Brand Name
Osphena
Generic Name
Ospemifene
View Brand Information FDA approval date: April 01, 2023
Classification: Estrogen Agonist/Antagonist
Form: Tablet
What is Osphena (Ospemifene)?
OSPHENA is indicated for: OSPHENA is an estrogen agonist/antagonist indicated for: The treatment of moderate to severe dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause.
Approved To Treat
Save this treatment for later
Not sure about your diagnosis?
Related Clinical Trials
There is no clinical trials being done for this treatment
Related Latest Advances
Brand Information
Osphena (Ospemifene)
1INDICATIONS AND USAGE
OSPHENA is indicated for:
2DOSAGE AND ADMINISTRATION
OSPHENA is an estrogen agonist/antagonist which has agonistic effects on the endometrium
Use OSPHENA for the shortest duration consistent with treatment goals and risks for the individual woman. Reevaluate postmenopausal women periodically as clinically appropriate to determine if treatment is still necessary.
2.1Treatment of Moderate to Severe Dyspareunia, a Symptom of Vulvar and Vaginal Atrophy, Due to Menopause
One 60 mg tablet taken orally with food once daily.
2.2Treatment of Moderate to Severe Vaginal Dryness, a Symptom of Vulvar and Vaginal Atrophy, Due to Menopause
One 60 mg tablet taken orally with food once daily.
3DOSAGE FORMS AND STRENGTHS
OSPHENA tablets are white to off-white, oval, biconvex, film coated tablets containing 60 mg of ospemifene and engraved with "60" on one side.
4CONTRAINDICATIONS
OSPHENA is contraindicated in women with any of the following conditions:
- Undiagnosed abnormal genital bleeding.
- Estrogen-dependent neoplasia.
- Active DVT, PE, or a history of these conditions.
- Active arterial thromboembolic disease (for example, stroke and 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/m
5ADVERSE REACTIONS
The following serious adverse reactions are discussed elsewhere in the labeling:
- Cardiovascular Disorders
- Malignant Neoplasms
5.1Clinical Trials Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
The safety of OSPHENA has been assessed in ten phase 2/3 trials (N=2209) with doses ranging from 5 to 90 mg per day. The duration of treatment in these studies ranged from 6 weeks to 15 months. The majority of women (N=1683) had treatment exposure up to 12 weeks; 847 had up to 52 weeks (1 year) of exposure.
The incidence rates of thromboembolic and hemorrhagic stroke were 1.13 per thousand women years (1 reported case of thromboembolic stroke) and 3.39 per thousand women years (3 reported cases of hemorrhagic stroke), respectively in OSPHENA 60 mg treatment group and 3.15 (1 case of thromboembolic stroke) and 0 per thousand women years, respectively in placebo. There were 2 reported cases of DVT among the 1459 women in the OSPHENA 60 mg treatment group and 1 case of DVT among the 1136 women in the placebo group.
Table 1 lists adverse reactions occurring more frequently in the OSPHENA 60 mg treatment group than in placebo and at a frequency ≥1% in the 12-week, double-blind, placebo-controlled clinical trials. Table 2 lists adverse reactions occurring more frequently in the OSPHENA 60 mg treatment group than in placebo and at a frequency ≥1% in all clinical trials up to 52-weeks.
5.2Postmarketing Experience
The following adverse reactions have been identified during post-approval use of ospemifene. Because these reactions are reported voluntarily from a population of uncertain size, it is not possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Neoplasms Benign, Malignant and Unspecified (incl. cysts and polyps): endometrial hyperplasia, endometrial cancer
Immune System Disorders: allergic conditions including hypersensitivity, angioedema
Nervous System Disorders: headache
Vascular Disorders: deep vein thrombosis, thrombosis, pulmonary embolism
Skin and Subcutaneous Tissue Disorders: rash, rash erythematous, rash generalized, pruritus, urticaria
6DRUG INTERACTIONS
OSPHENA is primarily metabolized by CYP3A4 and CYP2C9. CYP2C19 and other pathways contribute to the metabolism of ospemifene.
6.1Estrogens and Estrogen Agonist/Antagonist
Do not use OSPHENA concomitantly with estrogens and estrogen agonists/antagonists. The safety of concomitant use of OSPHENA with estrogens and estrogen agonists/antagonists has not been studied.
6.2Fluconazole
Do not use OSPHENA concomitantly with fluconazole, a moderate CYP3A / strong CYP2C9 / moderate CYP2C19 inhibitor. Fluconazole increases the systemic exposure of ospemifene by 2.7-fold. Administration of fluconazole with ospemifene may increase the risk of OSPHENA-related adverse reactions
6.3Rifampin
Rifampin, a strong CYP3A4 / moderate CYP2C9 / moderate CYP2C19 inducer, decreases the systemic exposure of ospemifene by 58%. Therefore, co-administration of OSPHENA with drugs such as rifampin which induce CYP3A4, CYP2C9 and/or CYP2C19 activity would be expected to decrease the systemic exposure of ospemifene, which may decrease the clinical effect
6.4Ketoconazole
Ketoconazole, a strong CYP3A4 inhibitor, increases the systemic exposure of ospemifene by 1.4-fold. Administration of ketoconazole chronically with ospemifene may increase the risk of OSPHENA-related adverse reactions
6.5Warfarin
Repeated administration of ospemifene had no effect on the pharmacokinetics of a single 10 mg dose of warfarin. No study was conducted with multiple doses of warfarin. The effect of ospemifene on clotting time such as the International Normalized Ratio (INR) or prothrombin time (PT) was not studied
6.6Highly Protein-Bound Drugs
Ospemifene is more than 99% bound to serum proteins and might affect the protein binding of other drugs. Use of OSPHENA with other drug products that are highly protein-bound may lead to increased exposure of either that drug or ospemifene
6.7Multiple Enzyme Inhibition
Co-administration of OSPHENA with a drug known to inhibit CYP3A4 and CYP2C9 isoenzymes may increase the risk of OSPHENA-related adverse reactions.
7DESCRIPTION
OSPHENA is an estrogen agonist/antagonist. OSPHENA is not a hormone. The chemical structure of ospemifene is shown in Figure 1.
The chemical designation is Z-2-[4-(4-chloro-1,2-diphenylbut-1-enyl)phenoxy]ethanol, and has the empirical formula C
Each OSPHENA tablet contains 60 mg of ospemifene. Inactive ingredients include colloidal silicon dioxide, hypromellose, lactose monohydrate, magnesium stearate, mannitol, microcrystalline cellulose, polyethylene glycol, povidone, pregelatinized starch, sodium starch glycolate, titanium dioxide, and triacetin.
8CLINICAL STUDIES
The effectiveness and safety of OSPHENA on moderate to severe symptoms of vulvar and vaginal atrophy in postmenopausal women were examined in four placebo-controlled clinical trials (three 12-week efficacy trials and one 52-week long-term safety trial). In the four placebo-controlled trials, a total of 1100 women received placebo and 1416 women received 60 mg OSPHENA.
Trial 1 was a 12-week, randomized, double-blind, placebo-controlled, parallel-group trial that enrolled 826 generally healthy postmenopausal women between 41 to 81 years of age (mean 59 years of age) who at baseline had ≤5 percent superficial cells on a vaginal smear, a vaginal pH >5.0, and who identified at least one moderate to severe vaginal symptom that was considered the most bothersome to her (vaginal dryness, pain during intercourse [dyspareunia], or vaginal irritation/itching). Treatment groups included 30 mg ospemifene (n=282), 60 mg ospemifene (n=276), and placebo (n=268). All women were assessed for improvement in the mean change from baseline to Week 12 for the co-primary efficacy variables of: most bothersome symptom (MBS) of vulvar and vaginal atrophy (defined as the individual moderate to severe symptom that was identified by the woman as most bothersome at baseline), percentage of vaginal superficial and vaginal parabasal cells on a vaginal smear, and vaginal pH. Following completion of 12-weeks, women with an intact uterus were allowed to enroll in a 40-week double-blind extension study, and women without an intact uterus were allowed to enroll in a 52-week open-label extension study.
Trial 2 was a 12-week, randomized, double-blind, placebo-controlled, parallel-group trial that enrolled 919 generally healthy postmenopausal women between 41 to 79 years of age (mean 59 years of age) who at baseline had ≤5 percent superficial cells on a vaginal smear, a vaginal pH >5.0, and who identified either moderate to severe vaginal dryness (dryness cohort) or moderate to severe dyspareunia (dyspareunia cohort) as most bothersome to her at baseline. Treatment groups included 60 mg ospemifene (n=463) and placebo (n=456). Primary endpoints and study conduct were similar to those in Trial 1.
Trial 3 was a 12-week, randomized, double-blind, placebo-controlled, parallel-group trial that enrolled 631 generally healthy postmenopausal women between 40 and 80 years of age (mean 60 years of age) who at baseline had ≤5 percent superficial cells on a vaginal smear, a vaginal pH >5.0, and had moderate to severe vaginal dryness as the self-reported most bothersome symptom of VVA. Treatment groups included 60 mg ospemifene (n=316) and placebo (n=315). Primary endpoints and study conduct were similar to those in Trials 1 and 2. In Trial 3, 52 healthy postmenopausal women in the 60 mg ospemifene treatment group and 53 in placebo received treatment for up to 52-weeks.
Trial 4 was a 52-week, randomized, double-blind, placebo-controlled, long-term safety trial that enrolled 426 generally healthy postmenopausal women between 49 to 79 years of age (mean 62 years of age) with an intact uterus. Treatment groups included 60 mg ospemifene (n=363) and placebo (n=63).
9PATIENT COUNSELING INFORMATION
Advise women to read the FDA-approved labeling (Patient Information).
10PRINCIPAL DISPLAY PANEL - 60 mg Tablet Bottle Label
NDC 55494-580-90
Osphena
For oral use only
DUCHESNAY
