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Exemestane

Indications and Usage Pharmacokinetics Drug interactions Side effects Clinical Research Contradictions Warnings and precautions
Exemestane
Exemestane structure
CAS No.
107868-30-4
Chemical Name:
Exemestane
Synonyms
AROMASIN;Exemestan;FCE-24304;EXALAMIDE;PNU155971;EXEMESTANE;ExeMestine;Exemestance;Exemestane D2;ExeMestane (USP)
CBNumber:
CB5760314
Molecular Formula:
C20H24O2
Formula Weight:
296.4
MOL File:
107868-30-4.mol

Exemestane Properties

Melting point:
155.13°C
storage temp. 
Store at -20°C
solubility 
DMSO: ≥20mg/mL
form 
powder
color 
white to off-white
optical activity
[α]/D +250 to +300°, c = 1 in methanol
InChIKey
BFYIZQONLCFLEV-DAELLWKTSA-N
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
WGK Germany  3
HS Code  29372900
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 price More Price(10)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich PHR1634 Exemestane Pharmaceutical Secondary Standard; Certified Reference Material 107868-30-4 1g $81.9 2018-11-20 Buy
Sigma-Aldrich 1269050 Exemestane United States Pharmacopeia (USP) Reference Standard 107868-30-4 150mg $352.8 2018-11-20 Buy
Cayman Chemical 15008 Exemestane ≥95% 107868-30-4 5mg $75 2018-11-13 Buy
Cayman Chemical 15008 Exemestane ≥95% 107868-30-4 10mg $105 2018-11-13 Buy
Sigma-Aldrich PZ0006 Exemestane ≥98% (HPLC) 107868-30-4 5mg $105 2018-11-20 Buy

Exemestane Chemical Properties,Uses,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.

Description

Exemestane was launched in US and other countries for the treatment of estrogendependent tumors and postmenopausal breast cancer. It is a novel steroidal compound structurally related to the natural substrate for the biosynthesis of estrogen, androstanedione, and can be synthesized by methylidenation of androsta-1, 4-dien- 17beta-ol-3-one in 6 position then oxidation of the alcohol function. Exemestane is an irreversible inactivator of the aromatase enzyme system, so inducing in vivo a dose-related sustained suppression of serum estrogen and minimal endocrine activity. It is the first steroidal representative of the third-generation of orally active aromatase inhibitors with a highly potent and selective mechanism of action, displaying good tolerability and safety profile. In rats with DMBA-induced mammary tumors, 10 to 100 mglkg of exemestan administered po twice-daily for 4 weeks resulted in 76 to 88% regression. In women failing anti-estrogen therapy with tamoxifen, this agent has demonstrated high activity in locally advanced or metastatic disease. In addition, it may also have potential for breast cancer prevention.

Chemical Properties

white to light yellow crystal powder

Originator

Farmitalia Carlo Erba (Italy)

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.

brand name

Aromasin (Pharmacia& Upjohn).

General Description

Exemestane, 6-methylenandrosta-1,4-diene-3,17-dione (Aromasin), is the first steroid-basedaromatase inhibitor approved for the treatment of breastcancer in the United States. It is a mechanism-based inactivatorthat irreversibly inhibits the enzyme. Plasma estrogenlevels are reduced by 85% to 95% within 2 to 3 days, and effectslast 4 to 5 days. Exemestane does not inhibit any of themajor cytochromes P450 and has essentially no interactionwith steroid receptors, with only a very weak affinity for theAR. The 17β-hydroxyexemestane reduction product, however,has much higher affinity for the AR than the parent(still several fold less than DHT, 0.28% for parent vs. 30%for metabolite). The clinical significance of the affinity islikely minimal because of the low levels of the metaboliteproduced.

Hazard

A reproductive hazard.

Exemestane Preparation Products And Raw materials

Raw materials

Preparation Products


Exemestane Suppliers

Global( 254)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Rixing Chemical CO.,LTD
13237129059
- [email protected] CHINA 235 55
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925 [email protected] CHINA 3202 55
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 [email protected] CHINA 1817 55
Hebei Jiangkai Trading Co., Ltd
0086-17197824289/17197824028
[email protected] CHINA 272 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 [email protected] CHINA 20672 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 [email protected] CHINA 32447 55
PI & PI BIOTECH INC.
020-81716320
020-81716319 [email protected] CHINA 2543 55
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070;[email protected]
[email protected] CHINA 3015 60
Hubei XinRunde Chemical Co., Ltd.
+8615102730682; +8618874586545
02783214688 [email protected] CHINA 535 55
Nanjing Finetech Chemical Co., Ltd.
025-85710122 17714198479
025-85710122 [email protected] CHINA 892 55

View Lastest Price from Exemestane manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2019-04-25 Exemestane
107868-30-4
US $10.00 / kg 1kg 99% 10 MT Hebei Guanlang Biotechnology Co., Ltd.
2019-05-29 Aromasin/exemestane
107868-30-4
US $1.00 / g 1g 99% 2000kg Cangzhou Wanyou New Material Technology Co.,Ltd
2018-12-16 Exemestane
107868-30-4
US $7.00 / kg 1kg 99% 100kg career henan chemical co

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