Ospemifene
OSPHENA
Pronunciation: os-PEM-i-feen (os-FEE-na)
What it isSelective estrogen receptor modulator with vaginal agonism; dyspareunia from menopausal atrophy.
Why this oneOral non-estrogen option for women unwilling to use vaginal products or estrogen.
What limits itCauses hot flushes and VTE; safety with breast cancer history not established.
Pearls
- Prasterone (vaginal DHEA) is the other non-estrogen alternative.
FDA-approved for
- dyspareunia from vulvovaginal atrophy (2013)
Classes and tags
Clinical profile
Legacy pregnancy categoryX
Defining liabilityVenous thromboembolism and hormone-related adverse effects; estrogen also lowers lamotrigine exposure.
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
Available strengths
- tab 60 mg
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)
Cost
| Strength | #/mo | generic $/mo | brand $/mo | CostPlus | |
|---|---|---|---|---|---|
| 60 mg | tab | 30 qd | — | $245.19 | not offered |
Generic entry2024
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Self-check
- Ospemifene: What route distinguishes this treatment for vaginal atrophy?
Oral. - Ospemifene: Which uterine effect is a concern?
Endometrial stimulation.