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

被引:11
作者
Bondi, Chiara [1 ,2 ]
Ferrero, Simone [1 ,2 ]
Scala, Carolina [1 ,2 ]
Tafi, Emanuela [1 ,2 ]
Racca, Annalisa [1 ,2 ]
Venturini, Pier Luigi [1 ,2 ]
Maggiore, Umberto Leone Roberti [1 ,2 ]
机构
[1] IRCCS AOU San Martino IST, Acad Unit Obstet & Gynaecol, Largo R Benzi 10, I-16132 Genoa, Italy
[2] Univ Genoa, Dept Neurosci Rehabil Ophthalmol Genet Maternal &, Genoa, Italy
关键词
Atrophy; dyspareunia; genitourinary syndrome; menopause; ospemifene; pharmacokinetics; pharmacodynamics; clinical efficacy; VULVO-VAGINAL ATROPHY; ESTROGEN-RECEPTOR MODULATORS; WOMENS SEXUAL HEALTH; QUALITY-OF-LIFE; POSTMENOPAUSAL WOMEN; INTERNATIONAL SOCIETY; FRACTIONAL CO2-LASER; BREAST-CANCER; GENITAL-TRACT; ERBIUM LASER;
D O I
10.1080/17425255.2016.1218847
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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. Expert opinion: 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.
引用
收藏
页码:1233 / 1246
页数:14
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