Compounds > sr 16234
Page last updated: 2024-11-11

sr 16234

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

Description

TS 108: an antiestrogen; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9874874
SCHEMBL ID2836841
MeSH IDM0461539

Synonyms (18)

Synonym
sr 16234
sr-16234
sr16234
ts 108
unii-9b29n23k7e
9b29n23k7e ,
229634-98-4
(7alpha)-21-(4-((diethylamino)methyl)-2-methoxyphenoxy)-7-methyl-19-norpregna-1,3,5(10)-trien-3-ol 2-hydroxy-1,2,3-propanetricarboxylate
SCHEMBL2836841
19-norpregna-1,3,5(10)-trien-3-ol, 21-(4-((diethylamino)methyl)-2-methoxyphenoxy)-7-methyl-, (7.alpha.)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) (salt)
hlx-801
tas-108 citrate
(7r,8s,9s,13r,14s,17r)-17-(2-(4-((diethylamino)methyl)-2-methoxyphenoxy)ethyl)-7,13-dimethyl-7,8,9,11,12,13,14,15,16,17-decahydro-6h-cyclopenta[a]phenanthren-3-ol 2-hydroxypropane-1,2,3-tricarboxylate
DTXSID30177512
DB05966
Q7669355
(7r,8s,9s,13r,14s,17r)-17-[2-[4-(diethylaminomethyl)-2-methoxyphenoxy]ethyl]-7,13-dimethyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-3-ol;2-hydroxypropane-1,2,3-tricarboxylic acid
tas 108

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"There was no dose-dependent increase in any adverse events (AEs), and there were no serious AEs or deaths."( Safety, tolerability, and pharmacokinetics of TAS-108 in normal healthy post-menopausal female subjects: a phase I study on single oral dose.
Buzdar, AU; Kuritani, J; Nagayama, S; Shindo, T; Tsuda, M; Yamaya, H; Yonezawa, J; Yonezawa, JI; Yoshida, K, 2005)		0.33
" We therefore investigated the safe dosage, tolerability, and effectiveness on hormone levels and bone metabolism markers and the pharmacokinetics of TAS-108 administered in postmenopausal Japanese women with metastatic breast cancer."( Evaluation of the safety and tolerability of oral TAS-108 in postmenopausal patients with metastatic breast cancer.
Aogi, K; Ikeda, T; Inaji, H; Noguchi, S; Saeki, T; Tabei, T, 2009)		0.35
" All adverse events were mild and involved transient symptoms that resolved without therapeutic intervention."( Safety, tolerability and pharmacokinetics of TAS-108, a novel anti-oestrogen, in healthy post-menopausal Japanese women: a phase I single oral dose study.
Fujita, T; Kumagai, Y; Maeda, M; Otani, Y; Ozaki, M; Shida, M; Tsuruta, H; Yamaya, H; Yokota, S, 2009)		0.35

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic data were obtained on day 1, 2, 15, and 28 of the first course."( A phase I and pharmacokinetic study of TAS-108 in postmenopausal female patients with locally advanced, locally recurrent inoperable, or progressive metastatic breast cancer.
Blakely, LJ; Booser, D; Buzdar, A; Chang, HY; Frye, D; Kuritani, J; Rivera, E; Theriault, R; Tsuda, M; Valero, V, 2004)		0.32
"Twelve healthy subjects participated in an open-label, ascending single-dose, alternating group, safety, tolerance, and pharmacokinetic study of TAS-108 administered orally to two groups of the subjects, one given alternating doses of 10, 40, 120 mg (group A) and the other of 20, 80, 160 mg (group B), in the fasting state."( Safety, tolerability, and pharmacokinetics of TAS-108 in normal healthy post-menopausal female subjects: a phase I study on single oral dose.
Buzdar, AU; Kuritani, J; Nagayama, S; Shindo, T; Tsuda, M; Yamaya, H; Yonezawa, J; Yonezawa, JI; Yoshida, K, 2005)		0.33
" Food did not affect the elimination half-life of TAS-108 or its metabolites."( Safety, tolerability and pharmacokinetics of TAS-108, a novel anti-oestrogen, in healthy post-menopausal Japanese women: a phase I single oral dose study.
Fujita, T; Kumagai, Y; Maeda, M; Otani, Y; Ozaki, M; Shida, M; Tsuruta, H; Yamaya, H; Yokota, S, 2009)		0.35

Bioavailability

ExcerptReferenceRelevance
" Administration of TAS-108 after a high-fat meal markedly increased the bioavailability of the drug."( Safety, tolerability, and pharmacokinetics of TAS-108 in normal healthy post-menopausal female subjects: a phase I study on single oral dose.
Buzdar, AU; Kuritani, J; Nagayama, S; Shindo, T; Tsuda, M; Yamaya, H; Yonezawa, J; Yonezawa, JI; Yoshida, K, 2005)		0.33
" The maximum and systemic exposure to TAS-108 tended to increase with increasing dose and its bioavailability markedly increased after high-fat food intake."( Safety, tolerability, and pharmacokinetics of TAS-108 in normal healthy post-menopausal female subjects: a phase I study on single oral dose.
Buzdar, AU; Kuritani, J; Nagayama, S; Shindo, T; Tsuda, M; Yamaya, H; Yonezawa, J; Yonezawa, JI; Yoshida, K, 2005)		0.33
" The pharmacokinetics of TAS-108 indicated dose proportionality, and its bioavailability was significantly increased by food intake."( Safety, tolerability and pharmacokinetics of TAS-108, a novel anti-oestrogen, in healthy post-menopausal Japanese women: a phase I single oral dose study.
Fujita, T; Kumagai, Y; Maeda, M; Otani, Y; Ozaki, M; Shida, M; Tsuruta, H; Yamaya, H; Yokota, S, 2009)		0.35

Dosage Studied

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

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's9 (75.00)29.6817
2010's3 (25.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.38

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.38 (24.57)
Research Supply Index2.94 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.38)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (50.00%)5.53%
Reviews2 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (33.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
anastrozole
[no description available]		3.1410nitrile;
triazoles		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
9,10-dimethyl-1,2-benzanthracene
9,10-Dimethyl-1,2-benzanthracene: Polycyclic aromatic hydrocarbon found in tobacco smoke that is a potent carcinogen.. 7,12-dimethyltetraphene : A tetraphene having methyl substituents at the 7- and 12-positions. It is a potent carcinogen and is present in tobacco smoke.		2.4320ortho-fused polycyclic arene;
tetraphenes		carcinogenic agent
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.		2.0210hydrochloridebone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
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.		3.14101,2,3-triazole
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.		3.542017beta-hydroxy steroid;
3-hydroxy steroid;
organofluorine compound;
sulfoxide		antineoplastic agent;
estrogen antagonist;
estrogen receptor antagonist
tamoxifen
[no description available]		3.5420stilbenoid;
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
ConditionIndicatedRelationship StrengthStudiesTrials
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.1710
Endometrioma
An enlarged area of ENDOMETRIOSIS that resembles a tumor. It is usually found in the OVARY. When it is filled with old blood, it is known as a chocolate cyst.		02.1710
Endometriosis
A condition in which functional endometrial tissue is present outside the UTERUS. It is often confined to the PELVIS involving the OVARY, the ligaments, cul-de-sac, and the uterovesical peritoneum.		02.1710
Breast Cancer
[description not available]		07.785
Metastase
[description not available]		05.5344
Breast Neoplasms
Tumors or cancer of the human BREAST.		07.785
Neoplasm Metastasis
The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.		05.5344
Hormone-Dependent Neoplasms
[description not available]		03.4611
Carcinoma, Anaplastic
[description not available]		02.0310
Experimental Neoplasms
[description not available]		02.0310
Carcinoma
A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm and not a synonym for cancer.		02.0310