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|Quality:||99.5%||Apperance:||White Or White Crystalline Powder|
|Usage:||Muscle To Reduce Fat||MOQ:||10G|
The chemical name of exemestane is 1,4-diene-3,17-dione-6-methylenesterrol or 6-methyleneandrost-1,4-diene-3,17-dione , white or off-white crystalline powder; odorless. Soluble in chloroform, soluble in ethyl acetate, acetone, methanol or ethanol, almost insoluble in water. Clinically applicable to postmenopausal women with advanced breast cancer who have progressed after treatment with tamoxifen.
Chinese name: Exemestane
Chinese alias: 1,4-diene-3,17-dione-6-methylene-androstane; exemestane (enterprise); 6-methylene-androst-1,4-diene-3 , 17-dione;
English name: exemestane
English alias: 6-methylenandrosta-1,4-diene-3,17-dione;androsta-1,4-diene-6-methylene-3,17-dione;6-METHYLENEANDROSTA-1,4-DIENE-3,17 -DIONE;Exemestance;6-Methylene-androsta-1,4-diene-3,17-dione;AROMASIN;EXALAMIDE;Exemestan;6-methylenandrost-1,4-diene-3,17-dione;Exemestane;6-Methyleneandrosta -1,4-diene-3,17-dione;
CAS No.: 107868-30-4
Molecular formula: C20H24O2
Molecular weight: 296.40300
Exact quality: 296.17800
Appearance and traits: white to light yellow crystal powder
Density: 1.13 g/cm3
Melting point: 155.13 ° C
Boiling point: 453.7oC at 760 mmHg
Flash point: 169oC
Refractive index: 1.572
Storage conditions: Store in original container in a cool dark place.
Steam pressure: 2.02E-08mmHg at 25°C
Signal word: danger
Hazard statement: H319; H360
Warning statement: P201; P305 + P351 + P338; P308 + P313
Packing level: III
Hazard category: 8
Customs code: 2937900090
Dangerous goods transport code: UN 3261 8/PG 2
WGK Germany: 3
Safety instructions: S26-S36/37/39 
|Melting point||155.13 ° C|
Exemestane Description :
The growth of breast cancer cells can depend on the presence of estrogen. Estrogen (estrone and estradiol) in the postmenopausal cycle of women is mainly composed of aromatase in peripheral tissues and androgen in the adrenal gland and ovary. Ketone and testosterone) are converted. Preventing estrogen production by inhibiting aromatase is an effective method for the selective treatment of postmenopausal hormone-dependent breast cancer. Exemestane is an irreversible steroidal aromatase inactivating agent, structurally similar to the natural substrate of the enzyme, androstenedione, which is a pseudo-substrate of aromatase, which can irreversibly interact with the active site of the enzyme. Point combination to inactivate it (this effect is also called "self-destructive inhibition"), which significantly reduces estrogen levels in the blood circulation of postmenopausal women, but has no significant effect on the biosynthesis of corticosteroids and aldosterol in the adrenal gland. At 600 times higher than the concentration of inhibitory aromatase, there was no significant effect on other enzymes in the steroidogenic pathway. 
Single-dose toxicity: A single oral dose of 3200 mg/kg (about 640 times the human clinically recommended dose) was observed in mice. The animals died when the single doses of rats and dogs were 5000 mg/kg and 3000 mg/kg, respectively (calculated as body surface area, approximately 2000 times and 4000 times the clinically recommended dose, respectively). The animals were convulsed when the single doses of mice and dogs were 400 mg/kg and 3000 mg/kg, respectively (calculated as body surface area, approximately 80 and 4000 times the clinically recommended dose, respectively).
In clinical studies, healthy people showed good tolerance in a single dose of 800 mg/kg and advanced breast cancer patients up to 600 mg for 12 weeks.
Reproductive toxicity: 14 days before mating to 15-20 days of gestation, the rats were given this product for 21 days during lactation, and the dose was 4 mg/kg/day (calculated as body surface area, equivalent to 1.5% of the human clinical recommended dose). When the dose is greater than or equal to 20mg/kg/day, the pregnancy is prolonged, the delivery is abnormal or difficult, and the increase of the absorption of the fetus, the decrease of the number of live fetuses, the decrease of the weight of the fetus, and the delay of ossification are also observed. . In the organogenesis phase of pregnant rats, when the dose is less than or equal to 810 mg/kg (calculated as the body surface area is about 320 times the clinical recommended dose), no obvious teratogenic effect occurs. When the rabbit organogenesis period is 90 mg/kg/day (calculated as 70 times of the recommended clinical dose according to the body surface area), the placental weight is reduced; when the dose is 270 mg/kg/day, abortion occurs and absorption occurs. The increase in fetus and the decrease in body weight of the fetus; the dose was less than or equal to 270 mg/kg/day (calculated as 210 times the clinical recommended dose by body surface area), and the rabbit malformation rate did not increase. At present, there is no clinical research data on the effects of this product on pregnant women. If this product is taken during pregnancy, the patient should be informed of the potential harm of the product to the fetus and the potential danger of miscarriage.
During the 63 days before mating and during the co-cage period, the male rats were given 500 mg/kg/day (about 200 times the human clinical recommendation according to the body surface area), and the fertility of the non-administered female rats can be mated. The force is reduced. When the dose of this product is 20mg/kg/day (calculated as body surface area, which is equivalent to 8 times of the human clinical recommended dose), there is no effect on the fertility parameters (such as ovarian function, mating behavior, conception rate) of female rats, but The average litter size is reduced. In addition, in the general toxicity study, when the dose is 3-20 times of the clinically recommended dose, the mice, rats and dogs have varying degrees of ovarian changes, including hyperplasia and increased number of ovarian cysts. And the number of corpus luteum decreased.
Rats were orally administered radiolabeled 14C-exemestane 1 mg/kg and found to pass the placenta. Radioactive exemestane appeared in the milk 15 minutes after administration. The concentration of this product and its metabolites in the maternal and fetal blood is equivalent 24 hours after the drug. It is not known whether this product is secreted by human milk. Because many drugs can be secreted by milk, lactating women should use this product with caution.
Genotoxicity: This product showed no mutagenic effects in the Ames test and the V79 Chinese hamster lung cell test. In the absence of metabolic activation in vitro, it showed mutagenic effects on human lymphocytes, but the mouse micronucleus test results were negative. This product does not increase the extra-program DNA synthesis of rat hepatocytes.
Carcinogenicity: There is no research data on the carcinogenic effect of this product. 
Suitable for postmenopausal women with advanced breast cancer after treatment with tamoxifen. 
It is forbidden to patients who are allergic to this product or the excipients in this product. 
One tablet at a time (25mg), once a day, orally after meals. Patients with mild liver and kidney dysfunction do not need to adjust the dose. 
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, there were reports of hypertension, depression, anxiety, difficulty breathing, and cough. Others include abnormal lymphocyte counts and abnormal liver function indicators (such as alanine transferase). In clinical trials, only 3% of patients discontinued treatment due to adverse events, mainly during the first 10 weeks of exemestane treatment; those who discontinued treatment due to adverse events were less common (0.3%). 
Premenopausal women generally do not use exemestane tablets. Exemestane should not be combined with estrogens to avoid interference. Moderate and severe liver function, renal insufficiency should be used with caution. Excessive use of exemestane can increase non-fatal adverse reactions.
Pregnant women and lactating women
Elderly patients medication
No special precautions