title: Pharmacokinetics, pharmacodynamics and clinical efficacy of ospemifene for the treatment of dyspareunia and genitourinary syndrome of menopause.
abstract: BACKGROUND
  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.
  
  
  METHODS
  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.
  
  
  CONCLUSIONS
  Ospemifene is efficacious for improving vaginal dryness or dyspareunia as the patient-identified most bothersome symptom, and Phase III clinical trials (4648 patients) have shown good efficacy in terms of improvement of objective and subjective signs and measures of GSM in postmenopausal women. Future studies with a long-term follow-up are required to better elucidate its safety profile. In particular, on the basis of preclinical and early clinical findings of antagonistic to neutral effect on breast tissue, more research is needed to assess the treatment with ospemifene in breast cancer survivors.
authors.affiliation: a Academic Unit of Obstetrics and Gynaecology , IRCCS AOU San Martino - IST , Genova , Italy.|b Department of Neurosciences, Rehabilitation, Ophthalmology, Genetics, Maternal and Child Health (DiNOGMI) , University of Genova , Genova , Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Bondi
authors.affiliation: a Academic Unit of Obstetrics and Gynaecology , IRCCS AOU San Martino - IST , Genova , Italy.|b Department of Neurosciences, Rehabilitation, Ophthalmology, Genetics, Maternal and Child Health (DiNOGMI) , University of Genova , Genova , Italy.
authors.forename: Simone
authors.initials: S
authors.lastname: Ferrero
authors.affiliation: a Academic Unit of Obstetrics and Gynaecology , IRCCS AOU San Martino - IST , Genova , Italy.|b Department of Neurosciences, Rehabilitation, Ophthalmology, Genetics, Maternal and Child Health (DiNOGMI) , University of Genova , Genova , Italy.
authors.forename: Carolina
authors.initials: C
authors.lastname: Scala
authors.affiliation: a Academic Unit of Obstetrics and Gynaecology , IRCCS AOU San Martino - IST , Genova , Italy.|b Department of Neurosciences, Rehabilitation, Ophthalmology, Genetics, Maternal and Child Health (DiNOGMI) , University of Genova , Genova , Italy.
authors.forename: Emanuela
authors.initials: E
authors.lastname: Tafi
authors.affiliation: a Academic Unit of Obstetrics and Gynaecology , IRCCS AOU San Martino - IST , Genova , Italy.|b Department of Neurosciences, Rehabilitation, Ophthalmology, Genetics, Maternal and Child Health (DiNOGMI) , University of Genova , Genova , Italy.
authors.forename: Annalisa
authors.initials: A
authors.lastname: Racca
authors.affiliation: a Academic Unit of Obstetrics and Gynaecology , IRCCS AOU San Martino - IST , Genova , Italy.|b Department of Neurosciences, Rehabilitation, Ophthalmology, Genetics, Maternal and Child Health (DiNOGMI) , University of Genova , Genova , Italy.
authors.forename: Pier Luigi
authors.initials: PL
authors.lastname: Venturini
authors.affiliation: a Academic Unit of Obstetrics and Gynaecology , IRCCS AOU San Martino - IST , Genova , Italy.|b Department of Neurosciences, Rehabilitation, Ophthalmology, Genetics, Maternal and Child Health (DiNOGMI) , University of Genova , Genova , Italy.
authors.forename: Umberto
authors.initials: U
authors.lastname: Leone Roberti Maggiore
mesh_terms: D000818:Animals; D004414:Dyspareunia / Q000188:drug therapy* / Q000473:pathology; D005260:Female; D052776:Female Urogenital Diseases / Q000188:drug therapy* / Q000209:etiology / Q000473:pathology; D006801:Humans; D008593:Menopause; D017698:Postmenopause; D020845:Selective Estrogen Receptor Modulators / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D013577:Syndrome; D013629:Tamoxifen / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D020845:Selective Estrogen Receptor Modulators; D013629:Tamoxifen; C119141:Ospemifene
keywords: Atrophy; clinical efficacy; dyspareunia; genitourinary syndrome; menopause; ospemifene; pharmacodynamics; pharmacokinetics