Ospemifene

OSPHENA is an estrogen receptor agonist/antagonist with tissue selective effects. Its biological actions are mediated through binding to estrogen receptors.

• 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. ( 1.1 ) The treatment of moderate to severe vaginal dryness, a symptom of vulvar and vaginal atrophy, due to menopause.ICD-10: N95.1

• OSPHENA is contraindicated in women with any of the following conditions: Undiagnosed abnormal genital bleeding. Estrogen-dependent neoplasia.contraindicated

OSPHENA is an estrogen agonist/antagonist which has agonistic effects on the endometrium [see Warnings and Precautions (5.2) ]. 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. One tablet taken orally once daily with food. ( 2.1 , 2.2 ) 2.1 Treatment 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. 2.2 Treatment 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.

Venous Thromboembolism: Risk of DVT and PE ( 5.1 ) Known, suspected, or history of breast cancer ( 5.2 ) Severe Hepatic Impairment ( 5.3 , 8.7 , 12.3 ) 5.1 Cardiovascular Disorders Manage appropriately any risk factors for cardiovascular disorders, arterial vascular disease (for example, hypertension, diabetes mellitus, tobacco use, hypercholesterolemia, and obesity) and/or venous thromboembolism (VTE) (for example, personal history or family history of VTE, obesity, and systemic lupus erythematosus). Stroke 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 OSPHENA 60 mg treatment group and 3.15 and 0 per thousand women years in placebo. Immediately discontinue OSPHENA if a thromboembolic or hemorrhagic stroke occurs or is suspected. The WHI estrogen-alone substudy reported a statistically significant increased risk of stroke in women 50 to 79 years of age receiving daily CE (0.625 mg)-alone compared to women in the same age group receiving placebo (45 versus 33 strokes per ten thousand women years, respectively). The increase in risk was demonstrated in year 1 and persisted. Coronary Heart Disease Two cases of myocardial infarction (MI) occurred in women receiving 60 mg of ospemifene in the OSPHENA clinical trials. The WHI estrogen-alone substudy reported no overall effect on coronary heart disease (CHD) events (defined as nonfatal MI, silent MI, or CHD death) in women receiving estrogen-alone compared to placebo.

The following serious adverse reactions are discussed elsewhere in the labeling: Cardiovascular Disorders [see Boxed Warning , Warnings and Precautions (5.1) ] Malignant Neoplasms [see Boxed Warning , Warnings and Precautions (5.2) ] The most common adverse reactions (≥1 percent) with OSPHENA are: hot flush, vaginal discharge, muscle spasms, headache, hyperhidrosis, vaginal hemorrhage, night sweats. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Duchesnay Inc. at 1-855-OSPHENA (1-855-677-4362) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical 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.

8.1 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. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. 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/m 2 )]. Drug-induced malformations were not observed in either rats or rabbits.

Metabolism

Absorption Following a single oral administration of OSPHENA 60 mg tablet in postmenopausal women under fasted condition, peak median serum concentration was reached at approximately 2 hours (range: 1 to 8 hours) post-dose (see Figure 2 ). Mean ospemifene C max and AUC 0-inf were 533 ng/mL and 4165 ng∙hr/mL, respectively.

• Feb 26, 2013NDANDA203505Duchesnay

1. 1Off Label Use45217%
2. 2Hot Flush37214%
3. 3Headache2098.1%
4. 4Muscle Spasms1947.5%
5. 5No Adverse Event1736.7%
6. 6Vaginal Haemorrhage1505.8%
7. 7Vaginal Discharge1345.2%
8. 8Labelled Drug-drug Interaction Medication Error1114.3%
9. 9Nausea1084.2%
10. 10Hyperhidrosis1074.1%
11. 11Drug Ineffective943.6%
12. 12Rash863.3%
13. 13Fatigue853.3%
14. 14Pain In Extremity783.0%
15. 15Therapeutic Response Unexpected752.9%

The 10 most recently updated of 11 ClinicalTrials.gov registrations naming Ospemifene as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Effects of Ospemifene on Brain Activation Patterns in Women With Sexual Interest-arousal Disorders
  Completed · Phase 4 · Interventional · 25 enrolled · Hospital Clinic of Barcelona
  NCT04677491updated 2025-09-15
• Vulvoscopy Changes of the Vulva, Vestibule and Vagina With Daily Ospemifene in Women With Dyspareunia From VVA
  Completed · Phase 4 · Interventional · 10 enrolled · Sue Goldstein
  NCT02784613updated 2019-04-02
• Study to Evaluate Ospemifene in Patients With Moderate to Severe Vaginal Dryness Due to Menopause
  Completed · Phase 3 · Interventional · 631 enrolled · Shionogi
  NCT02638337updated 2019-04-02
• Long-Term Safety of Ospemifene 60 mg Oral Daily Dose for the Treatment of Vulvar and Vaginal Atrophy (VVA) in Postmenopausal Women Without a Uterus
  Completed · Phase 3 · Interventional · 301 enrolled · Shionogi
  NCT01586364updated 2018-05-21
• Long-Term Safety of 30 mg and 60 mg Oral Daily Dose of Ospemifene in the Treatment of Vulvar and Vaginal Atrophy (VVA) in Postmenopausal Women With Intact Uterus
  Completed · Phase 3 · Interventional · 180 enrolled · Shionogi
  NCT01585558updated 2018-05-21
• Efficacy and Safety of Ospemifene in the Treatment of Moderate to Severe Vaginal Dryness and Vaginal Pain Associated With Sexual Activity
  Completed · Phase 3 · Interventional · 919 enrolled · Shionogi
  NCT00729469updated 2018-05-18
• A Clinical Study to Evaluate the Safety of Ospemifene
  Completed · Phase 3 · Interventional · 426 enrolled · Shionogi
  NCT00566982updated 2018-05-18
• Ospemifene vs. Conjugated Estrogens in the Treatment of Postmenopausal Sexual Dysfunction
  Terminated · Phase 4 · Interventional · 1 enrolled · Emory University
  NCT03018106updated 2018-01-23
• Effects of Ospemifene on Pelvic Vascularity and Blood Flow
  Withdrawn · Observational · 0 enrolled · University of Oklahoma
  NCT02010580updated 2014-12-03
• A Clinical Study to Evaluate Ospemifene in the Treatment of Vulvar and Vaginal Atrophy in Postmenopausal Women
  Completed · Phase 3 · Interventional · 826 enrolled · Shionogi
  NCT00276094updated 2013-06-28

Frequently asked questions

How does Ospemifene work?

OSPHENA is an estrogen receptor agonist/antagonist with tissue selective effects. Its biological actions are mediated through binding to estrogen receptors.

What is Ospemifene used for?

According to FDA labeling, Ospemifene carries indications including: 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. ( 1.1 ) The treatment of moderate to severe vaginal dryness, a symptom of vulvar and vaginal atrophy, due to menopause.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Ospemifene?

Ospemifene is classified as Selective estrogen receptor modulators, Estrogen Agonist/Antagonist, Selective Estrogen Receptor Modulators, Increased Vaginal Muscle Tone, Increased Vaginal Secretion.

What are the brand names for Ospemifene?

Ospemifene is marketed under brand names including Osphena.

What are the contraindications for Ospemifene?

Ospemifene labeling lists contraindications including: OSPHENA is contraindicated in women with any of the following conditions: Undiagnosed abnormal genital bleeding. Estrogen-dependent neoplasia.. Always consult the full prescribing information and a clinician.