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Brand Name :
Aromasin
(United States) [Available]Synonyms :
Class :
Antineoplastic agents & Aromatase Inhibitor
Brand Name :
Aromasin
(United States) [Available]Synonyms :
Class :
Antineoplastic agents & Aromatase Inhibitor
Dosage Forms & Strengths
Tablet, Oral:
25 mg
First-line adjuvant therapy:
25
mg
Orally 
once a day
for 5 years
Postmenopausal patients: 25 mg orally once a day for 5 years of endocrine therapy, following 2 to 3 years of tamoxifen therapy
Advanced Breast cancer:
25 mg orally once a day in combination with everolimus
Risk reduction treatment for Breast cancer:
Premenopausal for women > 35 years: 25 mg orally once a day for 5 years
Dose Adjustments
Decreased mineral density of bone: manage bone density with suitable supplements as clinically indicated
Vitamine D deficiency: administer the supplement as clinically indicated
No safe dosing is established
Acute Lymphoblastic Leukemia(All)
MRD-positive Acute lymphoblastic leukemia:
Premedication of prednisone:
100
mg
Intravenous (IV)
every hour
prior to the first dose of each 6-week cycle of blinatumomab
Premedication of dexamethasone: 16 mg IV once an hour prior to the first dose of each 6-week cycle of blinatumomab
<45 kg: 15 mcg/m2 IV once a day with continuous infusion on the day 1 to 28 of a 6-week cycle for 4 cycles (fixed dose)
Relapsed/refractory acute lymphoblastic leukemia:
<45 kg: 5 mcg/m2 IV once a day with continuous infusion on days 1 to 7 and 15 mcg/m2 IV once a day on days 8 to 28 of cycle-1 of 6-weeks (do not exceed 28 mcg/day)
15 mcg/m2 IV once a day with continuous infusion on days 1 to 28 of cycles 2 to 5 of 6-weeks (do not exceed 28 mcg/day)
15 mcg/m2 IV once a day with continuous infusion on days 1 to 28 of cycles 6 to 9 of the 12-weeks cycle (do not exceed 28 mcg/day)
Dose Adjustments
Terminate the therapy temporarily if transaminases > 5 times ULN and/or bilirubin > 3 times ULN (hepatotoxicity)
exemestane: they may diminish the serum concentration of CYP3A4 Inducers
exemestane: they may diminish the serum concentration of CYP3A4 Inducers
exemestane: they may diminish the serum concentration of CYP3A4 Inducers
exemestane: they may diminish the serum concentration of CYP3A4 Inducers
exemestane: they may diminish the serum concentration of CYP3A4 Inducers
may decrease the therapeutic effect when combined with growth hormone analogs
may decrease the therapeutic effect when combined with growth hormone analogs
may decrease the therapeutic effect when combined with growth hormone analogs
may decrease the therapeutic effect when combined with growth hormone analogs
exemestane: they may diminish the serum concentration of hormonal contraceptives
exemestane: they may diminish the serum concentration of hormonal contraceptives
exemestane: they may diminish the serum concentration of hormonal contraceptives
exemestane: they may diminish the serum concentration of hormonal contraceptives
exemestane: they may diminish the serum concentration of hormonal contraceptives
may have a decreased diagnostic effect when combined with cosyntropin
may decrease the diagnostic effect when combined with metyrapone
the therapeutic effect of exemestane may be reduced by the use of estrogen derivatives
the therapeutic effect of exemestane may be reduced by the use of estrogen derivatives
bazedoxifene/conjugated estrogens
the therapeutic effect of exemestane may be reduced by the use of estrogen derivatives
the therapeutic effect of exemestane may be reduced by the use of estrogen derivatives
the therapeutic effect of exemestane may be reduced by the use of estrogen derivatives
The Therapeutic effectiveness of exemestane may be reduced by the presence of Estrogen Derivatives
The Therapeutic effectiveness of exemestane may be reduced by the presence of Estrogen Derivatives
may enhance the serum concentration when combined with corticosteroids
may enhance the serum concentration when combined with corticosteroids
may enhance the serum concentration when combined with corticosteroids
may enhance the serum concentration when combined with corticosteroids
may enhance the serum concentration when combined with corticosteroids
CYP3A strong enhancers of the small intestine may reduce the bioavailability of exemestane
the therapeutic effect of exemestane may be reduced by the use of estrogen derivatives
estrogens esterified/methyltestosterone            Â
may decrease the therapeutic effect of estrogen derivatives
The therapeutic efficacy of hemin may be reduced by estrogen derivative
dehydroepiandrosterone (DHEA)Â
It may intensify the toxicity of Estrogen Derivatives
may reduce the serum concentration of CYP3A4 substrates
may reduce the serum concentration of CYP3A4 substrates
exemestane (aromatase inhibitors) may decrease the serum concentration of levomethadone
exemestane (aromatase inhibitors) may decrease the serum concentration of methadone
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
may increase the levels of serum concentration
May have an increased the thrombogenic effect when combined with anthrax immune globulin
May have an increased the thrombogenic effect when combined with anthrax immune globulin
May have an increased the thrombogenic effect when combined with anthrax immune globulin
May have an increased the thrombogenic effect when combined with anthrax immune globulin
May have an increased the thrombogenic effect when combined with anthrax immune globulin
It may diminish the metabolism when combined with Estrogens
It may diminish the metabolism when combined with Estrogens
human rabies immune globulin (HRIG)
May have an increased the thrombogenic effect when combined with anthrax immune globulin
may enhance the concentration of serum when combined with corticosteroids
may enhance the concentration of serum when combined with corticosteroids
may enhance the concentration of serum when combined with corticosteroids
may enhance the concentration of serum when combined with corticosteroids
the effect of exemestane is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
It may enhance the thrombogenic activities when combined with sotrovimab
estrogen derivatives may potentially amplify the hepatotoxic effect of dantrolene
methadone concentration serum may be enhanced by aromatase inhibitors
The therapeutic efficacy of guanethidine may be reduced by estrogen derivative
The concentration serum of melatonin may be intensified by estrogen derivative
estrogen derivatives could potentially increase the toxicity of ajmaline
It may diminish the metabolism when combined with Ergot alkaloids
It may diminish the metabolism when combined with Ergot alkaloids
It may diminish the metabolism when combined with Ergot alkaloids
It may diminish the metabolism when combined with Ergot alkaloids
It may diminish the metabolism when combined with Ergot alkaloids
It may enhance the risk of adverse effects when combined with Hormone antagonists
Exemestane is a type of aromatase inhibitor that reduces estrogen levels in the body. By decreasing this hormone, it helps slow or halt the growth of certain breast cancer cells that rely on estrogen to develop.Â
Frequency defined:Â
>10%:Â
Hypertension (25%)Â
Alopecia (15%)Â
NauseaÂ
Excessive sweatingÂ
Depression (13%)Â
FatigueÂ
HeadacheÂ
Insomnia (12%)Â
PainÂ
Joint pain (15%)Â Â
1% to 10%Â
Angina pectoris (2%)Â
Chest pain (5%)Â
Edema (7%)Â
Peripheral edema (7%)Â
Skin rash (5%)Â
Weight gain (8%0Â
Vomiting (7%)Â
Urinary tract infection (5%)Â
Constipation (5%)Â
Dyspepsia (5%)Â
Anxiety (10%)Â
Dizziness (8%)Â
Tumor pain (8%)Â
Back pain (9%0Â
Muscle cramps (2%)Â
Fever  Â
<1%Â
Heart failureÂ
Gastric ulcerÂ
NeuropathyÂ
Endometrial hyperplasiaÂ
Abnormal bone growth Â
Â
Frequency not defined:Â
Decreased bone mineral densityÂ
Increased serum transaminases  Â
Post-marketing:Â
Urticaria Â
Anaphylaxis Â
HepatitisÂ
Acute generalized exanthematous pustulosisÂ
No blackbox warning presentÂ
Contraindication/CautionÂ
ContraindicationÂ
HypersensitivityÂ
CautionsÂ
Avoid Estrogen Co-administration: Estrogen-containing medications should not be used with exemestane, as they may counteract its therapeutic effects.Â
Vitamin D Monitoring: Check 25-hydroxy vitamin D levels before starting treatment due to common deficiency in women with early breast cancer. Supplement if deficient.Â
Bone Health: Exemestane may decrease bone mineral density (BMD) over time. Women with or at risk of osteoporosis should undergo a BMD scan at treatment initiation and be monitored and managed accordingly.Â
Premenopausal Use: Exemestane is not recommended for use in premenopausal women with breast cancer.Â
Contraception: Women who can become pregnant should use reliable birth control during treatment and for at least one month after the last dose.Â
Fertility: Animal studies suggest that exemestane may affect fertility in both men and women.Â
Pregnancy consideration: Based on animal reproduction research data, exemestane may cause fetal harm and potential fetal loss.Â
Lactation: Not recommended for lactating females due to potential severe adverse reactions in breastfeeding infants. Â
Pregnancy category:Â
Â
Exemestane is a steroidal, irreversible aromatase inhibitor that functions by permanently inactivating the aromatase enzyme, which is responsible for converting androgens (such as androstenedione and testosterone) into estrogens (estrone and estradiol). By suppressing estrogen synthesis, exemestane significantly lowers circulating estrogen levels in postmenopausal women, which is essential for treating estrogen receptor-positive breast cancer, as these tumors rely on estrogen for growth and proliferation.Â
After oral administration, exemestane is rapidly absorbed and undergoes extensive hepatic metabolism, primarily via oxidation by CYP3A4 and subsequent conjugation. Its half-life is approximately 24 hours, and it is eliminated mainly through urine and feces. Exemestane does not significantly inhibit or induce major cytochrome P450 enzymes, minimizing drug interaction potential.Â
PharmacokineticsÂ
AbsorptionÂ
Exemestane is well absorbed after oral administration, with peak plasma concentrations reached approximately 1.2 hours after dosing in women with breast cancer.Â
DistributionÂ
It is highly protein-bound, with about 90% of the drug bound to plasma proteins, facilitating systemic distribution.Â
MetabolismÂ
Exemestane undergoes extensive hepatic metabolism, primarily via the cytochrome P450 enzyme CYP3A4, resulting in inactive metabolites.Â
Elimination/ExcretionÂ
The drug is eliminated through both renal and fecal routes—approximately 39–45% via urine and 35–48% via feces.Â
The terminal half-life of exemestane is around 24 hours, supporting once-daily dosing.Â
PharmacodynamicsÂ
Effect on Estrogens: Exemestane effectively reduces estrogen levels in postmenopausal women. Estrogen suppression begins at doses as low as 5 mg/day, with maximum reductions of 85–95% observed at the standard 25 mg daily dose. At this dosage, exemestane suppresses whole-body aromatization by approximately 98%, as measured using radiolabeled androstenedione. A single 25 mg dose leads to peak estrogen suppression within 2 to 3 days, and this effect can last up to 4 to 5 days.Â
Effect on Corticosteroids: Exemestane exhibits high selectivity for aromatase inhibition without interfering with adrenal steroidogenesis. Even at doses up to 200 mg/day, there is no significant impact on cortisol or aldosterone production, either at baseline or following ACTH stimulation. Therefore, corticosteroid replacement therapy is not required during exemestane treatment.Â
Exemestane should be taken orally once daily, preferably after a meal to enhance absorption.Â
Generic Name: exemestaneÂ
Pronounced: eg-ZEM-eh-staneÂ
Why do we use exemestane? Â
Exemestane is used as a hormone therapy for treating hormone receptor-positive breast cancer in postmenopausal women. By irreversibly inhibiting the aromatase enzyme, it reduces estrogen production in the body, which helps slow or stop the growth of estrogen-dependent tumors. It is commonly prescribed in early and advanced stages of breast cancer, particularly after treatment with other hormonal therapies like tamoxifen.Â
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