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107868-30-4

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High purity 99% Exemestane,Aromasin 25mg Tablet and Raw Material Fast delivery
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107868-30-4 Usage

Pharmacokinetics

This drug has no noticeable effect on adrenal corticosteroids biosynthesis. Even when its concentration is over 600 times the concentration required to inhibit aromatase, it still has no noticeable effect the other enzymes in the corticosteroid production pathway.
This drug is absorbed quickly when taken orally and will affect food absorption. Its oral bioavailability is 42%. Postmenopausal women have a higher absorption rate than healthy test subjects. Patients reach peak blood concentration 2-4 hours after intake, and the peak lasts for an average of 1.2 hours, which is 2.9 hours shorter than healthy subjects. It mainly binds to Α1-acid glycoprotein and protein, and its overall binding rate to protein is 90%. It is mainly metabolized by the liver, the metabolite is inactive 17-Hydrecoxetron, and its clearing half-life is 24 hours. It is mostly excreted through urine and feces, which both account for 42% of the consumed amount.

Drug interactions

1. This drug cannot be used in combination with estrogen-based drugs to avoid counteracting its medicinal effects.
2. Exemestane is mostly metabolized by CYP3A4, but when used in combination with a strong CYP3A4 inhibitor (Ketoconazole), its pharmacokinetics do not exhibit any change. This is because the inhibitor does not seem to affect the drug’s pharmacokinetics, but it is also possible that the known CYP3A4 inducer lowers the blood concentration of Exemestane.

Indications and Usage

Exemestane is an irreversible steroid aromatase inhibitor. Its structure is similar to that of aromatase’s natural substrate, androstenedione, and acts as a pseudosubstrate. Postmenopausal women’s estrogen is mainly converted from androgen (produced by the adrenal cortex) by aromatase in the surrounding tissue. This drug irreversibly binds with the active site on aromatase to deactivate it, thus dramatically lower estrogen levels in the blood circulation of postmenopausal women. By inhibiting aromatase to lower estrogen levels, it can be used to treat hormone-dependent breast cancer in postmenopausal women.
Exemestane is suitable for treating advanced breast cancer in naturally or artificially postmenopausal women that has not responded well to tamoxifen treatment. It is also suitable for treating estrogen and progesterone receptor positive postmenopausal advanced breast cancer, and it can also be used to treat metastasized breast cancer and as adjuvant therapy for early breast cancer.

Contradictions

1. Not to be used by patients allergic to this drug.
2. Not to be used by pregnant women, breastfeeding women, and children.

Uses

Labeled Exemestane, intended for use as an internal standard for the quantification of Exemestane by GC- or LC-mass spectrometry.

Clinical Research

For patients resistant to tamoxifen, 25mg of Exemestane, qd, can achieve an objective efficacy rate of 15-28% and a median continuation period of 69-76 weeks. Exemestane is superior to Megestrol, and it can extend the disease progression time. For patients who have worsened conditions following Megestrol treatment, Exemestane can still achieve an objective efficacy rate of 11-13%. A daily 25mg dose of Exemestane has an objective efficacy rate of 6.6% on patients who have not responded to non-steroidal aromatase inhibitors, and the two drugs are not cross-resistant.

Uses

antiinfective

Brand name

Aromasin (Pharmacia& Upjohn).

Chemical Properties

white to light yellow crystal powder

Definition

ChEBI: A 17-oxo steroid that is androsta-1,4-diene-3,17-dione in which the hydrogens at position 6 are replaced by a double bond to a methylene group. A selective inhibitor of the aromatase (oestrogen synthase) system, it is used in the treatment of advanced brea t cancer.

Uses

An antineoplastic (hormonal)

Warnings and precautions

1. Premenopausal women usually do not use Exemestane.
2. Patients with moderate to severe liver or renal failure should use with caution. Exceeding the recommended dosage of Exemestane may increase the occurrence of nonfatal adverse effects.
3. FDA labeled this drug’s pregnancy safety as level D.
4. Elderly patients do not require any special precautions.

Side effects

Adverse effects include nausea, dryness, constipation, diarrhea, dizziness, insomnia, rash, fatigue, fever, swelling, pain, vomiting, abdominal pain, increased appetite, weight gain, etc. Additionally, some literature reports cases of hypertension, depression, anxiety, difficulty breathing, coughing, etc. There may also be decreases lymph cell amounts, abnormalities in liver function indicators (such as alanine aminotransferase), etc.
InChI:InChI=1/C20H24O2/c1-12-10-14-15-4-5-18(22)20(15,3)9-7-16(14)19(2)8-6-13(21)11-17(12)19/h6,8,11,14-16H,1,4-5,7,9-10H2,2-3H3/t14?,15?,16?,19-,20+/m1/s1

107868-30-4 Well-known Company Product Price

Brand (Code)Product description CAS number Packaging Price Detail
Sigma (PZ0006)  Exemestane  ≥98% (HPLC) 107868-30-4 PZ0006-5MG 1,115.01CNY Detail
USP (1269050)  Exemestane  United States Pharmacopeia (USP) Reference Standard 107868-30-4 1269050-150MG 4,326.66CNY Detail
Sigma-Aldrich (Y0001756)  Exemestane for system suitability  European Pharmacopoeia (EP) Reference Standard 107868-30-4 Y0001756 1,880.19CNY Detail
Sigma-Aldrich (Y0001747)  Exemestane  European Pharmacopoeia (EP) Reference Standard 107868-30-4 Y0001747 1,880.19CNY Detail
Sigma-Aldrich (PHR1634)  Exemestane  (pharmaceutical secondary standard; traceable to USP) 107868-30-4 PHR1634-1G 1,027.26CNY Detail

107868-30-4SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 20, 2017

Revision Date: Aug 20, 2017

1.Identification

1.1 GHS Product identifier

Product name exemestane

1.2 Other means of identification

Product number -
Other names 6-methylenandrosta-1,4-diene-3,17-dione

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:107868-30-4 SDS

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