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L Del Pup
OBJECTIVE: Vaginal atrophy is a chronic, progressive medical condition that affects fifty percent of postmenopausal women, causing symptoms like dyspareunia, vaginal dryness, and vaginal irritation. Until recently, the only prescription options were systemic and vaginal estrogen therapies that might be limited by concerns about long-term safety and breast cancer risk. The objective is to analyze the literature about ospemifene, a tissue-selective estrogen receptor modulator (SERM) recently approved for the treatment of vulvovaginal atrophy and dyspareunia and to compare its effects with those of the other SERMs to assess its safety...
September 2016: European Review for Medical and Pharmacological Sciences
Sermed Mezher, Mariam Rahm, Sunanda Sudarsanan, Surendran Chandrasekaran
No abstract text is available yet for this article.
2016: Global Pediatric Health
Tatiana Traboulsi, Mohamed El Ezzy, James Gleason, Sylvie Mader
About 70% of breast tumors express estrogen receptor alpha (ERα), which mediates the proliferative effects of estrogens on breast epithelial cells, and are candidates for treatment with antiestrogens, steroidal or non-steroidal molecules designed to compete with estrogens and antagonize ERs. The variable patterns of activity of antiestrogens (AEs) in estrogen target tissues and the lack of systematic cross-resistance between different types of molecules have provided evidence for different mechanisms of action...
October 11, 2016: Journal of Molecular Endocrinology
Jaime Stella Moses Richardson, Gautam Sethi, Guan Serm Lee, Sri Nurestri Abdul Malek
BACKGROUND: Cancer has been one of the leading causes of mortality in this era. Ruta angustifolia L. Pers has been traditionally used as an abortifacient, antihelmintic, emmenagogue and ophthalmic. In Malaysia and Singapore, the local Chinese community used it for the treatment of cancer. METHODS: In this study, the methanol and fractionated extracts (hexane, chloroform, ethyl acetate and water) of R. angustifolia were tested for its cytotoxicity using the sulforhodamide (SRB) cytotoxicity assay against HCT-116, A549, Ca Ski and MRC5 cell lines...
October 12, 2016: BMC Complementary and Alternative Medicine
Julia Hamer, Rachel McDonald, Liying Zhang, Sunil Verma, Angela Leahey, Christine Ecclestone, Gillian Bedard, Natalie Pulenzas, Anchal Bhatia, Ronald Chow, Carlo DeAngelis, Janet Ellis, Eileen Rakovitch, Justin Lee, Edward Chow
PURPOSE: The purpose of this study was to determine the quality of life (QOL) and symptom burden (SB) among breast cancer patients. METHODS: Patients with DCIS, early stage, locally advanced, or metastatic breast cancer completed the Edmonton Symptom Assessment System (ESAS) and the Functional Assessment of Cancer Therapy for Breast Cancer (FACT-B). Patients were divided into subsequent cohorts based on their last day of treatment, age at enrollment, radiation, chemotherapy, and hormone therapy...
September 30, 2016: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
Agnieszka Bratek, Krzysztof Krysta, Karolina Drzyzga, Justyna Barańska, Krzysztof Kucia
BACKGROUND: Gender differences in schizophrenia have been recognized for a long time and it has been widely accepted that sex steroid hormones, especially estradiol, are strongly attributed to this fact. Two hypotheses regarding estradiol action in psychoses gained special research attention - the estrogen protection hypothesis and hypoestrogenism hypothesis. A growing number of studies have shown benefits in augmenting antipsychotic treatment with estrogens or selective estrogen receptor modulators (SERM)...
September 2016: Psychiatria Danubina
Alka Kriplani, Astha Srivastava, Vidushi Kulshrestha, Garima Kachhawa, Nutan Agarwal, Neerja Bhatla, Smriti Hari
AIM: To compare ormeloxifene with combined oral contraceptive (COC) in abnormal uterine bleeding (AUB) due to leiomyoma (AUB-L). METHODS: Fifty women with AUB-L were randomized after informed consent and institute ethics clearance. Group I (n = 25) was given ormeloxifene (a SERM i.e. selective estrogen receptor modulator) 60 mg twice per week and group II (n = 25) was given COC (ethinyl estradiol 30 μg with desogestrel 150 μg) on days 1-21 for 6 months...
September 20, 2016: Journal of Obstetrics and Gynaecology Research
Li-Ming Zhao, Hai-Shan Jin, Jinzhong Liu, Todd C Skaar, Joseph Ipe, Wei Lv, David A Flockhart, Mark Cushman
The design and synthesis of dual aromatase inhibitors/selective estrogen receptor modulators (AI/SERMs) is an attractive strategy for the discovery of new breast cancer therapeutic agents. Previous efforts led to the preparation of norendoxifen (4) derivatives with dual aromatase inhibitory activity and estrogen receptor binding activity. In the present study, some of the structural features of the potent AI letrozole were incorporated into the lead compound (norendoxifen) to afford a series of new dual AI/SERM agents based on a symmetrical diphenylmethylene substructure that eliminates the problem of E,Z isomerization encountered with norendoxifen-based AI/SERMs...
November 1, 2016: Bioorganic & Medicinal Chemistry
Andrée-Anne Poirier, Mélissa Côté, Mélanie Bourque, Marc Morissette, Thérèse Di Paolo, Denis Soulet
Motor symptoms in Parkinson's disease (PD) are often preceded by nonmotor symptoms related to dysfunctions of the autonomic nervous system such as constipation, defecatory problems, and delayed gastric emptying. These gastrointestinal impairments are associated with the alteration of dopaminergic (DAergic) neurons in the myenteric plexus of the gut. Recently, we demonstrated the anti-inflammatory properties of estrogens to treat intestinal neurodegeneration in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) mouse model of PD...
August 16, 2016: Neurobiology of Aging
Nuri Peker, Savas Gundogan, Fatih Sendag
To present the feasibility of laparoscopic management of huge myoma nascendi DESIGN: Step by step explanation of the surgery using video SETTING: Uterine fibroids are the most common benign neoplasm of the female reproductive tract with the estimated incidence of 25-30% at reproductive age. Patients generally have no symptoms however patients those have symptoms such as severe pelvic pain, heavy uterine bleeding or infertility may undergo surgery. The traditional management is surgery however uterine artery embolization, hormonal therapy using GnRH (Gonadotropin-Releasing Hormone) agonists or SERM (Selective Estrogen Receptor Modulator) should be preferred as the medical approach...
September 12, 2016: Journal of Minimally Invasive Gynecology
Nuri Peker, Savaş Gundogan, Fatih Şendağ
To present the feasibility of laparoscopic management of huge cervical myoma DESIGN: Step by step explanation of the surgery using video SETTING: Uterine fibroids are the most common benign neoplasm of the female reproductive tract with the estimated incidence of 25-30% at reproductive age. Patients generally have no symptoms however patients those have symptoms such as severe pelvic pain, heavy uterine bleeding or infertility may undergo surgery. The traditional management is surgery however uterine artery embolization, hormonal therapy using GnRH (Gonadotropin-Releasing Hormone) agonists or SERM (Selective Estrogen Receptor Modulator) should be preferred as the medical approach...
September 12, 2016: Journal of Minimally Invasive Gynecology
Susan Hum, Melinda Wu, Sandhya Pruthi, Ruth Heisey
The uptake of selective estrogen receptor modulators (SERMs) and aromatase inhibitors (AIs) for the primary prevention of breast cancer is low, despite their proven efficacy in several randomized clinical trials. This review summarizes the latest data on physicians' and women's barriers to breast cancer preventive therapy. Physicians' challenges include: identifying suitable candidates for preventive therapy, inadequate training and confidence in risk assessment and counselling, insufficient knowledge of risk-reducing medications, and lack of time...
2016: Current Breast Cancer Reports
Amarnath Rambhatla, Jesse N Mills, Jacob Rajfer
Estradiol, normally considered a female hormone, appears to play a significant role in men in a variety of physiologic functions, such as bone metabolism, cardiovascular health, and testicular function. As such, estradiol has been targeted by male reproductive and sexual medicine specialists to help treat conditions such as infertility and hypogonadism. The compounds that modulate estradiol levels in these clinical conditions are referred to as selective estrogen receptor modulators (SERMs) and aromatase inhibitors (AIs)...
2016: Reviews in Urology
María E Fernández-Suárez, Joan C Escolà-Gil, Oscar Pastor, Alberto Dávalos, Francisco Blanco-Vaca, Miguel A Lasunción, Javier Martínez-Botas, Diego Gómez-Coronado
Selective estrogen receptor modulators (SERMs) are widely prescribed drugs that alter cellular and whole-body cholesterol homeostasis. Here we evaluate the effect of SERMs on the macrophage-specific reverse cholesterol transport (M-RCT) pathway, which is mediated by HDL. Treatment of human and mouse macrophages with tamoxifen, raloxifene or toremifene induced the accumulation of cytoplasmic vesicles of acetyl-LDL-derived free cholesterol. The SERMs impaired cholesterol efflux to apolipoprotein A-I and HDL, and lowered ABCA1 and ABCG1 expression...
2016: Scientific Reports
Timothy K O'Rourke, Matthew S Wosnitzer
Opioid-induced androgen deficiency (OPIAD) was initially recognized as a possible consequence of opioid use roughly four decades ago. Long-acting opioid use carries risks of addiction, tolerance, and systemic side effects including hypogonadotropic hypogonadism with consequent testosterone depletion leading to multiple central and peripheral effects. Hypogonadism is induced through direct inhibitory action of opioids on receptors within the hypothalamic-pituitary-gonadal (HPG) and hypothalamic-pituitary-adrenal (HPA) axes as well as testosterone production within the testes...
October 2016: Current Urology Reports
Sarah Mikelman, Natalie Mardirossian, Margaret E Gnegy
Although best known as a selective estrogen receptor modulator (SERM), tamoxifen is a drug with a wide range of activities. Tamoxifen has demonstrated some efficacy has a therapeutic for bipolar mania and is believed to exert these effects through inhibition of protein kinase C (PKC). As the symptoms of amphetamine treatment in rodents are believed to mimic the symptoms of a manic episode, many of the preclinical studies for this indication have demonstrated that tamoxifen inhibits amphetamine action. The amphetamine-induced increase in extracellular dopamine which gives rise to the 'manic' effects is due to interaction of amphetamine with the dopamine transporter...
August 30, 2016: Journal of Chemical Neuroanatomy
Nicoletta Provinciali, Chen Suen, Barbara K Dunn, Andrea DeCensi
INTRODUCTION: Raloxifene is an estrogen receptor modulator which competes with estrogens for binding to the estrogen receptor . Based on the results of the STAR (Study of Tamoxifen And Raloxifene) trial, raloxifene has been approved by the U.S. Food and Drug Administration for the reduction of breast cancer (BC) risk in postmenopausal women at increased risk. AREAS COVERED: This analysis reviews the activity of raloxifene and the clinical trials for non-BC indications which led to investigate its use as BC preventive agent...
September 1, 2016: Expert Review of Clinical Pharmacology
Arti Yadav, Bhavna Kumar, Theodoros N Teknos, Pawan Kumar
Recent studies have shown that IL-6 signaling plays an important role in the aggressive and metastatic phenotype of head and neck squamous cell carcinoma (HNSCC). Therefore, we hypothesized that targeting of IL-6 signaling in HNSCC could enhance the therapeutic efficacy of standard chemoradiation treatment. We used both in vitro and in vivo models to test the efficacy of Bazedoxifene (BZA), a drug that was originally developed as a newer-generation selective estrogen receptor modulator (SERM) for the treatment of postmenopausal osteoporosis...
August 22, 2016: Oncotarget
Kentaro Nakai
Selective estrogen receptor modulators(SERMs)have beneficial effects on the improvement of bone mineral density of the spine and hip, and decrease the vertebral fracture in postmenopausal women. Similar to patients with advanced chronic kidney disease, including dialysis patients, however, SERMs cannot decrease the risk of hip fracture, which is extremely high in Japanese dialysis patients. One of the most important disadvantages of SERMs is an increase in the risk of venous thromboembolic events and fatal stroke in high-risk groups of the Framingham Stroke Risk Score...
September 2016: Clinical Calcium
Ki-Chan An
Selective estrogen receptor modulators (SERMs) are now being used as a treatment for breast cancer, osteoporosis and postmenopausal symptoms, as these drugs have features that can act as an estrogen agonist and an antagonist, depending on the target tissue. After tamoxifen, raloxifene, lasofoxifene and bazedoxifene SERMs have been developed and used for treatment. The clinically decisive difference among these drugs (i.e., the key difference) is their endometrial safety. Compared to bisphosphonate drug formulations for osteoporosis, SERMs are to be used primarily in postmenopausal women of younger age and are particularly recommended if there is a family history of invasive breast cancer, as their use greatly reduces the incidence of this type of cancer in women...
August 2016: Asian Spine Journal
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