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Medicine information : FEMARA Film-coated Tablets
| Drug class description : | Non-steroidal aromatase inhibitor (inhibitor of oestrogen biosynthesis); antineoplastic agent |
| Generic Name : | Letrozole |
| Drug description : | Film-coated tablets. |
| Presentation : | Active substance: 4, 4'-[(1H-1, 2, 4-triazol-1-yl)-methylene]bis-benzonitrile (INN/USAN= letrozole). Each film-coated tablet contains 2.5 mg letrozole. |
| Indications : | Adjuvant treatment of postmenopausal women with hormone receptor positive invasive early breast cancer. Treatment of early invasive breast cancer in postmenopausal women who have received prior standard adjuvant tamoxifen therapy. First-line treatment in postmenopausal women with advanced breast cancer. Advanced breast cancer in postmenopausal women in whom tamoxifen or other anti-oestrogen therapy has failed. Pre-operative therapy in postmenopausal women with localised hormone receptor positive breast cancer, to allow subsequent breast-conserving surgery in women not originally considered candidates for breast-conserving surgery. Subsequent treatment after surgery should be in accordance with standard of care. |
| Adult Dosage : | Adult and elderly patients The recommended dose of Femara is 2.5 mg once daily. In the adjuvant setting, treatment with Femara should continue for 5 years or until tumour relapse occurs, whichever comes first. Following standard adjuvant tamoxifen therapy, treatment with Femara should continue for 3 years or until tumour relapse occurs, whichever comes first. Currently there is a lack of long-term data, therefore the optimal duration of therapy has not yet been established. In patients with metastatic disease, treatment with Femara should continue until tumour progression is evident. Regular monitoring to observe progression during the pre-operative treatment period is recommended. No dose adjustment is required for elderly patients. Patients with hepatic and/or renal impairment No dosage adjustment is required for patients with mild to moderate hepatic impairment (Child-Pugh grade A and B) or renal impairment (creatinine clearance 10 mL/min.). |
| Child Dosage : | Not recommended for use in children |
| Elderly Dosage : | See Adult Dosage |
| Contra Indications : | Hypersensitivity to the active substance or to any of the excipients. Premenopausal, pregnant or lactating women (See Interactions). Patients with severe hepatic impairment (Child-Pugh grade C). Pre-operative use of letrozole is contraindicated if the receptor status is negative or unknown. |
| Special Precautions : | Femara is not recommended for use in children as efficacy and safety in this patient group have not been assessed in clinical studies. There are no efficacy data to support the use of Femara in men with breast cancer. Femara has not been investigated in patients with creatinine clearance < 10 mL/min. The potential risk/benefit to such patients should be carefully considered before administration of Femara. As Femara is a potent oestrogen lowering agent, reductions in bone mineral density can be anticipated. The impact of Femara on long-term fracture risk remains undetermined. During adjuvant treatment with Femara, women with osteoporosis or at risk of osteoporosis should have their bone mineral density formally assessed by bone densitometry e.g. DEXA scanning at the commencement of treatment. Although adequate data to show the effects of therapy in the treatment of the bone mineral density loss caused by Femara are not available, treatment for osteoporosis should be initiated as appropriate and patients treated with Femara should be carefully monitored. |
| Interactions : | Clinical interaction studies with cimetidine and warfarin indicated that the coadministration of Femara with these drugs does not result in clinically significant drug interactions, even though cimetidine is a known inhibitor of one of the cytochrome P450 isoenzymes capable of metabolising letrozole in vitro. There was no evidence of other clinically relevant interaction in patients receiving other commonly prescribed drugs (e.g. benzodiazepines; barbiturates; NSAIDs such as diclofenac sodium, ibuprofen; paracetamol; furosemide; omeprazole). There is no clinical experience to date on the use of Femara in combination with other anti-cancer agents. Letrozole inhibits in vitro the cytochrome P450-isoenzymes 2A6 and moderately 2C19, however, CYP2A6 does not play a major role in drug metabolism. In in vitro experiments letrozole was not able to substantially inhibit the metabolism of diazepam (a substrate of CYP2C19) at concentrations approximately 100-fold higher than those observed in plasma at steady-state. Thus, clinically relevant interactions with CYP2C19 are unlikely to occur. Nevertheless, caution should be used in the concomitant administration of drugs whose disposition is mainly dependent on these isoenzymes and whose therapeutic index is narrow. Pregnancy: Femara is contraindicated during pregnancy (See Contraindications). Lactation: Femara is contraindicated during lactation (See Contraindications). Women of child-bearing potential The physician needs to discuss the necessity of adequate contraception with women who have the potential to become pregnant including women who are perimenopausal or who have recently become postmenopausal, until their postmenopausal status is fully established. There are no adequate data from the use of Femara in pregnant women. Embryotoxicity and foetotoxicity were seen in pregnant rats following oral administration of Femara, and there was an increase in the incidence of foetal malformation among the animals treated. However, it is not known whether this was an indirect consequence of the pharmacological activity of Femara (inhibition of oestrogen biosynthesis) or a direct drug effect. |
| Adverse Reactions : | Femara was generally well tolerated across all studies as first-line and second-line treatment for advanced breast cancer, as adjuvant treatment of early breast cancer as well as in the treatment of women who have received prior standard tamoxifen therapy. Approximately one third of the patients treated with Femara in the metastatic and neoadjuvant settings, approximately 70-75% of the patients in the adjuvant setting (both Femara and tamoxifen arms), and approximately 40% of the patients treated following standard adjuvant tamoxifen (both Femara and placebo arms) experienced adverse reactions. Generally, the observed adverse reactions are mainly mild or moderate in nature, and most are associated with oestrogen deprivation. The most frequently reported adverse reactions in the clinical studies were hot flushes, arthralgia, nausea and fatigue. Many adverse reactions can be attributed to the normal pharmacological consequences of oestrogen deprivation (e.g. hot flushes, alopecia and vaginal bleeding). After standard adjuvant tamoxifen, the following adverse events irrespective of causality were reported significantly more often with Femara than with placebo – hot flushes (49.7 % vs. 43.3 %), arthralgia/arthritis (27.7 % vs. 22.2 %) and myalgia (9.5 % vs. 6.7 %). The majority of these adverse events were observed during the first year of treatment. The incidence of self-reported osteoporosis was higher in patients who received Femara than in patients who received placebo (6.9 % vs. 5.5 %). The incidence of clinical fractures was only slightly higher in patients who received Femara than in placebo patients (5.9 % vs. 5.5 %). The fracture rate per 1000-women years in the letrozole group (24.6) is in the range of aged-matched postmenopausal healthy women. The following adverse drug reactions, listed below, were reported from clinical studies and from post marketing experience with Femara. Adverse reactions are ranked under headings of frequency, the most frequent first, using the following convention: very common = 10%; common = 1% to < 10%; uncommon = 0.1% to < 1%; rare = 0.01% to < 0.1%; very rare < 0.01%, including isolated report. Infections and infestations - Uncommon: Urinary tract infection. Neoplasms, benign, malignant and unspecified (including cysts and polyps) - Uncommon: Tumour pain (6) Blood and the lymphatic system disorders - Uncommon: Leucopenia. Metabolism and nutrition disorders - Common: Anorexia, appetite increase, raised serum cholesterol, Uncommon: General oedema. Psychiatric disorders - Common: Depression, Uncommon: Anxiety (1). Nervous system disorders - Common: Headache, dizziness, Uncommon: Somnolence, insomnia, memory impairment, dysaesthesia (2) , taste disturbance, Cerebrovascular accident Eye disorders - Uncommon: Cataract, eye irritation, blurred vision. Cardiac disorders - Uncommon: Palpitations, tachycardia Vascular disorders - Uncommon: Thrombophlebitis (3) , hypertension, ischemic cardiac events (7), Rare: Pulmonary embolism, arterial thrombosis, cerebrovascular infarction Respiratory, thoracic and mediastinal disorders - Uncommon: Dyspnoea, cough Gastrointestinal disorders - Common: Nausea, vomiting, dyspepsia, constipation, diarrhoea, Uncommon: Abdominal pain, stomatitis, dry mouth Hepatobiliary disorders - Uncommon: Increased hepatic enzymes Skin and subcutaneous tissue disorders - Common: Alopecia, increased sweating, rash (4), Uncommon: Pruritus, dry skin, urticaria Musculoskeletal and connective tissue disorders - Very common: Arthralgia, Common: Myalgia, bone pain, osteoporosis, bone fractures, Uncommon: Arthritis Renal and urinary disorders - Uncommon: Increased urinary frequency Reproductive system and breast disorders - Uncommon: Vaginal bleeding, vaginal discharge, vaginal dryness, breast pain General disorders and administration site conditions - Very common: Hot flushes, Common: Fatigue (5) , peripheral oedema, Uncommon: Pyrexia, mucosal dryness, thirst Investigations - Common: Weight increase, Uncommon: Weight loss, *Including: (1) including nervousness, irritability (2) including paraesthesia, hypoaesthesia (3) including superficial and deep thrombophlebitis (4) including erythematous, maculopapular, psoriaform and vesicular rash (5) including aesthenia and malaise (6) in metastatic/neoadjuvant setting only (7) in the adjuvant setting, irrespective of causality, the following adverse events occurred in the Femara and tamoxifen groups respectively: thromboembolic events (1.2% vs. 3.0%), angina pectoris (0.8% vs. 0.8%), myocardial infarction (0.5% vs. 0.4%), cardiac failure (0.8% vs. 0.3%). 1 Based on number of patients with normal serum cholesterol levels at baseline, and developing at least one value greater than 1.5 times the upper limit of normal in the laboratory measuring total serum cholesterol. Approximately 90% of the measured values were non-fasting measurements. 2 Denominator is number of patients with baseline measurements of total serum cholesterol – letrozole, n=3207; tamoxifen, n=3228 3 Denominator is number of patients not having undergone hysterectomy at baseline – letrozole, n=3090; tamoxifen, n=3157 |
| Manufacturer : | Novartis |
| Drug Availability : | (POM) |
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