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Exemestane

Indications and Usage Pharmacokinetics Drug interactions Side effects Clinical Research Contradictions Warnings and precautions

CAS No. 107868-30-4
Chemical Name: Exemestane
Synonyms: AROMASIN;PNU155971;FCE-24304;Exemestan;EXALAMIDE;ExeMestine;EXEMESTANE;Exemestance;Exemestane D2;ExeMestane (USP)
CBNumber: CB5760314
Molecular Formula: C20H24O2
Formula Weight: 296.4
MOL File: 107868-30-4.mol
Exemestane Property
Melting point : 155.13°C
storage temp. : Store at -20°C
solubility : DMSO: ≥20mg/mL
color : white to off-white
CAS DataBase Reference: 107868-30-4(CAS DataBase Reference)
SAFETY
  • Risk and Safety Statements
  • Hazard and Precautionary Statements (GHS)
Hazard Codes : T,N
Risk Statements : 60-61-51
Safety Statements : 53-22-36/37-57
Hazardous Substances Data: 107868-30-4(Hazardous Substances Data)
Symbol(GHS):
Signal word: Danger
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H319 Causes serious eye irritation Serious eye damage/eye irritation Category 2A Warning P264, P280, P305+P351+P338,P337+P313P
H360 May damage fertility or the unborn child Reproductive toxicity Category 1A, 1B Danger
Precautionary statements:
P201 Obtain special instructions before use.
P280 Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P308+P313 IF exposed or concerned: Get medical advice/attention.

Exemestane Chemical Properties,Usage,Production

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.
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.
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.
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.
Contradictions
1. Not to be used by patients allergic to this drug.
2. Not to be used by pregnant women, breastfeeding women, and children.
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.
Chemical Properties
white to light yellow crystal powder
Uses
An antineoplastic (hormonal)
Uses
antiinfective
Uses
Labeled Exemestane, intended for use as an internal standard for the quantification of Exemestane by GC- or LC-mass spectrometry.
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.
Exemestane Preparation Products And Raw materials
Raw materials
p-Toluenesulfonic acid Etanol Formaldehyde Tetrahydrofuran Benzoic acid
Preparation Products
Exemestane Suppliers      Global( 199)Suppliers     
Supplier Tel Fax Email Country ProdList Advantage
Shenzhen Sendi Biotechnology Co.Ltd. 0755-23311925 18102838259
0755-23311925 Abel@chembj.com CHINA 3230 55
Hubei XinyuanShun Chemical Co., Ltd. 13971561712 / 13995564702 / 027-50664929
027-50664927 hbeixys2001@163.com China 3137 55
Wuhan DKY Technology Co.,Ltd. 027-81302488 18007166089
027-81302088 info@dkybpc.com;2851686510@qq.com China 1936 58
CSSBIO COMPANY LIMITED 0756-8828-109 13411325831
0756-8828 309 54770379@qq.com China 980 58
INTATRADE GmbH +49 3493/605464
+49 3493/605470 sales@intatrade.de Germany 3589 66
3B Pharmachem (Wuhan) International Co.,Ltd. 86-21-50328103 * 801、802、803、804 Mobile:18930552037
86-21-50328109 3bsc@sina.com China 15950 69
Arden pharmaceutical &chemical Co., Ltd +86-(0)533-3595900 13793319233
+86-(0)533-3595900 info@chems.com.cn China 670 61
Chembest Research Laboratories Limited +86(0)21-20908456
+86(0)21-58180499 sales@biochembest.com; market@biochembest.com China 6041 61
Capot Chemical Co., Ltd +86 (0) 571 85 58 67 18
0086-571-85864795 sales@capotchem.com China 18279 66
Pure Chemistry Scientific Inc. 001-857-928-2050 or 1-888-588-9418
001-617-206-9595 sales@chemreagents.com United States 9946 62
 
107868-30-4(Exemestane)Related Search:
EXEMESTANE-19-D3 Androsta-1,4-diene-3,17-dione 1,2-DIMETHYLENE-CYCLOHEXANE Exemestane 6-Methyl-5-hepten-2-one Methyl cyclopentenolone Dimethyl disulfide N,N-Dimethylformamide Dimethyl carbonate Dimethyl ether Dimethyl sulfoxide ETHANE 1-Methyl-2-pyrrolidinone MESITYL OXIDE Dimethyl phthalate Dacthal Dimethyl sulfate METHYL-2-PYRROLIDONE
Intermediates & Fine Chemicals Pharmaceuticals Steroids 156-1-31 (8R,9S,10R,13S,14S)-10,13-Dimethyl-6-methylene-7,8,9,11,12,13,15,16-octahydro-6H-cyclopenta[a]phenanthrene-3,17(10H,14H)-dione Pfizer compounds Steroid and Hormone ExeMestane (USP) ExeMestane(AroMasin) 1,4-Androstadien-3,17-dione-6-Methylene-d2 API ExeMestine (8R,9S,10R,13S,14S)-10,13-diMethyl-6-Methylene-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthrene-3,17(6H)-dione 7868-30-4 Anti-cancer&immunity ExeMestane SynonyMs 6-Methylenandrosta-1,4-diene-3,17-dione PNU155971 Inhibitors Exemestance:6-methyleneandrosta-1,4-diene-3,17-dione Exemestane D2 Exemestane for system suitability 6-methylenandrosta-1,4-diene-3,17-dione 6-METHYLENEANDROSTA-1,4-DIENE-3,17-DIONE 107868-30-4 10,13-dimethyl-6-methylidene-7,8,9,10,11,12,13,14,15,16-decahydrocyclopenta[a]phenanthrene- EXEMESTANE FCE-24304 AROMASIN Exemestan Exemestance C20H24O2 6-Methyleneandrosta-1,4-diene-3,17-dione, FCE-24304, Aromasin 107968-30-4 Androsta-1,4-diene-3,17-dione, 6-methylene Active Pharmaceutical Ingredients chiral Antineoplastic (Hormonal) EXALAMIDE
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