Ospemifene use in postmenopausal women.
BACKGROUND
Selective estrogen receptor modulators (SERMs) are structurally different compounds that interact with intracellular estrogen receptors in target organs as estrogen agonists and antagonists. These drugs have been intensively studied over the past decades and have proven to be a highly versatile group for the treatment of different conditions associated with menopause, including hormone-responsive cancer and osteoporosis. However, currently available SERMS are also responsible for side effects such as thromboembolic disorders, or gynecological symptoms (especially vaginal dryness and hot flushes).


OBJECTIVE
The purpose of this article is to review the clinical trials of ospemifene, a new SERM in Phase III development for the treatment of vulvar and vaginal atrophy. The medical literature was reviewed for appropriate articles containing the terms 'ospemifene' and 'SERMs'.


CONCLUSIONS
The recently released results from a pivotal Phase III study in postmenopausal women demonstrated statistically significant improvements of ospemifene 60 mg/day in symptoms of vulvar and vaginal atrophy over the use of non-hormonal vaginal lubricant. Ospemifene also appeared to be well tolerated, with few patients experiencing side effects. The additional positive results on bone and the breast observed in preclinical studies need to be clinically confirmed to extend the therapeutic potential of this new SERM.
Gennari
Luigi
L
Department of Internal Medicine, Endocrine-Metabolic Sciences and Biochemistry, University of Siena, Viale Bracci 1, Policlinico Le Scotte, Siena, Italy. gennari@unisi.it
Merlotti
Daniela
D
Valleggi
Fabrizio
F
Nuti
Ranuccio
R
D001284:Atrophy / Q000188:drug therapy*; D002986:Clinical Trials as Topic; D004353:Drug Evaluation, Preclinical; D015507:Drugs, Investigational / Q000494:pharmacology / Q000627:therapeutic use*; D005260:Female; D006801:Humans; D015394:Molecular Structure; D010330:Patents as Topic; D017698:Postmenopause / Q000187:drug effects*; D020845:Selective Estrogen Receptor Modulators / Q000494:pharmacology / Q000627:therapeutic use; D013629:Tamoxifen / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D014621:Vagina / Q000473:pathology*; D014844:Vulva / Q000473:pathology*
D015507:Drugs, Investigational; D020845:Selective Estrogen Receptor Modulators; D013629:Tamoxifen; C119141:Ospemifene