Ospemifene
SERMs
Selective oestrogen receptor modulators (SERMs)Pregnancy: contraindicated
Intended for women after menopause; it may harm a fetus and is not used in pregnancy or breastfeeding.
Oral SERM that acts like oestrogen on the vaginal lining. For painful intercourse and vaginal dryness after menopause; risk of clots and endometrial cancer.
Quick facts
- Group
- Selective oestrogen receptor modulators (SERMs)
- Target
- Oestrogen receptor (ERα)
- Used for
- Painful intercourse
- Key effects
- Hot flushes · Vaginal discharge · Muscle spasms
- Monitor
- Any abnormal vaginal bleeding
- ATC
- G03XC05
No doses: the clinician sets them by the current guideline.
Mechanism of action
Ospemifene is a selective oestrogen receptor modulator. On the vaginal lining it acts like oestrogen, so the thinned, dry tissue of menopause becomes thicker and moister and intercourse hurts less. Its oestrogen-like action can also thicken the endometrium, and like other SERMs it raises the risk of blood clots.
- Ospemifene binds the oestrogen receptor
- In the vagina it acts like oestrogen
- The lining thickens: less dryness and pain
Indications
- Painful intercourse (dyspareunia) and vaginal dryness from menopause. Genitourinary syndrome of menopause (atrophic vaginitis) →
Adverse effects
Common
- Hot flushes
- Vaginal discharge
- Muscle spasms
- Increased sweating
Contraindications
- Known or suspected cancer, or undiagnosed abnormal vaginal bleeding (generally not used)
- Previous stroke, heart attack or blood clots (generally not used)
- Pregnancy
Key interactions
- St John's wort
- Interacts with ospemifene and is not started without medical advice.
- Grapefruit
- May change ospemifene levels; it is discussed with the doctor.
What is monitored
- Any abnormal vaginal bleeding, investigated promptly
- Signs of clots and stroke
- Cardiovascular risk factors: smoking, blood pressure, lipids, diabetes
Administration and safety
- Oral tablet once a day with food, at about the same time.
Pregnancy and breastfeeding
Intended for women after menopause; it may harm a fetus and is not used in pregnancy or breastfeeding.
Nursing care
- Ask about cancer, abnormal bleeding, stroke, heart attack, clots (personal or family), smoking, lupus and liver disease before starting.
- Teach to report any vaginal bleeding at once.
- Teach the signs of a clot or stroke: leg swelling or pain, chest pain, sudden breathlessness, slurred speech, one-sided weakness.
Pharmacokinetics
- Absorption
- Oral tablet once a day, taken with food.
- Metabolism
- St John's wort and grapefruit can interact with it.
Test yourself
Think of the answer, then tap the question to see it.
For which menopausal symptoms is ospemifene used?
Painful intercourse (dyspareunia) and vaginal dryness.
Which two serious risks appear in the ospemifene warning?
Endometrial cancer, and stroke and blood clots.
A woman on ospemifene reports vaginal bleeding. What should happen?
It is reported to the doctor at once and investigated, because ospemifene can thicken the endometrium.
Connections
← Back to the class: Selective oestrogen receptor modulators (SERMs)
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Ospemifene: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2025); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.