| Attributes | Values |
|---|
| rdf:type
| |
| http://linked.open...gbank/description
| - Exemestane is an oral steroidal aromatase inhibitor used in the adjuvant treatment of hormonally-responsive (also called hormone-receptor-positive, estrogen-responsive) breast cancer in postmenopausal women. It acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme causing its inactivation. (en)
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| http://linked.open...y/drugbank/dosage
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| http://linked.open...generalReferences
| - # Coombes RC, Kilburn LS, Snowdon CF, Paridaens R, Coleman RE, Jones SE, Jassem J, Van de Velde CJ, Delozier T, Alvarez I, Del Mastro L, Ortmann O, Diedrich K, Coates AS, Bajetta E, Holmberg SB, Dodwell D, Mickiewicz E, Andersen J, Lonning PE, Cocconi G, Forbes J, Castiglione M, Stuart N, Stewart A, Fallowfield LJ, Bertelli G, Hall E, Bogle RG, Carpentieri M, Colajori E, Subar M, Ireland E, Bliss JM: Survival and safety of exemestane versus tamoxifen after 2-3 years' tamoxifen treatment (Intergroup Exemestane Study): a randomised controlled trial. Lancet. 2007 Feb 17;369(9561):559-70. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17307102 # Robinson A: A review of the use of exemestane in early breast cancer. Ther Clin Risk Manag. 2009 Feb;5(1):91-8. Epub 2009 Mar 26. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19436613 # Untch M, Jackisch C: Exemestane in early breast cancer: a review. Ther Clin Risk Manag. 2008 Dec;4(6):1295-304. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19337436 # Abrial C, Durando X, Mouret-Reynier MA, Thivat E, Bayet-Robert M, Nayl B, Dubray P, Pomel C, Chollet P, Penault-Llorca F: Role of neo-adjuvant hormonal therapy in the treatment of breast cancer: a review of clinical trials. Int J Gen Med. 2009 Jul 30;2:129-40. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20360896 # Nabholtz JM: Long-term safety of aromatase inhibitors in the treatment of breast cancer. Ther Clin Risk Manag. 2008 Feb;4(1):189-204. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18728707 (en)
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| http://linked.open...gy/drugbank/group
| - approved (en)
- investigational (en)
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| http://linked.open...drugbank/halfLife
| |
| http://linked.open...ugbank/indication
| - For the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy. (en)
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| http://linked.open...bank/manufacturer
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| sameAs
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| Title
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| adms:identifier
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| http://linked.open...mechanismOfAction
| - Breast cancer cell growth may be estrogen-dependent. Aromatase (exemestane) is the principal enzyme that converts androgens to estrogens both in pre- and postmenopausal women. While the main source of estrogen (primarily estradiol) is the ovary in premenopausal women, the principal source of circulating estrogens in postmenopausal women is from conversion of adrenal and ovarian androgens (androstenedione and testosterone) to estrogens (estrone and estradiol) by the aromatase enzyme in peripheral tissues. Estrogen deprivation through aromatase inhibition is an effective and selective treatment for some postmenopausal patients with hormone-dependent breast cancer. Exemestane is an irreversible, steroidal aromatase inactivator, structurally related to the natural substrate androstenedione. It acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme causing its inactivation, an effect also known as "suicide inhibition". Exemestane significantly lowers circulating estrogen concentrations in postmenopausal women, but has no detectable effect on the adrenal biosynthesis of corticosteroids or aldosterone. This reduction in serum and tumor concentrations of estrogen delays tumor growth and disease progression. Exemestane has no effect on other enzymes involved in the steroidogenic pathway up to a concentration at least 600 times higher than that inhibiting the aromatase enzyme. (en)
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| http://linked.open...drugbank/packager
| |
| http://linked.open...y/drugbank/patent
| |
| http://linked.open.../drugbank/synonym
| - Exemestane (en)
- 6-Methyleneandrosta-1,4-diene-3,17-dione (en)
- Exemestano (en)
- Exemestanum (en)
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| http://linked.open...drugbank/toxicity
| |
| http://linked.open.../drug/hasAHFSCode
| |
| http://linked.open...k/foodInteraction
| - High-fat meals increase plasma exemestane concentrations by approximately 40%. (en)
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| http://linked.open...nk/proteinBinding
| - 90% (mainly α1-acid glycoprotein and albumin) (en)
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| http://linked.open...ynthesisReference
| - Kevin Kunnen, Nathan W. Stehle, Scot W. Weis, John M. Pascone, Richard J. Pariza, Scott G. Van Ornum, Paul Zizelman, "Exemestane and Its Intermediates and Methods of Making the Same." U.S. Patent US20080234505, issued September 25, 2008. (en)
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| foaf:page
| |
| http://linked.open...ugbank/IUPAC-Name
| |
| http://linked.open...gy/drugbank/InChI
| |
| http://linked.open...Molecular-Formula
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| http://linked.open.../Molecular-Weight
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| http://linked.open...noisotopic-Weight
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| http://linked.open...y/drugbank/SMILES
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| http://linked.open.../Water-Solubility
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| http://linked.open...ogy/drugbank/logP
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| http://linked.open...ogy/drugbank/logS
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| http://linked.open...l/drug/hasATCCode
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| http://linked.open...nd-Acceptor-Count
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| http://linked.open...-Bond-Donor-Count
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| http://linked.open...drugbank/InChIKey
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| http://linked.open...urface-Area--PSA-
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| http://linked.open...nk/Polarizability
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| http://linked.open...bank/Refractivity
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| http://linked.open...atable-Bond-Count
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| http://linked.open...ugbank/absorption
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| http://linked.open.../affectedOrganism
| - Humans and other mammals (en)
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| http://linked.open...casRegistryNumber
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| http://linked.open...drugbank/category
| |
| http://linked.open...gbank/containedIn
| |
| http://linked.open...k/Bioavailability
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| http://linked.open...bank/Ghose-Filter
| |
| http://linked.open...nk/MDDR-Like-Rule
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| http://linked.open...ank/Melting-Point
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| http://linked.open...k/Number-of-Rings
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| http://linked.open...siological-Charge
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| http://linked.open...bank/Rule-of-Five
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| http://linked.open...tional-IUPAC-Name
| |
| http://linked.open...strongest-acidic-
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| http://linked.open...-strongest-basic-
| |
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