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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
Chiara Bondi, Simone Ferrero, Carolina Scala, Emanuela Tafi, Annalisa Racca, Pier Luigi Venturini, Umberto Leone Roberti Maggiore
INTRODUCTION: Ospemifene is a selective estrogen receptor modulator recently approved by the FDA for the treatment postmenopausal women experiencing moderate-to-severe dyspareunia and by the EMA for the treatment of moderate-to-severe symptomatic genitourinary syndrome of menopause (GSM) in women who are not suitable candidates for local vaginal estrogen therapy. AREAS COVERED: This review offers an explanation of the pharmacodynamics and of the pharmacokinetics of ospemifene, and gives readers a complete overview of Phase II and III studies on the clinical efficacy, tolerability and safety of this agent in the setting of GSM...
October 2016: Expert Opinion on Drug Metabolism & Toxicology
Ginger D Constantine, David F Archer, Ricki Pollycove, Wei Jiang, Corrado Altomare, JoAnn V Pinkerton
OBJECTIVE: To examine the effect of ospemifene 60 mg/d on vasomotor symptoms in postmenopausal women using clinical safety and efficacy data from five phase 2 and 3 studies. METHODS: The incidence of hot flush treatment-emergent adverse events (TEAEs) was compiled from five randomized, placebo-controlled clinical studies; baseline parameters associated with hot flush incidence were also identified. Ospemifene's effects on the frequency and severity of hot flushes were evaluated in a previously unpublished, 6-week, placebo-controlled study...
September 2016: Menopause: the Journal of the North American Menopause Society
Andrew T Goldstein, Michelle A King
INTRODUCTION: Ospemifene (Osphena, Shionogi Inc, Florham, NJ, USA) is an estrogen agonist and antagonist approved by the U.S. Federal Drug Administration for the treatment of "moderate to severe dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause." Although published, peer-reviewed, placebo-controlled studies have shown objective improvement in dyspareunia and in vaginal atrophy, there are no published data that have assessed changes in vulvar atrophy after the use of ospemifene...
September 2016: Sexual Medicine
James H Pickar
No abstract text is available yet for this article.
July 2016: Menopause: the Journal of the North American Menopause Society
Natalija Eigeliene, Lauri Kangas, Christina Hellmer, Tommi Kauko, Risto Erkkola, Pirkko Härkönen
OBJECTIVE: Ospemifene (Osp) is a novel selective estrogen-receptor modulator (SERM) accepted for the treatment of dyspareunia, a symptom of postmenopausal vulvovaginal atrophy. We aimed to analyze the effects of Osp on human breast tissue (HBT), in comparison with the clinically established SERMs raloxifene (Ral) and tamoxifen (Tam), using ex vivo explant cultures. METHODS: HBT samples were obtained from postmenopausal women undergoing mammoplasty and cultured with or without Osp, Ral, Tam, or 17β-estradiol (E2) for 7 and 14 days, and studied for morphology, proliferation, and apoptosis...
July 2016: Menopause: the Journal of the North American Menopause Society
Ginger D Constantine, Risa Kagan, Paul D Miller
OBJECTIVE: Ospemifene is an estrogen-receptor agonist/antagonist (also known as a selective estrogen-receptor modulator) that is FDA approved for the treatment of moderate-to-severe dyspareunia, a symptom of vulvovaginal atrophy, due to menopause. Preclinical and clinical data suggest that ospemifene may also have an effect on bone health in postmenopausal women. METHODS: Relevant articles, including cellular and preclinical studies and clinical trials written in English pertaining to ospemifene and bone health, were identified from a database search of PubMed (from its inception to June 2015) and summarized in this comprehensive review...
June 2016: Menopause: the Journal of the North American Menopause Society
Gurleen Kaur, Mohinder P Mahajan, Manoj K Pandey, Parvesh Singh, Srinivasa R Ramisetti, Arun K Sharma
The synthesis of novel triarylethylene analogs, designed based on well-known Selective Estrogen Receptor Modulators (SERMs), i.e., ospemifene and tamoxifen, as potential anti-breast cancer agents is described. The cytotoxic potential of these analogs against ER-positive (MCF-7) and ER-negative (MDA-MB-231) human breast cancer cell lines was determined and compared with the standards, ospemifene and tamoxifen. In initial screening, analogs 5, 14 and 15 were found to be much more effective than the standards against both the cell lines...
April 15, 2016: Bioorganic & Medicinal Chemistry Letters
Nanette Santoro, Roisin Worsley, Karen K Miller, Sharon J Parish, Susan R Davis
INTRODUCTION: Sex steroids are important in female sexual function and dysfunction. AIM: To review the role of estrogens in the physiology and pathophysiology of female sexual functioning and the evidence for efficacy of estrogen therapy for female sexual dysfunction to update the previously published International Society of Sexual Medicine Consensus on this topic. METHODS: Panel members reviewed the published literature using online databases for studies pertaining to estrogen in female sexual function and dysfunction...
March 2016: Journal of Sexual Medicine
JoAnn V Pinkerton, Risa Kagan
INTRODUCTION: Vulvar vaginal atrophy (VVA), a component of genitourinary syndrome of menopause, is a chronic, progressive medical condition that results from estrogen deficiency at menopause. Ospemifene is a nonhormonal, estrogen receptor agonist/antagonist (ERAA) FDA-approved for the treatment of moderate to severe dyspareunia, a symptom of VVA, due to menopause. AREAS COVERED: PubMed was searched from inception to March 2015 with keywords ospemifene and vulvar vaginal atrophy; no other similar clinical reviews were found...
2015: Expert Opinion on Pharmacotherapy
Natalija Eigeliene, Risto Erkkola, Pirkko Härkönen
Explant tissue culture provides a model for studying the direct effects of steroid hormones, their analogs, and novel hormonally active compounds on normal freshly isolated human breast tissues (HBTs). For this purpose, pre- and postmenopausal HBTs can be maintained in this culture system. The results demonstrate that the morphological integrity of HBT explants can be maintained in tissue culture up to 2 weeks and expression of differentiation markers, steroid hormone receptors, proliferation and apoptosis ratios can be evaluated as a response to hormonal stimulation...
2016: Methods in Molecular Biology
Jouko Uusitalo, Miia Turpeinen, Ari Tolonen, Pasi Koskimies, Risto Lammintausta, Olavi Pelkonen
BACKGROUND: Metabolite profiles of ospemifene, a novel nonsteroidal selective estrogen receptor modulator, were surveyed as part of its development. METHODS: The pharmacokinetics of ospemifene and its two major, pharmacologically active metabolites 4-hydroxyospemifene and 4'-hydroxyospemifene, was elucidated in studies of volunteer humans given various doses of ospemifene and in experiments of several animal species (rat, mouse, dog, and cynomolgus monkey), which had been used either for pharmacological or toxicological studies of ospemifene...
March 1, 2016: Drug Metabolism and Personalized Therapy
Cynthia A Stuenkel, Susan R Davis, Anne Gompel, Mary Ann Lumsden, M Hassan Murad, JoAnn V Pinkerton, Richard J Santen
OBJECTIVE: The objective of this document is to generate a practice guideline for the management and treatment of symptoms of the menopause. PARTICIPANTS: The Treatment of Symptoms of the Menopause Task Force included six experts, a methodologist, and a medical writer, all appointed by The Endocrine Society. EVIDENCE: The Task Force developed this evidenced-based guideline using the Grading of Recommendations, Assessment, Development, and Evaluation (GRADE) system to describe the strength of recommendations and the quality of evidence...
November 2015: Journal of Clinical Endocrinology and Metabolism
Santiago Palacios, Andrea Mejias
INTRODUCTION: Vasomotor symptoms (VMS) and the genitourinary syndrome of menopause (GSM) are recognized as the most frequent and bothersome symptoms associated with menopause. There are different treatments for both groups of symptoms, being necessary to individualize them. AREAS COVERED: There are different therapies for VMS including hormonal treatments with estrogen, with and without progestins; the new alternative, tissue-selective estrogen complex (TSEC), tibolone, phytoestrogens and only progestins...
2015: Expert Opinion on Pharmacotherapy
James H Pickar, Barry S Komm
Traditional menopausal hormone therapy containing estrogens/progestin has been associated with an increased risk of breast cancer, and estrogen exposure is known to promote growth and proliferation of a majority of breast cancers. Therefore, it is important for clinicians to consider the breast safety profile of any hormone-based therapy used in postmenopausal women. This review provides an overview of the breast safety and tolerability profiles of currently marketed selective estrogen receptor modulators, antiestrogens, and the first tissue selective estrogen complex combining conjugated estrogens with the selective estrogen receptor modulator bazedoxifene in postmenopausal women...
September 2015: Post Reproductive Health
Nicoletta Biglia, Valentina E Bounous, Luca G Sgro, Marta D'Alonzo, Silvia Pecchio, Rossella E Nappi
Breast cancer survivors (BCSs) often suffer from menopausal symptoms induced by systemic treatments, with a consequent negative effect on quality of life. Since the introduction of aromatase inhibitors as the standard therapy for hormone-dependent tumors, genitourinary syndrome of menopause (GSM) has become a main problem for BCSs. This new terminology refers to the wide range of vaginal and urinary symptoms related to menopause, which can be relieved by estrogen therapy. Unfortunately, systemic hormone therapy is contraindicated for BCSs and also vaginal estrogens at standard dosage might influence the risk of recurrence because they cause a significant increase of circulating estrogens...
December 2015: Clinical Breast Cancer
Erin C Raney
Two new products recently approved for the treatment of menopausal symptoms contain estrogen receptor agonists/antagonists, which have varying effects on bone, breast, endometrial, and vaginal tissues. Ospemifene improves symptoms of dyspareunia associated with vulvovaginal atrophy. Bazedoxifene combined with conjugated estrogens improves vasomotor symptoms and bone mineral density in postmenopausal women. Clinicians must consider the increased risk for venous and arterial thromboembolic disease posed by these drugs...
July 2015: JAAPA: Official Journal of the American Academy of Physician Assistants
Amanda J Ellis, Vicky M Hendrick, Robert Williams, Barry S Komm
INTRODUCTION: Selective estrogen receptor (ER) modulators (SERMs) are a class of nonsteroidal compounds that interact with ERs, each with a distinct tissue-specific profile. Depending upon the degree of ER agonism/antagonism at the target tissue, SERMs show efficacy for various indications including osteoporosis, dyspareunia, and breast cancer, and are associated with safety risks. AREAS COVERED: This review describes the safety profile of SERMs (tamoxifen, raloxifene, toremifene, bazedoxifene, lasofoxifene, and ospemifene) and fulvestrant (a pure ER antagonist) from Phase III trials, long-term extension studies, and active comparator studies...
June 2015: Expert Opinion on Drug Safety
Rossella E Nappi, Laura Cucinella
INTRODUCTION: 'Female sexual dysfunction' (FSD) is an umbrella term comprising a range of common disorders, including hypoactive sexual desire, reduced subjective and/or physical genital arousal (poor sensation, vasocongestion, lubrication), sexual pain and inability to achieve orgasm/satisfaction, which are multidimensional by nature and often coexisting. Psychological and contextual factors have a significant influence on organic components of sexual response and behavior and a tailored medical approach to sexual symptoms is inevitably limited...
April 2015: Expert Opinion on Pharmacotherapy
Sheryl A Kingsberg, Terri Woodard
Low or absent sexual desire is the most common sexual dysfunction in women, and its prevalence peaks during midlife. Its etiology is complex and may include biologic, psychologic, and social elements. Major risk factors for its development include poor health status, depression, certain medications, dissatisfaction with partner relationship, and history of physical abuse, sexual abuse, or both. Diagnosis is based on criteria set by the Diagnostic and Statistical Manual of Mental Disorders (5th Edition) and requires that a woman experience personal distress...
February 2015: Obstetrics and Gynecology
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