Aromasin Exemestane/For Advanced Breast Cancer
Aromasin Exemestane/For Advanced Breast Cancer
Exemestane is an irreversible steroidal aromatase inhibitor structurally similar to its substrate natural androstenedione. Estrogen deprivation by aromatase inhibition is an effective and alternative approach for the treatment of hormone-dependent breast cancer in postmenopausal women, natural or artificial postmenopause whose disease has not progressed despite tamoxifen therapy Advanced breast cancer in women.
Function and Usage of Exemestane
Exemestane is a steroidal aromatase inactivator, its structure is similar to the natural substrate of aromatase androstenedione, and it is a pseudo-substrate of aromatase. Estrogen in postmenopausal women is mainly produced by the transformation of androgen (produced by the adrenal cortex) under the action of aromatase in peripheral tissues. This product is irreversibly combined with the active site of aromatase to inactivate it, thereby significantly reducing the estrogen level in the blood circulation of postmenopausal women. This product has no obvious effect on the biosynthesis of adrenocortical hormone, even if the concentration is 600 times higher than the concentration of inhibiting aromatase, it has no obvious effect on other Chemicalbook enzymes in the corticosteroid production pathway. This product is rapidly absorbed orally, and the absorption is affected by food. The oral bioavailability is 42%. Postmenopausal women have a higher absorption rate of the drug than healthy subjects. Patients reach the peak plasma concentration 2 to 4 hours after oral administration of this product, and the peak time is 1.2 hours on average, which is shorter than healthy subjects (2.9 hours). It is mainly bound to α1-acid glycoprotein and protein, and the total protein binding rate is 90%. Mainly metabolized by the liver, the metabolite is inactive 17-hydroexemestane, and the elimination half-life is 24 hours. It is mainly excreted through urine or feces, each accounting for 42% of the dose.
Indications
It is suitable for postmenopausal women with advanced breast cancer who are estrogen and progesterone receptor positive.
Dosage
25mg at a time, once a day, orally after meals. Mild hepatic and renal insufficiency patients 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, the literature reports include hypertension, depression, anxiety, dyspnea, cough and so on. Others include decreased lymphocyte count and abnormal liver function indicators (such as alanine transferase, etc.).
Taboo
1. People who are allergic to this product should not take it.
2. Pregnant women, lactating women, and children are prohibited.
Clinical Evaluation
Exemestane is an oral, highly potent, irreversible steroidal aromatase inhibitor. For patients resistant to tamoxifen, exemestane 25mg, qd, can obtain an objective effective rate of 15% to 28% and a median duration of 69 to 76 weeks. Exemestane is superior to megestrol, and can prolong the time of disease progression. For patients who have deteriorated after megestrol treatment, exemestane can still achieve an objective effective rate of 11% to 13%. Exemestane 25mg/d has an objective effective rate of 6.6% for patients who have failed treatment with non-steroidal aromatase inhibitors, and there is no cross-resistance between the two drugs. The overview, functions and uses, synthesis, indications, precautions, etc. of exemestane are organized by the Eastern editor of Chemicalbook.
Precautions
1. Premenopausal women generally do not use exemestane tablets.
2. Use with caution in patients with moderate to severe liver or renal insufficiency. Overdose of exemestane can increase its non-fatal adverse reactions.
3. The pregnancy safety classification of this drug is grade D by FDA.
4. There are no special precautions for elderly medication.
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