Ospemifene (2 brand names, 1 dosage form, 1 route)
Available dosage forms: TABLET.
Routes of administration: ORAL.
Brand Names
- OSPEMIFENE
- OSPHENA
Indications and Usage
OSPHENA is indicated for:
Dosage and Administration
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.
Contraindications
OSPHENA is contraindicated in women with any of the following conditions: Undiagnosed abnormal genital bleeding. Estrogen-dependent neoplasia. Active DVT, PE, or a history of these conditions. Active arterial thromboembolic disease (for example, stroke and MI), or a history of these conditions. Hypersensitivity (for example, angioedema, urticaria, rash, pruritus) to OSPHENA or any ingredients. OSPHENA is contraindicated in women who are or may become pregnant. OSPHENA may cause fetal harm when administered to a pregnant woman. Ospemifene was embryo-fetal lethal with labor difficulties and increased pup deaths in rats at doses below clinical exposures, and embryo-fetal lethal in rabbits at 10 times the clinical exposure based on mg/m 2. 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.
Adverse Reactions
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)]
Drug Interactions
OSPHENA is primarily metabolized by CYP3A4 and CYP2C9. CYP2C19 and other pathways contribute to the metabolism of ospemifene.
Mechanism of Action
OSPHENA is an estrogen receptor agonist/antagonist with tissue selective effects. Its biological actions are mediated through binding to estrogen receptors. This binding results in activation of estrogenic pathways in some tissues (agonism) and blockade of estrogenic pathways in others (antagonism).