Toremifene Uses, Side Effects & Warnings

Toremifene belongs to the group of class non-steroidal selective estrogen receptor modulator (SERM). It is a chlorinated derivative of tamoxifen and shows equal efficacy in treating breast cancer. It exhibits estrogenic activity in bones and antiestrogenic action in breast tissues. As an FDA-approved drug, it is primarily indicated for the treatment of estrogen receptor-positive breast cancer and cancer of unknown receptor status in postmenopausal women.

• In animal studies, toremifene crossed the placenta and accumulated in the rodent fetus.
• Toremifene is an antineoplastic hormonal agent primarily used in the treatment of advanced breast cancer.
• It is recommended that users take toremifene citrate every other day in order to ensure that there is an adequate level of the drug in their system at all times.

This product may contain inactive ingredients, which can cause allergic reactions or other problems. Toremifene has rarely caused very serious (possibly fatal) blood clots in the lungs/legs, brain (stroke), and heart (heart attack). Always inform your health care provider if you experience any unusual symptoms.

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Discuss the use of birth control, and the risks and benefits of this medication with your doctor. Because of the possible risk to the infant, breastfeeding is not recommended while using this drug. Mainly by CYP3A4 to N-demethyltoremifene, which exhibits antiestrogenic effects but has weak antitumor potency in vivo.

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Talk to your care team about what symptoms are possible and what to do if you have these symptoms. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal https://www.musettimobiliantichi.it/new-research-reveals-optimal-methyltestosterone/ drugs. Specific interactions with foods that inhibit CYP3A4, including grapefruit juice, have not been studied but may increase toremifene concentrations. Patients should avoid grapefruit products and other foods that are known to inhibit CYP3A4 during FARESTON treatment.

Toremifene Citrate is a Selective Estrogen Receptor Modulator (SERM) best known by the popular trade name given to it by GTx Inc. A relatively new SERM to the market, Toremifene Citrate was first approved by the FDA in 1997 and is available in countries worldwide. Very similar to Nolvadex (Tamoxifen Citrate) and Clomid (Clomiphene Citrate), Fareston is medically used to treat breast cancer in post-menopausal women.

The plasma concentration time profile of toremifene declines biexponentially after absorption with a mean distribution half-life of about 4 hours and an elimination half-life of about 5 days. Elimination half-lives of major metabolites, N-demethyltoremifene and (Deaminohydroxy) toremifene, were 6 and 4 days, respectively. Toremifene is eliminated as metabolites primarily in the feces, with about 10% excreted in the urine during a 1-week period. Elimination of toremifene is slow, in part because of enterohepatic circulation. The pharmacokinetics of toremifene and N-demethyltoremifene were similar in normals and in patients with impaired kidney function. The pharmacokinetic characteristics (absorption, distribution, metabolism and elimination) of both drugs vary as a result of slight differences in structure.

The pharmacokinetics of Ndemethyltoremifene were unchanged in these patients. Ten patients on anticonvulsants (phenobarbital, clonazepam, phenytoin, and carbamazepine) showed a twofold increase in clearance and a decrease in the elimination half-life of toremifene. Following multiple dosing with toremifene in 20 healthy volunteers, plasma toremifene exposure was lower on Day 17 compared to Day 5 by approximately 14%. N-demethyltoremifene exposure was higher on Day 17 compared to Day 5 by approximately 80%.

In cytosols derived from human breast adenocarcinomas, Toremifene competes with estradiol for estrogen receptor protein. Studies on toremifene’s effects on osteoporosis prevention have been conducted in addition to its use in the treatment of breast cancer. Toremifene, a SERM, has demonstrated potential in preserving bone density and lowering the risk of fractures in postmenopausal women. Studies look into how it affects fracture rates, markers of bone turnover, and bone mineral density. The findings reveal prospective substitute therapies for postmenopausal osteoporosis and advance our knowledge of toremifene’s function in maintaining bone health. The use of toremifene in treating breast cancer is a prominent field of research.

Patients with a history of thromboembolic diseases should generally not be treated with FARESTON. Patients with bone metastases should be monitored closely for hypercalcemia during the first weeks of treatment [see Hepatotoxicity]. Treatment is generally continued until disease progression is observed. FARESTON has been shown to prolong the QTc interval in a dose- and concentration-related manner [see CLINICAL PHARMACOLOGY]. 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.