Dosage & Administration
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Osphena Prescribing Information
Endometrial Cancer
OSPHENA is an estrogen agonist/antagonist with tissue selective effects. In the endometrium, OSPHENA has estrogen agonistic effects. There is a potential increased risk of endometrial cancer in a woman with a uterus who uses unopposed estrogens. Adequate diagnostic measures, including directed and random endometrial sampling when indicated, should be undertaken to rule out malignancy in postmenopausal women with undiagnosed persistent or recurring abnormal genital bleeding [see Warnings and Precautions (5.2)].
Cardiovascular Disorders
In the clinical trials for OSPHENA (duration of treatment up to 15 months), the incidence rates of thromboembolic and hemorrhagic stroke were 1.13 and 3.39 per thousand women years, respectively in the OSPHENA 60 mg treatment group and 3.15 and 0 with placebo [see Warnings and Precautions (5.1)]. The incidence of DVT was 2.26 per thousand women years (2 reported cases) in the OSPHENA 60 mg treatment group and 3.15 per thousand women years (1 reported case) with placebo [see Warnings and Precautions (5.1)]. OSPHENA should be prescribed for the shortest duration consistent with treatment goals and risks for the individual woman.
There is a reported increased risk of stroke and deep vein thrombosis (DVT) in postmenopausal women (50 to 79 years of age) who received daily oral conjugated estrogens (CE) [0.625 mg]-alone therapy over 7.1 years as part of the Women's Health Initiative (WHI) [see Warnings and Precautions (5.1)].
1 INDICATIONS AND USAGE
OSPHENA is indicated for:
The Treatment of Moderate to Severe Dyspareunia, a Symptom of Vulvar and Vaginal Atrophy, Due to Menopause.
The Treatment of Moderate to Severe Vaginal Dryness, a Symptom of Vulvar and Vaginal Atrophy, Due to Menopause.
OSPHENA is an estrogen agonist/antagonist which has agonistic effects on the endometrium [see Warnings and Precautions (5.2)].
Use of OSPHENA should be for the shortest duration consistent with treatment goals and risks for the individual woman. Postmenopausal women should be re-evaluated periodically as clinically appropriate to determine if treatment is still necessary.
Treatment of Moderate to Severe Dyspareunia, a Symptom of Vulvar and Vaginal Atrophy, Due to Menopause
Take one 60 mg tablet with food once daily.
Treatment of Moderate to Severe Vaginal Dryness, a Symptom of Vulvar and Vaginal Atrophy, Due to Menopause
Take one 60 mg tablet with food once daily.
OSPHENA tablets are white to off-white, oval, biconvex, film coated tablets containing 60 mg of ospemifene and engraved with "60" on one side.
Pregnancy
Risk Summary
Not Recommended During Pregnancy
OSPHENA is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if a woman becomes pregnant while taking this drug, she should be apprised of the potential hazard to a fetus [see Contraindications (4)].
Based on animal data, OSPHENA is likely to increase the risk of adverse outcomes during pregnancy and labor. Adverse findings at maternally toxic doses included embryofetal lethality in rats and rabbits, and neonatal mortality and difficult labor in rats. The reproductive effects observed are consistent with and are considered to be related to estrogen receptor activity of OSPHENA.
The background risk of major birth defects and miscarriage for the indicated population is unknown. However, the background risk in the U.S. general population of major birth defects is 2 to 4%, and of miscarriage is 15 to 20% of clinically recognized pregnancies.
Data
Animal Data
The effects of ospemifene on embryo-fetal development were studied in rats (0.1, 1, or 4 mg/kg/day) and rabbits (3, 10, or 30 mg/kg/day) when treated from implantation through organogenesis [Gestation Day (GD) 6-16 in the rat and GD6-18 in the rabbit. In rabbits, there was an increase in the incidence of total resorptions at 30 mg/kg/day (10 times the human exposure based on body surface area mg/m2)]. Drug-induced malformations were not observed in either rats or rabbits.
The effects of ospemifene on pre- and postnatal development were studied in pregnant rats (0.01, 0.05, and 0.25 mg/kg/day) treated from implantation (GD6) through lactation (Lactation Day (LD) 21). Pregnant rats given 0.05 or 0.25 mg/kg/day ospemifene (0.8% to 4% the human exposure based on body surface area mg/m2) had a significantly prolonged and difficult gestation, increased post-implantation loss, increased number of dead pups at birth, and an increased incidence of postnatal loss. Ospemifene did not induce adverse effects in the surviving offspring of pregnant rats at drug exposures up to 4% the human exposure.
Lactation
Risk Summary
It is not known whether OSPHENA is excreted in human breast milk. There are no data on the effects of OSPHENA on the breastfed child or the effects on milk production. Do not breastfeed while taking OSPHENA. Ospemifene was excreted in rat milk [see Data].
Data
In a nonclinical study, ospemifene was excreted in rat milk and detected at concentrations higher than that in maternal plasma.
Pediatric Use
OSPHENA is not indicated in children. Clinical studies have not been conducted in the pediatric population.
Geriatric Use
Of the 2209 OSPHENA-treated women enrolled in the ten phase 2/3 trials of OSPHENA, >19 percent were 65 years of age or older. No clinically meaningful differences in safety or effectiveness were observed between these women and younger women less than 65 years of age.
Renal Impairment
The pharmacokinetics of ospemifene in women with severe renal impairment (CrCL <30 mL/min) was similar to those in women with normal renal function [see Clinical Pharmacology (12.3)].
No dose adjustment of OSPHENA is required in women with renal impairment.
Hepatic Impairment
The pharmacokinetics of ospemifene has not been studied in women with severe hepatic impairment (Child-Pugh Class C); therefore, do not use OSPHENA in women with severe hepatic impairment [see Warnings and Precautions (5.3), and Clinical Pharmacology (12.3)].
No clinically important pharmacokinetic differences with OSPHENA were observed between women with mild to moderate hepatic impairment and healthy women [see Clinical Pharmacology (12.3)].
No dose adjustment of OSPHENA is required in women with mild (Child-Pugh Class A) or moderate (Child-Pugh Class B) hepatic impairment.
OSPHENA is contraindicated in women with any of the following conditions:
- Undiagnosed abnormal genital bleeding.
- Known or suspected estrogen-dependent neoplasia.
- Active DVT, pulmonary embolism (PE), or a history of these conditions.
- Active arterial thromboembolic disease [for example, stroke and myocardial infarction (MI)], or a history of these conditions.
- Hypersensitivity (for example, angioedema, urticaria, rash, pruritus) to OSPHENA or any ingredients.
- OSPHENA is contraindicated in women who are or may become pregnant. OSPHENA may cause fetal harm when administered to a pregnant woman. Ospemifene was embryo-fetal lethal with labor difficulties and increased pup deaths in rats at doses below clinical exposures, and embryo-fetal lethal in rabbits at 10 times the clinical exposure based on mg/m2. If this drug is used during pregnancy, or if a woman becomes pregnant while taking this drug, she should be apprised of the potential hazard to a fetus.