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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
    EXE;AROMASIN;PNU155971;Exemestan;FCE-24304;EXALAMIDE;ExeMestine;Exemestone;EXEMESTANE;Exemestance
    CBNumber:
    CB5760314
    Molecular Formula:
    C20H24O2
    Formula Weight:
    296.4
    MOL File:
    107868-30-4.mol

    Exemestane Properties

    Melting point:
    155.13°C
    Boiling point:
    453.7±45.0 °C(Predicted)
    Density 
    1.13±0.1 g/cm3(Predicted)
    storage temp. 
    2-8°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)
    FDA UNII
    NY22HMQ4BX
    NCI Dictionary of Cancer Terms
    Aromasin; exemestane
    NCI Drug Dictionary
    Aromasin
    SAFETY
    • Risk and Safety Statements
    Symbol(GHS) 
    GHS07,GHS08
    Signal word  Danger
    Hazard statements  H319-H360
    Precautionary statements  P201-P280-P305+P351+P338-P308+P313
    Hazard Codes  T,N
    Risk Statements  60-61-51
    Safety Statements  53-22-36/37-57
    WGK Germany  3
    HS Code  29372900

    Exemestane price More Price(12)

    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 $95.8 2021-03-22 Buy
    Sigma-Aldrich Y0001756 Exemestane for system suitability European Pharmacopoeia (EP) Reference Standard 107868-30-4 $190 2021-03-22 Buy
    Sigma-Aldrich Y0001747 Exemestane European Pharmacopoeia (EP) Reference Standard 107868-30-4 $190 2021-03-22 Buy
    Sigma-Aldrich 1269050 Exemestane United States Pharmacopeia (USP) Reference Standard 107868-30-4 150mg $366 2021-03-22 Buy
    Cayman Chemical 15008 Exemestane ≥95% 107868-30-4 5mg $35 2021-03-22 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.

    Manufacturing Process

    0.50 g of 6-methylenandrost-4-ene-3,17-dione and 0.57 g of dichlorodicyanobenzoquinone were refluxed in 20 ml of anhydrous dioxane for about 15 hours. To remove the DDQ the suspension was filtered through alumina. After evaporation of the solvent the residue was dissolved in ethyl acetate, the organic layer washed with water, dried over sodium sulfate and the solvent removed under vacuum. The crude product was chromatographed on silica gel using hexane/ethyl acetate to yield 0.25 g of pure 6- methylenandrosta-1,4-diene-3,17-dione, m.p. 188-191°C, λmax 247 nm (ε 13.750).

    brand name

    Aromasin (Pharmacia& Upjohn).

    Therapeutic Function

    Antineoplastic

    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( 379)Suppliers
    Supplier Tel Fax Email Country ProdList Advantage
    Shanghai Longyu Biotechnology Co., Ltd.
    +8615821988213
    info@longyupharma.com CHINA 2462 58
    Hebei Bonster Technology Co.,Limited
    +86-13315996897
    0086-13315996897 Wendy@bsterltd.com CHINA 998 58
    WUHAN CIRCLE POWDER TECHNOLOGY CO.,LTD
    15327141851 027-81302090
    027-81302088 2851686515@qq.com CHINA 280 58
    Shijiazhuang Erche Biotechnology Co., Ltd
    13343119830 8613343119830
    QQ: 956730943 info07@byyq-cn.com CHINA 408 58
    Changzhou Xuanming Chemical Co., Ltd.
    18068519287 +8618068519287
    sales@xuanmingchem.com CHINA 301 58
    Hebei Ruiyao Biotechnology Co. Ltd
    15532235888 15632182983
    031188180881 admin@ruiyaobio.com CHINA 846 58
    Hebei Yirun Sega Biological Technology Co. Ltd
    19932103556 +8619932103556
    +8619932103556 linda@yrsjbiotech.com CHINA 734 58
    Zhejiang J&C Biological Technology Co.,Limited
    +8615857007529
    sales@sarms4muscle.com CHINA 297 58
    Beijing Cooperate Pharmaceutical Co.,Ltd
    010-60279497
    010-60279497 sales01@cooperate-pharm.com CHINA 1817 55
    Henan Tianfu Chemical Co.,Ltd.
    0371-55170693
    0371-55170693 info@tianfuchem.com CHINA 22607 55

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    View Lastest Price from Exemestane manufacturers

    Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
    2021-10-20 Exemestane
    107868-30-4
    US $10.00 / KG 1KG 99.9% 100MT/Month Wuhan wingroup Pharmaceutical Co., Ltd
    2021-10-20 Exemestane
    107868-30-4
    US $0.00 / KG 100g 98%+ 100kg WUHAN CIRCLE POWDER TECHNOLOGY CO.,LTD
    2021-10-19 Exemestane
    107868-30-4
    US $370.00 / g 10g 99% 1000kg/month Shanxi Lianxu New Material Co., LTD

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