Ospemifene
OSPHENA
What it isSelective estrogen receptor modulator with vaginal agonism; dyspareunia from menopausal atrophy.
Why this oneOral treatment for vulvovaginal atrophy in women who will not use a vaginal preparation.
What limits itVTE and stroke risk, and endometrial stimulation. Hot flushes.
FDA-approved for
- dyspareunia from vulvovaginal atrophy (2013)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Moderate-severe dyspareunia (vulvar/vaginal atrophy of menopause) | Postmenopausal women | 60 mg QD | 60 mg QD | 60 mg QD |
| Moderate-severe vaginal dryness (vulvar/vaginal atrophy of menopause) | Postmenopausal women | 60 mg QD | 60 mg QD | 60 mg QD |
Renal No adjustment needed (PK in severe renal impairment similar to normal)
Hepatic Do not use in severe hepatic impairment (Child-Pugh C); not studied
Instructions
- Take with food once daily
- Use shortest duration consistent with treatment goals
Contraindications
- Undiagnosed abnormal genital bleeding
- Estrogen-dependent neoplasia
- Active or history of DVT or pulmonary embolism
- Active or history of arterial thromboembolic disease (stroke, MI)
- Women who are or may become pregnant
Cautions
- Venous thromboembolism (DVT/PE)
- Stroke
- Known, suspected, or history of breast cancer
- Severe hepatic impairment
Adverse reactions
- Hot flush
- Vaginal discharge
- Muscle spasms
- Headache
- Hyperhidrosis
- Vaginal hemorrhage
- Night sweats
Pregnancy Contraindicated in pregnancy; can cause fetal harm (embryo-fetal lethality in animals)
Lactation Not known if present in human milk (excreted in rat milk)
⚠ BOXED WARNINGS
- Endometrial cancer
- Cardiovascular disorders
Cost, est. cash$300–$2,500/month
Generic entry2024
Classes and tags
Clinical profile
Legacy pregnancy categoryX
Defining liabilityVenous thromboembolism and hormone-related adverse effects; estrogen also lowers lamotrigine exposure.
Mechanism of action: Ospemifene ballicule
