Dosing & Uses
Dosage Forms & Strengths
tablet
- 60mg
Breast Cancer
60 mg PO qDay until disease progresses
Monitor patients on warfarin for increased PT
Desmoid Tumors (Orphan)
Indicated for treatment of desmoid tumors
Orphan indication sponsor
- Orion Corporation; PO Box 65; 02101 Espoo; FINLAND
Other Indications & Uses
Estrogen-receptor positive or unknown metastatic breast cancer in postmenopausal women
Not recommended
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
>10%
Hot flashes (35%)
Sweating (20%)
Nausea (14%)
Vaginal discharge (13%)
1-10%
Cataracts (10%)
Dizziness (9%)
Edema (5%)
Vomiting (4%)
Dry eyes (4%)
Hypercalcemia (3%)
Thrombophlebitis (2%)
Vaginal bleeding (2%)
<1%
Alopecia
Angina
Hepatitis
Dermatitis
Depression
Corneal opacity
Postmarketing
Hepatototoxicity
Risk of uterine malignancy
Warnings
Black Box Warnings
Prolongs QTc interval in a dose- and concentration-related manner
QT prolongation can result in Torsade de pointes, which may result in syncope, seizure, and/or death
Should not be prescribed to patients with congenital/acquired QT prolongation, uncorrected hypokalemia or uncorrected hypomagnesemia
Drugs known to prolong QT interval and strong CYP3A4 inhibitors should be avoided
Contraindications
Hypersensitivity
Estrogen receptor-negative tumors
Thromboembolic history
Should not be prescribed to patients with congenital/acquired QT prolongation, uncorrected hypokalemia or uncorrected hypomagnesemia
Cautions
May increase risk of ovarian CA, osteosarcoma
Risk of hypercalcemia & tumor flare
Long-term treatment discouraged in preexisting endometrial hyperplasia
Prolongs QTc interval; avoid in patients with congenital/acquired QT prolongation or uncorrected hypokalemia/hypomagnesemia
Avoid concomitant use of drugs known to prolong QT interval
Hepatotoxicity, both increases in serum concentration for grade 3 and 4 transaminitis; hyperbilirubinemia, including jaundice, hepatitis, and non-alcoholic fatty liver disease, have also been reported in clinical trials and postmarketing; liver function tests should be performed periodically
Endometrial cancer, endometrial hypertrophy, hyperplasia, and uterine polyps reported; endometrial hyperplasia of uterus observed in animals treated with toremifene; long-term use has not been established in patients with pre-existing endometrial hyperplasia; all patients should have baseline and annual gynecological examinations; patients at high risk of endometrial cancer should be closely monitored
Pregnancy & Lactation
Pregnancy Category: D
Lactation: Not known if excreted in breast milk, indicated in postmenopausal women
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Selective estrogen receptor modulator: nonsteroidal estrogen, agonist/antagonist, competes for estrogen binding sites on breast tumor cells
Pharmacokinetics
Half-Life: 5 days
Peak Plasma Time: 3 hr
Protein Bound: >99.5%
Vd: 580 L
Metabolism: Hepatic CYP3A4
Metabolites: N-demethyltoremifene, (deamino-hydroxy) toremifene
Clearance: 5 L/hr
Excretion: Feces (primarily); urine (10%)
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Patient Handout
Formulary
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