis of 4-benzylidene and 4-[bis-(4-methoxyphenyl)-methylene-2-substituted phenyl-benzopyrans as potential selective estrogen receptor modulators (SERMs) using McMurry coupling reaction.
AID187060Estrogenic activity as mean uterine weight in rats on 10 ug dose1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans.
AID101921Effect on [3H]thymidine incorporation into estrogen receptor positive MCF-7 human breast carcinoma cells at 10e-6 M (ex 2)1987Journal 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.
AID1395723Cytotoxicity against human DLD1 cells preincubated for 4 hrs followed by incubation in compound free media for 24 hrs by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Antiproliferative efficacy of curcumin mimics through microtubule destabilization.
AID1578360Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability after 24 hrs by neutral red dye based assay2020European journal of medicinal chemistry, Jan-01, Volume: 185Novel thiazolidinedione-hydroxamates as inhibitors of Mycobacterium tuberculosis virulence factor Zmp1.
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1464222Displacement of [3H]E2 from GST-fused ERbeta-LBD (unknown origin) expressed in Escherichia coli BL21 incubated for 1 hr by liquid scintillation counting method2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Design and synthesis of benzoacridines as estrogenic and anti-estrogenic agents.
AID1662872Cytotoxicity against human HepG2 cells2020Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13
Design and synthesis of amphiphilic 2-hydroxybenzylphosphonium salts with antimicrobial and antitumor dual action.
AID1752365Antitumor activity against human MCF7 cells xenografted in mouse assessed as tumor growth inhibition at 60 mg/kg, po QD for 4 weeks2021Bioorganic & medicinal chemistry letters, 10-15, Volume: 50Discovery of GNE-502 as an orally bioavailable and potent degrader for estrogen receptor positive breast cancer.
AID1464221Displacement of [3H]E2 from GST-fused ERalpha-LBD (unknown origin) expressed in Escherichia coli BL21 incubated for 1 hr by liquid scintillation counting method2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Design and synthesis of benzoacridines as estrogenic and anti-estrogenic agents.
AID471239Antagonist activity at estrogen receptor in human Ishikawa cells assessed as 17-beta-estradiol-induced alkaline phosphatase activity after 3 days by chemiluminescence assay2009Journal 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.
AID1350727Aqueous solubility in PBS buffer at pH 7.4 at 100 uM after 1 hr by LC-MS/MS analysis2018Journal 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.
AID239849Relative binding affinity (RBA) for human recombinant estrogen receptor alpha compared to [3H]-Estradiol at 4 nM2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Potent estrogen receptor ligands based on bisphenols with a globular hydrophobic core.
AID1254839Antiproliferative activity against human GBM2 cells assessed as reduction in cell viability at 10 uM incubated for 72 hrs by WST-1 method2015European journal of medicinal chemistry, Oct-20, Volume: 103Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID1564355Antimycobacterial activity against Mycobacterium tuberculosis H37Ra lux incubated for 7 days by luminometric assay2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID42280Percent of inhibitory activity against proliferation of BT-20 cells in presence of TPE at 10e-5 M concentration.1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Effect of triphenylacrylonitrile derivatives on estradiol-receptor binding and on human breast cancer cell growth.
AID1356844AUC in mouse at 10 mg/kg, po2018Journal 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.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID70030Inhibitory concentration against estrogen receptor 2 using estrogen response element (ERE) assay.2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.
AID1566500Cytotoxicity against human MCF7 Cells after 48 hrs by neutral red dye-based assay2019European journal of medicinal chemistry, Sep-01, Volume: 177Developments in the anticancer activity of structurally modified curcumin: An up-to-date review.
AID1079936Choleostatic 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]
AID69535Relative binding affinity determined by displacement of [3H]estradiol relative to unlabeled estradiol1983Journal 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.
AID1624907In vivo antagonist activity at estrogen receptor in Sprague-Dawley rat assessed as reduction in ethynylestradiol-stimulated increase in uterine wet weight at 60 mg/kg, po administered once daily via gavage for 3 days measured 24 hrs post last dose relativ2019Bioorganic & medicinal chemistry letters, 04-01, Volume: 29, Issue:7
Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.
AID1596589Solubility of compound in PBS after 2 hrs by turbidity based absorbance analysis2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID1705334Antiproliferative activity against human LOX IMVI cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID103559Cytostaticity against MCF-7 cells in the presence of 1 uMolar E2 (estradiol)1997Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
Cytotoxicity and antiestrogenicity of a novel series of basic diphenylethylenes.
AID1507354Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by SRB assay2017European journal of medicinal chemistry, Aug-18, Volume: 136Design, synthesis, molecular docking and cytotoxic evaluation of novel 2-furybenzimidazoles as VEGFR-2 inhibitors.
AID188609The compound was tested for the % change of tumor area at 1 mg/kg dose after peroral administration (experiment-2)1984Journal 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
AID1768149Distribution coefficient, logD of the compound at pH 7.4
AID1688060Antiproliferative activity against human MCF-7 cells assessed as proportion of live cells at 5.39 ug/ml measured after 3 weeks by crystal violet staining based soft agar colony formation assay (Rvb = 100%)2020European journal of medicinal chemistry, Feb-15, Volume: 188Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition.
AID1387906Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length untagged estrogen receptor beta expressed in insect cells by fluorescence polarization assay2018Journal 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.
AID101922Effect on [3H]thymidine incorporation into estrogen receptor positive MCF-7 human breast carcinoma cells at 10e-7 M (experiment 2)1987Journal 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.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1177821Inhibition of VEGF production in human MCF7 cells at cytotoxic IC50 level after 24 hrs by ELISA2014European journal of medicinal chemistry, Nov-24, Volume: 87Part I. Synthesis, biological evaluation and docking studies of new 2-furylbenzimidazoles as antiangiogenic agents.
AID1763181Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 05-15, Volume: 38Design, synthesis and molecular docking studies of thymol based 1,2,3-triazole hybrids as thymidylate synthase inhibitors and apoptosis inducers against breast cancer cells.
AID1911287Antitumor activity against human MCF7 cells xenografted in BALB/C mouse assessed as decrease in cell proliferation at 20 mg/kg, po by Ki67 staining based immunohistochemical analysis2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Discovery of Novel Bicyclic Phenylselenyl-Containing Hybrids: An Orally Bioavailable, Potential, and Multiacting Class of Estrogen Receptor Modulators against Endocrine-Resistant Breast Cancer.
AID140521Anti-tumor activity in hormone-dependent transplant MXT mammary tumor bearing mice at 8.8 mg (control=388+/-269)1991Journal 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.
AID70180Displacement of [3H]E2 from calf uterine estrogen receptor2003Journal 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.
AID171780Uterotrophic and anti-uterotrophic activities in immature rats at 0.1 mg/kg dose as %agonist:%antagonist = 35:461983Journal 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.
AID451832Estrogenic antagonistic activity in bilaterally ovariectomized Sprague-Dawley rat assessed as inhibition of ethynylesterol-induced uterine weight at 10 mg/kg, po once daily for 3 days measured on day 31 of age2009Bioorganic & 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.
AID1705373Antiproliferative activity against human breast cancer cells2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1705355Antiproliferative activity against human UO-31 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID220010Inhibition of calmodulin dependent cAMP phosphodiesterase.1992Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
A molecular modeling study of the interactions between the antiestrogen drug tamoxifen and several derivatives, and the calcium-binding protein calmodulin.
AID1312681Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents.
AID561222Inhibition of Myo2-GFP binding to Saccharomyces cerevisiae BY4741 calmodulin at 50 ug/ml by Western blot analysis2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1705326Antiproliferative activity against human HT29 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1061212Inhibition of trypsin-like activity of human 20S proteasome beta 2 subunit assessed as hydrolysis of Boc-LRR-AMC fluorogenic substrate at 10 uM measured for 1 hr by fluorometric analysis relative to control2014European journal of medicinal chemistry, Jan, Volume: 71A novel tamoxifen derivative, ridaifen-F, is a nonpeptidic small-molecule proteasome inhibitor.
AID1545817Antiproliferative activity against human MCF7 cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID467754Cytotoxicity against human MCF7 cells by WST-1 assay2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Cytotoxic and PTP1B inhibitory activities from Erythrina abyssinica.
AID1243939Kinetic solubility of the compound in PBS2015European journal of medicinal chemistry, Aug-28, Volume: 101Discovery and characterization of aryl isonitriles as a new class of compounds versus methicillin- and vancomycin-resistant Staphylococcus aureus.
AID561042Antifungal activity against Saccharomyces cerevisiae BY4741 expressing PKC1 at 62 to 125 ug/mL after 3 days by photographic analysis2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID1443551Antagonist activity at ERalpha in human MCF7 cells assessed as inhibition of estrogen-induced transcription preincubated overnight followed by estrogen addition measured after 24 hrs by dual luciferase reporter gene assay2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer.
AID358591Cytotoxicity against human A549 cells by alamar blue assay2001Journal of natural products, Nov, Volume: 64, Issue:11
Isolation and biological evaluation of filiformin, plakortide F, and plakortone G from the Caribbean sponge Plakortis sp.
AID734197Inhibition of Delta(8)-Delta(7) sterol isomerase/Delta(24)-sterol reductase-mediated cholesterol biosynthesis in human HL60 cells assessed as increase in zymostenol and zymosterol accumulation2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Stereoselective synthesis of a new class of potent and selective inhibitors of human Δ8,7-sterol isomerase.
AID402740Antiestrogenic activity in human Ishikawa cells assessed as inhibition of estrogen-induced alkaline phosphatase activity after 4 days by ELISA1998Journal of natural products, Oct, Volume: 61, Issue:10
Activity-guided isolation of steroidal alkaloid antiestrogen-binding site inhibitors from Pachysandra procumbens.
AID597273Antiproliferative activity against estrogen receptor-deficient human MCF12A 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 NuSerum2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Biomimetic syntheses and antiproliferative activities of racemic, natural (-), and unnnatural (+) glyceollin I.
AID173691Percent decrease in serum cholesterol relative to OVX control at 0.1 mg/kg in rat was determined (in vivo)1997Journal 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.
AID187059Antiestrogenic activity in presence of unlabeled estradiol as mean uterine weight in rats at 0.3 ug dose1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans.
AID614549Antiproliferative activity against estrogen receptor-deficient human MDA-MB-231 cells expressing estrogen receptor after 48 hrs by MTT assay2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Design and synthesis of 1,3-biarylsulfanyl derivatives as new anti-breast cancer agents.
AID23271Partition coefficient (logD7.4)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Structure-activity relationships of antineoplastic agents in multidrug resistance.
AID1705340Antiproliferative activity against human SK-MEL-5 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1312620Antiproliferative activity against human MCF7 cells2016European journal of medicinal chemistry, Aug-25, Volume: 119Recent developments of C-4 substituted coumarin derivatives as anticancer agents.
AID1719770Cytotoxicity against human HEK-293 cells incubated for 23 hrs by CO-ADD method
AID70341Displacement of [3H]17-beta-estradiol from human estrogen receptor alpha1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Carboxylic acid analogues of tamoxifen: (Z)-2-[p-(1, 2-diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine. Estrogen receptor affinity and estrogen antagonist effects in MCF-7 cells.
AID1164494Antiproliferative activity against CHO cells after 2 days by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of new estradiol-cationic lipid hybrids: ten-carbon twin chain cationic lipid is a more suitable partner for estradiol to elicit better anticancer activity.
AID614555Displacement of [3H]-estradiol from estrogen receptor in rat uteri after 18 hrs by scintillation counting relative to 17beta-estradiol2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Design and synthesis of 1,3-biarylsulfanyl derivatives as new anti-breast cancer agents.
AID723540Cytotoxicity against human MCF7 cells assessed as change in cell viability at 5 uM after 48 hrs by MTT assay2013European journal of medicinal chemistry, Feb, Volume: 60Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent.
AID1209447Activity at CYP2B6 (unknown origin) expressed in Escherichia coli C41 DE3 cells assessed as enzyme-mediated 4-hydroxytamoxifen quinone methide metabolite formation by measuring reactive metabolite adduct with GSHEE at 60 uM by LC-MS/MS analysis2012Drug 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.
AID1500956Inhibition of fluorescent estrogen binding to full length untagged human ERalpha expressed in insect cells at 10 uM after 2 hrs by fluorescent polarization assay relative to control2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel 2-methoxyestradiol analogs as dual selective estrogen receptor modulators (SERMs) and antiangiogenic agents.
AID171782Uterotrophic and anti-uterotrophic activities in immature rats at 1 mg/kg dose as %agonist:%antagonist = 42:521983Journal 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.
AID1602671Mitochondrial toxicity in human HepG2 cells assessed as reduction in cell viability after 24 hrs in presence of glucose by CellTiter-Glo assay2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
A Cinchona Alkaloid Antibiotic That Appears To Target ATP Synthase in Streptococcus pneumoniae.
AID1311874Antiproliferative activity against ER-positive human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by AlamarBlue assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis, antiproliferative and pro-apoptotic activity of 2-phenylindoles.
AID1891822Cytotoxicity against HEK293 cells assessed as cell growth inhibition measured after 20 hrs by resazurin dye based assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Valorisation of the diterpene podocarpic acid - Antibiotic and antibiotic enhancing activities of polyamine conjugates.
AID409603Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes at 20 uM2009Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1
Identification of aquaporin 4 inhibitors using in vitro and in silico methods.
AID1688051Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 48 hrs by SRB assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition.
AID680524TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical)(Digoxin: 5 uM, Tamoxifen: 100 uM) in Caco-2 cells1999Pharmaceutical research, Mar, Volume: 16, Issue:3
Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein.
AID101643Effect on [3H]thymidine incorporation into MDA-MB 231 human breast cancer cells at 1x10E-5 M1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Indolo[2,1-a]isoquinolines. Syntheses, steroid hormone receptor binding affinities, and cytostatic activity.
AID673824Growth inhibition of human MCF7 cells at 10'-7 M after 5 days relative to control2012ACS medicinal chemistry letters, Apr-06, Volume: 3, Issue:5
Boron-Based 4-Hydroxytamoxifen Bioisosteres for Treatment of de Novo Tamoxifen Resistant Breast Cancer.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1705357Antiproliferative activity against human DU-145 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1628317Antiestrogenic activity in human MCF7 cells assessed as compound concentration required to decrease 100 pM E2-induced cell proliferation to equivalent levels induced by 50 pM E2 after 96 hrs by alamar blue assay2016Journal of natural products, 05-27, Volume: 79, Issue:5
Furofuran Lignan Glucosides with Estrogen-Inhibitory Properties from the Bangladeshi Medicinal Plant Terminalia citrina.
AID1310517Induction of apoptosis in human HeLa cells assessed as late apoptotic cells at 50 uM after 28 hrs by annexin V/FITC/propidium iodide staining-based flow cytometry (Rvb = 1.2%)2016European journal of medicinal chemistry, Aug-08, Volume: 1184-(1,2-diarylbut-1-en-1-yl)isobutyranilide derivatives as inhibitors of topoisomerase II.
AID1705352Antiproliferative activity against human CAKI-1 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1415058Aqueous solubility of the compound in simulated gastric fluid2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.
AID1283268Inhibition of delta 8-7 isomerase in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis2016Journal 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.
AID1254845Antiproliferative activity against human GBM3 cells assessed as reduction in cell viability at 10 uM incubated for 72 hrs by WST-1 method2015European journal of medicinal chemistry, Oct-20, Volume: 103Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID1562215Antiproliferative activity against human A2058 cells assessed as reduction in cell viability measured after 24 hrs by celltiter-blue assay2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Nitric Oxide-Releasing Selective Estrogen Receptor Modulators: A Bifunctional Approach to Improve the Therapeutic Index.
AID1395068Displacement of Fluormone ES2 Green from full length human ER-alpha expressed in insect cells at 10 uM after 2 hrs by fluorescence polarization assay relative to control2018European journal of medicinal chemistry, Apr-25, Volume: 150Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ERα/VEGFR-2 ligands with anti-breast cancer activity.
AID68897Antiproliferative activity against estrogen receptor positive MCF-7 human breast cancer cell line at 10e-9 M. (p<0.05)1991Journal 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.
AID102273Inhibition of [3H]thymidine incorporation into hormone sensitive MCF-7 human breast cancer cells at 10e-5 M1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity.
AID1530770Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2.
AID1233701Cytotoxicity against human MDA-MB-435S cells assessed as cell viability by MTT assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Synthesis and cancer cell growth inhibitory activity of icaritin derivatives.
AID234090Selectivity for relative binding affinity against estrogen receptor at 2 hrs and 5 hr in calf uterus cytosol1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Effect of triphenylacrylonitrile derivatives on estradiol-receptor binding and on human breast cancer cell growth.
AID548939Growth inhibition of human MDA-MB-231 cells at 50 ug/ml after 24 hrs by MTT colorimetric assay2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Isochaihulactone analogues: synthesis and anti-proliferative activity of novel dibenzylbutyrolactones.
AID324365Induction of light chain 3-GFP level in human H4 cells at 4.4 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings 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.
AID1694959Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2020RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2
Development of potent CPP6-gemcitabine conjugates against human prostate cancer cell line (PC-3).
AID1768142Kinetic solubility of compound at pH 7.4
AID1684754Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay2021Bioorganic & medicinal chemistry letters, 02-01, Volume: 33Synthesis of mitochondria-targeted coumarin-3-carboxamide fluorescent derivatives: Inhibiting mitochondrial TrxR2 and cell proliferation on breast cancer cells.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID282034Decrease in DOX-TEG-TAM uptake in MDA-MB-435 cells after 1 hr2004Journal 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.
AID124178Uterine weight after 9 day treatment at 4.2 ug by oral gavage to ovariectomised mice without estrone1997Journal 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.
AID1666649Displacement 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 assay2020Bioorganic & 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.
AID1251784Antiproliferative activity against human MCF7 cells2015Journal 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
AID1666655Antagonist activity at ERbeta (unknown origin)2020Bioorganic & 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.
AID451833Displacement of [3H]estradiol from rat estrogen receptor by radiometric assay relative to estradiol2009Bioorganic & 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.
AID1356852Reduction 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 as2018Journal 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.
AID1662875Selectivity index, ratio of IC50 for human Chang cells to IC50 for human M-HeLa cells2020Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13
Design and synthesis of amphiphilic 2-hydroxybenzylphosphonium salts with antimicrobial and antitumor dual action.
AID1662871Cytotoxicity against human MCF7 cells2020Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13
Design and synthesis of amphiphilic 2-hydroxybenzylphosphonium salts with antimicrobial and antitumor dual action.
AID68895Antiproliferative activity against estrogen receptor positive MCF-7 human breast cancer cell line at a dose of 10e-7 M. (p<0.05)1991Journal 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.
AID497607Cytotoxicity against human MCF7 cells assessed as reduction of cell proliferation at 6 uM after 96 hrs by MTT assay2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha.
AID68910Apparent inhibition constant for estrogen receptor in Human uterine cytosol in 3.3%ethanol1997Journal 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.
AID1161694Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents.
AID71134Relative binding affinity against estrogen receptor in calf uterus cytosol using [3H]E2 as radioligand, incubated at 5 hours at 25 degree Centigrade.1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Effect of triphenylacrylonitrile derivatives on estradiol-receptor binding and on human breast cancer cell growth.
AID1277628Antiproliferative activity against human AsPC1 cells assessed as cell viability at 10 uM after 48 hrs by MTS assay2016Bioorganic & 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.
AID667226Cytotoxicity against human 518A2 cells after 96 hrs by SRB assay2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel (E) stilbene-based antitumor agents.
AID723538Cytotoxicity against human T47D cells assessed as change in cell viability at 5 uM after 48 hrs by MTT assay2013European journal of medicinal chemistry, Feb, Volume: 60Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent.
AID70482Inhibition of estrogen receptor alpha mediated transcriptional activation; Not determined2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.
AID657123Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay2012Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9
Synthesis and anticancer activity of 2-benzylidene indanones through inhibiting tubulin polymerization.
AID1666654Antagonist activity at ERalpha (unknown origin)2020Bioorganic & 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.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1164491Antiproliferative activity human ER-negative MDA-MB-231 cells after 2 days by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of new estradiol-cationic lipid hybrids: ten-carbon twin chain cationic lipid is a more suitable partner for estradiol to elicit better anticancer activity.
AID69070Relative Binding Affinity for estrogen receptor in Human Breast cancer or normal uterine cytosol in 3.3%ethanol compared to estradiol1997Journal 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.
AID150616Concentration giving half of the maximal ATPase activity calculated for the high-affinity binding site of the CHO P-Glycoprotein (P-gp) in two-affinity model2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
AID620849Binding affinity to bovine serum albumin at 1 to 100 uM at pH 7.4 by fluorescence spectroscopy2011European 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.
AID592683Apparent permeability from basolateral side to apical side of human Caco2 cells by LC/MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID695960Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
New prenylated isoflavonoids as protein tyrosine phosphatase 1B (PTP1B) inhibitors from Erythrina addisoniae.
AID1209972Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1443550Displacement of [3H]-estradiol from recombinant human N-terminal His-tagged ERalpha LBD harboring C381S/C417S/C530S mutant expressed in Rosetta 2 DE3 competent cells after 1 hr by SPA binding assay2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer.
AID1158150Antiproliferative activity against human PC3 cells after 24 hrs by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Synthesis and anticancer activity of γ-(triazolyl ethylidene)butenolides and polyfunctional pyrrolinones.
AID103515Incorporation of [3H]thymidine into estrogen-responsive MCF-7 human breast tumor cells at 10e-8 M with hexestrol1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
N,N'-Dialkyl-1,2-bis(hydroxyphenyl)ethylenediamines and N,N-dialkyl-4,5-bis(4-hydroxyphenyl)imidazolidines: syntheses and evaluation of their mammary tumor inhibiting activity.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1284729Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
AID1473741Inhibition of human MRP4 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 assay2013Toxicological 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.
AID1217711Metabolic activation in human liver microsomes assessed as [3H]GSH adduct formation rate measured per mg of protein at 100 uM by [3H]GSH trapping assay2011Drug 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.
AID68744Binding affinity for estrogen receptor, by competition with [3H]estradiol1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Novel 5-aminoflavone derivatives as specific antitumor agents in breast cancer.
AID723805Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay2013European journal of medicinal chemistry, Feb, Volume: 60Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent.
AID1465923Cytotoxicity against human MCF7 cells assessed as reduction in cell viability at 1 uM after 24 hrs by MTT assay relative to control2017Journal 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.
AID1069844Cytotoxicity against human HEK293 cells after 24 hrs by MTT assay2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Synthesis of neolignans as microtubule stabilisers.
AID1415059Apparent permeability across apical to basolateral side in human Caco2 cells at pH 6.5 to 7.5 after 2 hrs by LC/MS/MS analysis2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.
AID101925Effect on [3H]-thymidine incorporation into estrogen receptor positive MCF-7 human breast carcinoma cells at 10e-7 M (ex 1)1987Journal 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.
AID1284718Cytotoxicity against human SKOV3 cells assessed as growth inhibition after 48 hrs by SRB assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
AID455710Anticancer activity against human DU145 cells after 24 hrs by SRB assay2009Bioorganic & 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.
AID1752633Antiproliferative activity against ER-positive human Ishikawa cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay2021Bioorganic & medicinal chemistry, 10-01, Volume: 47Benzothiophene derivatives as selective estrogen receptor covalent antagonists: Design, synthesis and anti-ERα activities.
AID1705366Antiproliferative activity against human Non-small cell lung cancer cells2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1193499Thermodynamic equilibrium solubility, log S of the compound simulated intestinal fluid at pH 6.8 at RT after 24 hrs by shake-flask method2015Bioorganic & 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.
AID1705336Antiproliferative activity against human M14 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID455711Anticancer activity against human SKOV3 cells after 24 hrs by SRB assay2009Bioorganic & 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.
AID1310524Induction of mitochondrial membrane depolarization in human HeLa cells at 10 uM after 28 hrs by JC-1 staining-based flow cytometric analysis (Rvb = 4%)2016European journal of medicinal chemistry, Aug-08, Volume: 1184-(1,2-diarylbut-1-en-1-yl)isobutyranilide derivatives as inhibitors of topoisomerase II.
AID1564357Selectivity index, ratio of MIC90 for antimycobacterial activity against Mycobacterium tuberculosis H37Ra lux to CC50 for cytotoxicity against mouse J774A.1 cells2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID1688059Antiproliferative activity against human MCF-7 cells assessed as proportion of live cells at 1.07 ug/ml measured after 3 weeks by crystal violet staining based soft agar colony formation assay (Rvb = 100%)2020European journal of medicinal chemistry, Feb-15, Volume: 188Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition.
AID1705313Antiproliferative activity against human A549 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1431913Antitumor activity against human MCF7:TAM1 cells xenografted in athymic nude mouse assessed as tumor regression at 100 mg/kg, po administered daily via gavage for 23 days relative to control2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Novel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer.
AID1209425Cytotoxicity against human hepatocytes assessed as reduction in cell viability after 24 hrs by ATP detection based assay2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
In vitro hepatotoxicity and cytochrome P450 induction and inhibition characteristics of carnosic acid, a dietary supplement with antiadipogenic properties.
AID103058Inhibition of hormone-sensitive MCF-7 mammary tumor cell proliferation at 1*10e-7 M1992Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19
6-Alkyl-12-formylindolo[2,1-a]isoquinolines. Syntheses, estrogen receptor binding affinities, and stereospecific cytostatic activity.
AID70167Inhibition of estrogen receptor beta mediated transcriptional activation; Not determined2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.
AID1177820Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Part I. Synthesis, biological evaluation and docking studies of new 2-furylbenzimidazoles as antiangiogenic agents.
AID1254840Antiproliferative activity against human GBM1 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method2015European journal of medicinal chemistry, Oct-20, Volume: 103Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID103533Inhibition of estrogen receptor positive MCF-7 cell proliferation as cell number after 10 days at 10e-7 M1981Journal 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.
AID1283267Cytotoxicity against human SLOS fibroblasts at 5 uM after 5 days by Cell Titer assay2016Journal 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.
AID1233700Cytotoxicity against human MCF7 cells assessed as cell viability by MTT assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Synthesis and cancer cell growth inhibitory activity of icaritin derivatives.
AID268619Agonist activity at ERalpha assessed as inhibition of E2-induced luciferase gene transactivation in MCF7 cells at >10 uM2006Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
m-Carborane bisphenol structure as a pharmacophore for selective estrogen receptor modulators.
AID1779059Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth incubated for 48 hrs by CCK8 assay2021European journal of medicinal chemistry, Oct-05, Volume: 221Design and synthesis of novel benzothiophene analogs as selective estrogen receptor covalent antagonists against breast cancer.
AID1469718Induction of selective estrogen receptor alpha degradation in human MCF7 cells assessed as ERalpha remaining at 10 uM after 18 to 24 hrs by in-cell Western analysis relative to control2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.
AID1602141Inhibition of estrogen receptor-alpha (unknown origin) by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Structure-based drug design, synthesis, In vitro, and In vivo biological evaluation of indole-based biomimetic analogs targeting estrogen receptor-α inhibition.
AID1170542Binding affinity to human ERbeta2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
β-Lactam estrogen receptor antagonists and a dual-targeting estrogen receptor/tubulin ligand.
AID99173Cross resistance profile versus L1210/R71 cells.1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Structure-activity relationships of antineoplastic agents in multidrug resistance.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID497602Displacement of [2,4,6,7-3H]estradiol from human ERalpha expressed in HeLa cells after 18 hrs by liquid scintillation counting2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha.
AID191673Uterotrophic effect in rats uterine at 0.1 ug/day dose1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent.
AID681139TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP)2003Pharmaceutical research, Apr, Volume: 20, Issue:4
Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites.
AID1395071Antiproliferative activity against human Ishikawa cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ERα/VEGFR-2 ligands with anti-breast cancer activity.
AID103375Effective concentration against MCF-7 breast tumor cells using MCF-7 assay.2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.
AID21910Estrogenic property of the compound; Weakly estrogenic1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
Molecular structures and conformational studies of triarylcyclopropyl and related nonsteroidal antiestrogens.
AID1302503Inhibition of Set7/9 in human MCF7 cells assessed as suppression of beta-estradiol-induced ERE promoter activation at 3 to 10 uM preincubated for 18 hrs followed by beta-estradiol addition measured after 24 hrs by luciferase reporter gene assay2016Journal 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.
AID667227Cytotoxicity against human 850C cells after 96 hrs by SRB assay2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel (E) stilbene-based antitumor agents.
AID723806Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2013European journal of medicinal chemistry, Feb, Volume: 60Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent.
AID1502307Cytotoxicity in human Ishikawa cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Novel 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.
AID1366614Induction of mitochondrial membrane potential loss in human MCF7 cells assessed as green to red fluorescence ratio after 24 hrs by JC1 staining based flow cytometry (Rvb = 0.1 No_unit)2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Syntheses of conformationally restricted benzopyran based triarylethylenes as growth inhibitors of carcinoma cells.
AID1079938Chronic 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]
AID90246Relative binding affinity for antiestrogen binding site compared to tamoxifen1989Journal of medicinal chemistry, Jan, Volume: 32, Issue:1
Phenolic metabolites of clomiphene: [(E,Z)-2-[4-(1,2-diphenyl-2-chlorovinyl)phenoxy]ethyl]diethylamine. Preparation, electrophilicity, and effects in MCF 7 breast cancer cells.
AID1158152Antiproliferative activity against human U937 cells after 24 hrs by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Synthesis and anticancer activity of γ-(triazolyl ethylidene)butenolides and polyfunctional pyrrolinones.
AID480630Displacement 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 estradiol2010Bioorganic & 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.
AID1754976Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Design, synthesis and broad spectrum antibreast cancer activity of diarylindoles via induction of apoptosis in aggressive breast cancer cells.
AID270142Cytotoxicity against human HS 587-T cells lacking ER2006Journal 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.
AID667229Cytotoxicity against human A549 cells after 96 hrs by SRB assay2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel (E) stilbene-based antitumor agents.
AID1775656Cytotoxicity against human MRC5 cells measured after 7 days by MTT assay2021Journal of natural products, 03-26, Volume: 84, Issue:3
Antiplasmodial Oleanane Triterpenoids from
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1705358Antiproliferative activity against human MCF7 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID258227Cell survival against human breast cancer MCF7 cell line after 72h at 10 uM2006Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2
Synthesis and biological activities of nucleoside-estradiol conjugates.
AID470164Antiestrogenic activity in human MCF7 cells assessed as drug level causing inhibition of 100 pM E2-enhanced cell proliferation to level equivalent to 10 pM E2 after 96 hrs by alamar blue assay2009Journal of natural products, Nov, Volume: 72, Issue:11
Antiestrogenic constituents of the Thai medicinal plants Capparis flavicans and Vitex glabrata.
AID270140Cytotoxicity against human ZR-75-1 cells expressing ER2006Journal 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.
AID1772392Inhibition of Escherichia coli DNA gyrase at 100 uM by fluorescence based assay relative to control
AID239296Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand2005Journal 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.
AID592682Apparent permeability from apical to basolateral side of human Caco2 cells after 2 hrs by LC/MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID667232Cytotoxicity against human Lipo cells after 96 hrs by SRB assay2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel (E) stilbene-based antitumor agents.
AID1313267Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by resazurin microplate assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and cytotoxic activities of semisynthetic zearalenone analogues.
AID759306Antagonist activity at Gal4 DBD-fused human ERalpha LBD expressed in HEK293T cells assessed as inhibition of estradiol-induced transcriptional activation after 20 hrs by luciferase reporter gene assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.
AID102427Effect of compound with 10e-8 M estradiol on the growth of MCF-7 cells at a concentration of,10 e-6 M, percentage of control value being 901985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Hydroxy derivatives of tamoxifen.
AID103392Growth inhibitory activity against MCF-7 human breast tumor cell line at a concentration of 10e-6 M in vitro.1989Journal of medicinal chemistry, Dec, Volume: 32, Issue:12
Derivatives of tamoxifen. Dependence of antiestrogenicity on the 4-substituent.
AID1356872Antitumor activity against human MCF7 cells xenografted in nu/nu mouse model of tamoxifen-resistant breast cancer xenograft implanted with 17beta-estradiol time release pellets assessed as reduction tumor volume at 120 mg/kg, po qd for 4 weeks2018Journal 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.
AID1646804Metabolic stability in mouse liver microsomes assessed as half life2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells.
AID1666646Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTT assay2020Bioorganic & 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.
AID276683Antiproliferative activity against MCF7 cells at 3 mg/kg/day after 48 hrs2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
Rapid synthesis of 4-benzylidene and 4-[bis-(4-methoxyphenyl)-methylene-2-substituted phenyl-benzopyrans as potential selective estrogen receptor modulators (SERMs) using McMurry coupling reaction.
AID239597Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand2005Journal 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.
AID437138Anticancer activity against estrogen-positive human MCF7 cells after 18 hrs by MTT assay2009European 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.
AID302456Antiproliferative activity against MCF7 cells after 72 hrs by MTT assay2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Target specific virtual screening: optimization of an estrogen receptor screening platform.
AID1315655Cytotoxicity against human MCF7 cells by resazurin microplate assay2016Journal of natural products, 06-24, Volume: 79, Issue:6
Lovastatin Analogues from the Soil-Derived Fungus Aspergillus sclerotiorum PSU-RSPG178.
AID470165Antiestrogenic activity in human MCF7 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 assay2009Journal of natural products, Nov, Volume: 72, Issue:11
Antiestrogenic constituents of the Thai medicinal plants Capparis flavicans and Vitex glabrata.
AID1366598Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Syntheses of conformationally restricted benzopyran based triarylethylenes as growth inhibitors of carcinoma cells.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1911286Antitumor activity against human MCF7 cells xenografted in BALB/C mouse assessed as increase in tumor necrosis area at 20 mg/kg, po by Ki67 staining based based immunohistochemical analysis2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Discovery of Novel Bicyclic Phenylselenyl-Containing Hybrids: An Orally Bioavailable, Potential, and Multiacting Class of Estrogen Receptor Modulators against Endocrine-Resistant Breast Cancer.
AID68894Antiproliferative activity against estrogen receptor positive MCF-7 human breast cancer cell line at a dose of 10e-5 M. (p<0.05)1991Journal 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.
AID1323682Inhibition of rat brain PKC assessed as reduction in phosphatidyl serine/Ca2+-stimulated calf thymus histone H1 phosphorylation after 3 mins in presence of [gamma32P]ATP by liquid scintillation counting method2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Design and synthesis of triarylacrylonitrile analogues of tamoxifen with improved binding selectivity to protein kinase C.
AID1705349Antiproliferative activity against human 786-0 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1646801Chaperone activity at GCase in wild-type human fibroblasts assessed as increase in GPN-induced reduction of calcium release using Fluo-8AM based fluorescence assay2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells.
AID191696Uterotrophic effect in rats uterine at 50 ug/day dose in the presence of 10 ug estradiol1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent.
AID407205Inhibition of P-glycoprotein-mediated [3H]vinblastine transport in human Caco-2 cells2008Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
Effect of some P-glycoprotein modulators on Rhodamine-123 absorption in guinea-pig ileum.
AID1507357Inhibition of VEGFR2 protein expression in human MCF7 cells at cytotoxic IC50 after 24 hrs by ELISA relative to untreated control2017European journal of medicinal chemistry, Aug-18, Volume: 136Design, synthesis, molecular docking and cytotoxic evaluation of novel 2-furybenzimidazoles as VEGFR-2 inhibitors.
AID1251781Antagonist activity at ERalpha receptor in human MCF7 cells2015Journal 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
AID248163Inhibition of estrogen receptor positive human breast carcinoma (MCF-7) cell proliferation2004Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
Benzoxepin-derived estrogen receptor modulators: a novel molecular scaffold for the estrogen receptor.
AID186919The compound was tested for anti-uterotrophic activity in immature rats(Dosage 1 ug)1984Journal 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
AID1251783Antagonist activity at progesterone receptor in human MCF cells assessed as estradiol-induced receptor response2015Journal 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
AID548938Growth inhibition of human MDA-MB-231 cells at 25 ug/ml after 24 hrs by MTT colorimetric assay2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Isochaihulactone analogues: synthesis and anti-proliferative activity of novel dibenzylbutyrolactones.
AID1209453Inactivation of CYP2B6 (unknown origin) expressed in Escherichia coli C41 DE3 cells assessed as modified apo-P450 2B6 adduct formation at 60 uM by ESI-LC-MS analysis in presence of NADPH and GSHEE2012Drug 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.
AID474295Inhibition of PKC at 0.025 to 0.05 mM after 90 mins by ELISA2010Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
Endoxifen is a new potent inhibitor of PKC: a potential therapeutic agent for bipolar disorder.
AID736611Growth inhibition of human M21 cells2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Synthesis and growth inhibition activity of fluorinated derivatives of tamoxifen.
AID255211Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881)2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Impact of induced fit on ligand binding to the androgen receptor: a multidimensional QSAR study to predict endocrine-disrupting effects of environmental chemicals.
AID124175Uterine weight after 9 day treatment at 14 ug by oral gavage to ovariectomised mice with estrone1997Journal 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.
AID561223Antifungal activity against Saccharomyces cerevisiae BY4741 after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID1389787Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6
Synthesis and biological evaluation of 4,6-diaryl-2-pyrimidinamine derivatives as anti-breast cancer agents.
AID723648Selectivity index, ratio of Ki for sigma 1 receptor (unknown origin) to Ki for emopamil binding protein (unknown origin)2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Synthesis and biological evaluation of ¹⁸F labeled fluoro-oligo-ethoxylated 4-benzylpiperazine derivatives for sigma-1 receptor imaging.
AID491599Cytotoxicity against human HeLa cells after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Synthesis and anti breast cancer activity of biphenyl based chalcones.
AID134365In vivo anti-estrogenic effect in immature mice at 5 ug1986Journal 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.
AID69520Receptor binding affinity(RBA) for rat uterine cytosolic estrogen receptor relative to estradiol1995Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2
Rationally designed analogues of tamoxifen with improved calmodulin antagonism.
AID1705362Antiproliferative activity against human T47D cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID537736Antifungal activity against yeast AD1-8u expressing Candida albicans CaCdr1p by agar disk diffusion assay2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID69536Relative binding affinity evaluated from the ability to displace [3H]estradiol from estrogen receptor in rat uterine cytosol preparation.1991Journal 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.
AID1369862Cytotoxicity against human MRC5 cells assessed as decrease in cell viability after 72 hrs by resazurin assay2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity.
AID1562223Effect on ER/PI3K pathway in HUVEC assessed as change COX2 expression up to 1 uM measured after 24 hrs by Western blot analysis2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Nitric Oxide-Releasing Selective Estrogen Receptor Modulators: A Bifunctional Approach to Improve the Therapeutic Index.
AID1057864Ratio of LC50 for dividing mouse ScN2a-cl3 cells to EC50 for inhibition of RML prion protein2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Antiprion compounds that reduce PrP(Sc) levels in dividing and stationary-phase cells.
AID597276Antiproliferative activity against androgen receptor-deficient human DU145 cells incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Biomimetic syntheses and antiproliferative activities of racemic, natural (-), and unnnatural (+) glyceollin I.
AID282033Decrease in doxorubicin uptake in MDA-MB-435 cells at 10 uM after 1 hr relative to DOX-TEG-TAM2004Journal 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.
AID471244Uterotropic activity in rat assessed as increase in uterine weight at 1 mg/kg, po QD after 3 days2009Journal 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.
AID1164492Antiproliferative activity mouse B16F10 cells after 2 days by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of new estradiol-cationic lipid hybrids: ten-carbon twin chain cationic lipid is a more suitable partner for estradiol to elicit better anticancer activity.
AID1297988Antiparasitic activity against promastigote stage of Leishmania braziliensis MHOM/BR/2001/BA788 infected in BALB/c mouse assessed as reduction in parasite load at 20 mg/kg, ip administered for 15 days measured after 6 weeks by limiting dillution method2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Repurposing strategies for tropical disease drug discovery.
AID673828Cytotoxicity against human MCF7 cells after 5 days2012ACS medicinal chemistry letters, Apr-06, Volume: 3, Issue:5
Boron-Based 4-Hydroxytamoxifen Bioisosteres for Treatment of de Novo Tamoxifen Resistant Breast Cancer.
AID1389790Stimulation of cell proliferation in human Ishikawa cells at 10 uM after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6
Synthesis and biological evaluation of 4,6-diaryl-2-pyrimidinamine derivatives as anti-breast cancer agents.
AID102448Inhibitory activity against proliferation of MCF-7 cells in presence of 10e-6 M concentration of [3H]- estradiol (E2)1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Effect of triphenylacrylonitrile derivatives on estradiol-receptor binding and on human breast cancer cell growth.
AID723803Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2013European journal of medicinal chemistry, Feb, Volume: 60Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent.
AID1283269Inhibition of DR24 in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis2016Journal 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.
AID620848Effect on secondary structure of bovine serum albumin assessed as alpha-helix content at 0.5 uM at pH 7.4 by circular dichroism method (Rvb = 63 %)2011European 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.
AID103393Growth inhibitory activity against MCF-7 human breast tumor cell line at a concentration of 10e-7 M in vitro.1989Journal of medicinal chemistry, Dec, Volume: 32, Issue:12
Derivatives of tamoxifen. Dependence of antiestrogenicity on the 4-substituent.
AID1533103Inhibition of P-gp-mediated doxorubicin efflux in human Lucena 1 cells assessed as ratio of doxorubicin fluorescence intensity in presence of compound to doxorubicin fluorescence intensity in absence of compound at 3.12 uM preincubated for 1 hr followed b2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Analogues of the Lignan Pinoresinol as Novel Lead Compounds for P-glycoprotein (P-gp) Inhibitors.
AID1228302Antitumor activity against tamoxifen-sensitive human MCF7 cells xenografted in po dosed nu/nu mouse supplemented with 17-beta estradiol pellets measured on day 702015Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.
AID1646803Aqueous solubility of compound in PBS2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells.
AID105943Estrogenicity of compound for maximal induction of MVLN cell luciferase activity in the absence of E2 (estradiol).1997Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
Cytotoxicity and antiestrogenicity of a novel series of basic diphenylethylenes.
AID1705346Antiproliferative activity against human OVCAR-5 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID467755Cytotoxicity against human tamoxifen-resistant MCF7 cells by WST-1 assay2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Cytotoxic and PTP1B inhibitory activities from Erythrina abyssinica.
AID501532Transactivation of human wild type ERalpha expressed in human HeLa cells co-expressing AP-1 by luciferase reporter gene assay2010Bioorganic & 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.
AID1312621Antiproliferative activity against human MDA-MB-231 cells2016European journal of medicinal chemistry, Aug-25, Volume: 119Recent developments of C-4 substituted coumarin derivatives as anticancer agents.
AID70338Inhibitory concentration against estrogen receptor alpha using estrogen response element (ERE) assay.2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.
AID471245Uterotropic activity in rat assessed as stimulation of estrone-induced uterine weight at 1 mg/kg, po QD after 3 days2009Journal 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.
AID538450Anticancer activity against human MCF7 cells expressing estrogen receptor by MTT assay2010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Neo-tanshinlactone inspired synthesis, in vitro evaluation of novel substituted benzocoumarin derivatives as potent anti-breast cancer agents.
AID1170545Cytotoxicity against human MCF7 cells assessed as induction of cell death at 10 uM after 72 hrs by lactate dehydrogenase assay2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
β-Lactam estrogen receptor antagonists and a dual-targeting estrogen receptor/tubulin ligand.
AID620856Binding affinity to bovine serum albumin at pH 7.4 by McGhee and von Hippel method2011European 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.
AID324584Increase in long-lived protein degradation in human H4 cells after 4 hrs relative to control2007Proceedings 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.
AID1705329Antiproliferative activity against human SF-295 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1242127Anti-proliferative activity against human DU145 cells incubated for 48 hrs by SRB assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Design, synthesis and anticancer properties of novel oxa/azaspiro[4,5]trienones as potent apoptosis inducers through mitochondrial disruption.
AID1542765Cytotoxicity against HEK293 cells measured after 20 hrs by resazurin dye based fluorescence assay2019Bioorganic & medicinal chemistry, 05-15, Volume: 27, Issue:10
6-Bromoindolglyoxylamido derivatives as antimicrobial agents and antibiotic enhancers.
AID71127Relative binding affinity for estrogen receptor of calf uterine cytosol with [3H]E22002Journal 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.
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID680276TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.5 uM, Tamoxifen: 20 uM) in MDR1-expressing NIH-3T3 cells2004Biochemical and biophysical research communications, Mar-19, Volume: 315, Issue:4
Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies.
AID468985Inhibition of human 17beta-HSD7 expressed in HEK293 cells assessed as inhibition of reduction of [14C]estrone into [14C]estradiol at 3 uM after 7 hrs2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Potent and selective steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 7, an enzyme that catalyzes the reduction of the key hormones estrone and dihydrotestosterone.
AID467757Cytotoxicity against human MDA-MB-231 cells by WST-1 assay2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Cytotoxic and PTP1B inhibitory activities from Erythrina abyssinica.
AID1500955Antiproliferative activity against human Ishikawa cells assessed as suppression of proliferation at 10 uM after 48 hrs by MTT assay relative to control2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel 2-methoxyestradiol analogs as dual selective estrogen receptor modulators (SERMs) and antiangiogenic agents.
AID1762624Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by resazurin based fluorescence assay
AID491598Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Synthesis and anti breast cancer activity of biphenyl based chalcones.
AID102276Inhibition of [3H]thymidine incorporation into hormone sensitive MCF-7 human breast cancer cells at 10e-6 M1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity.
AID67456Inhibition of [3H]thymidine incorporation into EL4 cell proliferation1992Journal 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.
AID1502306Cytotoxicity in human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Novel 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.
AID1693884Resistance index in human MCF7 cells assessed as increase in compound IC50 treated with varying concentration from IC10 to IC30 for 10 weeks and measured every 2 weeks by MTT assay2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Synthesis, antitumor activity and structure-activity studies of novel pyridoxine-based bioisosteric analogs of estradiol.
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1705338Antiproliferative activity against human SK-MEL-2 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1533167Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay2018ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
Potent Antimalarial 2-Pyrazolyl Quinolone
AID482993Antiproliferative activity against human MCF7 cells by MTT assay2010Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11
Synthesis of new cis-fused tetrahydrochromeno[4,3-b]quinolines and their antiproliferative activity studies against MDA-MB-231 and MCF-7 breast cancer cell lines.
AID1702532Cytotoxicity against human MCF7 cells assessed as reduction in cell viability at 5 to 80 uM after 48 hrs by MTT assay2020European journal of medicinal chemistry, Feb-01, Volume: 187Development of cell-permeable peptide-based PROTACs targeting estrogen receptor α.
AID537733Binding affinity to Candida albicans CaCdr1p expressed in yeast AD1-8u2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID537734Antifungal activity against yeast AD1-8u expressing Candida albicans CaMdr1p by agar disk diffusion assay2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID1161696Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 96 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents.
AID474294Inhibition of PKC at 0.1 mM after 90 mins by ELISA2010Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
Endoxifen is a new potent inhibitor of PKC: a potential therapeutic agent for bipolar disorder.
AID1705322Antiproliferative activity against human COLO 205 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1662870Cytotoxicity against human M-HeLa cells2020Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13
Design and synthesis of amphiphilic 2-hydroxybenzylphosphonium salts with antimicrobial and antitumor dual action.
AID1667152Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition at 100 uM measured after 72 hrs by MTT assay relative to control
AID103091Inhibition of MCF-7/Adr breast cancer cell proliferation2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Design, synthesis, and biological evaluation of doxorubicin-formaldehyde conjugates targeted to breast cancer cells.
AID762247Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
3-Acyl-5-hydroxybenzofuran derivatives as potential anti-estrogen breast cancer agents: a combined experimental and theoretical investigation.
AID614557Antiestrogenic activity in Sprague-Dawley rat assessed as inhibition of uterine weight gain administered as po daily once for 3 days relative to 17alpha-ethynylestradiol2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Design and synthesis of 1,3-biarylsulfanyl derivatives as new anti-breast cancer agents.
AID1387881Antiproliferative activity against ER-dependent human MCF7 cells after 72 hrs by MTT assay2018Journal 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.
AID1312688Antiestrogenic activity at ER-alpha in human MCF7 cells assessed as inhibition of E2-induced progesterone receptor mRNA expression at 1 uM by RT-PCR method relative to control2016European journal of medicinal chemistry, Aug-08, Volume: 118Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents.
AID1161697Cytotoxicity against MEFs assessed as reduction in cell viability up to 100 uM after 48 to 96 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents.
AID134366In vitro estrogenic effect in immature mice at 100 ug1986Journal 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.
AID91598Maximum stimulation of alkaline phosphatase activity expressed as a percent of the maximum induced by 10 nM estradiol1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
3-[4-(1,2-Diphenylbut-1-enyl)phenyl]acrylic acid: a non-steroidal estrogen with functional selectivity for bone over uterus in rats.
AID1254838Antiproliferative activity against human GBM1 cells assessed as reduction in cell viability at 10 uM incubated for 72 hrs by WST-1 method2015European journal of medicinal chemistry, Oct-20, Volume: 103Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID20068Approximate pKa value of compound was determined1982Journal of medicinal chemistry, Feb, Volume: 25, Issue:2
Antiestrogen basicity--activity relationships: a comparison of the estrogen receptor binding and antiuterotrophic potencies of several analogues of (Z)-1,2-diphenyl-1-[4-[2-(dimethylamino)ethoxy]phenyl]-1-butene (tamoxifen, Nolvadex) having altered basici
AID498488Stimulation of GFP-tagged human PLD2 expressed in human HEK293 cells assessed as phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID1323679Inhibition of PKC in human SH-SY5Y cells assessed as inhibition of PMA-stimulated MARCKS phosphorylation at 10 uM preincubated for 1 hr followed by PMA-stimulation for 15 mins by Western blot analysis relative to control2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Design and synthesis of triarylacrylonitrile analogues of tamoxifen with improved binding selectivity to protein kinase C.
AID173700Percent decrease in serum cholesterol relative to OVX controls, at 1.0 mg/Kg compound dose1998Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
Synthesis and pharmacology of conformationally restricted raloxifene analogues: highly potent selective estrogen receptor modulators.
AID1277629Antiproliferative activity against human MIAPaCa2 cells assessed as cell viability at 10 uM after 48 hrs by MTS assay2016Bioorganic & 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.
AID1210014Inhibition of recombinant CYP2J2 (unknown origin)-mediated astemizole O-demethylation assessed as remaining activity at 30 uM after 5 mins by LC-MS/MS analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1702561Antitumour activity against mouse 4T1 cells implanted in BALB/c mouse assessed as inhibition in tumor growth at 10 umol/kg administered peri-tumor injection for 21 days relative to control2020European journal of medicinal chemistry, Feb-01, Volume: 187Development of cell-permeable peptide-based PROTACs targeting estrogen receptor α.
AID1768138Antagonist activity at estrogen receptor in human T47D cells incubated for 18 hrs by ultra high sensitivity luminescence reporter gene assay
AID1564356Cytotoxicity against mouse J774A.1 cells assessed as reduction in cell viability incubated for 24 hrs by neutral red uptake assay2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID444842Induction of human MCF7 cell differentiation assessed as milk fat accumulation in intracytoplasmic vesicle at 5 uM after 48 hrs by Bligh and Dyer method2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis of new alkylaminooxysterols with potent cell differentiating activities: identification of leads for the treatment of cancer and neurodegenerative diseases.
AID1385439Antitumor activity against human MCF7 cells xenografted in nude Balb/c mouse assessed as reduction in tumor burden at 25 mg/kg, po administered once every 2 days via gavage measured on day 122018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Novel Hybrid Conjugates with Dual Suppression of Estrogenic and Inflammatory Activities Display Significantly Improved Potency against Breast Cancer.
AID1297989Antiparasitic activity against amastigote stage of Leishmania chagasi MHOM/BR/1972/LD infected in golden hamster assessed as reduction in parasite load at 20 mg/kg, ip administered for 15 days measured after 4 weeks by limiting dillution method2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Repurposing strategies for tropical disease drug discovery.
AID1705344Antiproliferative activity against human OVCAR-3 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1438378Cytotoxicity against human T47D cells assessed as growth inhibition after 120 hrs by MTT assay2017European journal of medicinal chemistry, Mar-10, Volume: 128Synthesis and biological evaluation of fluorinated N-benzoyl and N-phenylacetoyl derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as steroid sulfatase inhibitors.
AID676724Inhibition of human AChE pre-incubated for 10 mins before acetylthiocholine iodide substrate addition2012Journal of natural products, Jul-27, Volume: 75, Issue:7
Geranylphenazinediol, an acetylcholinesterase inhibitor produced by a Streptomyces species.
AID437139Anticancer activity against estrogen-positive human MDA-MB-231 cells after 18 hrs by MTT assay2009European 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.
AID302178Antiproliferative activity against human HL60 cells assessed as cell viability at 20 ug/ml after 4 hrs by MTT assay2007Bioorganic & 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.
AID392053Antiproliferative activity against human MCF7 cells after 24 hrs by MTS assay2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Synthesis and preliminary biological evaluation of new carbon-11 labeled tetrahydroisoquinoline derivatives as SERM radioligands for PET imaging of ER expression in breast cancer.
AID1438377Cytotoxicity against human MCF7 cells assessed as growth inhibition after 120 hrs by MTT assay2017European journal of medicinal chemistry, Mar-10, Volume: 128Synthesis and biological evaluation of fluorinated N-benzoyl and N-phenylacetoyl derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as steroid sulfatase inhibitors.
AID682125TP_TRANSPORTER: RT-PCR in vivo, liver of Lewis rat2000Biochemical pharmacology, Jul-15, Volume: 60, Issue:2
Association of tamoxifen biliary excretion rate with prior tamoxifen exposure and increased mdr1b expression.
AID1593146Cytotoxicity against human HEK293 cells assessed as reduction in cell growth incubated for 20 hrs by resazurin dye-based fluorometric assay2019European journal of medicinal chemistry, Apr-15, Volume: 168Cationic biaryl 1,2,3-triazolyl peptidomimetic amphiphiles: synthesis, antibacterial evaluation and preliminary mechanism of action studies.
AID1372346Antiproliferative activity against human MCF7 cells2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Design, synthesis and biological evaluation of novel indole-xanthendione hybrids as selective estrogen receptor modulators.
AID1518641Antiproliferative activity against human M-HeLa cells by fluorescence based viable cell counting method2019European journal of medicinal chemistry, Dec-15, Volume: 184New 2,6-diaminopyridines containing a sterically hindered benzylphosphonate moiety in the aromatic core as potential antioxidant and anti-cancer drugs.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal 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.
AID242363Inhibition of [3H]estradiol binding to human estrogen receptor beta expressed in HeLa cells; not determined2005Journal 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.
AID1693877Selectivity index, ratio of IC50 for ER- negative human MDA-MB-231 cells to IC50 for ER and PR-positive human MCF7 cells2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Synthesis, antitumor activity and structure-activity studies of novel pyridoxine-based bioisosteric analogs of estradiol.
AID1676125Selectivity index, ratio of CC50 for human A549 cells to IC50 for antiviral activity against pseudotyped Ebola virus - Mayinga, Zaire infected in human A549 cells2020Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors.
AID345065Estrogenic stimulatory activity in human Ishikawa cells assessed as alkaline phosphatase activity at 1 uM after 72 hrs in absence of estradiol2008Bioorganic & 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.
AID197475Minimum fully effective dose that prevented implantation of eggs in three out of three rats (MFED) (antifertility)1983Journal 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.
AID103541Inhibition of MCF-7 cell proliferation at 100 nM1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Carboxylic acid analogues of tamoxifen: (Z)-2-[p-(1, 2-diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine. Estrogen receptor affinity and estrogen antagonist effects in MCF-7 cells.
AID38726Relative binding affinity against Antiestrogen binding site(AEBS)1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans.
AID188122Initial tumor number in DMBA-induced tumor bearing rats at 3 mg dose (experiment-1)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity.
AID1350707Apparent permeability cross apical to basolateral side in MDCK-MDR1 cells at 5 uM after 90 mins by LC-MS/MS analysis2018Journal 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.
AID1705384Antiproliferative activity against human SF-268 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID248083Inhibition of estrogen-mediated human breast adenocarcinoma (MCF-7) cell proliferation2005Journal 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.
AID242722Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor alpha; ERE assay2005Journal 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.
AID1570858Toxicity in BALB/c mouse implanted with mouse 4T1 cells assessed as body weight at 5 mg/kg/day, ip for 2 weeks measured during compound dosing (Rvb = -1.48 %)2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
A Bioreductive Prodrug of Cucurbitacin B Significantly Inhibits Tumor Growth in the 4T1 Xenograft Mice Model.
AID778637Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay2013European journal of medicinal chemistry, Sep, Volume: 673D-QSAR using pharmacophore-based alignment and virtual screening for discovery of novel MCF-7 cell line inhibitors.
AID41241In vivo antitumor activity against hormone-dependent MXT-M 3.2 mammary tumor in BDF1 mouse at a dose of 20 umol/kg.2002Journal 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.
AID1310512Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 72 hrs by trypan blue assay2016European journal of medicinal chemistry, Aug-08, Volume: 1184-(1,2-diarylbut-1-en-1-yl)isobutyranilide derivatives as inhibitors of topoisomerase II.
AID759308Therapeutic index, ratio of IC50 for african green monkey Vero cells to IC50 for human MCF7 cells expressing ERalpha and ERbeta2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.
AID764643Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Design, synthesis and biological evaluation of novel triaryl (Z)-olefins as tamoxifen analogues.
AID124167Uterine weight after 9 day treatment at 0.42 ug by oral gavage to ovariectomised mice without estrone1997Journal 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.
AID1161693Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents.
AID1170541Binding affinity to human ERalpha2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
β-Lactam estrogen receptor antagonists and a dual-targeting estrogen receptor/tubulin ligand.
AID455712Anticancer activity against human NCI-H460 cells after 24 hrs by SRB assay2009Bioorganic & 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.
AID1576206Antiproliferative activity against human MCF7cells assessed as reduction in cell viability after 24 hrs by DAPI/propidium iodide staining based assay2019MedChemComm, Aug-01, Volume: 10, Issue:8
Synthesis and anti-cancer activities of glycosides and glycoconjugates of diterpenoid isosteviol.
AID765191Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2013Bioorganic & 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.
AID455713Inhibition of bovine tubulin polymerization after 30 mins by turbidimetrically2009Bioorganic & 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.
AID1705335Antiproliferative activity against human Malme-3M cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1662876Selectivity index, ratio of IC50 for human Chang cells to IC50 for human MCF7 cells2020Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13
Design and synthesis of amphiphilic 2-hydroxybenzylphosphonium salts with antimicrobial and antitumor dual action.
AID103891Inhibition of 10e-4 uM estradiol induced estrogen receptor positive MCF-7 human breast cancer cell proliferation1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Novel 5-aminoflavone derivatives as specific antitumor agents in breast cancer.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1197743Inhibition of human OATP1B1-mediated [3H]estrone 3-sulfate at 100 uM after 5 mins relative to control2015European journal of medicinal chemistry, Mar-06, Volume: 92Interaction of human organic anion transporter polypeptides 1B1 and 1B3 with antineoplastic compounds.
AID1254842Cytotoxicity against normal human astrocytes assessed as cell viability incubated for 72 hrs by WST-1 method2015European journal of medicinal chemistry, Oct-20, Volume: 103Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID597267Antiproliferative activity against human MCF7 cells expressing estrogen receptor 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 NuSerum2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Biomimetic syntheses and antiproliferative activities of racemic, natural (-), and unnnatural (+) glyceollin I.
AID667233Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel (E) stilbene-based antitumor agents.
AID258224Relative binding affinity for ER by a competitive [3H]estradiol binding assay2006Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2
Synthesis and biological activities of nucleoside-estradiol conjugates.
AID1464227Antagonist activity at full length ERbeta (unknown origin) expressed in human HeLa cells incubated for 24 hrs by ERE-driven luciferase reporter gene assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Design and synthesis of benzoacridines as estrogenic and anti-estrogenic agents.
AID358590Cytotoxicity against human HT-29 cells by alamar blue assay2001Journal of natural products, Nov, Volume: 64, Issue:11
Isolation and biological evaluation of filiformin, plakortide F, and plakortone G from the Caribbean sponge Plakortis sp.
AID1646797Chaperone activity at GCase L444P GBA gene mutant in human fibroblasts derived from Gaucher patient assessed as increase in GPN-induced reduction of calcium release using Fluo-8AM based fluorescence assay2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells.
AID1284734Cytotoxicity against human MDA-MB-468 cells assessed as growth inhibition after 48 hrs by SRB assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
AID1463976Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
Synthesis and electronic properties of ester substituted 1,4-dicyanodibenzodioxins and evaluation of anti-proliferative activity of all isomeric 1,2-, 2,3- and 1,4-dicyanodibenzodioxins against HeLa cell line.
AID667231Cytotoxicity against human DLD1 cells after 96 hrs by SRB assay2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel (E) stilbene-based antitumor agents.
AID1065294Cytotoxicity against human MG63 cells after 48 hrs by MTT assay2013European journal of medicinal chemistry, Aug, Volume: 66Diversity-oriented synthesis of α-aminophosphonates: a new class of potential anticancer agents.
AID1595023Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 20 hrs by resazurin dye-based fluorescence assay2019European journal of medicinal chemistry, May-15, Volume: 170Cationic biaryl 1,2,3-triazolyl peptidomimetic amphiphiles targeting Clostridioides (Clostridium) difficile: Synthesis, antibacterial evaluation and an in vivo C. difficile infection model.
AID471237Inhibition of fluormone ES2 binding to estrogen receptor beta after 1 hr by fluorescence polarization assay2009Journal 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.
AID1628321Antiestrogenic activity in human T47D cells assessed as compound concentration required to decrease 100 pM E2-induced cell proliferation to equivalent levels induced by 10 pM E2 after 96 hrs by alamar blue assay2016Journal of natural products, 05-27, Volume: 79, Issue:5
Furofuran Lignan Glucosides with Estrogen-Inhibitory Properties from the Bangladeshi Medicinal Plant Terminalia citrina.
AID1562216Antiproliferative activity against human MelJuSo cells assessed as reduction in cell viability measured after 24 hrs by celltiter-blue assay2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Nitric Oxide-Releasing Selective Estrogen Receptor Modulators: A Bifunctional Approach to Improve the Therapeutic Index.
AID597277Antiproliferative activity against human LNCAP cells expressing androgen receptor incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Biomimetic syntheses and antiproliferative activities of racemic, natural (-), and unnnatural (+) glyceollin I.
AID597274Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Biomimetic syntheses and antiproliferative activities of racemic, natural (-), and unnnatural (+) glyceollin I.
AID1209428Induction of apoptosis in human hepatocytes assessed as caspase 3/7 activation by caspase-Glo 3/7 assay2012Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
In vitro hepatotoxicity and cytochrome P450 induction and inhibition characteristics of carnosic acid, a dietary supplement with antiadipogenic properties.
AID1057863Cytotoxicity against mouse dividing ScN2a-cl3 cells assessed as cell viability after 5 days by calcein-AM staining-based fluorescence assay2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Antiprion compounds that reduce PrP(Sc) levels in dividing and stationary-phase cells.
AID101569Inhibition of estrogen receptor positive MCF-7 human breast cancer cell proliferation1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Inhibition of tubulin polymerization by 5,6-dihydroindolo[2,1-alpha]isoquinoline derivatives.
AID1242129Anti-proliferative activity against human HepG2 cells incubated for 48 hrs by SRB assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Design, synthesis and anticancer properties of novel oxa/azaspiro[4,5]trienones as potent apoptosis inducers through mitochondrial disruption.
AID178720Dose required to reduce serum cholesterol by 50% relative to ovariectomized (OVX) controls1998Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
Synthesis and pharmacology of conformationally restricted raloxifene analogues: highly potent selective estrogen receptor modulators.
AID306817Antagonist activity at human recombinant ERalpha expressed in MCF7 cells assessed as ERE-driven transactivation at 2.5 uM by luciferase reporter assay relative to estradiol2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Identification of a series of tetrahydroisoquinoline derivatives as potential therapeutic agents for breast cancer.
AID250404Percent antagonist activity against human breast adenocarcinoma (MCF-7) cell proliferation2005Journal 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.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1676126Antiviral activity against pseudotyped Ebola virus - Mayinga, Zaire infected in human A549 cells assessed as reduction in viral infection incubated for 48 hrs by luciferase reporter gene assay2020Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors.
AID70988Binding affinity towards calf uterine estrogen receptor using [3H]17-beta-estradiol as radioligand1991Journal 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.
AID468984Inhibition of human 17beta-HSD7 expressed in HEK293 cells assessed as inhibition of reduction of [14C]estrone into [14C]estradiol at 0.3 uM after 7 hrs2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Potent and selective steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 7, an enzyme that catalyzes the reduction of the key hormones estrone and dihydrotestosterone.
AID1562214Antiproliferative activity against human MelJuSo cells assessed as cell viability at 50 uM measured after 24 hrs by celltiter-blue assay relative to control2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Nitric Oxide-Releasing Selective Estrogen Receptor Modulators: A Bifunctional Approach to Improve the Therapeutic Index.
AID761776Cytotoxicity against human MCF7 cells by SRB assay2013Journal of natural products, Jul-26, Volume: 76, Issue:7
Bioactive compounds from the roots of Strophioblachia fimbricalyx.
AID561221Antifungal activity against Candida albicans SC5314 at 16 ug/ml after 2 hrs by alexa fluor-phalloidin staining2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID102768Percent of effective dose for [3H]estradiol against proliferation of MCF-7 cells.1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Effect of triphenylacrylonitrile derivatives on estradiol-receptor binding and on human breast cancer cell growth.
AID71132Relative binding affinity was measured on calf uterus estrogen receptor after 5 hr at 25C.1992Journal 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.
AID678714Inhibition 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 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID681588TP_TRANSPORTER: ATPase assay in membrane vesicle from BCRP-expressing Lactococcus lactis cells2003The Journal of biological chemistry, Jun-06, Volume: 278, Issue:23
Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis.
AID723802Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay2013European journal of medicinal chemistry, Feb, Volume: 60Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent.
AID1079931Moderate 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]
AID1693880Cytotoxicity against ER-negative human MDA-MB-231 cells assessed as reduction in colony formation incubated for 7 days by crystal violet staining based assay2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Synthesis, antitumor activity and structure-activity studies of novel pyridoxine-based bioisosteric analogs of estradiol.
AID324577Effect on FYVE-RFP+ vesicle intensity per cell in human H4 cells after 4 hrs relative to control2007Proceedings 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.
AID673829Cytotoxicity against human T47D cells after 5 days2012ACS medicinal chemistry letters, Apr-06, Volume: 3, Issue:5
Boron-Based 4-Hydroxytamoxifen Bioisosteres for Treatment of de Novo Tamoxifen Resistant Breast Cancer.
AID1545844Antiproliferative activity against human HeLa cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID38612Relative binding affinity for antiestrogen binding site (AEBS) of calf uterus 2 hr incubation at 0C1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Effect of triphenylacrylonitrile derivatives on estradiol-receptor binding and on human breast cancer cell growth.
AID759311Cytotoxicity against ERalpha-deficient human DU145 cells expressing ERbeta assessed as growth inhibition after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.
AID620853Effect 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 %)2011European 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.
AID188612The compound was tested for the growth of tumors at 10 mg/kg dose start of the experiment after peroral administration (experiment-2)1984Journal 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
AID324575Induction of autophagy in human H4 cells2007Proceedings 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.
AID1310510Cytotoxicity against human OVCAR5 cells assessed as cell growth inhibition after 72 hrs by MTS assay2016European journal of medicinal chemistry, Aug-08, Volume: 1184-(1,2-diarylbut-1-en-1-yl)isobutyranilide derivatives as inhibitors of topoisomerase II.
AID1254844Selectivity index, ratio of IC50 for normal human astrocytes to IC50 for human GBM2 cells2015European journal of medicinal chemistry, Oct-20, Volume: 103Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID71148Displacement of 5 nM [3H]-estradiol from the estrogen receptor of MCF-7 whole cell lysates1992Journal 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.
AID491954Cytotoxicity against human HepG2 cells after 24 hrs by CellTiter-BlueCell viability assay2010Journal of natural products, Jul-23, Volume: 73, Issue:7
Mayamycin, a cytotoxic polyketide from a Streptomyces strain isolated from the marine sponge Halichondria panicea.
AID1284375Selectivity ratio of IC50 for human ER-alpha to IC50 for human ER-beta2016European journal of medicinal chemistry, Apr-13, Volume: 112Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
AID344794Antiproliferative activity against hormone independent human MDA-MB-231 cells upto 100 nM after 72 hrs by MTT assay2008Bioorganic & 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.
AID68906Inhibition of estradiol binding to estrogen receptor in Human Breast cancer cytosol (3.3% ethanol)1997Journal 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.
AID471240Antagonist activity at estrogen receptor in human MCF7 cells assessed as 17-beta-estradiol-induced cell proliferation after 24 hrs by [14C]thymidine incorporation assay2009Journal 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.
AID620852Effect 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 %)2011European 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.
AID1366597Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Syntheses of conformationally restricted benzopyran based triarylethylenes as growth inhibitors of carcinoma cells.
AID1705311Antiproliferative activity against human MOLT-4 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID561043Antifungal activity against Saccharomyces cerevisiae BY4741 expressing CMD1 at 62 to 125 ug/mL after 3 days by photographic analysis2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID482354Selectivity ratio for ERalpha to ERbeta2010Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14
Discovery of potent ligands for estrogen receptor beta by structure-based virtual screening.
AID1705361Antiproliferative activity against human BT-549 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1628322Antiestrogenic 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 assay2016Journal of natural products, 05-27, Volume: 79, Issue:5
Furofuran Lignan Glucosides with Estrogen-Inhibitory Properties from the Bangladeshi Medicinal Plant Terminalia citrina.
AID1254841Antiproliferative activity against human GBM2 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method2015European journal of medicinal chemistry, Oct-20, Volume: 103Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID188611The compound was tested for the growth of tumors at 10 mg/kg dose finish of the experiment after peroral administration (experiment-2)1984Journal 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
AID1686038Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 4 hrs by CellTiter-Glo assay2016Journal 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.
AID1518642Antiproliferative activity against human MCF7 cells by fluorescence based viable cell counting method2019European journal of medicinal chemistry, Dec-15, Volume: 184New 2,6-diaminopyridines containing a sterically hindered benzylphosphonate moiety in the aromatic core as potential antioxidant and anti-cancer drugs.
AID1283275Inhibition of DR24 in mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis2016Journal 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.
AID1524896Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 24 hrs by resazurin dye based fluorimetric assay2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Phosphonodiamidate prodrugs of N-alkoxy analogs of a fosmidomycin surrogate as antimalarial and antitubercular agents.
AID103526Inhibition of estrogen receptor positive MCF-7 cell proliferation as cell number after 10 days at 10e-6 M1981Journal 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.
AID1217729Intrinsic 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 formation2011Drug 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.
AID1693882Selectivity 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 cells2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Synthesis, antitumor activity and structure-activity studies of novel pyridoxine-based bioisosteric analogs of estradiol.
AID69514Relative binding affinity(RBA) against estrogen (ER) in rat liver1992Journal 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.
AID1291378Cytotoxicity against human ER-positive MCF7 cells assessed as cell viability after 72 hrs by MTT assay2016Bioorganic & 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.
AID1705321Antiproliferative activity against human NCI-H522 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1193494Thermodynamic equilibrium solubility, log S of the compound in simulated gastric fluid at pH 1.2 at RT after 4 hrs by 96 well plate method2015Bioorganic & 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.
AID191676Uterotrophic effect in rats uterine at 1 ug/day dose1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent.
AID1660979Inhibition of Escherichia coli shiga toxin2020Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
Structure-Activity Relationship Studies of Retro-1 Analogues against Shiga Toxin.
AID239347Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand2005Journal 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.
AID1688066Antiproliferative 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 assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition.
AID1471126Antiproliferative activity against human Ishikawa cells after 48 hrs by MTT assay2017Bioorganic & 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.
AID491597Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Synthesis and anti breast cancer activity of biphenyl based chalcones.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID728186Antagonist activity at ERalpha receptor in human MCF7 cells assessed as inhibition of cell growth after 6 days by crystal violet staining method2013Journal 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.
AID103535Inhibition of estrogen receptor positive MCF-7 cell proliferation as cell number after 10 days at 10e-8 M1981Journal 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.
AID1833429Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay
AID243422log (1/Km) value for human liver microsome cytochrome P450 3A42005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Modeling K(m) values using electrotopological state: substrates for cytochrome P450 3A4-mediated metabolism.
AID1158153Cytotoxicity against human HEK293 cells after 24 hrs by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Synthesis and anticancer activity of γ-(triazolyl ethylidene)butenolides and polyfunctional pyrrolinones.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID1833412Toxicity in Sprague-Dawley rat inoculated with rat LA7 cells assessed as increase in uterine tissue at 10 mg/kg administered daily for 21 days
AID1530771Stimulation of cell proliferation in human Ishikawa cells at 1 to 10 uM after 48 hrs by MTT assay2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2.
AID1465924Cytotoxicity against human MCF7 cells assessed as reduction in cell viability at 5 uM after 24 hrs by MTT assay relative to control2017Journal 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.
AID344802Antiestrogenic activity in human Ishikawa cells assessed as inhibition of estrogen-induced alkaline phosphatase activity after 72 hrs2008Bioorganic & 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.
AID124168Uterine weight after 9 day treatment at 0.42 ug by oral gavage to ovariectomised mice with estrone1997Journal 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.
AID548941Growth inhibition of human MCF7 cells at 50 ug/ml after 24 hrs by MTT colorimetric assay2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Isochaihulactone analogues: synthesis and anti-proliferative activity of novel dibenzylbutyrolactones.
AID1530774Antagonist 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 method2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2.
AID102757Effect on hormone-dependent MCF-7 human breast cancer cell proliferation at 1x10E-6M1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Indolo[2,1-a]isoquinolines. Syntheses, steroid hormone receptor binding affinities, and cytostatic activity.
AID781329pKa (acid-base dissociation constant) as determined by other workers2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1348843Growth inhibition of human MCF7 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143New estrogen receptor antagonists. 3,20-Dihydroxy-19-norpregna-1,3,5(10)-trienes: Synthesis, molecular modeling, and biological evaluation.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1578359Antimycobacterial activity activity against Mycobacterium tuberculosis H37Rv after 7 days by rezasurin-dye based spectrophotometric analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Novel thiazolidinedione-hydroxamates as inhibitors of Mycobacterium tuberculosis virulence factor Zmp1.
AID1754977Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Design, synthesis and broad spectrum antibreast cancer activity of diarylindoles via induction of apoptosis in aggressive breast cancer cells.
AID491600Cytotoxicity against HEK293 cells after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Synthesis and anti breast cancer activity of biphenyl based chalcones.
AID1473740Inhibition 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 assay2013Toxicological 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.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1310518Induction 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%)2016European journal of medicinal chemistry, Aug-08, Volume: 1184-(1,2-diarylbut-1-en-1-yl)isobutyranilide derivatives as inhibitors of topoisomerase II.
AID643383Induction of phospholipidosis in bovine corneal fibroblasts assessed as lamellar inclusion bodies after 72 hrs by light microscopy2012Journal 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.
AID103745Inhibition of [3H]thymidine incorporation into MCF-7 cells1992Journal 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.
AID188737The compound was tested for the progression of no of tumors at 10 mg/kg dose after peroral administration (experiment-2)1984Journal 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
AID302174Antiproliferative activity against human HL60 cells assessed as cell viability after 4 hrs by MTT assay2007Bioorganic & 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.
AID681126TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells2001Biochemical and biophysical research communications, Nov-30, Volume: 289, Issue:2
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
AID191680Uterotrophic effect in rats uterine at 10 ug/day dose in presence of 0.16 ug estradiol1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent.
AID136040Relative tumor weight in treated compared to control mice bearing hormone-dependent transplanted MXT mammary tumors at 8.8mg1991Journal 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.
AID398078Displacement of [3H]estradiol form ERalpha in rat uterine cytosol after 22 hrs by charcol adsorption method relative to 17-beta-estradiol2009Bioorganic & 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.
AID470168Antiestrogenic 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 assay2009Journal of natural products, Nov, Volume: 72, Issue:11
Antiestrogenic constituents of the Thai medicinal plants Capparis flavicans and Vitex glabrata.
AID1401998Inhibition of estrogen receptor (unknown origin)2018European journal of medicinal chemistry, Jan-01, Volume: 143Tamoxifen a pioneering drug: An update on the therapeutic potential of tamoxifen derivatives.
AID103267Inhibition of estrogen-induced proliferation in human MCF-7 breast cancer cells1997Journal 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.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1366607Cell 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%)2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Syntheses of conformationally restricted benzopyran based triarylethylenes as growth inhibitors of carcinoma cells.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1348845Growth inhibition of human MCF10A cells at <25 uM after 72 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143New estrogen receptor antagonists. 3,20-Dihydroxy-19-norpregna-1,3,5(10)-trienes: Synthesis, molecular modeling, and biological evaluation.
AID1323680Displacement of Fluormone ES2 Green from human recombinant full length ERalpha expressed in insect cells measured up to 4 hrs by fluorescence polarization assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Design and synthesis of triarylacrylonitrile analogues of tamoxifen with improved binding selectivity to protein kinase C.
AID1530769Antiproliferative activity against HUVEC after 48 hrs by MTT assay2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2.
AID176940Dose required to reduce serum cholesterol by 50% relative to OVX controls was determined (in vivo)1997Journal 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.
AID540237Phospholipidosis-positive literature compound observed in rat
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID561227Antifungal activity against Candida dubliniensis CD1 after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID1688053Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 48 hrs by SRB assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition.
AID1140199Displacement of fluorescent estrogen from recombinant ERalpha (unknown origin) at 0.1 mg/ml by competition binding assay2014Bioorganic & 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.
AID1323678Inhibition 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 control2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Design and synthesis of triarylacrylonitrile analogues of tamoxifen with improved binding selectivity to protein kinase C.
AID184853Minimally effective dose(MED) (mg/kg body weight) at which a statistically significant (p<= 0.05) increase in uterine weight/body weight was observed1998Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
Synthesis and pharmacology of conformationally restricted raloxifene analogues: highly potent selective estrogen receptor modulators.
AID1705312Antiproliferative activity against human RPMI-8226 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID548942Growth inhibition of human T47D cells at 25 ug/ml after 24 hrs by MTT colorimetric assay2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Isochaihulactone analogues: synthesis and anti-proliferative activity of novel dibenzylbutyrolactones.
AID1693876Cytotoxicity against human HSF cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Synthesis, antitumor activity and structure-activity studies of novel pyridoxine-based bioisosteric analogs of estradiol.
AID1530767Displacement of fluorescent estrogen ligand from recombinant human full length untagged ERalpha expressed in Spodoptera frugiperda insect cells measured after 2 hrs by fluorescence polarization assay2019European journal of medicinal chemistry, Jan-01, Volume: 161Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2.
AID136219In vivo inhibition of hormone-dependent MXT mammary tumor in mice1986Journal 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.
AID1209973Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID282035Decrease DOX-TEG-TAM uptake in MDA-MB-435 cells at 10 uM after 1 hr relative to control2004Journal 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.
AID1140201Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2014Bioorganic & 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.
AID1705354Antiproliferative activity against human TK-10 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID497603Displacement of [2,4,6,7-3H]estradiol from human ERalpha expressed in HeLa cells after 18 hrs by liquid scintillation counting relative to estradiol2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha.
AID101600Inhibitory concentration against MCF-7 (ER+) cell line using SRB assay2003Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3
A facile synthesis of C(2)-symmetric 17 beta-estradiol dimers.
AID103059Inhibition of hormone-sensitive MCF-7 mammary tumor cell proliferation at 5*10e-6 M1992Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19
6-Alkyl-12-formylindolo[2,1-a]isoquinolines. Syntheses, estrogen receptor binding affinities, and stereospecific cytostatic activity.
AID1646800Inhibition of beta-estradiol-induced estradiol receptor activation (unknown origin) at 10 uM relative to control2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells.
AID393028Cytotoxicity against rat L6 cells2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
New potent imidazoisoquinolinone derivatives as anti-Trypanosoma cruzi agents: biological evaluation and structure-activity relationships.
AID270146Cytotoxicity against human KB cells2006Journal 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.
AID678555Cytotoxicity against human HL60 cells after 72 hrs by WST1 assay in presence of 20% FBS2012Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
Synthesis and cytotoxic activity of non-naturally substituted 4-oxycoumarin derivatives.
AID1171738Antiproliferative activity against human K562 cells after 72 hrs2014Journal of natural products, Dec-26, Volume: 77, Issue:12
Injury-induced biosynthesis of methyl-branched polyene pigments in a white-rotting basidiomycete.
AID1254847Selectivity index, ratio of IC50 for normal human astrocytes to IC50 for human GBM3 cells2015European journal of medicinal chemistry, Oct-20, Volume: 103Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID1740176Cytotoxicity against HEK293 cells measured after 20 hrs by resazurin dye based fluorescence assay2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis, antibacterial and antifungal activity of new 3-biphenyl-3H-Imidazo[1,2-a]azepin-1-ium bromides.
AID1284701Cytotoxicity against human SNB75 cells assessed as growth inhibition after 48 hrs by SRB assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
AID1366601Selectivity index, ratio of IC50 for HEK293 cells to IC50 for human MCF7 cells2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Syntheses of conformationally restricted benzopyran based triarylethylenes as growth inhibitors of carcinoma cells.
AID71133Relative binding affinity against estrogen receptor in calf uterus cytosol using [3H]E2 as radioligand, incubated at 2 hours at 0 degree Centigrade.1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Effect of triphenylacrylonitrile derivatives on estradiol-receptor binding and on human breast cancer cell growth.
AID1283248Inhibition of delta 8-7 isomerase in Dhcr7-deficient mouse Neuro2a cells assessed as increase in zymostenol levels at 1 uM by LC-MS/GC-MS analysis2016Journal 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.
AID1356870Antitumor activity against human MCF7 cells xenografted in nu/nu mouse model of tamoxifen-sensitive breast cancer xenograft implanted with 17beta-estradiol time release pellets assessed as reduction tumor volume at 60 mg/kg, po qd for 4 weeks2018Journal 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.
AID1636454Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 25.5 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of N2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID179472Percentage static unchanged DMBA-induced mammary tumors in rats at 3 mg dose (experiment-1)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity.
AID69517In vitro relative binding affinity for rat uterine estrogen receptor compared to [3H]estradiol1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Hydroxy derivatives of tamoxifen.
AID759300Cytotoxicity against ERalpha and ERbeta-deficient human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.
AID736612Growth inhibition of human HT-29 cells2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Synthesis and growth inhibition activity of fluorinated derivatives of tamoxifen.
AID1536898Cytotoxicity against human MRC5 SV2 cells after 3 days by resazurin dye based fluorescence assay2019Bioorganic & medicinal chemistry, 02-15, Volume: 27, Issue:4
Synthesis and antimicrobial activities of N
AID173696Percent decrease in serum cholesterol relative to OVX control at 10 mg/kg in rat was determined (in vivo)1997Journal 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.
AID681613TP_TRANSPORTER: intracellular accumulation in MDR1-expressing LLC-PK1 cells2000Molecular pharmacology, Jan, Volume: 57, Issue:1
Cloning and expression of murine sister of P-glycoprotein reveals a more discriminating transporter than MDR1/P-glycoprotein.
AID1310511Induction of mitochondrial membrane depolarization in human HeLa cells at 25 uM after 28 hrs by JC-1 staining-based flow cytometric analysis (Rvb = 4%)2016European journal of medicinal chemistry, Aug-08, Volume: 1184-(1,2-diarylbut-1-en-1-yl)isobutyranilide derivatives as inhibitors of topoisomerase II.
AID498479Stimulation of human PLD2 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins by exogenous substrate assay2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID105213Inhibition of MDA-MB-435 breast cancer cell proliferation2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Design, synthesis, and biological evaluation of doxorubicin-formaldehyde conjugates targeted to breast cancer cells.
AID392617Growth inhibition of human estrogen-dependent T47D cells after 72 hrs2009Bioorganic & 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).
AID1705324Antiproliferative activity against human HCT-116 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1545837Cytotoxicity against HEK293 cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID561039Antifungal activity against Candida albicans SC5314 assessed as disruption of cell wall integrity-associated adenylate kinase release at 32 ug/ml by hemocytometry2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID1545927Antiproliferative activity against human DU145 cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID561229Antifungal activity against Candida tropicalis MR064-H after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID1418620Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay2018Bioorganic & medicinal chemistry, 11-15, Volume: 26, Issue:21
Synthesis, computational studies and antiproliferative activities of coumarin-tagged 1,3,4-oxadiazole conjugates against MDA-MB-231 and MCF-7 human breast cancer cells.
AID1209452Inactivation of CYP2B6 (unknown origin) expressed in Escherichia coli C41 DE3 cells assessed as modified apo-P450 2B6 adduct formation at 60 uM after 10 mins by ESI-LC-MS analysis in presence of NADPH2012Drug 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.
AID1366599Antiproliferative activity against HEK293 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Syntheses of conformationally restricted benzopyran based triarylethylenes as growth inhibitors of carcinoma cells.
AID1327717Anticancer activity against human ER-positive MCF7 cells measured after 48 hrs by SRB assay2016Bioorganic & 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.
AID358592Cytotoxicity against human SK-MEL-28 cells by alamar blue assay2001Journal of natural products, Nov, Volume: 64, Issue:11
Isolation and biological evaluation of filiformin, plakortide F, and plakortone G from the Caribbean sponge Plakortis sp.
AID561225Antifungal activity against Candida albicans SC5314 after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID1705353Antiproliferative activity against human SN12C cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID1129456Solubility of the compound in PBS buffer after 45 mins2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID1387894Antagonist activity at estrogen receptor alpha/beta in human Ishikawa cells after 72 hrs by alkaline phosphatase assay2018Journal 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.
AID1209450Drug metabolism in human liver microsomes assessed as 4-hydroxytamoxifen quinone methide formation by measuring reactive metabolite adduct with GSHEE at 90 uM by LC-MS/MS analysis2012Drug 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.
AID1323681Inhibition of PKC in human SH-SY5Y cells assessed as inhibition of PMA-stimulated MARCKS phosphorylation preincubated for 1 hr followed by PMA-stimulation for 15 mins by Western blot analysis2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Design and synthesis of triarylacrylonitrile analogues of tamoxifen with improved binding selectivity to protein kinase C.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID184852Minimally effective dose(MED) (mg/kg body weight) at which a significant increase in EPO activity was observed in rats1998Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
Synthesis and pharmacology of conformationally restricted raloxifene analogues: highly potent selective estrogen receptor modulators.
AID667230Cytotoxicity against human A2780 cells after 96 hrs by SRB assay2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel (E) stilbene-based antitumor agents.
AID1284372Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
AID102423Effect of compound with 10e-8 M estradiol on the growth of MCF-7 cells at a concentration 10 e-7 M, percentage of control value being 911985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Hydroxy derivatives of tamoxifen.
AID561228Antifungal activity against Candida glabrata MR084-G12 after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID1768141Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by Cell-titer Glo assay
AID164971Percent stimulation or inhibition of protein kinase C III activity for phosphatidylserine (PS) in the presence of [Ca2+].1992Journal 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.
AID55209Inhibition of Calmodulin activation of cyclic nucleotide phosphodiesterase1992Journal of medicinal chemistry, Mar-06, Volume: 35, Issue:5
Antiestrogens. 3. Estrogen receptor affinities and antiproliferative effects in MCF-7 cells of phenolic analogues of trioxifene, [3,4-dihydro-2-(4- methoxyphenyl)-1-naphthalenyl][4-[2-(1-pyrrolidinyl)ethoxy]- phenyl]methanone.
AID102624Percent of inhibitory activity versus 0.1 nm [3H]estradiol against proliferation of MCF-7 cells.1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Effect of triphenylacrylonitrile derivatives on estradiol-receptor binding and on human breast cancer cell growth.
AID69068Relative affinity for estrogen receptor of Human Breast cancer or normal uterine cytosol (3.3%ethanol) compared to estradiol1997Journal 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.
AID134368In vitro estrogenic effect in immature mice at 1 ug1986Journal 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.
AID103082Inhibition of estradiol induced estrogen receptor transcriptional activation in MCF-7-2a cells2003Journal 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.
AID1567373Cytotoxicity against human MDA-MB-231 cells2019European journal of medicinal chemistry, Sep-15, Volume: 178Tetrazole hybrids with potential anticancer activity.
AID759301Cytotoxicity against human MCF7 cells expressing ERalpha and ERbeta assessed as growth inhibition after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.
AID101601Inhibition of estrogen receptor positive MCF-7 breast cancer cell proliferation2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Design, synthesis, and biological evaluation of doxorubicin-formaldehyde conjugates targeted to breast cancer cells.
AID1364838Inhibition of estradiol-induced proliferation in human MDA-MB-231 cells after 72 hrs by Cell-titer-Glo assay2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Functional evaluation of synthetic flavonoids and chalcones for potential antiviral and anticancer properties.
AID179143Complete remission of DMBA-induced mammary tumors in rats at 3 mg dose1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity.
AID1464224Antagonist activity at full length ERalpha (unknown origin) expressed in human HeLa cells incubated for 24 hrs by ERE-driven luciferase reporter gene assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Design and synthesis of benzoacridines as estrogenic and anti-estrogenic agents.
AID597270Antiproliferative activity against human MCF7 cells expressing estrogen receptor incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Biomimetic syntheses and antiproliferative activities of racemic, natural (-), and unnnatural (+) glyceollin I.
AID614547Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 48 hrs by MTT assay2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Design and synthesis of 1,3-biarylsulfanyl derivatives as new anti-breast cancer agents.
AID1705332Antiproliferative activity against human SNB-75 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1387898Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length estrogen receptor beta after 2 hrs by fluorescence polarization assay relative to estradiol2018Journal 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.
AID276686Agonist activity at ER receptor assessed as increase in uterine weight of Sprague-Dawley rat at 3 mg/kg/day, po relative to control2006Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23
Rapid synthesis of 4-benzylidene and 4-[bis-(4-methoxyphenyl)-methylene-2-substituted phenyl-benzopyrans as potential selective estrogen receptor modulators (SERMs) using McMurry coupling reaction.
AID1210016Inhibition of CYP2C8 in human liver microsomes using paclitaxel as substrate after 8 mins by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1493790Aqueous solubility in PBS after 2 hrs2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID1395070Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ERα/VEGFR-2 ligands with anti-breast cancer activity.
AID1705360Antiproliferative activity against human Hs-578T cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID186067Uterotrophic effect in rats at 10.0 ug/day dose1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent.
AID69058Percent relative binding affinity (RBA) for estrogen receptor compared to estradiol1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
Molecular structures and conformational studies of triarylcyclopropyl and related nonsteroidal antiestrogens.
AID1387892Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length estrogen receptor alpha after 2 hrs by fluorescence polarization assay relative to estradiol2018Journal 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.
AID1465916Inhibition of recombinant human GFP-fused ERalpha LBD (301 to 553 residues) expressed in human U2O2 cells assessed as downregulation of 17beta-estradiol-induced transcription at 1 uM preincubated for 4 hrs followed by E2 addition measured after 20 hrs by 2017Journal 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.
AID1666645Toxicity in human MCF7 cells assessed as cell death at 10 uM incubated for 72 hrs by LDH assay relative to control2020Bioorganic & 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.
AID1693883Therapeutic index, ratio of CC50 for inhibition of colony formation in human HSF cells to IC50 for inhibition of colony formation in ER and PR-positive human MCF7 cells2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Synthesis, antitumor activity and structure-activity studies of novel pyridoxine-based bioisosteric analogs of estradiol.
AID115224Inhibition of estradiol-induced uterine weight gain in ovariectomized BALB/c mice at 20 ug dose twice daily1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Synthesis and biological activity of new halo-steroidal antiestrogens.
AID1524923Cytotoxicity in human MRC5 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin-based cytotoxicity assay2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Double prodrugs of a fosmidomycin surrogate as antimalarial and antitubercular agents.
AID765187Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay2013Bioorganic & 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.
AID1705345Antiproliferative activity against human OVCAR-4 cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1389792Antagonist activity at ERalpha in human MCF7 cells assessed as reduction in estradiol-induced PgR mRNA expression at 1 uM by SYBR Green dye based RT-PCR analysis2018Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6
Synthesis and biological evaluation of 4,6-diaryl-2-pyrimidinamine derivatives as anti-breast cancer agents.
AID1567374Cytotoxicity against human PANC1 cells2019European journal of medicinal chemistry, Sep-15, Volume: 178Tetrazole hybrids with potential anticancer activity.
AID747466Antagonist activity at human estrogen receptor-alpha by yeast two-hybrid assay in presence of SRC12013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Discovery of natural estrogen receptor modulators with structure-based virtual screening.
AID1251780Binding affinity to ERalpha receptor (unknown origin)2015Journal 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
AID270144Cytotoxicity against human A431 cells2006Journal 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.
AID1193493Thermodynamic equilibrium solubility, log S of the compound in PBS at pH 7.4 at RT after 4 hrs by 96 well plate method2015Bioorganic & 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.
AID191679Uterotrophic effect in rats uterine at 10 ug/day dose1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent.
AID186916The compound was tested for anti-uterotrophic activity in immature rats(Dosage 10 microg)1984Journal 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
AID604741Displacement of radiolabeled warfarin from fatty acid-free human serum albumin site 1 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions.
AID101820Inhibition of estrogen receptor negative MDA-MB-231 breast cancer cell proliferation2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Design, synthesis, and biological evaluation of doxorubicin-formaldehyde conjugates targeted to breast cancer cells.
AID1222793Dissociation constant, pKa of the compound2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Which metabolites circulate?
AID103538Inhibition of estrogen-induced MCF-7 cell proliferation at 10000 nM1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Carboxylic acid analogues of tamoxifen: (Z)-2-[p-(1, 2-diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine. Estrogen receptor affinity and estrogen antagonist effects in MCF-7 cells.
AID765189Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2013Bioorganic & 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.
AID1170538Displacement of fluorescein-labeled estrogen from human recombinant ERbeta by fluorescence polarization based competitive binding affinity assay2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
β-Lactam estrogen receptor antagonists and a dual-targeting estrogen receptor/tubulin ligand.
AID103083Inhibition of MCF-7 cell proliferation at 5 uM2003Journal 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.
AID188603The compound was tested for no of tumors with partial remission at 10 mg/kg dose after peroral administration (experiment-2)1984Journal 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
AID1676124Selectivity index, ratio of CC50 for human A549 cells to IC50 for antiviral activity against pseudotyped Marburgvirus-Musoke infected in human A549 cells2020Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors.
AID678554Cytotoxicity against human MCF7 cells after 72 hrs by WST1 assay in presence of 20% FBS2012Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
Synthesis and cytotoxic activity of non-naturally substituted 4-oxycoumarin derivatives.
AID628346Antiestrogenic 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 assay2011Journal of natural products, Aug-26, Volume: 74, Issue:8
Using the pER8:GUS reporter system to screen for phytoestrogens from Caesalpinia sappan.
AID106463Median tumor weight of MXT ER+ (mammary carcinoma) determined at the end of 6 week therapy at a dose of 8 mg1988Journal 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.
AID26936Dissociation constant was evaluated.1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent.
AID69366Relative binding affinity against estrogen receptor in whole cell assay1986Journal 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.
AID1069846Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Synthesis of neolignans as microtubule stabilisers.
AID374714Cytotoxicity against estrogen receptor deficient human SKBR3 cells overexpressing human epidermal growth factor receptor 2 after 72 hrs by SRB assay2009Journal 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.
AID1424439Induction of apoptosis in human MCF7 cells incubated for 24 hrs by flow cytometry2017European journal of medicinal chemistry, Dec-15, Volume: 142From the hive: Honey, a novel weapon against cancer.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID270141Cytotoxicity against human MDA-MB-231 cells lacking ER2006Journal 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.
AID191698Uterotrophic effect in rats uterine at 50 ug/day dose in the presence of 0.5 ug hexestrol1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent.
AID1251782Agonist activity at progesterone receptor in human MCF7 cells2015Journal 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
AID70337Inhibition of [3H]E2 binding to estrogen receptor alpha in MCF-7 cell lysate2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Design, synthesis, and biological evaluation of doxorubicin-formaldehyde conjugates targeted to breast cancer cells.
AID561218Antifungal activity against Saccharomyces cerevisiae BY4741 assessed as inhibition fungal bud formation at 8 ug/ml2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Antifungal activity of tamoxifen: in vitro and in vivo activities and mechanistic characterization.
AID1327721Anticancer activity against human FADU cells measured after 48 hrs by SRB assay2016Bioorganic & 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.
AID669589Displacement of [3H]estradiol from ERbeta after 4 hrs by scintillation counting2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Hydrophobic Interactions Improve Selectivity to ERα for Ben-zothiophene SERMs.
AID437140Cytotoxicity against HEK293 cells after 18 hrs by MTT assay2009European 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.
AID101645Effect on [3H]-thymidine incorporation into MDA-MB 231 human breast cancer cells at 1x10E-6M1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Indolo[2,1-a]isoquinolines. Syntheses, steroid hormone receptor binding affinities, and cytostatic activity.
AID104076In vitro cytotoxicity against hormone-responsive MCF-7 cell line.1995Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2
Rationally designed analogues of tamoxifen with improved calmodulin antagonism.
AID164972Percent stimulation or inhibition of protein kinase C III activity for protamine sulfate in the presence of EGTA.1992Journal 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.
AID68739Estrogenic activity in MCF-7-2a cells as percent activation of 10e-8 M estradiol2002Journal 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.
AID470163Antiestrogenic 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 assay2009Journal of natural products, Nov, Volume: 72, Issue:11
Antiestrogenic constituents of the Thai medicinal plants Capparis flavicans and Vitex glabrata.
AID493960Inhibition of LuxR-dependent quorum sensing in Vibrio fischeri assessed as reduction of 3-oxo-C6-HSL-induced bioluminescence intensity at 40 uM2010Bioorganic & 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.
AID186917The compound was tested for anti-uterotrophic activity in immature rats(Dosage 1000 ug)1984Journal 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
AID242378Inhibition of [3H]estradiol binding to human estrogen receptor alpha expressed in HeLa cells; not determined2005Journal 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.
AID134367In vitro estrogenic effect in immature mice at 10 ug1986Journal 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.
AID723800Antiproliferative activity against mouse fibroblasts after 48 hrs by MTT assay2013European journal of medicinal chemistry, Feb, Volume: 60Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent.
AID1217709Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system2011Drug 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.
AID1768145Clearance in Sprague-Dawley rat at 1 mg/kg, iv or po measured after 0.033 to 24 hrs by LC/MS/MS analysis
AID1646805Metabolic stability in human liver microsomes assessed as half life2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells.
AID1061217Inhibition 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 control2014European journal of medicinal chemistry, Jan, Volume: 71A novel tamoxifen derivative, ridaifen-F, is a nonpeptidic small-molecule proteasome inhibitor.
AID620851Effect 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 %)2011European 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.
AID1545836Antiproliferative activity against human MDA-MB-231 cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID392616Antiestrogenic activity in human T47D cells expressing estrogen receptor assessed as estrogen-dependent transcription by luciferase reporter gene assay2009Bioorganic & 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).
AID1464226Agonist activity at full length ERalpha (unknown origin) expressed in human HeLa cells incubated for 24 hrs by ERE-driven luciferase reporter gene assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Design and synthesis of benzoacridines as estrogenic and anti-estrogenic agents.
AID1473739Inhibition 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 assay2013Toxicological 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.
AID186918The compound was tested for anti-uterotrophic activity in immature rats(Dosage 100 ug)1984Journal 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
AID1705347Antiproliferative activity against human NCI/ADR-RES cells assessed as growth inhibition at 10 uM relative to control2020European journal of medicinal chemistry, Dec-15, Volume: 208Triphenylethylene analogues: Design, synthesis and evaluation of antitumor activity and topoisomerase inhibitors.
AID1277627Antiproliferative activity against human BxPC3 cells assessed as cell viability at 10 uM after 48 hrs by MTS assay2016Bioorganic & 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.
AID187053The compound was tested for uterotropic activity in immature rats(Dosage 10 ug)1984Journal 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
AID1688068Antiproliferative 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 assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition.
AID191677Uterotrophic effect in rats uterine at 1 ug/day dose in presence of estradiol1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent.
AID480631Selectivity ratio of relative binding affinity for human ERalpha to relative binding affinity for human ERbeta2010Bioorganic & 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.
AID172431Change in DMBA-induced mammary tumor area in rats after 28 day therapy at 3 mg dose (experiment-1)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug 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.
AID1545842Antiproliferative activity against human A549 cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1284733Cytotoxicity against human T47D cells assessed as growth inhibition after 48 hrs by SRB assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.
AID134364Antiestrogenic effect in immature mouse at a dose of 25 ug.1986Journal 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.
AID187687Final tumor number in DMBA-induced tumor bearing rats at 3 mg dose (experiment-1)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Benzo[a]carbazole derivatives. Synthesis, estrogen receptor binding affinities, and mammary tumor inhibiting activity.
AID501531Antagonist activity at human wild type ERalpha expressed in human HeLa cells co-expressing ERE assessed as inhibition of transactivation activity by luciferase reporter gene assay2010Bioorganic & 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.
AID1866705Antiproliferative activity against human MCF7 cells assessed as cell viability after 24 hrs by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Rational 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.
AID1312622Antiproliferative activity against human PC3 cells2016European journal of medicinal chemistry, Aug-25, Volume: 119Recent developments of C-4 substituted coumarin derivatives as anticancer agents.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal 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.
AID1350706Apparent permeability cross basolateral to apical side in MDCK-MDR1 cells at 5 uM after 90 mins by LC-MS/MS analysis2018Journal 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.
AID1636506Drug 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 N2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1164495Antiproliferative activity mouse NIH/3T3 cells after 2 days by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of new estradiol-cationic lipid hybrids: ten-carbon twin chain cationic lipid is a more suitable partner for estradiol to elicit better anticancer activity.
AID1129457Solubility of the compound in PBS buffer after 16 hrs2014European journal of medicinal chemistry, Apr-09, Volume: 76Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.
AID1534873Binding affinity to rRNA-A site in human MDA-MB-231 cells assessed as inhibition of protein translation2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis, antimicrobial activity, attenuation of aminoglycoside resistance in MRSA, and ribosomal A-site binding of pyrene-neomycin conjugates.
AID187054The compound was tested for uterotropic activity in immature rats(Dosage 1 ug)1984Journal 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
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. 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.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. 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.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. 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.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & 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.
AID1801141Exogenous PldA Assay from Article 10.1021/cb500828m: \\Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes.\\2015ACS chemical biology, Feb-20, Volume: 10, Issue:2
Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes.
AID1804127No assay is provided from Article 10.1002/med.21724: \\The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.\\2021Medicinal research reviews, 01, Volume: 41, Issue:1
The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.
AID1797989ER-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.\\2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.
AID1799396d.311 Enzymatic Inhibition Assay from Article 10.1038/nchembio.140: \\Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.\\2009Nature chemical biology, Feb, Volume: 5, Issue:2
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
AID1801851LoxA HTP Assay from Article 10.1021/acs.biochem.6b00338: \\Biochemical and Cellular Characterization and Inhibitor Discovery of Pseudomonas aeruginosa 15-Lipoxygenase.\\2016Biochemistry, 06-14, Volume: 55, Issue:23
Biochemical and Cellular Characterization and Inhibitor Discovery of Pseudomonas aeruginosa 15-Lipoxygenase.
AID1797992ER-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 2005Journal 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.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS 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.
AID1347411qHTS 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) Libary2020ACS 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.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal 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.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2005Journal of molecular biology, Sep-09, Volume: 352, Issue:1
Structural insights into drug processing by human carboxylesterase 1: tamoxifen, mevastatin, and inhibition by benzil.
AID1811Experimentally measured binding affinity data derived from PDB2005Journal 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]

Research

Studies (19,545)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902501 (12.80)18.7374
1990's4322 (22.11)18.2507
2000's5883 (30.10)29.6817
2010's5476 (28.02)24.3611
2020's1363 (6.97)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 110.33

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.

MetricThis Compound (vs All)
Research Demand Index110.33 (24.57)
Research Supply Index10.04 (2.92)
Research Growth Index4.72 (4.65)
Search Engine Demand Index210.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (110.33)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2,227 (10.79%)5.53%
Reviews2,768 (13.42%)6.00%
Case Studies1,253 (6.07%)4.05%
Observational61 (0.30%)0.25%
Other14,321 (69.42%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (375)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
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 42,000 participants (Actual)Interventional2010-06-17Completed
Genotype and Phenotype Guided Supplementation of TAMoxifen Standard Therapy With ENDOXifen in Breast Cancer Patients (TAMENDOX) [NCT03931928]Phase 2356 participants (Actual)Interventional2019-09-10Completed
Association Between Genetic Polymorphisms of CYP2D6 and Outcomes in Breast Cancer Patients With Tamoxifen Treatment [NCT01169792]0 participants ObservationalCompleted
A Clinical Trial Comparing Anastrozole With Tamoxifen in Postmenopausal Patients With Ductal Carcinoma in Situ (DCIS) Undergoing Lumpectomy With Radiation Therapy [NCT00053898]Phase 33,104 participants (Actual)Interventional2003-01-31Completed
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 246 participants (Anticipated)Interventional2023-01-01Not 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 39,779 participants (Actual)Interventional2001-08-31Completed
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 281 participants (Actual)Interventional2015-03-06Active, 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 35,018 participants (Actual)Interventional2011-01-15Active, 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 2140 participants (Actual)Interventional2009-09-30Completed
Phase III Randomized Study of Immediate Versus Luteal Phase Adjuvant Oophorectomy and Tamoxifen in Premenopausal Women With Hormone Receptor-positive Breast Cancer [NCT00201851]Phase 3740 participants (Actual)Interventional2004-01-31Completed
A Phase II Study of Pembrolizumab And Tamoxifen Among Women With Advanced Hormone Receptor Positive Breast Cancer And Esr1 Mutation [NCT03879174]Phase 225 participants (Anticipated)Interventional2019-08-01Not 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 142 participants (Actual)Interventional2010-07-31Completed
Tamoxifen Versus Estradiol in the Prevention of Unscheduled Bleeding in Etonogestrel Implant Users, a Randomized Controlled Pilot Trial [NCT04933240]Phase 40 participants (Actual)Interventional2022-05-31Withdrawn(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 329 participants (Actual)Interventional2003-08-31Terminated(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)Observational2019-01-02Enrolling 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 216 participants (Anticipated)Interventional2020-12-18Recruiting
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 3104 participants (Anticipated)Interventional2021-07-26Recruiting
Chemotherapy-free Trastuzumab and Pertuzumab in HER2-positive (Human Epidermal Receptor) Breast Cancer: FDG-PET Response-adapted Strategy. The PHERGain Study [NCT03161353]Phase 2377 participants (Actual)Interventional2017-06-26Completed
H-16848 - Phase II Pilot Study With Correlative Markers of Tamoxifen for Progressive Transitional Cell Carcinoma Following Previous Chemotherapy [NCT00710970]Phase 228 participants (Actual)Interventional2007-01-31Completed
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 3223 participants (Actual)Interventional2017-08-21Terminated(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 17 participants (Actual)Interventional2016-02-23Completed
DCIS: RECAST Trial -Ductal Carcinoma In Situ: Re-Evaluating Conditions for Active Surveillance Suitability as Treatment: a Breast Cancer Prevention Pilot Study [NCT06075953]Phase 2400 participants (Anticipated)Interventional2023-11-30Recruiting
[NCT02132000]Phase 2/Phase 33,036 participants (Anticipated)Interventional2014-04-30Recruiting
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 3300 participants (Anticipated)Interventional2018-08-09Enrolling by invitation
Tamoxifen to Reduce Unscheduled Bleeding in New Users of the Levonorgestrel-releasing Intrauterine System (LNG-IUS) [NCT02824224]Phase 442 participants (Actual)Interventional2016-09-06Completed
The Study of Tamoxifen Treatment in Patients With Motor Neuron Disease [NCT02166944]Phase 1/Phase 220 participants (Actual)Interventional2014-04-30Completed
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)Interventional2001-11-30Completed
A Multi-Centre Study of Tamoxifen Dose Escalation Study in Breast Cancer Patients With CYP2D6 Polymorphisms [NCT01075802]121 participants (Actual)Interventional2010-03-31Completed
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 2226 participants (Actual)Interventional2005-10-31Completed
A Phase II Trial of Tamoxifen and Bortezomib in Patients With Recurrent High-Grade Gliomas [NCT00108069]Phase 243 participants (Actual)Interventional2005-04-30Completed
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 3180 participants (Anticipated)Interventional2018-02-09Active, 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 33,066 participants (Actual)Interventional2003-12-17Active, 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 3844 participants (Anticipated)Interventional2017-11-30Recruiting
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]2018-08-10Recruiting
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)Interventional2021-01-01Active, not recruiting
Clomiphene Citrate Versus Tamoxifen for Induction of Ovulation in Women With Polycystic Ovary Syndrome: Randomized Controlled Trial [NCT02479256]Phase 4600 participants (Actual)Interventional2015-06-30Completed
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 2200 participants (Anticipated)Interventional2018-03-20Recruiting
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 31,294 participants (Actual)Interventional2004-03-31Active, 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 3913 participants (Actual)InterventionalCompleted
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 248 participants (Actual)Interventional2014-12-31Completed
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 270 participants (Actual)Interventional2015-10-19Completed
Safety of Toremifene and Tamoxifen Therapy in Premenopausal Patients With Operable Breast Cancer: A Randomized, Controlled, Prospective, Observational Study [NCT02344940]Phase 4104 participants (Actual)Interventional2014-12-31Completed
Comparison of the Efficacy of the Tamoxifen and Tamoxifen With Antioxidants on Semen Quality of Infertile Male With Abnormal Semen Parameters. [NCT05200663]Phase 2110 participants (Anticipated)Interventional2021-10-15Recruiting
Tamoxifen to Treat Barrett's Metaplasia [NCT02089386]Early Phase 17 participants (Actual)Interventional2014-07-09Terminated(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 14 participants (Actual)Interventional2020-10-13Terminated(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)Interventional2023-05-16Recruiting
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 175 participants (Actual)Interventional2020-12-23Active, not recruiting
Low-Dose Tamoxifen for Radiation-Induced Breast Cancer Risk Reduction: A Phase IIB Randomized Placebo-Controlled Trial [NCT01196936]Phase 284 participants (Actual)Interventional2010-09-30Active, 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]2016-03-15Completed
The Effect of Tamoxifen on Endometrial Thickness and Pregnancy Outcome in Women With Thin Endometrium Undergoing Frozen Thawed Cycle. [NCT03060304]Phase 4100 participants (Anticipated)Interventional2017-03-31Not 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 240 participants (Actual)Interventional2022-04-04Active, not recruiting
Randomized Placebo-controlled Phase III Trial of Low Dose Tamoxifen in Women With Breast Intraepithelial Neoplasia - Long Term Follow-up [NCT01357772]Phase 3500 participants (Actual)Interventional2008-11-12Active, not recruiting
Prognostic Evaluation of Changing Endocrine Therapy in Perimenopausal and Recently Postmenopausal Women With Early-stage Hormone Receptor-Positive Breast Cancer [NCT02097459]Phase 3600 participants (Anticipated)Interventional2014-03-31Recruiting
A Trial of Endocrine Response in Women With Invasive Lobular Breast Cancer [NCT02206984]Phase 2201 participants (Anticipated)Interventional2015-09-30Recruiting
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 250 participants (Actual)Interventional1997-11-30Completed
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 36,000 participants (Anticipated)Interventional2022-10-04Recruiting
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 3394 participants (Actual)Interventional2008-05-15Active, 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 220 participants (Actual)Interventional2021-11-16Active, not recruiting
Analgesic Efficacy of Pulsed Radiofrequency in Non-cyclic Mastalgia [NCT03715413]Phase 264 participants (Actual)Interventional2018-08-15Completed
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 3200 participants (Anticipated)Interventional2017-12-20Not 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)Observational2023-06-01Not 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)Interventional2008-06-30Completed
Choosing Neoadjuvant Chemotherapy Versus Hormonal Therapy for Breast Cancer Based on Gene Expression Profile [NCT01293032]59 participants (Actual)Interventional2011-04-30Completed
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 3250 participants (Anticipated)Interventional2022-12-28Enrolling 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 3250 participants (Anticipated)Interventional2021-07-01Recruiting
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 273 participants (Actual)Interventional2008-09-30Completed
[NCT02866955]Phase 2100 participants (Actual)Interventional2011-06-15Completed
Comparison of Tamoxifen and Clomiphene Citrate in Mild Stimulation IVF: a Prospective Cohort Study [NCT02690870]Phase 4210 participants (Anticipated)Interventional2017-01-31Not 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 144 participants (Anticipated)Interventional2022-09-04Recruiting
Genetic Study of CYP2D6 Enzyme and Therapeutic Drug Monitoring of Tamoxifen in Premenopausal Women With Breast Cancer [NCT03582865]100 participants (Anticipated)Observational2019-09-01Not 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 34,300 participants (Anticipated)Interventional2023-03-31Recruiting
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 290 participants (Anticipated)Interventional2022-05-17Recruiting
Herceptin and Paclitaxel in Locally Advanced Breast Cancer With Her-2 Overexpression [NCT00009997]Phase 10 participants Interventional1999-03-31Completed
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 2363 participants (Actual)Interventional2019-10-22Active, 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 3260 participants (Actual)Interventional2014-02-27Active, 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 292 participants (Anticipated)Interventional2023-07-20Recruiting
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 3177 participants (Actual)Interventional2008-12-31Completed
A Phase II Study of Sulindac and Tamoxifen in Patients With Desmoid Tumors That Are Recurrent or Not Amenable to Standard Therapy [NCT00068419]Phase 270 participants (Actual)Interventional2004-02-29Completed
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 32,672 participants (Actual)Interventional2003-11-03Active, 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 34,740 participants (Actual)Interventional1998-02-28Completed
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 3810 participants (Anticipated)Interventional2019-04-30Recruiting
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 3672 participants (Actual)Interventional2014-11-20Completed
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 3139 participants (Actual)Interventional2003-02-28Completed
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 230 participants (Actual)Interventional2000-06-30Completed
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 3260 participants (Anticipated)Interventional2008-12-31Recruiting
Tamoxifen Resistance in Breast Cancer [NCT00899197]2 participants (Actual)Observational2007-05-31Terminated
A Pilot Study of FES Imaging to Optimize Tamoxifen Dose for Metastatic Breast Cancer Patients With ESR1 Mutations [NCT04174352]Early Phase 112 participants (Anticipated)Interventional2020-10-20Recruiting
Randomized Study of the Use of Tamoxifen Versus Ointment Lidocaine for Reducing the Pain and Discomfort in Mammography [NCT02801786]Phase 2/Phase 3450 participants (Anticipated)Interventional2018-11-30Not 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 20 participants Interventional2002-11-30Completed
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 4150 participants (Anticipated)Interventional2018-03-01Recruiting
A Randomized Study of Chemotherapy Versus Hormonal Treatment in Patients With Ovarian Cancer Resistant or Refractory to Platinum and Taxane [NCT02728622]Phase 3241 participants (Actual)Interventional2002-03-31Completed
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 236 participants (Actual)Interventional2002-04-30Completed
Pre-Operative Window of Adjuvant Endocrine Therapy to Inform Radiation Therapy Decisions In Older Women With Early-Stage Breast Cancer [NCT04272801]Phase 283 participants (Anticipated)Interventional2020-04-07Recruiting
PErsonalized TREatment of High-risk MAmmary Cancer - the PETREMAC Trial [NCT02624973]Phase 2200 participants (Actual)Interventional2016-04-15Active, not recruiting
Impact of Neoadjuvant Hormonal Therapy on the Surgical Management of Extensive Ductal Carcinomas in Situ [NCT04666961]Phase 2262 participants (Anticipated)Interventional2021-02-03Recruiting
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 310 participants (Actual)Interventional2008-04-30Terminated(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 2162 participants (Actual)Interventional2014-01-31Completed
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 3197 participants (Actual)Interventional2007-10-31Completed
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 31,558 participants (Actual)Interventional1989-05-31Completed
Efficacy and Safety of High Dose Tamoxifen to Advanced Hormone Receptor-High Expressed Endocrine Therapy Resisted Breast Cancer [NCT03045653]Phase 230 participants (Actual)Interventional2017-09-01Completed
Tamoxifen Metabolism and the Impact of Tamoxifen Dose on the Level of the Active Metabolites in Endocrine Sensitive Breast Cancer Patients [NCT00963209]Phase 3140 participants (Anticipated)Interventional2009-06-30Recruiting
Impact of CYP2D6 Genotype on the Clinical Effects of Tamoxifen Using With Samples From Prospective Randomized Multicenter Study [NCT00973037]922 participants (Anticipated)Observational2009-03-31Recruiting
A Phase II Study of GW572016 and Tamoxifen in Patients With Metastatic Breast Cancer Resistant to Single-Agent Tamoxifen [NCT00118157]Phase 219 participants (Actual)Interventional2005-05-31Completed
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 31,946 participants (Anticipated)Interventional2023-03-30Recruiting
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 31,234 participants (Anticipated)Interventional2009-05-31Enrolling by invitation
Validating CYP2D6 Genotype-Guided Tamoxifen Therapy for a Multiracial U.S. Population [NCT00764322]Phase 2501 participants (Actual)Interventional2008-06-18Completed
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 293 participants (Actual)Interventional2008-08-31Completed
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 242 participants (Actual)Interventional2015-03-31Completed
Phase II Study of Soy Protein to Treat Vasomotor Symptoms in Postmenopausal Women Taking Tamoxifen [NCT00031720]Phase 2112 participants (Actual)Interventional2002-03-31Completed
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 2181 participants (Actual)Interventional2015-02-28Active, 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 2250 participants (Anticipated)Interventional2008-07-31Suspended(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 4256 participants (Actual)Interventional2008-01-31Completed
Investigating Cognitive Function for Patients Participating in the SOFT Trial in Selected Centers [NCT00659373]Phase 386 participants (Actual)Interventional2007-12-31Completed
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 2132 participants (Anticipated)Interventional2022-08-01Recruiting
Pre-surgical Phase IIb Trial of Transdermal 4-Hydroxytamoxifen vs. Oral Tamoxifen in Women With Ductal Carcinoma in Situ of the Breast [NCT00952731]Phase 227 participants (Actual)Interventional2009-12-31Completed
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 3285 participants (Actual)Interventional1997-06-30Completed
Pilot Study to Analyze a Novel Mechanism Underlying Response to Tamoxifen Therapy in Breast Cancer Patients [NCT01027416]59 participants (Actual)Interventional2009-12-14Completed
Hormone Replacement Versus Tamoxifen Combined Of Hormone Replacement in Women With a Thin Endometrium Undergoing Frozen-thawed Embryo Transfer [NCT04292886]120 participants (Anticipated)Interventional2019-10-01Recruiting
Selective Estrogen Receptor Modulators to Enhance the Efficacy of Viral Reactivation With Histone Deacetylase Inhibitors [NCT03382834]Phase 231 participants (Actual)Interventional2018-04-26Active, 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]2024-07-31Not 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 20 participants (Actual)Interventional2019-10-18Withdrawn(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 360 participants (Anticipated)Interventional2009-02-28Recruiting
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 3308 participants (Actual)Interventional1998-04-30Completed
Fourteen Day Safety of Low-Dose Tamoxifen in Patients With Chronic Hepatitis C Who Have Failed Standard Medical Therapy [NCT00749138]Phase 118 participants (Anticipated)Interventional2008-11-30Completed
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 33,697 participants (Actual)Interventional2007-03-31Active, 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 39,358 participants (Actual)Interventional1998-06-30Completed
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 3308 participants (Actual)Interventional1998-06-30Completed
An Umbrella, Randomized, Controlled, Pre-Operative Trial Testing Integrative Subtype-Targeted Therapeutics in Hormone Receptor-Positive, HER2-Negative Breast Cancer [NCT05101564]Phase 2150 participants (Anticipated)Interventional2023-03-20Recruiting
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 215 participants (Actual)Interventional2002-01-31Completed
Tamoxifen in Duchenne Muscular Dystrophy: A Multicenter, Randomised, Double-blind, Placebo-controlled, Phase 3 Safety and Efficacy 48-week Trial [NCT03354039]Phase 393 participants (Actual)Interventional2018-06-12Completed
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 4137 participants (Anticipated)Interventional2022-07-07Recruiting
Dose-Intense Chemotherapy and Stem Cell Rescue in the Treatment of Inflammatory Breast Carcinoma [NCT00003042]Phase 241 participants (Actual)Interventional1997-05-30Active, 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 290 participants (Anticipated)Interventional2024-02-29Recruiting
A Phase IB Randomized Study of an Antiestrogen in Women With Newly Diagnosed Breast Cancer [NCT00005886]Phase 10 participants Interventional2000-07-31Completed
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 39,358 participants (Actual)Interventional1996-07-31Completed
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 33,436 participants (Actual)Interventional2000-05-19Completed
A Phase II Trial of High Dose Tamoxifen For The Treatment of Newly Diagnosed Supratentorial Glioblastoma Multiforme (GBM) [NCT00006388]Phase 277 participants (Actual)Interventional2000-12-31Completed
A Phase I Pharmacokinetic, Pharmacodynamic, and Clinical Study of the Combination of the Angiogenesis Inhibitor SU5416 and Doxorubicin in Inflammatory Breast Cancer [NCT00005822]Phase 121 participants (Actual)Interventional2000-04-30Completed
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 3396 participants (Actual)Interventional2001-05-31Terminated(stopped due to Administratively complete.)
The Comparative Trial of UFT + TAM With CMF + TAM in Adjuvant Therapy for Breast Cancer (CUBC) [NCT00152178]Phase 3680 participants (Anticipated)Interventional1996-07-31Completed
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 210 participants (Actual)Interventional2015-10-31Active, not recruiting
A Pilot Study of Varying Doses of Tamoxifen in the Setting of Genetic Polymorphisms of CYP2D6 [NCT00900744]121 participants (Actual)Observational2009-01-31Completed
[NCT00538330]2,000 participants (Anticipated)Interventional2007-09-30Active, 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 3826 participants (Actual)Interventional2006-01-31Completed
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 279 participants (Actual)Interventional2002-02-19Completed
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 2138 participants (Actual)Interventional2017-12-26Active, 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 3180 participants Interventional2003-12-31Completed
Anti-Estrogens - A Potential Treatment for Bipolar Affective Disorder in Women? [NCT00206544]Phase 251 participants (Actual)Interventional2004-01-31Completed
A Pilot Trial Correlating Metabolic Profile of Tamoxifen With Pharmacogenetic Predictors and Clinical Effects [NCT00228930]297 participants (Actual)Observational2002-09-30Completed
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 23 participants (Actual)Interventional2003-07-31Terminated(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 2238 participants (Anticipated)Interventional2021-10-21Recruiting
A Randomized, Double-Blind, Placebo-Controlled Study of 4-hydroxytamoxifen Topical Gel in Women With Mammographically Dense Breast [NCT03063619]Phase 2194 participants (Actual)Interventional2017-05-01Active, 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 3392 participants (Actual)Interventional2013-09-16Completed
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 351 participants (Actual)Interventional1998-11-30Completed
Surgical Therapy With or Without Axillary Node Clearance for Breast Cancer in the Elderly Who Receive Adjuvant Therapy With Tamoxifen. [NCT00002528]Phase 3473 participants (Actual)Interventional1993-05-31Completed
A Phase I, First-in-Human, Dose Escalation Trial of MSC2363318A, a Dual p70S6K/Akt Inhibitor, in Subjects With Advanced Malignancies [NCT01971515]Phase 1101 participants (Actual)Interventional2013-12-13Completed
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 2151 participants (Actual)Interventional2013-10-31Completed
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 2180 participants (Actual)Interventional2016-04-08Completed
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 10 participants Interventional1996-09-30Completed
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 23 participants (Actual)Interventional2002-01-31Completed
Pilot Study of Preservation of Fertility by Ovarian Stimulation Associated With Tamoxifen, and Freezing Oocyte or Embryo Prior Chemotherapy for Breast Cancer [NCT02890082]Phase 2102 participants (Actual)Interventional2014-02-28Active, not recruiting
Tamoxifen Dose Adjustment on ER+ Breast Cancer Patients Based on Genomic and Metabolite Concentrations Analysis [NCT04312347]151 participants (Actual)Interventional2019-09-06Completed
Protocol of a Randomized Trial for the Management of Small Well-Differentiated and Special Type Carcinomas of the Breast [NCT00006030]Phase 30 participants Interventional1992-01-31Active, not recruiting
[NCT00000529]Phase 30 participants Interventional1992-05-31Completed
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 260 participants (Anticipated)Interventional2024-06-01Not yet recruiting
A Study to Evaluate the Effect of Letrozole and Tamoxifen on Bone and Lipids in Postmenopausal Women With Breast Cancer [NCT00171704]Phase 3263 participants (Actual)Interventional2005-04-30Completed
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 160 participants (Anticipated)Interventional2020-12-07Recruiting
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 3452 participants (Actual)Interventional2000-08-31Completed
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)Interventional2021-02-12Recruiting
A Phase 1b Study of Abemaciclib in Combination With Therapies for Patients With Metastatic Breast Cancer [NCT02057133]Phase 1198 participants (Anticipated)Interventional2014-03-10Active, 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 2234 participants (Actual)Interventional2016-09-14Active, 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 283 participants (Actual)Interventional2012-08-31Terminated(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 125 participants (Actual)Interventional2013-04-30Completed
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 4384 participants (Actual)Interventional2007-09-30Completed
¹³C - Dextromethorphan (DM) Breath Test for Determination of CYP2D6 Enzyme Activity in Patients Receiving Tamoxifen [NCT00873366]92 participants (Actual)Observational2009-05-31Terminated(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 35,500 participants (Anticipated)Interventional2023-10-05Recruiting
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 3320 participants (Anticipated)Interventional2022-08-03Recruiting
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 430 participants (Actual)Interventional2010-08-31Completed
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 32,500 participants (Anticipated)Interventional2007-12-31Recruiting
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 30 participants Interventional2001-05-31Terminated
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 2189 participants (Actual)Interventional2014-11-30Completed
An Open Label Trial of Perifosine in Patients Currently Being Treated on Perifosine Trials in Solid Tumors or Multiple Myeloma [NCT00847366]10 participants (Actual)Interventional2008-05-31Completed
A Feasibility Study of Tamoxifen Prevention of Breast Cancer in Hodgkin's Disease Survivors [NCT00165308]29 participants (Actual)Interventional2001-04-30Completed
a Phase 3 Randomized Double Blind Evaluation of LY353381 Compared With Tamoxifen in Women With Locally Advanced or Metastatic Breast Cancer. [NCT00034125]Phase 30 participants InterventionalCompleted
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 3926 participants (Anticipated)Interventional2021-02-08Recruiting
Assessing REsponse to Neoadjuvant Taxotere and Trastuzumab in Nigerian Women With HER2-positive Breast Cancer (ARETTA) [NCT03879577]Phase 260 participants (Anticipated)Interventional2019-11-25Recruiting
Refining Tamoxifen Dose for Premenopausal Breast Cancer Risk Reduction (RENAISSANCE): A Phase II Single Arm Trial [NCT06184750]Phase 2200 participants (Anticipated)Interventional2024-06-10Not 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 360 participants (Anticipated)Interventional1996-08-13Completed
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 2100 participants Interventional2001-01-31Completed
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 268 participants (Actual)Interventional2015-08-28Completed
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 243 participants (Actual)Interventional2006-02-28Completed
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 221 participants (Actual)Interventional2006-06-30Terminated(stopped due to planned to design a prospective study)
PROTOCOL FOR THE SCOTTISH PREMENOPAUSAL CHEMO-ENDOCRINE TRIAL [NCT00002580]Phase 31,000 participants (Anticipated)Interventional1993-06-30Completed
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)Interventional2007-05-31Recruiting
A Randomised Trial of Prednisone and Tamoxifen in Patients With Idiopathic Retroperitoneal Fibrosis [NCT00440349]Phase 238 participants Interventional2000-10-31Active, 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 280 participants (Anticipated)Interventional2006-12-31Recruiting
A Phase II Pilot Trial of Sutent, Tamoxifen, and Cisplatin in Patients With High-Risk Ocular Melanoma [NCT00489944]Phase 250 participants (Anticipated)Interventional2007-05-31Recruiting
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 2111 participants (Actual)Interventional2008-03-31Completed
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)Observational2020-07-01Active, not recruiting
Pharmacokinetics Study of Combined Treatment Lapatinib and Tamoxifen in Advanced/Metastatic Breast Cancer [NCT00424164]Phase 120 participants (Anticipated)Interventional2006-11-30Active, not recruiting
A Phase 1 Study of Maprotiline in Combination With Tamoxifen and Temozolomide for Recurrent Glioblastoma [NCT04200066]Phase 10 participants (Actual)Interventional2022-06-01Withdrawn(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 21 participants (Actual)Interventional2021-03-11Terminated(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 30 participants Interventional1987-09-30Active, 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 31,500 participants (Anticipated)Interventional1995-10-31Completed
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 3602 participants (Actual)Interventional1996-07-31Terminated(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 3344 participants (Actual)Interventional1996-06-30Completed
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 320,000 participants (Anticipated)Interventional1991-05-31Active, not recruiting
Study of Tamoxifen and Raloxifene (STAR) for the Prevention of Breast Cancer [NCT00003906]Phase 319,747 participants (Actual)Interventional1999-05-31Completed
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 3280 participants (Anticipated)Interventional1998-07-31Completed
Evaluating Multiparameter Gene Testing as a Predictor of Short Term Endocrine Therapy Response in Hormone Receptor Positive Breast Cancers: The EMPOwER Study [NCT03211572]Phase 282 participants (Anticipated)Interventional2017-08-31Not yet recruiting
Program for the Assessment of Clinical Cancer Tests (PACCT-1): Trial Assigning Individualized Options for Treatment:The TAILORx Trial [NCT00310180]Phase 310,273 participants (Actual)Interventional2006-04-07Active, 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 2130 participants (Anticipated)Interventional2000-02-29Terminated(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 39,779 participants (Actual)Interventional2002-01-31Completed
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 22,000 participants (Anticipated)Interventional2004-04-30Active, 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 3448 participants (Actual)Interventional1998-03-31Completed
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 2500 participants (Anticipated)Interventional2023-06-12Recruiting
A Phase II Pilot Trial of Sorafenib, Tamoxifen and Cisplatin as Adjuvant Therapy for Patients With Stage III Malignant Melanoma [NCT00492505]Phase 2200 participants (Anticipated)Interventional2007-04-30Recruiting
Effects of Selective Estrogen Receptor Modulators on Cognitive Aging: Cognition in the Study of Tamoxifen and Raloxifene [NCT00687102]Phase 31,498 participants (Actual)Interventional2001-10-31Completed
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 17 participants (Actual)Interventional2018-04-24Active, 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 250 participants (Anticipated)Interventional2003-05-31Completed
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 2250 participants (Actual)Interventional1998-04-30Completed
A Pilot Clinical Trial to Evaluate the Biological Activity of Fulvestrant (Faslodex) in Breast Ductal Carcinoma (DCIS) [NCT00126464]100 participants (Anticipated)Interventional2004-11-30Active, not recruiting
Double Blind Placebo Controlled Trial of a Protein Kinase C Inhibitor: Tamoxifen Citrate in Treatment of Acute Mania [NCT00411203]Phase 366 participants (Actual)Interventional2003-04-30Completed
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 31,939 participants (Actual)Interventional2013-09-12Active, not recruiting
Phase 2 Selection Trial of High Dosage Creatine and Two Dosages of Tamoxifen in Amyotrophic Lateral Sclerosis (ALS) [NCT01257581]Phase 260 participants (Actual)Interventional2011-03-31Completed
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 31,670 participants (Anticipated)Interventional2021-06-07Recruiting
PreOperative Endocrine Therapy for Individualised Care With Abemaciclib [NCT04584853]Phase 32,500 participants (Anticipated)Interventional2020-12-23Recruiting
The Effect of Antidepressants and Gabapentin on Tamoxifen Pharmacokinetics: A Prospective Study [NCT00667121]85 participants (Anticipated)Observational2011-03-16Active, 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 22 participants (Actual)Interventional2011-03-31Terminated(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 429 participants (Actual)Interventional2011-12-31Completed
Weekly Paclitaxel During Radiation Therapy for Locally Advanced Breat Cancer [NCT00003050]Phase 246 participants (Actual)Interventional1997-04-30Completed
PROTOCOL FOR THE SCOTTISH POSTMENOPAUSAL CHEMO-ENDOCRINE TRIAL [NCT00002581]Phase 31,000 participants (Anticipated)Interventional1993-06-30Completed
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 3300 participants (Anticipated)Interventional1998-11-30Active, 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 3450 participants (Anticipated)Interventional1996-10-31Completed
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 216 participants (Actual)Interventional2000-07-31Completed
A Multicenter Randomized Trial of Sequential Epirubicin and Docetaxel Versus Epirubicin in Node Positive Postmenopausal Breast Cancer Patients [NCT00010140]Phase 30 participants Interventional1997-08-31Active, not recruiting
A Phase I Study of OncoLAR® (Registered Trademark) (NSC 685403) With/Without Tamoxifen in Patients With Osteosarcoma [NCT00001436]Phase 124 participants Interventional1995-05-31Completed
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 260 participants (Anticipated)Interventional2016-10-31Completed
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 30 participants Interventional2002-11-30Terminated
ZD1839 (IRESSA) In Tamoxifen-Resistant Metastatic Breast Cancer [NCT00080743]Phase 22 participants (Actual)Interventional2004-01-31Completed
Treatment of Children With Newly Diagnosed Diffuse Pontine Gliomas Using Conventional Radiotherapy and High Dose Tamoxifen [NCT00024336]Phase 20 participants Interventional1999-08-31Active, 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 34,400 participants (Anticipated)Interventional2001-12-31Completed
Circulating miRNAs as Biomarkers of Hormone Sensitivity in Breast Cancer? Pilot Study. [NCT01612871]Phase 439 participants (Actual)Interventional2012-06-27Completed
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 120 participants (Actual)Interventional2020-02-05Active, not recruiting
A Phase II Trial Of Tipifarnib (R15777, ZARNESTRA) In Combination With Tamoxifen In Subjects With Metastatic Breast Cancer [NCT00052728]Phase 20 participants Interventional2002-12-31Completed
A Double-Blind Study Examining the Efficacy of the Protein Kinase C Inhibitor Tamoxifen in the Treatment of Acute Mania [NCT00026585]Phase 250 participants Interventional2001-11-09Completed
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 20 participants Interventional2001-02-28Active, not recruiting
International Breast Cancer Intervention Study II (IBIS-II) (DCIS) [NCT00072462]Phase 32,980 participants (Actual)Interventional2003-09-30Completed
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 240 participants Interventional2003-08-31Terminated
A Pragmatic Randomised, Multicentre Trial Evaluating Optimal Timing of Endocrine Therapy and Radiation Therapy in Early-stage Breast Cancer (REaCT-RETT) [NCT03948568]Phase 4262 participants (Actual)Interventional2019-09-17Completed
A Randomized Phase III Trial Comparing FEC-Chemotherapy vs. EC-Doc-Chemotherapy in Patients With Primary Breast Cancer [NCT00047099]Phase 3446 participants (Anticipated)Interventional2001-08-31Completed
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 30 participants (Actual)InterventionalWithdrawn(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 294 participants (Anticipated)Interventional2006-10-31Active, 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 20 participants InterventionalCompleted
A Randomized Trial of Tamoxifen Combined With Amphotericin B and Fluconazole for Cryptococcal Meningitis [NCT03112031]Phase 250 participants (Actual)Interventional2017-10-10Completed
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 249 participants (Actual)Interventional2016-06-30Active, not recruiting
Phase IIB Pre-Surgical Trial of Oral Tamoxifen Versus Transdermal 4-hydroxytamoxifen in Women With DCIS of the Breast [NCT02993159]Phase 2100 participants (Anticipated)Interventional2017-05-31Recruiting
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 230 participants (Actual)Interventional2005-10-31Completed
Preoperative Window of Endocrine Therapy Provides Information to Increase Compliance [NCT01614210]Phase 252 participants (Actual)Interventional2012-08-31Completed
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 2195 participants (Actual)Interventional2016-05-24Active, not recruiting
Phase 2 Study of Neoadjuvant Endocrine Therapy in ER-positive, HER2-negative Early Stage Breast Cancer [NCT05150652]Phase 270 participants (Anticipated)Interventional2022-02-18Recruiting
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 2317 participants (Actual)Interventional2003-10-31Completed
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 3766 participants (Anticipated)Interventional2023-06-01Recruiting
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 33,858 participants (Actual)Interventional1996-01-31Completed
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 21,059 participants (Anticipated)Interventional1996-11-30Completed
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 2375 participants (Anticipated)Interventional2021-01-11Recruiting
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 2257 participants (Actual)Interventional2017-10-05Active, not recruiting
Cancer Risk and Biomarkers of Tamoxifen Chemoprevention [NCT00295100]Phase 278 participants Interventional2000-09-30Completed
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 2200 participants (Anticipated)Interventional2004-03-31Recruiting
A Randomized Phase III Study Comparing Tamoxifen vs. Tamoxifen + Aminoglutethimide in Postmenopausal, Hormone Receptor-positive Patients [NCT00309491]Phase 32,021 participants (Actual)Interventional1990-12-31Completed
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)Interventional2011-12-31Recruiting
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 3290 participants (Anticipated)Interventional2012-06-30Recruiting
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 356 participants (Actual)Interventional2012-08-31Completed
UKCCCR RANDOMISED TRIAL OF ADJUVANT ENDOCRINE THERAPY AND CHEMOTHERAPY IN WOMEN WITH EARLY BREAST CANCER, THE ADJUVANT BREAST CANCER (ABC) TRIAL [NCT00002582]Phase 36,000 participants (Anticipated)Interventional1993-06-30Completed
Neoadjuvant Endocrine Therapy in Breast Cancer. Real Clinical Practice in Russia [NCT05800197]300 participants (Anticipated)Observational2014-04-15Recruiting
Impact of Obesity on the Efficacy of Endocrine Therapy With Aromatase Inhibitors in Postmenopausal Patients With Early Breast Cancer [NCT01758146]Phase 3412 participants (Anticipated)Interventional2012-01-31Recruiting
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 2185 participants (Anticipated)Interventional2019-07-31Recruiting
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 2742 participants (Actual)Interventional2012-10-31Active, not recruiting
Combination Therapy With Isotretinoin and Tamoxifen Expected to Provide Complete Protection Against Severe Acute Respiratory Syndrome Coronavirus [NCT04389580]Phase 2160 participants (Anticipated)Interventional2021-09-30Not yet recruiting
Neoadjuvant Intratumoral Injection of Dendritic Cells in Breast Cancer Translation of Biotechnology Into the Clinic [NCT00499083]Phase 217 participants (Actual)Interventional2006-05-01Completed
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 280 participants (Anticipated)Interventional2024-03-01Not yet recruiting
Treatment of Unfavorable Bleeding Patterns in Contraceptive Implant Users [NCT02903121]Phase 4109 participants (Actual)Interventional2017-01-20Completed
Preoperative Neoadjuvant Hormonal Therapy and Neoadjuvant Chemotherapy for Stage IIIB and IV Breast Cancer Patients in Dharmais National Cancer Center Hospital, Indonesia [NCT02995772]Phase 3122 participants (Actual)Interventional2011-11-30Completed
A Randomized Controlled Trial of Tamoxifen Versus Etoposide for Patients With First Recurrence of Glioblastoma Multiforme [NCT04765098]Phase 260 participants (Anticipated)Interventional2022-01-28Recruiting
A Pilot Clinical Trial to Evaluate the Biological Activity of Fulvestrant in Breast Ductal Carcinoma in Situ (DCIS) [NCT00183963]Phase 24 participants (Actual)Interventional2006-08-31Terminated(stopped due to Insufficient accrual)
ETHAN: A Phase II Study Comparing Different Endocrine THerapies for mAle Breast caNcer [NCT05501704]Phase 260 participants (Anticipated)Interventional2023-10-11Recruiting
Adjuvant Therapy for Post/Perimenopausal Patients With Node Positive Breast Cancer Who Are Suitable for Endocrine Therapy Alone. [NCT00002529]Phase 3452 participants (Actual)Interventional1993-05-31Completed
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 289 participants (Actual)Interventional1994-02-28Completed
Tamoxifen Versus Anastrozole, Alone or in Combination With Zoledronic Acid, in Premenopausal, Hormone Receptor-positive Breast Cancer Patients (Stage I, II) [NCT00295646]Phase 31,803 participants (Actual)Interventional1999-06-30Completed
[NCT00375622]Phase 260 participants Interventional2005-02-28Completed
Neoadjuvant Endocrine Therapy in Hormone Receptor-Positive HER2-Negative Node-Negative Breast Cancer Patients to Assess Responses and Mechanisms of Endocrine Resistance [NCT03219476]Phase 237 participants (Actual)Interventional2017-02-05Active, 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 36,600 participants (Anticipated)Interventional2007-02-28Completed
Comparison in the Change of Proliferation Index Between Fulvestrant and Tamoxifen in Cyclin D1 +, Estrogen Receptor + Breast Cancer [NCT02936206]Phase 12 participants (Actual)Interventional2016-10-31Terminated(stopped due to low accrual rate)
Low-Dose Tamoxifen to Reduce High Background Parenchymal Uptake on Molecular Breast Imaging [NCT02979301]22 participants (Actual)Interventional2017-03-01Completed
A Phase II Study of the Determinants of Transdermal Drug Delivery to the Normal and the Radiated Breast [NCT04009044]Phase 2156 participants (Anticipated)Interventional2020-02-17Recruiting
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 3672 participants (Actual)Interventional1993-07-20Completed
Phase II Trial of Sequential High-Dose Alkylating Agents in Metastatic Breast Cancer [NCT00002680]Phase 240 participants (Actual)Interventional1994-02-28Completed
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 3313 participants (Actual)Interventional1997-03-31Completed
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 34,400 participants (Anticipated)Interventional1998-02-28Active, not recruiting
Randomised Trial of Tamoxifen Versus Placebo for the Treatment of Inoperable Hepatocellular Carcinoma [NCT00003424]Phase 3300 participants (Anticipated)Interventional1997-04-30Completed
Reliable Assessment of the Efficacy and Safety of Prolonging the Use of Adjuvant Tamoxifen: A Large, Simple, Randomised Study [NCT00003016]Phase 320,000 participants (Anticipated)Interventional1995-10-31Active, 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 2126 participants (Actual)Interventional2007-08-31Completed
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 2290 participants (Anticipated)Interventional2019-09-23Active, 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 30 participants Interventional1999-11-16Completed
Phase I Study of Z-Endoxifen as a Hormonal Therapy for Breast Cancer [NCT01327781]Phase 162 participants (Actual)Interventional2011-03-25Active, 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 250 participants (Actual)Interventional2003-10-31Completed
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 217 participants (Actual)Interventional2021-11-22Completed
Assessing the REsponse Rate of Weekly Neo-adjuvanT pacliTAxel (Taxol) in Nigerian Women With Breast Cancer (ARETTA) [NCT03058939]Phase 20 participants (Actual)Interventional2018-11-30Withdrawn(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)Observational2021-01-01Recruiting
Treatment Effect of Tamoxifen on Patients With DMD [NCT02835079]Phase 119 participants (Actual)Interventional2016-11-30Completed
Tamoxifen Therapy to Treat Pulmonary Arterial Hypertension [NCT03528902]Phase 218 participants (Actual)Interventional2018-10-01Completed
Fertility Preservation Using Tamoxifen and Letrozole in Estrogen Sensitive Tumors Trial [NCT03011684]Phase 3144 participants (Anticipated)Interventional2016-07-21Recruiting
Efficacy Of Tocotrienol a Natural Vitamin E In Biopsy Wound. [NCT01579227]101 participants (Anticipated)Observational2012-01-31Active, not recruiting
Cisplatin, Doxorubicin and Tamoxifen in the Treatment of Incurable Soft Tissue and Endocrine Malignancies [NCT00002608]Phase 230 participants (Anticipated)Interventional1994-05-31Completed
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 31,884 participants (Actual)Interventional2002-03-31Active, 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 2124 participants (Actual)Interventional2011-01-07Completed
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 3680 participants (Anticipated)Interventional2016-03-30Recruiting
Phase II Open Label Study of Everolimus in Combination With Anti-estrogen Therapy in Hormone Receptor-Positive HER2-Negative Advanced Breast Cancer [NCT02291913]Phase 248 participants (Actual)Interventional2014-12-18Completed
QUADRANTECTOMY PLUS AXILLARY DISSECTION VERSUS QUADRANTECTOMY ALONE IN MAMMOGRAPHIC STAGE T1N0 BREAST CANCER PATIENTS AGED OVER 65 YEARS [NCT00002720]Phase 3642 participants (Anticipated)Interventional1995-12-31Completed
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 3224 participants (Actual)Interventional1997-04-25Completed
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 3667 participants (Actual)Interventional1996-09-24Completed
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 32,411 participants (Actual)Interventional1995-12-31Completed
PROSPECTIVE RANDOMISED EVALUATION OF HIGH-INTENSITY CHEMOTHERAPY WITH PERIPHERAL BLOOD PROGENITOR SUPPORT IN PATIENTS WITH HIGH RISK BREAST CANCER [NCT00002755]Phase 3600 participants (Anticipated)Interventional1995-11-30Completed
Reversing Therapy Resistance With Epigenetic-immune Modification: Phase II Trial of Vorinostat, Tamoxifen and Pembrolizumab in Hormone Receptor Expressing Advanced Breast Cancer [NCT02395627]Phase 238 participants (Actual)Interventional2015-05-04Terminated(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 3180 participants (Actual)Interventional2006-05-16Completed
Combination of Chemopreventive Agents (All- Trans Retinoic Acid and Tamoxifen) as Potential Treatment for the Lung Complication of COVID-19 [NCT04568096]Phase 2160 participants (Anticipated)Interventional2020-11-30Not 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 3350 participants (Anticipated)Interventional1998-11-30Active, not recruiting
RANDOMIZED PHASE II STUDY IN FIRST LINE HORMONAL TREATMENT FOR METASTATIC BREAST CANCER WITH EXEMESTANE OR TAMOXIFEN IN POSTMENOPAUSAL PATIENTS [NCT00002777]Phase 3342 participants (Anticipated)Interventional1996-05-31Completed
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 30 participants Interventional1997-05-31Completed
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 252 participants (Actual)Interventional1996-05-31Completed
Tamoxifen for the Treatment of Unfavorable Bleeding Patterns in Etonogestrel Contraceptive Implant Users [NCT02070692]Phase 456 participants (Actual)Interventional2014-02-28Completed
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 31,099 participants (Actual)Interventional1990-12-31Completed
[NCT02062489]Phase 3688 participants (Anticipated)Interventional2014-05-31Recruiting
Neoadjuvant Endocrine Therapy in Locally Advanced Hormone Receptor Positive Breast Cancer in a Low-Resource, Middle-Income Setting (Guatemala) [NCT02806544]Phase 235 participants (Actual)Interventional2013-01-31Completed
Phase II Study of Hormone Therapy With Tamoxifen in Patients With Well Differentiated Neuroendocrine Tumors and Hormone Receptor Positive Expression [NCT03870399]Phase 223 participants (Actual)Interventional2019-03-13Active, 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 228 participants (Actual)Interventional2017-04-24Completed
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 25 participants (Actual)Interventional2010-07-31Terminated(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 3160 participants (Anticipated)Interventional2021-08-31Not yet recruiting
An Investigator Initiated Registry of Simple Oral Therapy for Low Risk Breast Cancer (SOLR) [NCT03238703]Phase 40 participants (Actual)Interventional2018-09-01Withdrawn(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 33 participants (Actual)Interventional2022-02-17Terminated(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 2200 participants (Actual)Interventional1999-08-31Completed
Predicting an Accurate Tamoxifen Dose: a Feasibility Study in Patients With Hormone Sensitive Breast Cancer [NCT05525481]Phase 4100 participants (Anticipated)Interventional2022-11-01Recruiting
A Phase III Study to Evaluate Letrozole as Adjuvant Endocrine Therapy for Postmenopausal Women With Receptor (ER and/or PgR) Positive Tumors [NCT00004205]Phase 38,028 participants (Actual)Interventional1998-03-31Completed
PROTOCOL FOR THE SCOTTISH CHEMO-ENDOCRINE TRIAL D [NCT00002579]Phase 32,000 participants (Anticipated)Interventional1993-03-31Completed
Twin Cities Brachytherapy Study for Ductal Carcinoma in Situ A Phase II Trial [NCT00290654]Phase 245 participants (Actual)Interventional2002-12-31Terminated(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 3249 participants (Actual)Interventional2006-02-28Completed
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 274 participants (Actual)Interventional2015-02-28Active, not recruiting
A Phase 1 Study of an Oral p38 MAPK Inhibitor in Patients With Advanced Cancer [NCT01393990]Phase 189 participants (Actual)Interventional2008-09-04Completed
A Pilot Study Evaluating Megestrol Acetate Modulation in Advanced Breast Cancer With Positive Hormonal Receptor [NCT03024580]Phase 220 participants (Anticipated)Interventional2017-03-06Recruiting
PROMOTE Study: Prediction of Response Of HorMOnal Treatment in Advanced and Recurrent Endometrial Cancer [NCT03621904]150 participants (Anticipated)Observational [Patient Registry]2022-10-15Recruiting
International Breast Cancer Intervention Study: A Multicentre Trial of Tamoxifen to Prevent Breast Cancer [NCT00002644]Phase 37,154 participants (Actual)Interventional1994-01-31Active, not recruiting
The Effects of Short-term Preoperative Treatment With Hormonal Therapy on Gene Profiles in Breast Cancer [NCT04129216]Phase 230 participants (Anticipated)Interventional2019-02-20Active, 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)Observational2017-09-01Recruiting
A Phase II Multi-Institutional Study of Concurrent Radiotherapy, Palbociclib, and Hormone Therapy for Treatment of Bone Metastasis in Breast Cancer Patients [NCT03691493]Phase 238 participants (Actual)Interventional2019-02-08Completed
A Pilot Trial Comparing Doxorubicin and Paclitaxel Induced Apoptosis in Locally Advanced Breast Cancer [NCT00003035]Phase 240 participants (Anticipated)Interventional1997-03-31Completed
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 239 participants (Actual)Interventional1999-02-28Completed
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 188 participants (Actual)Interventional2015-02-04Completed
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 179 participants (Actual)Interventional2014-09-01Completed
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)Observational2009-09-30Completed
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 21,440 participants (Actual)Interventional2016-11-30Completed
Low Dose TamOxifen and LifestylE Changes for bReast cANcer prevenTion: a Randomized Phase II Biomarker Trial in Subjects at Increased Risk [NCT06033092]Phase 2200 participants (Anticipated)Interventional2023-09-01Not yet recruiting
Phase I Trial of Endoxifen Gel Versus Placebo Gel in Women Undergoing Breast Surgery [NCT03317405]Phase 132 participants (Actual)Interventional2018-10-31Active, 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 244 participants (Anticipated)Interventional2015-05-31Recruiting
Effects of Cimicifuga Racemosa L. Nutt Sexuality of Women With Breast Cancer Using Tamoxifen or Aromatase Inhibitor [NCT02467686]Phase 460 participants (Anticipated)Interventional2014-01-31Recruiting
Endocrine Treatment Alone as Primary Treatment for Elderly Patients With Estrogen Receptor Positive Operable Breast Cancer and Low Recurrence Score [NCT02476786]Phase 250 participants (Anticipated)Interventional2017-01-17Recruiting
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 28 participants (Actual)Interventional2015-01-31Terminated(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 3636 participants (Actual)Interventional1999-12-31Completed
Neoadjuvant Treatment of Breast Cancer - a Prospective Observational Study, PANnon ONCology (PANONC) Group Non-commercial Clinical Trial [NCT05131893]300 participants (Anticipated)Observational [Patient Registry]2022-03-31Not yet recruiting
Elacestrant for Treating ER+/HER2- Breast Cancer Patients With ctDNA Relapse [NCT05512364]Phase 3220 participants (Anticipated)Interventional2023-12-15Not 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 21,100 participants (Anticipated)Interventional2022-03-30Recruiting
Phase II Study of Bicalutamide and Dutasteride for Prostate Cytoreduction Prior to Permanent Implant I-125 Prostate Brachytherapy [NCT00866554]Phase 260 participants (Actual)Interventional2009-03-31Completed
Utilization of Decision Aids for Tamoxifen Treatment in Breast Cancer Patients: A Randomized Controlled Trial. [NCT02488603]360 participants (Anticipated)Interventional2015-08-31Not yet recruiting
A Pilot Study of Tamoxifen in Oesophageal Cancer [NCT02513849]Phase 120 participants (Anticipated)Interventional2015-12-31Recruiting
Phase II Trial of Estrogen Receptor Targeted Treatment of Non-Muscle Invasive Bladder Cancer With Tamoxifen. [NCT02197897]Phase 215 participants (Actual)Interventional2015-04-01Completed
Phase II Study of Everolimus Beyond Progression in Postmenopausal Women With Advanced, Hormone Receptor Positive Breast Cancer [NCT02269670]Phase 23 participants (Actual)Interventional2014-11-25Terminated(stopped due to Slow to accrual)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00003042 (2) [back to overview]Three-year Relapse-free Survival
NCT00003042 (2) [back to overview]Five-year Overall Survival
NCT00003199 (3) [back to overview]Overall Survival
NCT00003199 (3) [back to overview]Number of Participants With Toxicity of a Combination of Low-dose IL-2 and GM-CSF
NCT00003199 (3) [back to overview]Event-free Survival
NCT00005908 (4) [back to overview]Number of Participants, e.g. Responders and Non-responders With a Percent Change in Expression Patterns After Chemotherapy With Changes in Expression Patterns After Chemotherapy in Preclinical Models
NCT00005908 (4) [back to overview]Overall Clinical Response Rate
NCT00005908 (4) [back to overview]Number of Participants With Adverse Events
NCT00005908 (4) [back to overview]Complementary Deoxyribonucleic Acid (cDNA) Expression
NCT00036270 (5) [back to overview]Number of Participants With New Primary Non-breast Cancers
NCT00036270 (5) [back to overview]Disease Free Survival (DFS): Number of Events (Disease Relapse or Death) From Baseline up to 2.75 Years
NCT00036270 (5) [back to overview]Disease Free Survival (DFS): Number of Events (Disease Relapse or Death) From Baseline up to 5 Years
NCT00036270 (5) [back to overview]Number of Events for Overall Survival (OS)
NCT00036270 (5) [back to overview]Number of Events for Time to Relapse
NCT00038467 (27) [back to overview]Percentage of Deoxy-pyridinoline (DPD) Urine Concentration Relative to Baseline: Bone Metabolism Sub-study
NCT00038467 (27) [back to overview]Percentage of C-Terminal Telopeptide (CTX) Serum Concentration Relative to Baseline: Bone Metabolism Sub-study
NCT00038467 (27) [back to overview]Percentage of Bone Specific Alkaline Phosphatase (BAP) Serum Concentration Relative to Baseline: Bone Metabolism Sub-study
NCT00038467 (27) [back to overview]Percent Change From Baseline in Lumbar Spine and Proximal Femur (Total Hip) Bone Mineral Density (BMD) at 6, 12, 24 Months On-treatment and 24 Months Post-treatment: Bone Metabolism Sub-study
NCT00038467 (27) [back to overview]Percent Change From Baseline in Femoral Neck and Femoral Wards Bone Mineral Density (BMD) at 6, 12 and 24 Months On-treatment and 24 Months Post-treatment: Bone Metabolism Sub-study
NCT00038467 (27) [back to overview]Number of Participants With Polyps, Fibroids and Ovarian Cysts: Endometrial Sub-study
NCT00038467 (27) [back to overview]Endometrial Thickness: Endometrial Sub-study
NCT00038467 (27) [back to overview]Change From Baseline in Relationship With Doctor (RWD) Subscale Score at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Substudy
NCT00038467 (27) [back to overview]Change From Baseline in Social/Family Well-Being (SWB) Sub-scale Score at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Sub-study
NCT00038467 (27) [back to overview]Change From Baseline in Total Functional Assessment of Cancer Therapy - General Breast and Endocrine (FACT-GBE) Score at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Sub-study
NCT00038467 (27) [back to overview]Change From Baseline in Physical Well-Being (PWB) Subscale Score at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Sub-study
NCT00038467 (27) [back to overview]Change From Baseline in Lumbar Spine and Proximal Femur (Total Hip) Bone Mineral Density (BMD) T-scores at 6, 12 and 24 Months On-treatment and 24 Months Post-treatment: Bone Metabolism Sub-study
NCT00038467 (27) [back to overview]Change From Baseline in Functional Well-Being (FWB) Sub-scale Score at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Sub-study
NCT00038467 (27) [back to overview]Change From Baseline in Functional Assessment of Cancer Therapy - Endocrine Subscale (FACT-ES) Total Score at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Sub-study
NCT00038467 (27) [back to overview]Number of Participants With Severe Endocrine Symptoms: QoL Sub-study
NCT00038467 (27) [back to overview]Change From Baseline in Emotional Well-Being (EWB) Subscale Score at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Sub-study
NCT00038467 (27) [back to overview]Change From Baseline in Breast Cancer Subscale (BCS) Score at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Sub-study
NCT00038467 (27) [back to overview]Percentage of Participants With at Least 1 Gynecological Symptoms: Endometrial Sub-study
NCT00038467 (27) [back to overview]Overall Survival (OS) at Month 36 Post-Randomization: Main Study
NCT00038467 (27) [back to overview]Number of Participants With Fracture: Bone Metabolism Sub-study
NCT00038467 (27) [back to overview]Number of Events of Second Breast Cancer in Contralateral Breast: Main Study
NCT00038467 (27) [back to overview]Change From Baseline in Treatment Outcome Index (TOI) at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Sub-study
NCT00038467 (27) [back to overview]Disease-Free Survival (DFS) at Month 36 Post-Randomization: Main Study
NCT00038467 (27) [back to overview]Uterine and Overall Ovary Volume: Endometrial Sub-study
NCT00038467 (27) [back to overview]Percentage of Participants With Endometrial Thickness Greater Than or Equal to (>=) 5 Millimeter (mm): Endometrial Sub-study
NCT00038467 (27) [back to overview]Percentage of Osteocalcin (OC) and Procollagen T1 C-Peptide (PICP) Serum Concentration Relative to Baseline: Bone Metabolism Sub-study
NCT00038467 (27) [back to overview]Percentage of N-telopeptide of Type 1 Collagen (NTX) Urine Concentration Relative to Baseline: Bone Metabolism Sub-study
NCT00041080 (1) [back to overview]Median Progression-free Survival
NCT00053898 (10) [back to overview]Percentage of Patients Alive and Disease-free
NCT00053898 (10) [back to overview]Percentage of Patients Free From Breast Cancer
NCT00053898 (10) [back to overview]Percentage of Patients Free From Contralateral Breast Cancer
NCT00053898 (10) [back to overview]Percentage of Patients Free From Invasive Breast Cancer
NCT00053898 (10) [back to overview]Percentage of Patients Free From Ipsilateral Recurrence
NCT00053898 (10) [back to overview]Percentage of Patients Free From Non-breast Secondary Cancer
NCT00053898 (10) [back to overview]Percentage of Patients Free From Osteoporotic Fractures
NCT00053898 (10) [back to overview]Quality of Life-Short Form 12 (SF-12) Physical Health Component Score
NCT00053898 (10) [back to overview]Quality-adjusted Survival Time
NCT00053898 (10) [back to overview]Percentage of Patients Alive (Overall Survival)
NCT00066690 (4) [back to overview]Overall Survival
NCT00066690 (4) [back to overview]Breast Cancer-free Interval
NCT00066690 (4) [back to overview]Disease-free Survival
NCT00066690 (4) [back to overview]Distant Recurrence-free Interval
NCT00066703 (4) [back to overview]Overall Survival
NCT00066703 (4) [back to overview]Distant Recurrence-free Interval
NCT00066703 (4) [back to overview]Disease-free Survival
NCT00066703 (4) [back to overview]Breast Cancer-free Interval
NCT00068419 (3) [back to overview]Percentage of Patients With Tumor Response From Imaging
NCT00068419 (3) [back to overview]Percentage of Patients Failure Free at 2 Years Following Study Entry
NCT00068419 (3) [back to overview]Percentage of Patients Experiencing a Grade 3 or Higher Adverse Event During Therapy.
NCT00108069 (3) [back to overview]Number of Participants With Adverse Events
NCT00108069 (3) [back to overview]Adverse Event Grades
NCT00108069 (3) [back to overview]Response, Defined as Stable Disease or Objective (Partial or Complete) Response.
NCT00118157 (1) [back to overview]Tumor Response Rate (Complete and Partial) Assessed by Response Evaluation Criteria in Solid Tumors (RECIST)
NCT00119262 (3) [back to overview]Proportion of Patients With Absolute Decrease in Left Ventricular Ejection Fraction (LVEF) Levels Post Doxorubicin and Cyclophosphamide(AC)
NCT00119262 (3) [back to overview]Proportion of Patients With Absolute Decrease in LVEF Levels Post Bevacizumab
NCT00119262 (3) [back to overview]Congestive Heart Failure Rate
NCT00171704 (8) [back to overview]Percentage Change From Baseline in Serum Lipids at 5 Years
NCT00171704 (8) [back to overview]Time to Disease Recurrence or Death
NCT00171704 (8) [back to overview]Percent Change From Baseline of Bone Mineral Density (BMD) of Total Hip
NCT00171704 (8) [back to overview]Percent Change From Baseline of Bone Mineral Density of the Lumbar Spine
NCT00171704 (8) [back to overview]Percent Change From Baseline of Bone Mineral Density of the Lumbar Spine (L2-l4)
NCT00171704 (8) [back to overview]Time to Overall Survival Events
NCT00171704 (8) [back to overview]Median Percent Change From Baseline of Serum Markers of Bone Turnover
NCT00171704 (8) [back to overview]Number of Participants With Clinically Relevant Changes From Baseline in Cholesterol
NCT00194779 (6) [back to overview]Relapse Rate in Patients With Operable Breast Cancer Treated With Neoadjuvant Chemotherapy for 12 Weeks Followed by Weekly Paclitaxel for 12 Weeks and Adjuvant Chemotherapy
NCT00194779 (6) [back to overview]Combined Rate of Microscopic pCR and Macroscopic Pathologic Complete Response (mCR)
NCT00194779 (6) [back to overview]Number and Percent of Patients Reporting Grade 2, 3, 4, or Fatal Toxicities of These Regimens, Need for Dose Reduction, or Treatment Interruption or Discontinuation
NCT00194779 (6) [back to overview]Time to Progression
NCT00194779 (6) [back to overview]Disease-free Survival
NCT00194779 (6) [back to overview]OS in Patients With Operable Breast Cancer Treated With Neoadjuvant Chemotherapy for 12 Weeks Followed Weekly Paclitaxel for 12 Weeks and Adjuvant Chemotherapy With XMN
NCT00201851 (1) [back to overview]Disease-free Survival
NCT00240071 (2) [back to overview]Objective Response Rate (Defined as the Rate of Complete and Partial Responses).
NCT00240071 (2) [back to overview]Progression Free Survival (PFS)
NCT00276094 (14) [back to overview]Change From Baseline in Severity of VVA Symptoms
NCT00276094 (14) [back to overview]Change From Baseline in Estradiol Levels
NCT00276094 (14) [back to overview]Change From Baseline in Follicle Stimulating Hormone Levels
NCT00276094 (14) [back to overview]Change From Baseline in Luteinizing Hormone Levels
NCT00276094 (14) [back to overview]Change From Baseline in Sex Hormone Binding Globulin Levels
NCT00276094 (14) [back to overview]Change From Baseline in Testosterone (Free) Levels
NCT00276094 (14) [back to overview]Change From Baseline in Testosterone (Total) Levels
NCT00276094 (14) [back to overview]Mean Change From Baseline in Percentage of Parabasal Cells in Maturation Index of Vaginal Smear
NCT00276094 (14) [back to overview]Mean Change From Baseline in the MBS of Vaginal Pain Associated With Sexual Activity
NCT00276094 (14) [back to overview]Mean Change From Baseline in the Most Bothersome Vulvar and Vaginal Atrophy (VVA) Symptom (MBS) of Vaginal Dryness
NCT00276094 (14) [back to overview]Mean Change From Baseline in the Percentage of Superficial Cells in Maturation Index of Vaginal Smear
NCT00276094 (14) [back to overview]Mean Change From Baseline in Vaginal pH
NCT00276094 (14) [back to overview]Change From Baseline in Visual Evaluation of the Vagina
NCT00276094 (14) [back to overview]Change From Baseline in Urinary Symptoms
NCT00290654 (8) [back to overview]Percentage of Physicians Judging the Cosmetic Outcome as Good or Excellent
NCT00290654 (8) [back to overview]Percentage of Patients Who Experienced Complications
NCT00290654 (8) [back to overview]Number of Patients With Ipsilateral Breast Tumor Recurrence
NCT00290654 (8) [back to overview]Percentage of Physicians Judging the Cosmetic Outcome as Good or Excellent
NCT00290654 (8) [back to overview]Percentage of Patients Judging the Cosmetic Outcome as Good or Excellent
NCT00290654 (8) [back to overview]Number of Patients With Ipsilateral Breast Tumor Recurrence
NCT00290654 (8) [back to overview]Percentage of Patients Judging the Cosmetic Outcome as Good or Excellent
NCT00290654 (8) [back to overview]Percentage of Patients Who Experienced Complications
NCT00290745 (9) [back to overview]Correlation Between Pathologic Tumor Size and Mammographic Tumor Size
NCT00290745 (9) [back to overview]Correlation Between Pathologic Tumor Size at Radiographic (MRI) Tumor Size
NCT00290745 (9) [back to overview]Median Reduction in Tumor Volume by Estrogen Receptor Hormone (ER H-) Quartile Group
NCT00290745 (9) [back to overview]Median Change in 6-month Tumor Volume Compared to Baseline Using Mammography
NCT00290745 (9) [back to overview]Median Change in 6-month Tumor Volume Compared to Baseline Using Magnetic Resonance Imaging (MRI)
NCT00290745 (9) [back to overview]Number of Responders to Neoadjuvant Therapy at Month 6
NCT00290745 (9) [back to overview]Number of Responders to Neoadjuvant Therapy at Month 3
NCT00290745 (9) [back to overview]Median Reduction in Tumor Volume by PgR H-score by Quartile Group
NCT00290745 (9) [back to overview]Median Reduction in Tumor Volume by Ki-67 Average Score
NCT00293540 (1) [back to overview]Overall Survival
NCT00310180 (5) [back to overview]5-year Disease-free Survival
NCT00310180 (5) [back to overview]5-year Distant Recurrence-free Interval
NCT00310180 (5) [back to overview]5-year Overall Survival
NCT00310180 (5) [back to overview]5-year Recurrence-free Interval
NCT00310180 (5) [back to overview]5-year Disease-free Survival by Age and Recurrence Score Groups
NCT00365599 (3) [back to overview]Time to Progression (TTP)
NCT00365599 (3) [back to overview]Number of Participants With Serious Adverse Events (SAEs)
NCT00365599 (3) [back to overview]Number of Participants With Objective Response (OR)
NCT00499083 (1) [back to overview]Number of Patients With Pathological Complete Response
NCT00537771 (3) [back to overview]Incidence of Fatty Liver Disease
NCT00537771 (3) [back to overview]Time to Treatment Failure
NCT00537771 (3) [back to overview]Incidence of Abnormal Liver Function
NCT00601900 (5) [back to overview]Progression-free Survival
NCT00601900 (5) [back to overview]Overall Survival (OS)
NCT00601900 (5) [back to overview]12 Month Progression Free Survival Rate
NCT00601900 (5) [back to overview]6 Month Progression-Free Survival Rate
NCT00601900 (5) [back to overview]Objective Response Rate
NCT00605267 (17) [back to overview]Endocrine Subscale (ES)
NCT00605267 (17) [back to overview]Serum Oestrone (E1) Concentrations
NCT00605267 (17) [back to overview]Human Epidermal Growth Factor Receptor 2 (HER2) Status
NCT00605267 (17) [back to overview]Functional Assessment of Cancer Therapy-Breast (FACT-B)
NCT00605267 (17) [back to overview]Histopathological Response Rate (HRR)
NCT00605267 (17) [back to overview]Progesterone Receptor (PgR) Status
NCT00605267 (17) [back to overview]Serum Oestradiol (E2) Concentrations
NCT00605267 (17) [back to overview]Oestrogen Receptor (ER) Status
NCT00605267 (17) [back to overview]Anastrozole Plasma Concentrations (Cmin)
NCT00605267 (17) [back to overview]Best Overall Response Rate (BORR) (Calliper)
NCT00605267 (17) [back to overview]Best Overall Response Rate (BORR) (MRI/CT)
NCT00605267 (17) [back to overview]Best Overall Response Rate (BORR) (US)
NCT00605267 (17) [back to overview]Bone Mineral Density (BMD) Cervical Thighbone
NCT00605267 (17) [back to overview]Bone Mineral Density (BMD) Lumbar Spine
NCT00605267 (17) [back to overview]Bone Turnover Marker (BAP) CLEIA Method
NCT00605267 (17) [back to overview]Bone Turnover Marker (BAP) EIA Method
NCT00605267 (17) [back to overview]Bone Turnover Marker (NTX)
NCT00630539 (11) [back to overview]Mean Change From Baseline in Vaginal pH
NCT00630539 (11) [back to overview]Mean Change From Baseline in Sex Hormone Binding Globulin Levels
NCT00630539 (11) [back to overview]Mean Change From Baseline in Percentage of Parabasal Cells in the Maturation Index of the Vaginal Smear
NCT00630539 (11) [back to overview]Mean Change From Baseline in Vaginal pH
NCT00630539 (11) [back to overview]Visual Evaluation of Vagina (by Gynecological Examination)
NCT00630539 (11) [back to overview]Mean Change From Baseline in Percentage of Superficial Cells in the Maturation Index
NCT00630539 (11) [back to overview]Mean Change From Baseline in Percentage of Superficial Cells in Maturation Index of the Vaginal Smear
NCT00630539 (11) [back to overview]Mean Change From Baseline in Percentage of Parabasal Cells in the Maturation Index
NCT00630539 (11) [back to overview]Mean Change From Baseline in Luteinizing Hormone Levels
NCT00630539 (11) [back to overview]Mean Change From Baseline in Follicle Stimulating Hormone Levels
NCT00630539 (11) [back to overview]Mean Change From Baseline in Estradiol Levels
NCT00659373 (1) [back to overview]Change in Cognitive Function Over 1 Year in Premenopausal Breast Cancer Patients Who Receive Adjuvant Tamoxifen (T) Alone Against Those Receive Adjuvant Tamoxifen (T+OFS) or Exemestane (E+OFS) With Ovarian Function Suppression (OFS)
NCT00687102 (8) [back to overview]Mean Change From Baseline on the Geriatric Depression Scale Scores by Treatment Group
NCT00687102 (8) [back to overview]Mean Change From Baseline on Card Rotations Test Scores by Treatment Group
NCT00687102 (8) [back to overview]Mean Change From Baseline on the Finger Tapping Test Scores by Treatment Group
NCT00687102 (8) [back to overview]Mean Change From Baseline on the Letter Fluency and Semantic Fluency Scores by Treatment Group
NCT00687102 (8) [back to overview]Mean Change From Baseline on the Positive and Negative Affect Schedule Scores by Treatment Group
NCT00687102 (8) [back to overview]Mean Change From Baseline on the the Benton Visual Retention Test Scores by Treatment Group
NCT00687102 (8) [back to overview]Mean Change From Baseline on the the California Verbal Learning Test Scores by Treatment Group
NCT00687102 (8) [back to overview]Mean Change From Baseline on Digit Span Test Scores by Treatment Group
NCT00710970 (1) [back to overview]Number of Participants With Freedom From Progression of Cancer at 4 Months
NCT00728949 (6) [back to overview]12-Month Survival Rate
NCT00728949 (6) [back to overview]Overall Survival (OS)
NCT00728949 (6) [back to overview]Percentage of Participants With Complete Response (CR) and Partial Response (PR) or Stable Disease (SD) Disease Control Rate [DCR])
NCT00728949 (6) [back to overview]Number of Participants Experiencing Adverse Events (AEs) in National Cancer Institute Common Toxicity Criteria for AE's (NCI-CTCAE) Version 3.0 Criteria for Adverse Events (NCI-CTCAE)
NCT00728949 (6) [back to overview]Progression-Free Survival (PFS)
NCT00728949 (6) [back to overview]Percentage of Participants With Complete Response (CR) and Partial Response (PR) (Objective Response Rate [ORR])
NCT00729586 (5) [back to overview]Incidence of Adverse Effects (Grade 3 or Higher) as Assessed by Common Terminology Criteria for Adverse Events Version 3.0
NCT00729586 (5) [back to overview]Duration of Progression-free Survival (PFS)
NCT00729586 (5) [back to overview]Duration of Overall Survival (OS)
NCT00729586 (5) [back to overview]Percentage of Participants With a Confirmed Objective Tumor Response Using RECIST Version 1.0
NCT00729586 (5) [back to overview]Number of Participants and Their Levels of Expression of the Candidate Markers
NCT00764322 (6) [back to overview]Patient Understanding of Pharmacogenomics
NCT00764322 (6) [back to overview]Change in Median Endoxifen Concentrations to Determine Feasibility of Obtaining Pharmacogenomic Information From Patients in the Clinical Setting and Using it to Guide Changes in Therapy
NCT00764322 (6) [back to overview]Change in Plasma Endoxifen Levels After an Increase in Tamoxifen Citrate Dose From 20 mg to 40 mg Daily in Patients With Poor-metabolizing Genotypes
NCT00764322 (6) [back to overview]CYP2D6 Allele Frequencies and Endoxifen Levels Among African-American Women Taking Tamoxifen Citrate
NCT00764322 (6) [back to overview]Endoxifen Concentrations in Participants Receiving Tamoxifen Citrate Dose of 20 mg or 40 mg Stratified by the Metabolizing CYP2D6 Genotypes
NCT00764322 (6) [back to overview]Number of Participants With Pulmonary Embolism (PE), Deep Vein Thrombosis (DVT), Stroke, and/or Endometrial Cancer
NCT00873366 (16) [back to overview]Median of 6 Month Tamoxifen Steady State Plasma Concentrations According to CYP2D6 Phenotype Group
NCT00873366 (16) [back to overview]Operating Characteristics of the ¹³C-dextromethorphan (13C-DM) Breath Test in Identifying Those Who Are CYP2D6 Genotypic Poor Metabolizers
NCT00873366 (16) [back to overview]Spearman's Rank Correlation Coefficient Between CYP2D6 Activity Score and Endoxifen Steady State Concentrations (Endx Css)
NCT00873366 (16) [back to overview]Spearman's Rank Correlation Coefficient Between CYP2D6 Activity Score and Endoxifen/N-desmethyl-tamoxifen (Endx/NDMT) Ratio
NCT00873366 (16) [back to overview]Spearman's Rank Correlation Coefficient Between CYP2D6 Genotype and ¹³Cdextromethorphan Breath Test (DM-BT)
NCT00873366 (16) [back to overview]Spearman's Rank Correlation Coefficient Between 3 Month DM-BT and 3 Month Endoxifen Steady State Concentrations
NCT00873366 (16) [back to overview]Spearman's Rank Correlation Coefficient Between 6 Month DM-BT and 6 Month Endoxifen Steady State Concentrations
NCT00873366 (16) [back to overview]Spearman's Rank Correlation Coefficient Between Baseline DM-BT and 3 Month Endoxifen Steady State Concentrations
NCT00873366 (16) [back to overview]Spearman's Rank Correlation Coefficient Between Baseline DM-BT and 3 Month Endoxifen/N-desmethyl-tamoxifen (Endx/NDMT) Ratio
NCT00873366 (16) [back to overview]Median of 3 Month 4-hydroxy-tamoxifen (4HT) Steady State Plasma Concentrations According to CYP2D6 Phenotype Group
NCT00873366 (16) [back to overview]Median of 3 Month Endoxifen Steady State Concentrations (Endx Css) According to CYP2D6 Phenotype Group and Activity Score
NCT00873366 (16) [back to overview]Median of 3 Month N-desmethyl-tamoxifen (NDMT) Steady State Plasma Concentrations According to CYP2D6 Phenotype Group
NCT00873366 (16) [back to overview]Median of 3 Month Tamoxifen Steady State Plasma Concentrations According to CYP2D6 Phenotype Group
NCT00873366 (16) [back to overview]Median of 6 Month 4-hydroxy-tamoxifen (4HT) Steady State Plasma Concentrations According to CYP2D6 Phenotype Group
NCT00873366 (16) [back to overview]Median of 6 Month Endoxifen Steady State Concentrations (Endx Css) According to CYP2D6 Phenotype Group and Activity Score
NCT00873366 (16) [back to overview]Median of 6 Month N-desmethyl-tamoxifen (NDMT) Steady State Plasma Concentrations According to CYP2D6 Phenotype Group
NCT00952731 (6) [back to overview]Difference in Mean Score for Vasomotor Symptoms Including Hot Flashes From Baseline to Time of Surgery
NCT00952731 (6) [back to overview]Difference in vWF Coagulation Protein in Blood Collected at Baseline and Just Prior to Surgery
NCT00952731 (6) [back to overview]Difference in Protein S Coagulation Protein in Blood Collected at Baseline and Just Prior to Surgery
NCT00952731 (6) [back to overview]Difference in Factor VIII Coagulation Protein in Blood Collected at Baseline and Just Prior to Surgery
NCT00952731 (6) [back to overview]Difference in Factor IX Coagulation Protein in Blood Collected at Baseline and Just Prior to Surgery
NCT00952731 (6) [back to overview]Difference Between Ki-67 Labeling Index in Tissue Samples Taken at Baseline and Post-treatment
NCT00999921 (3) [back to overview]Number of Participants Analysed for Response of Cyclical Mastalgia (Good Response Was Defined as Disappearance of Mastalgia)
NCT00999921 (3) [back to overview]Number of Participants Analysed for Reduction in Mastalgia (Cardiff Breast Pain Score).
NCT00999921 (3) [back to overview]Number of Participants Analysed for Reduction in Lump Size ( 60% Reduction in Lump Size Considered to be a Satisfactory Response)
NCT01027416 (2) [back to overview]Total Number of Over-expressed Genes, Across All Participants With Tumor Protein p53-wild Type Breast Tumors That Had RNA Samples Available.
NCT01027416 (2) [back to overview]Mean Percent Positive Proximity Ligation Assays of All Tumor Protein p53-wild Type Breast Tumors in Participants by Treatment Arm
NCT01124695 (6) [back to overview]Endoxifen Concentration by Response
NCT01124695 (6) [back to overview]Progression-free Survival by CYP2D6 Status in 2 Categories
NCT01124695 (6) [back to overview]Progression-free Survival by CYP2D6 Status in 3 Categories
NCT01124695 (6) [back to overview]Progression-free Survival From 3 Months Post Registration
NCT01124695 (6) [back to overview]Proportion of Patients Progression-free at 6 Months
NCT01124695 (6) [back to overview]Proportion of Patients With Response
NCT01189500 (22) [back to overview]4-hydroxy-tamoxifen (Metabolite) Time for Cmax (Tmax) Following Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]Endoxifen (Metabolite) Area Under the Plasma Concentration-time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) Following Endoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]Endoxifen (Metabolite) Maximum Observed Concentration (Cmax) Following Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]Tamoxifen Terminal Half-life (t 1/2) Following Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]Endoxifen (Metabolite) Terminal Half-life (t 1/2) Following Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]Plasma 4-hydroxy-tamoxifen (Metabolite) Concentration Versus Time Summary: Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]Plasma Endoxifen (Metabolite) Concentration Versus Time Summary: Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]Tamoxifen Time for Cmax (Tmax) Following Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]Plasma Tamoxifen Concentration Versus Time Summary: Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]N-desmethyl-tamoxifen (Metabolite) Area Under the Plasma Concentration-time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) Following Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]Plasma N-desmethyl-tamoxifen (Metabolite) Concentration Versus Time Summary: Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]N-desmethyl-tamoxifen (Metabolite) Maximum Observed Concentration (Cmax) Following Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]N-desmethyl-tamoxifen (Metabolite) Terminal Half-life (t 1/2) Following Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]N-desmethyl-tamoxifen (Metabolite) Time for Cmax (Tmax) Following Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]Tamoxifen Apparent Clearance (CL/F) Following Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]Tamoxifen Apparent Volume of Distribution (Vz/F) Following Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]Tamoxifen Area Under the Plasma Concentration-time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) Following Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]Tamoxifen Maximum Observed Concentration (Cmax) Following Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]Endoxifen (Metabolite) Time for Cmax (Tmax) Following Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]4-hydroxy-tamoxifen (Metabolite) Area Under the Plasma Concentration-time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) Following Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]4-hydroxy-tamoxifen (Metabolite) Maximum Observed Concentration (Cmax) Following Tamoxifen Alone and When Coadministered With DVS SR
NCT01189500 (22) [back to overview]4-hydroxy-tamoxifen (Metabolite) Terminal Half-life (t 1/2) Following Tamoxifen Alone and When Coadministered With DVS SR
NCT01196936 (9) [back to overview]Number of Participants With Different Patient Reported Symptoms, Measured by Questionnaire
NCT01196936 (9) [back to overview]Number of Grade 2-4 Toxicities
NCT01196936 (9) [back to overview]Mammographic Breast Density
NCT01196936 (9) [back to overview]Insulin Growth Factor Levels (IGF3 )
NCT01196936 (9) [back to overview]Insulin Growth Factor Levels (IGF1)
NCT01196936 (9) [back to overview]Biomarker Levels - Urine N-telopeptide
NCT01196936 (9) [back to overview]Biomarker Levels
NCT01196936 (9) [back to overview]Percentage of Pills Taken Out of the Total Prescribed
NCT01196936 (9) [back to overview]Biomarker Levels - Alkaline Phosphatase
NCT01257581 (11) [back to overview]Dose Adjustments
NCT01257581 (11) [back to overview]Lab Abnormal Reports by Treatment Assignment
NCT01257581 (11) [back to overview]HHD Upper Z-score
NCT01257581 (11) [back to overview]Tracheostomy-free Survival
NCT01257581 (11) [back to overview]Accurate Test of Limb Isometric Strength (ATLIS) Lower Percentage of Predicted Normal (PPN)
NCT01257581 (11) [back to overview]ATLIS Upper Percentage of Predicted Normal (PPN)
NCT01257581 (11) [back to overview]Change in ALS Functional Rating Scale - Revised (ALSFRS-R)
NCT01257581 (11) [back to overview]Hand Held Dynamometry (HHD) Lower Z-score
NCT01257581 (11) [back to overview]HHD Lower % Baseline
NCT01257581 (11) [back to overview]HHD Upper % Baseline
NCT01257581 (11) [back to overview]Vital Capacity/Pulmonary Function Testing
NCT01272037 (3) [back to overview]Distant Relapse-Free Survival (DRFS)
NCT01272037 (3) [back to overview]Invasive Disease-Free Survival (IDFS)
NCT01272037 (3) [back to overview]Number of Participants With Gr 3 Through 5 Adverse Events That Are Related to Study Drugs
NCT01293032 (1) [back to overview]The Proportion of Patients With RS 11-25 Who Refused the Assigned Treatment
NCT01393990 (6) [back to overview]PK: Maximum Plasma Concentration (Cmax) of LY2228820
NCT01393990 (6) [back to overview]PK: Area Under the Concentration-Time Curve From Time Zero to 8 Hours (AUC0-8) of LY2228820
NCT01393990 (6) [back to overview]Recommended Dose for Phase 2 Studies
NCT01393990 (6) [back to overview]Pharmacodynamics (PD): Number of Participants With Greater Than 50% Inhibition of p38 Mitogen-Activated Protein Kinase (MAPK) Activity on Day 1
NCT01393990 (6) [back to overview]Percentage of Participants With Best Overall Response [Complete Response (CR)+Partial Response (PR)+Stable Disease (SD)]
NCT01393990 (6) [back to overview]Number of Participants With Clinically Significant Effects (Physical Assessments and Safety Lab Tests)
NCT01585558 (58) [back to overview]Assessment of Breast Palpation
NCT01585558 (58) [back to overview]Assessment of Breast Palpation
NCT01585558 (58) [back to overview]Assessment of Cervical Pap Smear Samples
NCT01585558 (58) [back to overview]Assessment of Endometrial Biopsy
NCT01585558 (58) [back to overview]Assessment of Hematology Test Values
NCT01585558 (58) [back to overview]Assessment of Hematology Tests
NCT01585558 (58) [back to overview]Assessment of Mammography
NCT01585558 (58) [back to overview]Change From Baseline in Visual Evaluation of the Vagina
NCT01585558 (58) [back to overview]Incidence of Adverse Events (AEs)
NCT01585558 (58) [back to overview]Mean Change in Blood Chemistry Parameters
NCT01585558 (58) [back to overview]Mean Change in Blood Chemistry Parameters
NCT01585558 (58) [back to overview]Mean Percent Change From Baseline in Serum Lipids
NCT01585558 (58) [back to overview]Mean Percent Change From Baseline in Serum Lipids
NCT01585558 (58) [back to overview]Change From Baseline in Weight
NCT01585558 (58) [back to overview]Change From Baseline in E2 Levels
NCT01585558 (58) [back to overview]Change From Baseline in Visual Evaluation of the Vagina
NCT01585558 (58) [back to overview]Assessment of Endometrial Safety With a Transvaginal Ultrasound (TVU)
NCT01585558 (58) [back to overview]Assessment of Endometrial Safety With a TVU
NCT01585558 (58) [back to overview]Change From Baseline in Antithrombin Antigen, P Levels
NCT01585558 (58) [back to overview]Change From Baseline in Antithrombin Antigen, P Levels
NCT01585558 (58) [back to overview]Change From Baseline in BMI
NCT01585558 (58) [back to overview]Change From Baseline in BMI
NCT01585558 (58) [back to overview]Change From Baseline in DBP
NCT01585558 (58) [back to overview]Change From Baseline in Diastolic Blood Pressure (DBP)
NCT01585558 (58) [back to overview]Change From Baseline in Erythrocyte (RBC) Levels
NCT01585558 (58) [back to overview]Change From Baseline in Erythrocyte (RBC) Levels
NCT01585558 (58) [back to overview]Change From Baseline in Estradiol (E2) Levels
NCT01585558 (58) [back to overview]Change From Baseline in Fibrinogen Levels
NCT01585558 (58) [back to overview]Change From Baseline in Fibrinogen Levels
NCT01585558 (58) [back to overview]Change From Baseline in Follicle Stimulating Hormone (FSH) Levels
NCT01585558 (58) [back to overview]Change From Baseline in FSH Levels
NCT01585558 (58) [back to overview]Change From Baseline in Hematocrit Levels
NCT01585558 (58) [back to overview]Change From Baseline in Hematocrit Levels
NCT01585558 (58) [back to overview]Change From Baseline in Hemoglobin Levels
NCT01585558 (58) [back to overview]Change From Baseline in Hemogobin Levels
NCT01585558 (58) [back to overview]Change From Baseline in LH Levels
NCT01585558 (58) [back to overview]Change From Baseline in Luteinizing Hormone (LH) Levels
NCT01585558 (58) [back to overview]Change From Baseline in pH of Urine
NCT01585558 (58) [back to overview]Change From Baseline in pH of Urine
NCT01585558 (58) [back to overview]Change From Baseline in Protein C Ag, P Levels
NCT01585558 (58) [back to overview]Change From Baseline in Protein C Ag, P Levels
NCT01585558 (58) [back to overview]Change From Baseline in Protein S Ag (Free), P Levels
NCT01585558 (58) [back to overview]Change From Baseline in Protein S Ag (Free), P Levels
NCT01585558 (58) [back to overview]Change From Baseline in Pulse Rate
NCT01585558 (58) [back to overview]Change From Baseline in Pulse Rate
NCT01585558 (58) [back to overview]Change From Baseline in SBP
NCT01585558 (58) [back to overview]Change From Baseline in Sex Hormone Binding Globulin (SHBG) Levels
NCT01585558 (58) [back to overview]Change From Baseline in SHBG Levels
NCT01585558 (58) [back to overview]Change From Baseline in Specific Gravity of Urine
NCT01585558 (58) [back to overview]Change From Baseline in Specific Gravtiy of Urine
NCT01585558 (58) [back to overview]Change From Baseline in Systolic Blood Pressure (SBP)
NCT01585558 (58) [back to overview]Change From Baseline in Testosterone (Free) Levels
NCT01585558 (58) [back to overview]Change From Baseline in Testosterone (Free) Levels
NCT01585558 (58) [back to overview]Change From Baseline in Testosterone (Total) Levels
NCT01585558 (58) [back to overview]Change From Baseline in Testosterone (Total) Levels
NCT01585558 (58) [back to overview]Change From Baseline in Thromboplastin Time
NCT01585558 (58) [back to overview]Change From Baseline in Thromboplastin Time
NCT01585558 (58) [back to overview]Change From Baseline in Weight
NCT01614210 (5) [back to overview]Change in FACT-ES Symptom Scores
NCT01614210 (5) [back to overview]Change in FACT-ES Symptom Scores
NCT01614210 (5) [back to overview]Change in Ki67 Expression in Tumors
NCT01614210 (5) [back to overview]Correlation Between Changes in Ki67 and Symptoms
NCT01614210 (5) [back to overview]Number of Participants With Long Term Endocrine Therapy Adherence
NCT01674140 (4) [back to overview]Distant Recurrence-Free Survival (DRFS)
NCT01674140 (4) [back to overview]Invasive Disease-Free Survival (IDFS)
NCT01674140 (4) [back to overview]Overall Survival (OS)
NCT01674140 (4) [back to overview]Toxicity Based on Common Terminology Criteria for Adverse Events (CTCAE) Version 4.0, Assessed up to 10 Years.
NCT01831076 (1) [back to overview]Overall Response Rate as Measured by Clinical Exam, Standard Imaging, and Surgical Pathology Findings
NCT01896050 (3) [back to overview]Effect of Medication on Change in Grip Strength
NCT01896050 (3) [back to overview]Effect of Change in Body Mass Index on Change in Grip Strength With Aromatase Inhibitor Therapy
NCT01896050 (3) [back to overview]Association Between Baseline Body Mass Index and Discontinuation of Aromatase Inhibitor Therapy Within the First 12 Months
NCT02040857 (6) [back to overview]All Grade Treatment-Related Fatigue Toxicity Rate
NCT02040857 (6) [back to overview]Rate of Treatment Related Discontinuation
NCT02040857 (6) [back to overview]2-year Treatment Discontinuation Rate by Aromatase Inhibitor and Tamoxifen-based Therapy Subgroup
NCT02040857 (6) [back to overview]2-Year Treatment Discontinuation Rate
NCT02040857 (6) [back to overview]All GradeTreatment-Related Alopecia Toxicity Rate
NCT02040857 (6) [back to overview]Grade 3-4 Treatment-Related Neutropenia Toxicity Rate
NCT02070692 (5) [back to overview]Bleeding Days
NCT02070692 (5) [back to overview]Consecutive Bleeding-free Days After Study Drug
NCT02070692 (5) [back to overview]Satisfaction (as Recorded on a 100mm Visual Analog Scale Where 0 is Not at All Satisfied and 100mm is Completely Satisfied)
NCT02070692 (5) [back to overview]Number of Participants Experiencing Ovulation After First Use of Study Drug
NCT02070692 (5) [back to overview]Bleeding/Spotting Days
NCT02093351 (12) [back to overview]Effect of Tamoxifen on Exposure to Olaparib - AUC0-τ
NCT02093351 (12) [back to overview]Effect of Olaparib on Exposure to Letrozole - Cmax ss
NCT02093351 (12) [back to overview]Effect of Olaparib on Exposure to Letrozole - AUC0-τ
NCT02093351 (12) [back to overview]Effect of Anastrozole on Exposure to Olaparib - AUC0-τ
NCT02093351 (12) [back to overview]Effect of Olaparib on Exposure to Anastrozole - AUC0-τ
NCT02093351 (12) [back to overview]Effect of Letrozole on Exposure to Olaparib - AUC0-τ
NCT02093351 (12) [back to overview]Effect of Letrozole on Exposure to Olaparib - Cmax ss
NCT02093351 (12) [back to overview]Effect of Olaparib on Exposure to Tamoxifen - Cmax ss
NCT02093351 (12) [back to overview]Effect of Olaparib on Exposure to Tamoxifen - AUC0-τ
NCT02093351 (12) [back to overview]Effect of Anastrozole on Exposure to Olaparib - Cmax ss
NCT02093351 (12) [back to overview]Effect of Olaparib on Exposure to Anastrozole - Cmax ss
NCT02093351 (12) [back to overview]Effect of Tamoxifen on Exposure to Olaparib - Cmax ss
NCT02101788 (7) [back to overview]Incidence of Adverse Events (AEs)
NCT02101788 (7) [back to overview]Overall Survival
NCT02101788 (7) [back to overview]Objective Tumor Response Rate (Complete Response and Partial Response)
NCT02101788 (7) [back to overview]Patients Reported Acute Quality of Life
NCT02101788 (7) [back to overview]Progression Free Survival
NCT02101788 (7) [back to overview]Patient Reported Acute Peripheral Neuropathy Symptoms
NCT02101788 (7) [back to overview]Progression-free Survival (PFS)
NCT02197897 (1) [back to overview]Evaluate the Efficacy for Treatment of Low/Intermediate- Risk Bladder Tumors, Assessing for the Clinical Response of the Marker Lesion
NCT02228681 (4) [back to overview]Frequency of Response
NCT02228681 (4) [back to overview]Median Progression-free Survival
NCT02228681 (4) [back to overview]Median Survival
NCT02228681 (4) [back to overview]Frequency and Severity of CTCAE (Common Toxicity Criteria for Adverse Events) Version 4
NCT02278120 (5) [back to overview]Clinical Benefit Rate (CBR)
NCT02278120 (5) [back to overview]Duration of Response (DOR) Per Investigator's Assessment - Patients With Confirmed Complete Response (CR) or Partial Response (PR)
NCT02278120 (5) [back to overview]Progression Free Survival (PFS) Per Investigator's Assessment
NCT02278120 (5) [back to overview]Overall Response Rate (ORR) Per Local Assessment
NCT02278120 (5) [back to overview]Time to Response (TTR) Per Local Investigator's Assessment
NCT02291913 (6) [back to overview]Median Overall Survival (OS)
NCT02291913 (6) [back to overview]Median Progression Free Survival (PFS)
NCT02291913 (6) [back to overview]Median Time From First Occurrence of CR or PR to Disease Progression or Death Also Called Duration of Response (DOR)
NCT02291913 (6) [back to overview]Number of Participants With CR, PR, or 6 Months of SD Also Called Clinical Benefit Rate (CBR)
NCT02291913 (6) [back to overview]Number of Patients With Adverse Events (AEs) as a Measure of Safety and Tolerability
NCT02291913 (6) [back to overview]Number of Patients With an Objective Response (CR or PR) Also Called the Overall Response Rate (ORR).
NCT02311933 (1) [back to overview]Progression Free Survival (PFS)
NCT02384239 (7) [back to overview]Percentage of Participants With Grade 3 or 4 Neutropenia
NCT02384239 (7) [back to overview]Progression-free Survival (PFS)
NCT02384239 (7) [back to overview]Proportion of Participants With an Objective Response
NCT02384239 (7) [back to overview]Proportion of Participants With Demonstrated Clinical Benefit
NCT02384239 (7) [back to overview]Median Change in Percent Positive Cells From Baseline of Ki-67
NCT02384239 (7) [back to overview]Median Change in Percent Positive Cells From Baseline of pS780-Rb
NCT02384239 (7) [back to overview]Median Change in Percent Positive Cells From Baseline of Total-Rb
NCT02395627 (6) [back to overview]Number of Participants With Tumor Responses Calculated by Immune Related Response-Criteria (irRC)
NCT02395627 (6) [back to overview]Progression Free Survival
NCT02395627 (6) [back to overview]Duration of Response
NCT02395627 (6) [back to overview]Overall Survival (OS)
NCT02395627 (6) [back to overview]Objective Response Rate (ORR)
NCT02395627 (6) [back to overview]Number of Participants With Treatment-related Adverse Events (AE)
NCT02586675 (3) [back to overview]Overall Survival (OS) at Six Months
NCT02586675 (3) [back to overview]Progression-free Survival (PFS) at Six Months
NCT02586675 (3) [back to overview]Recommended Phase II Dose (RP2D)
NCT02630693 (3) [back to overview]Duration of Response
NCT02630693 (3) [back to overview]Overall Survival
NCT02630693 (3) [back to overview]Progression Free Survival Using the RECIST 1.1 Criteria
NCT02747004 (9) [back to overview]Change From Baseline in Pain and Symptom Burden Assessment on the Modified Brief Pain Inventory-Short Form (mBPI-sf)
NCT02747004 (9) [back to overview]Change From Baseline in Symptom Burden on the European Organization for Research and Treatment of Cancer Quality of Life Questionnaire-C30 (EORTC QLQ-C30)
NCT02747004 (9) [back to overview]PK: Mean Single Dose Concentration of Tamoxifen and Endoxifen
NCT02747004 (9) [back to overview]Pharmacokinetics (PK): Mean Single Dose Concentration of Abemaciclib and Its Metabolites
NCT02747004 (9) [back to overview]Duration of Response (DoR)
NCT02747004 (9) [back to overview]PK: Multiple Dose Concentration of Tamoxifen and Endoxifen
NCT02747004 (9) [back to overview]Pharmacokinetics (PK): Steady State Concentration of Abemaciclib and Its Metabolites
NCT02747004 (9) [back to overview]Objective Response Rate (ORR): Percentage of Participants With a Complete Response (CR) or Partial Response (PR)
NCT02747004 (9) [back to overview]Progression Free Survival (PFS)
NCT02764541 (6) [back to overview]Percentage of Participants With Clinical Response in Arm C and Arm D in the Treatment Phase
NCT02764541 (6) [back to overview]Number of Participants With RCB Response in Arm C and Arm D During the Treatment Phase
NCT02764541 (6) [back to overview]Change in RCB Index Between Arm C and Arm D During the Treatment Phase
NCT02764541 (6) [back to overview]Odds Ratio of Achieving Cell Cycle Arrest at the End of Window Phase
NCT02764541 (6) [back to overview]Pathologic Complete Response (pCR) of Patients Given Endocrine Therapy Plus Palbociclib and of Endocrine Therapy Alone During the Treatment Phase
NCT02764541 (6) [back to overview]Difference in Anti-proliferative Activity of Patients Given Letrozole Versus Tamoxifen During the Window Phase
NCT02806544 (6) [back to overview]Pathologic Complete Response
NCT02806544 (6) [back to overview]Overall Clinical Response Rate
NCT02806544 (6) [back to overview]Number of Participants With Definitive Surgery in Responders to Neoadjuvant Tamoxifen
NCT02806544 (6) [back to overview]Number of Participants Who Were Successfully Accrued in the Study, as a Measure of Feasibility
NCT02806544 (6) [back to overview]Ki67 Suppression Rate at 4-6 Weeks in Patients Who Underwent an On-treatment Biopsy
NCT02806544 (6) [back to overview]Breast Conserving Therapy
NCT02824224 (4) [back to overview]Adverse Events
NCT02824224 (4) [back to overview]Bleeding Pattern Satisfaction
NCT02824224 (4) [back to overview]IUD Satisfaction
NCT02824224 (4) [back to overview]Number of Bleeding and Spotting Days
NCT02903121 (4) [back to overview]Total Number of Consecutive Bleeding-free Days in First 30 Days From Day 1 of First Treatment (TX1)
NCT02903121 (4) [back to overview]Total Number of Bleeding Free Days Over the Second 90 Day Reference Period From Day 1 of Treatment Number 4 to Day 90
NCT02903121 (4) [back to overview]Total Number of Bleeding Free Days Over the First 90 Day Reference Period From Day 1 of Treatment 1.
NCT02903121 (4) [back to overview]Patient Satisfaction With Bleeding Pattern
NCT02979301 (1) [back to overview]Change in Background Parenchymal Uptake (BPU) on Molecular Breast Imaging (MBI)
NCT02988986 (3) [back to overview]Number of Participants Meeting Certain Preoperative Endocrine Prognostic Index (PEPI)
NCT02988986 (3) [back to overview]Number of Participants With Pathological Complete Response (pCR)
NCT02988986 (3) [back to overview]Ki67 Expression
NCT03045653 (1) [back to overview]Progression-free Survival (PFS)
NCT03199963 (6) [back to overview]Change in Serum Concentration of Sex Hormone Binding Globulin (SHBG) From Baseline to Week 52/End of Study (EOS)
NCT03199963 (6) [back to overview]Change in Serum Concentration of: Cholesterol, Triglycerides, High-density Lipoprotein (HDL), and Low-density Lipoprotein (LDL).
NCT03199963 (6) [back to overview]Number and Severity of Adverse Events (AEs)
NCT03199963 (6) [back to overview]Number of Participants With Measurable Plasma Concentrations of the E and Z Isomers of 4-OHT by Visit
NCT03199963 (6) [back to overview]Change in Serum Concentration of Select Bone Biomarkers:Type I Collagen C-Telopeptides (CTx) (pg/mL)
NCT03199963 (6) [back to overview]Change in Serum Concentration of Select Bone Biomarkers: Bone Specific Alkaline Phosphatase (BSAP) (U/L)
NCT03219476 (3) [back to overview]Change in Baseline of Cancer Cell Protein Levels of Human Epidermal Growth Factor Receptor (HER) Family Members (HER1-4) Following Neoadjuvant Endocrine Therapy.
NCT03219476 (3) [back to overview]Number of Subjects Who Achieve a Partial Radiographic Response.
NCT03219476 (3) [back to overview]Number of Subjects Who Achieve Complete Radiographic Response.
NCT03317405 (5) [back to overview]Number of Participants With Dermal Toxicity on Breast Skin at the Application Site
NCT03317405 (5) [back to overview]Change in Plasma Estrogenic and Coagulation Parameters
NCT03317405 (5) [back to overview]Change in Pre-therapy and Post-therapy Symptoms Captured by BESS Questionnaire
NCT03317405 (5) [back to overview]Drug Concentration in Plasma
NCT03317405 (5) [back to overview]Drug Concentration in Tissue
NCT03382834 (4) [back to overview]Number of Participants With HIV-1 RNA Levels (Measured by Single Copy Assay) Greater or Equal to the Lower Limit of Quantification
NCT03382834 (4) [back to overview]Change From Baseline in Total HIV-1 DNA Levels in CD4+ T Cells
NCT03382834 (4) [back to overview]Change From Baseline in Cell-associated HIV-1 RNA in CD4+ T Cells
NCT03382834 (4) [back to overview]Proportion of Participants With New Grade 3 or Greater Adverse Events
NCT04059484 (13) [back to overview]Percentage of Participants With Objective Response
NCT04059484 (13) [back to overview]Percentage of Participants With Disease Control
NCT04059484 (13) [back to overview]Change From Baseline in European Organization for Research and Treatment of Cancer Quality of Life Breast Cancer Specific Module (EORTC-QLQ-BR23) Domain Scores
NCT04059484 (13) [back to overview]Pharmacokinetics: Plasma Concentrations of Amcenestrant
NCT04059484 (13) [back to overview]Change From Baseline in European Organization for Research and Treatment of Cancer Core Quality of Life Questionnaire (EORTC-QLQ-C30) Domain Scores
NCT04059484 (13) [back to overview]Within-Participant Steady State Ctrough of Amcenestrant
NCT04059484 (13) [back to overview]Progression Free Survival (PFS)
NCT04059484 (13) [back to overview]Percentage of Participants With Clinical Benefit
NCT04059484 (13) [back to overview]Overall Survival (OS)
NCT04059484 (13) [back to overview]Duration of Response (DOR)
NCT04059484 (13) [back to overview]Progression Free Survival (PFS) According to Estrogen Receptor 1 Gene (ESR1) Mutation Status
NCT04059484 (13) [back to overview]Change From Baseline in European Quality of Life Working Group Health Status Measure 5 Dimensions (5D), 5 Levels (5L) (EQ-5D-5L) Score: Health Utility Index Value
NCT04059484 (13) [back to overview]Change From Baseline in European Quality of Life Working Group Health Status Measure 5 Dimensions (5D), 5 Levels (5L) (EQ-5D-5L) Score: Visual Analog Scale (VAS) Score
NCT04190056 (5) [back to overview]Percentage of Participants With Tumor Responses
NCT04190056 (5) [back to overview]Overall Response Rate (ORR)
NCT04190056 (5) [back to overview]Median Progression Free Survival (PFS)
NCT04190056 (5) [back to overview]Median Overall Survival (OS)
NCT04190056 (5) [back to overview]Duration of Response (DOR)
NCT04504331 (4) [back to overview]Progression-free Survival (PFS)
NCT04504331 (4) [back to overview]Number of Treatment Emergent Adverse Events (TEAE)
NCT04504331 (4) [back to overview]Number of Dose-limiting Toxicities (DLTs)
NCT04504331 (4) [back to overview]Clinical Benefit Rate
NCT05128773 (2) [back to overview]Overall Survival (OS)
NCT05128773 (2) [back to overview]Breast Cancer-specific Survival (BCSS)

Three-year Relapse-free Survival

Estimated using the product-limit method of Kaplan and Meier. Relapse defined as appearance of any new lesions during or after protocol treatment. (NCT00003042)
Timeframe: From date of mastectomy until date of relapse or death from any cause, 3 years post mastectomy.

Interventionpercentage of participants (Number)
Neoadjuvant Chemo Followed by Surgery & High-dose Chemo With PSC Rescue61.5
High-dose Chemo With Rescue77.8

[back to top]

Five-year Overall Survival

Estimated using the product-limit method of Kaplan and Meier. Endpoint is defined as death due to any cause. (NCT00003042)
Timeframe: From date of mastectomy until date of death, 5 years post mastectomy.

Interventionpercentage of participants (Number)
Neoadjuvant Chemo Followed by Surgery & High-dose Chemo With PSC Rescue69.2
High-dose Chemo With Rescue70.4

[back to top]

Overall Survival

Overall survival of patients treated for inflammatory (Stage IIIb) and responsive stage IV breast cancer with BUMELTT and PBSC support and low dose immunotherapy with IL2 and GM-CSF. (NCT00003199)
Timeframe: 11 years

InterventionParticipants (Count of Participants)
TX/Maintenance Therapy for Stage IIIB/IV Breast Cancer18

[back to top]

Number of Participants With Toxicity of a Combination of Low-dose IL-2 and GM-CSF

IL-2/GM-CSF toxicity assessed using the NCI Toxicity Criteria. Toxicity was defined as any grade 2, 3, 4 or 5 CNS (except grade 0-3 malaise and fatigue) toxicity; any grade 3, 4, or 5 non-CNS or non-hematological toxicity (except grade 0-3 bilirubin); or any grade 4 or 5 hematological toxicity. (NCT00003199)
Timeframe: 16 Weeks

InterventionParticipants (Count of Participants)
TX/Maintenance Therapy for Stage IIIB/IV Breast Cancer6

[back to top]

Event-free Survival

Event-free survival of patients treated for inflammatory (Stage IIIb) and responsive stage IV breast cancer with BUMELTT and PBSC support and low dose immunotherapy with IL2 and GM-CSF. (NCT00003199)
Timeframe: 11 years

InterventionParticipants (Count of Participants)
Stage IIIB DiseaseStage IV Disease
TX/Maintenance Therapy for Stage IIIB/IV Breast Cancer119

[back to top]

Number of Participants, e.g. Responders and Non-responders With a Percent Change in Expression Patterns After Chemotherapy With Changes in Expression Patterns After Chemotherapy in Preclinical Models

Patients were classified as responders or non-responders based on change in tumor size by clinical exam and pathologic response.For instance, patients with a pathological complete response, micro-invasive disease at surgery, or clinical complete response after four cycles of treatment were considered responders. Changes in gene expression associated with treatment was assessed before/after chemotherapy. All gene expression summary intensities below 50 were thresholded to the value of 50 and genes showing variability significantly smaller than the median gene variability were screened out. (NCT00005908)
Timeframe: 6 years

InterventionParticipants (Number)
RespondersNon-responders
Dose A & B-Cohort 1 & 2-Arm 1 & 2-Docetaxel & Capecitabine813

[back to top]

Overall Clinical Response Rate

Overall response rate is defined as the percentage of participants with a CR (complete disappearance of all target lesions), PR (a 30% decrease in the sum of the longest diameter of target lesions) determined by clinical measurements per the Response Evaluation Criteria in Solid Tumors (RECIST) and/or a complete pathologic response (disappearance of all invasive tumor pathologically or presence of ductal carcinoma in situ) per the Chevallier criteria. For details about the RECIST or Chevallier criteria see the protocol link module. (NCT00005908)
Timeframe: 6 years

InterventionPercentage of participants (Number)
Complete ResponsePartial ResponseComplete pathologic response
Dose A & B-Cohort 1 & 2-Arm 1& 2-Docetaxel & Capecitabine315910

[back to top]

Number of Participants With Adverse Events

Here is the number of participants with adverse events. For the detailed list of adverse events see the adverse event module. (NCT00005908)
Timeframe: 6 years

InterventionParticipants (Number)
Dose A-Cohort 1-Arm 1-Docetaxel & Capecitabine9
Dose B-Cohort 2-Arm 2 Reduced Dose-Docetaxel & Capecitabine20

[back to top]

Complementary Deoxyribonucleic Acid (cDNA) Expression

Patients were classified as responders or non-responders based on change in tumor size by clinical exam and pathologic response.For instance, patients with a pathological complete response, micro-invasive disease at surgery, or clinical complete response after four cycles of treatment were considered responders. Changes in gene expression associated with treatment was assessed before/after chemotherapy. All gene expression summary intensities below 50 were thresholded to the value of 50 and genes showing variability significantly smaller than the median gene variability were screened out. (NCT00005908)
Timeframe: 6 years

,
InterventionParticipants (Number)
RespondersNon-responders
Dose A-Cohort 1-Arm 1-Docetaxel & Capecitabine82
Dose B-Cohort 2-Arm 2 Reduced Dose-Docetaxel & Capecitabine713

[back to top]

Number of Participants With New Primary Non-breast Cancers

Number of participants with new primary non-breast cancers which included colorectal cancer, lung cancer, endometrial cancer, ductal carcinoma in situ (DCIS) and other primary cancer types. (NCT00036270)
Timeframe: Baseline (Month 0) up to 5 years

,
InterventionParticipants (Number)
Colorectal cancerLung cancerEndometrial cancerDCISOther primary cancer types
Exemestane432473110
Tamoxifen Followed by Exemestane3217174106

[back to top]

Disease Free Survival (DFS): Number of Events (Disease Relapse or Death) From Baseline up to 2.75 Years

Number of events (disease relapse or death) to time of observation for DFS. DFS defined as time from randomization to earliest documentation of disease relapse or death from any cause in postmenopausal, receptor positive, node negative or node positive breast cancer patients for adjuvant treatment with exemestane compared with adjuvant tamoxifen therapy at 2.75 years. Disease relapse: primary tumor recurrence (locoregional or distant) and ipsilateral or contralateral breast cancer (CBC). Intercurrent death: death without disease relapse. (NCT00036270)
Timeframe: Baseline (Month 0) up to 2.75 years

InterventionEvents (disease relapse or death) (Number)
Exemestane352
Tamoxifen Followed by Exemestane388

[back to top]

Disease Free Survival (DFS): Number of Events (Disease Relapse or Death) From Baseline up to 5 Years

Number of events (disease relapse or death) to time of observation for DFS. DFS defined as time from randomization to earliest documentation of disease relapse or death from any cause in postmenopausal, receptor positive, node negative or node positive breast cancer patients for adjuvant treatment with exemestane compared with adjuvant tamoxifen therapy at 5 years. Disease relapse: primary tumor recurrence (locoregional or distant) and ipsilateral or contralateral breast cancer (CBC). Intercurrent death: death without disease relapse. (NCT00036270)
Timeframe: Baseline (Month 0) up to 5 years

InterventionEvents (disease relapse or death) (Number)
Exemestane712
Tamoxifen Followed by Exemestane714

[back to top]

Number of Events for Overall Survival (OS)

Number of events (death) to time of observation for OS. OS is the duration from randomization to death. For participants who are alive, overall survival is censored at the last contact. (NCT00036270)
Timeframe: Baseline (Month 0) up to 5 years

InterventionEvents (death) (Number)
Exemestane485
Tamoxifen Followed by Exemestane476

[back to top]

Number of Events for Time to Relapse

Number of events to time of observation for relapse. Relapse is defined as all recurrences of the primary tumor (loco-regional and distant recurrence), second primary breast cancer, contralateral breast cancer. (NCT00036270)
Timeframe: Baseline (Month 0) up to 5 years

InterventionEvents (disease relapse) (Number)
Exemestane499
Tamoxifen Followed by Exemestane521

[back to top]

Percentage of Deoxy-pyridinoline (DPD) Urine Concentration Relative to Baseline: Bone Metabolism Sub-study

Deoxy-pyridinoline (DPD) urine concentration (adjusted for urinary creatinine) analyzed using competitive EIA at post-baseline time points was expressed as percentage of baseline DPD urine concentration. 'N' (number of participants analyzed) signifies those participants who were evaluable for this measure and 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: Baseline, 3, 6, 9, 12, 18, 24, 30 months after randomization (on-treatment), 36 months after randomization (end of treatment), 12, 24 months post-treatment

,
Interventionpercentage of baseline concentration (Geometric Mean)
3 months: on-treatment (n=82, 91)6 months: on-treatment (n=83, 95)9 months: on-treatment (n=80, 92)12 months: on-treatment (n=82, 97)18 months: on-treatment (n=77, 96)24 months: on-treatment (n=78, 90)30 months: on-treatment (n=49, 63)36 months: end of treatment (n=19, 31)12 months: post-treatment (n=65, 84)24 months: post-treatment (n=61, 77)
Exemestane130.49145.13160.12155.53139.57135.30121.39107.64117.94105.50
Tamoxifen106.99103.42101.08104.5199.2599.1195.97101.04128.47120.84

[back to top]

Percentage of C-Terminal Telopeptide (CTX) Serum Concentration Relative to Baseline: Bone Metabolism Sub-study

C-terminal telopeptide (CTX) serum concentration analyzed using competitive enzyme-linked immunosorbent assay (ELISA) at post-baseline time points was expressed as percentage of baseline CTX serum concentration. 'N' (number of participants analyzed) signifies those participants who were evaluable for this measure and 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: Baseline, 3, 6, 9, 12, 18, 24, 30 months after randomization (on-treatment), 36 months after randomization (end of treatment), 12, 24 months post-treatment

,
Interventionpercentage of baseline concentration (Geometric Mean)
3 months: on-treatment (n=81, 93)6 months: on-treatment (n=83, 95)9 months: on-treatment (n=79, 92)12 months: on-treatment (n=81, 96)18 months: on-treatment (n=80, 95)24 months: on-treatment (n=81, 90)30 months: on-treatment (n=50, 65)36 months: end of treatment (n=19, 31)12 months: post-treatment (n=67, 87)24 months: post-treatment (n=62, 77)
Exemestane144.14197.47226.04232.69199.68177.80179.29130.00110.87100.34
Tamoxifen99.1993.6794.4094.5990.3588.8091.6299.34136.50124.03

[back to top]

Percentage of Bone Specific Alkaline Phosphatase (BAP) Serum Concentration Relative to Baseline: Bone Metabolism Sub-study

Bone specific alkaline phosphatase (BAP) serum concentration analyzed using enzyme immuno assay (EIA) at post-baseline time points was expressed as percentage of baseline BAP serum concentration. 'N' (number of participants analyzed) signifies those participants who were evaluable for this measure and 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: Baseline, 3, 6, 9, 12, 18, 24, 30 months after randomization (on-treatment), 36 months after randomization (end of treatment), 12, 24 months post-treatment

,
Interventionpercentage of baseline concentration (Geometric Mean)
3 months: on-treatment (n=81, 92)6 months: on-treatment (n=83, 95)9 months: on-treatment (n=79, 92)12 months: on-treatment (n=82, 96)18 months: on-treatment (n=80, 95)24 months: on-treatment (n=81, 90)30 months: on-treatment (n=50, 65)36 months: end of treatment (n=19, 31)12 months: post-treatment (n=67, 87)24 months: post-treatment (n=62, 77)
Exemestane113.47121.01139.62148.96158.33155.89144.89150.82140.19128.73
Tamoxifen104.35104.3498.17100.47102.72105.12108.33113.87149.69142.20

[back to top]

Percent Change From Baseline in Lumbar Spine and Proximal Femur (Total Hip) Bone Mineral Density (BMD) at 6, 12, 24 Months On-treatment and 24 Months Post-treatment: Bone Metabolism Sub-study

BMD measurements for Lumbar spine (LS) and Proximal Femur (Total Hip [TH]) were performed using dual energy X-ray absorptiometry (DXA) for participants who entered the bone-metabolism sub-study. 'N' (number of participants analyzed) signifies those participants who were evaluable for this outcome measure and 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: Baseline, 6, 12, 24 months after randomization (on-treatment), 24 months post-treatment

,
Interventionpercent change (Mean)
Change at 6 months on-treatment: LS (n=84,96)Change at 6 months on-treatment: TH (n=82,96)Change at 12 months on-treatment: LS (n=82,96)Change at 12 months on-treatment: TH (n=82,95)Change at 24 months on-treatment: LS (n=82,92)Change at 24 months on-treatment: TH (n=79,93)Change at 24 months post-treatment: LS (n=74,81)Change at 24 months post-treatment: TH (n=73,84)
Exemestane-2.64-1.31-2.98-2.17-3.69-2.81-2.17-3.06
Tamoxifen-0.22-0.13-0.19-0.39-0.47-0.91-3.44-4.15

[back to top]

Percent Change From Baseline in Femoral Neck and Femoral Wards Bone Mineral Density (BMD) at 6, 12 and 24 Months On-treatment and 24 Months Post-treatment: Bone Metabolism Sub-study

BMD measurements for femoral neck (FN) and femoral wards (FW) were performed using dual energy X-ray absorptiometry (DXA) for participants who entered the bone-metabolism sub-study. 'N' (number of participants analyzed) signifies those participants who were evaluable for this outcome measure and 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: Baseline, 6, 12, 24 months after randomization (on-treatment), 24 months post-treatment

,
Interventionpercent change (Mean)
Change at 6 months on-treatment: FN (n=82,94)Change at 6 months on-treatment: FW (n=82,94)Change at 12 months on-treatment: FN (n=82,95)Change at 12 months on-treatment: FW (n=81,95)Change at 24 months on-treatment: FN (n=78,89)Change at 24 months on-treatment: FW (n=72,87)Change at 24 months post-treatment: FN (n=61,69)Change at 24 months post-treatment: FW (n=60,68)
Exemestane-1.91-2.02-2.56-3.51-4.00-4.75-4.10-6.07
Tamoxifen-0.300.32-0.32-1.30-0.78-1.86-4.95-8.60

[back to top]

Number of Participants With Polyps, Fibroids and Ovarian Cysts: Endometrial Sub-study

Number of participants with presence of polyps (POL) and fibroids (FIB) at post-baseline time points compared to the baseline (BL) status of 'yes', 'no' or 'missing' (that is, participants reporting POL/FIB at post-baseline time points who had yes, no or missing POL/FIB status at baseline, respectively) were presented. Result for number of participants with ovarian cysts was not analyzed at post-baseline time points as very few participants reported ovarian cysts at baseline. (NCT00038467)
Timeframe: 6, 12, 24, 36 months after randomization, 6, 12, 24 months post-treatment

,
Interventionparticipants (Number)
FIB: 6 months, BL Yes (n=60,50)FIB: 6 months, BL No (n=60,50)FIB: 6 months, BL Missing (n=60,50)POL: 6 months, BL Yes (n=60,50)POL: 6 months, BL No (n=60,50)POL: 6 months, BL Missing (n=60,50)FIB: 12 months, BL Yes (n=61,52)FIB: 12 months, BL No (n=61,52)FIB: 12 months, BL Missing (n=61,52)POL: 12 months, BL Yes (n=61,52)POL: 12 months, BL No (n=61,52)POL: 12 months, BL Missing (n=61,52)FIB: 24 months, BL Yes (n=61,52)FIB: 24 months, BL No (n=61,52)FIB: 24 months, BL Missing (n=61,52)POL: 24 months, BL Yes (n=61,52)POL: 24 months, BL No (n=61,52)POL: 24 months, BL Missing (n=61,52)FIB: 36 months, BL Yes (n=33,18)FIB: 36 months, BL No (n=33,18)FIB: 36 months, BL Missing (n=33,18)POL: 36 months, BL Yes (n=33,18)POL: 36 months, BL No (n=33,18)POL: 36 months, BL Missing (n=33,18)FIB: 6 months post-treatment, BL Yes (n=16,17)FIB: 6 months post-treatment, BL No (n=16,17)FIB: 6 months post-treatment,BL Missing(n=16,17)POL: 6 months post-treatment, BL Yes (n=16,17)POL: 6 months post-treatment, BL No (n=16,17)POL: 6 months post-treatment,BL Missing(n=16,17)FIB: 12 months post-treatment, BL Yes (n=51,38)FIB: 12 months post-treatment, BL No (n=51,38)FIB: 12 months post-treatment, BL Missing(n=51,38)POL: 12 months post-treatment, BL Yes (n=51,38)POL: 12 months post-treatment, BL No (n=51,38)POL: 12 months post-treatment, BL Missing (n=51,38FIB: 24 months post-treatment, BL Yes (n=43,31)FIB: 24 months post-treatment, BL No (n=43,31)FIB: 24 months post-treatment, BL Missing(n=43,31)POL: 24 months post-treatment, BL Yes (n=43,31)POL: 24 months post-treatment, BL No (n=43,31)POL: 24 months post-treatment, BL Missing(n=43,31)
Exemestane422021324001330100230010110001121000221012
Tamoxifen610000711000502010100000002000101002212001

[back to top]

Endometrial Thickness: Endometrial Sub-study

Endometrial thickness was assessed using transvaginal ultrasound examination. 'N' (number of participants analyzed) signifies those participants who were evaluable for this outcome and 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: Baseline, 6, 12, 24, 36 months after randomization, 6, 12, 24 months post-treatment

,
Interventionmm (Median)
Baseline (n=60, 52)6 months (n=58, 49)12 months (n=59, 52)24 months (n=60, 52)36 months (n=31, 17)6 months post-treatment (n=16, 17)12 months post-treatment (n=49, 37)24 months post-treatment (n=40, 31)
Exemestane6.04.03.34.03.03.03.03.0
Tamoxifen6.05.95.55.07.05.84.03.8

[back to top]

Change From Baseline in Relationship With Doctor (RWD) Subscale Score at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Substudy

The RWD subscale assessed relationship with doctor in participants with breast cancer. RWD subscale comprised of 2 items (confidence in doctors, doctor answered questions). Participants indicated how true a statement had been for them using a 5-point scale from 0 (not at all) to 4 (very much). Total RWD score was calculated as the sum of the 2 items and ranged from 0 to 8, where higher score indicated better relationship with doctor. 'N' (number of participants analyzed) signifies those participants who were evaluable for this measure and 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: Baseline, 3, 6, 9, 12, 18, 24, 30, 36, 48, 60 months after randomization

,
Interventionunits on a scale (Mean)
Change at 3 months (n=254, 250)Change at 6 months (n=244, 240)Change at 9 months (n=243, 235)Change at 12 months (n=233, 233)Change at 18 months (n=233, 222)Change at 24 months (n=221, 213)
Exemestane0.07-0.02-0.06-0.01-0.03-0.005
Tamoxifen0.08-0.04-0.07-0.07-0.21-0.12

[back to top]

Change From Baseline in Social/Family Well-Being (SWB) Sub-scale Score at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Sub-study

The SWB subscale assessed social/family well-being related QoL in participants with breast cancer. SWB subscale comprised of 7 items (distant from friends, emotional support, support from friends, family acceptance, family communication, close to main support, sexual satisfaction). Participants indicated how true a statement had been for them using a 5-point scale from 0 (not at all) to 4 (very much). For items that were negatively framed, the scores were reversed for the analysis so that higher scores equated to a good QoL. Total SWB score was calculated as the sum of all the 7 items and ranged from 0 to 28, where higher score indicated better social/family well-being related QoL. 'N' (number of participants analyzed) signifies those participants who were evaluable for this measure and 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: Baseline, 3, 6, 9, 12, 18, 24, 30, 36, 48, 60 months after randomization

,
Interventionunits on a scale (Mean)
Change at 3 months (n=252, 249)Change at 6 months (n=245, 241)Change at 9 months (n=242, 235)Change at 12 months (n=231, 235)Change at 18 months(n=234, 226)Change at 24 months (n=219, 212)
Exemestane-0.25-0.43-0.580.05-0.5-0.99
Tamoxifen-0.37-0.47-0.53-0.56-0.69-0.72

[back to top]

Change From Baseline in Total Functional Assessment of Cancer Therapy - General Breast and Endocrine (FACT-GBE) Score at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Sub-study

FACT-GBE assessed health-related quality of life (QoL) in participants with breast cancer. It consisted of 56 items,summarized to 7 subscales(subscale 1 to 6 constituted total FACT-B and subscale 7 constituted total ES):physical well-being(7 items), social/family well-being(7 items),relationship with doctor (2 items),emotional well-being(6 items),functional well-being(7 items),breast cancer subscale(9 items),endocrine symptoms(18 items). Participants indicated how true a statement had been for them using 5-point scale from 0(not at all) to 4(very much). For items that were negatively framed,scores were reversed for analysis so that higher scores equated to good QoL. Total FACT-GBE score=sum of all 56 items(range 0 to 224, where higher score indicated better QoL. 'N' (number of participants analyzed) signifies those participants who were evaluable for this measure and 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: Baseline, 3, 6, 9, 12, 18, 24, 30, 36, 48, 60 months after randomization

,
Interventionunits on a scale (Mean)
Change at 3 months (n=252, 252)Change at 6 months (n=244, 243)Change at 9 months (n=243, 236)Change at 12 months (n=229, 236)Change at 18 months (n=232, 225)Change at 24 months (n=220, 212)
Exemestane-0.91-3.12-1.280.38-0.67-1.48
Tamoxifen-0.38-0.04-0.38-0.530.061.43

[back to top]

Change From Baseline in Physical Well-Being (PWB) Subscale Score at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Sub-study

The PWB subscale assessed physical well-being related QoL in participants with breast cancer. PWB subscale comprised of 7 items (energy lack, nausea, family needs, pain, side effects, felt ill, forced to stay in bed). Participants indicated how true a statement had been for them using a 5-point scale from 0 (not at all) to 4 (very much). For items that were negatively framed, the scores were reversed for the analysis so that higher scores equated to a good QoL. Total PWB score was calculated as the sum of all the 7 items and ranged from 0 to 28, where higher score indicated better physical well-being related QoL. 'N' (number of participants analyzed) signifies those participants who were evaluable for this measure and 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: Baseline, 3, 6, 9, 12, 18, 24, 30, 36, 48, 60 months after randomization

,
Interventionunits on a scale (Mean)
Change at 3 months (n=253, 252)Change at 6 months(n=246, 244)Change at 9 months (n=242, 237)Change at 12 months (n=233, 238)Change at 18 months(n=234, 228)Change at 24 months (n=223, 214)
Exemestane-0.32-1.08-0.37-0.26-0.19-0.005
Tamoxifen-0.020.130.06-0.120.020.22

[back to top]

Change From Baseline in Lumbar Spine and Proximal Femur (Total Hip) Bone Mineral Density (BMD) T-scores at 6, 12 and 24 Months On-treatment and 24 Months Post-treatment: Bone Metabolism Sub-study

BMD measurements for Lumbar spine (LS) and Proximal Femur (Total Hip [TH]) were performed using dual energy X-ray absorptiometry (DXA) for participants who entered the bone-metabolism sub-study. Results were scored as T-score. T-score indicated how many standard deviations higher or lower participant's value was when compared to the young normal reference mean. Using the World Health Organization (WHO) criteria for osteoporosis, a T-score of greater than or equal to (>=)-1.0 was classified as normal, a T-score of greater than -2.5 to less than -1.0 as osteopenic, and a T-score less than or equal to (<=)-2.5 as osteoporotic. Here 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: Baseline, 6, 12, 24 months after randomization (on-treatment), 24 months post-treatment

,
InterventionT-score (Mean)
Baseline: LS (n=86,99)Baseline: TH (n=86,99)Change at 6 months on-treatment: LS (n=84,96)Change at 6 months on-treatment: TH (n=82,96)Change at 12 months on-treatment: LS (n=82,96)Change at 12 months on-treatment: TH (n=82,95)Change at 24 months on-treatment: LS (n=82,92)Change at 24 months on-treatment: TH (n=79,93)Change at 24 months post-treatment: LS (n=74,81)Change at 24 months post-treatment: TH (n=73,84)
Exemestane-0.62-0.27-0.24-0.10-0.26-0.16-0.32-0.21-0.21-0.25
Tamoxifen-0.45-0.12-0.02-0.00-0.02-0.03-0.04-0.07-0.33-0.34

[back to top]

Change From Baseline in Functional Well-Being (FWB) Sub-scale Score at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Sub-study

The FWB subscale assessed functional well-being related QoL in participants with breast cancer. FWB subscale comprised of 7 items (able to work, work fulfilled, able to enjoy life, acceptance of illness, sleeping well, enjoyed normal fun activities, contented with QoL). Participants indicated how true a statement had been for them using a 5-point scale from 0 (not at all) to 4 (very much). Total FWB score was calculated as the sum of the 7 items and ranged from 0 to 28, where higher score indicated better functional well-being related QoL. 'N' (number of participants analyzed) signifies those participants who were evaluable for this measure and 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: Baseline, 3, 6, 9, 12, 18, 24, 30, 36, 48, 60 months after randomization

,
Interventionunits on a scale (Mean)
Change at 3 months (n=254, 253)Change at 6 months (n=246, 244)Change at 9 months (n=243, 238)Change at 12 months (n=232, 238)Change at 18 months (n=232, 227)Change at 24 months (n=222, 214)
Exemestane-0.32-0.77-1.03-0.68-0.83-0.91
Tamoxifen-0.18-0.43-0.38-0.91-0.8-0.45

[back to top]

Change From Baseline in Functional Assessment of Cancer Therapy - Endocrine Subscale (FACT-ES) Total Score at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Sub-study

The FACT-ES assessed health-related QoL in participants with breast cancer. ES subscale comprised of 18 items (hot flushes,cold sweats,night sweats, vaginal discharge,vaginal irritation,vaginal bleeding,vaginal dryness,discomfort with intercourse,lost interest in sex,gained weight,light headed/dizzy,vomiting,had diarrhea,headaches,felt bloated,breast tenderness,mood swings, felt irritable).Participants indicated how true a statement was for them using a 5-point scale from 0 (not at all) to 4 (very much). For items that were negatively framed, the scores were reversed for the analysis so that higher scores equated to a good QoL. Total FACT-ES score was calculated as sum of all the 18 items and ranged from 0 to 72, where higher score indicated better QoL. 'N' (number of participants analyzed) signifies those participants who were evaluable for this measure and 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: Baseline, 3, 6, 9, 12, 18, 24, 30, 36, 48, 60 months after randomization

,
Interventionunits on a scale (Mean)
Change at 3 months (n=254, 253)Change at 6 months (n=245, 243)Change at 9 months (n=243, 238)Change at 12 months (n=233, 236)Change at 18 months (n=235, 226)Change at 24 months (n=222, 214)
Exemestane0.040.171.101.981.251.93
Tamoxifen0.700.961.321.151.411.51

[back to top]

Number of Participants With Severe Endocrine Symptoms: QoL Sub-study

"Participants indicated prevalence of an endocrine subscale items using a 5-point scale, where 0 (not at all), 1 (a little bit), 2 (somewhat), 3 (quite a bit), 4 (very much). Endocrine items were grouped in five categories vasomotor (hot flushes, cold sweats, night sweats, sleeping difficulties), neuropsychological (lack of energy, nervous feeling, lightheaded/dizzy, headaches, mood swings, feeling irritable), gastrointestinal symptoms (nausea, gained weight, vomiting, diarrhea, bloated feeling), gynecological symptoms (vaginal discharge, vaginal irritation, vaginal bleeding, vaginal dryness, discomfort with intercourse, lost interest in sex, breast tenderness) and other symptoms (pain, feeling ill, side effects). Number of participants who reported severe endocrine symptoms (defined as response categories quite a bit and very much) were presented." (NCT00038467)
Timeframe: Baseline up to 24 months after randomization

,
Interventionparticipants (Number)
Hot flushesCold sweatsNight sweatsSleeping difficultiesLack of energyNervous feelingLightheaded/dizzyHeadachesMood swingsFeeling irritableNauseaGained weightVomitingDiarrheaBloated feelingVaginal dischargeVaginal irritationVaginal bleedingVaginal drynessDiscomfort with intercourseLost interest in sexBreast tendernessPainFeeling illSide effects
Exemestane1516011511011568345670531615062075363710784712866662454
Tamoxifen1465211711010865374966481415262188554511884514276602457

[back to top]

Change From Baseline in Emotional Well-Being (EWB) Subscale Score at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Sub-study

The EWB subscale assessed emotional well-being related QoL in participants with breast cancer. EWB subscale comprised of 6 items (felt sad, proud of coping, lost hope, felt nervous, worried about dying, worried about condition worsening). Participants indicated how true a statement had been for them using a 5-point scale from 0 (not at all) to 4 (very much). For items that were negatively framed, the scores were reversed for the analysis so that higher scores equate to a good QoL. Total EWB score was calculated as the sum of the 6 items and ranged from 0 to 24, where higher score indicated better emotional well-being related QoL. 'N' (number of participants analyzed) signifies those participants who were evaluable for this measure and 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: Baseline, 3, 6, 9, 12, 18, 24, 30, 36, 48, 60 months after randomization

,
Interventionunits on a scale (Mean)
Change at 3 months (n=255, 252)Change at 6 months (n=246, 243)Change at 9 months (n=243, 236)Change at 12 months (n=232, 235)Change at 18 months (n=235, 226)Change at 24 months (n=222, 214)
Exemestane0.06-0.32-0.47-0.03-0.3-0.18
Tamoxifen-0.01-0.1-0.27-0.33-0.040.07

[back to top]

Change From Baseline in Breast Cancer Subscale (BCS) Score at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Sub-study

The BCS subscale assessed health related QoL in participants with breast cancer. BCS subscale comprised of 9 items (short of breath, self-conscious dress, tender/swollen arms, sexually attractive, bothered by hair loss, worried about familial risk, worried about family stress, bothered by weight change, able to feel like a woman). Participants indicated how true a statement had been for them using a 5-point scale from 0 (not at all) to 4 (very much). For items that were negatively framed, the scores were reversed for the analysis so that higher scores equated to a good QoL. Total BCS score was calculated as the sum of the 9 items and ranged from 0 to 36, where higher score indicated better QoL. 'N' (number of participants analyzed) signifies those participants who were evaluable for this measure and 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: Baseline, 3, 6, 9, 12, 18, 24, 30, 36, 48, 60 months after randomization

,
Interventionunits on a scale (Mean)
Change at 3 months (n=255, 252)Change at 6 months (n=246, 244)Change at 9 months (n=243, 239)Change at 12 months (n=233, 238)Change at 18 months (n=233, 227)Change at 24 months (n=222, 214)
Exemestane0.05-0.330.30.610.060.36
Tamoxifen-0.0030.170.480.380.670.72

[back to top]

Percentage of Participants With at Least 1 Gynecological Symptoms: Endometrial Sub-study

Gynecological symptoms included bleeding/spotting, pelvic pain, leucorrhoea and vaginal itching. (NCT00038467)
Timeframe: Baseline up to 24 months post-treatment

Interventionpercentage of participants (Number)
Exemestane16.28
Tamoxifen21.28

[back to top]

Overall Survival (OS) at Month 36 Post-Randomization: Main Study

OS was defined as the duration from randomization to death (due to any cause). OS at Month 36 post-randomization was defined as probability of participants' survival at 36 months after the randomization. For participants who were alive, OS was censored at the last available assessment. Probability of OS at Month 36 post-randomization was reported using Kaplan-Meier estimates at Month 36 post-randomization based on 120-month follow-up data. (NCT00038467)
Timeframe: Baseline up to Month 120

Interventionprobability of OS (Number)
Exemestane0.953
Tamoxifen0.941

[back to top]

Number of Participants With Fracture: Bone Metabolism Sub-study

(NCT00038467)
Timeframe: Baseline up to 24 months post-treatment

Interventionparticipants (Number)
Exemestane7
Tamoxifen10

[back to top]

Number of Events of Second Breast Cancer in Contralateral Breast: Main Study

Number of events of second primary breast cancer in contralateral breast (excluding ductal carcinoma in situ) were reported. (NCT00038467)
Timeframe: Baseline up to Month 120

Interventionevents (Number)
Exemestane57
Tamoxifen75

[back to top]

Change From Baseline in Treatment Outcome Index (TOI) at 3, 6, 9, 12, 18, 24, 30, 36, 48 and 60 Months: QoL Sub-study

The TOI was defined as the sum of 23 items based on following Functional Assessment of Cancer Therapy - Breast version [FACT-B] subscales: Physical well-being (7 items), Functional well-being (7 items), Breast cancer subscale (9 items). Each item was scaled from 0='Not at all' to 4='Very much'. Total TOI score ranged from 0 to 92, where higher TOI score indicated better health-related quality of life (QoL). A change of five points in the TOI scores was considered clinically meaningful. 'N' (number of participants analyzed) signifies those participants who were evaluable for this measure and 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. Results for 30, 36, 48, 60 months were not reported because data for these time points was only summarized as graphical presentation. (NCT00038467)
Timeframe: Baseline, 3, 6, 9, 12, 18, 24, 30, 36, 48, 60 months after randomization

,
Interventionunits on a scale (Mean)
Change at 3 months (n=251, 251)Change at 6 months (n=244, 243)Change at 9 months (n=242, 235)Change at 12 months (n=230, 238)Change at 18 months (n=232, 227)Change at 24 months (n=221, 213)
Exemestane-0.61-2.10-1.18-0.40-0.95-0.57
Tamoxifen-0.16-0.010.17-0.66-0.110.54

[back to top]

Disease-Free Survival (DFS) at Month 36 Post-Randomization: Main Study

DFS defined as time from randomization to earliest documentation of breast cancer relapse or death from any cause. DFS at Month 36 post-randomization was defined as probability of participants alive and disease-free at 36 months after the randomization. Participants withdrawn from the study for any reason in the absence of relapse were censored at the date they were last seen. Relapse was categorized as follows: loco-regional: ipsilateral breast or axillary nodal relapse; distant: distant relapse, including supraclavicular nodes; second primary breast cancer: contralateral breast cancer, excluding ductal carcinoma in situ. (NCT00038467)
Timeframe: Baseline up to Month 36

Interventionprobability of DFS (Number)
Exemestane0.90
Tamoxifen0.86

[back to top]

Uterine and Overall Ovary Volume: Endometrial Sub-study

Uterine volume (UV) and ovarian volume was estimated using ultrasonography. Uterine volume = (longitudinal diameter * transverse diameter * anteroposterior diameter of uterus)/(2*1000). Ovary volume = [(longitudinal diameter * transverse diameter * anteroposterior diameter of ovary) * 3.14]/(6*1000). Overall ovary volume (OV) is calculated as the sum of the right and left ovary volume. 'N' (number of participants analyzed) signifies those participants who were evaluable for this outcome and 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: 6, 12, 24, 36 months after randomization, 6, 12, 24 months post-treatment

,
Interventioncubic centimeter (cm^3) (Median)
UV: 6 months (n=57, 47)OV: 6 months (n=8, 6)UV: 12 months (n=56, 49)OV: 12 months (n=6, 5)UV: 24 months (n=54, 51)OV: 24 months (n=5, 6)UV: 36 months (n=30, 18)OV: 36 months (n=3, 2)UV: 6 months post-treatment (n=14, 16)OV: 6 months post-treatment (n=2, 4)UV: 12 months post-treatment (n=42, 35)OV: 12 months post-treatment (n=5, 4)UV: 24 months post-treatment (n=38, 28)OV: 24 months post-treatment (n=4, 4)
Exemestane25.21.823.32.326.32.021.51.525.610.121.72.822.61.6
Tamoxifen36.51.239.22.240.32.736.82.531.64.730.02.927.83.4

[back to top]

Percentage of Participants With Endometrial Thickness Greater Than or Equal to (>=) 5 Millimeter (mm): Endometrial Sub-study

Endometrial thickness was assessed using transvaginal ultrasound examination. 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: 6, 12, 24, 36 months after randomization, 6, 12, 24 months post-treatment

,
Interventionpercentage of participants (Number)
6 months (n=58, 49)12 months (n=60, 52)24 months (n=61, 52)36 months (n=32, 17)6 months post-treatment (n=16, 17)12 months post-treatment (n=50, 37)24 months post-treatment (n=41, 31)
Exemestane46.630.036.121.931.330.034.1
Tamoxifen69.455.863.576.570.632.429.0

[back to top]

Percentage of Osteocalcin (OC) and Procollagen T1 C-Peptide (PICP) Serum Concentration Relative to Baseline: Bone Metabolism Sub-study

Osteocalcin (OC) serum concentration analyzed using ELISA and procollagen T1 c-peptide (PICP) serum concentration analyzed using sandwich EIA at post-baseline time points was expressed as percentage of baseline OC serum concentration and baseline PICP serum concentration, respectively. 'N' (number of participants analyzed) signifies those participants who were evaluable for this measure and 'n' signifies those participants who were evaluable for this measure at given time points, for each group respectively. (NCT00038467)
Timeframe: Baseline, 3, 6, 9, 12, 18, 24, 30 months after randomization (on-treatment), 36 months after randomization (end of treatment), 12, 24 months post-treatment

,
Interventionpercentage of baseline concentration (Geometric Mean)
3 months, on-treatment: OC (n=81, 92)3 months, on-treatment: PICP (n=81, 92)6 months, on-treatment: OC (n=83, 95)6 months, on-treatment: PICP (n=83, 95)9 months, on-treatment: OC (n=79, 93)9 months, on-treatment: PICP (n=79, 92)12 months, on-treatment: OC (n=82, 96)12 months, on-treatment: PICP (n=82, 96)18 months, on-treatment: OC (n=80, 95)18 months, on-treatment: PICP (n=80, 95)24 months, on-treatment: OC (n=81, 90)24 months: on-treatment: PICP (n=81, 90)30 months, on-treatment: OC (n=50, 65)30 months, on-treatment: PICP (n=50, 65)36 months, end of treatment: OC (n=19, 30)36 months, end of treatment: PICP (n=19, 31)12 months, post-treatment: OC (n=67, 87)12 months, post-treatment: PICP (n=67, 87)24 months, post-treatment: OC (n=62, 77)24 months, post-treatment: PICP (n=62, 77)
Exemestane149.49117.23193.44133.50230.41131.73227.59128.68230.72125.40190.18123.75187.23113.76167.0395.33143.8591.53130.7890.46
Tamoxifen101.02102.1997.6999.7892.5296.5295.75100.1893.98103.2589.29103.9487.34103.3690.7787.22152.32108.67146.36100.74

[back to top]

Percentage of N-telopeptide of Type 1 Collagen (NTX) Urine Concentration Relative to Baseline: Bone Metabolism Sub-study

N-telopeptide of Type 1 collagen (NTX) urine concentration (adjusted for urinary creatinine) analyzed using competitive inhibition EIA at post-baseline time points was expressed as percentage of baseline NTX urine concentration. 'N' (number of participants analyzed) signifies those participants who were evaluable for this measure and 'n' signifies those participants who were evaluable for this measure at given time points for each group, respectively. (NCT00038467)
Timeframe: Baseline, 3, 6, 9, 12, 18, 24, 30 months after randomization (on-treatment), 36 months after randomization (end of treatment), 12, 24 months post-treatment

,
Interventionpercentage of baseline concentration (Geometric Mean)
3 months: on-treatment (n=82, 91)6 months: on-treatment (n=83, 95)9 months: on-treatment (n=80, 92)12 months: on-treatment (n=82, 97)18 months: on-treatment (n=77, 96)24 months: on-treatment (n=78, 90)30 months: on-treatment (n=49, 63)36 months: end of treatment (n=19, 31)12 months: post-treatment (n=65, 84)24 months: post-treatment (n=61, 77)
Exemestane128.35153.67168.15177.58171.46167.87168.52152.13121.00108.18
Tamoxifen101.92100.64101.44104.4298.74104.5596.51105.58158.12143.98

[back to top]

Median Progression-free Survival

(NCT00041080)
Timeframe: from enrollment onto the study until first disease progression or death due to any cause

Interventionmonths (Median)
Grp - 13.2
Grp - 24.5

[back to top]

Percentage of Patients Alive and Disease-free

Percentage of patients free from a disease-free survival event where events include any recurrence, second primary cancer, and death from any cause. Lobular carcinoma in situ (LCIS), basal cell or squamous cell carcinoma of the skin, carcinoma in situ of the colon, melanoma in situ, and cervical carcinoma in situ will not be included as recurrences or second primary cancer. (NCT00053898)
Timeframe: 10 years

Interventionpercentage of participants event-free (Number)
Group 1: Tamoxifen + Anastrozole Placebo77.9
Group 2: Anastrozole + Tamoxifen Placebo82.7

[back to top]

Percentage of Patients Free From Breast Cancer

Percentage of patients free from breast cancer event at 10 years where events include local, regional, or distant recurrence or contralateral breast cancer, invasive or DCIS. (NCT00053898)
Timeframe: 10 years

Interventionpercentage of participants event-free (Number)
Group 1: Tamoxifen + Anastrozole Placebo89.1
Group 2: Anastrozole + Tamoxifen Placebo93.1

[back to top]

Percentage of Patients Free From Contralateral Breast Cancer

Percentage of patients free from a breast cancer recurrence in the contralateral breast (invasive and DCIS), occurring as a first cancer event. (NCT00053898)
Timeframe: 10 years

Interventionpercentage of participants event-free (Number)
Group 1: Tamoxifen + Anastrozole Placebo94.7
Group 2: Anastrozole + Tamoxifen Placebo97.0

[back to top]

Percentage of Patients Free From Invasive Breast Cancer

Percentage of patients free from an invasive breast cancer event where events include invasive local, regional, or distant recurrence, or contralateral breast cancer, occurring as a first cancer event. Note that this endpoint includes only invasive breast cancers and the primary endpoint includes both invasive and DCIS breast cancers. (NCT00053898)
Timeframe: 10 years

Interventionpercentage of participants event-free (Number)
Group 1: Tamoxifen + Anastrozole Placebo93.3
Group 2: Anastrozole + Tamoxifen Placebo96.4

[back to top]

Percentage of Patients Free From Ipsilateral Recurrence

Percentage of patients free from a breast cancer recurrence in the ipsilateral breast (invasive and DCIS), occurring as a first cancer event. (NCT00053898)
Timeframe: 10 years

Interventionpercentage of participants event-free (Number)
Group 1: Tamoxifen + Anastrozole Placebo94.6
Group 2: Anastrozole + Tamoxifen Placebo96.4

[back to top]

Percentage of Patients Free From Non-breast Secondary Cancer

Percentage of patients free from any non-breast second primary cancer other than squamous or basal cell carcinoma of the skin, carcinoma in situ of the colon, melanoma in situ, or carcinoma in situ of the cervix, occurring as a first cancer event. (NCT00053898)
Timeframe: 10 years

Interventionpercentage of participants event-free (Number)
Group 1: Tamoxifen + Anastrozole Placebo91.5
Group 2: Anastrozole + Tamoxifen Placebo91.9

[back to top]

Percentage of Patients Free From Osteoporotic Fractures

Percentage of patients free from fractures of the hip, spine, and wrist. (NCT00053898)
Timeframe: 10 years

Interventionpercentage of participants event-free (Number)
Group 1: Tamoxifen + Anastrozole Placebo96.0
Group 2: Anastrozole + Tamoxifen Placebo95.3

[back to top]

Quality of Life-Short Form 12 (SF-12) Physical Health Component Score

The primary outcome of the QOL substudy was the Medical Outcomes Study-Short Form 12 (SF-12) physical health component scale score. The SF-12 physical score was calculated to have a range of 0-100 and was normalized to have a mean of 50 and a standard deviation of 10 in the general population. Higher scores indicate better health. (NCT00053898)
Timeframe: 5 years

Interventionunits on a scale (Mean)
Group 1: Tamoxifen + Anastrozole Placebo46.20
Group 2: Anastrozole + Tamoxifen Placebo45.38

[back to top]

Quality-adjusted Survival Time

The mean quality-adjusted survival time (in months) in each treatment group, estimated by the Quality-Adjusted Time without Symptoms and Toxicity (Q-TWIST) method. (NCT00053898)
Timeframe: 10 years

Interventionmonths (Mean)
Group 1: Tamoxifen + Anastrozole Placebo104.4
Group 2: Anastrozole + Tamoxifen Placebo102.9

[back to top]

Percentage of Patients Alive (Overall Survival)

Percentage of patients alive. (NCT00053898)
Timeframe: 10 years

Interventionpercentage of participants event-free (Number)
Group 1: Tamoxifen + Anastrozole Placebo92.1
Group 2: Anastrozole + Tamoxifen Placebo92.5

[back to top]

Overall Survival

Estimated percentage of patients alive at 8 years from randomization, where overall survival is defined as the time from randomization to death from any cause; or censored at date last known alive. (NCT00066690)
Timeframe: 8-year estimates, reported at a median follow-up of 8 years

Interventionpercentage of participants (Number)
Tamoxifen91.5
T+OFS93.3
E+OFS92.1

[back to top]

Breast Cancer-free Interval

Estimated percentage of patients alive and disease-free at 5 years from randomization, where breast cancer-free interval is defined as the time from randomization to invasive breast cancer recurrence at local, regional, or distant site, or invasive contralateral breast cancer; or censored at date of last follow up. (NCT00066690)
Timeframe: 5-year estimates, reported at a median follow-up of 67 months.

Interventionpercentage of participants (Number)
Tamoxifen86.4
T+OFS88.4
E+OFS90.9

[back to top]

Disease-free Survival

Estimated percentage of patients alive and disease-free at 5 years from randomization, where disease-free survival is defined as the time from randomization to the first appearance of one of the following: invasive breast cancer recurrence at local, regional, or distant site, invasive contralateral breast cancer, second (non-breast) invasive cancer, or death without cancer event; or censored at date of last follow-up. (NCT00066690)
Timeframe: 5-year estimates, reported at a median follow-up of 67 months.

Interventionpercentage of participants (Number)
Tamoxifen84.7
T+OFS86.6
E+OFS89

[back to top]

Distant Recurrence-free Interval

Estimated percentage of patients alive and disease-free at 5 years from randomization, where distant recurrence-free Interval is defined as the time from randomization to invasive breast cancer recurrence at distant site, or invasive contralateral breast cancer; or censored at date of last follow up. (NCT00066690)
Timeframe: 5-year estimates, reported at a median follow-up of 67 months.

Interventionpercentage of participants (Number)
Tamoxifen90.7
T+OFS91.3
E+OFS93.0

[back to top]

Overall Survival

Estimated percentage of patients alive at 8 years from randomization, where overall survival is defined as the time from randomization to death from any cause; or censored at date last known alive. (NCT00066703)
Timeframe: 8-year estimates, reported at a median follow-up of 9 years

Interventionpercentage of participants (Number)
T+OFS93.3
E+OFS93.4

[back to top]

Distant Recurrence-free Interval

Estimated percentage of patients alive and disease-free at 5 years from randomization, where distant recurrence-free interval is defined as the time from randomization to breast cancer recurrence at a distant site; or censored at date of last follow-up (NCT00066703)
Timeframe: 5-year estimates reported at a median follow-up of 72 months

Interventionpercentage of participants (Number)
T+OFS92.0
E+OFS93.8

[back to top]

Disease-free Survival

Estimated percentage of patients alive and disease-free at 5 years from randomization, where disease-free survival is defined as the time from randomization to the first appearance of one of the following: invasive breast cancer recurrence at local, regional, or distant site, invasive contralateral breast cancer, second (non-breast) invasive cancer, or death without cancer event; or censored at date of last follow up. (NCT00066703)
Timeframe: 5-year estimate reported at a median follow-up of 72 months

Interventionpercentage of participants (Number)
T+OFS87.3
E+OFS91.1

[back to top]

Breast Cancer-free Interval

Estimated percentage of patients alive and disease-free at 5 years from randomization, where breast cancer-free interval is defined as the time from randomization to the invasive breast cancer recurrence at local, regional, or distant site, or invasive contralateral breast cancer; or censored at date of last follow up. (NCT00066703)
Timeframe: 5-year estimate reported at a median follow-up of 72 months

Interventionpercentage of participants (Number)
T+OFS88.8
E+OFS92.8

[back to top]

Percentage of Patients With Tumor Response From Imaging

Percentage of patients with a tumor response where tumor response is assessed according to Response Evaluation Criteria in Solid Tumors (RECIST) (NCT00068419)
Timeframe: Baseline up to 5 years

InterventionPercentage of participants (Number)
Treatment (Enzyme Inhibitor Therapy, Anti-estrogen Therapy)8.0

[back to top]

Percentage of Patients Failure Free at 2 Years Following Study Entry

Kaplan Meier estimate of failure free survival at 2 years, where failure free survival is defined as the time to relapse, progression, second malignancy, and death whichever occurs first. (NCT00068419)
Timeframe: Up to 2 years

Interventionpercentage of participants (Number)
Treatment (Enzyme Inhibitor Therapy, Anti-estrogen Therapy)36

[back to top]

Percentage of Patients Experiencing a Grade 3 or Higher Adverse Event During Therapy.

The percentage of patients experiencing a grade 3 or higher adverse event as assessed by the National Cancer Institute Common Toxicity Terminology for Adverse Events v3.0 (NCT00068419)
Timeframe: Up to 12 months

InterventionPercentage of participants (Number)
Treatment (Enzyme Inhibitor Therapy, Anti-estrogen Therapy)3.4

[back to top]

Number of Participants With Adverse Events

Here is the number of participants with adverse events. For a detailed list of adverse events, see the adverse event module. (NCT00108069)
Timeframe: 7.5 years

InterventionParticipants (Number)
GBM (Glioblastoma Multiforme)30
AG (Anaplastic Glioma)12

[back to top]

Adverse Event Grades

The combined serious and non-serious adverse event Table describes count of patients whose highest grade adverse event for any CTC (common terminology criteria) term was related to study drugs for the GBM (Glioblastoma multiforme) and AG (Anaplastic glioma) cohorts. (NCT00108069)
Timeframe: 7.5 years

,,,,,
Interventionparticipants (Number)
thrombocytopenialymphopeniahypophosphatemiaALT/sGPTanemia (Decreased Hgb)hyponatremiaheadacheleukopeniaAST/sGOTdyspneafatiguefeverhyperkalemiacoughdepression (mood alteration)diarrheadizzinessvenous thrombosisedemahyperbilirubinemiahypermagnesemiahypocalcemiahypokalemiahypotensionelevated creatinineinfection with unknown ANCneutropeniapainrashhemorrhage (rectal)somnolenceurinary frequency
Grade 1194066401212121001011111110001101
Grade 234610022000100110000000000110000
Grade 314300110010000000100000001000010
Grade 410000000000000000000000000000000
Grade 500000000000000000000000000000000
Total2412976533222221111111111111111111

[back to top]

Response, Defined as Stable Disease or Objective (Partial or Complete) Response.

Complete response (CR) is complete disappearance of all measurable and evaluable disease. No new lesions. No evidence of non-evaluable disease. All measurable, evaluable and non-evaluable lesions and site must be assessed using the same techniques as baseline. Patients who respond must be on the same or decreasing doses of dexamethasone. Partial response (PR) is greater than or equal to a 50% decrease compared to baseline in the sum of products of perpendicular diameters of all measurable disease. No new lesions. All measurable and evaluable lesions and sites must be assessed using same techniques as baseline. Responders must be on the same decreasing doses of dexamethasone. Stable disease (SD) does not qualify for CR, PR, or progression (e.g., a 25% increase in the sum of products of all measurable lesions). The designation of stable/no response requires a minimum of 6 weeks duration. All measurable and evaluable sites must be assessed using the same techniques as baseline. (NCT00108069)
Timeframe: Patients were followed for an average of six weeks for assessment of response

,
InterventionParticipants (Number)
Complete responsePartial responseStable diseaseProgressive disease
AG (Anaplastic Glioma)00012
GBM (Glioblastoma Multiforme)00127

[back to top]

Tumor Response Rate (Complete and Partial) Assessed by Response Evaluation Criteria in Solid Tumors (RECIST)

(NCT00118157)
Timeframe: 4 weeks

Interventionparticipants (Number)
Arm 11

[back to top]

Proportion of Patients With Absolute Decrease in Left Ventricular Ejection Fraction (LVEF) Levels Post Doxorubicin and Cyclophosphamide(AC)

The endpoint was measured by absolute decrease from baseline in LVEF of >15% or >10% decline from baseline to below the LLN post doxorubicin and cyclophosphamide (AC) Day 1 Cycle 5 (DIC5). 207 patients who were treated and had baseline and DIC5 LVEF values were included in the analysis. (NCT00119262)
Timeframe: assessed on day 1 of cycles 5, 9, 17, 25, and at end of treatment

Interventionpercentage of participants (Number)
Arm A (ddBAC > BT > B)7.4
Arm B (ddAC > BT > B)3.5

[back to top]

Proportion of Patients With Absolute Decrease in LVEF Levels Post Bevacizumab

The endpoint was measured by absolute decrease from baseline in LVEF of >15% or >10% decline from baseline to below the LLN post bevacizumab (the end of treatment). 158 patients who were treated and had baseline and end of treatment LVEF values were included in the analysis. (NCT00119262)
Timeframe: assessed on day 1 of cycles 5, 9, 17, 25, and at end of treatment

Interventionpercentage of participants (Number)
Arm A (ddBAC > BT > B)15.3
Arm B (ddAC > BT > B)11.6

[back to top]

Congestive Heart Failure Rate

Clinical congestive heart failure includes patients with symptomatic decline in LVEF to at or below the lower limit of normal (LLN), or symptomatic diastolic dysfunction. 223 treated patients were included in the analysis. (NCT00119262)
Timeframe: assessed on day 1 of cycles 5, 9, 17 and 25, and at end of treatment, then every 3 months for <2 years and every 6 months for 2-3 years from study entry

Interventionpercentage of participants (Number)
Arm A (ddBAC > BT > B)2.9
Arm B (ddAC > BT > B)2.5

[back to top]

Percentage Change From Baseline in Serum Lipids at 5 Years

Serum lipid profile (fasting serum cholesterol [total, HDL and calculated LDL], triglycerides, and lipoprotein [a]) were measured at baseline/screening and at each visit thereafter. A central laboratory was used to analyze the samples. The analysis of serum lipids was on the treatment group median percent change from baseline (and range) at 5 years. (NCT00171704)
Timeframe: Baseline, 60 months

,
InterventionPercent Change (Median)
Total Cholesterol (n=91, 82)LDL Cholesterol (n=91, 82)HDL Cholesterol (n=91, 82)
Letrozole-7.3-12.78.7
Tam-Let-2.45-11.058.9

[back to top]

Time to Disease Recurrence or Death

Disease-free survival was defined as the interval between randomization and earliest confirmed event of loco-regional recurrence, distant metastases, invasive contralateral breast cancer, or death from any cause. (NCT00171704)
Timeframe: 60 months

InterventionDays (Median)
LetrozoleNA
Tam-LetNA

[back to top]

Percent Change From Baseline of Bone Mineral Density (BMD) of Total Hip

Total hip BMD measurements by dual energy X-ray absorptiometry (DXA) were performed after surgery and within 2 weeks prior to randomization and repeated every 6 months for the first 2 years and annually thereafter until 5 years after enrollment. All DXA scans were evaluated by a central reader. (NCT00171704)
Timeframe: Baseline, 60 months

InterventionPercent Change (Median)
Letrozole-5.77
Tam-Let-3.98

[back to top]

Percent Change From Baseline of Bone Mineral Density of the Lumbar Spine

Lumbar spine (L2-L4)BMD measurements by dual energy X-ray absorptiometry (DXA) were performed after surgery and within 2 weeks prior to randomization and repeated every 6 months for the first 2 years and annually thereafter until 5 years after enrollment. The primary scanning site was the lumbar spine (L2 to L4) and the secondary scanning site was the total hip. All DXA scans were evaluated by a central reader. (NCT00171704)
Timeframe: Baseline, 60 months

InterventionPercent change (Median)
Letrozole-5.66
Tam-Let-3.3

[back to top]

Percent Change From Baseline of Bone Mineral Density of the Lumbar Spine (L2-l4)

Lumbar spine (L2-L4) BMD measurements by dual energy X-ray absorptiometry (DXA) were performed after surgery and within 2 weeks prior to randomization and repeated every 6 months for the first 2 years and annually thereafter until 5 years after enrollment. The primary scanning site was the lumbar spine (L2 to L4) and the secondary scanning site was the total hip. All DXA scans were evaluated by a central reader. (NCT00171704)
Timeframe: Baseline, 24 months

InterventionPercent Change (Median)
Letrozole-4.63
Tam-Let0.37

[back to top]

Time to Overall Survival Events

Overall survival was measured from date of randomization to date of death. (NCT00171704)
Timeframe: 60 Months

Interventiondays (Median)
LetrozoleNA
Tam-LetNA

[back to top]

Median Percent Change From Baseline of Serum Markers of Bone Turnover

Bone turnover markers (fasting serum procollagen-I extension peptide [P1NP], C-telopeptide [CTX], skeletal bone-specific alkaline phosphatase [BSAP, N-telopeptide [NTX]) were measured at baseline/screening and at each visit thereafter. A central laboratory was used to analyze the samples. The analysis of bone markers was based on analysis of variance of the regression slopes calculated for each individual patient and each bone marker over time. In the following summary, only the median treatment group percent change from baseline (and range) at 5 years is presented for each bone marker. (NCT00171704)
Timeframe: Baseline, 60 months

,
InterventionPercent Change (Median)
Procollagen-I (PINP) (n=86, 78)Bone Specific alkaline Phosphatase (n=87,78)C-telopeptide (CTX) (n=88, 78)N-telopeptide (NTX) (n=-88, 77)
Letrozole-14.1516.2-12.05-53.05
Tam-Let-0.519.154.55-50.7

[back to top]

Number of Participants With Clinically Relevant Changes From Baseline in Cholesterol

Serum lipid profile (fasting serum cholesterol [total, HDL and calculated LDL], triglycerides, and lipoprotein [a]) were measured at baseline/screening and at each visit thereafter. A central laboratory was used to analyze the samples. Numbers are not additive, as patients could be included in multiple rows. (NCT00171704)
Timeframe: Baseline, 60 months

,
InterventionParticipants (Number)
Patients with one or more change≥8 mmol/L total (T) cholesterol≥7 mmol/L T.choles. & ≥1 risk for cardiac disease≥6 mmol/L T. choles. & ≥2 risk for cardiac disease
Letrozole3071811
Tam-Let215129

[back to top]

Relapse Rate in Patients With Operable Breast Cancer Treated With Neoadjuvant Chemotherapy for 12 Weeks Followed by Weekly Paclitaxel for 12 Weeks and Adjuvant Chemotherapy

Count of patients that relapsed. (NCT00194779)
Timeframe: Up to 8 years

InterventionParticipants (Count of Participants)
Treatment (Neoadjuvant Therapy, Adjuvant Therapy)7

[back to top]

Combined Rate of Microscopic pCR and Macroscopic Pathologic Complete Response (mCR)

"Microscopic pCR: No evidence of microscopic invasive tumor at the primary site or in the regional lymph nodes at the time of definitive surgical resection. mCR: The examining pathologist cannot identify gross residual tumor mass in the surgical specimen. This differs from a pCR where the specimen must also be negative for invasive tumor by microscopy. For this study, we are using a definition of mCR that will make the trial more translatable to other institutions. For this study, mCR will be defined as no focus of invasive cancer >= 1 cm.~Count of participants with either a pCR or mCR." (NCT00194779)
Timeframe: Up to 16 weeks

InterventionParticipants (Count of Participants)
Treatment (Neoadjuvant Therapy, Adjuvant Therapy)29

[back to top]

Number and Percent of Patients Reporting Grade 2, 3, 4, or Fatal Toxicities of These Regimens, Need for Dose Reduction, or Treatment Interruption or Discontinuation

(NCT00194779)
Timeframe: From the initiation of study treatments to 30 days after the end of neoadjuvant treatment or adjuvant treatment if received

InterventionParticipants (Count of Participants)
Treatment (Neoadjuvant Therapy, Adjuvant Therapy)32

[back to top]

Time to Progression

Median time to progression free survival. (NCT00194779)
Timeframe: Up to 5 years

Interventionmonths (Median)
Treatment (Neoadjuvant Therapy, Adjuvant Therapy)NA

[back to top]

Disease-free Survival

Kaplan-Meier estimate of disease-free survival, assessed at 1, 2, and 5 years. (NCT00194779)
Timeframe: 1, 2, and 5 years

Interventiondisease-free survival probability (Number)
1 year2 years5 years
Treatment (Neoadjuvant Therapy, Adjuvant Therapy).97.90.84

[back to top]

OS in Patients With Operable Breast Cancer Treated With Neoadjuvant Chemotherapy for 12 Weeks Followed Weekly Paclitaxel for 12 Weeks and Adjuvant Chemotherapy With XMN

Kaplan-Meier estimate of overall survival, assessed at 1, 2, and 5 years. (NCT00194779)
Timeframe: 1, 2, and 5 years

Interventionsurvival probability (Number)
1 year2 years5 years
Treatment (Neoadjuvant Therapy, Adjuvant Therapy)1.94.90

[back to top]

Disease-free Survival

5-year disease-free survival (NCT00201851)
Timeframe: two- to three-year accrual and initial two or more years of follow-up period

Interventionpercentage of participants (Number)
A - Scheduled Surgery64
B - Immediate Surgery71
C- Immediate Surgery - Nonrandomized70

[back to top]

Objective Response Rate (Defined as the Rate of Complete and Partial Responses).

(NCT00240071)
Timeframe: From date of registration until disease progression or death, whichever occurs first

Interventionparticipants (Number)
Avastin0

[back to top]

Progression Free Survival (PFS)

Progression free survival is defined as time from date of registration until the date of first documented disease progression or date of death from any cause, whichever occurs first. (NCT00240071)
Timeframe: From date of registration until disease progression or death, whichever occurs first

Interventiondays (Median)
Avastin (Bevacizumab) Plus Hormone125.5

[back to top]

Change From Baseline in Severity of VVA Symptoms

This outcome measure was analyzed using CMH row mean scores test controlling for study center and uterine status. VVA Symptom Score: 0 = None, 1 = Mild, 2 = Moderate, 3 = Severe (NCT00276094)
Timeframe: Baseline (Randomization) to Week 12

,,
InterventionUnits on a scale (Mean)
Vaginal drynessVaginal pain associated with sexual activityVulvar/vaginal itching or irritationDifficult/painful urinationVaginal bleeding associated with sexual activity
Ospemifene 30 mg/Day and Nonhormonal Vaginal Lubricant-0.96-0.77-0.40-0.17-0.26
Ospemifene 60 mg/Day and Nonhormonal Vaginal Lubricant-1.17-0.87-0.58-0.20-0.23
Placebo Tablets and Nonhormonal Vaginal Lubricant-0.63-0.57-0.44-0.097-0.12

[back to top]

Change From Baseline in Estradiol Levels

(NCT00276094)
Timeframe: Baseline (Screening) to Week 12

Interventionpg/mL (Mean)
Ospemifene 30 mg/Day and Nonhormonal Vaginal Lubricant-1.44
Ospemifene 60 mg/Day and Nonhormonal Vaginal Lubricant1.02
Placebo Tablets and Nonhormonal Vaginal Lubricant0.30

[back to top]

Change From Baseline in Follicle Stimulating Hormone Levels

(NCT00276094)
Timeframe: Baseline (Screening) to Week 12

InterventionIU/L (Mean)
Ospemifene 30 mg/Day and Nonhormonal Vaginal Lubricant-5.93
Ospemifene 60 mg/Day and Nonhormonal Vaginal Lubricant-8.71
Placebo Tablets and Nonhormonal Vaginal Lubricant-1.33

[back to top]

Change From Baseline in Luteinizing Hormone Levels

(NCT00276094)
Timeframe: Baseline (Screening) to Week 12

InterventionIU/L (Mean)
Ospemifene 30 mg/Day and Nonhormonal Vaginal Lubricant-2.85
Ospemifene 60 mg/Day and Nonhormonal Vaginal Lubricant-3.73
Placebo Tablets and Nonhormonal Vaginal Lubricant0.41

[back to top]

Change From Baseline in Sex Hormone Binding Globulin Levels

(NCT00276094)
Timeframe: Baseline (Screening) to Week 12

Interventionnmol/L (Mean)
Ospemifene 30 mg/Day and Nonhormonal Vaginal Lubricant11.1
Ospemifene 60 mg/Day and Nonhormonal Vaginal Lubricant22.8
Placebo Tablets and Nonhormonal Vaginal Lubricant-2.17

[back to top]

Change From Baseline in Testosterone (Free) Levels

(NCT00276094)
Timeframe: Baseline (Screening) to Week 12

Interventionng/dL (Mean)
Ospemifene 30 mg/Day and Nonhormonal Vaginal Lubricant0.002
Ospemifene 60 mg/Day and Nonhormonal Vaginal Lubricant-0.031
Placebo Tablets and Nonhormonal Vaginal Lubricant-0.008

[back to top]

Change From Baseline in Testosterone (Total) Levels

(NCT00276094)
Timeframe: Baseline (Screening) to Week 12

Interventionng/dL (Mean)
Ospemifene 30 mg/Day and Nonhormonal Vaginal Lubricant1.55
Ospemifene 60 mg/Day and Nonhormonal Vaginal Lubricant1.92
Placebo Tablets and Nonhormonal Vaginal Lubricant-0.059

[back to top]

Mean Change From Baseline in Percentage of Parabasal Cells in Maturation Index of Vaginal Smear

(NCT00276094)
Timeframe: Baseline (Screening) to Week 12

Interventionpercentage of parabasal cells (Mean)
Ospemifene 30 mg/Day and Nonhormonal Vaginal Lubricant-21.9
Ospemifene 60 mg/Day and Nonhormonal Vaginal Lubricant-30.1
Placebo Tablets and Nonhormonal Vaginal Lubricant3.98

[back to top]

Mean Change From Baseline in the MBS of Vaginal Pain Associated With Sexual Activity

This outcome measure was analyzed using CMH row mean scores test controlling for study center and uterine status. VVA Symptom Score: 0 = None, 1 = Mild, 2 = Moderate, 3 = Severe (NCT00276094)
Timeframe: Baseline (Randomization) to Week 12

InterventionUnits on a scale (Mean)
Ospemifene 30 mg/Day and Nonhormonal Vaginal Lubricant-1.02
Ospemifene 60 mg/Day and Nonhormonal Vaginal Lubricant-1.19
Placebo Tablets and Nonhormonal Vaginal Lubricant-0.89

[back to top]

Mean Change From Baseline in the Most Bothersome Vulvar and Vaginal Atrophy (VVA) Symptom (MBS) of Vaginal Dryness

This outcome measure was analyzed using Cochran-Mantel-Haenszel (CMH) row mean scores test controlling for study center and uterine status. VVA Symptom Score: 0 = None, 1 = Mild, 2 = Moderate, 3 = Severe (NCT00276094)
Timeframe: Baseline (Randomization) to Week 12

InterventionUnits on a scale (Mean)
Ospemifene 30 mg/Day and Nonhormonal Vaginal Lubricant-1.22
Ospemifene 60 mg/Day and Nonhormonal Vaginal Lubricant-1.26
Placebo Tablets and Nonhormonal Vaginal Lubricant-0.84

[back to top]

Mean Change From Baseline in the Percentage of Superficial Cells in Maturation Index of Vaginal Smear

(NCT00276094)
Timeframe: Baseline (Screening) to Week 12

Interventionpercentage of superficial cells (Mean)
Ospemifene 30 mg/Day and Nonhormonal Vaginal Lubricant7.78
Ospemifene 60 mg/Day and Nonhormonal Vaginal Lubricant10.8
Placebo Tablets and Nonhormonal Vaginal Lubricant2.18

[back to top]

Mean Change From Baseline in Vaginal pH

(NCT00276094)
Timeframe: Baseline (Screening) to Week 12

InterventionpH (Mean)
Ospemifene 30 mg/Day and Nonhormonal Vaginal Lubricant-0.67
Ospemifene 60 mg/Day and Nonhormonal Vaginal Lubricant-1.01
Placebo Tablets and Nonhormonal Vaginal Lubricant-0.096

[back to top]

Change From Baseline in Visual Evaluation of the Vagina

Exam Rating Scale: 0 = None, 1 = Mild, 2 = Moderate, 3 = Severe (NCT00276094)
Timeframe: Baseline (Screening) to Week 12

,,
InterventionUnits on a scale (Mean)
PetechiaePallorFriabilityVaginal dryness in mucosaVaginal redness in mucosa
Ospemifene 30 mg/Day and Nonhormonal Vaginal Lubricant-0.50-0.75-0.57-1.05-0.44
Ospemifene 60 mg/Day and Nonhormonal Vaginal Lubricant-0.60-0.93-0.71-1.22-0.60
Placebo Tablets and Nonhormonal Vaginal Lubricant-0.037-0.30-0.16-0.48-0.23

[back to top]

Change From Baseline in Urinary Symptoms

(NCT00276094)
Timeframe: Baseline (Randomization) to Week 12

,,
InterventionParticipants (Number)
Frequent urination-ImprovedFrequent urination-WorsenedUrine leakage (feeling of urgency)-ImprovedUrine leakage (feeling of urgency)-WorsenedUrine leakage with physical exertion-ImprovedUrine leakage with physical exertion-WorsenedSmall amount of urine leakage-ImprovedSmall amount of urine leakage-WorsenedDifficulty emptying bladder-ImprovedDifficulty emptying bladder-WorsenedPain in lower abdominal/genital area-ImprovedPain in lower abdominal or genital area-Worsened
Ospemifene 30 mg/Day and Nonhormonal Vaginal Lubricant492452245024593025143717
Ospemifene 60 mg/Day and Nonhormonal Vaginal Lubricant632553265623553226114113
Placebo Tablets and Nonhormonal Vaginal Lubricant602257324727582724153716

[back to top]

Percentage of Physicians Judging the Cosmetic Outcome as Good or Excellent

"The following items will be evaluated by comparing the treated breast with the untreated breast: overall cosmetic result; appearance of the surgical scar; breast size; breast shape; nipple position; and shape of areola. In scoring these items, a 4-point scale will be used, classifying the results into one of the following categories: 0 representing an excellent result; 1 a good result; 2 a fair result; and 3 a poor result." (NCT00290654)
Timeframe: 12 months after treatment

Interventionpercentage of physicians (Number)
Evaluable Patients86.7

[back to top]

Percentage of Patients Who Experienced Complications

Complications to be measured include: breast tenderness/pain,reddening of the skin, bruising, formation of blood or fluid under the skin, skin ulceration, infection, discoloration of the skin, development of telangiectasia (spider veins), hardening of the breast tissue, and retraction of the breast tissue. (NCT00290654)
Timeframe: within 6 months of treatment

Interventionpercentage of participants (Number)
Evaluable Patients65.8

[back to top]

Number of Patients With Ipsilateral Breast Tumor Recurrence

Count of patients with early stage breast cancer who developed an ipsilateral breast tumor recurrence (IBTR) and failed after receiving breast-conserving therapy. (NCT00290654)
Timeframe: 1 year after treatment

Interventionparticipants (Number)
Evaluable Patients0

[back to top]

Percentage of Physicians Judging the Cosmetic Outcome as Good or Excellent

"The following items will be evaluated by comparing the treated breast with the untreated breast: overall cosmetic result; appearance of the surgical scar; breast size; breast shape; nipple position; and shape of areola. In scoring these items, a 4-point scale will be used, classifying the results into one of the following categories: 0 representing an excellent result; 1 a good result; 2 a fair result; and 3 a poor result." (NCT00290654)
Timeframe: 6 months after treatment

Interventionpercentage of physicians (Number)
Evaluable Patients100

[back to top]

Percentage of Patients Judging the Cosmetic Outcome as Good or Excellent

"The following items will be evaluated by comparing the treated breast with the untreated breast: overall cosmetic result; appearance of the surgical scar; breast size; breast shape; nipple position; and shape of areola. In scoring these items, a 4-point scale will be used, classifying the results into one of the following categories: 0 representing an excellent result; 1 a good result; 2 a fair result; and 3 a poor result." (NCT00290654)
Timeframe: 6 months after treatment

Interventionpercentage of participants (Number)
Evaluable Patients96.8

[back to top]

Number of Patients With Ipsilateral Breast Tumor Recurrence

Count of patients with early stage breast cancer who developed an ipsilateral breast tumor recurrence (IBTR) and failed after receiving breast-conserving therapy. (NCT00290654)
Timeframe: 5 years after treatment

Interventionparticipants (Number)
Evaluable Patients4

[back to top]

Percentage of Patients Judging the Cosmetic Outcome as Good or Excellent

"The following items will be evaluated by comparing the treated breast with the untreated breast: overall cosmetic result; appearance of the surgical scar; breast size; breast shape; nipple position; and shape of areola. In scoring these items, a 4-point scale will be used, classifying the results into one of the following categories: 0 representing an excellent result; 1 a good result; 2 a fair result; and 3 a poor result." (NCT00290654)
Timeframe: 12 months after treatment

Interventionpercentage of participants (Number)
Evaluable Patients92.3

[back to top]

Percentage of Patients Who Experienced Complications

Complications to be measured include: breast tenderness/pain,reddening of the skin, bruising, formation of blood or fluid under the skin, skin ulceration, infection, discoloration of the skin, development of telangiectasia (spider veins), hardening of the breast tissue, and retraction of the breast tissue. (NCT00290654)
Timeframe: more than 6 months after treatment, for up to 5 years

Interventionpercentage of participants (Number)
Evaluable Patients24.4

[back to top]

Correlation Between Pathologic Tumor Size and Mammographic Tumor Size

Correlations between pathologic tumor size and maximum diameters of baseline and pre-surgical mammographic extent of disease were evaluated using Spearman correlation coefficient measure of association. The Spearman's rank-order correlation (rs) measures the strength and direction of association between two variables. The Spearman correlation coefficient, rs, can take values from +1 to -1 where a value of +1 indicates a perfect association, an rs of 0 indicates no association and an rs of -1 indicates a perfect negative association. The closer rs is to 0, the weaker the association. (NCT00290745)
Timeframe: 6 months

InterventionSpearman correlation coefficient (rs) (Number)
Tamoxifen or Letrozole0.02

[back to top]

Correlation Between Pathologic Tumor Size at Radiographic (MRI) Tumor Size

Correlations between pathologic tumor size and maximum diameters of baseline and 6-month MRI extent of disease were evaluated using Spearman correlation coefficient measure of association. The Spearman's rank-order correlation (rs) measures the strength and direction of association between two variables. The Spearman correlation coefficient, rs, can take values from +1 to -1 where a value of +1 indicates a perfect association, an rs of 0 indicates no association and an rs of -1 indicates a perfect negative association. The closer rs is to 0, the weaker the association. (NCT00290745)
Timeframe: 6 months

InterventionSpearman correlation coefficient (rs) (Number)
Tamoxifen or Letrozole0.46

[back to top]

Median Reduction in Tumor Volume by Estrogen Receptor Hormone (ER H-) Quartile Group

Tumor volume changes between baseline and surgery were calculated at month 6 and compared across baseline ER Hormone (H-) Score quartile. The ER H- scores are a percentage that tells you how many cells out of 100 stain positive for hormone receptors. Each participant is assigned an ER H- score at baseline with the full score range between 0 (none have receptors) and 100 (all have receptors). The participants were grouped into quartiles (four equal groups) based on their baseline ER H- score. ER H- score and the reduction in tumor volume from baseline to month 6 was measured for each quartile group. (NCT00290745)
Timeframe: Baseline and 6 months

Interventiondecrease in tumor volume (cm^3) (Median)
Baseline ER Score quartile = 0-25Baseline ER Score quartile = 26-50Baseline ER Score quartile = 51-75Baseline ER Score quartile = 76-100
Tamoxifen or Letrozole-58.8-70.3-80.3-71.1

[back to top]

Median Change in 6-month Tumor Volume Compared to Baseline Using Mammography

Change in size of Ductal Carcinoma in situ (DCIS) for participants on hormonal therapy, as determined by mammography are determined by (1) largest diameter of tumor, as visualized on mammography (2) extent of disease on mammography (3) quantification of mammographically-detected change from baseline to 6-month and used to generate the change in tumor volume of mammographic extent of disease from baseline. Since values were not normally distributed, the median change was calculated, and Wilcoxon sign rank tests were used to evaluate the significance of these changes (NCT00290745)
Timeframe: Baseline and 6 months

Interventionchange in tumor volume (mm) (Median)
Tamoxifen or Letrozole-5.0

[back to top]

Median Change in 6-month Tumor Volume Compared to Baseline Using Magnetic Resonance Imaging (MRI)

Change in size of Ductal Carcinoma in situ (DCIS) on hormonal therapy, as determined by MRI are determined by (1) largest diameter of tumor, as visualized on MRI (2) extent of disease on MRI (3) quantification of MR-detected change from baseline to 6-month and used to generate the change in tumor volume of MRI extent of disease from baseline. Since values were not normally distributed, the median change was calculated, and Wilcoxon sign rank tests were used to evaluate the significance of these changes. (NCT00290745)
Timeframe: Baseline and 6 months

Interventionchange in tumor volume (cm3) (Median)
Tamoxifen or Letrozole-0.8

[back to top]

Number of Responders to Neoadjuvant Therapy at Month 6

MRI volume response at each time point was classified as follows: 90% image-complete response (ICR90) is defined as a >90% reduction in tumor volume, 80% image-complete response (ICR80) is defined as an 81-90% reduction in tumor volume , partial response (PR) is defined as a 20-80% reduction in tumor volume, and sustained disease or progressive disease (SD/PD) defined as a <20% reduction or increase in volume. (NCT00290745)
Timeframe: 6 months

InterventionParticipants (Count of Participants)
ICR90ICR80PRSD/PD
Tamoxifen or Letrozole2272612

[back to top]

Number of Responders to Neoadjuvant Therapy at Month 3

MRI volume response at each time point was classified as follows: 90% image-complete response (ICR90) is defined as a >90% reduction in tumor volume, 80% image-complete response (ICR80) is defined as an 81-90% reduction in tumor volume , partial response (PR) is defined as a 20-80% reduction in tumor volume, and sustained disease or progressive disease (SD/PD) defined as a <20% reduction or increase in volume. (NCT00290745)
Timeframe: 3 months

InterventionParticipants (Count of Participants)
ICR90ICR80PRSD/PD
Tamoxifen or Letrozole13102717

[back to top]

Median Reduction in Tumor Volume by PgR H-score by Quartile Group

"Tumor volume changes between baseline and surgery were calculated at month 6 and compared across baseline PgR Hormone (H-) Score quartile. The PgR H-scores are a percentage that tells you how many cells out of 100 stain positive for hormone receptors. Each participant is assigned a PgR H- score at baseline with the full PgR H score ranges between 0 (none have receptors) and 100 (all have receptors). The participants were grouped into quartiles (four equal groups) based on their baseline PgR H- score and the reduction in tumor volume from baseline to month 6 was measured for each quartile group.~A wilcoxon sign rank tests were used to evaluate the significance of these changes" (NCT00290745)
Timeframe: Baseline and 6 months

Interventionreduction in tumor volume (cm^3) (Median)
Baseline PgR Score Quartile = 0-25Baseline PgR Score Quartile = 26-50Baseline PgR Score Quartile = 51-75Baseline PgR Score Quartile = 76-100
Tamoxifen or Letrozole-69.1-45.8-69.6-96.2

[back to top]

Median Reduction in Tumor Volume by Ki-67 Average Score

"Tumor volume changes between baseline and surgery were calculated at month 6 by Baseline Ki-67 Average Score which is divided into 2 groups: (1) <=10% or (2) >10% to 100%. In est results, the Ki-67 findings expressed as a percentage with less than 10% considered low Ki-67 expression and > than 10% or higher considered high. A high score means that the breast tumor is more likely to be aggressive and spread quickly. A wilcoxon sign rank tests were used to evaluate the significance of these changes" (NCT00290745)
Timeframe: Baseline and 6 months

Interventionreduction in tumor volume (cm^3) (Median)
Baseline Ki67 Average <=10%Baseline Ki67 Average > 10%
Tamoxifen or Letrozole-73.0-70.3

[back to top]

Overall Survival

Assess whether patients who undergo surgical oophorectomy in the history-estimated mid-luteal phase of their menstrual cycles survive longer than patients who undergo this surgery in the history-estimated mid-follicular phase of their menstrual cycles. (NCT00293540)
Timeframe: Up to 9 years

Interventionyears (Median)
A Mid-luteal Surgery2.14
B Mid-follicular Surgery2.00

[back to top]

5-year Disease-free Survival

Disease-free survival (DFS) is defined to be time from randomization to first event, where the first event is any of ipsilateral breast tumor recurrence, local recurrence, regional recurrence, distant recurrence, contralateral second primary invasive cancer, second primary non-breast invasive cancer (excluding non-melanoma skin cancers), or death without evidence of recurrence. The distribution of DFS (eg, 5-year DFS rate) is estimated using Kaplan-Meier method, and compared between the two randomized arms (arm B vs. arm C) using stratified log rank test and stratified Cox proportional hazard model. (NCT00310180)
Timeframe: Assessed every 6 months within 5 years from registration and then annually up to 20 years, DFS rate estimated at 5 years

Interventionpercentage of participants (Number)
Arm A94.0
Arm B92.8
Arm C93.1
Arm D87.6

[back to top]

5-year Distant Recurrence-free Interval

Distant recurrence-free interval (DRFI) is defined as time from date of randomization or registration to the date of distant recurrence of breast cancer, or of death with distant recurrence, if death is the first manifestation of distant recurrence. The distribution of DRFI (eg, 5-year DRFI rate) is estimated using Kaplan-Meier method. (NCT00310180)
Timeframe: Assessed every 6 months within 5 years from registration and then annually up to 20 years, DRFI rate estimated at 5 years

Interventionpercentage of participants (Number)
Arm A99.3
Arm B98.0
Arm C98.2
Arm D93.0

[back to top]

5-year Overall Survival

Overall survival (OS) is defined as time from date of randomization or registration to date of death from any cause. The distribution of OS (eg, 5-year OS rate) is estimated using Kaplan-Meier method. (NCT00310180)
Timeframe: Assessed every 6 months within 5 years from registration and then annually up to 20 years, OS rate estimated at 5 years

Interventionpercentage of participants (Number)
Arm A98.0
Arm B98.0
Arm C98.1
Arm D95.9

[back to top]

5-year Recurrence-free Interval

Recurrence-free interval (RFS) is defined as time from date of randomization or registration to the date of first recurrence of breast cancer (ipsilateral breast tumor recurrence, local/regional recurrence, distant recurrence) or to the date of death with recurrence, if death is the first manifestation of recurrence. The distribution of RFS (eg, 5-year RFS rate) is estimated using Kaplan-Meier method. (NCT00310180)
Timeframe: Assessed every 6 months within 5 years from registration and then annually up to 20 years, RFS rate estimated at 5 years

Interventionpercentage of participants (Number)
Arm A98.8
Arm B96.9
Arm C97.0
Arm D91.0

[back to top]

5-year Disease-free Survival by Age and Recurrence Score Groups

Disease-free survival (DFS) is defined to be time from randomization to first event, where the first event is any of ipsilateral breast tumor recurrence, local recurrence, regional recurrence, distant recurrence, contralateral second primary invasive cancer, second primary non-breast invasive cancer (excluding non-melanoma skin cancers), or death without evidence of recurrence. DFS is evaluated by recurrence score (0-10 vs. 11-15 vs. 16-20 vs. 21-25 vs. >25) and age groups (<=50 vs. 51-65 vs. 65-75). The distribution of DFS (eg, 5-year DFS rate) is estimated using Kaplan-Meier method. (NCT00310180)
Timeframe: Assessed every 6 months within 5 years from registration and then annually up to 20 years, DFS rate estimated at 5 years

,,,
Interventionpercentage of participants (Number)
RS 0-10 & Age<=50RS 0-10 & Age 51-65RS 0-10 & Age 66-75RS 11-15 & Age <=50RS 11-15 & Age 51-65RS 11-15 & Age 66-75RS 16-20 & Age <=50RS 16-20 & Age 51-65RS 16-20 & Age 66-75RS 21-25 & Age <=50RS 21-25 & Age 51-65RS 21-25 & Age 66-75RS >25 & Age <=50RS >25 & Age 51-65RS >25 & Age 66-75
Arm A95.194.790.5NANANANANANANANANANANANA
Arm BNANANA95.195.587.192.094.390.186.391.693.8NANANA
Arm CNANANA94.393.991.494.792.290.292.193.490.9NANANA
Arm DNANANANANANANANANANANANA86.487.589.8

[back to top]

Time to Progression (TTP)

The median response duration in months. Response and progression were evaluated in this study using the new international criteria proposed by the Response Evaluation Criteria in Solid Tumors (RECIST). (NCT00365599)
Timeframe: Up to 30 months

Interventionmonths (Median)
Vorinostat and Tamoxifen10.3

[back to top]

Number of Participants With Serious Adverse Events (SAEs)

Safety evaluation according to descriptions and grading scales found in the revised NCI Common Terminology Criteria for Adverse Events (CTCAE) version 3.0. (NCT00365599)
Timeframe: 4 years, 7 months

Interventionparticipants (Number)
Vorinostat and Tamoxifen4

[back to top]

Number of Participants With Objective Response (OR)

The Objective Response Rate. Response and progression were evaluated in this study using the new international criteria proposed by the Response Evaluation Criteria in Solid Tumors (RECIST). Changes in only the largest diameter (unidimensional measurement) of the tumor lesions are used in the RECIST criteria. For the purposes of this study, patients were evaluated for response every 8 weeks. In addition to a baseline scan, confirmatory scans were also obtained ≥ 4 weeks following initial documentation of objective response. (NCT00365599)
Timeframe: 24 weeks

Interventionparticipants (Number)
Vorinostat and Tamoxifen8

[back to top]

Number of Patients With Pathological Complete Response

"Assessed by the institutional pathologist.~Grade 1: disappearance of all tumor on microscopic assessment in the breast and LNs~Grade 2: presence of in situ carcinoma only in the breast, no invasive tumor, and no tumor found in the LNs~Grade 3: presence of invasive carcinoma with stromal alteration, such as sclerosis or fibrosis~Grade 4: no or few modifications of the tumor appearance" (NCT00499083)
Timeframe: At definitive surgery.

Interventionparticipants (Number)
Vaccine2

[back to top]

Incidence of Fatty Liver Disease

The primary objective is to compare ARIMIDEX (anastrozole) 1 mg once daily with Tamoxifen 20 mg once daily as adjuvant treatment in terms of: incidence of fatty liver diseases. (NCT00537771)
Timeframe: At 48 weeks, 96 weeks, 144 weeks

,
Interventionparticipants (Number)
48 weeks96 weeks144 weeks
Arimidex Group91526
TAM Group536672

[back to top]

Time to Treatment Failure

(NCT00537771)
Timeframe: Within 3 years

Interventiondays (Median)
Arimidex Group1112
TAM Group454

[back to top]

Incidence of Abnormal Liver Function

The second objectives are to compare ARIMIDEX (anastrozole) 1 mg once daily with Tamoxifen 20 mg once daily as adjuvant treatment in terms of: incidences of abnormal liver function test, and time to treatment failure. (NCT00537771)
Timeframe: At 48 weeks, 96 weeks, 144 weeks

,
Interventionparticipants (Number)
48 weeks96 weeks144 weeks
Arimidex Group293744
TAM Group364043

[back to top]

Progression-free Survival

The Primary Endpoint for this study was to compare the progression-free survival of letrozole therapy alone with the combination of letrozole therapy plus bevacizumab as first-line treatment in women with estrogen- and/or progesterone-receptor-positive advanced breast cancer. Progression-free survival (PFS) was defined as the time from randomization until disease progression or death, whichever occurs first. The median PFS was estimated using the Kaplan-Meier method. Progression was assessed per RECIST criteria, and defined as at least a 20% increase in the sum of the longest diameters of target lesions from baseline or the appearance of new lesions. (NCT00601900)
Timeframe: From randomization until disease progression or death whichever occurs first, assessed up to 5 years

Interventionmonths (Median)
Arm I (Endocrine Therapy With Monoclonal Antibody)20.2
Arm II (Endocrine Therapy)15.6

[back to top]

Overall Survival (OS)

OS is defined as the time from study entry to death from any cause. The median OS was estimated using the Kaplan-Meier method. (NCT00601900)
Timeframe: Assessed up to 5 years

Interventionmonths (Median)
Arm I (Endocrine Therapy With Monoclonal Antibody)47.2
Arm II (Endocrine Therapy)43.9

[back to top]

12 Month Progression Free Survival Rate

The 12 month progression-free survival rate was defined as the proportion of patients who were alive progression-free 12 months after registration into the study. (NCT00601900)
Timeframe: At 12 months

Interventionpercentage of participants (Number)
Arm I (Endocrine Therapy With Monoclonal Antibody)73
Arm II (Endocrine Therapy)61

[back to top]

6 Month Progression-Free Survival Rate

The 6 month progression-free survival rate was defined as the proportion of patients who were alive progression-free 6 months after registration into the study. (NCT00601900)
Timeframe: At 6 months

Interventionpercentage of participants (Number)
Arm I (Endocrine Therapy With Monoclonal Antibody)87
Arm II (Endocrine Therapy)77

[back to top]

Objective Response Rate

Response was defined using RECIST criteria: Complete Response (CR): disappearance of all target lesions; Partial Response (PR) 30% decrease in sum of longest diameter of target lesions. (NCT00601900)
Timeframe: Assessed up to 5 years

,
Interventionpercentage of participants (Number)
Complete Response (CR)Partial Response (PR)Stable Disease (SD)
Arm I (Endocrine Therapy With Monoclonal Antibody)46522
Arm II (Endocrine Therapy)74234

[back to top]

Endocrine Subscale (ES)

"Change from baseline in Endocrine Symptom Subscale (ES)) in the ITT population at 24 weeks. ES score = the sum of the responses to all the questions on ES, low scores reflect poor quality of life and high scores reflects better quality of life.~Score range: 0-72" (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment

InterventionES score (Mean)
Anastrozole 1 mg-8.85
Tamoxifen 20 mg-6.27

[back to top]

Serum Oestrone (E1) Concentrations

Ratio of serum Oestrone (E1) concentration (pg/mL) in the ITT population from baseline at 24 weeks. (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment

InterventionRatio (Mean)
Anastrozole 1 mg0.028
Tamoxifen 20 mg0.341

[back to top]

Human Epidermal Growth Factor Receptor 2 (HER2) Status

HER2 status in the ITT population is categorized as Positive or Negative (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment

,
InterventionParticipants (Number)
Baseline Positive & 24 weeks NegativeBaseline Positive & 24 weeks PositiveBaseline Negative & 24 weeks NegativeBaseline Negative & 24 weeks Positive
Anastrozole 1 mg00922
Tamoxifen 20 mg00882

[back to top]

Functional Assessment of Cancer Therapy-Breast (FACT-B)

"Change from baseline in Functional Assessment of Cancer Therapy-Breast (FACT-B)in the ITT population at 24 weeks. Trial Outcome Index (TOI) = the sum of the Physical Well-Being (PWB), Functional Well-Being (FWB), and Breast Cancer Scale (BCS) subscales of FACT-B.~FACT-B includes 36 questions; 7 in PWB (Physical Well-Being); 7 inSWB (Social / Family Well-Being); 6 in EWB (Emotional Well-Being); 7 in FWB (Functional Well-Being); 9 in BCS (Breast Cancer Subscale).~Total score of subscores or TOI is calculated from each score of question. Higher score means better and lower score means worthier.~Score range; 0-28 in PWB; 0-28 in SWB; 0-24 in EWB; 0-28 in FWB; 0-36 in BCS; 0-92 in TOI." (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment

InterventionTrial Outcome Index (TOI) (Prorated) (Mean)
Anastrozole 1 mg-4.42
Tamoxifen 20 mg-2.65

[back to top]

Histopathological Response Rate (HRR)

Number of patients in the ITT population defined as histopathological responders over the total number of patients x 100. An histopathological responder = a patient classified as Grade 1b, 2 or 3 for the histopathological response (Grade 0 = no response, 1a = mild response, 1b = moderate response, 2 = marked response or 3 = complete response) (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment

InterventionPercentage of Participants (Number)
Anastrozole 1 mg41.8
Tamoxifen 20 mg27.3

[back to top]

Progesterone Receptor (PgR) Status

PgR status in the ITT population is categorized as Positive or Negative. (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment

,
InterventionParticipants (Number)
Baseline Positive & 24 weeks NegativeBaseline Positive & 24 weeks PositiveBaseline Negative & 24 weeks NegativeBaseline Negative & 24 weeks Positive
Anastrozole 1 mg602941
Tamoxifen 20 mg195993

[back to top]

Serum Oestradiol (E2) Concentrations

Ratio of serum Oestradiol (E2) concentration (pg/mL) in the ITT population from baseline at 24 weeks. (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment

InterventionRatio (Mean)
Anastrozole 1 mg0.041
Tamoxifen 20 mg0.082

[back to top]

Oestrogen Receptor (ER) Status

ER status in the ITT population is categorized as Positive or Negative (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment

,
InterventionParticipants (Number)
Baseline Positive & 24 weeks NegativeBaseline Positive & 24 weeks PositiveBaseline Negative & 24 weeks NegativeBaseline Negative & 24 weeks Positive
Anastrozole 1 mg29200
Tamoxifen 20 mg18900

[back to top]

Anastrozole Plasma Concentrations (Cmin)

Trough Plasma concentrations (Cmin) of Anastrozole - only Anastrozole arm was evaluated for Trough Plasma concentrations. (NCT00605267)
Timeframe: Assessed at week 12

Interventionng/mL (Geometric Mean)
Anastrozole 1 mg29.7

[back to top]

Best Overall Response Rate (BORR) (Calliper)

"The BORR were defined as the percentage of patients with confirmed CR or PR in the ITT population during 24 weeks pre-operative treatment period (based on the data from calliper measurement).~CR (or PR) criteria are met at 2 or more time in points every 4 weeks. Per RECIST Criteria (V1.0) and assessed by Calliper: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >= 30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR." (NCT00605267)
Timeframe: 24 weeks

InterventionPercentage of Participants (Number)
Anastrozole 1 mg70.4
Tamoxifen 20 mg50.5

[back to top]

Best Overall Response Rate (BORR) (MRI/CT)

"The BORR were defined as the percentage of patients with confirmed CR or PR in the ITT population during 24 weeks pre-operative treatment period(based on the data from magnetic resonance imaging (MRI) or computed tomography (CT) measurement).~CR (or PR) criteria are met at either 12 weeks or 24 weeks. Per RECIST Criteria (V1.0) and assessed by MRI or CT: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >= 30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR." (NCT00605267)
Timeframe: 24 weeks

InterventionPercentage of Participants (Number)
Anastrozole 1 mg64.3
Tamoxifen 20 mg37.4

[back to top]

Best Overall Response Rate (BORR) (US)

"The BORR were defined as the percentage of patients with confirmed CR or PR in the ITT population during 24 weeks pre-operative treatment period (based on the data from ultra sound (US) measurement).~CR (or PR) criteria are met at 2 or more time in points every 4 weeks. Per RECIST Criteria (V1.0) and assessed by US: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >= 30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR." (NCT00605267)
Timeframe: 24 weeks

InterventionParticipants (Number)
Anastrozole 1 mg58.2
Tamoxifen 20 mg42.4

[back to top]

Bone Mineral Density (BMD) Cervical Thighbone

Change from baseline in Bone Mineral Density value (percentage), in all subjects who used DXA(Dual-energy X-ray absorptiometry) method throughout the study, at 24 weeks measured at cervical thighbone. (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment

InterventionPercentageBMD=Patient'sBMD/standard BMD) (Mean)
Anastrozole 1 mg-2.5
Tamoxifen 20 mg-0.5

[back to top]

Bone Mineral Density (BMD) Lumbar Spine

Change from baseline in Bone Mineral Density value (percentage), in all subjects who used DXA(Dual-energy X-ray absorptiometry) method throughout the study, at 24 weeks measured at lumbar spine. (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment

InterventionPercentageBMD=Patient's BMD/standard BMD (Mean)
Anastrozole 1 mg-5.8
Tamoxifen 20 mg-2.9

[back to top]

Bone Turnover Marker (BAP) CLEIA Method

Change from baseline in serum Bone-Alkaline Phosphatase (BAP) at 24 weeks measured by CLEIA method (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment

Interventionug/L (Mean)
Anastrozole 1 mg3.96
Tamoxifen 20 mg-0.75

[back to top]

Bone Turnover Marker (BAP) EIA Method

Change from baseline in serum Bone-Alkaline Phosphatase (BAP) at 24 weeks measured by EIA method (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment

InterventionU/L (Mean)
Anastrozole 1 mg7.1941
Tamoxifen 20 mg0.7333

[back to top]

Bone Turnover Marker (NTX)

Change from baseline in serum crosslinked N-Telopeptide of type I collagen (NTX) at 24 weeks (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment

InterventionnmolBCE(Bone Collagen Equivalent) /L (Mean)
Anastrozole 1 mg9.17
Tamoxifen 20 mg2.59

[back to top]

Mean Change From Baseline in Vaginal pH

(NCT00630539)
Timeframe: Week 4

InterventionpH (Mean)
Subjects on Placebo-0.12
Subjects on Ospemifene 5 mg/Day-0.26
Subjects on Ospemifene 15 mg/Day-0.53
Subjects on Ospemifene 30 mg/Day-0.78

[back to top]

Mean Change From Baseline in Sex Hormone Binding Globulin Levels

(NCT00630539)
Timeframe: Week 12

Interventionnmol/L (Mean)
Subjects on Placebo-2.4
Subjects on Ospemifene 5 mg/Day2.9
Subjects on Ospemifene 15 mg/Day6.3
Subjects on Ospemifene 30 mg/Day18.0

[back to top]

Mean Change From Baseline in Percentage of Parabasal Cells in the Maturation Index of the Vaginal Smear

(NCT00630539)
Timeframe: 12 weeks

Interventionpercentage of parabasal cells (Mean)
Subjects on Placebo-3.0
Subjects on Ospemifene 5 mg/Day-2.8
Subjects on Ospemifene 15 mg/Day-24.1
Subjects on Ospemifene 30 mg/Day-26.8

[back to top]

Mean Change From Baseline in Vaginal pH

(NCT00630539)
Timeframe: 12 weeks

InterventionpH (Mean)
Subjects on Placebo-0.07
Subjects on Ospemifene 5 mg/Day-0.37
Subjects on Ospemifene 15 mg/Day-0.95
Subjects on Ospemifene 30 mg/Day-1.11

[back to top]

Visual Evaluation of Vagina (by Gynecological Examination)

(NCT00630539)
Timeframe: Screening & Week 12

,,,,,,,
Interventionpercentage of subjects (Number)
Petechiae-NonePetechiae-MildPetechiae-ModeratePetechiae-SeverePetechiae-Not donePallor-NonePallor-MildPallor-ModeratePallor-SeverePallor-Not doneFriability-NoneFriability-MildFriability-ModerateFriability-SevereFriability-Not doneVaginal dryness in the mucosa-NoneVaginal dryness in the mucosa-MildVaginal dryness in the mucosa-ModerateVaginal dryness in the mucosa-SevereVaginal dryness in the mucosa-Not doneVaginal redness in the mucosa-NoneVaginal redness in the mucosa-MildVaginal redness in the mucosa-ModerateVaginal redness in the mucosa-SevereVaginal redness in the mucosa-Not done
Subjects on Ospemifene 15 mg/Day10.355.231.03.40.013.848.331.06.90.010.334.548.36.90.010.341.437.910.30.017.248.331.03.40.0
Subjects on Ospemifene 30 mg/Day10.053.326.710.00.06.740.043.310.00.016.740.023.320.00.010.043.333.313.30.010.050.023.316.70.0
Subjects on Ospemifene 30 mg/Day (Week 12)60.030.03.33.30.046.743.36.70.00.060.033.33.30.00.073.316.76.70.00.053.340.00.03.30.0
Subjects on Ospemifene 5 mg/Day24.242.412.121.20.06.130.357.66.10.015.227.336.421.20.06.121.263.69.10.018.233.333.315.20.0
Subjects on Ospemifene 5 mg/Day (Week 12)36.439.46.115.23.015.248.530.33.03.030.330.333.33.03.027.336.430.33.03.039.421.221.215.23.0
Subjects on Ospemifine 15 mg/Day (Week 12)55.224.117.20.03.437.948.310.30.03.444.844.86.90.03.451.737.96.90.03.451.727.617.20.03.4
Subjects on Placebo14.747.126.511.80.08.844.141.25.90.08.841.238.211.80.08.847.138.25.90.08.852.926.511.80.0
Subjects on Placebo (Week 12)35.329.426.58.80.014.747.135.32.90.020.632.441.25.90.023.541.232.42.90.020.641.226.511.80.0

[back to top]

Mean Change From Baseline in Percentage of Superficial Cells in the Maturation Index

(NCT00630539)
Timeframe: Week 4

Interventionpercentage of superficial cells (Mean)
Subjects on Placebo0.6
Subjects on Ospemifene 5 mg/Day0.6
Subjects on Ospemifene 15 mg/Day2.5
Subjects on Ospemifene 30 mg/Day5.0

[back to top]

Mean Change From Baseline in Percentage of Superficial Cells in Maturation Index of the Vaginal Smear

(NCT00630539)
Timeframe: 12 weeks

Interventionpercentage of superficial cells (Mean)
Subjects on Placebo0.2
Subjects on Ospemifene 5 mg/Day0.9
Subjects on Ospemifene 15 mg/Day5.0
Subjects on Ospemifene 30 mg/Day5.6

[back to top]

Mean Change From Baseline in Percentage of Parabasal Cells in the Maturation Index

(NCT00630539)
Timeframe: Week 4

Interventionpercentage of parabasal cells (Mean)
Subjects on Placebo-0.6
Subjects on Ospemifene 5 mg/Day-0.6
Subjects on Ospemifene 15 mg/Day-19.7
Subjects on Ospemifene 30 mg/Day-22.0

[back to top]

Mean Change From Baseline in Luteinizing Hormone Levels

(NCT00630539)
Timeframe: Week 12

InterventionU/L (Mean)
Subjects on Placebo-1.36
Subjects on Ospemifene 5 mg/Day-2.89
Subjects on Ospemifene 15 mg/Day-0.34
Subjects on Ospemifene 30 mg/Day-3.78

[back to top]

Mean Change From Baseline in Follicle Stimulating Hormone Levels

(NCT00630539)
Timeframe: Week 12

InterventionU/L (Mean)
Subjects on Placebo-10.36
Subjects on Ospemifene 5 mg/Day-7.04
Subjects on Ospemifene 15 mg/Day-5.99
Subjects on Ospemifene 30 mg/Day-15.32

[back to top]

Mean Change From Baseline in Estradiol Levels

(NCT00630539)
Timeframe: Week 12

Interventionnmol/L (Mean)
Subjects on Placebo-0.004
Subjects on Ospemifene 5 mg/Day0.004
Subjects on Ospemifene 15 mg/Day-0.010
Subjects on Ospemifene 30 mg/Day-0.003

[back to top]

Change in Cognitive Function Over 1 Year in Premenopausal Breast Cancer Patients Who Receive Adjuvant Tamoxifen (T) Alone Against Those Receive Adjuvant Tamoxifen (T+OFS) or Exemestane (E+OFS) With Ovarian Function Suppression (OFS)

Objective cognitive function measured with CogState, a computerized test battery of 7 tasks: Detection, Identification, Monitoring, Memory, Learning, International Shopping List Task (ISLT) and ISLT-Delayed Recall. Performance speed is measured for Detection/Identification/Monitoring and performance accuracy is measured for Memory/Learning/ISLT/ISLT-Delayed Recall. Performance speed calculated as mean of the log10 transformed reaction time for correct responses (lower score=better); performance accuracy calculated as arcsine transformation of the proportion of correct responses (higher scores=better). Main outcome measure is a composite score (average of task scores after transformation and standardization by age-specific norms). A positive standardized score indicates that a patient performed better than average; a negative standardized score indicates below average results. Patients complete assessments at baseline and 1 year after randomization to parent IBCSG 24-02 (SOFT) study. (NCT00659373)
Timeframe: 1 year after patient randomization to parent IBCSG 24-02 study

Interventionstandardized units (Mean)
Tamoxifen-.04
Ovarian Function Suppression-0.21

[back to top]

Mean Change From Baseline on the Geriatric Depression Scale Scores by Treatment Group

"Mean Change From Baseline on the Geriatric Depression Scale. Adjusted for age, ethnicity, education, and baseline measure, for participants with true baseline measures.~Measures depression in older adults. Mood is also assessed with the 15-item short form of the GDS which measures non-somatic features of depressed mood. Participants indicate the presence or absence of each symptom. The GDS-SF score is the total number of positive depressive items. Score range is 0-15, with 0-4 denoting better outcomes and a score of 5 and above denoting worse outcomes (depression)." (NCT00687102)
Timeframe: Baseline and 3 Years

Interventionunits on a scale (Mean)
Star Participants Assigned to Tamoxifen0.57
Star Participants Assigned to Raloxifene0.13

[back to top]

Mean Change From Baseline on Card Rotations Test Scores by Treatment Group

"Mean Change From Baseline on the Card Rotations Test scores. Adjusted for age, ethnicity, education, and baseline measure, for participants with true baseline measures.~Measures the ability to mentally manipulate figures in two and three-dimensions. On each of 28 trials, participants view sample line drawings of a geometric figure and 8 alterations representing 2 or 3-dimensional rotations of the drawing. Participants are asked to identify alternatives that show the sample in 2-D but not in 3-D. Total range 0 - 160 and the number of incorrect/correct responses is measure. Higher number of correct answers is a better outcome." (NCT00687102)
Timeframe: Baseline and 3 Years

Interventioncorrect responses (Mean)
Star Participants Assigned to Tamoxifen6.10
Star Participants Assigned to Raloxifene5.40

[back to top]

Mean Change From Baseline on the Finger Tapping Test Scores by Treatment Group

"Mean Change From Baseline on the the Finger Tapping Test scores. Adjusted for age, ethnicity, education, and baseline measure, for participants with true baseline measures.~Measures motor speed, coordination, attention, alertness, slowing of responses, and motor control. In this test of motor speed and dexterity participants are asked to depress a lever as many times as possible in each of 7, 10-second trials, first with the right hand and next with the left hand. The highest and lowest scores are dropped; the score is the average of the remaining five trials for each hand.Higher scores represent better outcomes." (NCT00687102)
Timeframe: Baseline and 3 Years

,
Interventionfinger taps (Mean)
Fine Tapping, DominantFine Tapping, Non-Dominant
Star Participants Assigned to Raloxifene-0.04-0.45
Star Participants Assigned to Tamoxifen0.26-0.18

[back to top]

Mean Change From Baseline on the Letter Fluency and Semantic Fluency Scores by Treatment Group

"Mean Change From Baseline on the Letter Fluency Test scores. Adjusted for age, ethnicity, education, and baseline measure, for participants with true baseline measures.~Measures cognitive function. In this test, the participant names as many words as possible in 1 minute, beginning with each letter for letter fluency (F, A, and S) and category for semantic fluency (fruits and vegetables). To score the administrator, counts up the total number letters or words that the individual is able to produce. The score minimum would be 0 and the maximum would be the total of correct items named within 1 minute. Higher scores represent better outcomes." (NCT00687102)
Timeframe: Baseline and 3 Years

,
Interventionchange in number of words (Mean)
Letter FluencySemantic Fluency
Star Participants Assigned to Raloxifene1.51-.56
Star Participants Assigned to Tamoxifen1.29-.51

[back to top]

Mean Change From Baseline on the Positive and Negative Affect Schedule Scores by Treatment Group

"Mean Change From Baseline on the Positive and Negative Affect Schedule (PANAS). Adjusted for age, ethnicity, education, and baseline measure, for participants with true baseline measures.~Measures positive and negative affect. Mood is assessed with the PANAS, a list of ten pleasant mood states (e.g., interested, proud, inspired) and ten unpleasant mood states (e.g., irritable, guilty, jittery). Respondents are asked to rate on a 5-point scale (1 being very slightly or not at all and 5 being extremely) the extent to which they have experienced each mood during a specific time frame. Ratings for each item can range from 0 to 4 with total scores for positive affect and negative affect subscales ranging from 0 to 40. For positive affect, higher scores denote higher levels of positive affect and for negative affect, lower scores denote lower levels of negative affect." (NCT00687102)
Timeframe: Baseline and 3 Years

,
Interventionunits on a scale (Mean)
PANAS-positivePANAS-negative
Star Participants Assigned to Raloxifene-0.04-0.06
Star Participants Assigned to Tamoxifen-0.100.00

[back to top]

Mean Change From Baseline on the the Benton Visual Retention Test Scores by Treatment Group

"Mean Change From Baseline on the Benton Visual Retention (BVRT) Test scores. Adjusted for age, ethnicity, education, and baseline measure, for participants with true baseline measures.~The BVRT measures short term visual memory and visuo-constructional abilities. Each of 10 designs was presented one at a time for 10 seconds, and immediately after the design was withdrawn, the participant was instructed to draw it from memory on a blank sheet of paper. The score on the BVRT is the total number of errors, 0-26 represents the total number of theoretically possible errors. Lower score denotes better outcomes." (NCT00687102)
Timeframe: Baseline and 3 Years

InterventionNumber of errors (Mean)
Star Participants Assigned to Tamoxifen-0.73
Star Participants Assigned to Raloxifene-1.41

[back to top]

Mean Change From Baseline on the the California Verbal Learning Test Scores by Treatment Group

"Adjusted for age, ethnicity, education, and baseline measure, for participants with true baseline measures.~The experimenter reads a list of 16 nouns aloud, at one-second intervals, in fixed order, over 3 learning trials (list A) . After each trial, the subject is asked to recall as many words as they can in any order (i.e., free recall) given a score 0-16 each. Total range as the sum of the 3 learning trials: 0 - 48. Participants were asked to recall a second interference list (List B) with a score range of 0-16. Free recall of list A are tested immediately after list B (short-delay) Total range 0- 16 , and again after 20 minutes (long-delay) 0-16. Each part of the scale is reported separately as Total List A trials, Total List B trials, Short-delay free recall, and Long-delay free recall." (NCT00687102)
Timeframe: Baseline and 3 Years

,
Interventioncorrect responses (Mean)
Total List A trialsTotal List B trialsShort-delay free recallLong-delay free recall
Star Participants Assigned to Raloxifene-1.89-1.74-0.360.10
Star Participants Assigned to Tamoxifen-3.31-1.56-0.96-0.23

[back to top]

Mean Change From Baseline on Digit Span Test Scores by Treatment Group

"Mean Change From Baseline on the Digit Span Test - Digits Forward and Digits backward Test scores. Adjusted for age, ethnicity, education, and baseline measure, for participants with true baseline measures.~Measures reasoning, verbal ability, and memory. The participant is asked to provide immediate recall of a series of digits in forward and backward sequences. The individual's score is the total number of items correctly repeated forwards or backwards. Total range 0 - 14, higher results denotes a better outcome." (NCT00687102)
Timeframe: Baseline and 3 Years

,
Interventionunits on a scale (Mean)
Digits ForwardDigits Backward
Star Participants Assigned to Raloxifene-0.08-0.27
Star Participants Assigned to Tamoxifen-0.02-0.16

[back to top]

Number of Participants With Freedom From Progression of Cancer at 4 Months

"Clinical Assessments were performed every 4 weeks and imaging every 8 weeks or earlier if indicated.~Patients were followed every month for clinical symptoms and signs of progression.~Patients underwent Radiographic CT scans every 8 weeks to look for progression." (NCT00710970)
Timeframe: Estimated from date of starting therapy until 4 months but up to progression or death which ever comes first.

InterventionParticipants (Count of Participants)
Single Arm Receiving 25mg Tamoxifen20

[back to top]

12-Month Survival Rate

The 12-month survival rate is defined as the percentage of participants who have not died 12 months after the date of randomization. (NCT00728949)
Timeframe: From randomization to until the date of first documented date of death from any cause within 12 months, assessed up to 35.1 months

Interventionpercentage of participants (Number)
IMC-A12 (Cixutumumab) + Antiestrogen Therapy15
IMC-A12 (Cixutumumab)7.6

[back to top]

Overall Survival (OS)

OS is defined as the interval between date of randomization and the date of death due to any cause. Participants who are alive at the time of study completion will be censored at the time the participants was last known to be alive. (NCT00728949)
Timeframe: From randomization up to 36.5 Months

Interventionmonths (Median)
IMC-A12 (Cixutumumab) + Antiestrogen Therapy20.3
IMC-A12 (Cixutumumab)NA

[back to top]

Percentage of Participants With Complete Response (CR) and Partial Response (PR) or Stable Disease (SD) Disease Control Rate [DCR])

DCR is defined as percentage of participants with CR, PR, or SD using RECIST v 1.0 criteria. CR: disappearance of all lesions, pathological lymph node reduction in short axis to <10 mm, and normalization of tumor marker levels of non-target lesions. PR: ≥30% decrease in SOD of target lesions taking as reference baseline sum diameter. PD: ≥20% increase in SOD of target lesions and short axes of target lymph nodes, taking as reference smallest sum of longest diameters recorded since treatment started and an absolute increase in sum diameter ≥5 mm; appearance of ≥1 new lesions and/or unequivocal progression of existing non-target lesions. SD: neither sufficient shrinkage to qualify for PR nor increase to qualify for PD. Participants who had no post baseline tumor assessments were considered non-responders and included in the denominator when calculating response rate. Percentage of participants=(number of participants with CR+PR+SD/total number of participants)*100. (NCT00728949)
Timeframe: Randomization to PD up to 35.1 Months

Interventionpercentage of participants (Number)
IMC-A12 (Cixutumumab) + Antiestrogen Therapy40.3
IMC-A12 (Cixutumumab)51.6

[back to top]

Number of Participants Experiencing Adverse Events (AEs) in National Cancer Institute Common Toxicity Criteria for AE's (NCI-CTCAE) Version 3.0 Criteria for Adverse Events (NCI-CTCAE)

The NCI-CTCAE provides descriptive terminology for adverse event reporting. A grading (severity) scale is provided for each adverse event term. Severity will be graded as mild (grade 1), moderate (grade 2), severe (grade 3), or very severe (life threatening - grade 4). Clinically significant events were defined as serious and other non-serious adverse events related to study drug regardless of causality. A summary of serious and other non-serious adverse events is located in the Reported Adverse Event module. (NCT00728949)
Timeframe: Randomization to End of Study up to 36.5 Months

,
InterventionParticipants (Count of Participants)
Participants with any AEParticipants with SAE'sAE of greater than Grade 3AE with outcome of DeathStudy drug-related AEStudy drug-related SAE'sStudy drug-related AE of greater than Grade 3AE leading to discontinuation of any study drug
IMC-A12 (Cixutumumab)361119231271
IMC-A12 (Cixutumumab) + Antiestrogen Therapy5516223485106

[back to top]

Progression-Free Survival (PFS)

PFS is defined as the time from the date of randomization until date of objectively determined progressive disease (PD) or death due to any cause. Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0), as a ≥20% increase in the sum of the longest diameter of target lesions, or a measurable increase in a non-target lesion, or the appearance of new lesions unequivocal progression of non-target lesions. Participants without documentation of progression or death will be censored at the date of last tumor assessment. The PFS will be estimated following the Kaplan-Meier method. (NCT00728949)
Timeframe: From randomization up to 35.1 Months

Interventionmonths (Median)
IMC-A12 (Cixutumumab) + Antiestrogen Therapy2.0
IMC-A12 (Cixutumumab)3.1

[back to top]

Percentage of Participants With Complete Response (CR) and Partial Response (PR) (Objective Response Rate [ORR])

Best overall response of CR or PR was defined using RECIST v 1.0 criteria. CR was defined as the disappearance of all lesions, pathological lymph node reduction in short axis to <10 mm, and normalization of tumor marker levels of non-target lesions. PR was defined as ≥30% decrease in sum of longest diameter (SOD) of target lesions taking as reference the baseline sum diameter. PD was defined as ≥20% increase in SOD of target lesions and short axes of target lymph nodes, taking as reference the smallest sum of the longest diameters recorded since treatment started and an absolute increase in sum diameter of ≥5 mm; appearance of ≥1 new lesions and/or unequivocal progression of existing non-target lesions. Participants who had no post baseline tumor assessments were considered non-responders and included in the denominator when calculating response rate. Percentage of participants=(number of participants with CR+PR/total number of participants)*100. (NCT00728949)
Timeframe: Randomization to PD up to 35.1 Months

Interventionpercentage of participants (Number)
IMC-A12 (Cixutumumab) + Antiestrogen Therapy1.6
IMC-A12 (Cixutumumab)0

[back to top]

Incidence of Adverse Effects (Grade 3 or Higher) as Assessed by Common Terminology Criteria for Adverse Events Version 3.0

Number of participants with a maximum grade of 3 or higher during the treatment period. (NCT00729586)
Timeframe: Assessed every 6 weeks while on treatment, 30 days after the last cycle of treatment.

InterventionParticipants (Count of Participants)
Arm 1: Temsirolimus29
Arm 2: Megestrol Acetate+Tamoxifen+ Temsirolimus15

[back to top]

Duration of Progression-free Survival (PFS)

Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0), as a 20% increase in the sum of the longest diameter of target lesions assessed radiographically and 50% increase if the only target lesion is a solitary pelvic mass measured by physical exam, or unequivocal progression of a non-target lesion, or the appearance of new lesions. (NCT00729586)
Timeframe: Radiologic tumor evaluations at baseline and every six weeks for the first 24 weeks and then repeated every 12 weeks until disease progression. Repeat after treatment discontinuation if patient was taken off study for reasons other than progression.

Interventionmonths (Median)
Arm 1: Temsirolimus5.6
Arm 2: Megestrol Acetate+Tamoxifen+ Temsirolimus4.2

[back to top]

Duration of Overall Survival (OS)

Overall survival is defined as the duration of time from study entry to time of death or the date of last contact. (NCT00729586)
Timeframe: Every 6 weeks during treatment, then every 3 months for one year.

Interventionmonths (Median)
Arm 1: Temsirolimus13.3
Arm 2: Megestrol Acetate+Tamoxifen+ Temsirolimus9.6

[back to top]

Percentage of Participants With a Confirmed Objective Tumor Response Using RECIST Version 1.0

RECIST 1.0 defines complete response as the disappearance of all target lesions and non-target lesions and no evidence of new lesions documented by two disease assessments at least 4 weeks apart. Partial response is defined as at least a 30% decrease in the sum of longest dimensions (LD) of all target measurable lesions taking as reference the baseline sum of LD. There can be no unequivocal progression of non-target lesions and no new lesions. Documentation by two disease assessments at least 4 weeks apart is required. In the case where the ONLY target lesion is a solitary pelvic mass measured by physical exam, which is not radiographically measurable, a 50% decrease in the LD is required. These patients will have their response classified according to the definitions stated above. Complete and partial responses are included in the objective tumor response rate. (NCT00729586)
Timeframe: Radiologic tumor evaluations at baseline and every 6 weeks for the first 24 weeks; then repeated every 12 weeks until disease progression. Repeat after treatment discontinuation if patient was taken off study for reasons other than progression.

Interventionpercentage of participants (Number)
Arm 1: Temsirolimus22
Arm 2: Megestrol Acetate+Tamoxifen+ Temsirolimus14.3

[back to top]

Number of Participants and Their Levels of Expression of the Candidate Markers

The levels of expression of the candidate markers measured prior to study treatment are tabulated. The expressions being tabulated include immunohistochemical expression of hormone receptors. The hormone receptors are estrogen receptor positive, progesterone receptors-A, progesterone receptor-B, PAKT Positive and PTEN Positive. The associations between the immunohistochemical expression of these biomarkers and between these biomarkers and treatment, outcome or clinical characteristics are reported for future investigation. (NCT00729586)
Timeframe: Baseline

Interventionparticipants (Number)
Estrogen Receptor PositiveProgesterone Receptor PositiveProgesterone Receptor B PositivePAKT PositivePTEN Positive
Receptor Analysis2030351130

[back to top]

Patient Understanding of Pharmacogenomics

To examine patients' beliefs about how hypothetical genotype information would affect their perceived recurrence risk and benefits of tamoxifen therapy, participants were given experimentally manipulated 6 vignettes to describe hypothetical tamoxifen treatment (no or yes) and hypothetical genotype (EM, IM or PM). For each vignette, participants gave their perceived recurrence risk (RR; 0-100%) (NCT00764322)
Timeframe: baseline

Interventionpercent chance of recurrence (Mean)
Perceived RR -No tamoxifen/EMPerceived RR -No tamoxifen/iMPerceived RR -No tamoxifen/PMPerceived RR - tamoxifen/EMPerceived RR -tamoxifen/IMPerceived RR -tamoxifen/PM
All Participants474853223040

[back to top]

Change in Median Endoxifen Concentrations to Determine Feasibility of Obtaining Pharmacogenomic Information From Patients in the Clinical Setting and Using it to Guide Changes in Therapy

If the key active tamoxifen metabolite, endoxifen, could be significantly increased by genotype-guided tamoxifen dosing in patients with intermediate CYP2D6 metabolism (by increasing tamoxifen dosing based on CYP2D6 genotype), then the study would be deemed feasible and the accrual expanded. (NCT00764322)
Timeframe: Baseline and 4 months after dose increase

Interventionng/mL (Median)
Extensive Metabolizers-1.5
Intermediate Metabolizers7.6
Poor Metabolizers6.1

[back to top]

Change in Plasma Endoxifen Levels After an Increase in Tamoxifen Citrate Dose From 20 mg to 40 mg Daily in Patients With Poor-metabolizing Genotypes

The intrapatient change in median endoxifen levels were calculated between baseline and 4 months after the increase in dose of Tamoxifen from 20mg/day to 40 mg/day (NCT00764322)
Timeframe: Baseline and 4 months after dose increase

Interventionng/mL (Median)
Poor Metabolizers6.1

[back to top]

CYP2D6 Allele Frequencies and Endoxifen Levels Among African-American Women Taking Tamoxifen Citrate

Mean endoxifen levels by CYP2D6 genotype among African Americans. Measurements of plasma concentrations of the key active metabolite of tamoxifen, endoxifen, were measured at baseline.The most common CYP2D6 alleles have been grouped by functional activity classifications with descending activity: ultra-rapid (UM), extensive (EM), intermediate (IM) or poor (PM) metabolism. A given patient has two alleles, giving them 10 possible allelic combinations, or diplotypes (UM/UM, UM/EM, EM/EM, etc.). These diplotypes are collapsed into four phenotypes, UM, EM, IM or PM. (NCT00764322)
Timeframe: baseline

Interventionng/ml (Mean)
UMEMIMPM
African Americans14.589.697.090.8

[back to top]

Endoxifen Concentrations in Participants Receiving Tamoxifen Citrate Dose of 20 mg or 40 mg Stratified by the Metabolizing CYP2D6 Genotypes

Measurements of plasma concentrations of the key active metabolite of tamoxifen, endoxifen, were measured at baseline and after 4 months of treatment; The most common CYP2D6 alleles have been grouped by functional activity classifications with descending activity: ultra-rapid (UM), extensive (EM), intermediate (IM) or poor (PM) metabolism. A given patient has two alleles, giving them 10 possible allelic combinations, or diplotypes (UM/UM, UM/EM, EM/EM, etc.). These diplotypes are collapsed into four phenotypes, UM, EM, IM or PM. (NCT00764322)
Timeframe: 4 months

,,,
Interventionng/mL (Mean)
Baseline endoxifen concentration4-Month endoxifen concentration
Extensive Metabolizers10.009.30
Intermediate Metabolizers7.1010.74
Poor Metabolizers3.425.52
Ultra-rapid Metabolizers8.415.35

[back to top]

Number of Participants With Pulmonary Embolism (PE), Deep Vein Thrombosis (DVT), Stroke, and/or Endometrial Cancer

"The doubling of tamoxifen dose is defined as unacceptable (i.e., not tolerable) if the prevalence of Pulmonary embolism (PE), Deep vein thrombosis (DVT), stroke, or endometrial cancer, either individually or in any combination, is greater than 2%." (NCT00764322)
Timeframe: Approximately ten months from registration to last follow-up

,
InterventionParticipants (Count of Participants)
Pulmonary embolism (PE)Deep vein thrombosis (DVT)StrokeEndometrial cancer
Tamoxifen 200000
Tamoxifen 400000

[back to top]

Median of 6 Month Tamoxifen Steady State Plasma Concentrations According to CYP2D6 Phenotype Group

"Participants were classified as having CYP2D6 decreased or non-decreased metabolism based on genotype and the co-prescription of inhibitors of the enzyme system.~The specific phenotype, alleles and their associated activity score (AS) assessed were as follows:~Ultrarapid metabolism (UM) or AS=2.0 (*1XN or *2XN), Extensive metabolism (EM) or AS=1.0 (*1, *2, and *2A), Intermediate metabolism (IM) or AS=0.5 (*9, *10, *17 and *41), and Poor metabolism (PM) or AS=0.0 (3, *4, *5, *7, *8, *11, and *12). The median of 6 month Tamoxifen steady state plasma concentrations for each CYP2D6 phenotype group are summarized below. Refer to Outcome Measure 1 Data Table for details on the combination of genotype for each participant that are defined for each CYP2D6 phenotype group." (NCT00873366)
Timeframe: 6 Month

InterventionnM (Median)
PM/PMIM/PMIM/IMPM/EMEM/IMEM/EMEM/UM
¹³C-DM-BT194.0200.5279.2259.7234.7179.7301.4

[back to top]

Operating Characteristics of the ¹³C-dextromethorphan (13C-DM) Breath Test in Identifying Those Who Are CYP2D6 Genotypic Poor Metabolizers

"Participants were classified as having CYP2D6 decreased or non-decreased metabolism based on genotype and the co-prescription of inhibitors of the enzyme system.~The specific phenotype, alleles and their associated activity score (AS) assessed were as follows:~Ultrarapid metabolism (UM) or AS=2.0 (*1XN or *2XN), Extensive metabolism (EM) or AS=1.0 (*1, *2, and *2A), Intermediate metabolism (IM) or AS=0.5 (*9, *10, *17 and *41), and Poor metabolism (PM) or AS=0.0 (3, *4, *5, *7, *8, *11, and *12). The distribution of CYP2D6 genotypes grouped by CYP2D6 metabolism phenotype for each participants are summarized below." (NCT00873366)
Timeframe: Baseline

InterventionParticipants (Count of Participants)
EM/UM (*1/*2AXN)EM/UM (*1/*1XN)IM/UM (*41/*2AXN)EM/EM (*1/*1)EM/EM (*1/*2A)EM/EM (*1/*2)EM/EM (*2/*2)EM/EM (*2A/*2A)EM/IM (*1/*9)EM/IM (*1/*10)EM/IM (*1/*41)EM/IM (*2A/*9)EM/IM (*2A/*41)EM/PM (*1/*3)EM/PM (*1/*4)EM/PM (*2/*4)EM/PM (*2/*4XN)EM/PM (*2A/*4)EM/PM (*2A/*5)EM/PM (*2A/*6)IM/IM (*41/*41)IM/PM (*3/*41)IM/PM (*4/*9)IM/PM (*4/*10)IM/PM (*4/*41)PM/PM (*3/*4)PM/PM (*4/*4)
¹³C-DM-BT11112132122371218116111111411

[back to top]

Spearman's Rank Correlation Coefficient Between CYP2D6 Activity Score and Endoxifen Steady State Concentrations (Endx Css)

Spearman rank order correlation coefficients were used to assess the strength of the association between CYP2D6 genotype activity score and Endx Css (NCT00873366)
Timeframe: 3 Month and 6 Month

InterventionCorrelation coefficient (Number)
3 Month6 Month
¹³C-DM-BT0.470.56

[back to top]

Spearman's Rank Correlation Coefficient Between CYP2D6 Activity Score and Endoxifen/N-desmethyl-tamoxifen (Endx/NDMT) Ratio

Spearman rank order correlation coefficients were used to assess the strength of the association between CYP2D6 genotype activity score and Endx/NDMT ratio (NCT00873366)
Timeframe: 3 Month and 6 Month

InterventionCorrelation coefficient (Number)
3 Month6 Month
¹³C-DM-BT0.600.61

[back to top]

Spearman's Rank Correlation Coefficient Between CYP2D6 Genotype and ¹³Cdextromethorphan Breath Test (DM-BT)

Spearman rank order correlation coefficients were used to assess the strength of the association between CYP2D6 genotype activity score and DM-BT values. (NCT00873366)
Timeframe: Baseline, 3 month and 6 month

InterventionCorrelation coefficient (Number)
Baseline3 Month6 Month
¹³C-DM-BT0.550.580.55

[back to top]

Spearman's Rank Correlation Coefficient Between 3 Month DM-BT and 3 Month Endoxifen Steady State Concentrations

Spearman rank order correlation coefficients were used to assess the strength of the association between baseline ¹³Cdextromethorphan breath test (DM-BT) and Endoxifen steady state concentrations (Endx Css) (NCT00873366)
Timeframe: 3 month

InterventionCorrelation coefficient (Number)
¹³C-DM-BT0.51

[back to top]

Spearman's Rank Correlation Coefficient Between 6 Month DM-BT and 6 Month Endoxifen Steady State Concentrations

Spearman rank order correlation coefficients were used to assess the strength of the association between baseline ¹³Cdextromethorphan breath test (DM-BT) and Endoxifen steady state concentrations (Endx Css) (NCT00873366)
Timeframe: 6 month

InterventionCorrelation coefficient (Number)
¹³C-DM-BT0.54

[back to top]

Spearman's Rank Correlation Coefficient Between Baseline DM-BT and 3 Month Endoxifen Steady State Concentrations

Spearman rank order correlation coefficients were used to assess the strength of the association between baseline ¹³Cdextromethorphan breath test (DM-BT) and Endoxifen steady state concentrations (Endx Css) (NCT00873366)
Timeframe: Baseline, 3 month

InterventionCorrelation coefficient (Number)
¹³C-DM-BT0.6

[back to top]

Spearman's Rank Correlation Coefficient Between Baseline DM-BT and 3 Month Endoxifen/N-desmethyl-tamoxifen (Endx/NDMT) Ratio

Spearman rank order correlation coefficients were used to assess the strength of the association between baseline ¹³Cdextromethorphan breath test (DM-BT) and Endoxifen/N-desmethyl-tamoxifen (Endx/NDMT) Ratio (NCT00873366)
Timeframe: Baseline, 3 month

InterventionCorrelation coefficient (Number)
¹³C-DM-BT0.56

[back to top]

Median of 3 Month 4-hydroxy-tamoxifen (4HT) Steady State Plasma Concentrations According to CYP2D6 Phenotype Group

"Participants were classified as having CYP2D6 decreased or non-decreased metabolism based on genotype and the co-prescription of inhibitors of the enzyme system.~The specific phenotype, alleles and their associated activity score (AS) assessed were as follows:~Ultrarapid metabolism (UM) or AS=2.0 (*1XN or *2XN), Extensive metabolism (EM) or AS=1.0 (*1, *2, and *2A), Intermediate metabolism (IM) or AS=0.5 (*9, *10, *17 and *41), and Poor metabolism (PM) or AS=0.0 (3, *4, *5, *7, *8, *11, and *12). The median of 3 month 4HT steady state plasma concentrations for each CYP2D6 phenotype group are summarized below. Refer to Outcome Measure 1 Data Table for details on the combination of genotype for each participant that are defined for each CYP2D6 phenotype group." (NCT00873366)
Timeframe: 3 Month

InterventionnM (Median)
PM/PMIM/PMIM/IMPM/EMEM/IMEM/EMEM/UM
¹³C-DM-BT3.131.53.523.625.413.644.21

[back to top]

Median of 3 Month Endoxifen Steady State Concentrations (Endx Css) According to CYP2D6 Phenotype Group and Activity Score

"Participants were classified as having CYP2D6 decreased or non-decreased metabolism based on genotype and the co-prescription of inhibitors of the enzyme system.~The specific phenotype, alleles and their associated activity score (AS) assessed were as follows:~Ultrarapid metabolism (UM) or AS=2.0 (*1XN or *2XN), Extensive metabolism (EM) or AS=1.0 (*1, *2, and *2A), Intermediate metabolism (IM) or AS=0.5 (*9, *10, *17 and *41), and Poor metabolism (PM) or AS=0.0 (3, *4, *5, *7, *8, *11, and *12). The median of 3 month Endx Css for each CYP2D6 phenotype group and the corresponding activity score are summarized below. Refer to Outcome Measure 1 Data Table for details on the combination of genotype for each participant that are defined for each CYP2D6 phenotype group." (NCT00873366)
Timeframe: 3 Month

InterventionnM (Median)
EM/UM (3.0)EM/EM (2.0)EM/IM (1.5)IM/IM (1.0)EM/PM (1.0)IM/PM (0.5)PM/PM (0)
¹³C-DM-BT23.630.527.911.521.56.15.5

[back to top]

Median of 3 Month N-desmethyl-tamoxifen (NDMT) Steady State Plasma Concentrations According to CYP2D6 Phenotype Group

"Participants were classified as having CYP2D6 decreased or non-decreased metabolism based on genotype and the co-prescription of inhibitors of the enzyme system.~The specific phenotype, alleles and their associated activity score (AS) assessed were as follows:~Ultrarapid metabolism (UM) or AS=2.0 (*1XN or *2XN), Extensive metabolism (EM) or AS=1.0 (*1, *2, and *2A), Intermediate metabolism (IM) or AS=0.5 (*9, *10, *17 and *41), and Poor metabolism (PM) or AS=0.0 (3, *4, *5, *7, *8, *11, and *12). The median of 3 month NDMT steady state plasma concentrations for each CYP2D6 phenotype group are summarized below. Refer to Outcome Measure 1 Data Table for details on the combination of genotype for each participant that are defined for each CYP2D6 phenotype group." (NCT00873366)
Timeframe: 3 Month

InterventionnM (Median)
PM/PMIM/PMIM/IMPM/EMEM/IMEM/EMEM/UM
¹³C-DM-BT633.3578.0691.6643.0630.7457.8576.9

[back to top]

Median of 3 Month Tamoxifen Steady State Plasma Concentrations According to CYP2D6 Phenotype Group

"Participants were classified as having CYP2D6 decreased or non-decreased metabolism based on genotype and the co-prescription of inhibitors of the enzyme system.~The specific phenotype, alleles and their associated activity score (AS) assessed were as follows:~Ultrarapid metabolism (UM) or AS=2.0 (*1XN or *2XN), Extensive metabolism (EM) or AS=1.0 (*1, *2, and *2A), Intermediate metabolism (IM) or AS=0.5 (*9, *10, *17 and *41), and Poor metabolism (PM) or AS=0.0 (3, *4, *5, *7, *8, *11, and *12). The median of 3 month Tamoxifen steady state plasma concentrations for each CYP2D6 phenotype group are summarized below. Refer to Outcome Measure 1 Data Table for details on the combination of genotype for each participant that are defined for each CYP2D6 phenotype group." (NCT00873366)
Timeframe: 3 Month

InterventionnM (Median)
PM/PMIM/PMIM/IMPM/EMEM/IMEM/EMEM/UM
¹³C-DM-BT219.6233.8272.3257.7279.1201.0313.3

[back to top]

Median of 6 Month 4-hydroxy-tamoxifen (4HT) Steady State Plasma Concentrations According to CYP2D6 Phenotype Group

"Participants were classified as having CYP2D6 decreased or non-decreased metabolism based on genotype and the co-prescription of inhibitors of the enzyme system.~The specific phenotype, alleles and their associated activity score (AS) assessed were as follows:~Ultrarapid metabolism (UM) or AS=2.0 (*1XN or *2XN), Extensive metabolism (EM) or AS=1.0 (*1, *2, and *2A), Intermediate metabolism (IM) or AS=0.5 (*9, *10, *17 and *41), and Poor metabolism (PM) or AS=0.0 (3, *4, *5, *7, *8, *11, and *12). The median of 6 month 4HT steady state plasma concentrations for each CYP2D6 phenotype group are summarized below. Refer to Outcome Measure 1 Data Table for details on the combination of genotype for each participant that are defined for each CYP2D6 phenotype group." (NCT00873366)
Timeframe: 6 Month

InterventionnM (Median)
PM/PMIM/PMIM/IMPM/EMEM/IMEM/EMEM/UM
¹³C-DM-BT3.171.691.53.815.862.965.38

[back to top]

Median of 6 Month Endoxifen Steady State Concentrations (Endx Css) According to CYP2D6 Phenotype Group and Activity Score

"Participants were classified as having CYP2D6 decreased or non-decreased metabolism based on genotype and the co-prescription of inhibitors of the enzyme system.~The specific phenotype, alleles and their associated activity score (AS) assessed were as follows:~Ultrarapid metabolism (UM) or AS=2.0 (*1XN or *2XN), Extensive metabolism (EM) or AS=1.0 (*1, *2, and *2A), Intermediate metabolism (IM) or AS=0.5 (*9, *10, *17 and *41), and Poor metabolism (PM) or AS=0.0 (3, *4, *5, *7, *8, *11, and *12). The median of 6 month Endx Css for each CYP2D6 phenotype group and the corresponding activity score are summarized below. Refer to Outcome Measure 1 Data Table for details on the combination of genotype for each participant that are defined for each CYP2D6 phenotype group." (NCT00873366)
Timeframe: 6 Month

InterventionnM (Median)
EM/UM (3.0)EM/EM (2.0)EM/IM (1.5)IM/IM (1.0)EM/PM (1.0)IM/PM (0.5)PM/PM (0)
¹³C-DM-BT38.526.730.411.319.14.76.7

[back to top]

Median of 6 Month N-desmethyl-tamoxifen (NDMT) Steady State Plasma Concentrations According to CYP2D6 Phenotype Group

"Participants were classified as having CYP2D6 decreased or non-decreased metabolism based on genotype and the co-prescription of inhibitors of the enzyme system.~The specific phenotype, alleles and their associated activity score (AS) assessed were as follows:~Ultrarapid metabolism (UM) or AS=2.0 (*1XN or *2XN), Extensive metabolism (EM) or AS=1.0 (*1, *2, and *2A), Intermediate metabolism (IM) or AS=0.5 (*9, *10, *17 and *41), and Poor metabolism (PM) or AS=0.0 (3, *4, *5, *7, *8, *11, and *12). The median of 6 month NDMT steady state plasma concentrations for each CYP2D6 phenotype group are summarized below. Refer to Outcome Measure 1 Data Table for details on the combination of genotype for each participant that are defined for each CYP2D6 phenotype group." (NCT00873366)
Timeframe: 6 Month

InterventionnM (Median)
PM/PMIM/PMIM/IMPM/EMEM/IMEM/EMEM/UM
¹³C-DM-BT554.6542.4718.2546.5525.9401.8552.9

[back to top]

Difference in Mean Score for Vasomotor Symptoms Including Hot Flashes From Baseline to Time of Surgery

Hot flashes were assessed by the Breast Cancer Prevention Trial Eight Symptom Scale (BESS) questionnaire. This questionnaire measures the incidence of a number of symptoms by asking participants how frequently they experienced them on a scale of 0-4 (0 being Not at All and 4 being Extremely often). BESS questionnaire was administered at baseline and time of surgery. The incidence of vasomotor symptoms (including hot flashes, night sweats, and cold sweats) was measured at baseline (Day 0) and end of treatment prior to surgery (at least 4 weeks later or up to 10 weeks, depending on scheduled surgery date), and changes in the mean score for hot flashes were observed. (NCT00952731)
Timeframe: Baseline and after 4-10 weeks of treatment

Interventionunits on a scale (Mean)
Treatment Gel + Oral Placebo0.33
Placebo Gel + Oral Treatment0.55

[back to top]

Difference in vWF Coagulation Protein in Blood Collected at Baseline and Just Prior to Surgery

The difference between vWF coagulation protein in blood samples collected at baseline and before surgery were measured using the immune-turbidimetric assay. (NCT00952731)
Timeframe: Baseline to immediately before surgery (after approximately 4-10 weeks)

Interventionpercentage of vWF protein in blood (Mean)
Treatment Gel + Oral Placebo-2.6
Placebo Gel + Oral Treatment51.2

[back to top]

Difference in Protein S Coagulation Protein in Blood Collected at Baseline and Just Prior to Surgery

The difference between protein S coagulation protein in blood samples collected at baseline and before surgery was measured using an ELISA Kit. (NCT00952731)
Timeframe: Baseline and immediately before surgery (after approximately 4-10 weeks)

Interventionpercentage of protein S in blood (Mean)
Treatment Gel + Oral Placebo-1.6
Placebo Gel + Oral Treatment-2.7

[back to top]

Difference in Factor VIII Coagulation Protein in Blood Collected at Baseline and Just Prior to Surgery

The difference between Factor VIII coagulation protein in blood samples collected at baseline and before surgery was measured with VisuLize antigen ELISA Kits. (NCT00952731)
Timeframe: Baseline and immediately before surgery (after approximately 4-10 weeks)

Interventionpercentage Factor VIII protein in blood (Mean)
Treatment Gel + Oral Placebo8.7
Placebo Gel + Oral Treatment11.6

[back to top]

Difference in Factor IX Coagulation Protein in Blood Collected at Baseline and Just Prior to Surgery

The difference between Factor IX coagulation protein in blood samples collected at baseline and before surgery was measured with VisuLize antigen ELISA Kits. (NCT00952731)
Timeframe: Baseline and immediately before surgery (after approximately 4-10 weeks)

Interventionpercentage of Factor IX protein in blood (Mean)
Treatment Gel + Oral Placebo-5.6
Placebo Gel + Oral Treatment0.4

[back to top]

Difference Between Ki-67 Labeling Index in Tissue Samples Taken at Baseline and Post-treatment

Ki-67 was measured in matched core and excision tissue samples containing DCIS (Ductal Carcinoma In-Situ) lesions, the core sample was at baseline while the excision sample was at surgery (after approximately 4-10 weeks of treatment). (NCT00952731)
Timeframe: Baseline and after 4-10 weeks of treatment

Interventionpercentage of 300 DCIS cells (Mean)
Treatment Gel + Oral Placebo-3.4
Placebo Gel + Oral Treatment-5.1

[back to top]

Number of Participants Analysed for Response of Cyclical Mastalgia (Good Response Was Defined as Disappearance of Mastalgia)

"All patients who had an increase in breast pain in the perimenstrual period were designated as having cyclical mastalgia. Response was assessed following treatment in terms of either persistence of cyclical mastalgia after 3 months of treatment or disappearance of cyclical mastalgia" (NCT00999921)
Timeframe: 3 months

,
Interventionparticipants (Number)
Fibroadenosis(total number)Fibroadenosis (good response)Fibroadenosis (poor response)Fibroadenoma (total number)Fibroadenoma (good response)Fibroadenoma (poor response)Mastalgia with no lump (total number)Mastalgia with no lump (good response)Mastalgia with no lump (poor response)
Evening Primrose Oil36112531217314
Tamoxifen3730733018171

[back to top]

Number of Participants Analysed for Reduction in Mastalgia (Cardiff Breast Pain Score).

All patients were categorized as Grade 0 for no pain, grade 1 for mild pain, grade 2 for moderate pain, Grade 3 for severe pain. Therapeutic response to mastalgia was expressed in terms of Cardiff Breast Pain Score (CBS) where CBS I = excellent response with no pain, CBS II = substantial response, CBS III = poor response and CBS IV = no response (NCT00999921)
Timeframe: 3 months

,
Interventionparticipants (Number)
CBS I (excellent response)CBS II (substantial response)CBS III (poor response)CBS IV (no response)
Evening Primrose Oil10151111
Tamoxifen711331

[back to top]

Number of Participants Analysed for Reduction in Lump Size ( 60% Reduction in Lump Size Considered to be a Satisfactory Response)

Ultrasonography of the breast was used to ascertain the lump size at the beginning of therapy and a repeat Ultrasonography of breast was done after 3 months at the end of the proposed therapy to record the posttreatment lump size by the same operator. The difference between the two findings were recorded and noted and a 60% or more reduction in the size of the lump was considered as a satisfactory response. (NCT00999921)
Timeframe: 3 months

,
Interventionparticipants (Number)
Fibroadenosis (total number)Fibroadenosis (60% or more reduction in size)Fibroadenosis (less than 60% reduction in size)Fibroadenoma (total number)Fibroadenoma (60% or more reduction in size)Fibroadenoma (less than 60% reduction in size)
Evening Primrose Oil61144738038
Tamoxifen6354939435

[back to top]

Total Number of Over-expressed Genes, Across All Participants With Tumor Protein p53-wild Type Breast Tumors That Had RNA Samples Available.

Total number of over-expressed genes, across all participants with tumor protein p53-wild type breast tumors that had ribonucleic acid (RNA) samples available. (NCT01027416)
Timeframe: 2 years

Interventiongenes (Number)
No Intervention196
Tamoxifen256

[back to top]

Mean Percent Positive Proximity Ligation Assays of All Tumor Protein p53-wild Type Breast Tumors in Participants by Treatment Arm

Status of estrogen receptor alpha (ERά) and tumor protein (p53) interaction in p53-wild type breast tumors in untreated patients verses patients treated with tamoxifen. Mean percent positive polylactide (PLA) of all p53-wild type breast tumors in participants by treatment arm (NCT01027416)
Timeframe: 2 years

Interventionpercentage of positive PLA (Mean)
No Intervention27.0
Tamoxifen4.4

[back to top]

Endoxifen Concentration by Response

"Endoxifen (ng/ml) was assessed at cycle 3.~Response Evaluation Criteria in Solid Tumors (RECIST) guideline (version 1.1) was used to evaluate response. Either complete response (CR) or partial response (PR) is considered as response. CR is defined as disappearance of all lesions. PR is defined as at least a 30% decrease in the sum of the diameters of target lesions, taking as reference the baseline sum diameters." (NCT01124695)
Timeframe: Endoxifen was assessed at cycle 3; response was assessed every 3 months for 2 years, then every 6 months up to 5 years

Interventionng/ml (Median)
Responders17.5
Non-responders17.2

[back to top]

Progression-free Survival by CYP2D6 Status in 2 Categories

Progression-free survival is defined as the time from registration to progression or death, whichever occurs first. Response Evaluation Criteria in Solid Tumors (RECIST) guideline (version 1.1) was used to evaluate progression. Progression is defined as appearance of one or more new lesions or unequivocal progression of existing non-target lesions or at least a 20% increase in the sum of the diameters of target lesions, taking as reference the smallest sum on study (this includes the baseline sum if that is the smallest on study). In addition to the relative increase of 20%, the sum must also demonstrate an absolute increase of at least 5 mm. (NCT01124695)
Timeframe: Assessed every 3 months for 2 years, then every 6 months up to 5 years

Interventionmonths (Median)
CYP2D6 - PM12.9
CYP2D6 - (IM+NM+UM)6.9

[back to top]

Progression-free Survival by CYP2D6 Status in 3 Categories

Progression-free survival is defined as the time from registration to progression or death, whichever occurs first. Response Evaluation Criteria in Solid Tumors (RECIST) guideline (version 1.1) was used to evaluate progression. Progression is defined as appearance of one or more new lesions or unequivocal progression of existing non-target lesions or at least a 20% increase in the sum of the diameters of target lesions, taking as reference the smallest sum on study (this includes the baseline sum if that is the smallest on study). In addition to the relative increase of 20%, the sum must also demonstrate an absolute increase of at least 5 mm. (NCT01124695)
Timeframe: Assessed every 3 months for 2 years, then every 6 months up to 5 years

Interventionmonths (Median)
CYP2D6 - PM12.9
CYP2D6 - IM4.8
CYP2D6 - NM+UM7.4

[back to top]

Progression-free Survival From 3 Months Post Registration

"This is a landmark progression-free survival analysis at 3 months post registration. Only patients who were progression-free and alive at 3 months were included.~Progression-free survival in this analysis is defined as the time from 3 months post registration to progression or death, whichever occurs first. Response Evaluation Criteria in Solid Tumors (RECIST) guideline (version 1.1) was used to evaluate progression. Progression is defined as appearance of one or more new lesions or unequivocal progression of existing non-target lesions or at least a 20% increase in the sum of the diameters of target lesions, taking as reference the smallest sum on study (this includes the baseline sum if that is the smallest on study). In addition to the relative increase of 20%, the sum must also demonstrate an absolute increase of at least 5 mm." (NCT01124695)
Timeframe: Assessed every 3 months for 2 years, then every 6 months up to 5 years

Interventionmonths (Median)
Endoxifen High13.8
Endoxifen Low11.1

[back to top]

Proportion of Patients Progression-free at 6 Months

Response Evaluation Criteria in Solid Tumors (RECIST) guideline (version 1.1) was used to evaluate progression. Progression is defined as appearance of one or more new lesions or unequivocal progression of existing non-target lesions or at least a 20% increase in the sum of the diameters of target lesions, taking as reference the smallest sum on study (this includes the baseline sum if that is the smallest on study). In addition to the relative increase of 20%, the sum must also demonstrate an absolute increase of at least 5 mm. (NCT01124695)
Timeframe: Assessed every 3 months for 6 months

Interventionproportion of participants (Number)
CYP2D6 - PM1.0
CYP2D6 - (IM+NM+UM)0.50

[back to top]

Proportion of Patients With Response

Response Evaluation Criteria in Solid Tumors (RECIST) guideline (version 1.1) was used to evaluate response. Either complete response (CR) or partial response (PR) is considered as response. CR is defined as disappearance of all lesions. PR is defined as at least a 30% decrease in the sum of the diameters of target lesions, taking as reference the baseline sum diameters. (NCT01124695)
Timeframe: Assessed every 3 months for 2 years, then every 6 months up to 5 years

Interventionproportion of participants (Number)
CYP2D6 - PM0
CYP2D6 - (IM+NM+UM)0.13

[back to top]

4-hydroxy-tamoxifen (Metabolite) Time for Cmax (Tmax) Following Tamoxifen Alone and When Coadministered With DVS SR

Time for maximum observed plasma concentration. (NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

Interventionhours (Median)
Tamoxifen 40 mg (Period 1)6.00
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)6.00

[back to top]

Endoxifen (Metabolite) Area Under the Plasma Concentration-time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) Following Endoxifen Alone and When Coadministered With DVS SR

Endoxifen is a metabolite of Tamoxifen. Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞). (NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

Interventionng*hr/mL (Geometric Mean)
Tamoxifen 40 mg (Period 1)677.7
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)505.6

[back to top]

Endoxifen (Metabolite) Maximum Observed Concentration (Cmax) Following Tamoxifen Alone and When Coadministered With DVS SR

(NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

Interventionng/mL (Geometric Mean)
Tamoxifen 40 mg (Period 1)1.077
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)1.226

[back to top]

Tamoxifen Terminal Half-life (t 1/2) Following Tamoxifen Alone and When Coadministered With DVS SR

Terminal half-life is the time measured for the plasma concentration to decrease by one half. (NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

Interventionhours (Mean)
Tamoxifen 40 mg (Period 1)250.5
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)242.3

[back to top]

Endoxifen (Metabolite) Terminal Half-life (t 1/2) Following Tamoxifen Alone and When Coadministered With DVS SR

Terminal half-life is the time measured for the plasma concentration to decrease by one half. (NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

Interventionhours (Mean)
Tamoxifen 40 mg (Period 1)207.5
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)232.5

[back to top]

Plasma 4-hydroxy-tamoxifen (Metabolite) Concentration Versus Time Summary: Tamoxifen Alone and When Coadministered With DVS SR

Summary statistics were to be calculated by setting concentration values below the lower limit of quantification (LLQ = 0.100 ng/mL) to zero. Summary statistics were not to be presented if number of observations above lower limit of quantification (NALQ) = 0. (NCT01189500)
Timeframe: Period 1 / Day 1 and Period 2 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing

,
Interventionng/mL (Median)
0 hour0.5 hour post dose1 hour post dose2 hours post dose3 hours post dose4 hours post dose6 hours post dose8 hours post dose12 hours post dose16 hours post dose24 hours post dose48 hours post dose72 hours post dose120 hours post dose168 hours post dose216 hours post dose264 hours post dose312 hours post dose384 hours post dose456 hours post dose528 hours post dose
Tamoxifen 40 mg (Period 1)NANANA0.20600.43350.59000.61450.62900.59100.49200.53950.49250.37950.28450.21800.18400.15900.13150.11250.00000.0000
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)0.00000.00000.00000.20300.39600.64200.70600.71000.58600.56400.57800.49100.40100.29200.22700.18700.16000.13800.11800.00000.0000

[back to top]

Plasma Endoxifen (Metabolite) Concentration Versus Time Summary: Tamoxifen Alone and When Coadministered With DVS SR

Summary statistics were to be calculated by setting concentration values below the lower limit of quantification (LLQ = 0.100 ng/mL) to zero. Summary statistics were not to be presented if number of observations above lower limit of quantification (NALQ) = 0. (NCT01189500)
Timeframe: Period 1 / Day 1 and Period 2 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing

,
Interventionng/mL (Median)
0 hour0.5 hour post dose1 hour post dose2 hours post dose3 hours post dose4 hours post dose6 hours post dose8 hours post dose12 hours post dose16 hours post dose24 hours post dose48 hours post dose72 hours post dose120 hours post dose168 hours post dose216 hours post dose264 hours post dose312 hours post dose384 hours post dose456 hours post dose528 hours post dose
Tamoxifen 40 mg (Period 1)NANANA0.00000.00000.17600.24850.28950.44700.43300.62150.90650.97401.0951.1201.1201.1451.0350.85600.70600.6210
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)0.29000.33700.34300.41000.50200.63500.58700.73100.73100.71300.99001.1801.1801.2401.1401.0801.1600.97600.94700.91500.7040

[back to top]

Tamoxifen Time for Cmax (Tmax) Following Tamoxifen Alone and When Coadministered With DVS SR

Time for maximum observed plasma concentration. (NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

Interventionhours (Median)
Tamoxifen 40 mg (Period 1)4.00
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)4.00

[back to top]

Plasma Tamoxifen Concentration Versus Time Summary: Tamoxifen Alone and When Coadministered With DVS SR

Summary statistics were to be calculated by setting concentration values below the lower limit of quantification (LLQ = 0.250 ng/mL) to zero. Summary statistics were not to be presented if number of observations above lower limit of quantification (NALQ) = 0. (NCT01189500)
Timeframe: Period 1 / Day 1 and Period 2 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing

,
Interventionng/mL (Median)
0 hour0.5 hour post dose1 hour post dose2 hours post dose3 hours post dose4 hours post dose6 hours post dose8 hours post dose12 hours post dose16 hours post dose24 hours post dose48 hours post dose72 hours post dose120 hours post dose168 hours post dose216 hours post dose264 hours post dose312 hours post dose384 hours post dose456 hours post dose528 hours post dose
Tamoxifen 40 mg (Period 1)NA1.87511.4537.2054.5068.2558.9554.7540.4027.3024.5015.4012.5510.559.1207.5557.5756.4455.1804.3003.560
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)1.3004.65013.9033.6055.6072.2060.9056.1035.3026.2025.5016.2012.6011.609.9308.1507.2706.9205.6004.3304.160

[back to top]

N-desmethyl-tamoxifen (Metabolite) Area Under the Plasma Concentration-time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) Following Tamoxifen Alone and When Coadministered With DVS SR

N-desmethyl-tamoxifen is a metabolite of Tamoxifen. Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞). (NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

Interventionng*hr/mL (Geometric Mean)
Tamoxifen 40 mg (Period 1)8187
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)9329

[back to top]

Plasma N-desmethyl-tamoxifen (Metabolite) Concentration Versus Time Summary: Tamoxifen Alone and When Coadministered With DVS SR

Summary statistics were to be calculated by setting concentration values below the lower limit of quantification (LLQ = 0.250 ng/mL) to zero. Summary statistics were not to be presented if number of observations above lower limit of quantification (NALQ) = 0. (NCT01189500)
Timeframe: Period 1 / Day 1 and Period 2 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing

,
Interventionng/mL (Median)
0 hour0.5 hour post dose1 hour post dose2 hours post dose3 hours post dose4 hours post dose6 hours post dose8 hours post dose12 hours post dose16 hours post dose24 hours post dose48 hours post dose72 hours post dose120 hours post dose168 hours post dose216 hours post dose264 hours post dose312 hours post dose384 hours post dose456 hours post dose528 hours post dose
Tamoxifen 40 mg (Period 1)NA0.00000.80504.2109.44012.5514.1014.9016.1014.5516.9016.4516.4515.1014.4013.5012.6511.4010.158.7308.730
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)3.6004.1205.6509.77014.8018.7019.3020.4019.0018.4021.9024.0019.8019.8016.8015.6015.4014.4013.1010.5010.40

[back to top]

N-desmethyl-tamoxifen (Metabolite) Maximum Observed Concentration (Cmax) Following Tamoxifen Alone and When Coadministered With DVS SR

(NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

Interventionng/mL (Geometric Mean)
Tamoxifen 40 mg (Period 1)18.30
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)24.42

[back to top]

N-desmethyl-tamoxifen (Metabolite) Terminal Half-life (t 1/2) Following Tamoxifen Alone and When Coadministered With DVS SR

Terminal half-life is the time measured for the plasma concentration to decrease by one half. (NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

Interventionhours (Mean)
Tamoxifen 40 mg (Period 1)256.0
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)265.6

[back to top]

N-desmethyl-tamoxifen (Metabolite) Time for Cmax (Tmax) Following Tamoxifen Alone and When Coadministered With DVS SR

Time for maximum observed plasma concentration. (NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

Interventionhours (Median)
Tamoxifen 40 mg (Period 1)35.9
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)47.9

[back to top]

Tamoxifen Apparent Clearance (CL/F) Following Tamoxifen Alone and When Coadministered With DVS SR

Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood calculated as (Dose/AUCinf); measured as milliliters per minute (mL/min). (NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

InterventionmL/min (Geometric Mean)
Tamoxifen 40 mg (Period 1)115.9
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)113.2

[back to top]

Tamoxifen Apparent Volume of Distribution (Vz/F) Following Tamoxifen Alone and When Coadministered With DVS SR

Calculated as Dose / (AUCinf * kel); where kel=terminal phase rate constant. (NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

Interventionliters (Geometric Mean)
Tamoxifen 40 mg (Period 1)2474
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)2321

[back to top]

Tamoxifen Area Under the Plasma Concentration-time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) Following Tamoxifen Alone and When Coadministered With DVS SR

Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞); measured as nanograms multiplied by hours divided by milliliters (ng*hr/mL). (NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

Interventionng*hr/mL (Geometric Mean)
Tamoxifen 40 mg (Period 1)5751
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)5888

[back to top]

Tamoxifen Maximum Observed Concentration (Cmax) Following Tamoxifen Alone and When Coadministered With DVS SR

Cmax measured as nanograms per milliliters (ng/mL). (NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

Interventionng/mL (Geometric Mean)
Tamoxifen 40 mg (Period 1)70.58
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)70.33

[back to top]

Endoxifen (Metabolite) Time for Cmax (Tmax) Following Tamoxifen Alone and When Coadministered With DVS SR

Time for maximum observed plasma concentration. (NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

Interventionhours (Median)
Tamoxifen 40 mg (Period 1)216
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)120

[back to top]

4-hydroxy-tamoxifen (Metabolite) Area Under the Plasma Concentration-time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) Following Tamoxifen Alone and When Coadministered With DVS SR

4-hydroxy-tamoxifen is a metabolite of Tamoxifen. Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞). (NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

Interventionng*hr/mL (Geometric Mean)
Tamoxifen 40 mg (Period 1)117.5
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)133.9

[back to top]

4-hydroxy-tamoxifen (Metabolite) Maximum Observed Concentration (Cmax) Following Tamoxifen Alone and When Coadministered With DVS SR

(NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

Interventionng/mL (Geometric Mean)
Tamoxifen 40 mg (Period 1)0.6716
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)0.7247

[back to top]

4-hydroxy-tamoxifen (Metabolite) Terminal Half-life (t 1/2) Following Tamoxifen Alone and When Coadministered With DVS SR

Terminal half-life is the time measured for the plasma concentration to decrease by one half. (NCT01189500)
Timeframe: Period 1 / Day 1: 0, 0.5, 1, 2, 3, 4, 6, 8, 12,16, 24, 48, 72, 120, 168, 216, 264, 312, 384, 456, and 528 hours after dosing; Period 2 / Day 1 and Day 7: 0, 0.5, 1, 2, 3, 4, 6, 8, 12 and 16 hours; 0 hour on Day 8, 9, 10, 12, 14, 16, 18, 20, 23, 26 and 29.

Interventionhours (Mean)
Tamoxifen 40 mg (Period 1)165.2
Tamoxifen 40 mg + DVS SR 100 mg (Period 2)177.0

[back to top]

Number of Participants With Different Patient Reported Symptoms, Measured by Questionnaire

The outcomes will be scored as a 5-point Likert-type scale (0-4) in response to questions on how much the patients are bothered by certain symptoms. The questionnaire will be administered every 6 months. The responses will be treated as normally distributed, as ordinal or dichotomized variable, and the linear mixed effects of general linear mixed model (GLMM) methods will be applied to compare changes between treatment groups. Piecewise models will also be fitted with join point at 6 months, considering linear and curvilinear trajectories between 6 and 24 month time points. (NCT01196936)
Timeframe: Up to 2 years

,
Interventionparticipants (Number)
Interrupted sleepGeneral aches or painsHot flashesJoint pain or stiffnessFeeling unusually tiredHeartburn and/or acid stomachHeadachesMuscle cramps or soreness
Arm I (Tamoxifen Citrate)1614131212111111
Arm II (Placebo)1681291010148

[back to top]

Number of Grade 2-4 Toxicities

Will be tabulated by treatment arm. Differences by treatment arm will be evaluated using Fisher exact tests. (NCT01196936)
Timeframe: Up to 2 years

InterventionAdverse Events (Number)
Arm I (Tamoxifen Citrate)77
Arm II (Placebo)40

[back to top]

Mammographic Breast Density

Mammographic density was quantified as percentage of fibroglandular tissue. Using an intention-to-treat analysis, mammographic breast density (MBD) was compared between patients in the low dose tamoxifen intervention and placebo group by applying the linear mixed effects model for normally distributed data. (NCT01196936)
Timeframe: At year two post treatment

Interventionpercentage of fibrogladular tissue (Least Squares Mean)
Arm I (Tamoxifen Citrate)45.2
Arm II (Placebo)48.6

[back to top]

Insulin Growth Factor Levels (IGF3 )

IGF3 will be treated as a continuous measure. The linear mixed effects model for between group comparisons of measures from 3 time points will be applied. The unstructured mean model and linear in time model will be employed. (NCT01196936)
Timeframe: Up to 2 years

Interventionng/mL (Least Squares Mean)
Arm I (Tamoxifen Citrate)4716.0
Arm II (Placebo)4315.2

[back to top]

Insulin Growth Factor Levels (IGF1)

IGF1 will be treated as a continuous measure. The linear mixed effects model for between group comparisons of measures from 3 time points will be applied. The unstructured mean model and linear in time model will be employed. (NCT01196936)
Timeframe: Up to 2 years

Interventionng/mL (Least Squares Mean)
Arm I (Tamoxifen Citrate)144.3
Arm II (Placebo)162.3

[back to top]

Biomarker Levels - Urine N-telopeptide

Urine n-telopeptide measurements will be treated as continuous variables. Transformed to normality as appropriate, the linear mixed effects model will be applied, using the unstructured mean model and linear in time model to assess the effects of low-dose tamoxifen on these measurements over time. (NCT01196936)
Timeframe: Up to 2 years

InterventionnM Bone Collagen Equiv. / nM Creatinine (Least Squares Mean)
Arm I (Tamoxifen Citrate)33.1
Arm II (Placebo)32.0

[back to top]

Biomarker Levels

Total cholesterol, low and high density lipoprotein, triglycerides, and anti-thrombin III enzymatic assay measurements will be treated as continuous variables. Transformed to normality as appropriate, the linear mixed effects model will be applied, using the unstructured mean model and linear in time model to assess the effects of low-dose tamoxifen on these measurements over time. (NCT01196936)
Timeframe: Up to 2 years

,
Interventionmg/dL (Least Squares Mean)
Total CholesterolLow-density lipoproteinHigh-density lipoproteinTriglyceridesAnti-thrombin III
Arm I (Tamoxifen Citrate)189.9105.457.6138.189.3
Arm II (Placebo)192.5108.656.5116.698.1

[back to top]

Percentage of Pills Taken Out of the Total Prescribed

The number of pills taken out of the total prescribed in a 3-month period will be modeled as a random effects binomial regression model. The binomial rates from 8 time points (month 3-24) will be modeled as unstructured mean model with 7 indicator variables as well as polynomial models over time. The random-intercept and the random intercept and slope models will be considered. The significance of the time indicators or parameters by treatment interaction will be evaluated for treatment difference in compliance. (NCT01196936)
Timeframe: Up to 2 years

Interventionpercentage of pills taken (Median)
Arm I (Tamoxifen Citrate)97.5
Arm II (Placebo)96.7

[back to top]

Biomarker Levels - Alkaline Phosphatase

Serum bone-specific alkaline phosphatase measurements will be treated as continuous variables. Transformed to normality as appropriate, the linear mixed effects model will be applied, using the unstructured mean model and linear in time model to assess the effects of low-dose tamoxifen on these measurements over time. (NCT01196936)
Timeframe: Up to 2 years

Interventionug/L (Least Squares Mean)
Arm I (Tamoxifen Citrate)12.2
Arm II (Placebo)12.4

[back to top]

Dose Adjustments

These events were due to a double-blinded study design. (NCT01257581)
Timeframe: 38 weeks of treatment followed by a telephone interview at 42 weeks.

,,
InterventionNumber of Events due to Adverse Events (Number)
Number of Creatine Reductions due to AEsTamoxifen Redutions due to AEsSuspensions due to AEsDiscontinuations due to AEs
Creatine 30gm65910
Tamoxifen 40mg3415
Tamoxifen 80mg0024

[back to top]

Lab Abnormal Reports by Treatment Assignment

The safety data is summarized according to treatment arm. Total number of Adverse Events (AEs), AEs that cause study drug withdrawal and abnormal laboratory tests are compared among treatment arms. A lab abnormality was a result that was out of range and considered clinically significant by the site investigator. (NCT01257581)
Timeframe: 38 weeks of treatment followed by a telephone interview at 42 weeks.

,,
InterventionEvents (Number)
ALT (SGOT)CreatinineGlucoseHematocritLymphocytesMCHNeutrophilsAbsolute NeutrophilsGFR Non-African AmericanPotassiumRed Blood Count (RBC)White Blood Count (WBC)
Creatine 30gm040111002011
Tamoxifen 40mg100000000000
Tamoxifen 80mg001000110100

[back to top]

HHD Upper Z-score

The HHD upper z-scores are means of z-scores for right and left shoulder flexion, elbow extension, elbow flexion, write extension and first dorsal interosseous muscles with z-scores calculated relative to the baseline mean and standard deviation strength of each muscle group across all participants. (NCT01257581)
Timeframe: 38 weeks of treatment followed by a telephone interview at 42 weeks.

InterventionZ-score (Mean)
Creatine 30gm-0.103
Tamoxifen 40mg-0.089
Tamoxifen 80mg-0.039

[back to top]

Tracheostomy-free Survival

Secondary efficacy will be assessed by analyzing rate of tracheostomy-free survival at nine months. (NCT01257581)
Timeframe: 38 weeks of treatment followed by a telephone interview at 42 weeks.

Interventionproportion of participants (Number)
Creatine 30gm0.455
Tamoxifen 40mg0.286
Tamoxifen 80mg0.412

[back to top]

Accurate Test of Limb Isometric Strength (ATLIS) Lower Percentage of Predicted Normal (PPN)

The ATLIS PPN measures are percentages of predicted normal strength based on age, gender, height, and weight using normative data. (NCT01257581)
Timeframe: 38 weeks of treatment followed by a telephone interview at 42 weeks.

Interventionpercentages of predicted normal strength (Mean)
Creatine 30gm-2.098
Tamoxifen 40mg-2.375
Tamoxifen 80mg-0.491

[back to top]

ATLIS Upper Percentage of Predicted Normal (PPN)

The ATLIS PPN measures are percentages of predicted normal strength based on age, gender, height, and weight using normative data. (NCT01257581)
Timeframe: 38 weeks of treatment followed by a telephone interview at 42 weeks.

Interventionpercentages of predicted normal strength (Mean)
Creatine 30gm-1.932
Tamoxifen 40mg-1.845
Tamoxifen 80mg0.436

[back to top]

Change in ALS Functional Rating Scale - Revised (ALSFRS-R)

Primary efficacy will be assessed by analyzing the mean rate of decline in the ALS Functional Rating Scale-Revised (ALSFRS-R) score over nine months. The ALSFRS-R is a quickly administered (5 min) ordinal rating scale used to determine a subject's assessment of their capability and independence in 12 functional activities. There are 12 questions, graded by the subject 0-4 (4 is normal). Score of 0 (worst) to 48 (best). Reflects speech and swallowing, fine motor skills, large motor skills, and breathing. (NCT01257581)
Timeframe: 38 weeks of treatment followed by a telephone interview at 42 weeks.

Interventionscores on a scale (Mean)
Creatine 30gm-0.905
Tamoxifen 40mg-0.983
Tamoxifen 80mg-0.743

[back to top]

Hand Held Dynamometry (HHD) Lower Z-score

The HHD lower z-scores are means of z-scores for right and left knee extension, knee flexion, hip flexion, and ankle dorsiflexion with z-scores calculated relative to the baseline mean and standard deviation strength of each muscle group across all participants. (NCT01257581)
Timeframe: 38 weeks of treatment followed by a telephone interview at 42 weeks.

InterventionZ-score (Mean)
Creatine 30gm-0.094
Tamoxifen 40mg-0.067
Tamoxifen 80mg-0.016

[back to top]

HHD Lower % Baseline

HHD % baseline measures are mean percent change for right and left knee extension, knee flexion, hip flexion, and ankle dorsiflexion from each participant's baseline. (NCT01257581)
Timeframe: 38 weeks of treatment followed by a telephone interview at 42 weeks.

Interventionpercent change (Mean)
Creatine 30gm-9.258
Tamoxifen 40mg-6.711
Tamoxifen 80mg-2.897

[back to top]

HHD Upper % Baseline

The HHD % baseline measures are mean percent change for shoulder flexion, elbow extension, elbow flexion, wrist extension, and first dorsal interosseous muscles from each participant's baseline. (NCT01257581)
Timeframe: 38 weeks of treatment followed by a telephone interview at 42 weeks.

Interventionpercent change (Mean)
Creatine 30gm-8.451
Tamoxifen 40mg-7.720
Tamoxifen 80mg-4.515

[back to top]

Vital Capacity/Pulmonary Function Testing

Secondary efficacy will be assessed by analyzing the change in the Slow Vital Capacity score over nine months. Vital Capacity is the maximum amount of air a person can expel from the lungs after a maximum inhalation. A subject's VC depends on their age, sex and height. The value is recorded as a percentage of predicted normal. (NCT01257581)
Timeframe: 38 weeks of treatment followed by a telephone interview at 42 weeks.

InterventionPercentage of predicted max value (Mean)
Creatine 30gm-3.386
Tamoxifen 40mg-2.915
Tamoxifen 80mg-3.377

[back to top]

Distant Relapse-Free Survival (DRFS)

"Time from date of randomization (2nd Registration) to date of invasive distant disease recurrence or death due to any cause. Participants last known to be alive who have not experienced distant recurrence are censored at their last contact date. This outcome requires continuing to follow the patient after local recurrence in order to ascertain subsequent distant recurrence. Kaplan-Meier estimates were calculated for the 5-year DRFS rate.~Due to the results of the third prespecified interim analysis, prespecified separate analyses were conducted for all outcomes by menopausal status. The NCI and the data and safety monitoring committee recommended early reporting of the data. Due to subsequent data collection and data cleaning, the population of eligible and evaluable participants differs slightly between the reporting of this outcome and the Participant Flow section." (NCT01272037)
Timeframe: 5 years after randomization

,
Interventionpercentage of participants (Number)
Premenopausal participantsPostmenopausal participants
Chemo and Endocrine Therapy96.194.4
Endocrine Therapy Alone92.894.4

[back to top]

Invasive Disease-Free Survival (IDFS)

"From date of randomization (2nd Registration) to date of first invasive recurrence (local, regional or distant), second invasive primary cancer (breast or not), or death due to any cause. Patients last known to be alive who have not experienced recurrence or second primary cancer are censored at their last contact date. This is the STEEP definition of invasive disease-free survival. Kaplan-Meier estimates were calculated for the 5-year IDFS rate.~Due to the results of the third prespecified interim analysis, prespecified separate analyses were conducted for all outcomes by menopausal status (see Statistical Analysis 2). The NCI and data and safety monitoring committee recommended early reporting of the data. After the primary analysis, changes in eligibility status were identified for three participants, making the population of eligible and evaluable participants different between the reporting of this outcome and both the Participant Flow section and the Adverse Events section." (NCT01272037)
Timeframe: 5 years after randomization

,
Interventionpercentage of participants (Number)
PremenopausalPostmenopausal
Chemo and Endocrine Therapy93.991.3
Endocrine Therapy Alone89.091.9

[back to top] [back to top]

The Proportion of Patients With RS 11-25 Who Refused the Assigned Treatment

The primary purpose of this trial is to determine the feasibility of carrying out a large multi-center trial with a similar design. Feasibility, in terms of less than 1/3 of patients with intermediate (11-25) Recurrence Score (RS) who refused the assigned treatment (Group 2) or refused randomization between hormonal (Arm 1) or chemotherapy (Arm 2). The confidence interval will be 95%. The proportion (and 95% confidence interval) of patients with RS 11-25 who refuse the assigned treatment will be calculated. (NCT01293032)
Timeframe: Up to 2 years

Interventionproportion of participants (Number)
Group 2 (RS 11-25)0.15

[back to top]

PK: Maximum Plasma Concentration (Cmax) of LY2228820

(NCT01393990)
Timeframe: Cycle 1, Days 1 and 14: predose, 0.5, 1, 2, 3, 4, 6 and 8 h postdose

,,,,,,,,,,,,,,
Interventionng/mL (Geometric Mean)
Cycle 1 Day 1Cycle 1 Day 14
Part A and Part B: 420 mg LY2228820 Tablets17002230
Part A and Part C: 300 mg LY2228820 Tablets10201400
Part A: 10 mg LY2228820 Capsules14.728.4
Part A: 120 mg LY2228820 Capsules405530
Part A: 160 mg LY2228820 Capsules6061930
Part A: 160 mg LY2228820 Tablets454574
Part A: 20 mg LY2228820 Capsules90.181.4
Part A: 200 mg LY2228820 Capsules6731330
Part A: 200 mg LY2228820 Tablets636963
Part A: 40 mg LY2228820 Capsules144252
Part A: 560 mg LY2228820 Tablets2360NA
Part A: 65 mg LY2228820 Capsules135415
Part A: 90 mg LY2228820 Capsules202208
Part D: 200 mg LY2228820 Tablets7181030
Part D: 300 mg LY2228820 Tablets18101700

[back to top]

PK: Area Under the Concentration-Time Curve From Time Zero to 8 Hours (AUC0-8) of LY2228820

(NCT01393990)
Timeframe: Cycle 1, Days 1 and 14: predose, 0.5, 1, 2, 3, 4, 6 and 8 h postdose

,,,,,,,,,,,,,,
Interventionnanograms*hour/milliliter (ng*hr/mL) (Geometric Mean)
Cycle 1 Day 1Cycle 1 Day 14
Part A and Part B: 420 mg LY2228820 Tablets578010200
Part A and Part C: 300 mg LY2228820 Tablets34606620
Part A: 10 mg LY2228820 Capsules55.6151
Part A: 120 mg LY2228820 Capsules13101960
Part A: 160 mg LY2228820 Capsules21206000
Part A: 160 mg LY2228820 Tablets17502810
Part A: 20 mg LY2228820 Capsules257372
Part A: 200 mg LY2228820 Capsules25506220
Part A: 200 mg LY2228820 Tablets1720NA
Part A: 40 mg LY2228820 Capsules3751070
Part A: 560 mg LY2228820 Tablets8880NA
Part A: 65 mg LY2228820 Capsules4451300
Part A: 90 mg LY2228820 Capsules707827
Part D: 200 mg LY2228820 Tablets23603810
Part D: 300 mg LY2228820 Tablets45006910

[back to top] [back to top]

Pharmacodynamics (PD): Number of Participants With Greater Than 50% Inhibition of p38 Mitogen-Activated Protein Kinase (MAPK) Activity on Day 1

The effect of LY2228820 on PD biomarker was measured as MAPK-activated protein kinase -2 (MAPKAP-K2) level which is regulated by p38 MAPK activity. Inhibition of p38 MAPK activity will result in lower levels of MAPKAPK-2. (NCT01393990)
Timeframe: Cycle 1 Day 1: predose, 1, 2, 4, and 6 h postdose

InterventionParticipants (Count of Participants)
Part A, C and D: LY2228820 300 mg Tablets14

[back to top]

Percentage of Participants With Best Overall Response [Complete Response (CR)+Partial Response (PR)+Stable Disease (SD)]

Response was defined using Response Evaluation Criteria In Solid Tumors (RECIST, version 1.1) criteria. CR was defined as the disappearance of all target and non-target lesions and normalization of tumor marker level in non-target lesions. PR was defined as having at least a 30% decrease in sum of longest diameter (LD) of target lesions. PD was defined as having at least a 20% increase in the sum of the LD of target lesion and appearance of ≥1 new lesion and/or unequivocal progression of existing nontarget lesions. SD was defined as small changes that did not meet the above criteria taking as reference the smallest sum LD since treatment started. (NCT01393990)
Timeframe: Baseline to study completion (Up to 41 months)

Interventionpercentage of participants (Number)
Part A: 10 mg LY2228820 Capsules25.0
Part A: 20 mg LY2228820 Capsules33.3
Part A: 40 mg LY2228820 Capsules33.3
Part A: 65 mg LY2228820 Capsules33.3
Part A: 90 mg LY2228820 Capsules40.0
Part A: 120 mg LY2228820 Capsules33.3
Part A: 160 mg LY2228820 Capsules66.7
Part A: 200 mg LY2228820 Capsules28.6
Part A: 160 mg Bridge LY222882016.7
Part A: 160 mg LY2228820 Tablets33.3
Part A: 200 mg LY2228820 Tablets33.3
Part A: 300 mg LY2228820 Tablets0.0
Part A: 420 mg LY2228820 Tablets33.3
Part A: 560 mg LY2228820 Tablets0.0
Part B: 420 mg LY2228820 Tablets16.7
Part C: 300 mg LY2228820 Tablets0.0
Part D: 200 mg LY2228820 Tablets0.0
Part D: 300 mg LY2228820 Tablets16.7

[back to top]

Number of Participants With Clinically Significant Effects (Physical Assessments and Safety Lab Tests)

Data presented are the number of participants who experienced at least one treatment emergent adverse event (TEAE). A TEAE is defined as an event that first occurred or worsened after the administration of at least 1 dose of study drug, regardless of causality. A summary of serious AEs (SAEs) and other non-serious AEs, regardless of causality, is located in the Reported Adverse Events module. (NCT01393990)
Timeframe: Baseline to study completion (Up to 41 months)

InterventionParticipants (Count of Participants)
Part A: 10 mg LY2228820 Capsules1
Part A: 20 mg LY2228820 Capsules3
Part A: 40 mg LY2228820 Capsules2
Part A: 65 mg LY2228820 Capsules3
Part A: 90 mg LY2228820 Capsules1
Part A: 120 mg LY2228820 Capsules1
Part A: 160 mg LY2228820 Capsules1
Part A: 200 mg LY2228820 Capsules5
Part A: 160 mg LY2228820 Bridge4
Part A: 160 mg LY2228820 Tablets1
Part A: 200 mg LY2228820 Tablets3
Part A: 300 mg LY2228820 Tablets3
Part A: 420 mg LY2228820 Tablets3
Part A: 560 mg LY2228820 Tablets4
Part B: 420 mg LY2228820 Tablets18
Part C: 300 mg LY2228820 Tablets7
Part D: 200 mg LY2228820 Tablets3
Part D: 300 mg LY2228820 Tablets6

[back to top]

Assessment of Breast Palpation

Breast palpation was done by the investigator to assess abnormalities in the breast. (NCT01585558)
Timeframe: Week 26 (Visit 5)

,,
InterventionParticipants (Number)
Not doneNormalAbnormal
Ospemifene 30 mg (Dose 1)0520
Ospemifene 60 mg (Dose 2)1640
Placebo0411

[back to top]

Assessment of Breast Palpation

Breast palpation was done by the investigator to assess abnormalities in the breast. (NCT01585558)
Timeframe: Week 52 (Visit 6)

,,
InterventionParticipants (Number)
NormalAbnormal
Ospemifene 30 mg (Dose 1)490
Ospemifene 60 mg (Dose 2)571
Placebo350

[back to top]

Assessment of Cervical Pap Smear Samples

Cervical Pap smear samples were used to evaluate: atypical squamous cells of undetermined significance (ASC-US), squamous intraepithelial lesions (SILs), intraepithelial lesions or malignancy, and reactive endocervical cells and/or metaplastic cells. (NCT01585558)
Timeframe: Week 52 (Visit 6)

,,
InterventionParticipants (Number)
ASC-USInadequate squamous epithelial componentLow grade SIL (slight dysplasia and/or HPV effect)Negative for intraepithelial lesion or malignancyReactive endocervical and/or metaplastic cellsUnsatisfactory: Due to reasons noted
Ospemifene 30 mg (Dose 1)1104511
Ospemifene 60 mg (Dose 2)2015410
Placebo0103300

[back to top]

Assessment of Endometrial Biopsy

Assessments were based on Blaustein's classification. (NCT01585558)
Timeframe: Week 52 (Visit 6)

,,
InterventionParticipants (Number)
Atrophic/inactive/insufficientWeakly proliferativeAtypical epithelial proliferationProliferative pattern, disordered typeOther (Polyp, atrophic type)Hyperplasia or carcinoma
Ospemifene 30 mg (Dose 1)4411000
Ospemifene 60 mg (Dose 2)5310100
Placebo3200000

[back to top]

Assessment of Hematology Test Values

Change from baseline (NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

,,
Intervention(x10(9)/L) (Mean)
Leukocytes (WBC)BasophilsLymphocytesMonocytesNeutrophilsEosinophilsPlatelet Count
Ospemifene 30 mg (Dose 1)0.0610.003-0.120-0.0240.194-0.003-11.2
Ospemifene 60 mg (Dose 2)-0.2170.0020.001-0.028-0.258-0.005-16.4
Placebo0.371-0.003-0.0280.0210.3770.021-11.3

[back to top]

Assessment of Hematology Tests

Change from baseline (NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

,,
Intervention(x10(9)/L) (Mean)
Leukocytes (WBC)BasophilsLymphocytesMonocytesNeutrophilsEosinophilsPlatelet Count
Ospemifene 30 mg (Dose 1)-0.0080.006-0.0350.025-0.010-0.010-5.2
Ospemifene 60 mg (Dose 2)-0.2110.001-0.064-0.042-0.094-0.009-5.6
Placebo0.207-0.0050.1160.0090.0830.002-4.5

[back to top]

Assessment of Mammography

Mammography was done for the detection of characteristic masses and microcalcifications in the breast. (NCT01585558)
Timeframe: Week 52 (Visit 6)

,,
InterventionParticipants (Number)
Breast cystBreast massBreast microcalcificationMammogram abnormal
Ospemifene 30 mg (Dose 1)0200
Ospemifene 60 mg (Dose 2)0111
Placebo1000

[back to top]

Change From Baseline in Visual Evaluation of the Vagina

Petechiae, pallor, friability, dryness in the mucosa, and redness in the mucosa were assessed on a 4-point scale (0=None, 1=Mild, 2=Moderate, 3=Severe). (NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

,,
InterventionUnits on a scale (Mean)
PetechiaePallorFriabilityVaginal Dryness in MucosaVaginal Redness in Mucosa
Ospemifene 30 mg (Dose 1)-0.7-1.3-0.9-1.6-0.8
Ospemifene 60 mg (Dose 2)-0.6-1.2-0.8-1.4-0.7
Placebo-0.3-0.5-0.6-0.8-0.4

[back to top]

Incidence of Adverse Events (AEs)

(NCT01585558)
Timeframe: Week 20 (Phone Contact) to Week 56 (Visit 7)

,,
InterventionParticipants (Number)
Treatment-Emergent AERelated AE (Possibly/Probably/Definitely Related)AE Causing Study Drug DiscontinuationSerious AESevere AE
Ospemifene 30 mg (Dose 1)3811326
Ospemifene 60 mg (Dose 2)4418457
Placebo225112

[back to top]

Mean Change in Blood Chemistry Parameters

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

,,
InterventionU/L (Mean)
Alanine Aminotransferase (ALT)Aspartate Aminotransferase (AST)Creatine Kinase (CK)
Ospemifene 30 mg (Dose 1)-1.20.81.1
Ospemifene 60 mg (Dose 2)-1.31.2-4.4
Placebo-1.30.518.7

[back to top]

Mean Change in Blood Chemistry Parameters

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

,,
InterventionU/L (Mean)
ALTASTCK
Ospemifene 30 mg (Dose 1)-2.11.57.3
Ospemifene 60 mg (Dose 2)-3.20.51.2
Placebo-2.20.3-6.0

[back to top]

Mean Percent Change From Baseline in Serum Lipids

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

,,
Interventionpercent change (Mean)
Total CholesterolLow-density-lipoprotein cholesterol (LDL-C)High-density-lipoprotein cholesterol (HDL-C)Triglycerides
Ospemifene 30 mg (Dose 1)-0.14-0.026.48-0.66
Ospemifene 60 mg (Dose 2)2.352.425.765.12
Placebo6.2410.382.3920.36

[back to top]

Mean Percent Change From Baseline in Serum Lipids

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

,,
Interventionpercent change (Mean)
Total CholesterolLDL-CHDL-CTriglycerides
Ospemifene 30 mg (Dose 1)-0.55-0.876.07-3.10
Ospemifene 60 mg (Dose 2)-2.45-6.201.2915.19
Placebo-1.05-0.42-4.4121.57

[back to top]

Change From Baseline in Weight

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

Interventionkg (Mean)
Ospemifene 30 mg (Dose 1)-0.99
Ospemifene 60 mg (Dose 2)0.98
Placebo1.99

[back to top]

Change From Baseline in E2 Levels

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

Interventionpg/mL (Mean)
Ospemifene 30 mg (Dose 1)0.06
Ospemifene 60 mg (Dose 2)-0.02
Placebo0.14

[back to top]

Change From Baseline in Visual Evaluation of the Vagina

Petechiae, pallor, friability, dryness in the mucosa, and redness in the mucosa were assessed on a 4-point scale (0=None, 1=Mild, 2=Moderate, 3=Severe). (NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

,,
InterventionUnits on a scale (Mean)
PetechiaePallorFriabilityVaginal Dryness in MucosaVaginal Redness in Mucosa
Ospemifene 30 mg (Dose 1)-0.8-1.3-0.9-1.7-0.8
Ospemifene 60 mg (Dose 2)-0.7-1.2-0.7-1.4-0.6
Placebo-0.4-0.6-0.5-1.1-0.5

[back to top]

Assessment of Endometrial Safety With a Transvaginal Ultrasound (TVU)

Mean change in endometrial thickness from baseline (NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

Interventionmm (Mean)
Ospemifene 30 mg (Dose 1)0.580
Ospemifene 60 mg (Dose 2)0.818
Placebo-0.119

[back to top]

Assessment of Endometrial Safety With a TVU

Mean change in endometrial thickness from baseline (NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

Interventionmm (Mean)
Ospemifene 30 mg (Dose 1)0.681
Ospemifene 60 mg (Dose 2)1.139
Placebo-0.041

[back to top]

Change From Baseline in Antithrombin Antigen, P Levels

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

Interventionpercent change (Mean)
Ospemifene 30 mg (Dose 1)0.7
Ospemifene 60 mg (Dose 2)-2.4
Placebo1.2

[back to top]

Change From Baseline in Antithrombin Antigen, P Levels

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

Interventionpercent change (Mean)
Ospemifene 30 mg (Dose 1)5.1
Ospemifene 60 mg (Dose 2)1.0
Placebo7.1

[back to top]

Change From Baseline in BMI

(NCT01585558)
Timeframe: Baseline to Week 26

Interventionkg/m^2 (Mean)
Ospemifene 30 mg (Dose 1)-0.331
Ospemifene 60 mg (Dose 2)0.253
Placebo0.293

[back to top]

Change From Baseline in BMI

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

Interventionkg/m^2 (Mean)
Ospemifene 30 mg (Dose 1)-0.379
Ospemifene 60 mg (Dose 2)0.376
Placebo0.748

[back to top]

Change From Baseline in DBP

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

InterventionmmHg (Mean)
Ospemifene 30 mg (Dose 1)-2.5
Ospemifene 60 mg (Dose 2)0.7
Placebo0.8

[back to top]

Change From Baseline in Diastolic Blood Pressure (DBP)

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

InterventionmmHg (Mean)
Ospemifene 30 mg (Dose 1)-2.0
Ospemifene 60 mg (Dose 2)0.5
Placebo0.3

[back to top]

Change From Baseline in Erythrocyte (RBC) Levels

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

Intervention(x10(12)/L) (Mean)
Ospemifene 30 mg (Dose 1)-0.081
Ospemifene 60 mg (Dose 2)-0.089
Placebo0.026

[back to top]

Change From Baseline in Erythrocyte (RBC) Levels

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

Intervention(x10(12)/L) (Mean)
Ospemifene 30 mg (Dose 1)-0.087
Ospemifene 60 mg (Dose 2)-0.155
Placebo0.028

[back to top]

Change From Baseline in Estradiol (E2) Levels

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

Interventionpg/mL (Mean)
Ospemifene 30 mg (Dose 1)0.75
Ospemifene 60 mg (Dose 2)0.94
Placebo0.15

[back to top]

Change From Baseline in Fibrinogen Levels

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

Interventionmg/dL (Mean)
Ospemifene 30 mg (Dose 1)-29.1
Ospemifene 60 mg (Dose 2)-25.9
Placebo12.1

[back to top]

Change From Baseline in Fibrinogen Levels

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

Interventionmg/dL (Mean)
Ospemifene 30 mg (Dose 1)-24.0
Ospemifene 60 mg (Dose 2)-36.0
Placebo7.4

[back to top]

Change From Baseline in Follicle Stimulating Hormone (FSH) Levels

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

InterventionIU/L (Mean)
Ospemifene 30 mg (Dose 1)-7.44
Ospemifene 60 mg (Dose 2)-9.87
Placebo-4.10

[back to top]

Change From Baseline in FSH Levels

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

InterventionIU/L (Mean)
Ospemifene 30 mg (Dose 1)-12.39
Ospemifene 60 mg (Dose 2)-15.60
Placebo-6.29

[back to top]

Change From Baseline in Hematocrit Levels

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

Interventionpercent change (Mean)
Ospemifene 30 mg (Dose 1)-0.435
Ospemifene 60 mg (Dose 2)-0.529
Placebo0.398

[back to top]

Change From Baseline in Hematocrit Levels

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

Interventionpercent change (Mean)
Ospemifene 30 mg (Dose 1)-0.445
Ospemifene 60 mg (Dose 2)-1.152
Placebo0.174

[back to top]

Change From Baseline in Hemoglobin Levels

(NCT01585558)
Timeframe: Baseine to Week 52 (Visit 6)

Interventiong/dL (Mean)
Ospemifene 30 mg (Dose 1)-0.141
Ospemifene 60 mg (Dose 2)-0.431
Placebo0.094

[back to top]

Change From Baseline in Hemogobin Levels

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

Interventiong/dL (Mean)
Ospemifene 30 mg (Dose 1)-0.150
Ospemifene 60 mg (Dose 2)-0.165
Placebo0.140

[back to top]

Change From Baseline in LH Levels

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

InterventionIU/L (Mean)
Ospemifene 30 mg (Dose 1)-2.65
Ospemifene 60 mg (Dose 2)-4.95
Placebo-0.09

[back to top]

Change From Baseline in Luteinizing Hormone (LH) Levels

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

InterventionIU/L (Mean)
Ospemifene 30 mg (Dose 1)-2.02
Ospemifene 60 mg (Dose 2)-2.86
Placebo-0.83

[back to top]

Change From Baseline in pH of Urine

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

InterventionpH (Mean)
Ospemifene 30 mg (Dose 1)0.2
Ospemifene 60 mg (Dose 2)0.0
Placebo0.1

[back to top]

Change From Baseline in pH of Urine

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

InterventionpH (Mean)
Ospemifene 30 mg (Dose 1)0.1
Ospemifene 60 mg (Dose 2)0.0
Placebo0.2

[back to top]

Change From Baseline in Protein C Ag, P Levels

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

Interventionpercent change (Mean)
Ospemifene 30 mg (Dose 1)8.2
Ospemifene 60 mg (Dose 2)-2.0
Placebo14.2

[back to top]

Change From Baseline in Protein C Ag, P Levels

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

Interventionpercent change (Mean)
Ospemifene 30 mg (Dose 1)4.9
Ospemifene 60 mg (Dose 2)-2.9
Placebo10.6

[back to top]

Change From Baseline in Protein S Ag (Free), P Levels

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

Interventionpercent change (Mean)
Ospemifene 30 mg (Dose 1)4.7
Ospemifene 60 mg (Dose 2)6.8
Placebo4.8

[back to top]

Change From Baseline in Protein S Ag (Free), P Levels

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

Interventionpercent change (Mean)
Ospemifene 30 mg (Dose 1)7.1
Ospemifene 60 mg (Dose 2)11.1
Placebo9.3

[back to top]

Change From Baseline in Pulse Rate

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

Interventionbpm (Mean)
Ospemifene 30 mg (Dose 1)2.0
Ospemifene 60 mg (Dose 2)0.8
Placebo2.2

[back to top]

Change From Baseline in Pulse Rate

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

Interventionbpm (Mean)
Ospemifene 30 mg (Dose 1)2.6
Ospemifene 60 mg (Dose 2)-0.5
Placebo2.9

[back to top]

Change From Baseline in SBP

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

InterventionmmHg (Mean)
Ospemifene 30 mg (Dose 1)-4.5
Ospemifene 60 mg (Dose 2)0.9
Placebo4.2

[back to top]

Change From Baseline in Sex Hormone Binding Globulin (SHBG) Levels

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

Interventionnmol/L (Mean)
Ospemifene 30 mg (Dose 1)11.71
Ospemifene 60 mg (Dose 2)22.64
Placebo-2.74

[back to top]

Change From Baseline in SHBG Levels

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

Interventionnmol/L (Mean)
Ospemifene 30 mg (Dose 1)11.94
Ospemifene 60 mg (Dose 2)28.09
Placebo-5.94

[back to top]

Change From Baseline in Specific Gravity of Urine

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

Interventionunits (Mean)
Ospemifene 30 mg (Dose 1)-0.001
Ospemifene 60 mg (Dose 2)-0.002
Placebo-0.001

[back to top]

Change From Baseline in Specific Gravtiy of Urine

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

Interventionunits (Mean)
Ospemifene 30 mg (Dose 1)-0.002
Ospemifene 60 mg (Dose 2)-0.003
Placebo-0.000

[back to top]

Change From Baseline in Systolic Blood Pressure (SBP)

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

InterventionmmHg (Mean)
Ospemifene 30 mg (Dose 1)-2.1
Ospemifene 60 mg (Dose 2)2.4
Placebo0.5

[back to top]

Change From Baseline in Testosterone (Free) Levels

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

Interventionng/dL (Mean)
Ospemifene 30 mg (Dose 1)-0.01
Ospemifene 60 mg (Dose 2)-0.00
Placebo-0.03

[back to top]

Change From Baseline in Testosterone (Free) Levels

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

Interventionng/dL (Mean)
Ospemifene 30 mg (Dose 1)0.02
Ospemifene 60 mg (Dose 2)-0.01
Placebo0.01

[back to top]

Change From Baseline in Testosterone (Total) Levels

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

Interventionng/dL (Mean)
Ospemifene 30 mg (Dose 1)1.61
Ospemifene 60 mg (Dose 2)2.59
Placebo-0.76

[back to top]

Change From Baseline in Testosterone (Total) Levels

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

Interventionng/dL (Mean)
Ospemifene 30 mg (Dose 1)1.92
Ospemifene 60 mg (Dose 2)3.48
Placebo-0.95

[back to top]

Change From Baseline in Thromboplastin Time

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

Interventions (Mean)
Ospemifene 30 mg (Dose 1)0.5
Ospemifene 60 mg (Dose 2)-0.6
Placebo0.3

[back to top]

Change From Baseline in Thromboplastin Time

(NCT01585558)
Timeframe: Baseline to Week 52 (Visit 6)

Interventions (Mean)
Ospemifene 30 mg (Dose 1)0.4
Ospemifene 60 mg (Dose 2)0.5
Placebo1.2

[back to top]

Change From Baseline in Weight

(NCT01585558)
Timeframe: Baseline to Week 26 (Visit 5)

Interventionkg (Mean)
Ospemifene 30 mg (Dose 1)-0.88
Ospemifene 60 mg (Dose 2)0.66
Placebo0.78

[back to top]

Change in FACT-ES Symptom Scores

Patients were given the Functional Assessment of Cancer Therapy - Endocrine Symptoms (FACT-ES) quality of life assessment at baseline (prior to tamoxifen administration) and again 18 months following breast surgery to assess quality of life. The difference in total score from baseline to 18 months was calculated. The FACT-ES total score ranges from 0-180, with higher scores indicating higher quality of life. (NCT01614210)
Timeframe: 18 months

Interventionchange in units on a scale (Mean)
Tamoxifen Pre and Post Breast Surgery-4.53

[back to top]

Change in FACT-ES Symptom Scores

Patients were given the Functional Assessment of Cancer Therapy - Endocrine Symptoms (FACT-ES) quality of life assessment at baseline (prior to tamoxifen administration) and again 7 days following start of tamoxifen to assess quality of life while on tamoxifen. The difference in total score from baseline to 7 days was calculated. The FACT-ES total score ranges from 0-180, with higher scores indicating higher quality of life. (NCT01614210)
Timeframe: 7 days

Interventionchange in units on a scale (Median)
Tamoxifen Pre and Post Breast Surgery1.5

[back to top]

Change in Ki67 Expression in Tumors

Demonstrate a significant change in Ki67 expression in tumors with 7 days of pre-surgical tamoxifen. (NCT01614210)
Timeframe: 7 days

Interventionpercentage change in Ki67 (Mean)
Tamoxifen Pre and Post Breast Surgery-40

[back to top]

Correlation Between Changes in Ki67 and Symptoms

Evaluate correlation between changes in Ki67 expression and symptom scores. Differences between changes in FACT-ES total score were correlated with changes in Ki67 expression using a the Spearman correlation method and results are expressed as the correlation coefficient. (NCT01614210)
Timeframe: 7 days

Interventionspearman correlation coefficient (Number)
Tamoxifen Pre and Post Breast Surgery-0.02

[back to top]

Number of Participants With Long Term Endocrine Therapy Adherence

For the patient population on this study, endocrine therapy was indicated for 5 years post-surgery according to the current standard of care recommendations for hormone positive breast cancer. Endocrine therapy was prescribed as standard of care as appropriate for each patient's situation. At 18 months post-surgery, patients were evaluated to determine if they were taking their endocrine therapy as prescribed. (NCT01614210)
Timeframe: 18 months

Interventionparticipants adhering to therapy (Number)
Tamoxifen Pre and Post Breast Surgery33

[back to top]

Distant Recurrence-Free Survival (DRFS)

Time from date of registration to date of invasive distant disease recurrence, second invasive primary cancer (breast or not) or death due to any cause. Patients last known to be alive who have not experienced distant recurrence, or second primary cancer are censored at their last contact date. The results were presented as 5-year DRFS estimate. (NCT01674140)
Timeframe: 5 years after last accrual

Interventionpercentage of participants (Number)
Placebo75.7
Everolimus76.9

[back to top]

Invasive Disease-Free Survival (IDFS)

Time from date of registration to date of first invasive recurrence (local, regional or distant), second invasive primary cancer (breast or not), or death due to any cause. Patients last known to be alive who have not experienced recurrence or second primary cancer are censored at their last contact date. The results were presented as 5-year IDFS estimate. (NCT01674140)
Timeframe: Up to 5 years post registration

Interventionpercentage of participants (Number)
Placebo74.4
Everolimus74.9

[back to top]

Overall Survival (OS)

Time from date of registration to date of death due to any cause. Patients last known to be alive are censored at their last contact date. The results were presented as 5-year OS estimate. (NCT01674140)
Timeframe: 5 years after last accrual

Interventionpercentage of participants (Number)
Placebo85.8
Everolimus88.1

[back to top]

Toxicity Based on Common Terminology Criteria for Adverse Events (CTCAE) Version 4.0, Assessed up to 10 Years.

Toxicity based on Common Terminology Criteria for Adverse Events (CTCAE) version 4.0. Only adverse events that are possibly, probably, or definitely related to study drug are reported. (NCT01674140)
Timeframe: Every 6 weeks while on protocol therapy. Adverse events (AEs) that occurred during follow up after protocol treatment were reported as late AEs, for every 6 months for the first 2 years and then yearly until 10 years after registration.

,
InterventionParticipants (Number)
Abdominal painAlanine aminotransferase increasedAllergic reactionAnemiaAnxietyAppendicitisAppendicitis perforatedArthralgiaAscitesAspartate aminotransferase increasedBack painBone painBreast infectionCardiac arrestCholecystitisCholesterol highColitisCoughDehydrationDepressionDiarrheaDizzinessDyspneaEdema faceEdema limbsEye disorders - Other, specifyEye infectionFatigueFeverGallbladder infectionGallbladder perforationGastrointestinal disorders - Other, specifyGeneral disorders and admin site conditions - OtherGeneralized muscle weaknessHeadacheHeart failureHip fractureHot flashesHyperglycemiaHyperhidrosisHyperkalemiaHypertensionHypertriglyceridemiaHypokalemiaHyponatremiaHypophosphatemiaHypoxiaImmune system disorders - Other, specifyInfections and infestations - Other, specifyInfusion related reactionInsomniaInvestigations - Other, specifyIrregular menstruationJoint infectionKidney infectionLeft ventricular systolic dysfunctionLipase increasedLung infectionLymphedemaLymphocyte count decreasedMenorrhagiaMucositis oralMuscle weakness lower limbMuscle weakness upper limbMusculoskeletal and connective tiss disorder - OtherMyalgiaNasal congestionNauseaNeck painNervous system disorders - Other, specifyNeuralgiaNeutrophil count decreasedObesityOtitis mediaPainPain in extremityPapulopustular rashParoxysmal atrial tachycardiaPeriorbital edemaPeripheral sensory neuropathyPlatelet count decreasedPleural effusionPneumonitisPortal vein thrombosisPostoperative hemorrhageProductive coughPruritusPsychiatric disorders - Other, specifyPulmonary edemaRadiation recall reaction (dermatologic)Rash acneiformRash maculo-papularRash pustularRespiratory failureSepsisSeromaSkin and subcutaneous tissue disorders - OtherSkin infectionSkin ulcerationSoft tissue infectionSore throatSuicidal ideationSuicide attemptThromboembolic eventTooth infectionUpper respiratory infectionUrinary tract infectionVascular access complicationVomitingWeight gainWeight lossWhite blood cell decreasedWound complicationWound dehiscenceWound infection
Everolimus74210012516016019123213271111231112114410332115355212151311122061360601012121012201001022427111201214207138221115112110220546
Placebo1100120101101100100030200006000000100210064000004000100012051201000011031011010110100011000001000300000300101202010

[back to top]

Overall Response Rate as Measured by Clinical Exam, Standard Imaging, and Surgical Pathology Findings

"Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and assessed by MRI: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR.~Evaluated using chi-square analysis." (NCT01831076)
Timeframe: Up to 6 months

InterventionParticipants (Count of Participants)
Exemestane23
Exemestane Plus Tamoxifen0

[back to top]

Effect of Medication on Change in Grip Strength

Effect of either aromatase inhibitor or tamoxifen therapy on change in grip strength between baseline and 12 months (NCT01896050)
Timeframe: baseline and 12 months

Interventionpercent change (Mean)
AI Therapy-7.0
Tamoxifen0.6

[back to top]

Effect of Change in Body Mass Index on Change in Grip Strength With Aromatase Inhibitor Therapy

Change in BMI between baseline and 12 months of endocrine therapy (NCT01896050)
Timeframe: baseline and 12 months

Interventionkg/m^2 (Mean)
AI Therapy-0.15
Tamoxifen2.44

[back to top]

Association Between Baseline Body Mass Index and Discontinuation of Aromatase Inhibitor Therapy Within the First 12 Months

Associations between baseline BMI and whether or not aromatase inhibitor-treated patients discontinued treatment by 12 months. In the original statistical analysis plan, it was only intended to examine the association with aromatase inhibitor-treated patients, and not tamoxifen-treated patients. The numbers below reflect the number of patients in each group who discontinued initial endocrine therapy within the first 12 months of treatment (NCT01896050)
Timeframe: baseline and 12 months

Interventionparticipants (Number)
Aromatase Inhibitor37
Tamoxifen2

[back to top] [back to top] [back to top]

2-year Treatment Discontinuation Rate by Aromatase Inhibitor and Tamoxifen-based Therapy Subgroup

The 2-year treatment discontinuation rate is the percentage of participants who do not complete the palbociclib treatment per protocol for reason due to toxicity, withdrawal of consent to be treated, or other events related to tolerability of all enrolled participants. (NCT02040857)
Timeframe: Evaluate upon completion of palbociclib, up to 2 years of treatment completion.

Interventionpercentage of participants (Number)
Aromatase Inhibitor + Palbociclib28
Tamoxifen + Palbociclib35

[back to top]

2-Year Treatment Discontinuation Rate

The 2-year treatment discontinuation rate is the percentage of participants who do not complete the palbociclib treatment per protocol for reasons due to toxicity, withdrawal of consent to be treated, or other events related to tolerability in uncensored participants. Participants who discontinued palbociclib early for reasons that were not treatment-related were censored. (NCT02040857)
Timeframe: Evaluate upon completion of palbociclib, up to 2 years of treatment completion.

Interventionpercentage of participants (Number)
Palbociclib With Adjuvant Endocrine Therapy31

[back to top] [back to top] [back to top]

Bleeding Days

The primary objective of this study is to determine whether tamoxifen taken by users of the ENG implant on an as-needed basis for frequent or prolonged bleeding can reduce the number of bleeding days by at least 40% over 180 days, when compared to placebo. (NCT02070692)
Timeframe: 180 days

Interventiondays (Mean)
Tamoxifen65.6
Placebo46.9

[back to top]

Consecutive Bleeding-free Days After Study Drug

Consecutive bleeding-free days after study drug (NCT02070692)
Timeframe: up to 180 days

Interventiondays (Mean)
Tamoxifen28.8
Placebo13.6

[back to top]

Satisfaction (as Recorded on a 100mm Visual Analog Scale Where 0 is Not at All Satisfied and 100mm is Completely Satisfied)

Secondary objective is to determine whether tamoxifen can improve satisfaction with the implant and with bleeding patterns. (NCT02070692)
Timeframe: 180 days

Interventionunits on a scale (Mean)
Tamoxifen61.4
Placebo53.6

[back to top]

Number of Participants Experiencing Ovulation After First Use of Study Drug

A third secondary objective is to determine whether taking tamoxifen at this dose compromises ovulation suppression in ENG users. Tamoxifen is known to transiently raise serum estradiol levels, but does not affect gonadotropin release in premenopausal women. Therefore, it is unlikely to interact with the ovulation suppression provided by the implant. However, to further investigate any theoretical interaction between tamoxifen and etonogestrel, urine markers of ovulation will be collected to document ongoing ovulation suppression with intermittent tamoxifen use. (NCT02070692)
Timeframe: 30 days

InterventionParticipants (Count of Participants)
Tamoxifen0
Placebo0

[back to top]

Bleeding/Spotting Days

Bleeding/spotting days (NCT02070692)
Timeframe: 30 days

Interventiondays (Mean)
Tamoxifen10.5
Placebo15.5

[back to top]

Effect of Tamoxifen on Exposure to Olaparib - AUC0-τ

Olaparib AUC0-τ, in the presence and absence of co-administered tamoxifen, and associated AUC0-τ treatment ratios (NCT02093351)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 12 hours post morning dose on Day 5 and Day 31

Interventionmcg*h/mL (Geometric Mean)
Cohort 1 - Olaparib (Treatment Period 1)62.12
Cohort 1 - Olaparib + Tamoxifen (Treatment Period 3)42.27

[back to top]

Effect of Olaparib on Exposure to Letrozole - Cmax ss

Letrozole Cmax ss in the presence and absence of co-administered olaparib, and associated Cmax ss treatment ratios (NCT02093351)
Timeframe: Pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post-dose on Day 38 and Day 43

Interventionmcg/mL (Geometric Mean)
Cohort 3 - Letrozole Alone (Treatment Period 2)118.9
Cohort 3 - Olaparib + Letrozole (Treatment Period 3)111.8

[back to top]

Effect of Olaparib on Exposure to Letrozole - AUC0-τ

Letrozole AUC0-τ, in the presence and absence of co-administered olaparib, and associated AUC0-τ treatment ratios (NCT02093351)
Timeframe: Pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post-dose on Day 38 and Day 43

Interventionmcg*h/mL (Geometric Mean)
Cohort 3 - Letrozole Alone (Treatment Period 2)2292
Cohort 3 - Olaparib + Letrozole (Treatment Period 3)2167

[back to top]

Effect of Anastrozole on Exposure to Olaparib - AUC0-τ

Olaparib AUC0-τ, in the presence and absence of co-administered anastrozole, and associated AUC0-τ treatment ratios (NCT02093351)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 12 hours post morning dose on Day 5 and Day 24

Interventionmcg*h/mL (Geometric Mean)
Cohort 2 - Olaparib (Treatment Period 1)55.49
Cohort 2 - Olaparib + Anastrozole (Treatment Period 3)44.33

[back to top]

Effect of Olaparib on Exposure to Anastrozole - AUC0-τ

Anastrozole Area under plasma concentration-time curve over the dosing interval at steady state (AUC0-τ), in the presence and absence of co-administered olaparib, and associated AUC0-τ treatment ratios (NCT02093351)
Timeframe: Pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post-dose on Day 19 and Day 24

Interventionmcg*h/mL (Geometric Mean)
Cohort 2 - Anastrozole Alone (Treatment Period 2)696.8
Cohort 2 - Olaparib + Anastrozole (Treatment Period 3)582.5

[back to top]

Effect of Letrozole on Exposure to Olaparib - AUC0-τ

Olaparib AUC0-τ, in the presence and absence of co-administered letrozole, and associated AUC0-τ treatment ratios (NCT02093351)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 12 hours post morning dose on Day 5 and Day 43

Interventionmcg*h/mL (Geometric Mean)
Cohort 3 - Olaparib (Treatment Period 1)61.77
Cohort 3 - Olaparib + Letrozole (Treatment Period 3)67.82

[back to top]

Effect of Letrozole on Exposure to Olaparib - Cmax ss

Olaparib Cmax ss in the presence and absence of co-administered letrozole, and associated Cmax ss treatment ratios (NCT02093351)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 12 hours post morning dose on Day 5 and Day 43

Interventionmcg/mL (Geometric Mean)
Cohort 3 - Olaparib (Treatment Period 1)10.05
Cohort 3 - Olaparib + Letrozole (Treatment Period 3)10.48

[back to top]

Effect of Olaparib on Exposure to Tamoxifen - Cmax ss

Tamoxifen, N-desmethyl tamoxifen (N-DMT) and endoxifen Cmax ss in the presence and absence of co-administered olaparib, and associated Cmax ss treatment ratios (NCT02093351)
Timeframe: Pre-dose and at 1, 2, 4, 5, 6, 8, 12 and 24 hours post-dose on Day 26 and Day 31

,
Interventionmcg/mL (Geometric Mean)
PK analysis of tamoxifenPK analysis of N-DMTPK analysis of endoxifen
Cohort 1 - Olaparib + Tamoxifen (Treatment Period 3)154.2149.15.727
Cohort 1 - Tamoxifen Alone (Treatment Period 2)130.3162.95.923

[back to top]

Effect of Olaparib on Exposure to Tamoxifen - AUC0-τ

Tamoxifen, N-DMT and endoxifen AUC0-τ, in the presence and absence of co-administered olaparib, and associated AUC0-τ treatment ratios (NCT02093351)
Timeframe: Pre-dose and at 1, 2, 4, 5, 6, 8, 12 and 24 hours post-dose on Day 26 and Day 31

,
Interventionmicrogram x hour/millilitre (mcg*h/mL) (Geometric Mean)
PK analysis of tamoxifenPK analysis of N-DMTPK analysis of endoxifen
Cohort 1 - Olaparib + Tamoxifen (Treatment Period 3)27512955115.8
Cohort 1 - Tamoxifen Alone (Treatment Period 2)22333189119.3

[back to top]

Effect of Anastrozole on Exposure to Olaparib - Cmax ss

Olaparib Cmax ss in the presence and absence of co-administered anastrozole, and associated Cmax ss treatment ratios (NCT02093351)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 12 hours post morning dose on Day 5 and Day 24

Interventionmcg/mL (Geometric Mean)
Cohort 2 - Olaparib (Treatment Period 1)9.490
Cohort 2 - Olaparib + Anastrozole (Treatment Period 3)8.256

[back to top]

Effect of Olaparib on Exposure to Anastrozole - Cmax ss

Anastrozole maximum plasma concentration at steady state (Cmax ss) in the presence and absence of co-administered olaparib, and associated Cmax ss treatment ratios (NCT02093351)
Timeframe: Pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post-dose on Day 19 and Day 24

Interventionmicrograms per millilitre (mcg/mL) (Geometric Mean)
Cohort 2 - Anastrozole Alone (Treatment Period 2)40.98
Cohort 2 - Olaparib + Anastrozole (Treatment Period 3)35.83

[back to top]

Effect of Tamoxifen on Exposure to Olaparib - Cmax ss

Olaparib Cmax ss in the presence and absence of co-administered tamoxifen, and associated Cmax ss treatment ratios (NCT02093351)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 12 hours post morning dose on Day 5 and Day 31

Interventionmcg/mL (Geometric Mean)
Cohort 1 - Olaparib (Treatment Period 1)9.456
Cohort 1 - Olaparib + Tamoxifen (Treatment Period 3)7.216

[back to top]

Incidence of Adverse Events (AEs)

Number of treated patients with Adverse Events (grade 3 or higher) observed while receiving randomized therapy. Excludes AEs observed among control patients treated with trametinib after crossover.Participants were analyzed based on their group of assignment. Patients on Arm A who progressed were permitted to receive Arm B treatment. Study time for Arm A patients who crossed over was not included in the AE endpoint definition. (NCT02101788)
Timeframe: During treatment period and up to 100 days after stopping the study treatment

,
Interventionparticipants (Number)
Abdominal painAnemiaDiarrheaFatigueHypertensionNauseaNeutrophil count decreasedRash maculo-papularSmall Intestinal ObstructionVomiting
Arm A - Control Arm22124561410910
Arm B - Experimental Arm7161310151289169

[back to top]

Overall Survival

Overall survival (OS) was defined as the number of months between study enrollment and death from any cause. Patients still alive at the last follow-up were censored on the date of last contact. Patients with disease progression on the Control arm were allowed to cross over to the trametinib arm. Per the protocol, the intent-to-treat OS analysis was not adjusted for crossover. (NCT02101788)
Timeframe: Time from study entry to time of death or date of last contact, an average of 29 months for arm A and 37 months for arm B

InterventionMonths (Median)
Arm A - Control Arm29.2
Arm B - Experimental Arm37.0

[back to top]

Objective Tumor Response Rate (Complete Response and Partial Response)

The Response Rates were estimated as the binomial proportion of patients with Best Overall Response of Complete or Partial response according to RECIST 1.1 criteria. (NCT02101788)
Timeframe: Time from study entry to time of progression or death, an average of 7 months for arm A and 13 months for arm B

Interventionparticipants (Number)
Arm A - Control Arm8
Arm B - Experimental Arm34

[back to top]

Patients Reported Acute Quality of Life

Patient reported quality of life was measured with the Treatment Outcome Index (TOI) of the Functional Assessment of Cancer Therapy for ovarian cancer (FACT-O TOI). The FACT-O TOI is a scale for assessing general QOL of ovarian cancer patients. It consists of three subscales: Physical Well Being (7 items), Functional Well Being (7 items), and Ovarian Cancer subscale (11 items). . The FACT-O TOI score is calculated as the sum of the subscale scores if more than 80% of the FACT-O TOI items provide valid answers and all of the component subscales have valid scores. The FACT-O TOI score ranges 0-100 with a large score suggesting better QOL. Participants were analyzed based on their group of assignment. Patients on Arm A who progressed were permitted to receive Arm B treatment. Study time for Arm A patients who crossed over was not included in the quality of life endpoint definition (NCT02101788)
Timeframe: 1. baseline (prior to cycle 1), 12 weeks (prior to cycle 4), 24 weeks (4 weeks post cycle 6), 36 weeks post cycle 1, 52 weeks post cycle 1.

,
Interventionscore on a scale (Mean)
Baseline12 Weeks24 Weeks36 Weeks52 Weeks
Arm A (Letrozole, Tamoxifen, Paclitaxel, PLD, Topotecan)74.574.270.269.372.1
Arm B (Trametinib)74.570.673.072.673.3

[back to top]

Progression Free Survival

Progression free survival (PFS) was defined as the number of months between study enrollment and documentation of disease progression (RECIST 1.1) or death from any cause. Patients still alive and disease free at the last followup were censored on the date of last CT Scan. RECIST v1.1 defines progression as at least a 20% increase in the sum of the diameters of target lesions, taking as reference the smallest sum on study (this includes the baseline sum if that is the smallest on study). In addition to the relative increase of 20%, the sum must also demonstrate an absolute increase of at least 5 mm. The appearance of one or more new lesions is also considered progression. (NCT02101788)
Timeframe: Time from study entry to time of progression or death, an average of 7 months for SOC and 13 months for the treatment (Trametinib) arm.

InterventionMonths (Median)
KRAS/BRAF/NRAS Mutant Group (MAPK Pathway) (Trametinib)13.2
KRAS/BRAF/NRAS Mutant Group (MAPK Pathway) (SOC)11.4
KRAS/BRAF/NRAS Wild-type (MAPK Pathway) (Trametinib)7.3
KRAS/BRAF/NRAS Wild-type (MAPK Pathway) (SOC)6.3

[back to top]

Patient Reported Acute Peripheral Neuropathy Symptoms

Patient reported peripheral neuropathy symptoms was measured with the Functional Assessment of Cancer Therapy/Gynecologic Oncology Group - neurotoxicity subscale (short version) (FACT/GOG-Ntx subscale). The FACT/GOG-Ntx subscale contains 4 items. Each item was scored using a 5-point scale (0=not at all; 1=a little bit; 2=somewhat; 3=quite a bit; 4=very much). According to the FACIT measurement system, the Ntx score was the summation of the individual item scores if more than 50% of subscale items were answered. When unanswered items existed, a subscale score was prorated by multiplying the mean of the answered item scores by the number of items in the scale. The Ntx score ranges 0-16 with a large score suggesting less peripheral neuropathy symptoms (NCT02101788)
Timeframe: Up to 52 weeks

,
Interventionscore on a scale (Mean)
Baseline12 Weeks24 Weeks36 Weeks52 Weeks
Arm A (Letrozole, Tamoxifen, Paclitaxel, PLD, Topotecan)13.212.512.412.312.8
Arm B (Trametinib)12.812.612.112.612.4

[back to top]

Progression-free Survival (PFS)

Progression free survival (PFS) was defined as the number of months between study enrollment and documentation of disease progression (RECIST 1.1) or death from any cause. Patients still alive and disease free at the last followup were censored on the date of last CT Scan.Participants were analyzed based on their group of assignment. Patients on Arm A who progressed were permitted to receive Arm B treatment. Study time for Arm A patients who crossed over was not included in the PFS endpoint definition. (NCT02101788)
Timeframe: Time from study entry to time of progression or death, an average of 7 months for arm A and 13 months for arm B

Interventionmonths (Median)
Arm A - Control Arm7.2
Arm B - Experimental Arm13.0

[back to top]

Evaluate the Efficacy for Treatment of Low/Intermediate- Risk Bladder Tumors, Assessing for the Clinical Response of the Marker Lesion

Evaluate the efficacy of tamoxifen for treatment of low/intermediate-risk bladder tumors, utilizing the RECIST criteria combined with the final biopsy of the marker lesion or the bed of the lesion in case of a complete response (NCT02197897)
Timeframe: 2.5 years

InterventionParticipants (Count of Participants)
Tamoxifen13

[back to top]

Frequency of Response

"A confirmed complete or partial response as defined by RECIST 1.1 was considered a response. Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.1) for target lesions and assessed by MRI: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR" (NCT02228681)
Timeframe: From date of randomization until the date of first documented progression or date of death , up to 3 years.

InterventionNumber of participants (Number)
Everolimus and Letrozole9
Tamoxifen and Medroxyprogesterone Acetate8

[back to top]

Median Progression-free Survival

Progression-free Survival is defined as the duration alive from study entry until progression is documented, or death; whichever comes sooner. Progressive disease is defined as at least a 5 mm absolute increase and a 20% relative increase in the sum of measurable target lesions' longest dimensions relative to the smallest sum at baseline or on study or the appearance of new lesions or unequivocal progression of existing non-target lesions. (NCT02228681)
Timeframe: Tumor measurements were done at 8 and 16 weeks after initiating treatment and then every 12 weeks and compared with baseline measurements prior to treatment. Measurements are continued until disease progression is documented or death.

Interventionmonths (Median)
Everolimus and Letrozole6.4
Tamoxifen and Medroxyprogesterone Acetate3.7

[back to top]

Median Survival

Survival is defined as the duration alive from study entry until death. (NCT02228681)
Timeframe: Following treatment discontinuation, patients are followed quarterly for 2 years, semi-annually for 3 more years, annually thereafter.

InterventionMonths (Median)
Everolimus and LetrozoleNA
Tamoxifen and Medroxyprogesterone Acetate16.6

[back to top]

Frequency and Severity of CTCAE (Common Toxicity Criteria for Adverse Events) Version 4

Maximum grade of physician assessed adverse events graded and categorized using Common Toxicity Criteria for Adverse Events (CTCAE) version 4 (NCT02228681)
Timeframe: Assessed throughout the treatment period and for 30 days after discontinuation of treatment. Treatment continues until progression of disease.

,
InterventionParticipants (Count of Participants)
Grade 1Grade 2Grade 3Grade 4Grade 5
Everolimus and Letrozole262720
Tamoxifen and Medroxyprogesterone Acetate2141721

[back to top]

Clinical Benefit Rate (CBR)

Percentage of participants with complete response (CR) or partial response (PR) or stable disease (SD) lasting 24 weeks or longer as defined in RECIST 1.1.CR = Disappearance of all non-nodal target lesions. In addition, any pathological lymph nodes assigned as target lesions must have a reduction in short axis to < 10 mm; PR = At least a 30% decrease in the sum of diameter of all target lesions, taking as reference the baseline sum of diameters; SD = Neither sufficient shrinkage to qualify for PR or CR nor an increase in lesions which would qualify for progressive disease: PD = At least a 20% increase in the sum of diameter of all measured target lesions, taking as reference the smallest sum of diameter of all target lesions recorded at or after baseline. In addition to the relative increase of 20% the sum must also demonstrate an absolute increase of at least 5 mm. (NCT02278120)
Timeframe: Up to approximately 25 months

InterventionPercentage of participants (Number)
LEE011 + NSAI/Tamoxifen + Goserelin79.1
LEE011 Placebo + NSAI/Tamoxifen+ Goserelin69.7

[back to top]

Duration of Response (DOR) Per Investigator's Assessment - Patients With Confirmed Complete Response (CR) or Partial Response (PR)

Time from the first documented response (CR or PR) to the first documented progression or death due to underlying cancer (NCT02278120)
Timeframe: Up to approximately 25 months

InterventionMonths (Median)
LEE011 + NSAI/Tamoxifen + Goserelin21.3
LEE011 Placebo + NSAI/Tamoxifen+ Goserelin17.5

[back to top]

Progression Free Survival (PFS) Per Investigator's Assessment

PFS, defined as the time from the date of randomization to the date of the first documented progression or death due to any cause and assessed according to Response Evaluation Criteria In Solid Tumors (RECIST) v1.1]. PFS was assessed via a local radiology assessment according to RECIST 1.1 (NCT02278120)
Timeframe: Up to approximatley 25 months

InterventionMonths (Median)
LEE011 + NSAI/Tamoxifen + Goserelin23.8
LEE011 Placebo + NSAI/Tamoxifen+ Goserelin13.0

[back to top]

Overall Response Rate (ORR) Per Local Assessment

ORR is the percentage of participants with the best overall response of complete response (CR) or partial response (PR) according to RECIST 1.1. CR = Disappearance of all non-nodal target lesions. In addition, any pathological lymph nodes assigned as target lesions must have a reduction in short axis to < 10 mm; PR = At least a 30% decrease in the sum of diameter of all target lesions, taking as reference the baseline sum of diameters. (NCT02278120)
Timeframe: Up to approximately 25 months

InterventionPercentage of participants (Number)
LEE011 + NSAI/Tamoxifen + Goserelin40.9
LEE011 Placebo + NSAI/Tamoxifen+ Goserelin29.7

[back to top]

Time to Response (TTR) Per Local Investigator's Assessment

Time to response is the time from the date of randomization to the first documented response (CR or PR, which must be confirmed subsequently) according to RECIST 1.1. All patients will be included in time to response calculations. Patients who do not achieve a confirmed response will be censored at the maximum follow-up time (i.e. first patient first visit to last patient last visit used for the analysis) for patients who had a PFS event (i.e. either progressed or died due to any cause) or at the date of last adequate tumor assessment otherwise. (NCT02278120)
Timeframe: Up to approximately 25 months

Interventionmonths (Median)
LEE011 + NSAI/Tamoxifen + GoserelinNA
LEE011 Placebo + NSAI/Tamoxifen+ GoserelinNA

[back to top]

Median Overall Survival (OS)

Defined as the time from date of first study treatment to date of death due to any cause. Patients who are alive will be censored at the date of last known date alive. (NCT02291913)
Timeframe: up to 3 years from first treatment

Interventionmonths (Median)
Everolimus26.7

[back to top]

Median Progression Free Survival (PFS)

PFS is defined as the time from Day 1 of study drug administration to disease progression as defined by RECIST (Response Evaluation Criteria in Solid Tumors) version 1.1 criteria, or death on study. Participants who are alive and free from disease progression will be censored at the date of last radiologic tumor assessment. Participants who receive non-protocol therapy (subsequent therapy) prior to incurring an event will be censored at the date of last tumor assessment prior to the start of subsequent therapy. Participants who do not have a post-baseline tumor assessment will be censored at the date of first treatment (Day 1). (NCT02291913)
Timeframe: up to 3 years

Interventionmonths (Median)
Everolimus7.2

[back to top]

Median Time From First Occurrence of CR or PR to Disease Progression or Death Also Called Duration of Response (DOR)

Only those patients who achieved Complete Response or Partial Response will be included in the summaries of DOR. DOR is defined as time from first date of response of CR or PR to disease progression or death as defined by RECIST v1.1 criteria. Participants who are alive and free from disease progression will be censored at the date of last tumor assessment. Patients who receive non-protocol therapy (subsequent therapy) prior to incurring an event will be censored at the date of last tumor assessment prior to the start of subsequent therapy. A CR is the complete disappearance of all target lesions. A PR is a decrease of 30% or more of the diameter(s) of all target lesions from the baseline sum of diameters. (NCT02291913)
Timeframe: every 8 weeks until discontinuation, up to 20 months

Interventionmonths (Median)
Everolimus8.8

[back to top]

Number of Participants With CR, PR, or 6 Months of SD Also Called Clinical Benefit Rate (CBR)

The proportion of patients with Complete Response (CR) or Partial Response (PR) or 6 months or more of Stable Disease (SD). A CR is the complete disappearance of all target lesions. A PR is a decrease of 30% or more of the diameter(s) of all target lesions from the baseline sum of diameters. SD is not meeting the criteria for PR or a 20% increase in target lesions called Progressive Disease (PD). (NCT02291913)
Timeframe: Up to 20 months

InterventionParticipants (Count of Participants)
Everolimus12

[back to top]

Number of Patients With Adverse Events (AEs) as a Measure of Safety and Tolerability

Assessments were made through analysis of the reported incidence of treatment-emergent AEs. All participants who received at least one dose of protocol treatment were followed for safety. Adverse events were collected from day of first dose to 30 days after last protocol treatment and graded according to National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 4.03. (NCT02291913)
Timeframe: Up to 20 months

InterventionParticipants (Count of Participants)
Everolimus48

[back to top]

Number of Patients With an Objective Response (CR or PR) Also Called the Overall Response Rate (ORR).

Defined as the number of patients with objective evidence of complete or partial response (CR or PR) using RECIST version 1.1. A CR is the complete disappearance of all target lesions. A PR is a decrease of 30% or more of the diameter(s) of all target lesions from the baseline sum of diameters. (NCT02291913)
Timeframe: every 8 weeks until discontinuation, up to 20 months

InterventionParticipants (Count of Participants)
Everolimus2

[back to top]

Progression Free Survival (PFS)

The primary endpoint is progression-free survival (PFS) defined as the time from randomization to documentation of local, regional or distant disease progression or death without progression of disease. (NCT02311933)
Timeframe: Assessed up to 5 years

Interventiondays (Median)
Arm I (Z-endoxifen Hydrochloride)130
Arm II (Tamoxifen Citrate)42

[back to top]

Percentage of Participants With Grade 3 or 4 Neutropenia

Grade 3/4 neutropenia as defined by NCI Common Terminology Criteria for Adverse Events (CTCAE) v4.03 in patients with prior exposure to 1-3 lines of chemotherapy for metastatic breast cancer (NCT02384239)
Timeframe: Up to 24 months

Interventionpercentage of participants (Number)
Palbociclib 100mg19.4
Palbociclib 125mg20.5

[back to top]

Progression-free Survival (PFS)

PFS defined as the interval from study entry to the first documented evidence of disease progression by Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1 as at least a 20% increase in the sum of the longest diameter (SLD) of target lesions, taking as reference the smallest sum SLD recorded since the treatment started and minimum 5 mm increase over the nadir, or the appearance of one or more new lesions. Patients who remain progression-free at the time of analysis will be censored at their last date of follow-up. (NCT02384239)
Timeframe: Up to 24 months

Interventionmonths (Median)
Palbociclib 100mg6.53
Palbociclib 125mg9.4

[back to top]

Proportion of Participants With an Objective Response

Defined as the proportion of patients whose best overall response, according to RECIST, is either complete response (CR), a partial response (PR) at 24 weeks. Only those patients who have measurable disease present at baseline, have received at least one cycle of therapy, and have had their disease re-evaluated will be considered evaluable for response. (NCT02384239)
Timeframe: 24 weeks

Interventionproportion of participants (Number)
Palbociclib 100mg0.1111
Palbociclib 125mg0.0625

[back to top]

Proportion of Participants With Demonstrated Clinical Benefit

Defined as the proportion of patients whose best overall response, according to RECIST, is either complete response (CR), a partial response (PR) or stable disease (SD) at 24 weeks. Only those patients who have measurable disease present at baseline, have received at least one cycle of therapy, and have had their disease re-evaluated will be considered evaluable for response. (NCT02384239)
Timeframe: 24 weeks

Interventionproportion of participants (Number)
Palbociclib 100mg0.67
Palbociclib 125mg0.75

[back to top]

Median Change in Percent Positive Cells From Baseline of Ki-67

Median change in percent positive cells of Ki-67 from baseline will be reported with IQR (NCT02384239)
Timeframe: Up to 24 months

Interventionchange in percent positive cells (Median)
Palbociclib 100mg-8
Palbociclib 125mg-6

[back to top]

Median Change in Percent Positive Cells From Baseline of pS780-Rb

Median change in percent positive cells of pS780-Rb from baseline will be reported with IQR (NCT02384239)
Timeframe: Up to 24 months

Interventionchange in percent positive cells (Median)
Palbociclib 100mg-3
Palbociclib 125mg-6

[back to top]

Median Change in Percent Positive Cells From Baseline of Total-Rb

Median change in percent positive cells of Total-Rb from baseline will be reported with interquartile range (IQR) (NCT02384239)
Timeframe: Up to 24 months

Interventionchange in percent positive cells (Median)
Palbociclib 100mg4
Palbociclib 125mg5

[back to top] [back to top]

Progression Free Survival

Progression-free survival (PFS) is defined as the length of time during and after the treatment that the participant has achieved an objective response, but does not progress as measured by RECIST v.1.1 (NCT02395627)
Timeframe: Up to 36 months

Interventionmonths (Median)
Pembrolizumab Group A2.57
Pembrolizumab Group B2.63

[back to top]

Duration of Response

The duration of overall response is measured from the time measurement criteria are met for CR or PR (whichever is first recorded) until the first date that recurrent or progressive disease is objectively documented (taking as reference for progressive disease the smallest measurements recorded since the treatment started). (NCT02395627)
Timeframe: Up to 24 months

Interventionmonths (Median)
Pembrolizumab Group A17.0
Pembrolizumab Group B8.8

[back to top]

Overall Survival (OS)

OS is defined as the length of time from the start of treatment for participants until death or the study has ended, whichever comes first. (NCT02395627)
Timeframe: Up to 36 months

Interventionmonths (Median)
Pembrolizumab Group A14.3
Pembrolizumab Group B15.0
Pembrolizumab Group C7.8

[back to top]

Objective Response Rate (ORR)

Objective response rate (ORR) will be defined as the proportion of participants whose status is stable disease (SD) or better (complete response (CR), partial response (PR)) at 24 weeks' follow-up as measured by Response Evaluation Criteria in Solid Tumors (RECIST). The best overall response is the best response recorded from the start of the treatment until disease progression/recurrence (taking as reference for progressive disease the smallest measurements recorded since the treatment started). The patient's best response assignment will depend on the achievement of both measurement and confirmation criteria. (NCT02395627)
Timeframe: Up to 24 weeks

Interventionpercentage of participants (Number)
Pembrolizumab Group A6.67
Pembrolizumab: Group B0

[back to top] [back to top]

Overall Survival (OS) at Six Months

Occurrence of Overall Survival at 6 months. OS: On study date to expired date or last visit date if not deceased. (NCT02586675)
Timeframe: 6 months

Interventionpercentage of participants (Number)
Tamoxifen and Ribociclib With Goserelin83.3

[back to top]

Progression-free Survival (PFS) at Six Months

Occurrence of Progression Survival at 6 months. PFS: On study date to date of progression or the same as overall survival time if not progressed. Progressive Disease (PD): At least a 20% increase in the sum of the longest diameter (LD) of target lesions, taking as reference the smallest sum LD recorded since the treatment started or the appearance of one or more new lesions. (NCT02586675)
Timeframe: 6 months

Interventionpercentage of participants (Number)
Tamoxifen and Ribociclib With Goserelin57.1

[back to top] [back to top]

Duration of Response

For patients with complete or partial response, duration of response is defined as days from first recorded response to the first date of recurrent or progression or death. (NCT02630693)
Timeframe: 2 years

Interventiondays (Median)
Palbociclib (100mg)126
Palbociclib (125mg)169

[back to top]

Overall Survival

Time from randomization to death of any cause. (NCT02630693)
Timeframe: 2 years

Interventionmonths (Median)
Palbociclib (100mg)20.73
Palbociclib (125mg)21.39

[back to top]

Progression Free Survival Using the RECIST 1.1 Criteria

progression free survival (PFS) is defined as time from randomization to progression or death from any cause. Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.1), as a 20% increase in the sum of the longest diameter of target lesions, or a measurable increase in a non-target lesion, or the appearance of new lesions. (NCT02630693)
Timeframe: 2 years

Interventionmonths (Median)
Palbociclib (100mg)9.33
Palbociclib (125mg)11.30

[back to top]

Change From Baseline in Pain and Symptom Burden Assessment on the Modified Brief Pain Inventory-Short Form (mBPI-sf)

mBPI-sf is an 11-item instrument used as a multiple-item measure of cancer pain intensity. In addition to pain intensity (4 items), the mBPI-sf is designed for participants to record the presence of pain in general, pain relief, and pain interference with function (general activity, mood, ability to walk, ability to perform normal work, relations with others, sleep, enjoyment of life). Responses for the mBPI-sf items are captured through the use of 11-point numeric rating scales anchored at 0 (no pain or does not interfere) and 10 (pain as bad as you can imagine or completely interferes). The mBPI-sf recall period is 24 hours and typical completion time for this instrument is less than 5 minutes. (NCT02747004)
Timeframe: Baseline, 21 Months

,,
Interventionscore on a scale (Least Squares Mean)
Pain at its Worst in Last 24 HoursPain at its Least in Last 24 HoursPain on the AveragePain Right NowMean Interference Score
150mg Abemaciclib-0.43-0.01-0.20-0.180.03
150mg Abemaciclib + 20mg Tamoxifen-0.53-0.09-0.34-0.28-0.09
200mg Abemaciclib + 2mg Prophylactic Loperamide-0.430.14-0.11-0.040.16

[back to top]

Change From Baseline in Symptom Burden on the European Organization for Research and Treatment of Cancer Quality of Life Questionnaire-C30 (EORTC QLQ-C30)

"The EORTC QLQ-C30 self-reported general cancer instrument consists of 30 items covered by 1 of 3 dimensions:~Global health status/quality of life (2 items) with scores ranging from 1 (Very Poor) to 7 (Excellent).~Functional scales (15 total items addressing either physical, role, emotional, cognitive, or social functioning), each item scores ranging from 1 (not at all) to 4 (very much)~Symptom scales (13 total items addressing either fatigue, nausea/vomiting, pain, dyspnea, insomnia, appetite loss, constipation, diarrhea, or financial impact), each item scores ranging from 1 (not at all) to 4 (very much).~Raw scores are linearly converted to a 0-100 scale with higher scores reflecting higher levels of function/QOL or higher levels of symptom burden." (NCT02747004)
Timeframe: Baseline, 21 Months

,,
Interventionscore on a scale (Least Squares Mean)
Global Health StatusFunctional Scales (Physical Functioning)Functional Scales (Role Functioning)Functional Scales (Emotional Functioning)Functional Scale (Cognitive Functioning)Functional Scales (Social Functioning)Symptom Scales (Fatigue)Symptom Scales (Nausea and Vomiting)Symptom Scales (Pain)Symptom Scales (Dyspnoea)Symptom Scales (Insomnia)Symptom Scales (Appetite Loss)Symptom Scales (Constipation)Symptom Scales (Diarrhoea)Symptom Scales (Functional Difficulties)
150mg Abemaciclib4.56-1.05-3.952.58-1.31-0.532.775.30-1.43-3.49-3.431.87-6.2920.17-3.81
150mg Abemaciclib + 20mg Tamoxifen1.56-2.01-0.444.400.143.232.395.59-3.094.21-5.025.82-0.2813.31-7.56
200mg Abemaciclib + 2mg Prophylactic Loperamide-2.77-2.65-5.871.86-2.39-0.944.05.09-2.01-2.0-2.987.760.0817.43-0.09

[back to top]

PK: Mean Single Dose Concentration of Tamoxifen and Endoxifen

Mean single dose concentrations of Tamoxifen and its metabolite (Endoxifen) were reported. (NCT02747004)
Timeframe: Cycle 1 Day 1 post dose

Interventionng/mL (Geometric Mean)
Tamoxifen (C1D1)Endoxifen (C1D1)
150mg Abemaciclib + 20mg Tamoxifen7.47NA

[back to top]

Pharmacokinetics (PK): Mean Single Dose Concentration of Abemaciclib and Its Metabolites

Mean single dose concentrations of Abemaciclib and its metabolites (M2 & M20) are reported. (NCT02747004)
Timeframe: Cycle (C) 1 Day (D) 1 post dose

,,
InterventionNanogram per Millilitre (ng/mL) (Geometric Mean)
Abemaciclib (C1D1)M2 (C1D1)M20 (C1D1)
150mg Abemaciclib3.052.142.54
150mg Abemaciclib + 20mg Tamoxifen10.96.056.50
200mg Abemaciclib + 2mg Prophylactic Loperamide8.596.857.91

[back to top]

Duration of Response (DoR)

DoR is defined as the time from the date of first evidence of a CR or PR to the date of objective progression or death from any cause, whichever is earlier as defined by Recist v1.1. CR was defined as the disappearance of all target and non-target lesions and no appearance of new lesions. PR was defined as at least a 30% decrease in the sum of the LD of target lesions (taking as reference the baseline sum LD), no progression of non-target lesions, and no appearance of new lesions. (NCT02747004)
Timeframe: Date of CR or PR to Date of Objective Disease Progression or Death Due to Any Cause (Up to 21 Months)

InterventionMonths (Median)
150mg Abemaciclib + 20mg Tamoxifen7.40
150mg Abemaciclib9.21
200mg Abemaciclib + 2mg Prophylactic Loperamide7.46

[back to top]

PK: Multiple Dose Concentration of Tamoxifen and Endoxifen

Mean multiple dose concentrations of Tamoxifen and its metabolite (Endoxifen) were reported. (NCT02747004)
Timeframe: Cycle 1 Day 15, Cycle 2 Day 1, Cycle 2 Day 15, Cycle 3 Day 1 post dose

Interventionng/mL (Geometric Mean)
Tamoxifen (C1D15)Endoxifen (C1D15)Tamoxifen (C2D1)Endoxifen (C2D1)Tamoxifen (C2D15)Endoxifen (C2D15)Tamoxifen (C3D1)Endoxifen (C3D1)
150mg Abemaciclib + 20mg Tamoxifen84.54.7698.77.411099.1711210.3

[back to top]

Pharmacokinetics (PK): Steady State Concentration of Abemaciclib and Its Metabolites

"Mean steady state concentrations of Abemaciclib and its metabolites (M2 & M20) are reported.~C=Cycle D= Day" (NCT02747004)
Timeframe: Cycle 1 Day 15, Cycle 2 Day 1, Cycle 2 Day 15, Cycle 3 Day 1 post dose

,,
InterventionNanogram per Millilitre (ng/mL) (Geometric Mean)
Abemaciclib (C1D15)M2 (C1D15)M20 (C1D15)Abemaciclib (C2D1)M2 (C2D1)M20 (C2D1)Abemaciclib (C2D15)M2 (C2D15)M20 (C2D15)Abemaciclib (C3D1)M2 (C3D1)M20 (C3D1)
150mg Abemaciclib25610819918285.414915771.712817778.4146
150mg Abemaciclib + 20mg Tamoxifen21496.518098.956.110013562.312012560.6109
200mg Abemaciclib + 2mg Prophylactic Loperamide31414725122010516417595.415420795.8171

[back to top]

Objective Response Rate (ORR): Percentage of Participants With a Complete Response (CR) or Partial Response (PR)

Objective response rate was defined as the percentage of participants with CR or PR according to RECIST v1.1. CR was defined as the disappearance of all target and non-target lesions and no appearance of new lesions. PR was defined as at least a 30% decrease in the sum of the LD (longest diameter) of target lesions (taking as reference the baseline sum LD), no progression of non-target lesions, and no appearance of new lesions. (NCT02747004)
Timeframe: Baseline to Objective Disease Progression (Up to 21 Months)

InterventionPercentage of participants (Number)
150mg Abemaciclib + 20mg Tamoxifen34.6
150mg Abemaciclib24.1
200mg Abemaciclib + 2mg Prophylactic Loperamide32.5

[back to top]

Progression Free Survival (PFS)

Progression-free survival time was measured from the date of randomization to the date of investigator-determined objective progression as defined by RECIST v1.1, or death from any cause, whichever occurred first. Progressive disease (PD) is defined as at least a 20% increase in the sum of the diameters of target lesions, with reference being the smallest sum on study and an absolute increase of at least 5 mm, or unequivocal progression of non-target lesions, or 1 or more new lesions. Participants who have neither progressed nor died were censored at the day of their last radiographic tumor assessment (if available) or date of randomization if no post baseline radiographic assessment is available. (NCT02747004)
Timeframe: Baseline to Objective Disease Progression or Death from Any Cause (Up to 21 Months)

InterventionMonths (Median)
150mg Abemaciclib + 20mg Tamoxifen9.07
150mg Abemaciclib6.48
200mg Abemaciclib + 2mg Prophylactic Loperamide7.43

[back to top]

Percentage of Participants With Clinical Response in Arm C and Arm D in the Treatment Phase

Percentage of Participants with Clinical Response in Arm C and Arm D in Breast cancer patients diagnosed with hormone receptor positive invasive breast cancer; Clinical response rate is defined as the number of partial and complete responses after preoperative endocrine therapy plus palbociclib (Arm C) and of endocrine therapy alone (Arm D) (NCT02764541)
Timeframe: day 15 to 24 weeks

Interventionpercentage of participants (Number)
Arm C Endocrine With Palbociclib57.8
Arm D Endocrine Therapy Alone43.3

[back to top]

Number of Participants With RCB Response in Arm C and Arm D During the Treatment Phase

RCB response is defined as RCB-0 or RCB-I; RCB not response is defined as RCB-II or RCB-III Residual Cancer Burden (RCB) considers residual disease in the tumor bed and lymph nodes after NAC, generating a continuous score which is then grouped into four categories: RCB-0, RCB-I, RCB-II and RCB-III. Higher RCB group reflects more tumor burden remaining, thus worse outcome (NCT02764541)
Timeframe: day 15 to 24 weeks

InterventionParticipants (Count of Participants)
Arm C Endocrine With Palbociclib10
Arm D Endocrine Therapy Alone3

[back to top]

Change in RCB Index Between Arm C and Arm D During the Treatment Phase

The estimate of RCB index change for patients who receive both endocrine and Palbociclib instead of endocrine alone, but have the same lymph node status, tumor size and menopausal status. RCB score is used to assess the response to neoadjuvant chemotherapy in breast cancer patients and is in a scale of 0 to infinity. Higher RCB score indicates more tumor burden remaining, thus worse outcome. (NCT02764541)
Timeframe: day 15 to 24 weeks

Interventionunits on a scale (Mean)
Endocrine With Palbociclib2.88
Endocrine Alone2.88

[back to top]

Odds Ratio of Achieving Cell Cycle Arrest at the End of Window Phase

Odds Ratio of Achieving Cell Cycle Arrest at the end of Window Phase in hormone receptor positive invasive breast cancer patients given Tamoxifen vs Letrozole. Cell cycle arrest is defined to be percentage of Ki67<2.7 (NCT02764541)
Timeframe: baseline to day 15

Interventionodds ratio (Number)
Tamoxifen vs Letrozole in Invasive Ductal Patients0.26
Tamoxifen vs Letrozole in Invasive Lobular Patients0.60

[back to top]

Pathologic Complete Response (pCR) of Patients Given Endocrine Therapy Plus Palbociclib and of Endocrine Therapy Alone During the Treatment Phase

Residual Cancer Burden index (RCB) between hormone receptor positive invasive breast cancer patients given endocrine therapy plus palbociclib (Arm C) and endocrine therapy alone (Arm D). RCB score is used to assess the response to neoadjuvant chemotherapy in breast cancer patients and is in a scale of 0 to infinity. Higher RCB score indicates more tumor burden remaining, thus worse outcome. (NCT02764541)
Timeframe: day 15 to 24 weeks

Interventionscore on a scale (Mean)
Arm C Endocrine With Palbociclib2.88
Arm D Endocrine Therapy Alone2.88

[back to top]

Difference in Anti-proliferative Activity of Patients Given Letrozole Versus Tamoxifen During the Window Phase

Log fold change in anti-proliferative activity of Letrozole versus Tamoxifen within cohorts of hormone receptor positive breast cancer for patients with invasive lobular and ductal carcinoma during the window phase. Higher absolute value indicates larger change in the anti-proliferative activity (NCT02764541)
Timeframe: baseline to day 15

Interventionlog fold-change (Mean)
Tamoxifen With Invasive Ductal-0.180
Letrozole With Invasive Ductal-1.304
Tamoxifen With Invasive Lobular-0.635
Letrozole With Invasive Lobular-1.944

[back to top]

Pathologic Complete Response

Pathologic complete response was defined as no residual tumor at the primary site or the axillary lymph nodes at the time of surgery. (NCT02806544)
Timeframe: 4-6 months

Interventionparticipants (Number)
Tamoxifen1

[back to top]

Overall Clinical Response Rate

Clinical response rate was assessed by palpation after 4 months of tamoxifen. Complete response was defined as no palpable primary tumor on clinical examination and lymph nodes < 10 mm. Partial response was defined as at least 30% decrease in the sum of the diameters compared to baseline sum of diameters. The overall clinical response was the sum of the complete clinical response and partial clinical response. (NCT02806544)
Timeframe: 4-6 months

Interventionparticipants (Number)
Tamoxifen13

[back to top]

Number of Participants With Definitive Surgery in Responders to Neoadjuvant Tamoxifen

"Rate of definitive surgery after 4 months of neoadjuvant tamoxifen therapy in patients who were deemed to be responders to neoadjuvant tamoxifen (Ki67 < or = 10% after 4-6 weeks on neoadjuvant tamoxifen therapy)" (NCT02806544)
Timeframe: 4-6 months

Interventionparticipants (Number)
Tamoxifen13

[back to top]

Number of Participants Who Were Successfully Accrued in the Study, as a Measure of Feasibility

Feasibility is defined as the ability to recruit the stated number of patients and fifty percent of participants completing the trial. Completing the trial is defined as reaching surgery if they are a responder to tamoxifen or obtaining the six week biopsy specimen if they are a non-responder. (NCT02806544)
Timeframe: 4-6 months

Interventionparticipants (Number)
Tamoxifen35

[back to top]

Ki67 Suppression Rate at 4-6 Weeks in Patients Who Underwent an On-treatment Biopsy

Result is the number of participants who had Ki67 suppression (< or = 10%) after 4-6 weeks of neoadjuvant tamoxifen out of patients who underwent an on-treatment biopsy. (NCT02806544)
Timeframe: 4-6 weeks

Interventionparticipants (Number)
Tamoxifen15

[back to top]

Breast Conserving Therapy

"The rate of breast conservation surgery (as opposed to mastectomy) after 4 months of neoadjuvant tamoxifen therapy in patients who were deemed to be responders to neoadjuvant tamoxifen (Ki67 < or = 10% after 4-6 weeks on neoadjuvant tamoxifen therapy)." (NCT02806544)
Timeframe: 4-6 months

Interventionparticipants (Number)
Tamoxifen0

[back to top]

Adverse Events

Descriptive reporting of adverse events for each arm (NCT02824224)
Timeframe: 30 days after initiation of study drug

InterventionEvents (Number)
Tamoxifen12
Placebo15

[back to top]

Bleeding Pattern Satisfaction

0-100 mm Visual Analog Scale (VAS) measurement of satisfaction with bleeding pattern. 0 mm = not at all satisfied, 100 mm = very satisfied. (NCT02824224)
Timeframe: 30 days after initiation of study drug

Interventionunits on a scale (Mean)
Tamoxifen50.7
Placebo58.6

[back to top]

IUD Satisfaction

0-100 mm Visual Analog Scale (VAS) measurement of satisfaction with IUD (intrauterine device). 0 mm = not at all satisfied, 100 mm = very satisfied. (NCT02824224)
Timeframe: 30 days after initiation of study drug

Interventionunits on a scale (Mean)
Tamoxifen82.7
Placebo75.3

[back to top]

Number of Bleeding and Spotting Days

Mean number of bleeding and spotting days in the tamoxifen group compared to the mean number of bleeding and spotting days in the placebo group (NCT02824224)
Timeframe: 30 days after initiation of study drug

Interventiondays (Mean)
Tamoxifen16.8
Placebo12.0

[back to top]

Total Number of Consecutive Bleeding-free Days in First 30 Days From Day 1 of First Treatment (TX1)

Bleeding free days in the first 30 days (NCT02903121)
Timeframe: Day 1 to Day 30

Interventiondays (Mean)
Tamoxifen18.5
Placebo8.7

[back to top]

Total Number of Bleeding Free Days Over the Second 90 Day Reference Period From Day 1 of Treatment Number 4 to Day 90

bleeding free days in the second 90 days (NCT02903121)
Timeframe: Day 1 of treatment number 4 to Day 90 (second 90 day reference period)

Interventiondays (Median)
Tamoxifen56
Placebo67.5

[back to top]

Total Number of Bleeding Free Days Over the First 90 Day Reference Period From Day 1 of Treatment 1.

bleeding free days in the first 90 days (NCT02903121)
Timeframe: Day 1 to Day 90

Interventiondays (Median)
Tamoxifen60
Placebo52

[back to top]

Patient Satisfaction With Bleeding Pattern

Patient satisfaction with bleeding pattern. Assessed by visual analog scale to determine satisfaction with bleeding patterns on a scale of 0-100 mm, where 0 mm represents not satisfied at all and 100 mm is totally satisfied. (NCT02903121)
Timeframe: Day 1 of treatment 1 to day 180

Interventionmm (Median)
Tamoxifen67.5
Placebo54.25

[back to top]

Change in Background Parenchymal Uptake (BPU) on Molecular Breast Imaging (MBI)

An image analysis tool to obtain a quantitative measure of background parenchymal uptake (BPU) was applied to pre-tamoxifen and post-tamoxifen MBI exams. The percent change in BPU from pre-tamoxifen to post-tamoxifen MBI was determined. (NCT02979301)
Timeframe: 30 days

Interventionpercent change in BPU (Mean)
Tamoxifen 5 mg/Day0.0
Tamoxifen 10 mg/Day-12

[back to top]

Number of Participants Meeting Certain Preoperative Endocrine Prognostic Index (PEPI)

"Evaluate the number of participants meeting certain PEPI score after treatment with TAK-228 plus tamoxifen.~PEPI score of 0 indicates low risk of disease recurrence (better outcome) PEPI score of 1-3 indicates intermediate risk of of disease recurrence (worse outcome) PEPI score of >4 indicates high risk of of disease recurrence (worst outcome)" (NCT02988986)
Timeframe: 16 weeks

InterventionParticipants (Count of Participants)
PEPI score of 0PEPI score of 1-3PEPI score of >4
Tamoxifen0615

[back to top]

Number of Participants With Pathological Complete Response (pCR)

Pathologic complete response was defined as the absence of residual invasive cancer on hematoxylin and eosin evaluation of the complete resected breast specimen and all sampled regional lymph nodes following completion of neoadjuvant systemic therapy (i.e., ypT0 ypN0 or ypTis ypN0 in the current American Joint Committee on Cancer staging system). (NCT02988986)
Timeframe: 16 weeks

InterventionParticipants (Count of Participants)
TAK-228 Plus Tamoxifen0

[back to top]

Ki67 Expression

Ki67 expression change from baseline to 6 weeks (NCT02988986)
Timeframe: Baseline to 6 weeks

InterventionPercentage of cells with Ki67 expression (Median)
Ki67 expression at baselineKi67 expression at 6 weeks
TAK-228 Plus Tamoxifen1510

[back to top]

Progression-free Survival (PFS)

(NCT03045653)
Timeframe: 36months

Interventionmonths (Median)
Treatment Arm5

[back to top]

Change in Serum Concentration of Sex Hormone Binding Globulin (SHBG) From Baseline to Week 52/End of Study (EOS)

SHBG levels at baseline will be compared to levels at Week 52/EOS (NCT03199963)
Timeframe: Blinded Phase: Baseline; Week 52/EOS

Interventionmg/L (Mean)
BHR-700 (0.2% 4-OHT Gel)0.1
Matching Placebo Gel0.3

[back to top]

Change in Serum Concentration of: Cholesterol, Triglycerides, High-density Lipoprotein (HDL), and Low-density Lipoprotein (LDL).

Lipid levels at baseline will be compared to levels measured at time-points in the study (NCT03199963)
Timeframe: Blinded Phase: Baseline; Weeks 26, 52/EOS.

,
Interventionmmol/L (Mean)
Cholesterol (mmol/L) - Change from Baseline to Week 26Cholesterol (mmol/L) - Change from Baseline to Week 52/EOSTriglycerides (mmol/L) - Change from Baseline to Week 26Triglycerides (mmol/L) - Change from Baseline to Week 52/EOSHDL Cholesterol (mmol/L) - Change from Baseline to Week 26HDL Cholesterol (mmol/L) - Change from Baseline to Week 52/EOSLDL Cholesterol (mmol/L) - Change from Baseline to Week 26LDL Cholesterol (mmol/L) - Change from Baseline to Week 52/EOS
BHR-700 (0.2% 4-OHT Gel)-0.10.1-0.2-0.1-0.00.00.00.1
Matching Placebo Gel-0.20.0-0.20.00.00.0-0.1-0.0

[back to top]

Number and Severity of Adverse Events (AEs)

AEs monitored and reported throughout study (NCT03199963)
Timeframe: Blinded Phase: Baseline; Weeks 13, 26, 39, 52/EOS and Open Label Phase

,,,
InterventionParticipants (Count of Participants)
Subjects with at least one mild AESubjects with at least one moderate AESubjects with at least one severe AE
BHR-700 (0.2% 4-OHT Gel) in Blinded Phase56498
Matching Placebo Gel in Blinded Phase31294
Open Label BHR-700 (0.2% 4-OHT Gel) Following BHR-700 in Blinded Phase221
Open Label BHR-700 (0.2% 4-OHT Gel) Following Placebo in Blinded Phase110

[back to top]

Number of Participants With Measurable Plasma Concentrations of the E and Z Isomers of 4-OHT by Visit

Blood samples will be taken to measure plasma concentrations of 4-OHT at time-points in the study (NCT03199963)
Timeframe: Blinded Phase: Weeks 13, 26, 52/EOS

InterventionParticipants (Count of Participants)
Week 13 E-4-OHT72545323Week 26 E-4-OHT72545323Week 52/EOS E-4-OHT72545323Week 13 Z-4-OHT72545323Week 26 Z-4-OHT72545323Week 52/EOS Z-4-OHT72545323
Participants with concentration below lower limit Participants with measurable concentration
BHR-700 (0.2% 4-OHT Gel)12
BHR-700 (0.2% 4-OHT Gel)128
BHR-700 (0.2% 4-OHT Gel)7
BHR-700 (0.2% 4-OHT Gel)88
BHR-700 (0.2% 4-OHT Gel)0
BHR-700 (0.2% 4-OHT Gel)179
BHR-700 (0.2% 4-OHT Gel)75
BHR-700 (0.2% 4-OHT Gel)65
BHR-700 (0.2% 4-OHT Gel)48
BHR-700 (0.2% 4-OHT Gel)47
BHR-700 (0.2% 4-OHT Gel)16
BHR-700 (0.2% 4-OHT Gel)163

[back to top]

Change in Serum Concentration of Select Bone Biomarkers:Type I Collagen C-Telopeptides (CTx) (pg/mL)

Bone biomarker levels (CTx) at baseline will be compared to levels measured at Week 52. (NCT03199963)
Timeframe: Blinded Phase: Baseline; Week 52/EOS

Interventionpg/mL (Mean)
BHR-700 (0.2% 4-OHT Gel)-19.6
Matching Placebo Gel3.7

[back to top]

Change in Serum Concentration of Select Bone Biomarkers: Bone Specific Alkaline Phosphatase (BSAP) (U/L)

Bone biomarker levels (BSAP) at baseline will be compared to levels measured at Week 52. (NCT03199963)
Timeframe: Blinded Phase: Baseline; Week 52/EOS

InterventionBSAP in U/L (Mean)
BHR-700 (0.2% 4-OHT Gel)1.0
Matching Placebo Gel0.7

[back to top]

Change in Baseline of Cancer Cell Protein Levels of Human Epidermal Growth Factor Receptor (HER) Family Members (HER1-4) Following Neoadjuvant Endocrine Therapy.

"ImmunoHistoChemistry (IHC) will be used. The IHC test gives a score of 0 to 3+ that measures the amount of HER2 receptor protein on the surface of cells in a breast cancer tissue sample. If the score is 0 to 1+ (up to 25% of cells stained), it's called HER2 negative. If the score is 2+ (approximately 50% of cells stained), it's called borderline. A score of 3+ (approximately 75% or more of cells stained) is called HER2 positive. Upregulation means increased staining from a prior observation; Downregulation means decreased staining from a prior observation; and No Change means similar staining from a prior observation." (NCT03219476)
Timeframe: At four weeks.

,,,
InterventionParticipants (Count of Participants)
UpregulationDownregulationNo Change
Change From Baseline in Human Epidermal Growth Factor Receptor 1 (HER1) Cell Protein Levels.1036
Change From Baseline in Human Epidermal Growth Factor Receptor 2 (HER2) Cell Protein Levels.17218
Change From Baseline in Human Epidermal Growth Factor Receptor 3 (HER3) Cell Protein Levels.11818
Change From Baseline in Human Epidermal Growth Factor Receptor 4 (HER4) Cell Protein Levels.11818

[back to top]

Number of Subjects Who Achieve a Partial Radiographic Response.

"This will be assessed by World Health Organization (WHO) criteria:~Complete Response (CR): The disappearance of all known disease, based on a comparison between the measurements at baseline and after four weeks of treatment with neoadjuvant therapy.~Partial Response (PR): A 50% or greater decrease in the product of the bi-dimensional measurements of the lesion (total tumor size), based on a comparison between the measurements at baseline and after four weeks of treatment with neoadjuvant therapy.~No Change (NC): A 50% decrease in total tumor size cannot be established nor has a 25% increase in the size of the lesion been demonstrated.~Progressive Disease (PD): A 25% or greater increase in the total tumor size of the measurable lesions (calculated on the smallest diameter recorded over time)." (NCT03219476)
Timeframe: At four weeks.

InterventionParticipants (Count of Participants)
Neoadjuvant Endocrine Therapy Treatment (Physician's Choice)1

[back to top]

Number of Subjects Who Achieve Complete Radiographic Response.

"This will be assessed by World Health Organization (WHO) criteria:~Complete Response (CR): The disappearance of all known disease, based on a comparison between the measurements at baseline and after four weeks of treatment with neoadjuvant therapy.~Partial Response (PR): A 50% or greater decrease in the product of the bi-dimensional measurements of the lesion (total tumor size), based on a comparison between the measurements at baseline and after four weeks of treatment with neoadjuvant therapy.~No Change (NC): A 50% decrease in total tumor size cannot be established nor has a 25% increase in the size of the lesion been demonstrated.~Progressive Disease (PD): A 25% or greater increase in the total tumor size of the measurable lesions (calculated on the smallest diameter recorded over time)." (NCT03219476)
Timeframe: At four weeks.

InterventionParticipants (Count of Participants)
Neoadjuvant Endocrine Therapy Treatment (Physician's Choice)0

[back to top]

Number of Participants With Dermal Toxicity on Breast Skin at the Application Site

Number of participants with dermal toxicity on breast skin at the transdermal gel application site. Will be assessed by Common Terminology Criteria for Adverse Events version 4. (NCT03317405)
Timeframe: Up to 60 days

InterventionParticipants (Count of Participants)
Endoxifen Hydrochloride Gel 10 mg Daily4
Endoxifen Hydrochloride Gel 20 mg Daily2
Placebo0

[back to top]

Change in Plasma Estrogenic and Coagulation Parameters

Change in plasma Estrogenic and Coagulation Parameters from baseline to end of intervention (up to 28 days) including: IGF1, IGFBP3, SHBG. (NCT03317405)
Timeframe: baseline and up to 28 days

,,
Interventionng/ml (Mean)
IGF1IGFBP3SHBG
Endoxifen Hydrochloride Gel 10 mg Daily-1.748-9.4
Endoxifen Hydrochloride Gel 20 mg3.0-2.51.9
Placebo-1.0-60-4.4

[back to top]

Change in Pre-therapy and Post-therapy Symptoms Captured by BESS Questionnaire

Assessed using the Breast Cancer Prevention Trial (BCPT) Eight Symptom Scale (BESS) questionnaire. A patient reported outcome, subscale scores range from 0 (Not at All) to 4 (Extremely) when asked about experiencing symptoms. A positive change in scores indicates an increase in symptoms experienced and a negative change in scores indicates a decrease in symptoms experienced. (NCT03317405)
Timeframe: baseline and up to 60 days

,,
Interventionchange in score on a scale (Mean)
CognitiveBody PainVasomotorGastrointestinalSexual ProblemsBody ImageVaginalBladder Problem
Endoxifen Hydrochloride Gel 10 mg Daily-0.16-0.18-0.02-0.070.13-0.200.130.03
Endoxifen Hydrochloride Gel 20 mg Daily-0.05-0.38-0.05-0.24-0.57-0.64-0.29-0.86
Placebo-0.19-0.100.190.10-0.29-0.43-0.240.07

[back to top]

Drug Concentration in Plasma

Concentration of (E) and (Z) Isomers ENX in plasma at the end of intervention (up to 4 weeks) (NCT03317405)
Timeframe: baseline and up to 28 days

,,
Interventionng/ml (Median)
Z_ENXE_ENX
Endoxifen Hydrochloride Gel 10 mg0.150.00
Endoxifen Hydrochloride Gel 20 mg0.440.00
Placebo0.000.00

[back to top]

Drug Concentration in Tissue

Concentrations of (E) and (Z) Isomers ENX in right and left breast tissue at end of intervention (up to 4 weeks) in tissue samples (NCT03317405)
Timeframe: up to 28 days

,,
Interventionng/g (Median)
Central Subareolar Left Breast Z_ENXCentral Subareolar Left Breast E_ENXCentral Subareolar Right Breast Z_ENXCentral Subareolar Right Breast E_ENXCentral Deepest Left Breast Z_ENXCentral Deepest Left Breast E_ENXCentral Deepest Right Breast Z_ENXCentral Deepest Right Breast E_ENXLateral Surface Left Breast Z_ENXLateral Surface Left Breast E_ENXLateral Surface Right Breast Z_ENXLateral Surface Right Breast E_ENX
Endoxifen Hydrochloride Gel 10 mg Daily0.470.160.370.160.400.160.460.280.340.160.450.16
Endoxifen Hydrochloride Gel 20 mg Daily0.760.251.000.301.550.912.571.700.810.271.200.39
Placebo0.000.000.000.000.000.000.000.000.000.000.000.00

[back to top]

Number of Participants With HIV-1 RNA Levels (Measured by Single Copy Assay) Greater or Equal to the Lower Limit of Quantification

Number of participants with HIV-1 RNA levels measured by single copy assay (SCA) greater or equal to the lower limit of quantification (LOQ). The lower limit of quantification for this study was 0.47 copies/mL. (NCT03382834)
Timeframe: Pre-entry, entry, Day 28, Day 35, Day 38 (5 hours post vorinostat), Day 45, Day 65

,
InterventionParticipants (Count of Participants)
Pre-entry SCA >= LOQEntry SCA >=LOQDay 28 SCA >=LOQDay 35 SCA >=LOQDay 38 SCA >=LOQDay 45 SCA >=LOQDay 65 SCA >=LOQ
Arm A: Tamoxifen + Vorinostat10911117910
Arm B: Vorinostat Alone6345545

[back to top]

Change From Baseline in Total HIV-1 DNA Levels in CD4+ T Cells

Baseline is defined as the average of the pre-entry and entry values. Change was calculated as the value of Total HIV-1 DNA on Day 38 (5 hours post vorinostat) minus the value at baseline. (NCT03382834)
Timeframe: Pre-entry, entry, and Day 38

Interventionlog10 copies/million CD4 cells (Mean)
Arm A: Tamoxifen + Vorinostat0
Arm B: Vorinostat Alone-0.04

[back to top]

Change From Baseline in Cell-associated HIV-1 RNA in CD4+ T Cells

Baseline is defined as the average of the pre-entry and entry values. Change was calculated as the value of Cell-associated HIV-1 RNA on Day 38 (5 hours post vorinostat) minus the value at baseline. (NCT03382834)
Timeframe: Pre-entry, entry, and Day 38

Interventionlog10 copies/million CD4 cells (Mean)
Arm A: Tamoxifen + Vorinostat0.06
Arm B: Vorinostat Alone0.17

[back to top]

Proportion of Participants With New Grade 3 or Greater Adverse Events

Proportion of participants with new Grade 3 or greater adverse events that are considered definitely, probably, or possibly related to study treatment (as judged by the core protocol team). The DAIDS AE Grading Table (corrected Version 2.1, July 2017) was used. (NCT03382834)
Timeframe: Measured from study entry through Day 65

Interventionproportion of participants (Number)
Arm A: Tamoxifen + Vorinostat0
Arm B: Vorinostat Alone0

[back to top]

Percentage of Participants With Objective Response

Objective response is defined as percentage of participants having a partial response (PR) or complete response (CR) according to the RECIST version 1.1 assessed by ICR. As per RECIST 1.1, CR was defined as disappearance of all target and non-target lesions and normalization of tumor marker level. Any pathological lymph nodes (whether target or non-target) must have reduction in short axis to less than (<) 10 millimeters (mm). PR was defined as at least a 30% decrease in the sum of diameters of target lesions, taking as reference the baseline sum diameters. (NCT04059484)
Timeframe: From randomization to the date of first documented tumor progression, death due to any cause or data cut-off date whichever comes first (maximum duration: 116 weeks)

Interventionpercentage of participants (Number)
Physician Choice Endocrine Monotherapy (PCEM)8.8
Amcenestrant11.9

[back to top]

Percentage of Participants With Disease Control

Disease control is defined as percentage of participants having a confirmed CR, PR, or stable disease (SD) or Non-CR/Non-PD as BOR determined by ICR as per RECIST 1.1 from the date of randomization to the date of end of treatment. As per RECIST 1.1, CR: disappearance of all target and non-target lesions and normalization of tumor marker level. Any pathological lymph nodes (whether target or non-target) must have reduction in short axis to <10 mm. PR: at least a 30% decrease in sum of diameters of target lesions, taking as reference baseline sum diameters. SD: neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for progressive disease (PD), taking as reference the smallest sum diameters. Non-CR/Non-PD: persistence of one or more nontarget lesion(s) and/or maintenance of tumor marker level above the normal limits. PD: at least 20% increase in sum of diameters of target lesions, unequivocal progression of existing non-target lesions. (NCT04059484)
Timeframe: From randomization to the date of first documented tumor progression, death due to any cause or data cut-off date whichever comes first (maximum duration: 116 weeks)

Interventionpercentage of participants (Number)
Physician Choice Endocrine Monotherapy (PCEM)53.7
Amcenestrant54.5

[back to top]

Change From Baseline in European Organization for Research and Treatment of Cancer Quality of Life Breast Cancer Specific Module (EORTC-QLQ-BR23) Domain Scores

QLQ-BR23: disease-specific Health-related QOL assesses impact of breast cancer & side effects of treatment. EORTC-QLQ-BR23 contains 23 items: multi-item scales & single-item measures. 4 functional scales (body image, sexual functioning, sexual enjoyment, future perspective) & 4 scales related to symptoms of disease or treatment (arm symptoms, breast symptoms, systemic therapy side effects, & upset by hair loss). All items scored 1 (not at all) to 4 (very much). Scores of all scales transformed from raw scores to linear scales ranging 0 to 100. Higher score for functional scales = better outcome; higher score for symptoms scales = higher symptom burden. LS mean and SE are derived from MMRM model with change from Baseline values as response variable, treatment, time, treatment-by-time interaction, Baseline value and stratifications factors as fixed effect. Average of LS mean change from baseline values of overall treatment (i.e., each cycle [Cycle 1 up to Cycle 30]) was reported. (NCT04059484)
Timeframe: Baseline, overall treatment duration (Cycle 1 up to Cycle 30 [i.e.,116 weeks])

,
Interventionscore on a scale (Least Squares Mean)
Body imageSexual functioningSexual enjoymentFuture perspectiveSystemic therapy side effectsBreast symptomsArm symptomsUpset by hair loss
Amcenestrant2.2-2.60.412.00.7-0.82.0-10.6
Physician Choice Endocrine Monotherapy (PCEM)1.8-2.4-1.110.60.2-0.41.8-9.7

[back to top]

Pharmacokinetics: Plasma Concentrations of Amcenestrant

Amcenestrant plasma concentrations at specified time points are reported. (NCT04059484)
Timeframe: Cycle 1 Day 1: 1.5 hours(h), 4h post-dose, Day 15: pre-dose, Cycle 2 Day 1: pre-dose, 1.5h, 4h, 8h post-dose, Cycle 3 Day 1: pre-dose, Cycle 4 Day 1: pre-dose, Cycle 6 Day 1: pre-dose

Interventionnanograms per milliliter (ng/mL) (Mean)
Cycle 1 Day 1: 1.5hCycle 1 Day 1: 4hCycle 1 Day 15: Pre-doseCycle 2 Day 1: Pre-doseCycle 2 Day 1: 1.5hCycle 2 Day 1: 4hCycle 2 Day 1: 8hCycle 3 Day 1: Pre-doseCycle 4 Day 1: Pre-doseCycle 6 Day 1: Pre-dose
Amcenestrant3185.74753.1516.4479.12719.63801.82303.8593.6661.5531.5

[back to top]

Change From Baseline in European Organization for Research and Treatment of Cancer Core Quality of Life Questionnaire (EORTC-QLQ-C30) Domain Scores

EORTC-QLQ-C30: cancer-specific instrument with 30 questions for evaluation of new chemotherapy & assessment of participant reported outcome. These include 5 functional scales, 9 symptom scales, & Global Health Status/quality of life scale (GHS/QoL). All 14 items/domains were scored on scale of 1 (not at all) to 4 (very much) and GHS/QoL, scored on scale of 1 (very poor) to 7 (excellent). All scales are transformed from raw scores to linear scales ranging 0 to 100. Higher score for functional & GHS/QoL = higher level of functioning, & higher score for symptoms scales = higher symptom burden. Least Square (LS) mean and Standard Error (SE) are derived from MMRM model with change from Baseline values as response variable, treatment, time, treatment-by-time interaction, Baseline value and stratifications factors as fixed effect. Average of LS mean change from baseline values of overall treatment (i.e., each cycle [Cycle 1 up to Cycle 30]) was reported in this outcome measure. (NCT04059484)
Timeframe: Baseline, overall treatment duration (Cycle 1 up to Cycle 30 [i.e.,116 weeks])

,
Interventionscore on a scale (Least Squares Mean)
GHS/QoLPhysical functioningRole functioningEmotional functioningCognitive functioningSocial functioningFatigueNausea and vomitingPainDyspnoeaInsomniaAppetite lossConstipationDiarrhoeaFinancial difficulties
Amcenestrant2.5-3.1-3.03.0-0.8-0.82.81.32.10.8-2.31.23.03.9-2.0
Physician Choice Endocrine Monotherapy (PCEM)1.8-1.2-2.4-2.2-0.9-2.51.11.71.11.0-1.12.4-2.30.31.7

[back to top]

Within-Participant Steady State Ctrough of Amcenestrant

Within-participant Steady state Ctrough was defined as the median value of the Ctrough across study using plasma concentration of predose samples at Cycle 1 Day 15 and Day 1 of Cycle 2, 3, 4 and 6 for each individual participant. Average (mean) of all calculated Ctrough values for all participants across study (Cycle 1 Day 15 and Day 1 of Cycle 2, 3, 4 and 6 ) was derived and reported in this outcome measure. (NCT04059484)
Timeframe: Predose on Cycle 1 Day 15; Cycle 2 Day 1; Cycle 3 Day 1; Cycle 4 Day 1; Cycle 6 Day 1

Interventionng/mL (Mean)
Amcenestrant491.35

[back to top]

Progression Free Survival (PFS)

PFS is defined as the time in months interval from the date of randomization to the date of first documented tumor progression as per Response Evaluation Criteria in Solid Tumors (RECIST 1.1) assessed by independent central review (ICR) or death (due to any cause), whichever comes first. Progressive Disease (PD) as per RECIST 1.1: at least a 20 percent (%) increase in sum of diameters of target lesions, unequivocal progression of existing non-target lesions. Analysis was performed by Kaplan-Meier method. (NCT04059484)
Timeframe: From randomization to the date of first documented tumor progression or death due to any cause or data cut-off date whichever comes first (maximum duration: 116 weeks)

Interventionmonths (Median)
Physician Choice Endocrine Monotherapy (PCEM)3.7
Amcenestrant3.6

[back to top]

Percentage of Participants With Clinical Benefit

Clinical Benefit is defined as percentage of participants having a confirmed CR, PR, SD, or Non-CR/Non-PD for at least 24 weeks determined by ICR as per RECIST 1.1 from the date of randomization to the date of end of treatment. As per RECIST 1.1, CR: disappearance of all target and non-target lesions and normalization of tumor marker level. Any pathological lymph nodes (whether target or non-target) must have reduction in short axis to <10 mm. PR: at least a 30% decrease in the sum of diameters of target lesions, taking as reference the baseline sum diameters. SD: neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for PD, taking as reference the smallest sum diameters. Non-CR/Non-PD: persistence of one or more nontarget lesion(s) and/or maintenance of tumor marker level above the normal limits. PD: at least 20% increase in sum of diameters of target lesions, unequivocal progression of existing non-target lesions. (NCT04059484)
Timeframe: From randomization to the date of first documented tumor progression, death due to any cause or data cut-off date whichever comes first (maximum duration: 116 weeks)

Interventionpercentage of participants (Number)
Physician Choice Endocrine Monotherapy (PCEM)29.3
Amcenestrant27.3

[back to top]

Overall Survival (OS)

OS is defined as the time interval from the date of randomization to the date of documented death (due to any cause). In the absence of observation of death, survival time was censored to last date the participant is known to be alive or at the cut-off date, whichever comes first. Analysis was performed by Kaplan-Meier method. (NCT04059484)
Timeframe: From randomization to the death due to any cause or data cut-off date whichever comes first (maximum duration: 116 weeks)

Interventionmonths (Median)
Physician Choice Endocrine Monotherapy (PCEM)NA
AmcenestrantNA

[back to top]

Duration of Response (DOR)

DOR is defined as time (in months) from first documented evidence of CR or PR until progressive disease (PD) determined by ICR as per RECIST 1.1 or death from any cause, whichever occurs first. For participants with ongoing response at the time of the analysis, DOR was censored at the date of the last valid disease assessment not showing documented progression performed before the initiation of a new anticancer treatment (if any). As per RECIST 1.1, CR: disappearance of all target and non-target lesions and normalization of tumor marker level. Any pathological lymph nodes (whether target or non-target) must have reduction in short axis to <10 mm. PR: at least a 30% decrease in the sum of diameters of target lesions, taking as reference the baseline sum diameters. PD: at least 20% increase in sum of diameters of target lesions, unequivocal progression of existing non-target lesions. (NCT04059484)
Timeframe: From the date of first response to the date of first documented tumor progression, death due to any cause or data cut-off date whichever comes first (maximum duration: 116 weeks)

Interventionmonths (Median)
Physician Choice Endocrine Monotherapy (PCEM)NA
Amcenestrant15.1

[back to top]

Progression Free Survival (PFS) According to Estrogen Receptor 1 Gene (ESR1) Mutation Status

PFS defined as the time (in months) interval from the date of randomization to the date of first documented tumor progression as per RECIST 1.1 assessed by ICR or death (due to any cause), whichever comes first. Progression as per RECIST 1.1: at least a 20 percent (%) increase in sum of diameters of target lesions, unequivocal progression of existing non-target lesions. The mutation status (wild type, mutant) of twelve specific mutations of the ESR1 gene was determined by multiplex droplet digital polymerase chain reaction (ddPCR), including their mutant frequency and concentration. Here, PFS is reported based on the ESR1 mutation status of participants: wild type and mutants. ESR1 was the gene encoding estrogen receptor alpha. ESR1 mutant type breast cancer was a disease where the ESR1 gene had a mutation (i.e., a type of error). ESR1 wild type breast cancer was a disease where the ESR1 gene was normal without a mutation. Analysis was performed by Kaplan-Meier method. (NCT04059484)
Timeframe: From randomization to the date of first documented tumor progression, death due to any cause or data cut-off date whichever comes first (maximum duration: 116 weeks)

,
Interventionmonths (Median)
MutatedWild type
Amcenestrant3.73.5
Physician Choice Endocrine Monotherapy (PCEM)2.03.9

[back to top]

Change From Baseline in European Quality of Life Working Group Health Status Measure 5 Dimensions (5D), 5 Levels (5L) (EQ-5D-5L) Score: Health Utility Index Value

EQ-5D-5L: consists of 2 sections: EQ-5D-5L health state utility index (descriptive system) & VAS. The EQ-5D descriptive system consists of 5 dimensions: mobility, self-care, usual activities, pain/discomfort & anxiety/depression. Each dimension has 5 levels: no problems, slight problems, moderate problems, severe problems, & extreme problems. Response options are measured with 5-point Likert scale (for 5L version). The EQ-5D-5L responses are converted into single index utility score between 0 to 1, where higher score indicates better health state & lower score indicate worse health state. LS mean and SE are derived from MMRM model with change from Baseline values as response variable, treatment, time, treatment-by-time interaction, Baseline value and stratifications factors as fixed effect. Average of LS mean change from baseline values overall treatment (i.e., each cycle [Cycle 1 up to Cycle 30]) was reported in this outcome measure. (NCT04059484)
Timeframe: Baseline, overall treatment duration (Cycle 1 up to Cycle 30 [i.e.,116 weeks])

Interventionscore on a scale (Least Squares Mean)
Physician Choice Endocrine Monotherapy (PCEM)-0.0
Amcenestrant-0.0

[back to top]

Change From Baseline in European Quality of Life Working Group Health Status Measure 5 Dimensions (5D), 5 Levels (5L) (EQ-5D-5L) Score: Visual Analog Scale (VAS) Score

EQ-5D-5L is a standardized measure of health status, provides a simple, generic measure of health for clinical and economic appraisal, and consists of 2 sections: the EQ-5D-5L health state utility index (descriptive system) and the EQ-5D-5L VAS. The Visual Analogue Scale is designed to rate the participant's current health state on a scale from 0 to 100, where 0 represents the worst imaginable health state and 100 represents the best imaginable health state. LS mean and SE are derived from MMRM model with change from baseline values as response variable, treatment, time, treatment-by-time interaction, Baseline value and stratifications factors as fixed effect. Average of LS mean change from Baseline values of overall treatment (i.e., each cycle [Cycle 1 up to Cycle 30]) was reported in this outcome measure. (NCT04059484)
Timeframe: Baseline, overall treatment duration (Cycle 1 up to Cycle 30 [i.e.,116 weeks])

Interventionscore on a scale (Least Squares Mean)
Physician Choice Endocrine Monotherapy (PCEM)0.9
Amcenestrant0.2

[back to top]

Percentage of Participants With Tumor Responses

Tumor responses will be classified using the Immune Related Response-Criteria (irRC)) through study completion. (NCT04190056)
Timeframe: Up to 24 months

Interventionpercentage of participants (Number)
Arm B (Pembrolizumab, Tamoxifen)0

[back to top]

Overall Response Rate (ORR)

ORR is defined as the proportion of participants randomized to that arm whose status is stable disease (SD) or better (complete response (CR), partial response (PR)). Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions: CR=Disappearance of all target lesions; PR = >=30% decrease in the sum of the longest diameter of target lesions, and SD=Neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for progressive disease,. (NCT04190056)
Timeframe: Up to 24 weeks

Interventionproportion of participants (Number)
Arm B (Pembrolizumab, Tamoxifen)0

[back to top]

Median Progression Free Survival (PFS)

Progression-free survival (PFS) is defined as the duration of time from start of treatment to time of progression or death from any cause on study, whichever occurs first. Will use median PFS (computed by the Kaplan-Meier estimator) to summarize. The respective confidence intervals will be computed as well. (NCT04190056)
Timeframe: Up to 27 months

Interventionmonths (Median)
Arm B (Pembrolizumab, Tamoxifen)NA

[back to top]

Median Overall Survival (OS)

Will use median OS (computed by the Kaplan-Meier estimator) to summarize from initiation of study treatment to the time of death from any cause on study. The respective confidence intervals will be computed as well. (NCT04190056)
Timeframe: Up to 27 months

Interventionmonths (Median)
Arm B (Pembrolizumab, Tamoxifen)NA

[back to top]

Duration of Response (DOR)

The duration of overall response is measured from the time measurement criteria are met for CR or PR (whichever is first recorded) until the first date that recurrent or progressive disease is objectively documented (taking as reference for progressive disease the smallest measurements recorded since the treatment started). The duration of overall CR is measured from the time measurement criteria are first met for CR until the first date that recurrent disease is objectively documented. Duration of stable disease is measured from the start of the treatment until the criteria for progression are met, taking as reference the smallest measurements recorded since the treatment started. Will use median DOR (computed by the Kaplan-Meier estimator) to summarize. The respective confidence intervals will be computed as well. (NCT04190056)
Timeframe: Up to 24 weeks

Interventionweeks (Median)
Arm B (Pembrolizumab, Tamoxifen)NA

[back to top]

Progression-free Survival (PFS)

"Progression free survival (PFS) means the participant remains alive without return or relapse of the tumor. The outcome is defined as the number of days to either progressive disease as defined per RECIST v1.1 or death. RECIST criteria are:~CR = Disappearance of all target lesions~PR = ≥ 30% decrease in the sum of the longest diameter of target lesions~Overall Response (OR) = CR + PR~Progressive disease (PD) = 20% increase in the sum of the longest diameter of target lesions, and/or the appearance of one or more new lesion(s)~Stable disease (SD) = Small changes that do not meet any of the above criteria" (NCT04504331)
Timeframe: up to 9 months

Interventiondays (Median)
Cohort 1: Infigratinib (100mg) + Tamoxifen61
Cohort 2: Infigratinib (125mg) + TamoxifenNA

[back to top]

Number of Treatment Emergent Adverse Events (TEAE)

Treatment emergent adverse events (TEAEs) are defined as adverse events of any grade with initial onset or increasing in severity after the first dose of study treatment until 30 days after last dose of study drug. Pregnancy during the reporting period will be classified as a serious adverse event. (NCT04504331)
Timeframe: From first dose to 30 days after the last dose of study drug (up to 94 days)

Interventionadverse events (Number)
Cohort 1: Infigratinib (100mg) + Tamoxifen49
Cohort 2: Infigratinib (125mg) + Tamoxifen26

[back to top]

Number of Dose-limiting Toxicities (DLTs)

The primary outcome for this study is dose-limiting toxicities (DLTs) during the first 2 cycles of therapy. All grades per the Common Terminology Criteria for Adverse Events (CTCAE). DLT is defined as a related and clinically significant adverse event (AE), including missed doses due to a related AE. (NCT04504331)
Timeframe: 8 weeks

InterventionDLTs (Number)
Cohort 1: Infigratinib (100mg) + Tamoxifen0
Cohort 2: Infigratinib (125mg) + Tamoxifen0

[back to top]

Clinical Benefit Rate

"Clinical benefit (CB) is defined as achieving a Response Evaluation Criteria in Solid Tumors (RECIST) v1.1 Complete Response (CR) ; Partial Response (PR); or Stable Disease (SD). The outcome will be reported as the number of subjects that achieve CR, PR, or SD. RECIST criteria are:~CR = Disappearance of all target lesions~PR = ≥ 30% decrease in the sum of the longest diameter of target lesions~SD = Small changes that do not meet any of the above criteria~Progressive disease (PD) = 20% increase in the sum of the longest diameter of target lesions, and/or the appearance of one or more new lesion(s)" (NCT04504331)
Timeframe: 6 months

InterventionParticipants (Count of Participants)
CRPRSDCB (CR + PR +SD)PD
Cohort 1: Infigratinib (100mg) + Tamoxifen00003

[back to top]

Overall Survival (OS)

Overall survival was defined as the time interval from the date of randomization to the date of documented death (due to any cause). (NCT05128773)
Timeframe: From randomization to the date of death due to any cause (maximum exposure duration: 155 days)

Interventionmonths (Median)
Amcenestrant 200 mg + Tamoxifen-Matching PlaceboNA

[back to top]

Breast Cancer-specific Survival (BCSS)

BCSS was defined as the time interval from the date of randomization to the date of documented death attributable to breast cancer cause. (NCT05128773)
Timeframe: From randomization to the date of death due to breast cancer (maximum exposure duration: 155 days)

Interventionmonths (Median)
Amcenestrant 200 mg + Tamoxifen-Matching PlaceboNA

[back to top]