2016
DOI: 10.1080/17425255.2016.1218847
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Pharmacokinetics, pharmacodynamics and clinical efficacy of ospemifene for the treatment of dyspareunia and genitourinary syndrome of menopause

Abstract: 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, m… Show more

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Cited by 10 publications
(4 citation statements)
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“…Ospemifene is well-tolerated; increase in hot flashes is reported as the most frequent adverse effect [56]. Clinical studies suggest a significant neutral or minimum effect on the endometrium, a safe profile on the bone and cardiovascular systems and no stimulation on the breast tissue; however, further long-term studies on endometrial and breast safety are needed [57]. Indeed, Ospemifene is contraindicated in women with undiagnosed abnormal genital bleeding and known or suspected estrogen-dependent neoplasia, including breast cancer undergoing active treatment.…”
Section: Treatment Options For Menopause—related Sexual Dysfunctionsmentioning
confidence: 99%
“…Ospemifene is well-tolerated; increase in hot flashes is reported as the most frequent adverse effect [56]. Clinical studies suggest a significant neutral or minimum effect on the endometrium, a safe profile on the bone and cardiovascular systems and no stimulation on the breast tissue; however, further long-term studies on endometrial and breast safety are needed [57]. Indeed, Ospemifene is contraindicated in women with undiagnosed abnormal genital bleeding and known or suspected estrogen-dependent neoplasia, including breast cancer undergoing active treatment.…”
Section: Treatment Options For Menopause—related Sexual Dysfunctionsmentioning
confidence: 99%
“…Ospemifene is metabolized mainly in the liver by cytochrome P450 enzymes, primarily excreted in the bile, and eliminated in the feces [60,61]. PK parameters are therefore not affected in patients with impaired renal function.…”
Section: Pharmacokineticsmentioning
confidence: 99%
“…PK parameters are therefore not affected in patients with impaired renal function. Ospemifene may be used cautiously in patients with moderate hepatic impairment and with coadministration of ketoconazole; however, ospemifene should not be given with concomitant fluconazole [60,61].…”
Section: Pharmacokineticsmentioning
confidence: 99%
“…11 It is metabolized by the liver, excreted in the bile, and eliminated in the feces in approximately 24 to 36 hours. 12 Being an oral medication negates the disadvantages of topical application.…”
Section: Introductionmentioning
confidence: 99%