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Fareston (TOREMIFENE)
Fareston works by binding to estrogen receptors in the body, which can help reduce the growth of breast cancer cells.
At a glance
| Generic name | TOREMIFENE |
|---|---|
| Sponsor | Kyowa Kirin |
| Drug class | Estrogen Agonist/Antagonist |
| Target | 5-hydroxytryptamine receptor 6 |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 1997 |
Mechanism of action
Toremifene is nonsteroidal triphenylethylene derivative. Toremifene binds to estrogen receptors and may exert estrogenic, antiestrogenic, or both activities, depending upon the duration of treatment, animal species, gender, target organ, or endpoint selected. In general, however, nonsteroidal triphenylethylene derivatives are predominantly antiestrogenic in rats and humans and estrogenic in mice. In rats, toremifene causes regression of established dimethylbenzanthracene (DMBA)-induced mammary tumors. The antitumor effect of toremifene in breast cancer is believed to be mainly due to its antiestrogenic effects, i.e., its ability to compete with estrogen for binding sites in the cancer, blocking the growth-stimulating effects of estrogen in the tumor.
Approved indications
- Metastatic Breast Carcinoma
Boxed warnings
- WARNING: QT PROLONGATION FARESTON has been shown to prolong the QTc interval in a dose- and concentration-related manner [see Clinical Pharmacology (12.2) ] . Prolongation of the QT interval can result in a type of ventricular tachycardia called Torsade de pointes, which may result in syncope, seizure, and/or death. Toremifene should not be prescribed to patients with congenital/acquired QT prolongation, uncorrected hypokalemia or uncorrected hypomagnesemia. Drugs known to prolong the QT interval and strong CYP3A4 inhibitors should be avoided [see Warnings and Precautions (5.1) ] . WARNING: QT PROLONGATION FARESTON has been shown to prolong the QTc interval in a dose- and concentration-related manner [see Clinical Pharmacology (12.2) ] . Prolongation of the QT interval can result in a type of ventricular tachycardia called Torsade de pointes, which may result in syncope, seizure, and/or death. Toremifene should not be prescribed to patients with congenital/acquired QT prolongation, uncorrected hypokalemia or uncorrected hypomagnesemia. Drugs known to prolong the QT interval and strong CYP3A4 inhibitors should be avoided [see Warnings and Precautions (5.1) ] .
Common side effects
- Hot Flashes
- Sweating
- Nausea
- Vaginal Discharge
- Dizziness
- Edema
- Vomiting
- Vaginal Bleeding
- Cardiac Failure
- Myocardial Infarction
- Cataracts
- Dry Eyes
Drug interactions
- High Risk QT Prolonging Agents
- abarelix
- acetophenazine
- amiodarone
- amitriptyline
- apomorphine
- arsenic trioxide
- artemether
- astemizole
- atazanavir
- bepridil
- carbamazepine
Key clinical trials
- De-escalation Therapy in Stage I ER-Positive Breast Cancer: A Non-Inferiority Trial (PHASE3)
- Compare Adjuvant Monotherapy With Endocrine or Accelerated Partial Breast Irradiation After Lumpectomy (PHASE2)
- Efficacy and Safety of Dalpiciclib Plus Toremifene in the Treatment of Advanced First-line HR Positive and HER2 Negative Breast Cancer: a Multicenter, Single Arm, Exploratory Phase II Clinical Study (PHASE2)
- Stage I HER2 Positive Invasive Breast Cancer De-escalation Study(IRIS) (PHASE2)
- Adjuvant Pyrotinib and Capecitabine For HER2 Positive Micro Invasive Breast Cancer (PHASE2)
- Efficacy and Safety of Fluzoparib Combined With Adjuvant Endocrine Therapy for HR+/HER2- SNF3-subtype Early Breast Cancer (BCTOP-L-A01) (PHASE3)
- Prostate Cancer Prevention Study for Men With High Grade PIN (Prostatic Intraepithelial Neoplasia) (PHASE3)
- Comparative Evaluation of Efficacy and Safety of Toremifene, Tamoxifen, and Aromatase Inhibitor Plus Ovarian Function Suppression in Hormone Receptor-Positive Early Breast Cancer Among Non-Low-Risk Premenopausal Women: A Real-World Study
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |