Consumer medicine information

Fareston

Toremifene

BRAND INFORMATION

Brand name

Fareston

Active ingredient

Toremifene

Schedule

S4

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Fareston.

What is in this leaflet

The name of your medicine is FARESTON. It contains an active ingredient called toremifene.

This leaflet answers some common questions about FARESTON.

It does not contain all of the available information.

It does not take the place of talking to your doctor or pharmacist.

All medicines have risks and benefits. Your doctor has weighed the risks of you taking FARESTON against the benefits this medicine is expected to have for you.

If you have any concerns about taking this medicine, ask your doctor or pharmacist.

Keep this leaflet with the medicine. You may want to read it again.

What FARESTON is used for

FARESTON is used to treat hormone-sensitive breast cancer in women who have had their menopause.

It belongs to the group of medicines known as anti-oestrogens. It helps to stop the tumour cells from growing and multiplying.

A doctor's prescription is required for FARESTON.

Your doctor, however, may prescribe FARESTON for another purpose.

Ask your doctor if you have any questions about why FARESTON has been prescribed for you.

Before you take FARESTON

When you must not take it

Do not take FARESTON if:

  • you have endometrial hyperplasia (an overgrowth in the lining of the uterus)
  • you have severe liver failure
  • you are pregnant or breastfeeding
  • you have a heart condition called QT prolongation, where the heart muscle takes longer to contract and then recover due to a disorder involving electrical impulses.
  • you have other heart conditions including bradycardia (slow heart rhythm), symptomatic arrhythmias (irregular heart rhythm) or heart failure.
  • you have electrolyte disturbances including uncorrected hypokalaemia (low blood potassium levels; which can in turn cause heart arrhythmia disorders).

FARESTON is for use by women who have had their menopause and should not be used by pregnant or breastfeeding women.

Do not take FARESTON after the expiry date (EXP) printed on the pack.

Do not take FARESTON if the packaging is torn or shows sign of tampering.

If you are not sure if you should start taking FARESTON, contact your doctor or pharmacist.

Before you start to take it

You must tell your doctor if:

  1. you are allergic to:
  • toremifene or other anti-oestrogens (e.g. tamoxifen) or any of the ingredients listed at the end of this leaflet.
  • any other medicines
  • any other substances such as foods, preservatives or dyes
  1. you have angina or a heart condition, including an irregular heart beat
  2. you feel pain in your bones
  3. you have had problems with blood clots in the past
    In severe cases, FARESTON is not recommended.
  4. you have liver problems
  5. you have any other medical conditions or health problems

If you have not told your doctor about any of the above, report them before you take any FARESTON.

Taking other medicines

Tell your doctor if you are taking any other medicines, including medicines that you buy without a prescription from a pharmacy, supermarket or health food shop.

Some medicines and FARESTON may interfere with each other. These include:

  • some diuretics, also called water or fluid tablets
  • phenytoin, carbamazepine and phenobarbitone, medicines used to treat epilepsy
  • warfarin, a medicine used to stop blood clots, and related medicines
  • certain antibiotics such as erythromycin and related medicines (including, moxifloxacin and pentamidine).
  • Certain antimalarials, particularly halofantrine.
  • certain medicines used to treat fungal infections, such as ketoconazole
  • Certain antiarrhythmics, including class IA (eg quinidine, hydroquinidine, disopyramide) and class III (eg amiodarone, sotalol, doretilide, ibutilide)
  • Some antihistamines, such as terfenadine, astemizole and mizolastine.

These medicines may be affected by FARESTON, or may affect how well FARESTON works. You may need to take different amounts of your medicine, or you may need to take different medicines. Your doctor will advise you.

Your doctor and pharmacist have more information about medicines to be careful with or avoid while taking FARESTON.

How to take FARESTON

Follow all directions given to you by your doctor and pharmacist carefully. They may differ from the information contained in this leaflet.

If you do not understand the instructions on the box, ask your doctor or pharmacist for help.

How much to take

The usual dose is one tablet by mouth, once a day.

However, your doctor may prescribe a different dose.

How to take it

Swallow FARESTON tablets with a glass of water.

When to take it

FARESTON can be taken with or without food. It is good practice to take FARESTON at about the same time each day.

How long to take it

Continue to take FARESTON regularly, even when you begin to feel better.

Do not stop taking this medicine without first checking with your doctor. Your doctor will tell you when to stop taking FARESTON.

If you forget to take it

If it is almost time for your next dose, skip the dose you missed and take your next dose when you are meant to.

Otherwise, take it as soon as you remember, and then go back to taking it as you would normally.

Do not take a double dose to make up for the dose that you missed.

If you have trouble remembering when to take your medicine, ask your pharmacist for some hints.

If you take too much (overdose)

Immediately telephone your doctor or Poisons Information Centre (Ph 13 11 26 - Australia) for advice, or go to the emergency department at your nearest hospital, if you think you or anyone else may have taken too much FARESTON. Do this even if there are no signs of discomfort or poisoning.

Keep this telephone number handy.

Very high doses of FARESTON may make you feel dizzy or give you a headache.

While you are taking FARESTON

Things you must do:

Use FARESTON exactly as your doctor has prescribed.

Tell all doctors, dentists and pharmacists who are treating you that you are taking FARESTON.

If you are about to be started on any new medicines tell your doctor or pharmacist that you are taking FARESTON.

If you become pregnant while taking FARESTON tell your doctor immediately.

Things you must not do

Do not take FARESTON to treat any other complaints unless your doctor tells you to.

Do not give FARESTON to anyone else, even if their symptoms seem similar to yours.

Things to be careful of

Make sure you know how you react to FARESTON before you drive a car, operate machinery, or do anything else that could be dangerous if you are dizzy or light-headed. As with other medicines, FARESTON may cause dizziness or light-headedness in some people.

If this occurs, do not drive.

Side effects

Check with your doctor as soon as possible if you have any problems while you are taking FARESTON, even if you do not think the problems are connected with the medicine or are not listed in this leaflet.

Like other medicines FARESTON can cause some side effects. If they occur, most are likely to be minor and temporary. However, some may be serious and need medical attention.

Ask your doctor or pharmacist to answer any questions you may have.

Tell your doctor if you notice any of the following and they worry you.

These are the more common side effects of FARESTON:

  • hot flushes
  • sweating
  • nausea (feeling sick) or vomiting
  • a white vaginal discharge
  • dizziness
  • swelling of the hands, feet and/or ankles (oedema)
  • pain

Other side effects that may occur include:

  • vaginal bleeding
  • chest pain, back pain
  • muscle weakness
  • headache, light-headedness
  • inability to sleep (insomnia)
  • weight increase
  • shortness of breath
  • tremor, weakness, tiredness
  • itching
  • skin discolouration or yellowing of the eyes and/or skin (jaundice)
  • constipation
  • loss of appetite (anorexia)
  • reduced vision

Other side effects not listed above may also occur in some patients.

Tell your doctor if you notice anything else that is making you feel unwell.

Do not be alarmed by this list of possible side effects. You may not experience any of them.

After using FARESTON

Storage

Keep your tablets in the pack until it is time to take them. If you take the tablets out of the pack they will not keep well.

Keep the tablets in a cool dry place where the temperature stays below 25 degrees C.

Do not store FARESTON in the freezer.

Do not store FARESTON or any other medicine in the bathroom or near a sink.

Do not leave it in the car or on window sills. Heat and dampness can destroy some medicines.

Keep it where children cannot reach it. A locked cupboard at least one-and-a-half metres above the ground is a good place to store medicines.

Disposal

Return any unused medicine to your pharmacist.

Product description

What it looks like

FARESTON tablets are white or almost white, flat, round, uncoated tablets marked with TO60 on one side of the tablet. It is available in blister packs of 30 tablets.

Ingredients

Active ingredient

Toremifene citrate equivalent to toremifene 60 mg/tablet.

Inactive ingredients

  • microcrystalline cellulose
  • lactose
  • maize starch
  • sodium starch glycollate
  • povidone
  • magnesium stearate
  • colloidal anhydrous silica

Sponsor

Fareston is supplied in Australia by:

Orion Pharma (Aus) Pty Limited
Level 24, Tower 3
300 Barangaroo Avenue, Sydney,
NSW 2000, Australia
Telephone: 1800 861 913

Australian Registration Number

AUST R 59743

This leaflet was updated in July 2022.

Published by MIMS September 2022

BRAND INFORMATION

Brand name

Fareston

Active ingredient

Toremifene

Schedule

S4

 

1 Name of Medicine

Toremifene citrate.

2 Qualitative and Quantitative Composition

Each Fareston Tablet contains toremifene citrate equivalent to toremifene 60 mg.

Excipients with known effects.

Lactose.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Tablet.
Fareston Tablets are white or almost white, round, flat, uncoated tablets with bevelled edges, embossed with "TO60" on one side.

4 Clinical Particulars

4.1 Therapeutic Indications

Fareston is indicated for first line treatment of hormone dependent metastatic breast cancer in postmenopausal patients. Fareston is not recommended for patients with oestrogen receptor negative tumours.

4.2 Dose and Method of Administration

The recommended dose is one tablet (60 mg) daily.
No dose adjustment is needed in renal insufficiency. Fareston should be used cautiously in patients with hepatic impairment (see Section 5.2 Pharmacokinetic Properties, Characteristics in patients).

4.3 Contraindications

Pregnancy (see Section 4.6 Fertility, Pregnancy and Lactation, Use in pregnancy).
Pre-existing endometrial hyperplasia and severe hepatic failure are contraindications for long-term use of toremifene.
Both in preclinical investigations and in humans, changes in cardiac electrophysiology have been observed following exposure to toremifene, in the form of QT prolongation. For reasons of drug safety, toremifene is therefore contraindicated in patients with:
congenital or documented acquired QT prolongation;
electrolyte disturbances, particularly in uncorrected hypokalaemia;
clinically relevant bradycardia;
clinically relevant heart failure with reduced left-ventricular ejection fraction;
previous history of symptomatic arrhythmias.
Toremifene should not be used concurrently with other drugs that prolong the QT interval.

4.4 Special Warnings and Precautions for Use

Gynaecological examination should be performed before treatment administration, closely looking at pre-existing endometrial abnormality. Afterwards gynaecological examination should be repeated at least once a year. Patients with additional risk of endometrial cancer, e.g. patients suffering from hypertension or diabetes, having high BMI (> 30) or history of hormone replacement therapy should be closely monitored.
Anemia, leukopenia and thrombocytopenia have been reported. Red blood cell, leukocyte or platelet counts should be monitored when using Fareston.
Cases of liver injury, including elevation of liver enzymes (> 10 times upper limit of normal), hepatitis and jaundice have been reported with toremifene. Most of them occurred during the first months of treatment. The pattern of the liver damage was predominantly hepatocellular.
In clinical trials, Fareston has been shown to prolong the QT/QTc interval on the electrocardiogram in a dose-related manner. The following information regarding the effects of toremifene on QT/QTc-prolongation is of special importance (also see Section 4.3 Contraindications).
A thorough QT/QTc study was conducted in 250 healthy men to characterize the effects of toremifene on the QT/QTc interval duration. In a randomized, multiple-dose 5-arm parallel group study subjects (n = 50 per treatment group) received either placebo, moxifloxacin 400 mg or toremifene 20 mg, 80 mg, or 300 mg per day. The results of this study show that toremifene causes dose related increases in QT/QTc with a mean change from baseline in QTc of 6, 24 and 57 msec the 20 mg, 80 mg and 300 mg groups, respectively. As women tend to have a longer baseline QTc interval compared with men, they may be more sensitive to QT-prolonging medications. Elderly patients may also be more susceptible to drug-associated effects on the QT interval.
Fareston should be used with caution in patients with ongoing proarrhythmic conditions (especially elderly patients) such as acute myocardial ischaemia or QT prolongation as this may lead to an increased risk for ventricular arrhythmias (including Torsade de pointes) and cardiac arrest. If signs or symptoms that may be associated with cardiac arrhythmia occur during treatment with Fareston, treatment should be stopped and an ECG should be performed.
If the QTc interval is > 500 msec, Fareston should not be used.
Patients with non-compensated cardiac insufficiency or severe angina pectoris should be monitored closely.
Hypercalcaemia may rarely occur during the first week of treatment, especially in patients with bone metastases. They should be informed about the clinical symptoms of hypercalcaemia and closely monitored.
Patients with a history of severe thromboembolic disease should generally not be treated.
There are no clinical data available in patients with labile or poorly controlled diabetes, in patients with severely altered performance status or in patients with non-compensated cardiac insufficiency or serious angina pectoris.
Experience of the long-term use of toremifene is limited.
Patients who have known hypersensitivity to anti-oestrogens or ingredients in Fareston tablets should not take Fareston.
Fareston tablets contain lactose (30 mg/tablet). Patients with rare hereditary problems of galactose intolerance, total lactase deficiency or glucose-galactose malabsorption should not take this medicine.

Use in the elderly.

See information above on QT interval.

Paediatric use.

No data available.

Effects on laboratory tests.

No data available.

4.5 Interactions with Other Medicines and Other Forms of Interactions

No specific interaction studies have been performed.
An additive effect on QT interval prolongation between Fareston and the following drugs and other medicinal products that may prolong the QT interval cannot be excluded. This might lead to an increased risk of ventricular arrhythmias, including Torsade de pointes. Therefore, co-administration of Fareston with any of the following medicinal products is contraindicated (also see Section 4.3 Contraindications):
Antiarrhythmics class IA (e.g. quinidine, hydroquinidine, disopyramide); or
Antiarrhythmics class III (e.g. amiodarone, sotalol, dofetilide, ibutilide);
Neuroleptics (e.g. phenothiazines, pimozide, sertindole, haloperidol, sultopride);
Certain antimicrobial agents (moxifloxacin, erythromycin IV, pentamidine, antimalarials particularly halofantrine);
Certain antihistamines (terfenadine, astemizole, mizolastine);
Others (cisapride, vincamine IV, bepridil, diphemanil).
Drugs which decrease renal calcium excretion, e.g. thiazide diuretics, may increase the risk of hypercalcaemia. Enzyme inducers, like phenobarbitone, phenytoin and carbamazepine, may increase the rate of toremifene metabolism thus lowering the steady-state concentration in serum. In such cases doubling of the daily dose may be necessary.
There is a known interaction between anti-oestrogens and warfarin-type anticoagulants leading to a seriously increased bleeding time. Therefore, the concomitant use of toremifene with such medicaments should be avoided.
Theoretically there is a metabolic interaction of toremifene with drugs known to inhibit the CYP3A4-6 enzyme system. Examples of such drugs are antifungal imidazoles (ketoconazole); other antifungal agents (itraconazole, voriconazole, posaconazole); protease inhibitors (ritonavir, nelfinavir), and similar macrolide antibiotics (clarithromycin, erythromycin, telithromycin, troleandomycin). Concomitant use of those drugs with toremifene should be carefully considered.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

No data available.
(Category D)
Drugs which have caused, are suspected to have caused or may be expected to cause, an increased incidence of human fetal malformations or irreversible damage. These drugs may also have adverse pharmacological effects. Accompanying texts should be consulted for further details.
Fareston must not be administered during pregnancy (see Section 4.3 Contraindications). Toremifene is recommended for postmenopausal patients. Owing to the lack of specific data in humans, toremifene should not be used during pregnancy. In animal reproduction studies toremifene has been shown to prevent implantation, to induce parturition failures and to reduce perinatal survival. In addition, treatment during organogenesis induced changes in ossification, rib abnormalities and oedematous foetuses.
Toremifene is recommended for postmenopausal patients. Owing to the lack of specific data in humans, toremifene should not be used during lactation. In preclinical studies in rats, decreased body weight gain of the offspring during lactation was observed.

4.7 Effects on Ability to Drive and Use Machines

The effects of this medicine on a person's ability to drive and use machines were not assessed as part of its registration.

4.8 Adverse Effects (Undesirable Effects)

Adverse drug reactions are usually mild. They are mostly due to the hormonal action of toremifene.
The frequency of adverse drug reactions reported in clinical trials or spontaneously is listed below and classified according to body system.

Very common (> 10%).

Skin and appendages disorders.

Hot flushes, sweating.

Common (> 1%, < 10%).

Central and peripheral nervous system disorders.

Dizziness.

Gastrointestinal disorders.

Nausea, vomiting.

Reproductive disorders.

Leucorrhoea.

General disorders.

Oedema, pain.

Uncommon (> 0.1%, < 1%).

Skin and appendages disorders.

Pruritus, skin discolouration.

Central and peripheral nervous system disorders.

Paresis, tremor, vertigo.

Vision disorders.

Reversible corneal verticillata (reversible corneal opacity).

Psychic disorders.

Insomnia.

Gastrointestinal disorders.

Constipation.

Respiratory system disorders.

Dyspnoea.

Reproductive disorders.

Vaginal bleeding, endometrial hypertrophy.

General disorders.

Anorexia, asthenia, back pain, chest pain, fatigue, headache, weight increase, loss of appetite.

Vascular disorders.

Thromboembolic events.

Rare (> 0.01%, < 0.1%).

Skin and appendages disorders.

Alopecia, dermatitis.

Psychic disorders.

Depression, emotional lability.

Central and peripheral nervous system disorders.

Stiffness.

Hepatic disorders.

Hepatic enzyme increase, jaundice.

Metabolic disorders.

Hypercalcaemia.

Reproductive system and breast disorders.

Endometrial polyps.

Very rare (< 1/10,000), not known (cannot be estimated from the available data).

Neoplasms benign, malignant and unspecified (including cysts and polyps).

Endometrial cancer.

Hepatobiliary disorders.

Hepatitis, hepatic steatosis.

Reproductive system and breast disorders.

Endometrial hyperplasia.
Thromboembolic events have been reported, although the causal relationship to toremifene treatment remains uncertain.
Treatment was discontinued due to adverse reactions in only about 3% of patients. Most of the cases were due to nausea, vomiting, vertigo, hypercalcaemia and vaginal bleeding. Development of hypercalcaemia in the beginning of the treatment is possible especially in patients with bone metastases.
Endometrial hypertrophy may develop during the treatment due to the hormonal (partial oestrogenic) effect of toremifene. It is unknown whether long-term toremifene use is associated with an increased risk of endometrial carcinoma.
Fareston increases the QTc interval in a dose related manner (also see Section 4.4 Special Warnings and Precautions for Use).

Reporting suspected adverse effects.

Reporting suspected adverse reactions after registration of the medicinal product is important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions at http://www.tga.gov.au/reporting-problems.

4.9 Overdose

No overdose cases are known. Vertigo, headache and dizziness were observed in healthy volunteer studies at a daily dose of 680 mg. The dose-related QTc interval prolongation potential of Fareston should also be taken into account in cases of overdose. There is no specific antidote and the treatment is symptomatic.
For information on the management of overdose, contact the Poisons Information Centre on 131126 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

Mechanism of action.

Toremifene is a non-steroidal triphenylethylene derivative. Like other members of this class, e.g. tamoxifen and clomifene, toremifene binds to oestrogen receptors and may exert oestrogenic, anti-oestrogenic or both activities, depending upon the duration of treatment, animal species, gender, target organ and variable selected. In general, however, non-steroidal triphenylethylene derivatives are predominantly anti-oestrogenic in rats and man and oestrogenic in mice.
In female rats the lowest dose of toremifene that exerts an intrinsic oestrogenic effect on the uterus is about 40 times higher than that of tamoxifen. In the same model the lowest anti-oestrogenically effective dose is 10 times higher than that of tamoxifen suggesting a lower oestrogenic to anti-oestrogenic ratio for toremifene than for tamoxifen. No data are available on this ratio in humans. In post-menopausal volunteers receiving oestrogen by oral or transdermal routes, toremifene was shown to exert an anti-oestrogenic effect on vaginal mucosa by reducing the cornification index. The latter effect was reproducibly found for toremifene doses ranging from 20 to 200 mg daily and could not be distinguished from that of 20 mg tamoxifen. Lower doses of toremifene did not oppose the oestrogenic stimulation of vaginal epithelium.
Toremifene binds specifically to oestrogen receptors, competitively with oestradiol, and inhibits oestrogen-induced stimulation of DNA synthesis and cell replication. In some experimental cancers and/or using high dose, toremifene displays anti-tumour effects which are not oestrogen-dependent.
The anti-tumour effect of toremifene in breast cancer is mainly due to the anti-oestrogenic effect, although other mechanisms (changes in oncogene expression, growth factor secretion, induction of apoptosis and influence on cell cycle kinetics) may also be involved in the antitumour effect.

Clinical trials.

Three prospective, randomised, controlled clinical studies (North American 5/044, Eastern European 5/050 and Nordic 5/049) were conducted to evaluate the efficacy of Fareston for the treatment of breast cancer in postmenopausal women. The patients were randomised to parallel groups receiving Fareston 60 mg (FAR60) or tamoxifen 20 mg (TAM20) in the North American study or tamoxifen 40 mg (TAM40) in the Eastern European and Nordic studies. The North American and Eastern European studies also included high dose toremifene arms of 200 and 240 mg daily, respectively. The studies included postmenopausal patients with tumour oestrogen receptor (ER) positive or ER unknown metastatic or locally advanced breast cancer. The patients had at least one measurable or evaluable lesion. The primary efficacy variables were response rate (RR), and time to progression (TTP). Survival (S) was also determined.
The studies showed similar response rates and two of the studies showed similar times to progression. The Nordic study showed a longer time to progression with tamoxifen in the tumour ER unknown group of patients. Survival in the three studies was similar between Fareston and tamoxifen. See Table 1.
Toremifene 200 mg daily in the North American study and 240 mg daily in the Eastern European study produced, respectively, 22.6% and 28.3% response rates, 5.7 and 6.1 month median times to progression, and 30.1 and 26.0 month median survival times.

5.2 Pharmacokinetic Properties

Absorption.

Toremifene is readily absorbed after oral administration. Peak concentrations in serum are obtained within 3 (range 2-5) hours. Food intake has no effect on the extent of absorption but may delay the peak concentrations by 1.5-2 hours. The changes due to food intake are not clinically significant.

Distribution.

The serum concentration curve can be described by a biexponential equation. The half-life of the first (distribution) phase is 4 (range 2-12) hours, and of the second (elimination) phase 5 (range 2-10) days.
The basal disposition parameters (CL and V) could not be estimated due to the lack of an intravenous formulation. Toremifene binds extensively (> 99.5%) to serum proteins, mainly to albumin. Toremifene obeys linear serum kinetics at oral daily doses between 10 and 680 mg. The mean concentration of toremifene at steady state is 0.9 (range 0.6-1.3) microgram/mL at the recommended dose of 60 mg daily.

Metabolism.

Toremifene is extensively metabolised. In human serum the main metabolite is N-demethyltoremifene with mean half-life of 11 (range 4-20) days. Its steady-state concentrations are about double those of the parent compound. It has similar anti-oestrogenic, albeit weaker antitumour activity than the parent compound. It is bound to plasma proteins even more extensively than toremifene, the protein bound fraction being > 99.9%. There is no significant potential for competition between toremifene and N-demethyltoremifene in protein binding. Three minor metabolites have been detected in human serum: (deaminohydroxy)toremifene, 4-hydroxytoremifene, and N,N-didemethyltoremifene. Although they have theoretically interesting hormonal effects, their concentration during toremifene treatment are too low to have any major biological importance.

Elimination.

Toremifene is eliminated mainly as metabolites in the faeces. Enterohepatic circulation of toremifene, but not its biologically active metabolites, can be expected. About 10% of the administered dose is eliminated via urine as metabolites. Owing to the slow elimination, steady-state concentrations in serum are reached in 4 to 6 weeks.

Characteristics in patients.

Clinical anti-tumour efficacy and serum concentration have no positive correlation at the standard recommended daily dose of 60 mg.
No information is available concerning polymorphic metabolism. The enzyme complex known to be responsible for the metabolism of toremifene in humans is cytochrome P450 dependent hepatic mixed function oxidase. The main metabolic pathway, N-demethylation, is mediated mainly by CYP3A4-6.
Renal insufficiency has no influence on toremifene kinetics.
Severe hepatic failure decreases the elimination rate of toremifene. The severity of hepatic failure when measured by liver enzymes does not, however, correlate with the elimination kinetics of toremifene.

5.3 Preclinical Safety Data

Genotoxicity.

Toremifene was not genotoxic in a range of in vitro and in vivo mutagenicity, clastogenicity and DNA effect studies.

Carcinogenicity.

Toremifene was not genotoxic in a range of in vitro and in vivo mutagenicity, clastogenicity and DNA effect studies. Toremifene has not been found to be carcinogenic in rats. In mice, oestrogens induce ovarian and testicular tumours as well as hyperostosis and osteosarcomas. Toremifene has a species specific oestrogen-like effect in mice and causes similar tumours. These findings are postulated to be of little relevance for the safety in humans, where toremifene acts mainly as an anti-oestrogen.

6 Pharmaceutical Particulars

6.1 List of Excipients

Microcrystalline cellulose, lactose monohydrate, maize starch, sodium starch glycollate, povidone, magnesium stearate and colloidal anhydrous silica.

6.2 Incompatibilities

Incompatibilities were either not assessed or identified as part of the registration of this medicine.

6.3 Shelf Life

3 years.

6.4 Special Precautions for Storage

Store below 25°C.

6.5 Nature and Contents of Container

Blister (PVC/Al) pack containing 30 tablets.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of by taking to your local pharmacy.

6.7 Physicochemical Properties

Chemical structure.


Toremifene citrate is a white or almost white crystalline powder. It is (Z)-4-Chloro-1,2-diphenyl-1-{4-[2-(N,N-dimethylamino) ethoxy] phenyl}-1-butene citrate.
The molecular formula is C32H36ClNO8. MW: 598.1.

CAS number.

Toremifene citrate [89778-27-8].

7 Medicine Schedule (Poisons Standard)

S4: Prescription Only Medicine.

Summary Table of Changes