EXEMESTANE 25 mg Tablet, Sugar Coated, 30-count
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Aromatase Inhibitor class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Exemestane is used to treat early breast cancer in women who have experienced menopause ('change of life'; end of monthly menstrual periods) and who have already been treated with a medication called tamoxifen (Nolvadex) for 2 to 3 years. This medication is also used to treat breast cancer in women who have experienced menopause whose breast cancer has worsened while they were taking tamoxifen. Exemestane is in a class of medications called aromatase inhibitors. It works by decreasing the amount of estrogen produced by the body. This can slow or stop the growth of some breast tumors that need...
Read the full MedlinePlus article ↗- Exemestane works by permanently switching off an enzyme called aromatase, which your body uses to make estrogen after menopause. Many breast cancer cells depend on estrogen to grow...
- What exactly is exemestane doing for my breast cancer?
- Yes, it really does matter. Taking exemestane after a meal — especially one with some fat in it — significantly improves how much of the drug your body actually absorbs. Make it a...
- The most common side effects are hot flushes, joint pain, fatigue, headache, trouble sleeping, and increased sweating — these tend to be mild to moderate for most women. You should...
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Supplement & herbal interactions
Some supplements/herbs that may interact with Exemestane — tap one for details:
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💊 What it looks like
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $0.718 | $21.53 / 30 tablets |
| Medicaid paysCMS SDUD · 12 mo | $1.11 | $33.30 / 30 tablets |
| Medicare drug plans payPart D · Q2 2026 | $1.36 | $40.84 / 30 tablets |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Exemestane 25 mg 00832-0595-30 | Upsher-Smith | 30 tablets | $0.718 | AB | Availability likely | — |
| Exemestane 25 mg 51991-0005-90 | Breckenridge | 90 tablets | $0.718 | AB | Availability likely | — |
| Exemestane 25 mg 59651-0516-30 | Aurobindo | 30 tablets | $0.718 | AB | Availability likely | — |
| Exemestane 25 mgthis 59762-2858-01 | Mylan | 30 tablets | $0.718 | AB | Availability likely | — |
| Exemestane 25 mg 68382-0383-06 | Zydus | 30 tablets | $0.718 | AB | Availability likely | — |
| Exemestane 25 mg 69097-0316-02 | Cipla | 30 tablets | $0.718 | AB | Availability likely | — |
| Exemestane 25 mg 71921-0190-33 | Florida | 30 tablets | $0.718 | AB | Availability likely | — |
| Exemestane 25 mg 72603-0329-01 | NorthStar | 30 tablets | $0.718 | AB | Availability likely | — |
| Aromasin 25 mg 00009-7663-04 | Pharmacia | 30 tablets | $38.979 | AB | Availability likely | +5331% |
| Exemestane 25 mg 63629-2056-01 | Bryant | 30 tablets | — | AB | FDA listed | — |
| Exemestane 25 mg 70771-1374-03 | Zydus | 30 tablets | — | AB | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
FDA-approved generic versions are listed, and recent pricing/market data suggests they may be available — see Therapeutic equivalents.
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🗺️ Medicaid utilization & spend
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
🔬 Reported adverse events (FAERS)
Top reported reactions
Age at onset
Reporter sex
Serious outcomes
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 59762-2858-01 You're viewing this | 30 TABLET, SUGAR COATED in 1 BOTTLE (59762-2858-1) | 2011-04-01 | Active |
📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE EXEMESTANE is 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 for completion of a total of five consecutive years of adjuvant hormonal therapy ( 14.1 ). • treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy ( 14.2 ).
1.1Adjuvant Treatment of Postmenopausal Women EXEMESTANE is 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 for completion of a total of five consecutive years of adjuvant hormonal therapy [see Clinical Studies (14.1) ].
1.2Advanced Breast Cancer in Postmenopausal Women EXEMESTANE is indicated for the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy [see Clinical Studies (14.2) ].
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Recommended Dose: One 25 mg tablet once daily after a meal ( 2.1 ).
2.1Recommended Dose The recommended dose of EXEMESTANE 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 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.
2.2Dose Modifications Concomitant use of strong CYP 3A4 inducers decreases exemestane exposure, For patients receiving EXEMESTANE with a strong CYP 3A4 inducer such as rifampicin or phenytoin, the recommended dose of EXEMESTANE is 50 mg once daily after a meal. [see Drug Interactions (7) and Clinical Pharmacology (12.3) ]
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS EXEMESTANE tablets are round, biconvex, off-white to slightly greyish sugar-coated tablets, about 6 mm diameter, printed with numbers 2858 on one side in black ink. Each tablet contains 25 mg of exemestane. Tablets: 25 mg ( 3 ).
⛔ Contraindications ▾
4 CONTRAINDICATIONS EXEMESTANE is 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 ).
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS • Reductions in bone mineral density (BMD) over time are seen with exemestane use ( 5.1 ). • Routine assessment of 25-hydroxy vitamin D levels prior to the start of aromatase inhibitor treatment should be performed ( 5.2 ). • Embryo-Fetal Toxicity: Can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception ( 5.6 , 8.1 , 8.3 ).
5.1Reductions 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. Control 1 IES 027 BMD Exemestane N=29 Tamoxifen 1 N=38 Exemestane N=59 Placebo 1 N=65 Lumbar spine (%) -3.1 -0.2 -3.5 -2.4 Femoral neck (%) -4.2 -0.3 -4.6 -2.6 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.
5.2Vitamin 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.
5.3Administration with Estrogen-Containing Agents EXEMESTANE should not be coadministered with systemic estrogen-containing agents as these could interfere with its pharmacologic action.
5.4Laboratory 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. Incidence of CTC grade 3 or 4 abnormalities was low (approximately 0.1%) 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. Patients did not have a significant increase in viral infections, and no opportunistic infections were observed.
Elevations of serum levels of AST, ALT, alkaline phosphatase, and gamma glutamyl transferase >5 times the upper value of the normal range (i.e., ≥ 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. In the comparative study in advanced breast cancer patients, CTC grade 3 or 4 elevation of gamma glutamyl transferase without documented evidence of liver metastasis was reported in 2.7% of patients treated with EXEMESTANE and in 1.8% 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. Treatment-emergent bilirubin elevations (any CTC grade) occurred in 5% of exemestane patients and 0.8% 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.
CTC grade 3–4 increases in bilirubin occurred in 0.9% of exemestane treated patients compared to 0.1% of tamoxifen treated patients. Alkaline phosphatase elevations of any CTC grade occurred in 15% of exemestane treated patients on the IES compared to 2.6% of tamoxifen treated patients, and in 14% of exemestane treated patients compared to 7% of placebo treated patients in study 027. C…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: • Reductions in Bone Mineral Density (BMD) [see Warnings and Precautions (5.1) ] • Early breast cancer: Adverse reactions occurring in ≥10% of patients in any treatment group (EXEMESTANE 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 and tamoxifen (6% vs. 5%).
Incidences of cardiac ischemic events (myocardial infarction, angina, and myocardial ischemia) were EXEMESTANE 1.6%, tamoxifen 0.6%. Incidence of cardiac failure: EXEMESTANE 0.4%, tamoxifen 0.3% ( 6 , 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.
6%) for EXEMESTANE and megestrol acetate, respectively ( 6 , 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Greenstone LLC at 1-877-446-3679 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
6.1Clinical 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 in 2325 postmenopausal women with early breast cancer. EXEMESTANE tolerability in postmenopausal women with early breast cancer was evaluated in two well-controlled trials: the IES study [see Clinical Studies (14.1) ] 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).
The median duration of adjuvant treatment was 27.4 months and 27.3 months for patients receiving EXEMESTANE or tamoxifen, respectively, within the IES study and 23.9 months for patients receiving EXEMESTANE or placebo within the 027 study. Median duration of observation after randomization for EXEMESTANE was 34.5 months and for tamoxifen was 34.6 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. 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. Within the IES study, discontinuations due to adverse reactions occurred in 6% and 5% of patients receiving EXEMESTANE and tamoxifen, respectively, and in 12% and 4.1% of patients receiving EXEMESTANE or placebo respectively within study 027. Deaths due to any cause were reported for 1.3% of the exemestane treated patients and 1.4% 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. The incidence of cardiac ischemic events (myocardial infarction, angina, and myocardial ischemia) was 1.6% in exemestane treated patients and 0.6% in tamoxifen treated patients in the IES study.
Cardiac failure was observed in 0.4% of exemestane treated patients and 0.3% of tamoxifen treated patients. In the adjuvant treatment of early breast cancer, the most common adverse reactions occur…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Strong CYP 3A4 inducers: Concomitant use of strong CYP 3A4 inducers decreases exemestane exposure. Increase the EXEMESTANE dose to 50 mg ( 2.2 , 7 ). Drugs That Induce CYP 3A4 Co-medications that induce CYP 3A4 (e.g., rifampicin, phenytoin, carbamazepine, phenobarbital, or St.
John's wort) may significantly decrease exposure to EXEMESTANE. Dose modification is recommended for patients who are also receiving a strong CYP 3A4 inducer [see Dosage and Administration (2.2) and Clinical Pharmacology (12.3) ] .
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Lactation: Advise not to breastfeed ( 8.2 ).
8.1Pregnancy Risk Summary Based on findings in animal studies and its mechanism of action , EXEMESTANE can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1) ] . Limited human data from case reports are insufficient to inform a drug-associated risk. In animal reproduction studies, administration of exemestane to pregnant rats and rabbits caused increased incidence of abortions, embryo-fetal toxicity, and prolonged gestation with abnormal or difficult labor [see Data ] .
Advise pregnant women of the potential risk to a fetus. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the US general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2–4% and 15–20%, respectively.
Data Animal Data In animal reproduction studies in rats and rabbits, exemestane caused embryo-fetal toxicity, and was abortifacient. Radioactivity related to 14 C-exemestane crossed the placenta of rats following oral administration of 1 mg/kg exemestane. The concentration of exemestane and its metabolites was approximately equivalent in maternal and fetal blood.
When rats were administered exemestane from 14 days prior to mating until either days 15 or 20 of gestation, and resuming for the 21 days of lactation, an increase in placental weight was seen at 4 mg/kg/day (approximately 1.5 times the recommended human daily dose on a mg/m2 basis). Increased resorptions, reduced number of live fetuses, decreased fetal weight, retarded ossification, prolonged gestation and abnormal or difficult labor was observed at doses equal to or greater than 20 mg/kg/day (approximately 7.5 times the recommended human daily dose on a mg/m 2 basis).
Daily doses of exemestane, given to rabbits during organogenesis, caused a decrease in placental weight at 90 mg/kg/day (approximately 70 times the recommended human daily dose on a mg/m 2 basis) and in the presence of maternal toxicity, abortions, an increase in resorptions, and a reduction in fetal body weight were seen at 270 mg/kg/day. No malformations were noted when exemestane was administered to pregnant rats or rabbits during the organogenesis period at doses up to 810 and 270 mg/kg/day, respectively (approximately 320 and 210 times the recommended human dose on a mg/m 2 basis, respectively).
8.2Lactation Risk Summary There is no information on the presence of exemestane in human milk, or on its effects on the breastfed infant or milk production. Exemestane is present in rat milk at concentrations similar to maternal plasma (see Data ) . Because of the potential for serious adverse reactions in breast-fed infants from EXEMESTANE, advise a woman not to breastfeed during treatment with EXEMESTANE and for 1 month after the final dose.
Data Radioactivity related to exemestane appeared in rat milk within 15 minutes of oral administration of radiolabeled exemestane. Concentrations of exemestane and its metabolites were approximately equivalent in the milk and plasma of rats for 24 hours after a single oral dose of 1 mg/kg 14 C-exemestane.
8.3Females and Males of Reproductive Potential Pregnancy Testing Pregnancy testing is recommended for females of reproductive potential within seven days prior to initiating EXEMESTANE. Contraception Females EXEMESTANE can cause fetal harm when administered to a pregnant woman [see Use in Specific Populations (8.1) ] . Advise females of reproductive potential to use effective contraception during treatment with EXEMESTANE and for 1 month after the final dose.
Infertility Based on findings in animals, male and female fertility may be impaired by treatment with EXEMESTANE [see Nonclinical Toxicology (13.1) ].
8.4Pediatric Use Safety and effectiveness in pediatric patients have not been established.
8.6 Hepatic Impairment The AUC of exemestane was increased i…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary Based on findings in animal studies and its mechanism of action , EXEMESTANE can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1) ] . Limited human data from case reports are insufficient to inform a drug-associated risk. In animal reproduction studies, administration of exemestane to pregnant rats and rabbits caused increased incidence of abortions, embryo-fetal toxicity, and prolonged gestation with abnormal or difficult labor [see Data ] .
Advise pregnant women of the potential risk to a fetus. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the US general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2–4% and 15–20%, respectively.
Data Animal Data In animal reproduction studies in rats and rabbits, exemestane caused embryo-fetal toxicity, and was abortifacient. Radioactivity related to 14 C-exemestane crossed the placenta of rats following oral administration of 1 mg/kg exemestane. The concentration of exemestane and its metabolites was approximately equivalent in maternal and fetal blood.
When rats were administered exemestane from 14 days prior to mating until either days 15 or 20 of gestation, and resuming for the 21 days of lactation, an increase in placental weight was seen at 4 mg/kg/day (approximately 1.5 times the recommended human daily dose on a mg/m2 basis). Increased resorptions, reduced number of live fetuses, decreased fetal weight, retarded ossification, prolonged gestation and abnormal or difficult labor was observed at doses equal to or greater than 20 mg/kg/day (approximately 7.5 times the recommended human daily dose on a mg/m 2 basis).
Daily doses of exemestane, given to rabbits during organogenesis, caused a decrease in placental weight at 90 mg/kg/day (approximately 70 times the recommended human daily dose on a mg/m 2 basis) and in the presence of maternal toxicity, abortions, an increase in resorptions, and a reduction in fetal body weight were seen at 270 mg/kg/day. No malformations were noted when exemestane was administered to pregnant rats or rabbits during the organogenesis period at doses up to 810 and 270 mg/kg/day, respectively (approximately 320 and 210 times the recommended human dose on a mg/m 2 basis, respectively).
🧒 Pediatric Use ▾
8.4Pediatric Use Safety and effectiveness in pediatric patients have not been established.
🆘 Overdosage ▾
10 OVERDOSAGE Clinical trials have been conducted with exemestane given as a single dose to healthy female volunteers at doses as high as 800 mg and daily for 12 weeks to postmenopausal women with advanced breast cancer at doses as high as 600 mg. These dosages were well tolerated. There is no specific antidote to overdosage and treatment must be symptomatic.
General supportive care, including frequent monitoring of vital signs and close observation of the patient, is indicated. A male child (age unknown) accidentally ingested a 25-mg tablet of exemestane. The initial physical examination was normal, but blood tests performed 1 hour after ingestion indicated leucocytosis (WBC 25000/mm 3 with 90% neutrophils).
Blood tests were repeated 4 days after the incident and were normal. No treatment was given. In mice, mortality was observed after a single oral dose of exemestane of 3200 mg/kg, the lowest dose tested (about 640 times the recommended human dose on a mg/m 2 basis).
In rats and dogs, mortality was observed after single oral doses of exemestane of 5000 mg/kg (about 2000 times the recommended human dose on a mg/m 2 basis) and of 3000 mg/kg (about 4000 times the recommended human dose on a mg/m 2 basis), respectively. Convulsions were observed after single doses of exemestane of 400 mg/kg and 3000 mg/kg in mice and dogs (approximately 80 and 4000 times the recommended human dose on a mg/m 2 basis), respectively.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Breast cancer cell growth may be estrogen-dependent. Aromatase is the principal enzyme that converts androgens to estrogens both in pre- and postmenopausal women. While the main source of estrogen (primarily estradiol) is the ovary in premenopausal women, the principal source of circulating estrogens in postmenopausal women is from conversion of adrenal and ovarian androgens (androstenedione and testosterone) to estrogens (estrone and estradiol) by the aromatase enzyme in peripheral tissues.
Exemestane is an irreversible, steroidal aromatase inactivator, structurally related to the natural substrate androstenedione. It acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme, causing its inactivation, an effect also known as "suicide inhibition". Exemestane significantly lowers circulating estrogen concentrations in postmenopausal women, but has no detectable effect on adrenal biosynthesis of corticosteroids or aldosterone.
Exemestane has no effect on other enzymes involved in the steroidogenic pathway up to a concentration at least 600 times higher than that inhibiting the aromatase enzyme.
12.2Pharmacodynamics Effect on Estrogens Multiple doses of exemestane ranging from 0.5 to 600 mg/day were administered to postmenopausal women with advanced breast cancer. Plasma estrogen (estradiol, estrone, and estrone sulfate) suppression was seen starting at a 5-mg daily dose of exemestane, with a maximum suppression of at least 85% to 95% achieved at a 25-mg dose. Exemestane 25 mg daily reduced whole body aromatization (as measured by injecting radiolabeled androstenedione) by 98% in postmenopausal women with breast cancer.
After a single dose of exemestane 25 mg, the maximal suppression of circulating estrogens occurred 2 to 3 days after dosing and persisted for 4 to 5 days. Effect on Corticosteroids In multiple-dose trials of doses up to 200 mg daily, exemestane selectivity was assessed by examining its effect on adrenal steroids. Exemestane did not affect cortisol or aldosterone secretion at baseline or in response to ACTH at any dose.
Thus, no glucocorticoid or mineralocorticoid replacement therapy is necessary with exemestane treatment. Other Endocrine Effects Exemestane does not bind significantly to steroidal receptors, except for a slight affinity for the androgen receptor (0.28% relative to dihydrotestosterone). The binding affinity of its 17-dihydrometabolite for the androgen receptor, however, is 100 times that of the parent compound.
Daily doses of exemestane up to 25 mg had no significant effect on circulating levels of androstenedione, dehydroepiandrosterone sulfate, or 17-hydroxyprogesterone, and were associated with small decreases in circulating levels of testosterone. Increases in testosterone and androstenedione levels have been observed at daily doses of 200 mg or more. A dose-dependent decrease in sex hormone binding globulin (SHBG) has been observed with daily exemestane doses of 2.5 mg or higher.
Slight, nondose-dependent increases in serum luteinizing hormone (LH) and follicle-stimulating hormone (FSH) levels have been observed even at low doses as a consequence of feedback at the pituitary level. Exemestane 25 mg daily had no significant effect on thyroid function [free triiodothyronine (FT3), free thyroxine (FT4), and thyroid stimulating hormone (TSH)]. Coagulation and Lipid Effects In study 027 of postmenopausal women with early breast cancer treated with exemestane (N=73) or placebo (N=73), there was no change in the coagulation parameters activated partial thromboplastin time (APTT), prothrombin time (PT), and fibrinogen.
Plasma HDL cholesterol was decreased 6–9% in exemestane treated patients; total cholesterol, LDL cholesterol, triglycerides, apolipoprotein-A1, apolipoprotein-B, and lipoprotein-a were unchanged. An 18% increase in homocysteine levels was also observed…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Breast cancer cell growth may be estrogen-dependent. Aromatase is the principal enzyme that converts androgens to estrogens both in pre- and postmenopausal women. While the main source of estrogen (primarily estradiol) is the ovary in premenopausal women, the principal source of circulating estrogens in postmenopausal women is from conversion of adrenal and ovarian androgens (androstenedione and testosterone) to estrogens (estrone and estradiol) by the aromatase enzyme in peripheral tissues.
Exemestane is an irreversible, steroidal aromatase inactivator, structurally related to the natural substrate androstenedione. It acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme, causing its inactivation, an effect also known as "suicide inhibition". Exemestane significantly lowers circulating estrogen concentrations in postmenopausal women, but has no detectable effect on adrenal biosynthesis of corticosteroids or aldosterone.
Exemestane has no effect on other enzymes involved in the steroidogenic pathway up to a concentration at least 600 times higher than that inhibiting the aromatase enzyme.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING EXEMESTANE tablets are round, biconvex, off-white to slightly greyish sugar-coated tablets, about 6 mm diameter, printed with numbers 2858 on one side in black ink. Each tablet contains 25 mg of exemestane. EXEMESTANE is packaged in HDPE bottles with a child-resistant screw cap, supplied in packs of 30 tablets.
30-tablet HDPE bottle NDC 59762-2858-1 Store at 25°C (77ºF); excursions permitted to 15°–30°C (59°–86°F) [see USP Controlled Room Temperature].
📦 Storage and Handling ▾
Store at 25°C (77ºF); excursions permitted to 15°–30°C (59°–86°F) [see USP Controlled Room Temperature].
📋 Description ▾
11 DESCRIPTION EXEMESTANE tablets for oral administration contain 25 mg of exemestane, an irreversible, steroidal aromatase inactivator. Exemestane is chemically described as 6-methylenandrosta-1,4-diene-3,17-dione. Its molecular formula is C 20 H 24 O 2 and its structural formula is as follows: The active ingredient is a white to slightly yellow crystalline powder with a molecular weight of 296.41.
Exemestane is freely soluble in N, N-dimethylformamide, soluble in methanol, and practically insoluble in water. Each EXEMESTANE tablet contains the following inactive ingredients: mannitol, crospovidone, polysorbate 80, hypromellose, colloidal silicon dioxide, microcrystalline cellulose, sodium starch glycolate, magnesium stearate, simethicone, polyethylene glycol 6000, sucrose, magnesium carbonate, titanium dioxide, methylparaben, and polyvinyl alcohol. Chemical Structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information). Bone Effects Advise patients that EXEMESTANE lowers the level of estrogen in the body. This may lead to reduction in bone mineral density (BMD) over time.
The lower the BMD, the greater the risk of osteoporosis and fracture [see Warnings and Precautions (5.1) ] . Other Estrogen-Containing Agents Advise patients that they should not take estrogen-containing agents while they are taking EXEMESTANE as these could interfere with its pharmacologic action [see Warnings and Precautions (5.3) ]. Use in Premenopausal Women Advise patients that EXEMESTANE is not for use for the treatment of breast cancer in premenopausal women [see Warnings and Precautions (5.5) ].
Embryo-Fetal Toxicity Advise pregnant women and females of reproductive potential that exposure during pregnancy or within 1 month prior to conception can result in fetal harm. Advise females to inform their healthcare provider of a known or suspected pregnancy [see Warnings and Precautions (5.6) and Use in Specific Populations (8.1) ]. Advise females of reproductive potential to use effective contraception while taking EXEMESTANE and for 1 month after the last dose [see Use in Specific Populations (8.3) ].
Lactation Advise women not to breastfeed during treatment with EXEMESTANE and for 1 month after the last dose [see Use in Specific Populations (8.2) ].