Presentation and Status in Health Basket
30 X 25 mg
Adult and elderly patients: The recommended dose of Aromasin is one 25 mg tablet to be taken once daily, preferably after a meal. In patients with early breast cancer, treatment with Aromasin should continue until completion of five years of adjuvant endocrine therapy, or until local or distant recurrence or new contralateral breast cancer.In patients with advanced breast cancer, treatment with Aromasin should continue until tumour progression is evident. No dose adjustments are required for patients with hepatic or renal insufficiency.
Children: Not recommended for use in children.
Advanced breast cancer (ABC) in women with natural/induced post-menopausal status (progressed following anti-estrogen therapy alone) and in post-menopausal women (progressed following multiple hormonal therapies). For the adjuvant treatment of postmenopausal women with estrogen receptor positive invasive early breast cancer, following 2-3 years of initial adjuvant tamoxifen therapy.
Aromasin tablets are contraindicated in patients with a known hypersensitivity to the active substance or to any of the excipients and in pre-menopausal women and in pregnant or lactating women.
Aromasin should not be administered to women with pre-menopausal endocrine status. Therefore, whenever clinically appropriate, the post-menopausal status should be ascertained by assessment of LH, FSH and oestradiol levels. Aromasin should be used with caution in patients with hepatic or renal impairment. Aromasin should not be coadministered with estrogen-containing medicines as these would negate its pharmacological action. As Aromasin is a potent estrogen lowering agent, reductions in bone mineral density (BMD) can be anticipated. During adjuvant treatment with Aromasin, women with osteoporosis or at risk of osteoporosis should have their bone mineral density formally assessed by bone densitometry at the commencement of treatment. Patients treated with Aromasin should be carefully monitored and treatment for osteoporosis should be initiated as appropriate. Routine assessment of 25 hydroxy vitamin D levels prior to the start of aromatase inhibitor treatment should be considered, due to the high prevalence of severe deficiency associated in women with early breast cancer (EBC). Women with Vitamin D deficiency should receive supplementation with Vitamin D.
Clinical Trials: Exemestane was generally well tolerated across all studies and in the clinical studies, conducted with exemestane 25mg/day, adverse events were usually mild to moderate.
The discontinuation rate due to adverse events in studies was 7.4% in patients with early breast cancer receiving adjuvant treatment with exemestane following initial adjuvant tamoxifen therapy. The most commonly reported adverse reactions were hot flushes (22%), arthralgia (18%), and fatigue (16%). The discontinuation rate due to adverse events was 2.8% in the overall patient population with advanced breast cancer.
The most commonly reported adverse reactions were hot flushes (14%) and nausea (12%). Most adverse reactions can be attributed to the normal pharmacological consequences of estrogen deprivation (e.g., hot flushes). The reported adverse reactions are listed below by MedDRA System Organ Class and by frequency. Frequencies are defined as: very common (>10%), common (>1%, ≤ 10%), uncommon (> 0.1%, ≤ 1%), rare (> 0.01%, ≤ 0.1%).
Metabolism and nutrition disorders: Common: Anorexia
Psychiatric disorders: Very common: Insomnia Common: Depression
Nervous system disorders: Very common: Headache Common: Dizziness, carpal tunnel syndrome Uncommon: Somnolence
Vascular disorders: Very common: Hot flushes
Gastrointestinal disorders: Very common: Nausea Common: Abdominal pain, vomiting, constipation, dyspepsia, diarrhea.
For full details see prescribing information.
In vitro evidence showed that the drug is metabolised through cytochrome P450 (CYP) 3A4 and aldoketoreductases and does not inhibit any of the major CYP isoenzymes. In a clinical pharmacokinetic study, the specific inhibition of CYP 3A4 by ketoconazole showed no significant effects on the pharmacokinetics of exemestane. CYP 3A4 is likely to catalyse a minor pathway in the metabolism of exemestane, however, a possible decrease of exemestane plasma levels by known inducers of CYP 3A4 cannot be excluded. Although pharmacokinetic effects were observed in a pharmacokinetic interaction study with rifampicin, a potent CYP3A4 inducer, the pharmacologic activity (i.e., estrogen suppression) was not affected, and a dosage adjustment is not required.Aromasin should be used cautiously with drugs that are metabolised via CYP3A4 and have a narrow therapeutic window. There is no clinical experience of the concomitant use of Aromasin with other anticancer drugs.
Pregnancy and Lactation
Women should not use Aromasin during pregnancy because it may cause harm to the fetus. In animal reproductive studies, Aromasin demonstrated some toxic effects. Aromasin should not be used in women who are lactating.
Clinical trials have been conducted with Aromasin given up to 800 mg in a single dose to healthy female volunteers and up to 600 mg daily to postmenopausal women with advanced breast cancer; these dosages were well tolerated. In rats and dogs, lethality was observed after single oral doses equivalent respectively to 2000 and 4000 times the recommended human dose on a mg/m2 basis. There is no specific antidote to overdose and treatment must be symptomatic.