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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;Exemestan;FCE-24304;EXALAMIDE;PNU155971;EXEMESTANE;ExeMestine;Exemestance;Exemestane D2
        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. 
        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
        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(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 $83.7 2019-12-02 Buy
        Sigma-Aldrich 1269050 Exemestane United States Pharmacopeia (USP) Reference Standard 107868-30-4 150mg $352.8 2019-12-02 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 2019-12-02 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( 279)Suppliers
        Supplier Tel Fax Email Country ProdList Advantage
        Rixing Chemical CO.,LTD. 13237129059
        - info@rixingchemi.com China 233 58
        Hubei Xinyuanshun Pharmaceutical Chemical Co., Ltd. 027-51831887 15337167856
        027-51837635 QQ1165326703 hubeixinyuanshun@163.com China 10324 58
        Shanghai Yuqing Chemical Co., Ltd. 18601759286/QQ2657504708
        13166185202 2603375875@qq.com China 57 58
        INTATRADE GmbH +49 3493/605464
        +49 3493/605470 sales@intatrade.de Germany 3579 66
        3B Pharmachem (Wuhan) International Co.,Ltd. 86-21-50328103 * 801、802、803、804 Mobile:18930552037
        86-21-50328109 3bsc@sina.com China 15881 69
        Arden pharmaceutical &chemical Co., Ltd +86-(0)533-3595900 13793319233
        +86-(0)533-3595900 info@chems.com.cn China 669 61
        Chembest Research Laboratories Limited 021-20908456-
        021-58180499 sales@BioChemBest.com China 5984 61
        Capot Chemical Co., Ltd +86 (0) 571 85 58 67 18
        0086-571-85864795 sales@capotchem.com China 18228 66
        Pure Chemistry Scientific Inc. 001-857-928-2050 or 1-888-588-9418
        001-617-206-9595 sales@chemreagents.com United States 9919 62
        Chemfun Medical Technology(Shanghai) Co., Ltd. 021-67220633 & 021-37212706
        +86-21-67220638 chemfun@chemfun.net China 21810 59

        Related articles


        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.
        2019-10-31 exemestane
        107868-30-4
        US $0.00 / KG 1g 99.9% 1 ton Hebei shuoxi biotechnology co. LTD
        2019-10-22 Exemestane
        107868-30-4
        US $66.00 / Kg/Bag 10g 99% 20tons Hebei shuoxi biotechnology co. LTD

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