lasofoxifene profile

Lasofoxifene: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

lasofoxifene : A member of the class of tetralins that is 5,6,7,8-tetrahydronaphthalen-2-ol in which the hydrogens at positions 5 and 6 are replaced by 4-[2-(pyrrolidin-1-yl)ethoxy]phenyl and phenyl groups, respectively (the 5R,6S-stereoisomer). It is a selective estrogen receptor modulator indicated for the prevention and treatment of osteoporosis in post-menopausal women. [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]

ID Source	ID
PubMed CID	216416
CHEMBL ID	328190
CHEBI ID	135938
SCHEMBL ID	26815
MeSH ID	M0377970

Synonym
oporia
(5r,6s)-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol
C3D ,
cp 336156
(-)-cis-5,6,7,8-tetrahydro-6-phenyl-5-(p-(2-(1-pyrrolidinyl)ethoxy)phenyl)-2-naphthol
cp-336,156
(5r,6s)-6-phenyl-5-{4-[2-(pyrrolidin-1-yl)ethoxy]phenyl}-5,6,7,8-tetrahydronaphthalen-2-ol
chembl328190 ,
bdbm20606
lasofoxifene
CHEBI:135938
lasofoxifenum
(-)-cis-(5r,6s)-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol
lasofoxifeno
180916-16-9
rac-lasofoxifene
(5r,6s)-5,6,7,8-tetrahydro-6-phenyl-5-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-2-naphthalenol
180915-78-0
(-)-cis-5,6,7,8-tetrahydro-6-phenyl-5-(p-(2-(1-pyrrolidinyl)ethoxy)phenyl)-2-naphthol.
lasofoxifene [inn:ban]
2-naphthalenol, 5,6,7,8-tetrahydro-6-phenyl-5-(4-(2-(1-pyrrolidinyl)ethoxy)phenyl)-, (5r,6s)-
2-naphthalenol, 5,6,7,8-tetrahydro-6-phenyl-5-(4-(2-(1-pyrrolidinyl)ethoxy)phenyl)-, (5r-cis)-
unii-337g83n988
337g83n988 ,
BCP9000842
BCP0726000177
SCHEMBL26815
gtpl7542
lasofoxifene [mi]
lasofoxifene [inn]
lasofoxifene [mart.]
lasofoxifene [who-dd]
lasofoxifene [ema epar]
GXESHMAMLJKROZ-IAPPQJPRSA-N
cis-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol
cis-6-phenvl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol
cis-6phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol
cis-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol
DTXSID50171037
AKOS030241621
J-011550
DB06202
BCP03626
(5r,6s)-6-phenyl-5-(4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)-5,6,7,8-tetrahydronaphthalen-2-ol.
Q644675
NCGC00487269-02
2-naphthalenol, 5,6,7,8-tetrahydro-6-phenyl-5-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-, (5r,6s)-
rel-(5r,6s)-6-phenyl-5-(4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)-5,6,7,8-tetrahydronaphthalen-2-ol
(5r,6s)-6-phenyl-5-(4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)-5,6,7,8-tetrahydronaphthalen-2-ol ,
EN300-18161169
HY-A0037
CS-0006740

Research Excerpts

Overview

Lasofoxifene (CP 336,156) is a naphthalene-derivative, third-generation SERM, struct. Lasofox ifene is a nonsteroidal selective estrogen receptor modulator (SERM) developed for the treatment of postmenopausal osteoporosis.

Excerpt	Reference	Relevance
"Lasofoxifene is a selective estrogen receptor modulator with benefits on bone health and breast cancer prevention potential."	( Lasofoxifene as a potential treatment for therapy-resistant ER-positive metastatic breast cancer. Chang, YF; Fanning, SW; Green, B; Greene, GL; Greene, ME; Komm, B; Kurleto, JD; Lainé, M; Phung, L, 2021)	2.79
"Lasofoxifene is a novel selective estrogen receptor modulator that is being developed for the treatment of postmenopausal osteoporosis. "	( A randomised, double-blinded, placebo-controlled, trial to determine the individual response in bone turnover markers to lasofoxifene therapy. Eastell, R; Glover, SJ; Rogers, A, 2009)	2
"Lasofoxifene is a third-generation SERM with markedly higher in vitro and in vivo potency and oral bioavailability than other SERMs. "	( Lasofoxifene: selective estrogen receptor modulator for the prevention and treatment of postmenopausal osteoporosis. Gennari, L; Naunton, M; Peterson, GM; Tichelaar, LK, 2011)	3.25
"Lasofoxifene is a nonsteroidal selective estrogen receptor modulator (SERM) with greater than 100-fold selectivity against all other steroid receptors and is a potentially superior treatment for postmenopausal osteoporosis. "	( Reproductive toxicity assessment of lasofoxifene, a selective estrogen receptor modulator (SERM), in male rats. Cappon, GD; Horimoto, M; Hurtt, ME, 2004)	2.04
"Lasofoxifene is a nonsteroidal selective estrogen receptor modulator (SERM). "	( Reproductive toxicity assessment of lasofoxifene, a selective estrogen receptor modulator (SERM), in female rats. Cappon, GD; Gupta, U; Hurtt, ME; Tassinari, MS; Terry, KK, 2004)	2.04
"Lasofoxifene is a nonsteroidal selective estrogen receptor modulator (SERM) developed for the treatment of postmenopausal osteoporosis. "	( Pre- and postnatal development studies of lasofoxifene, a selective estrogen receptor modulator (SERM), in Sprague-Dawley rats. Hagler, AR; Tassinari, MS; Weisenburger, WP, 2004)	2.03
"Lasofoxifene [CP 336156] is a potent, nonsteroidal, tissue-selective estrogen receptor modulator (SERM). "	( Lasofoxifene: CP 336156, CP-336156. , 2005)	3.21
"Lasofoxifene (CP 336,156) is a naphthalene-derivative, third-generation SERM, structurally distinct from the first- and second-generation SERMs."	( Lasofoxifene: a new type of selective estrogen receptor modulator for the treatment of osteoporosis. Gennari, L, 2006)	2.5
"Lasofoxifene is a new and potent selective estrogen receptor modulator (SERM). "	( The 2.0 A crystal structure of the ERalpha ligand-binding domain complexed with lasofoxifene. Ammirati, MJ; Danley, DE; Geoghegan, KF; Hoth, LR; LeMotte, PK; Pandit, J; Simons, SP; Vajdos, FF, 2007)	2.01

Effects

Lasofoxifene has demonstrated significant reductions in vertebral and non-vertebral fracture risk, but has been associated with endometrial/uterine effects. The drug should not affect drugs metabolized by other cytochrome P450 isoenzymes.

Excerpt	Reference	Relevance
"Lasofoxifene also has a remarkably improved oral bioavailability with respect to other SERMs such as raloxifene and tamoxifen, owing to increased resistance to intestinal wall glucuronidation."	( Lasofoxifene, a new selective estrogen receptor modulator for the treatment of osteoporosis and vaginal atrophy. Gennari, L, 2009)	2.52
"Lasofoxifene also has a remarkably improved oral bioavailability with respect to other SERMs such as raloxifene and tamoxifen, owing to increased resistance to intestinal wall glucuronidation."	( Lasofoxifene, a new selective estrogen receptor modulator for the treatment of osteoporosis and vaginal atrophy. Gennari, L, 2009)	2.52
"Lasofoxifene has only been studied in postmenopausal osteoporotic women in the PEARL trial."	( Clinical issues regarding cardiovascular disease and selective estrogen receptor modulators in postmenopausal women. de Villiers, TJ, 2009)	1.07
"Lasofoxifene has demonstrated significant reductions in vertebral and non-vertebral fracture risk, but has been associated with endometrial/uterine effects."	( An update on selective estrogen receptor modulators for the prevention and treatment of osteoporosis. Chines, AA; Komm, BS, 2012)	1.1
"Lasofoxifene has no effect on CYP2E1- or CYP2D6-mediated drug metabolism and should not affect drugs metabolized by other cytochrome P450 isoenzymes."	( Effects of steady-state lasofoxifene on CYP2D6- and CYP2E1-mediated metabolism. Fisher, JM; Gardner, MJ; Kolluri, S; Moller, RA; Obach, RS; Taylor, AE; Walsky, RL, 2006)	2.08
"Lasofoxifene has no clinically meaningful effect on the pharmacokinetics of warfarin. "	( Effects of lasofoxifene on the pharmacokinetics and pharmacodynamics of single-dose warfarin. Bramson, C; Carvajal-Gonzalez, S; Gardner, MJ; Ouellet, D; Randinitis, E; Remmers, A; Roman, D, 2006)	2.17

Actions

Lasofoxifene did not increase uterine weight or endometrial thickness. Did not change mammary, vaginal, or cervical histologic condition. Had no effect on breast, vagina, or cervix.

Excerpt	Reference	Relevance
"Lasofoxifene did not increase uterine weight or endometrial thickness and did not change mammary, vaginal, or cervical histologic condition. "	( Effects of lasofoxifene on the uterus, vagina, and breast in ovariectomized cynomolgus monkeys (Macaca fascicularis). Botts, S; Brommage, R; Cline, JM; Lees, CJ, 2008)	2.18
"Lasofoxifene did not increase uterine weight and produced minor histologic uterine changes at the doses that were given and had no effect on the breast, vagina, or cervix."	( Effects of lasofoxifene on the uterus, vagina, and breast in ovariectomized cynomolgus monkeys (Macaca fascicularis). Botts, S; Brommage, R; Cline, JM; Lees, CJ, 2008)	2.18

Treatment

Lasofoxifene treatment resulted in a small increase in endometrial thickness. Animals did not differ from ovariectomized controls in mechanical strength testing of the third lumbar vertebra or right femur.

Excerpt	Reference	Relevance
"Lasofoxifene treatment resulted in a small increase in endometrial thickness versus placebo (least-squares mean change from baseline 1.19 mm [P = 0.001], 1.43 mm [P < 0.001], and -0.72 mm for 0.25 mg/day lasofoxifene, 0.5 mg/day lasofoxifene, and placebo)."	( Postmenopausal Evaluation and Risk Reduction With Lasofoxifene (PEARL) trial: 5-year gynecological outcomes. Colgan, T; Cummings, S; Goldstein, SR; Johnson, M; Krpan, D; Neven, P; Proulx, J; Runowicz, CD; Sriram, U; Thompson, D; Thompson, J, 2011)	1.34
"Lasofoxifene-treated animals did not differ from ovariectomized controls in mechanical strength testing of either the third lumbar vertebra or right femur."	( Effects of lasofoxifene on bone in surgically postmenopausal cynomolgus monkeys. Brommage, R; Lees, C; Shen, V, )	1.24

Toxicity

Excerpt	Reference	Relevance
" During the mating phase, no adverse effects occurred in pregnancy success or reproductive parameters."	( Reproductive toxicity assessment of lasofoxifene, a selective estrogen receptor modulator (SERM), in female rats. Cappon, GD; Gupta, U; Hurtt, ME; Tassinari, MS; Terry, KK, 2004)	0.6
" 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

Pharmacokinetics

Excerpt	Reference	Relevance
"6-165) and 138% (112-169), respectively; mean terminal half-life was 252 hr compared to 193 hr in healthy subjects."	( A single-dose pharmacokinetic study of lasofoxifene in healthy volunteers and subjects with mild and moderate hepatic impairment. Bramson, C; Gardner, MJ; Ouellet, D; Randinitis, E; Roman, D, 2006)	0.6
" The mean PT AUC and Cmax ratio (90% confidence interval) was 91."	( Effects of lasofoxifene on the pharmacokinetics and pharmacodynamics of single-dose warfarin. Bramson, C; Carvajal-Gonzalez, S; Gardner, MJ; Ouellet, D; Randinitis, E; Remmers, A; Roman, D, 2006)	0.72

Bioavailability

Lasofoxifene is a third-generation SERM with markedly higher in vitro and in vivo potency and oral bioavailability than other SERMs. Due to increased resistance to intestinal wall glucuronidation, lasofox ifene has a remarkably improved oral bio availability with respect to other SER Ms.

Excerpt	Reference	Relevance
" 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
" Moreover, due to increased resistance to intestinal wall glucuronidation, lasofoxifene has a remarkably improved oral bioavailability with respect to other SERMs."	( Lasofoxifene: a new type of selective estrogen receptor modulator for the treatment of osteoporosis. Gennari, L, 2006)	2.01
" Lasofoxifene also has a remarkably improved oral bioavailability with respect to other SERMs such as raloxifene and tamoxifen, owing to increased resistance to intestinal wall glucuronidation."	( Lasofoxifene, a new selective estrogen receptor modulator for the treatment of osteoporosis and vaginal atrophy. Gennari, L, 2009)	2.71
"Lasofoxifene is a third-generation SERM with markedly higher in vitro and in vivo potency and oral bioavailability than other SERMs."	( Lasofoxifene: selective estrogen receptor modulator for the prevention and treatment of postmenopausal osteoporosis. Gennari, L; Naunton, M; Peterson, GM; Tichelaar, LK, 2011)	3.25

Dosage Studied

Excerpt	Relevance	Reference
" Male rats were euthanized after 66-70 days of dosing and epididymal sperm motility and concentration were assayed."	( Reproductive toxicity assessment of lasofoxifene, a selective estrogen receptor modulator (SERM), in male rats. Cappon, GD; Horimoto, M; Hurtt, ME, 2004)	0.6
" On GD 18 (rat) and GD 19 (rabbit) drug concentrations were measured in maternal plasma and in fetal tissue 2 hr post dosing to determine the fetal to maternal drug ratio."	( Embryo/fetal toxicity assessment of lasofoxifene, a selective estrogen receptor modulator (SERM), in rats and rabbits. Gupta, U; Ozolins, TR, 2004)	0.6
"01-10 mg/kg on parturition and lactation in pregnant rats and on the early postnatal development of the offspring, and to optimize the dosing regimen."	( Pre- and postnatal development studies of lasofoxifene, a selective estrogen receptor modulator (SERM), in Sprague-Dawley rats. Hagler, AR; Tassinari, MS; Weisenburger, WP, 2004)	0.59
" No dosage adjustment should be required when lasofoxifene is coadministered with ketoconazole, fluconazole, paroxetine or other agents that inhibit these CYP enzymes."	( Effects of three cytochrome P450 inhibitors, ketoconazole, fluconazole, and paroxetine, on the pharmacokinetics of lasofoxifene. Bramson, C; Gardner, M; Milton, A; Ouellet, D; Randinitis, E; Remmers, AE; Roman, D, 2007)	0.81
" 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

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

Role	Description
antineoplastic agent	A substance that inhibits or prevents the proliferation of neoplasms.
cardioprotective agent	Any protective agent that is able to prevent damage to the heart.
estrogen receptor agonist	An agonist at the estrogen receptor.
estrogen receptor antagonist	An antagonist at the estrogen receptor.
bone density conservation agent	An agent that inhibits bone resorption and/or favor bone mineralization and bone regeneration. Used to heal bone fractures and to treat bone diseases such as osteopenia and osteoporosis.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
naphthols	Any hydroxynaphthalene derivative that has a single hydroxy substituent.
N-alkylpyrrolidine
tetralins	Compounds containing a tetralin skeleton.
aromatic ether	Any ether in which the oxygen is attached to at least one aryl substituent.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Estrogen receptor	Homo sapiens (human)	IC50 (µMol)	0.0046	0.0000	0.7237	32.7000	AID1797989; AID1797992; AID240848; AID242068; AID242722; AID247489; AID248083; AID256998
Estrogen receptor	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0112	0.0007	4.1521	14.1600	AID69383
Estrogen receptor beta	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0112	0.0012	4.7652	14.1600	AID69383
Estrogen receptor beta	Homo sapiens (human)	IC50 (µMol)	0.0077	0.0001	0.5294	32.7000	AID1797989; AID1797992; AID240821; AID242043; AID242704; AID247489; AID248083; AID256999
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
positive regulation of transcription by RNA polymerase II	Estrogen receptor	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Estrogen receptor	Homo sapiens (human)
antral ovarian follicle growth	Estrogen receptor	Homo sapiens (human)
epithelial cell development	Estrogen receptor	Homo sapiens (human)
chromatin remodeling	Estrogen receptor	Homo sapiens (human)
regulation of DNA-templated transcription	Estrogen receptor	Homo sapiens (human)
signal transduction	Estrogen receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Estrogen receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Estrogen receptor	Homo sapiens (human)
androgen metabolic process	Estrogen receptor	Homo sapiens (human)
male gonad development	Estrogen receptor	Homo sapiens (human)
negative regulation of gene expression	Estrogen receptor	Homo sapiens (human)
positive regulation of phospholipase C activity	Estrogen receptor	Homo sapiens (human)
intracellular steroid hormone receptor signaling pathway	Estrogen receptor	Homo sapiens (human)
intracellular estrogen receptor signaling pathway	Estrogen receptor	Homo sapiens (human)
response to estradiol	Estrogen receptor	Homo sapiens (human)
regulation of toll-like receptor signaling pathway	Estrogen receptor	Homo sapiens (human)
negative regulation of smooth muscle cell apoptotic process	Estrogen receptor	Homo sapiens (human)
negative regulation of canonical NF-kappaB signal transduction	Estrogen receptor	Homo sapiens (human)
negative regulation of DNA-binding transcription factor activity	Estrogen receptor	Homo sapiens (human)
response to estrogen	Estrogen receptor	Homo sapiens (human)
positive regulation of DNA-templated transcription	Estrogen receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Estrogen receptor	Homo sapiens (human)
fibroblast proliferation	Estrogen receptor	Homo sapiens (human)
positive regulation of fibroblast proliferation	Estrogen receptor	Homo sapiens (human)
stem cell differentiation	Estrogen receptor	Homo sapiens (human)
regulation of inflammatory response	Estrogen receptor	Homo sapiens (human)
positive regulation of DNA-binding transcription factor activity	Estrogen receptor	Homo sapiens (human)
RNA polymerase II preinitiation complex assembly	Estrogen receptor	Homo sapiens (human)
uterus development	Estrogen receptor	Homo sapiens (human)
vagina development	Estrogen receptor	Homo sapiens (human)
prostate epithelial cord elongation	Estrogen receptor	Homo sapiens (human)
prostate epithelial cord arborization involved in prostate glandular acinus morphogenesis	Estrogen receptor	Homo sapiens (human)
regulation of branching involved in prostate gland morphogenesis	Estrogen receptor	Homo sapiens (human)
mammary gland branching involved in pregnancy	Estrogen receptor	Homo sapiens (human)
mammary gland alveolus development	Estrogen receptor	Homo sapiens (human)
epithelial cell proliferation involved in mammary gland duct elongation	Estrogen receptor	Homo sapiens (human)
protein localization to chromatin	Estrogen receptor	Homo sapiens (human)
cellular response to estradiol stimulus	Estrogen receptor	Homo sapiens (human)
negative regulation of miRNA transcription	Estrogen receptor	Homo sapiens (human)
regulation of epithelial cell apoptotic process	Estrogen receptor	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Estrogen receptor	Homo sapiens (human)
cellular response to estrogen stimulus	Estrogen receptor	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Estrogen receptor beta	Homo sapiens (human)
regulation of DNA-templated transcription	Estrogen receptor beta	Homo sapiens (human)
signal transduction	Estrogen receptor beta	Homo sapiens (human)
cell-cell signaling	Estrogen receptor beta	Homo sapiens (human)
negative regulation of cell growth	Estrogen receptor beta	Homo sapiens (human)
intracellular estrogen receptor signaling pathway	Estrogen receptor beta	Homo sapiens (human)
positive regulation of DNA-templated transcription	Estrogen receptor beta	Homo sapiens (human)
positive regulation of DNA-binding transcription factor activity	Estrogen receptor beta	Homo sapiens (human)
cellular response to estradiol stimulus	Estrogen receptor beta	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Estrogen receptor beta	Homo sapiens (human)
cellular response to estrogen stimulus	Estrogen receptor beta	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Estrogen receptor	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Estrogen receptor	Homo sapiens (human)
TFIIB-class transcription factor binding	Estrogen receptor	Homo sapiens (human)
transcription coregulator binding	Estrogen receptor	Homo sapiens (human)
transcription corepressor binding	Estrogen receptor	Homo sapiens (human)
transcription coactivator binding	Estrogen receptor	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Estrogen receptor	Homo sapiens (human)
chromatin binding	Estrogen receptor	Homo sapiens (human)
DNA-binding transcription factor activity	Estrogen receptor	Homo sapiens (human)
nuclear receptor activity	Estrogen receptor	Homo sapiens (human)
steroid binding	Estrogen receptor	Homo sapiens (human)
protein binding	Estrogen receptor	Homo sapiens (human)
calmodulin binding	Estrogen receptor	Homo sapiens (human)
beta-catenin binding	Estrogen receptor	Homo sapiens (human)
zinc ion binding	Estrogen receptor	Homo sapiens (human)
TBP-class protein binding	Estrogen receptor	Homo sapiens (human)
enzyme binding	Estrogen receptor	Homo sapiens (human)
protein kinase binding	Estrogen receptor	Homo sapiens (human)
nitric-oxide synthase regulator activity	Estrogen receptor	Homo sapiens (human)
nuclear estrogen receptor activity	Estrogen receptor	Homo sapiens (human)
nuclear estrogen receptor binding	Estrogen receptor	Homo sapiens (human)
estrogen response element binding	Estrogen receptor	Homo sapiens (human)
identical protein binding	Estrogen receptor	Homo sapiens (human)
ATPase binding	Estrogen receptor	Homo sapiens (human)
14-3-3 protein binding	Estrogen receptor	Homo sapiens (human)
sequence-specific double-stranded DNA binding	Estrogen receptor	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Estrogen receptor beta	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Estrogen receptor beta	Homo sapiens (human)
DNA binding	Estrogen receptor beta	Homo sapiens (human)
nuclear steroid receptor activity	Estrogen receptor beta	Homo sapiens (human)
nuclear receptor activity	Estrogen receptor beta	Homo sapiens (human)
steroid binding	Estrogen receptor beta	Homo sapiens (human)
protein binding	Estrogen receptor beta	Homo sapiens (human)
zinc ion binding	Estrogen receptor beta	Homo sapiens (human)
enzyme binding	Estrogen receptor beta	Homo sapiens (human)
nuclear estrogen receptor activity	Estrogen receptor beta	Homo sapiens (human)
estrogen response element binding	Estrogen receptor beta	Homo sapiens (human)
receptor antagonist activity	Estrogen receptor beta	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
nucleus	Estrogen receptor	Homo sapiens (human)
nucleoplasm	Estrogen receptor	Homo sapiens (human)
transcription regulator complex	Estrogen receptor	Homo sapiens (human)
cytoplasm	Estrogen receptor	Homo sapiens (human)
Golgi apparatus	Estrogen receptor	Homo sapiens (human)
cytosol	Estrogen receptor	Homo sapiens (human)
plasma membrane	Estrogen receptor	Homo sapiens (human)
membrane	Estrogen receptor	Homo sapiens (human)
chromatin	Estrogen receptor	Homo sapiens (human)
euchromatin	Estrogen receptor	Homo sapiens (human)
protein-containing complex	Estrogen receptor	Homo sapiens (human)
nucleus	Estrogen receptor	Homo sapiens (human)
nucleus	Estrogen receptor beta	Homo sapiens (human)
nucleoplasm	Estrogen receptor beta	Homo sapiens (human)
mitochondrion	Estrogen receptor beta	Homo sapiens (human)
intracellular membrane-bounded organelle	Estrogen receptor beta	Homo sapiens (human)
chromatin	Estrogen receptor beta	Homo sapiens (human)
nucleus	Estrogen receptor beta	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (37)

Assay ID	Title	Year	Journal	Article
AID24852	Oral bioavailability in cynomolgus monkey.	1998	Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16	Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene.
AID24853	Oral bioavailability in rat	1998	Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16	Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene.
AID236196	Total clearance of compound in rat after administration of 1 mg/kg (iv) and 5 mg/kg (po)	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
AID1283268	Inhibition of delta 8-7 isomerase in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis	2016	Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3	The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts.
AID250368	Percent agonist activity against human breast adenocarcinoma (MCF-7) cell proliferation	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
AID1431897	Oral bioavailability in rat	2017	Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4	Novel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer.
AID242068	Inhibition of [3H]estradiol binding to human estrogen receptor alpha expressed in HeLa cells	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
AID240821	Binding affinity for human estrogen receptor beta	2005	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3	Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.
AID179989	In vivo prevention of reduced serum cholesterol in ovariectomised rats on oral administration	1998	Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16	Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene.
AID236579	Steady state volume of distribution in rat after administration of 1 mg/kg (iv) and 5 mg/kg (po)	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
AID252114	Anti-estrogenic effect in rat uterine weight assay	2005	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3	Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.
AID1283252	Inhibition of C-24 reductase in Dhcr7-deficient mouse Neuro2a cells assessed as increase in desmosterol levels at 1 uM by LC-MS/GC-MS analysis	2016	Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3	The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts.
AID251711	Estrogenic effect in rat uterine weight assay	2005	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3	Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.
AID242722	Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor alpha; ERE assay	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
AID248083	Inhibition of estrogen-mediated human breast adenocarcinoma (MCF-7) cell proliferation	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
AID257003	In vivo agonism of estradiol in rat uterine tissue after 1 mg/kg, po by uterine weight assay	2005	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23	Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms.
AID1283269	Inhibition of DR24 in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis	2016	Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3	The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts.
AID240848	Binding affinity for human estrogen receptor alpha	2005	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3	Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.
AID1283251	Inhibition of C-24 reductase in Dhcr7-deficient mouse Neuro2a cells assessed as increase in zymosterol levels at 1 uM by LC-MS/GC-MS analysis	2016	Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3	The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts.
AID257001	Antiproliferative activity against human breast cancer MCF7 cell line in presence of 0.003 nM estradiol	2005	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23	Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms.
AID257002	In vivo antagonism of estradiol in rat uterine tissue after 1 mg/kg, po by uterine weight assay	2005	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23	Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms.
AID1283247	Inhibition of delta 8-7 isomerase in mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis	2016	Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3	The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts.
AID242704	Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor beta; ERE assay	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
AID236640	Maximum plasma concentration of compound in rat after peroral administration of 5 mg/kg	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
AID69383	Inhibition of estradiol binding to estrogen receptor	1998	Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16	Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene.
AID179988	In vivo prevention of bone loss in ovariectomised rats on oral administration	1998	Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16	Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene.
AID236026	Oral bioavailability in rat (dose 5 mg/kg)	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
AID256999	Inhibition of binding to recombinant human ERbeta by scintillation proximity assay	2005	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23	Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms.
AID257000	Selectivity for human ERbeta over ERalpha	2005	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23	Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms.
AID256998	Inhibition of binding to recombinant human ERalpha by scintillation proximity assay	2005	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23	Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms.
AID247489	Inhibition of MCF-7 cell proliferation	2005	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3	Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.
AID1283275	Inhibition of DR24 in mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis	2016	Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3	The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts.
AID242043	Inhibition of [3H]estradiol binding to human estrogen receptor beta expressed in HeLa cells	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
AID1797989	ER-alpha Radioligand Binding Assay and ERE-Luciferase Reporter Assay. from Article 10.1021/jm030086h: \\Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.\\	2003	Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14	Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.
AID1797992	ER-alpha Radioligand Binding Assay and ERE-Luciferase Reporter Assay. from Article 10.1021/jm040858p: \\Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
AID1346845	Human Estrogen receptor-alpha (3A. Estrogen receptors)	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
AID1346880	Human Estrogen receptor-beta (3A. Estrogen receptors)	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	3 (3.66)	18.2507
2000's	41 (50.00)	29.6817
2010's	37 (45.12)	24.3611
2020's	1 (1.22)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	14 (15.91%)	5.53%
Reviews	25 (28.41%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	49 (55.68%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
catechol [no description available]	2.07	1	0	catechols	allelochemical; genotoxin; plant metabolite
anastrozole [no description available]	4.08	1	0	nitrile; triazoles	antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor
bay h 4502 bifonazole : A racemate comprising equimolar amounts of R- and S-bifonazole. It is a broad spectrum antifungal drug used for the treatment of fungal skin and nail infections.. 1-[biphenyl-4-yl(phenyl)methyl]imidazole : A member of the class of imidazoles carrying an alpha-(biphenyl-4-yl)benzyl substituent at position 1.	2.13	1	0	biphenyls; imidazoles
chloroxine chloroxine : A monohydroxyquinoline that is quinolin-8-ol in which the hydrogens at positions 5 and 7 have been substituted by chlorine. A synthetic antibacterial prepared by chlorination of quinolin-8-ol, it is used for the treatment of dandruff and seborrhoeic dermatitis of the scalp.	2.13	1	0	monohydroxyquinoline; organochlorine compound	antibacterial agent; antifungal drug; antiseborrheic
chlorzoxazone Chlorzoxazone: A centrally acting central muscle relaxant with sedative properties. It is claimed to inhibit muscle spasm by exerting an effect primarily at the level of the spinal cord and subcortical areas of the brain. (From Martindale, The Extra Pharmacopoea, 30th ed, p1202). chlorzoxazone : A member of the class of 1,3-benzoxazoles that is 1,3-benzoxazol-2-ol in which the hydrogen atom at position 5 is substituted by chlorine. A centrally acting muscle relaxant with sedative properties, it is used for the symptomatic treatment of painful muscle spasm.	3.41	1	1	1,3-benzoxazoles; heteroaryl hydroxy compound; organochlorine compound	muscle relaxant; sedative
6-hydroxychlorzoxazone 6-hydroxychlorzoxazone: chlorzoxazone metabolite in humans	3.41	1	1	benzoxazole
clomiphene [no description available]	2.13	1	0	tertiary amine	estrogen antagonist; estrogen receptor modulator
clotrimazole [no description available]	2.13	1	0	conazole antifungal drug; imidazole antifungal drug; imidazoles; monochlorobenzenes	antiinfective agent; environmental contaminant; xenobiotic
doxepin Doxepin: A dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors.. doxepin : A dibenzooxepine that is 6,11-dihydrodibenzo[b,e]oxepine substituted by a 3-(dimethylamino)propylidene group at position 11. It is used as an antidepressant drug.	2.13	1	0	dibenzooxepine; tertiary amino compound	antidepressant
econazole Econazole: An imidazole derivative that is commonly used as a topical antifungal agent.. econazole : A racemate composed of equimolar amounts of (R)- and (S)-econazole. Used (as its nitrate salt) to treat skin infections such as athlete's foot, jock itch, ringworm and other fungal skin infections.. 1-{2-(4-chlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl}imidazole : A member of the class of imidazoles that is 1-(2,4-dichlorophenyl)-2-(imidazol-1-yl)ethanol in which the hydroxyl hydrogen is replaced by a 4-chlorobenzyl group.	2.13	1	0	dichlorobenzene; ether; imidazoles; monochlorobenzenes
fluconazole Fluconazole: Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.. fluconazole : A member of the class of triazoles that is propan-2-ol substituted at position 1 and 3 by 1H-1,2,4-triazol-1-yl groups and at position 2 by a 2,4-difluorophenyl group. It is an antifungal drug used for the treatment of mucosal candidiasis and for systemic infections including systemic candidiasis, coccidioidomycosis, and cryptococcosis.	8.42	1	1	conazole antifungal drug; difluorobenzene; tertiary alcohol; triazole antifungal drug	environmental contaminant; P450 inhibitor; xenobiotic
fluphenazine [no description available]	2.13	1	0	N-alkylpiperazine; organofluorine compound; phenothiazines	anticoronaviral agent; dopaminergic antagonist; phenothiazine antipsychotic drug
haloperidol Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.	2.13	1	0	aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol	antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist
hexachlorophene Hexachlorophene: A chlorinated bisphenol antiseptic with a bacteriostatic action against Gram-positive organisms, but much less effective against Gram-negative organisms. It is mainly used in soaps and creams and is an ingredient of various preparations used for skin disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p797). hexachlorophene : An organochlorine compound that is diphenylmethane in which each of the phenyl groups is substituted by chlorines at positions 2, 3, and 5, and by a hydroxy group at position 6. An antiseptic that is effective against Gram-positive organisms, it is used in soaps and creams for the treatment of various skin disorders. It is also used in agriculture as an acaricide and fungicide, but is not approved for such use within the European Union.	2.13	1	0	bridged diphenyl fungicide; polyphenol; trichlorobenzene	acaricide; antibacterial agent; antifungal agrochemical; antiseptic drug
hydroxyzine Hydroxyzine: A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.. hydroxyzine : A N-alkylpiperazine that is piperzine in which the nitrogens atoms are substituted by 2-(2-hydroxyethoxy)ethyl and (4-chlorophenyl)(phenyl)methyl groups respectively.	2.13	1	0	hydroxyether; monochlorobenzenes; N-alkylpiperazine	anticoronaviral agent; antipruritic drug; anxiolytic drug; dermatologic drug; H1-receptor antagonist
ketoconazole 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.	8.42	1	1	dichlorobenzene; dioxolane; ether; imidazoles; N-acylpiperazine; N-arylpiperazine
metformin Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289). metformin : A member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1.	4.08	1	0	guanidines	environmental contaminant; geroprotector; hypoglycemic agent; xenobiotic
miconazole Miconazole: An imidazole antifungal agent that is used topically and by intravenous infusion.. 1-[2-(2,4-dichlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl]imidazole : A member of the class of imidazoles that is 1-(2,4-dichlorophenyl)-2-(imidazol-1-yl)ethanol in which the hydroxyl hydrogen is replaced by a 2,4-dichlorobenzyl group.. miconazole : A racemate composed of equimolar amounts of (R)- and (S)-miconazole. Used (as its nitrate salt) to treat skin infections such as athlete's foot, jock itch, ringworm and other fungal skin infections. It inhibits the synthesis of ergosterol, a critical component of fungal cell membranes.	2.13	1	0	dichlorobenzene; ether; imidazoles
nafoxidine Nafoxidine: An estrogen antagonist that has been used in the treatment of breast cancer.	1.99	1	0	benzenes; naphthalenes; ring assembly
perphenazine Perphenazine: An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.. perphenazine : A phenothiazine derivative in which the phenothiazine tricycle carries a chloro substituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at N-10.	2.13	1	0	N-(2-hydroxyethyl)piperazine; N-alkylpiperazine; organochlorine compound; phenothiazines	antiemetic; dopaminergic antagonist; phenothiazine antipsychotic drug
prochlorperazine Prochlorperazine: A phenothiazine antipsychotic used principally in the treatment of NAUSEA; VOMITING; and VERTIGO. It is more likely than CHLORPROMAZINE to cause EXTRAPYRAMIDAL DISORDERS. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612). prochlorperazine : A member of the class of phenothiazines that is 10H-phenothiazine having a chloro substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position.	2.13	1	0	N-alkylpiperazine; N-methylpiperazine; organochlorine compound; phenothiazines	alpha-adrenergic antagonist; antiemetic; cholinergic antagonist; dopamine receptor D2 antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; first generation antipsychotic
raloxifene raloxifene : A member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogens at positions 2, 3, and 6 have been replaced by p-hydroxyphenyl, p-[2-(piperidin-1-yl)ethoxy]benzoyl, and hydroxy groups, respectively.	3.12	5	0	1-benzothiophenes; aromatic ketone; N-oxyethylpiperidine; phenols	bone density conservation agent; estrogen antagonist; estrogen receptor modulator
imatinib [no description available]	2.13	1	0	aromatic amine; benzamides; N-methylpiperazine; pyridines; pyrimidines	antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor
trazodone Trazodone: A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309). trazodone : An N-arylpiperazine in which one nitrogen is substituted by a 3-chlorophenyl group, while the other is substituted by a 3-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propyl group.	2.13	1	0	monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; triazolopyridine	adrenergic antagonist; antidepressant; anxiolytic drug; H1-receptor antagonist; sedative; serotonin uptake inhibitor
trifluoperazine [no description available]	2.13	1	0	N-alkylpiperazine; N-methylpiperazine; organofluorine compound; phenothiazines	antiemetic; calmodulin antagonist; dopaminergic antagonist; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor; phenothiazine antipsychotic drug
trimebutine Trimebutine: Proposed spasmolytic with possible local anesthetic action used in gastrointestinal disorders.	2.13	1	0	trihydroxybenzoic acid
ethinyl estradiol Ethinyl Estradiol: A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.. 17alpha-ethynylestradiol : A 3-hydroxy steroid that is estradiol substituted by a ethynyl group at position 17. It is a xenoestrogen synthesized from estradiol and has been shown to exhibit high estrogenic potency on oral administration.	2.41	2	0	17-hydroxy steroid; 3-hydroxy steroid; terminal acetylenic compound	xenoestrogen
triparanol Triparanol: Antilipemic agent with high ophthalmic toxicity. According to Merck Index, 11th ed, the compound was withdrawn from the market in 1962 because of its association with the formation of irreversible cataracts.	2.13	1	0	stilbenoid	anticoronaviral agent
thiophenes Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.	7.71	11	0	mancude organic heteromonocyclic parent; monocyclic heteroarene; thiophenes; volatile organic compound	non-polar solvent
trans-1,4-bis(2-chlorobenzaminomethyl)cyclohexane dihydrochloride trans-1,4-Bis(2-chlorobenzaminomethyl)cyclohexane Dihydrochloride: An anti-cholesteremic agent that inhibits delta 7-reductase, delta 14 reductase, and sterol biosynthesis.	2.13	1	0
methylnitrosourea Methylnitrosourea: A nitrosourea compound with alkylating, carcinogenic, and mutagenic properties.. N-methyl-N-nitrosourea : A member of the class of N-nitrosoureas that is urea in which one of the nitrogens is substituted by methyl and nitroso groups.	2	1	0	N-nitrosoureas	alkylating agent; carcinogenic agent; mutagen; teratogenic agent
dronabinol Dronabinol: A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.. Delta(9)-tetrahydrocannabinol : A diterpenoid that is 6a,7,8,10a-tetrahydro-6H-benzo[c]chromene substituted at position 1 by a hydroxy group, positions 6, 6 and 9 by methyl groups and at position 3 by a pentyl group. The principal psychoactive constituent of the cannabis plant, it is used for treatment of anorexia associated with AIDS as well as nausea and vomiting associated with cancer chemotherapy.	2.1	1	0	benzochromene; diterpenoid; phytocannabinoid; polyketide	cannabinoid receptor agonist; epitope; hallucinogen; metabolite; non-narcotic analgesic
molindone Molindone: An indole derivative effective in schizophrenia and other psychoses and possibly useful in the treatment of the aggressive type of undersocialized conduct disorder. Molindone has much lower affinity for D2 receptors than most antipsychotic agents and has a relatively low affinity for D1 receptors. It has only low to moderate affinity for cholinergic and alpha-adrenergic receptors. Some electrophysiologic data from animals indicate that molindone has certain characteristics that resemble those of CLOZAPINE. (From AMA Drug Evaluations Annual, 1994, p283)	2.13	1	0	indoles
levormeloxifene levormeloxifene: RN refers to (trans)-isomer	2.46	2	0
paroxetine Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.. paroxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo.	8.42	1	1	aromatic ether; benzodioxoles; organofluorine compound; piperidines	antidepressant; anxiolytic drug; hepatotoxic agent; P450 inhibitor; serotonin uptake inhibitor
lovastatin Lovastatin: A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver.. lovastatin : A fatty acid ester that is mevastatin carrying an additional methyl group on the carbobicyclic skeleton. It is used in as an anticholesteremic drug and has been found in fungal species such as Aspergillus terreus and Pleurotus ostreatus (oyster mushroom).	2.13	1	0	delta-lactone; fatty acid ester; hexahydronaphthalenes; polyketide; statin (naturally occurring)	anticholesteremic drug; antineoplastic agent; Aspergillus metabolite; prodrug
simvastatin Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug.	2.13	1	0	delta-lactone; fatty acid ester; hexahydronaphthalenes; statin (semi-synthetic)	EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor; EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor; ferroptosis inducer; geroprotector; prodrug
pravastatin Pravastatin: An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).. pravastatin : A carboxylic ester resulting from the formal condensation of (S)-2-methylbutyric acid with the hydroxy group adjacent to the ring junction of (3R,5R)-7-[(1S,2S,6S,8S,8aR)-6,8-dihydroxy-2-methyl-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid. Derived from microbial transformation of mevastatin, pravastatin is a reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA). The sodium salt is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin.	2.13	1	0	3-hydroxy carboxylic acid; carbobicyclic compound; carboxylic ester; hydroxy monocarboxylic acid; secondary alcohol; statin (semi-synthetic)	anticholesteremic drug; environmental contaminant; metabolite; xenobiotic
raloxifene hydrochloride Raloxifene Hydrochloride: A second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.. raloxifene hydrochloride : A hydrochloride salt resulting from the reaction of equimolar amounts of raloxifene and hydrogen chloride.	8.71	22	0	hydrochloride	bone density conservation agent; estrogen antagonist; estrogen receptor modulator
aromasil [no description available]	4.08	1	0	17-oxo steroid; 3-oxo-Delta(1),Delta(4)-steroid	antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor; environmental contaminant; xenobiotic
aripiprazole Aripiprazole: A piperazine and quinolone derivative that is used primarily as an antipsychotic agent. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A. It is used for the treatment of SCHIZOPHRENIA and BIPOLAR DISORDER, and as an adjunct therapy for the treatment of depression.. aripiprazole : An N-arylpiperazine that is piperazine substituted by a 4-[(2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)oxy]butyl group at position 1 and by a 2,3-dichlorophenyl group at position 4. It is an antipsychotic drug used for the treatment of Schizophrenia, and other mood disorders.	2.13	1	0	aromatic ether; delta-lactam; dichlorobenzene; N-alkylpiperazine; N-arylpiperazine; quinolone	drug metabolite; H1-receptor antagonist; second generation antipsychotic; serotonergic agonist
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol [no description available]	2.01	1	0	stilbenoid
mevastatin mevastatin: antifungal metabolite from Penicillium brevicopactum; potent inhibitory activity to sterol synthesis; structure. mevastatin : A carboxylic ester that is pravastatin that is lacking the allylic hydroxy group. A hydroxymethylglutaryl-CoA reductase inhibitor (statin) isolated from Penicillium citrinum and from Penicillium brevicompactum, its clinical use as a lipid-regulating drug ceased following reports of toxicity in animals.	2.13	1	0	2-pyranones; carboxylic ester; hexahydronaphthalenes; polyketide; statin (naturally occurring)	antifungal agent; apoptosis inducer; EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor; fungal metabolite; Penicillium metabolite
triazoles Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.	4.08	1	0	1,2,3-triazole
artemisinin (+)-artemisinin : A sesquiterpene lactone obtained from sweet wormwood, Artemisia annua, which is used as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.	2.13	1	0	organic peroxide; sesquiterpene lactone	antimalarial; plant metabolite
artemether Artemether: An artemisinin derivative that is used in the treatment of MALARIA.. artemether : An artemisinin derivative that is artemisinin in which the lactone has been converted to the corresponding lactol methyl ether. It is used in combination with lumefantrine as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.	2.13	1	0	artemisinin derivative; cyclic acetal; organic peroxide; semisynthetic derivative; sesquiterpenoid	antimalarial
fulvestrant Fulvestrant: An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer.. fulvestrant : A 3-hydroxy steroid that is 17beta-estradiol in which the 7alpha hydrogen has been replaced by a nonyl group in which one of the hydrogens of the terminal methyl has been replaced by a (4,4,5,5,5-pentafluoropentyl)sulfinyl group. An estrogen receptor antagonist, it is used in the treatment of breast cancer.	3.06	4	0	17beta-hydroxy steroid; 3-hydroxy steroid; organofluorine compound; sulfoxide	antineoplastic agent; estrogen antagonist; estrogen receptor antagonist
pyridinoline pyridinoline: 3-hydroxypyridinium derivative collagen crosslink; structure	2.02	1	0	organonitrogen compound; organooxygen compound
deoxypyridinoline deoxypyridinoline: structure given in first source	4.1	3	1
1,1-dimethylheptyl-11-hydroxytetrahydrocannabinol HU 211: structure given in first source; HU 211 is active & HU 210 is inactive as canibinoids; functional N-methyl-D-aspartate receptor blocker; RN given is for (6aS-trans)-isomer	2.1	1	0
bazedoxifene [no description available]	8.42	21	0	phenylindole
bis(4-piperidinophenol)diimidonaphthalene-1,4,5,8-tetracarboxylic acid dibenzosulfoethylate ritetronium: RN given refers to parent cpd; structure	3.11	1	0
ly 353381 LY 353381: structure in first source	7.71	11	0
tibolone tibolone: used in prevention of postmenopausal osteoporosis. tibolone : Estran-3-one with a double bond between positions 5 and 10, and bearing both an ethynyl group and a hydroxy group at position 17 (R-configuration). A synthetic steroid hormone drug which acts as an agonist at all five type I steroid hormone receptors, it is used in the prevention of postmenopausal osteoporosis and for treatment of endometriosis.	5.02	2	0	17beta-hydroxy steroid; terminal acetylenic compound	bone density conservation agent; hormone agonist
afimoxifene afimoxifene : A tertiary amino compound that is tamoxifen in which the phenyl group which is in a Z- relationship to the ethyl substituent is hydroxylated at the para- position. It is the active metabolite of tamoxifen.	2.01	1	0	phenols; tertiary amino compound	antineoplastic agent; estrogen receptor antagonist; metabolite
stilbenes Stilbenes: Organic compounds that contain 1,2-diphenylethylene as a functional group.. trans-stilbene : The trans-isomer of stilbene.	3.11	1	0	stilbene
digoxin Digoxin: A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666). digoxin : A cardenolide glycoside that is digitoxin beta-hydroxylated at C-12. A cardiac glycoside extracted from the foxglove plant, Digitalis lanata, it is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation, but the margin between toxic and therapeutic doses is small.	8.41	1	1	cardenolide glycoside; steroid saponin	anti-arrhythmia drug; cardiotonic drug; EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor; epitope
tamoxifen [no description available]	8.69	19	0	stilbenoid; tertiary amino compound	angiogenesis inhibitor; antineoplastic agent; bone density conservation agent; EC 1.2.3.1 (aldehyde oxidase) inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; estrogen antagonist; estrogen receptor antagonist; estrogen receptor modulator
toremifene Toremifene: A first generation selective estrogen receptor modulator (SERM). Like TAMOXIFEN, it is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on mammary and uterine tissue.	5.28	3	0	aromatic ether; organochlorine compound; tertiary amine	antineoplastic agent; bone density conservation agent; estrogen antagonist; estrogen receptor modulator
idoxifene idoxifene: structure given in first source	3.11	1	0	stilbenoid
ospemifene Ospemifene: structure in first source. ospemifene : An organochlorine compound that is a selective estrogen receptor modulator; used for treatment of dyspareunia.	6.28	5	0	aromatic ether; organochlorine compound; primary alcohol	anti-inflammatory agent; antineoplastic agent; estrogen receptor modulator
pulmicort Budesonide: A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.. budesonide : A glucocorticoid steroid having a highly oxygenated pregna-1,4-diene structure. It is used mainly in the treatment of asthma and non-infectious rhinitis and for treatment and prevention of nasal polyposis.	2.13	1	0	11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; cyclic acetal; glucocorticoid; primary alpha-hydroxy ketone	anti-inflammatory drug; bronchodilator agent; drug allergen
pitavastatin pitavastatin : A dihydroxy monocarboxylic acid that is (6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]hept-6-enoic acid in which the two hydroxy groups are located at positions 3 and 5 (the 3R,5S-stereoisomer). Used as its calcium salt for treatment of hypercholesterolemia (elevated levels of cholesterol in the blood) on patients unable to sufficiently lower their cholesterol levels by diet and exercise.	2.13	1	0	cyclopropanes; dihydroxy monocarboxylic acid; monofluorobenzenes; quinolines; statin (synthetic)	antioxidant
fenretinide Fenretinide: A synthetic retinoid that is used orally as a chemopreventive against prostate cancer and in women at risk of developing contralateral breast cancer. It is also effective as an antineoplastic agent.. 4-hydroxyphenyl retinamide : A retinoid obtained by formal condensation of the carboxy group of all-trans retinoic acid and the anilino group of 4-hydroxyaniline. Synthetic retinoid agonist. Antiproliferative, antioxidant and anticancer agent with a long half-life in vivo. Apoptotic effects appear to be mediated by a mechanism distinct from that of 'classical' retinoids.	4.08	1	0	monocarboxylic acid amide; retinoid	antineoplastic agent; antioxidant
gw 5638 3-(4-(1,2-diphenylbut-1-enyl)phenyl)acrylic acid: exhibits estrogen agonist activity in bone and estrogen antagonist activity in uterus; structure in first source	3.11	1	0
palbociclib [no description available]	2.31	1	0	aminopyridine; aromatic ketone; cyclopentanes; piperidines; pyridopyrimidine; secondary amino compound; tertiary amino compound	antineoplastic agent; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
dextromethorphan Dextromethorphan: Methyl analog of DEXTRORPHAN that shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (RECEPTORS, N-METHYL-D-ASPARTATE) and acts as a non-competitive channel blocker. It is one of the widely used ANTITUSSIVES, and is also used to study the involvement of glutamate receptors in neurotoxicity.. dextromethorphan : A 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene in which the sterocenters at positions 4a, 10 and 10a have S-configuration. It is a prodrug of dextrorphan and used as an antitussive drug for suppressing cough.	3.41	1	1	6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene	antitussive; environmental contaminant; neurotoxin; NMDA receptor antagonist; oneirogen; prodrug; xenobiotic
tan 67 [no description available]	2.13	1	0	quinolines
odanacatib odanacatib: a selective inhibitor of cathepsin K for the treatment of post-menopausal osteoporosis; structure in first source	3.25	1	0
piperidines Piperidines: A family of hexahydropyridines.	7.79	12	0
warfarin Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group.	8.41	1	1	benzenes; hydroxycoumarin; methyl ketone

Condition	Indicated	Relationship Strength	Studies	Trials
Breast Cancer [description not available]	0	11.69	24	3
Hormone-Dependent Neoplasms [description not available]	0	2.44	2	0
Breast Neoplasms Tumors or cancer of the human BREAST.	1	13.69	24	3
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	3.7	3	0
Metastase [description not available]	0	2.31	1	0
Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.	0	2.31	1	0
Deep Vein Thrombosis [description not available]	0	3	1	0
Apoplexy [description not available]	0	7.87	5	2
Cardiovascular Diseases Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.	0	4.46	3	0
Menopause The last menstrual period. Permanent cessation of menses (MENSTRUATION) is usually defined after 6 to 12 months of AMENORRHEA in a woman over 45 years of age. In the United States, menopause generally occurs in women between 48 and 55 years of age.	0	4.16	3	0
Venous Thrombosis The formation or presence of a blood clot (THROMBUS) within a vein.	0	3	1	0
Stroke A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)	0	7.87	5	2
Urogenital Prolapse [description not available]	0	3.01	1	0
Vulvar Diseases Pathological processes of the VULVA.	0	3.01	1	0
Atrophy Decrease in the size of a cell, tissue, organ, or multiple organs, associated with a variety of pathological conditions such as abnormal cellular changes, ischemia, malnutrition, or hormonal changes.	0	9.45	3	0
Vaginal Diseases Pathological processes of the VAGINA.	0	4.45	3	0
Pelvic Organ Prolapse Abnormal descent of a pelvic organ resulting in the protrusion of the organ beyond its normal anatomical confines. Symptoms often include vaginal discomfort, DYSPAREUNIA; URINARY STRESS INCONTINENCE; and FECAL INCONTINENCE.	0	3.01	1	0
Age-Related Osteoporosis [description not available]	0	6.87	11	0
Bone Loss, Perimenopausal [description not available]	0	12.5	29	6
Dyspareunia Recurrent genital pain occurring during, before, or after SEXUAL INTERCOURSE in either the male or the female.	0	3.93	1	0
Osteoporosis Reduction of bone mass without alteration in the composition of bone, leading to fractures. Primary osteoporosis can be of two major types: postmenopausal osteoporosis (OSTEOPOROSIS, POSTMENOPAUSAL) and age-related or senile osteoporosis.	1	8.87	11	0
Osteoporosis, Postmenopausal Metabolic disorder associated with fractures of the femoral neck, vertebrae, and distal forearm. It occurs commonly in women within 15-20 years after menopause, and is caused by factors associated with menopause including estrogen deficiency.	0	12.5	29	6
Hot Flashes A sudden, temporary sensation of heat predominantly experienced by some women during MENOPAUSE. (Random House Unabridged Dictionary, 2d ed)	0	5.4	3	0
Adjuvant Arthritis [description not available]	0	2.13	1	0
Arthritis, Degenerative [description not available]	0	2.13	1	0
Osteoarthritis A progressive, degenerative joint disease, the most common form of arthritis, especially in older persons. The disease is thought to result not from the aging process but from biochemical changes and biomechanical stresses affecting articular cartilage. In the foreign literature it is often called osteoarthrosis deformans.	0	2.13	1	0
Osteoporotic Fractures Breaks in bones resulting from low bone mass and microarchitectural deterioration characteristic of OSTEOPOROSIS.	0	3.06	1	0
Thromboembolism, Venous [description not available]	0	5.96	3	1
Venous Thromboembolism Obstruction of a vein or VEINS (embolism) by a blood clot (THROMBUS) in the blood stream.	0	5.96	3	1
Fracture, Pathologic [description not available]	0	2.05	1	0
Adverse Drug Event [description not available]	0	2.97	1	0
Drug-Related Side Effects and Adverse Reactions Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.	0	2.97	1	0
Bone Fractures [description not available]	0	8.74	9	3
Coronary Heart Disease [description not available]	0	6.08	3	2
Hangman Fracture [description not available]	0	5.97	3	1
Coronary Disease An imbalance between myocardial functional requirements and the capacity of the CORONARY VESSELS to supply sufficient blood flow. It is a form of MYOCARDIAL ISCHEMIA (insufficient blood supply to the heart muscle) caused by a decreased capacity of the coronary vessels.	0	6.08	3	2
Spinal Fractures Broken bones in the vertebral column.	0	5.97	3	1
Fractures, Bone Breaks in bones.	0	8.74	9	3
Carcinoma, Non-Small Cell Lung [description not available]	0	2.05	1	0
Cancer of Lung [description not available]	0	2.05	1	0
Carcinoma, Non-Small-Cell Lung A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.	0	2.05	1	0
Lung Neoplasms Tumors or cancer of the LUNG.	0	2.05	1	0
Thromboembolism Obstruction of a blood vessel (embolism) by a blood clot (THROMBUS) in the blood stream.	0	3.39	2	0
Corpus Luteum Cyst [description not available]	0	3.45	1	1
Cancer of Ovary [description not available]	0	3.45	1	1
Polyps Discrete abnormal tissue masses that protrude into the lumen of the DIGESTIVE TRACT or the RESPIRATORY TRACT. Polyps can be spheroidal, hemispheroidal, or irregular mound-shaped structures attached to the MUCOUS MEMBRANE of the lumen wall either by a stalk, pedunculus, or by a broad base.	0	3.45	1	1
Endometrial Diseases [description not available]	0	3.45	1	1
Ovarian Cysts General term for CYSTS and cystic diseases of the OVARY.	0	3.45	1	1
Ovarian Neoplasms Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.	0	3.45	1	1
Urinary Incontinence Involuntary loss of URINE, such as leaking of urine. It is a symptom of various underlying pathological processes. Major types of incontinence include URINARY URGE INCONTINENCE and URINARY STRESS INCONTINENCE.	0	3.45	1	1
Uterine Diseases Pathological processes involving any part of the UTERUS.	0	3.45	1	1
Carcinoma, Ductal, Breast An invasive (infiltrating) CARCINOMA of the mammary ductal system (MAMMARY GLANDS) in the human BREAST.	0	3.44	1	1
Bone Loss, Osteoclastic [description not available]	0	3.63	3	0
Orthopedic Disorders [description not available]	0	3.83	2	0
Musculoskeletal Diseases Diseases of the muscles and their associated ligaments and other connective tissue and of the bones and cartilage viewed collectively.	0	3.83	2	0
Female Genitourinary Diseases [description not available]	0	2.06	1	0
Cancer of Endometrium [description not available]	0	4.16	3	0
Endometrial Neoplasms Tumors or cancer of ENDOMETRIUM, the mucous lining of the UTERUS. These neoplasms can be benign or malignant. Their classification and grading are based on the various cell types and the percent of undifferentiated cells.	0	4.16	3	0
Adenocarcinoma, Basal Cell [description not available]	0	3	1	0
Adenocarcinoma A malignant epithelial tumor with a glandular organization.	0	3	1	0
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	0	3.27	6	0
Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.	0	2.42	2	0
Anal Atresia [description not available]	0	2.02	1	0
Delayed Effects, Prenatal Exposure [description not available]	0	2.02	1	0
Indigestion [description not available]	0	3.41	1	1
Daytime Sleepiness [description not available]	0	3.41	1	1
Dyspepsia Impaired digestion, especially after eating.	0	3.41	1	1
Disorders of Excessive Somnolence Disorders characterized by hypersomnolence during normal waking hours that may impair cognitive functioning. Subtypes include primary hypersomnia disorders (e.g., IDIOPATHIC HYPERSOMNOLENCE; NARCOLEPSY; and KLEINE-LEVIN SYNDROME) and secondary hypersomnia disorders where excessive somnolence can be attributed to a known cause (e.g., drug affect, MENTAL DISORDERS, and SLEEP APNEA SYNDROME). (From J Neurol Sci 1998 Jan 8;153(2):192-202; Thorpy, Principles and Practice of Sleep Medicine, 2nd ed, p320)	0	3.41	1	1
Liver Dysfunction [description not available]	0	3.41	1	1
Liver Diseases Pathological processes of the LIVER.	0	3.41	1	1
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	0	2.03	1	0
Cirrhosis [description not available]	0	2.04	1	0
Fibrosis Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.	0	2.04	1	0
Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.	0	7.69	3	0
Weight Gain Increase in BODY WEIGHT over existing weight.	0	2.4	2	0
Elevated Cholesterol [description not available]	0	2	1	0
Hypercholesterolemia A condition with abnormally high levels of CHOLESTEROL in the blood. It is defined as a cholesterol value exceeding the 95th percentile for the population.	0	2	1	0
Experimental Mammary Neoplasms [description not available]	0	2	1	0

lasofoxifene

Description

Cross-References

Synonyms (52)

Research Excerpts

Overview

Effects

Actions

Treatment

Toxicity

Pharmacokinetics

Bioavailability

Dosage Studied

Roles (5)

Drug Classes (4)

Protein Targets (4)

Inhibition Measurements

Biological Processes (44)

Molecular Functions (29)

Ceullar Components (13)

Bioassays (37)

Research

Studies (82)

Market Indicators

Research Demand Index: 42.21

Study Types

lasofoxifene

Description

Cross-References

Synonyms (52)

Research Excerpts

Overview

Effects

Actions

Treatment

Toxicity

Pharmacokinetics

Bioavailability

Dosage Studied

Roles (5)

Drug Classes (4)

Protein Targets (4)

Inhibition Measurements

Biological Processes (44)

Molecular Functions (29)

Ceullar Components (13)

Bioassays (37)

Research

Studies (82)

Market Indicators

Research Demand Index: 42.21

Study Types

Related Drugs (71)

Related Conditions (78)