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Exemestane is a brand name for Exemestane. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: 1 INDICATIONS AND USAGE Exemestane tablets are an aromatase inhibitor indicated for: adjuvant treatment of postmenopausal women with estrogen-receptor positive early breast cancer who have received two to three years of tamoxifen and are switched to exemestane tablets for completion of a total of five consecutive…
Verbatim from this product's FDA label. Tap a section to expand.
1 ). 1 Recommended Dose The recommended dose of exemestane tablets in early and advanced breast cancer is one 25 mg tablet once daily after a meal. adjuvant treatment of postmenopausal women with estrogen-receptor positive early breast cancer who have received two to three years of tamoxifen and are switched to exemestane tablets for completion of a total of five consecutive years of adjuvant hormonal therapy.
the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy. 2 Dose Modifications Concomitant use of strong CYP 3A4 inducers decreases exemestane exposure. 3) ].
1) ] Early breast cancer: Adverse reactions occurring in ≥10% of patients in any treatment group (exemestane tablets vs. tamoxifen) were hot flushes (21% vs. 20%), fatigue (16% vs. 15%), arthralgia (15% vs. 9%), headache (13% vs. 11%), insomnia (12% vs.
9%), and increased sweating (12% vs. 10%). Discontinuation rates due to AEs were similar between exemestane tablets and tamoxifen (6% vs. 5%). 6%. 1 ).
Advanced breast cancer:
Most common adverse reactions were mild to moderate and included hot flushes (13% vs. 5%), nausea (9% vs. 5%), fatigue (8% vs. 10%), increased sweating (4% vs. 8%), and increased appetite (3% vs. 1 ). To report SUSPECTED ADVERSE REACTIONS, contact Breckenridge Pharmaceutical, Inc.
gov/medwatch. 1 Clinical Trial Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.
Adjuvant Therapy The data described below reflect exposure to exemestane tablets in 2325 postmenopausal women with early breast cancer. 1) ] and the 027 study (a randomized, placebo-controlled, double-blind, parallel group study specifically designed to assess the effects of exemestane on bone metabolism, hormones, lipids, and coagulation factors over 2 years of treatment).
9 months for patients receiving exemestane tablets or placebo within the 027 study. 6 months. Median duration of observation was 30 months for both groups in the 027 study. Certain adverse reactions, which were expected based on the known pharmacological properties and side effect profiles of test drugs, were actively sought through a positive checklist.
1 ). 2 ).
Embryo-Fetal Toxicity:
Can cause fetal harm. 3 ). 1 Reductions in Bone Mineral Density (BMD) Reductions in bone mineral density (BMD) over time are seen with exemestane use. Table 1 describes changes in BMD from baseline to 24 months in patients receiving exemestane compared to patients receiving tamoxifen (IES) or placebo (027).
Concomitant use of bisphosphonates, vitamin D supplementation, and calcium was not allowed. Table 1. Percent Change in BMD from Baseline to 24 months, Exemestane vs. 6 During adjuvant treatment with exemestane, women with osteoporosis or at risk of osteoporosis should have their bone mineral density formally assessed by bone densitometry at the commencement of treatment.
Monitor patients for bone mineral density loss and treat as appropriate. 2 Vitamin D Assessment Routine assessment of 25-hydroxy vitamin D levels prior to the start of aromatase inhibitor treatment should be performed, due to the high prevalence of vitamin D deficiency in women with early breast cancer (EBC).
Women with vitamin D deficiency should receive supplementation with vitamin D. 3 Administration with Estrogen-Containing Agents Exemestane tablets should not be coadministered with systemic estrogen-containing agents as these could interfere with its pharmacologic action.
4 Laboratory Abnormalities In patients with early breast cancer, the incidence of hematological abnormalities of Common Toxicity Criteria (CTC) grade ≥1 was lower in the exemestane treatment group, compared with tamoxifen. 1%) in both treatment groups.
Approximately 20% of patients receiving exemestane in clinical studies in advanced breast cancer experienced CTC grade 3 or 4 lymphocytopenia. Of these patients, 89% had a pre-existing lower grade lymphopenia. Forty percent of patients either recovered or improved to a lesser severity while on treatment.
4 CONTRAINDICATIONS Exemestane tablets are contraindicated in patients with a known hypersensitivity to the drug or to any of the excipients. Patients with a known hypersensitivity to the drug or to any of the excipients ( 4 ).
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Signs and symptoms were graded for severity using CTC in both studies. Within the IES study, the presence of some illnesses/conditions was monitored through a positive checklist without assessment of severity. These included myocardial infarction, other cardiovascular disorders, gynecological disorders, osteoporosis, osteoporotic fractures, other primary cancer, and hospitalizations.
1% of patients receiving exemestane or placebo respectively within study 027. 4% of the tamoxifen treated patients within the IES study. There were 6 deaths due to stroke on the exemestane arm compared to 2 on tamoxifen. There were 5 deaths due to cardiac failure on the exemestane arm compared to 2 on tamoxifen.
6% in tamoxifen treated patients in the IES study. 3% of tamoxifen treated patients. In the adjuvant treatment of early breast cancer, the most common adverse reactions occurring in ≥10% of patients in any treatment group (exemestane tablets vs.
tamoxifen) were hot flushes (21% vs. 20%), fatigue (16% vs. 15%), arthralgia (15% vs. 9%), headache (13% vs. 11%), insomnia (12% vs. 9%), and increased sweating (12% vs. 10%). Discontinuation rates due to AEs were similar between exemestane tablets and tamoxifen (6% vs.
5%). 6%. 3%. Treatment-emergent adverse reactions and illnesses including all causalities and occurring with an incidence of ≥5% in either treatment group of the IES study during or within one month of the end of treatment are shown in Table 2.
Table 2. Incidence (%) of Adverse Reactions of all Grades Graded according to Common Toxicity Criteria; and Illnesses Occurring in (≥5%) of Patients in Any Treatment Group in Study IES in Postmenopausal Women with Early Breast Cancer % of patients Body system and Adverse Reaction by MedDRA dictionary Exemestane Tablets 25 mg daily (N=2252) Tamoxifen 20 mg daily 75 patients received tamoxifen 30 mg daily; (N=2280) Eye Visual disturbances Event actively sought.
6% vs. 3% vs. 6% vs. 4% vs. 6% vs. 1%]). 2% vs. 2%). 1%). 7% vs. 1%). The majority of patients on exemestane tablets with gastric ulcer received concomitant treatment with non-steroidal anti-inflammatory agents and/or had a prior history. 1% vs.
0% vs. 7% vs. 4% vs. 4%]. Common adverse reactions occurring in study 027 are described in Table 3. Table 3. 1 Edema 6 7 Treatment of Advanced Breast Cancer A total of 1058 patients were treated with exemestane 25 mg once daily in the clinical trials program.
One death was considered possibly related to treatment with exemestane; an 80-year-old woman with known coronary artery disease had a myocardial infarction with multiple organ failure after 9 weeks on study treatment. 7% of patients discontinued exemestane within the first 10 weeks of treatment.
In the comparative study, adverse reactions were assessed for 358 patients treated with exemestane tablets and 400 patients treated with megestrol acetate. Fewer patients receiving exemestane tablets discontinued treatment because of adverse reactions than those treated with megestrol acetate (2% vs.
5%). Adverse reactions that were considered drug related or of indeterminate cause included hot flashes (13% vs. 5%), nausea (9% vs. 5%), fatigue (8% vs. 10%), increased sweating (4% vs. 8%), and increased appetite (3% vs. 6%) for exemestane tablets and megestrol acetate, respectively.
The proportion of patients experiencing an excessive weight gain (>10% of their baseline weight) was significantly higher with megestrol acetate than with exemestane tablets (17% vs. 8%). In the treatment of advanced breast cancer, the most common adverse reactions included hot flushes (13% vs.
5%), nausea (9% vs. 5%), fatigue (8% vs. 10%), increased sweating (4% vs. 8%), and increased appetite (3% vs. 6%) for exemestane tablets and megestrol acetate, respectively. Table 4 shows the adverse reactions of all CTC grades, regardless of causality, reported in 5% or greater of patients in the study treated either with exemestane tablets or megestrol acetate.
Table 4. Incidence (%) of Adverse Reactions of all Grades Graded according to Common Toxicity Criteria and Causes Occurring in ≥5% of Advanced Breast Cancer Patients In Each Treatment Arm in the Comparative Study Body system and Adverse Reaction by WHO ART dictionary Exemesane Tablets 25 mg once daily (N=358) Megestrol Acetate 40 mg QID (N=400) Autonomic Nervous Increased sweating 6 9 Body as a Whole Fatigue 22 29 Hot flashes 13 6 Pain 13 13 Influenza-like symptoms 6 5 Edema (includes edema, peripheral edema, leg edema) 7 6 Cardiovascular Hypertension 5 6 Nervous Depression 13 9 Insomnia 11 9 Anxiety 10 11 Dizziness 8 6 Headache 8 7 Gastrointestinal Nausea 18 12 Vomiting 7 4 Abdominal pain 6 11 Anorexia 6 5 Constipation 5 8 Diarrhea 4 5 Increased appetite 3 6 Respiratory Dyspnea 10 15 Coughing 6 7 Adverse reactions of any cause (from 2% to 5%) reported in the comparative study for patients receiving exemestane tablets 25 mg once daily were fever, generalized weakness, paresthesia, pathological fracture, bronchitis, sinusitis, rash, itching, urinary tract infection, and lymphedema.
Additional adverse reactions of any cause observed in the overall clinical trials program (N = 1058) in 5% or greater of patients treated with exemestane 25 mg once daily but not in the comparative study included pain at tumor sites (8%), asthenia (6%), and fever (5%).
Adverse reactions of any cause reported in 2% to 5% of all patients treated with exemestane 25 mg in the overall clinical trials program but not in the comparative study included chest pain, hypoesthesia, confusion, dyspepsia, arthralgia, back pain, skeletal pain, infection, upper respiratory tract infection, pharyngitis, rhinitis, and alopecia.
2 Post-Marketing Experience The following adverse reactions have been identified during post approval use of exemestane tablets. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Immune system disorders - hypersensitivity Hepatobiliary disorders - hepatitis including cholestatic hepatitis Nervous system disorders- paresthesia Musculoskeletal and connective tissue disorder- tenosynovitis stenosans Skin and subcutaneous tissue disorders- acute generalized exanthematous pustulosis, urticaria, pruritus
Patients did not have a significant increase in viral infections, and no opportunistic infections were observed. , ≥ CTC grade 3) have been rarely reported in patients treated for advanced breast cancer but appear mostly attributable to the underlying presence of liver and/or bone metastases.
8% of patients treated with megestrol acetate. In patients with early breast cancer, elevations in bilirubin, alkaline phosphatase, and creatinine were more common in those receiving exemestane than either tamoxifen or placebo. 8% of tamoxifen patients on the Intergroup Exemestane Study (IES), and in 7% of exemestane treated patients vs.
0% of placebo treated patients in the 027 study. 1% of tamoxifen treated patients. 6% of tamoxifen treated patients, and in 14% of exemestane treated patients compared to 7% of placebo treated patients in study 027. 3% of tamoxifen treated patients on the IES and in 6% of exemestane treated patients and 0% of placebo treated patients in study 027.
5 Use in Premenopausal Women Exemestane tablets are not indicated for the treatment of breast cancer in premenopausal women. 6 Embryo-Fetal Toxicity Based on findings from animal studies and its mechanism of action, exemestane tablets can cause fetal harm when administered to a pregnant woman.
In animal reproduction studies, administration of exemestane to pregnant rats and rabbits caused increased incidence of abortions and embryo-fetal toxicity. Advise pregnant women of the potential risk to a fetus. 1) ] .