Pharmacokinetics, pharmacodynamics and clinical efficacy of ospemifene for the treatment of dyspareunia and genitourinary syndrome of menopause

• Published in: Expert opinion on drug metabolism & toxicology Vol. 12; no. 10; p. 1233
• Main Authors: Bondi, Chiara, Ferrero, Simone, Scala, Carolina, Tafi, Emanuela, Racca, Annalisa, Venturini, Pier Luigi, Leone Roberti Maggiore, Umberto
• Format: Journal Article
• Language: English
• Published: England 02.10.2016
• Subjects: Animals; Dyspareunia - drug therapy; Dyspareunia - pathology; Female; Female Urogenital Diseases - drug therapy; Female Urogenital Diseases - etiology; Female Urogenital Diseases - pathology; Humans; Menopause; Postmenopause; Selective Estrogen Receptor Modulators - pharmacokinetics; Selective Estrogen Receptor Modulators - pharmacology; Selective Estrogen Receptor Modulators - therapeutic use; Syndrome; Tamoxifen - analogs & derivatives; Tamoxifen - pharmacokinetics; Tamoxifen - pharmacology; Tamoxifen - therapeutic use; Atrophy; menopause; genitourinary syndrome; pharmacodynamics; pharmacokinetics; clinical efficacy; dyspareunia; ospemifene
• ISSN: 1744-7607
• DOI: 10.1080/17425255.2016.1218847

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. 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. 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.