Exemestane Brand Name– Aromasin
What is Exemestane
Exemestane is an irreversible, steroidal aromatase inhibitor.
Exemestane is used in postmenopausal women as second-line hormonal therapy of advanced breast cancer and as adjuvant therapy in postmenopausal women with estrogen-receptor positive early breast cancer.
An advantage of exemestane is the lack of cross-resistance with other non-steroidal aromatase inhibitors, anastrazole and letrozole, and tamoxifen; patients whose breast cancer progresses while receiving these agents may still respond to exemestane.
Exemestane produces more complete estrogen blockade than anastrazole or letrozole.
In comparison to megestrol in postmenopausal women with advanced breast cancer, exemestane achieved a similar objective response rate as megestrol, but the time to tumor progression and survival was significantly prolonged with exemestane.
In a subset of patients with visceral disease (lung and liver involvement), exemestane achieved higher overall response rates and survival than megestrol.
In addition, exemestane caused less weight gain than megestrol.
In early breast cancer, the results of the Intergroup Exemestane Study (IES), which investigated whether switching to exemestane after 2—3 years of tamoxifen, indicate that exemestane provides a disease-free survival advantage over 5 years of continuous tamoxifen.
The trial was discontinued early because of a significant disease-free survival advantage seen with exemestane after a median of 30.6 months (32% relative risk reduction; 4.7% absolute risk reduction).
Aromatase inhibitors are considered to be a standard of therapy and drug class of choice for the treatment of early breast cancer in postmenopausal women with hormone-receptor positive disease.
The American Society of Clinical Oncology recommends that all postmenopausal women with hormone receptor-positive early breast cancer receive adjuvant aromatase inhibitor therapy. Options include 5 years of an aromatase inhibitor or sequential therapy with 2—3 years or 5 years of tamoxifen followed by 2—3 years or 5 years of an aromatase inhibitor.
The optimal duration of therapy and regimen are not known.
The FDA approved exemestane for the treatment of advanced breast cancer in postmenopausal women who have progressed on tamoxifen therapy in October 1999.
In October 2005, exemestane was approved as adjuvant hormonal therapy in postmenopausal women with estrogen-receptor positive early breast cancer.
Specifically, women who have received 2—3 years of tamoxifen therapy can be switched to exemestane for the completion of a total of five years of adjuvant hormonal therapy.
Indications
- breast cancer
For the treatment of breast cancer in postmenopausal women
for the adjuvant treatment of estrogen receptor-positive early breast cancer in postmenopausal women who have already received 2 to 3 years of tamoxifen therapy, and who are switched to exemestane for completion of a total of 5 consecutive years of adjuvant hormonal therapy
Side Effects
- abdominal pain
- alopecia
- anorexia
- anxiety
- arthralgia
- asthenia
- back pain
- bone fractures
- carpal tunnel syndrome
- chest pain (unspecified)
- cholestasis
- confusion
- constipation
- cough
- depression
- diarrhea
- dizziness
- dyspepsia
- dyspnea
- edema
- elevated hepatic enzymes
- elevated hepatic enzymes
- endometrial hyperplasia
- fatigue
- fever
- headache
- hepatitis
- hot flashes
- hyperbilirubinemia
- hyperbilirubinemia
- hyperhidrosis
- hypertension
- hypoesthesia
- infection
- influenza
- insomnia
- lymphopenia
- muscle cramps
- myalgia
- nausea
- osteoporosis
- paresthesias
- peptic ulcer
- peripheral edema
- pharyngitis
- pruritus
- rash
- rhinitis
- sinusitis
- thromboembolism
- urticaria
- visual impairment
- vomiting
- weakness
- weight gain
Monitoring Parameters
- pregnancy testing
- serum 25(OH)hydroxyvitamin D concentrations
Contraindications
- breast-feeding
- contraception requirements
- infertility
- osteoporosis
- pregnancy
- pregnancy testing
- reproductive risk
- vitamin D deficiency
Interactions
- Apalutamide
- Atropine; Hyoscyamine; Phenobarbital; Scopolamine
- Belladonna Alkaloids; Ergotamine; Phenobarbital
- Carbamazepine
- Conjugated Estrogens
- Conjugated Estrogens; Bazedoxifene
- Conjugated Estrogens; Medroxyprogesterone
- Dienogest; Estradiol valerate
- Diethylstilbestrol, DES
- Drospirenone; Estradiol
- Drospirenone; Ethinyl Estradiol
- Drospirenone; Ethinyl Estradiol; Levomefolate
- Elagolix; Estradiol; Norethindrone acetate
- Enzalutamide
- Eslicarbazepine
- Esterified Estrogens
- Esterified Estrogens; Methyltestosterone
- Estradiol
- Estradiol Cypionate; Medroxyprogesterone
- Estradiol; Levonorgestrel
- Estradiol; Norethindrone
- Estradiol; Norgestimate
- Estradiol; Progesterone
- Estrogens
- Estropipate
- Ethinyl Estradiol
- Ethinyl Estradiol; Desogestrel
- Ethinyl Estradiol; Ethynodiol Diacetate
- Ethinyl Estradiol; Etonogestrel
- Ethinyl Estradiol; Levonorgestrel
- Ethinyl Estradiol; Levonorgestrel; Ferrous bisglycinate
- Ethinyl Estradiol; Levonorgestrel; Folic Acid; Levomefolate
- Ethinyl Estradiol; Norelgestromin
- Ethinyl Estradiol; Norethindrone
- Ethinyl Estradiol; Norethindrone Acetate
- Ethinyl Estradiol; Norethindrone Acetate; Ferrous fumarate
- Ethinyl Estradiol; Norethindrone; Ferrous fumarate
- Ethinyl Estradiol; Norgestimate
- Ethinyl Estradiol; Norgestrel
- Fosphenytoin
- Isoniazid, INH; Pyrazinamide, PZA; Rifampin
- Isoniazid, INH; Rifampin
- Lumacaftor; Ivacaftor
- Mephobarbital
- Mestranol; Norethindrone
- Mitotane
- Phenobarbital
- Phenytoin
- Prasterone, Dehydroepiandrosterone, DHEA (Dietary Supplements)
- Prasterone, Dehydroepiandrosterone, DHEA (FDA-approved)
- Primidone
- Rifampin
- Segesterone Acetate; Ethinyl Estradiol
- St. John’s Wort, Hypericum perforatum
