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Topic: Selective estrogen receptor modulator


  
 United States Patent Application: 0010036949
Fifteen clinical studies examining the role of estrogen replacement therapy in cognition demonstrate statistically significant improvements in cognitive function [Haskell et al., Journal of Clinical Epidemiology, 50(11), 1249-1264 (1997)].
In either case drug testing is discontinued to allow the adjustment(if necessary) of delay intervals until a typical and stable level of baseline performance is once again attained [Paule et al., Neurotoxicology and Teratology, 20, 493-502 (1998); Buccafusco et al., Behavioral Pharmacology, 10, 681-690 (1999)].
Chinese hamster ovary cells (CHO-K1) stably transformed to express human m1-m5_receptors can be obtained from Dr. Tom Bonner (Laboratory of Cell Biology, National Institute of Mental Health, Building 36, Rm 3A-17, National Institute of Health, Bethesda, Md. 20892).
http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=/netahtml/PTO/srchnum.html&r=1&f=G&l=50&s1='20010036949'.PGNR.&OS=DN/20010036949&RS=DN/20010036949   (6363 words)

  
 Estrogen and Selective Estrogen Receptor Modulator LY117018 Enhance Release of Nitric Oxide in Rat Aorta -- Rahimian et ...
Although estrogen replacement therapy is both cardioprotective and bone preserving in postmenopausal women, it is accompanied
from sham rats and ovariectomized rats receiving estrogen relaxed
Effect of chronic estrogen treatment of ovariectomized rats (A, implanted groups; B, orally treated groups) on the relaxation-response
http://jpet.aspetjournals.org/cgi/content/full/283/1/116   (4201 words)

  
 OHSU team discovers compound that lacks estrogen's risks
The hypothalamus is a thumb-sized, central area on the underside of the brain that controls endocrine and autonomic functions, such as ovulation, lactation, stress responses, body temperature and energy balance.
The hypothalamus "controls all autonomic functions and maintains homeostasis — eating, drinking, sex behavior, maternal and even paternal behavior," Kelly said.
"At least at the basic level, existing SERMs do not seem to help.
http://www.eurekalert.org/pub_releases/2003-12/ohs-otd123003.php   (811 words)

  
 [No title]
Correlations observed in the prior art are not believed to suggest treatment or prophylactic methods that are effective, or as free of undesirable side-effects, as are combination therapies disclosed here.
It should be mentioned that the serum lipid profile is markedly different between rats and humans.
Importantly, the combination of EM-800 and DHEA in ovariectomized rats treated for 12 months has beneficial effects on bone morphometry.
http://www.wipo.int/cgi-pct/guest/getbykey5?KEY=99/63974.991216&ELEMENT_SET=DECL   (7739 words)

  
 NEJM -- Selective Estrogen-Receptor Modulators -- Mechanisms of Action and Application to Clinical Practice
Selective Estrogen-Receptor Modulators — Mechanisms of Action and Application to Clinical Practice
NEJM -- Selective Estrogen-Receptor Modulators -- Mechanisms of Action and Application to Clinical Practice
Brass, L. Hormone Replacement Therapy and Stroke: Clinical Trials Review.
http://content.nejm.org/cgi/content/short/348/7/618?query=TOC   (951 words)

  
 MedlinePlus Drug Information: Raloxifene (Systemic)
Raloxifene (ral-OX-i-feen) is used to help prevent and treat thinning of the bones (osteoporosis) only in postmenopausal women.
If you experience vaginal bleeding, breast pain or enlargement, or swelling of hands or feet while on raloxifene, you should report it to your doctor.
Also, raloxifene does not stimulate the breast or uterus as estrogen does.
http://www.nlm.nih.gov/medlineplus/druginfo/uspdi/203396.html   (1328 words)

  
 Triphenylalkene derivatives and their use as selective estrogen receptor modulators - Patent 6875775
Terenius L: Structure-activity relationship of anti-oestrogens with regard to interaction with 17.beta.-oestradiol in the mouse uterus and vagina.
Therefore the examples above should be understood as examples of the usefulness in different conditions.
The new SERMs of the present invention thus have tissue-specific estrogenic and/or antiestrogenic effects in vitro and in vivo and are useful in the prevention and treatment of osteoporosis, cardiovascular diseases and Alzheimer's disease in men and women, as well as in the treatment of climacteric symptoms and breast cancer in women.
http://www.freepatentsonline.com/6875775.html   (14067 words)

  
 Raloxifene: A Selective Estrogen Receptor Modulator (SERM) with Multiple Target System Effects -- Muchmore 5 (5): 388 ...
Heart and Estrogen/progestin Replacement Study (HERS) Research Group.
In human studies, raloxifene does not cause any increase
supports the hypothesis that these SERMs reduce the incidence
http://theoncologist.alphamedpress.org/cgi/content/full/5/5/388   (2437 words)

  
 Selective estrogen receptor modulator - Wikipedia, the free encyclopedia
Selective estrogen-receptor modulators - mechanisms of action and application to clinical practice.
Although the SERMs have no immediate structural relationship with 17β-estradiol, they are stereochemically similar to this estrogen.
Some SERMs, through this process, also augment the transcription of coactivator molecules, which may be indispensable for their pharmacological action.
http://en.wikipedia.org/wiki/Selective_estrogen_receptor_modulator   (388 words)

  
 Idoxifene: A Novel Selective Estrogen Receptor Modulator Prevents Bone Loss and Lowers Cholesterol Levels in ...
This suggests that 1) the effects of idoxifene are mediated
A separate study was done in which groups of 9–10 rats
and therefore behaving as an estrogen agonist in osteoblasts.
http://endo.endojournals.org/cgi/content/full/139/12/5224   (6534 words)

  
 Estren Is a Selective Estrogen Receptor Modulator with Transcriptional Activity -- Movérare et al. 64 (6): 1428 ...
Riggs BL and Hartmann LC (2003) Selective estrogen-receptor modulators—mechanisms of action and application to clinical practice.
Estrogen replacement therapy is beneficial for the treatment
The response values for each concentration of ligand are the means of triplicate determinations with the means ± S.D. for each value indicated.
http://molpharm.aspetjournals.org/cgi/content/full/64/6/1428   (3364 words)

  
 Is Black Cohosh a Selective Estrogen Receptor Modulator
A rat and mouse study presented in 1996 in Maturitas was apparently one of the first indicators that BC may have SERM activities.
SERM is a relatively new concept in the spectrum of women’s healthcare.
The drug is currently being marketed heavily to postmenopausal women as an alternative to hormone replacement therapy (HRT) for prevention and treatment of osteoporosis.
http://www.herbalgram.org/tomsofmaine/herbalgram/articleview.asp?a=2638   (2126 words)

  
 Drug Mini-Monograph: Selective estrogen receptor modulators (SERMs) in the prevention and treatment of osteoporosis
The authors, editors, developers, testers, and the University of Washington School of Medicine are not responsible for any errors in diagnosis or treatment that may result from the use of this material.
Tamoxifen, a SERM used in the prevention and treatment of breast cancer, weakly increases bone mineral density to a much lesser degree and is not used for treatment or prevention of osteoporosis.
For more information on the use of SERMs in the prevention and treatment of osteoporosis, work through the SERM case
http://www.osteoed.org/faq/drug_therapy/serms.html   (336 words)

  
 Cancer Issues - Existing Drugs May Protect Against Certain Cancers
The apparent protective effect of raloxifene was most pronounced during the first three years of use, said lead investigator Dr. Angela DeMichele, an assistant professor of medicine at the Abramson Cancer Center and Center for Clinical Epidemiology and Biostatistics at the University of Pennsylvania.
Yet a third study, this one a new analysis of patients taking the breast cancer drugs raloxifene and tamoxifen, found raloxifene may reduce the risk of endometrial cancer -- cancer of the uterine lining -- by 50 percent.
For example, the hormone drug toremifene (brand name Acapodene) reduced the risk of developing prostate cancer by nearly half in men at high risk for the disease.
http://www.cancerissues.com/ms/news/525733/main.html   (850 words)

  
 jPT: the journal of Pharmacy Technology: Volume 15 Abstracts
STUDY SELECTION: Literature was reviewed to evaluate the pharmacology, pharmacokinetics, therapeutic use, adverse effects, and drug interactions of raloxifene.
CONCLUSIONS: Clinical trials have found that raloxifene is effective in the prevention of osteoporosis, making the drug an alternative choice for the prevention of osteoporosis in patients who are concerned about the proliferative effects of estrogen replacement therapy on the endometrium or breast tissue.
As a result of binding to estrogen receptors, raloxifene therapy, like estrogen treatment, causes positive changes in biochemical markers of bone turnover such as serum osteocalcin, serum alkaline phosphatase, urinary pyridinoline cross-links, and urinary calcium excretion.
http://www.jpharmtechnol.com/abstracts/volume15/March-April/37.html   (307 words)

  
 INTRODUCTION TO MEDICAL PHARMACOLOGY
Tolerance can be reduced by which therapeutic regimen?
For questions concerning content, please email Dr. Carol Walsh
4. An antagonist at the androgen receptor that is used for palliative treatment of prostatic cancer.
http://www.bumc.bu.edu/www/busm/pharmacology/imp/final-98.html   (1838 words)

  
 Patent 6,352,970
This invention also relates to methods for treating bone fracture, enhancing bone healing following facial reconstruction, maxillary reconstruction or madibular reconstruction, enhancing long bone extension, enhancing the healing rate of a bone graft, enhancing prosthetic growth and inducing vertebral synostosis by administering a therapeutically effective amount of leptin or a leptin mimetic.
This invention further relates to methods and compositions comprising leptin or a leptin mimetic and estrogen, a selective estrogen receptor modulator or a bisphonate for treating the above-recited diseases and conditions.
A method for augmenting bone mass and preventing bone loss in a mammal in need thereof comprising administering to said mammal a therapeutically effective amount of a combination of 1) leptin, a fragment thereof or a leptin mimetic, and 2) estrogen.
http://www.pharmcast.com/Patents/Yr2002/Mar2002/030502/6352970_Skeletal030502.htm   (842 words)

  
 UIC College of Pharmacy: department of biopharmaceutical sciences
In the treatment setting, this drug is highly effective; the eventual resistance to tamoxifen limits its use, however.
Tamoxifen is a selective estrogen receptor modulator (SERM) used for the treatment of estrogen receptor positive breast cancers and is approved as a preventive therapy for women at high risk for developing the disease.
Estrogen is known to be essential in the initiation and development of most breast cancers.
http://www.uic.edu/pharmacy/depts/pmpcpd/faculty/tonetti.html   (610 words)

  
 Selective Estrogen Receptor Modulator Effects on Serum Lipoproteins and Vascular Function in Postmenopausal Women and ...
and basic laboratory research suggest that estrogen therapy
Estrogen has a multitude of biological effects that may
Selective Estrogen Receptor Modulator Effects on Serum Lipoproteins and Vascular Function in Postmenopausal Women and in Hypercholesterolemic Men -- BLUM and CANNON 949 (1): 168 -- Annals of the New York Academy of Sciences
http://www.annalsnyas.org/cgi/content/abstract/949/1/168   (275 words)

  
 Fareston®- Glossary
A term meaning that the cancer has spread from its place of origination to other parts of the body.
Estrogen may stimulate the growth of certain cancers.
A type of therapy that interferes with the actions of hormones, such as estrogen, that support cancer-cell growth.
http://www.fareston.com/b_about/b6.html   (202 words)

  
 Osteoporosis: Study finds phyto selective estrogen receptor modulator increases BMD, August 14, 2004
The study was published by Israel Yoles, MD, of the Sheba Medical Center, Tel Hashomer, Israel, and colleagues in the Journal of Clinical and Experimental Obstetrics and Gynecology (2004;31(2):123-126).
The company claims this is good news for menopausal women looking for nonmedical relief following on the heels of the recent Journal of the American Medical Associaiton report (July 7, 2004), which concluded that soy protein containing isoflavone was not effective in improving BMD, cognitive function, or plasma lipids in healthy postmenopausal women.
OBGYN.net has been selected as a featured site in Lightspan's StudyWeb as one of the best educational resources on the Web.
http://www.obgyn.net/newsheadlines/womens_health-Osteoporosis-20040814-122.asp   (587 words)

  
 Arzoxifene: A Promising New Selective Estrogen Receptor Modulator for Clinical Chemoprevention of Breast Cancer: ...
Therefore, it is not surprising that there has been intense
Hobson’s choice and the need for combinations of new agents for the prevention and treatment of breast cancer.
which estrogen exerts beneficial effects, such as bone and the
http://clincancerres.aacrjournals.org/cgi/content/full/10/16/5313   (2024 words)

  
 Selective Estrogen Receptor Modulators: Clinical Spectrum -- Cosman and Lindsay 20 (3): 418 -- Endocrine Reviews
Selective Androgen Receptor Modulators (SARMs): A Novel Approach to Androgen Therapy for the New Millennium
Estrogen and Tamoxifen Interplay with T3 in Male Rats: Pharmacologically Distinct Classes of Estrogen Responses Affecting Growth, Bone, and Lipid Metabolism, and Their Relation to Serum GH and IGF-I
Estrogenic and Antiproliferative Properties of Glabridin from Licorice in Human Breast Cancer Cells
http://edrv.endojournals.org/cgi/content/abstract/20/3/418   (914 words)

  
 NAMS: Novel Selective Estrogen Receptor Modulator Has Beneficial Effects on Bone Turnover, Cardiovascular Markers
Whether it will offer any advantage (for example, in the treatment of vaginal atrophy) must await larger trials, Dr. Ylikorkala said.
These results suggest some degree of estrogenic activity, especially in the vagina.
There was also an increase in the frequency of superficial cells in the Pap smear, from 3 percent to 14 percent at the highest dose (p < 0.01).
http://www.docguide.com/dg.nsf/PrintPrint/98E033FEB9BD0F6585256C4B006AA776   (469 words)

  
 Evista Drug Description - Raloxifene - HealthScout
To find more information on specific conditions, please visit our partner sites:
EVISTA (raloxifene hydrochloride) is a selective estrogen receptor modulator (SERM) that belongs to the benzothiophene class of compounds.
http://www.healthscout.com/rxdetail/1/45/1/main.html   (162 words)

  
 The effect of a selective estrogen receptor modulator on the progression of spontaneous autoimmune disease in MRL ...
These studies demonstrate that SERMs may be potentially useful for the treatment of autoimmune disorders.
The state of the art may have changed since the publication date.
Finally, flow cytometric analysis documented that thymuses from animals treated for 7 months with LY139478 but not with EE2 contained predominantly CD4+/CD+ T cells consistent with a normal thymic phenotype observed in non-MRL lpr/lpr mouse strains.
http://www.aegis.com/aidsline/1997/feb/M9721073.html   (533 words)

  
 Category:Selective estrogen receptor modulators - Wikipedia, the free encyclopedia
Their use is in infertility, osteoporosis and menopause symptoms.
Selective estrogen receptor modulators have varying effects on different isoforms of the estrogen receptor.
http://en.wikipedia.org/wiki/Category:Selective_estrogen_receptor_modulators   (78 words)

  
 Hexapedia - Tamoxifen
Tamoxifen is an oral selective estrogen receptor modulator which is used in breast cancer, and is currently the world's largest selling breast cancer treatment.
http://www.hexafind.com/encyclopedia/tamoxifen   (168 words)

  
 SELECTIVE ESTROGEN RECEPTOR MODULATOR
Also referred to as selective estrogen receptor modulators (SERM), this relatively new class of drugs is used in the treatment of osteoporosis (and in one case breast cancer).
Physiologically, this leads to a reduction in the resorption of bone and a decrease in overall bone turnover.
The SERMs exert their effect by binding to estrogen receptors on cells.
http://www.medhelp.org/glossary2/new/GLS_4150.HTM   (92 words)

  
 Selective Estrogen-Receptor Modulator (SERM) definition - Medical Dictionary definitions of popular medical terms
Selective Estrogen-Receptor Modulator (SERM) definition - Medical Dictionary definitions of popular medical terms
For example, raloxifene (trade name EVISTA) is classified as a SERM because it prevents bone loss (like estrogen) and lowers serum cholesterol (like estrogen) but (unlike estrogen) does not stimulate the endometrial lining of the uterus.
Please consult your healthcare provider before beginning any course of supplementation or treatment.
http://www.medterms.com/script/main/art.asp?articlekey=5444   (235 words)

  
 Imaginis - Ductal Carcinoma in Situ (DCIS)
Presently, there are no drug therapies approved by the FDA to treat DCIS.
Tamoxifen is an "anti-estrogen" and works by competing with estrogen to bind to estrogen receptors in breast cancer cells.
By blocking estrogen in the breast, tamoxifen helps slow the growth and reproduction of breast cancer cells.
http://www.imaginis.com/breasthealth/dcis.asp   (2419 words)

  
 A Phase II Clinical Trial of a Selective Estrogen Receptor Modulator (LY353381HCl) in High Risk Women with Fine Needle ...
A Phase II Clinical Trial of a Selective Estrogen Receptor Modulator (LY353381HCl) in High Risk Women with Fine Needle Aspirat
A Phase II Clinical Trial of a Selective Estrogen Receptor Modulator (LY353381HCl) in High Risk Women with Fine Needle Aspiration Cytologic Evidence of Hyperplasia
http://www2.kumc.edu/kci/protocols/sermhyper.html   (90 words)

  
 Altered pharmacology and distinct coactivator usage for estrogen receptor-dependent transcription through activating ...
Estrogen signaling occurs through at least two distinct molecular
Coregulators in Nuclear Estrogen Receptor Action: From Concept to Therapeutic Targeting
pathways: (i) direct binding of liganded estrogen receptors
http://www.pnas.org/cgi/content/abstract/102/3/559   (449 words)

  
 Information on the herb black cohosh.
It is a spasmolytic, vasodilatory and hypotensive and is used with success in controlling menopausal symptoms - especially hot flushes.
It has estrogen-like activity due to the isoflavonoids and triterpenoids and acts as a selective estrogen-receptor modulator and may suppress the activity of luteinizing hormone.
http://www.ageless.co.za/herb-black-cohosh.htm   (645 words)

  
 Phytomedicine: International Journal of Phytotherapy & Phytopharmacology: Belamcanda chinensis and the thereof purified ...
Belamcanda chinensis (BC) belongs to the family of iridaceae and the isoflavone tectorigenin has been isolated from the rhizome of this plant.
Therefore, we performed binding studies with recombinant human ER[alpha] and ER[beta] to show that tectorigenin binds to both receptor subtypes.
Whether this isoflavone has estrogenic, possibly selective estrogen receptor modulator activities and if so, whether they are mediated via the estrogen receptor [alpha] or [beta] is unknown at present.
http://www.highbeam.com/library/doc0.asp?DOCID=1G1:122454606&refid=holomed_1   (239 words)

  
 Distinct mechanisms of action of selective estrogen receptor modulators in breast and osteoblastic cells -- Nuttall et ...
difference in this mechanism via the estrogen response element
Although these SERMs exhibit a similar antagonist activity profile
This article has been cited by other articles:
http://ajpcell.physiology.org/cgi/content/abstract/279/5/C1550   (267 words)

  
 Impact of the selective estrogen receptor modulator, tamoxifen, on neuronal outgrowth and survival following toxic ...
Low concentrations of TMX or OHT were without effect on a marker of neuronal viability, basal release of lactate dehydrogenase (LDH), whereas high concentrations of both SERMs (2500 ng/ml) induced a significant increase in LDH, indicating the potential toxicity of both SERMs at high concentrations.
Impact of the selective estrogen receptor modulator, tamoxifen, on neuronal outgrowth and survival following toxic insults associated with aging and Alzheimer's disease.
We investigated the estrogen agonist/antagonist properties of the selective estrogen receptor modulators (SERMs), tamoxifen (TMX) and 4-hydroxy-tamoxifen (OHT), using an in vitro neuron model system to determine the impact of the neuroprotective and neurotrophic properties of these SERMs.
http://www.arclab.org/medlineupdates/abstract_15246826.html   (165 words)

  
 Bazedoxifene Acetate: A Selective Estrogen Receptor Modulator with Improved Selectivity -- Komm et al. 146 (9): 3999 -- ...
receptors and promote increased bone mineral density and bone
for less uterine and vasomotor effects than selective estrogen
Bazedoxifene Acetate: A Selective Estrogen Receptor Modulator with Improved Selectivity -- Komm et al.
http://endo.endojournals.org/cgi/content/abstract/146/9/3999   (252 words)

  
 LY353381.HCl, a Selective Estrogen Receptor Modulator, and Experimental Stroke Editorial Comment -- Rossberg et al. 31 ...
LY353381.HCl, a Selective Estrogen Receptor Modulator, and Experimental Stroke Editorial Comment -- Rossberg et al.
http://stroke.ahajournals.org/cgi/reprint/31/12/3041   (15 words)

  
 Arch Surg -- Abstract: Inhibition of Intimal Hyperplasia Using the Selective Estrogen Receptor Modulator Raloxifene, ...
From the Division of Cardiothoracic Surgery, Department of Surgery, University of Colorado Health Sciences Center, Denver (Drs Selzman, Miller, and Harken) and the College of Veterinary Medicine, Colorado State University, Fort Collins (Drs Turner, Gaynor, and Monnet).
Arch Surg -- Abstract: Inhibition of Intimal Hyperplasia Using the Selective Estrogen Receptor Modulator Raloxifene, March 2002, Selzman et al.
Inhibition of Intimal Hyperplasia Using the Selective Estrogen Receptor Modulator Raloxifene
http://archsurg.ama-assn.org/cgi/content/abstract/137/3/333   (138 words)

  
 Effects of the Selective Estrogen Receptor Modulator, Raloxifene, on the Somatotropic Axis and Insulin-Glucose ...
In addition to direct effects on bone cells, estrogen and raloxifene
Address all correspondence and requests for reprints to: Paul Lips, M.D., Department of Endocrinology, Academic Hospital, Vrije Universiteit, P.O. Box 7057, 1007 MB Amsterdam, The Netherlands.
Comparison of the Metabolic Effects of Raloxifene and Oral Estrogen in Postmenopausal and Growth Hormone-Deficient Women
http://jcem.endojournals.org/cgi/content/abstract/86/6/2763   (746 words)

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