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Exemestane (exemestane) instructions

Generic name: exemestane tablets
Trade name: Arnosin
All names: exemestane, exemestane tablets, Arnosin, exemestane

Indications:
Applicable to postmenopausal patients with advanced breast cancer whose disease has progressed after treatment with tamoxifen.

Usage and dosage:
Take one tablet (25 mg) once a day, orally after meals.
Patients with mild hepatic and renal insufficiency do not need to adjust the dosage.

Adverse reactions:
The main adverse reactions of this product are: nausea, dry mouth, constipation, diarrhea, dizziness, insomnia, rash, fatigue, fever, edema, pain, vomiting, abdominal pain, increased appetite, weight gain, etc.
Secondly, literature reports include hypertension, depression, anxiety, dyspnea, and cough.
Others include decreased lymphocyte count and abnormal liver function indicators (such as alanine transferase, etc.).
In clinical trials, only 3% of patients discontinued treatment due to adverse reactions, mainly within the first 10 weeks of exemestane treatment; discontinuation of treatment due to adverse reactions in the later stages was less common (0.3%).

Contraindications:
Contraindicated for patients allergic to this product or the excipients in this product.
Contraindicated for premenopausal and pregnant or lactating women.

Note:
Athletes should use with caution.
This product is not suitable for women with premenopausal endocrine status. Therefore, if clinically possible, LH, FSH, and estradiol levels should be tested to determine whether the patient is in the postmenopausal state. It should also not be used in combination with estrogen-containing drugs, as these drugs will affect their pharmacological effects.
Patients with liver or renal impairment should use with caution.
Exemestane tablets contain sucrose and should not be used in patients with rare hereditary disorders of glucose intolerance, glucose-galactose malabsorption, or sucrase-isomaltase deficiency.
Effects on driving and mechanical operation: There are reports of drowsiness, drowsiness, weakness, and dizziness after using this product. Patients using this product should be reminded that if these symptoms occur, their physical and/or mental status to operate machinery or drive may be affected.

Storage:
Store below 30℃.

Mechanism of action:
The growth of breast cancer cells can depend on the presence of estrogen. The circulating estrogens (esstrone and estradiol) in women after menopause are mainly converted by aromatase in peripheral tissues from androgens (androstenedione and testosterone) in the adrenal glands and ovaries. Blocking estrogen production by inhibiting aromatase is an effective selective treatment for postmenopausal hormone-dependent breast cancer. Exemestane is an irreversible steroidal aromatase inactivator. It is structurally similar to androstenedione, the natural substrate of the enzyme. It is a pseudo-substrate of aromatase. It can inactivate it by irreversibly binding to the active site of the enzyme (this effect is also called "self-destructive inhibition"), thereby significantly reducing the estrogen level in the blood circulation of postmenopausal women, but has no obvious effect on the biosynthesis of corticosteroids and aldosterols in the adrenal gland. At a concentration 600 times higher than the concentration that inhibits aromatase, it has no significant effect on other enzymes in the steroidogenic pathway.

Safety and efficacy:
EORTC trial: exemestane vs tamoxifen, first-line treatment of postmenopausal metastatic breast cancer. ORR: 46% vs 31%. TTP: 11.8 months vs 8.1 months. IES trial: 2-3 years of tamoxifen treatment, followed by exemestane for a total of 5 years. The results showed that the sequential efficacy of exemestane was better than that of tamoxifen monotherapy for 5 years.
B33 NSABP trial: exemestane vs placebo, exemestane prolongs DFS and increases tumor response after 4-5 years of tamoxifen treatment. TEXT trial and SOFT trial: Premenopausal patients were given exemestane or tamoxifen as adjuvant therapy after ovarian suppression. The 5-year DFS are: 91.1% vs 87.3%. Reduced risk of recurrence: 34% vs 28%. Spanish Breast Cancer Group 2001-03 Randomized Trial Phase-II trial: first-line treatment of advanced or metastatic breast cancer, exploring the appropriate medication sequence of aromatase inhibitors. The results showed that: first-line anastrozole followed by exemestane gave patients more clinical benefit than exemestane first followed by anastrozole. Another study also demonstrated the effectiveness of exemestane after resistance to nonsteroidal aromatase inhibitors. Currently, no cross-resistance between steroidal and non-steroidal aromatase inhibitors has been found.
Neoadjuvant treatment: Exemestane can maximize the conservative resection rate of breast cancer and improve the surgical effect. The test results of PTEX46 and TEAM IIA show that the maximum effective time is 4-6 months. Mammary Prevention 3 trial: This trial evaluated the rate of disease recurrence after 35 months of exemestane treatment. Results: Reduced risk of breast cancer invasion by 65% ​​compared to placebo. MA.27B Trial: Exemestane vs Anastrozole with Calcium and Vitamin D. After 2 years, there was no difference in bone density between the two groups.