Glossary · Treatments

Ospemifene (Osphena)

Also called: Osphena, SERM.

Definition: Ospemifene is an oral selective estrogen receptor modulator (SERM) FDA-approved for moderate-to-severe dyspareunia from menopause-related vulvovaginal atrophy. Unlike estrogen, it has tissue-selective effects — agonist on vaginal tissue, antagonist on breast — and is taken as a once-daily 60 mg pill.

Detailed definition

Ospemifene (Osphena) is a SERM that acts as an estrogen receptor agonist on vulvovaginal tissue and an antagonist or weak agonist on breast tissue. It was FDA-approved in 2013 for moderate-to-severe dyspareunia from menopause-related vulvovaginal atrophy and in 2014 for moderate-to-severe vaginal dryness. Standard dosing is 60 mg orally once daily. Compared to vaginal estrogen, ospemifene has the convenience of an oral pill but a different side effect profile — most notably hot flashes (4–7% of users), and an increase in VTE risk similar to oral estrogen because it is metabolized hepatically. It is contraindicated in women with current or prior VTE, undiagnosed vaginal bleeding, or estrogen-dependent neoplasia. Ospemifene's breast safety profile from clinical trials looks favorable, though the long-term breast outcomes data are still maturing.

Why it matters in menopause

Ospemifene is a useful option for women who cannot or do not want to use vaginal estrogen — particularly those who find local applications inconvenient or who prefer pills. The trade-offs are oral-route VTE risk and hot flashes as a paradoxical side effect.

Sources

External references: Wikipedia.

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