Pharmaceutical Insights: toremifene citrate’s R&D Progress and its Mechanism of Action on Drug Target

Pharmaceutical Insights: toremifene citrate’s R&D Progress and its Mechanism of Action on Drug Target

ONS is committed to promoting excellence in oncology nursing and the transformation of cancer care. Ask your healthcare professional how you should dispose of any medicine you do not use. The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine. Medicines used to treat cancer are very strong and can have many side effects. Before receiving this medicine, make sure you understand all the risks and benefits.

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]. Drugs that decrease renal calcium excretion, e.g., thiazide diuretics, may increase the risk of hypercalcemia in patients receiving FARESTON. Treatment is generally continued until disease progression is observed.

  • Discuss the use of birth control, the risks and benefits of this medication, and any other concerns about using this medication with your doctor.
  • Toremifene produced ovarian atrophy in dogs administered doses ≥3 mg/kg/day (approximately 1.5 times the daily maximum recommended human dose of 60 mg, on a mg/m2 basis) for 16 weeks.
  • Moreover, TOR suppressed angiogenesis in rabbit cornea and lung metastasis of human fibrosarcoma HT-1080 cells in nude mice.
  • Patients who must take medications known to prolong the QT interval, or potent CYP3A4 inhibitors, should be informed of the effect of toremifene on QT interval.

You are encouraged to report negative side effects of prescription drugs to the FDA. Patients with bone metastases should be informed about the typical signs and symptoms of hypercalcemia and instructed to contact their physician for further assessment if such signs or symptoms occur. Two of the 3 studies showed similar results for all effectiveness endpoints. However, the Nordic Study showed a longer time to progression for tamoxifen (see table).

Toremifene Citrate CAS 89778-27-8

The United States, China, and the European Union are the countries/locations that are developing fastest, with the United States leading in terms of approved drugs. China has shown notable progress, particularly in the approved and preclinical stages. Overall, the target ER presents a competitive landscape with promising future development potential. ERs modulators can have different effects on estrogen receptors depending on their specific properties. Some modulators can act as agonists, meaning they bind to the receptors and activate them, mimicking the effects of estrogen. These agonists can be used in hormone replacement therapy to alleviate symptoms of menopause or to treat certain conditions such as osteoporosis.

  • There is no indication for use of FARESTON in pediatric patients.
  • Drugs that decrease renal calcium excretion, e.g., thiazide diuretics, may increase the risk of hypercalcemia in patients receiving FARESTON.
  • In patients at increased risk, electrocardiograms (ECGs) should be obtained and patients monitored as clinically indicated [see BOX WARNING and WARNINGS AND PRECAUTIONS].

In patients at increased risk, electrocardiograms (ECGs) should be obtained at baseline and as clinically indicated [see DRUG INTERACTIONS and CLINICAL PHARMACOLOGY]. In a study of 20 healthy subjects, 500 mg tolbutamide once daily (days 7 and 19) coadministered with toremifene as a 480 mg loading dose followed by 80 mg once daily for 16 days. Following coadministration on days 7 and 19 plasma tolbutamide Cmax and AUC were increased by less than 30%. A reduction of similar magnitude was observed for hydroxytolbutamide and carboxytolbutamide Cmax and AUC. Three prospective, randomized, controlled clinical studies (North American, Eastern European, and Nordic) were conducted. The North American and Eastern European studies also included high-dose toremifene arms of 200 and 240 mg daily, respectively [see Clinical Studies].

Toremifene caused embryo-fetal toxicities at maternal doses that were lower than the 60 mg daily recommended human dose on a mg/m2 basis. There are no adequate and well-controlled studies in pregnant women using FARESTON. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus. The significance of the mouse findings is uncertain because of the different role of estrogens in mice and the estrogenic effect of toremifene in mice. An increased incidence of ovarian and testicular tumors in mice has also been observed with other human estrogen agonists/antagonists that have primarily estrogenic activity in mice.

Common Brand(S): Fareston

The antiangiogenic activity in vitro was apparent at the concentration of 5 microM which is clinically achievable by oral administration of 120 mg/kg of TOR. These results suggest that clinical treatment with 120 mg/day of TOR might be expected to exhibit antiangiogenesis buysteroidsgroup and antimetastasis effects, in addition to inhibition of estrogen-dependent tumor cell growth. The pharmacokinetics of toremifene were studied in 10 healthy young males and 10 elderly females following a single 120 mg dose under fasting conditions.

It is important for you to work closely with your doctor during your treatment. Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of toremifene in the elderly. However, elderly patients are more likely to have age-related liver problems, which may require caution and an adjustment in the dose for patients receiving toremifene.

Viewing your signed in accounts

All patients should have baseline and annual gynecological examinations. In particular, patients at high risk of endometrial cancer should be closely monitored. Caution should be exercised in patients with congestive heart failure, hepatic impairment and electrolyte abnormalities. Hypokalemia or hypomagnesemia must be corrected prior to initiating toremifene and these electrolytes should be monitored periodically during therapy.

Toremifene Citrate is a small molecule drug that falls under the category of biomedicine. It primarily targets the estrogen receptor (ER) and is used in the treatment of neoplasms, skin diseases, and musculoskeletal diseases. The drug has been approved for the treatment of metastatic breast cancer and breast cancer. Decreases in high-density lipoprotein (HDL) levels have been observed in men on testosterone therapy (TTh). Niacin is commonly used as a therapy for low HDL, although its side effect (SE) profile often leads to frequent discontinuation.


Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention. It is very important that your doctor check your progress at regular visits to make sure that this medicine is working properly.

Possible Side Effects While Using This Medicine:

Fourteen percent of patients in the North American Study were non-Caucasian. No significant race-related differences in FARESTON effectiveness or safety were noted. 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.

Leave a Reply

Your email address will not be published. Required fields are marked *