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Namespace Prefixes

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Statements

Subject Item
n2:DB00990
rdf:type
n8:Drug
n8: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.
n8:dosage
n9:271B4AAE-363D-11E5-9242-09173F13E4C5 n9:271B4AAF-363D-11E5-9242-09173F13E4C5 n9:271B4AAD-363D-11E5-9242-09173F13E4C5
n8: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
n8:group
investigational approved
n8:halfLife
24 hours
n8:indication
For the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy.
n8:manufacturer
n17:271B4AAB-363D-11E5-9242-09173F13E4C5
owl:sameAs
n6:DB00990 n11:DB00990
dcterms:title
Exemestane
adms:identifier
n4:Exemestane n20:60198 n21:46508243 n22:D00963 n23:0009-7663-04 n26:4953 n27:C08162 n28:54278 n29:DB00990 n31:PA449563
n8: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.
n8:packager
n17:271B4AA9-363D-11E5-9242-09173F13E4C5 n17:271B4AAA-363D-11E5-9242-09173F13E4C5 n17:271B4AA8-363D-11E5-9242-09173F13E4C5
n8:patent
n24:2409059 n24:4808616
n8:synonym
Exemestanum 6-Methyleneandrosta-1,4-diene-3,17-dione Exemestano Exemestane
n8:toxicity
Convulsions
n18:hasAHFSCode
n25:10-00-00
n8:foodInteraction
High-fat meals increase plasma exemestane concentrations by approximately 40%.
n8:proteinBinding
90% (mainly α1-acid glycoprotein and albumin)
n8:synthesisReference
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.
n13:hasConcept
n14:M0158502
foaf:page
n16:exemest.htm n30:exemestane.html
n8:IUPAC-Name
n10:271B4AB4-363D-11E5-9242-09173F13E4C5
n8:InChI
n10:271B4ABA-363D-11E5-9242-09173F13E4C5
n8:Molecular-Formula
n10:271B4AB9-363D-11E5-9242-09173F13E4C5
n8:Molecular-Weight
n10:271B4AB6-363D-11E5-9242-09173F13E4C5
n8:Monoisotopic-Weight
n10:271B4AB7-363D-11E5-9242-09173F13E4C5
n8:SMILES
n10:271B4AB8-363D-11E5-9242-09173F13E4C5
n8:Water-Solubility
n10:271B4ACA-363D-11E5-9242-09173F13E4C5 n10:271B4AB2-363D-11E5-9242-09173F13E4C5
n8:logP
n10:271B4ACC-363D-11E5-9242-09173F13E4C5 n10:271B4AB3-363D-11E5-9242-09173F13E4C5 n10:271B4AB0-363D-11E5-9242-09173F13E4C5
n8:logS
n10:271B4AB1-363D-11E5-9242-09173F13E4C5
n18:hasATCCode
n19:L02BG06
n8:H-Bond-Acceptor-Count
n10:271B4AC0-363D-11E5-9242-09173F13E4C5
n8:H-Bond-Donor-Count
n10:271B4AC1-363D-11E5-9242-09173F13E4C5
n8:InChIKey
n10:271B4ABB-363D-11E5-9242-09173F13E4C5
n8:Polar-Surface-Area--PSA-
n10:271B4ABC-363D-11E5-9242-09173F13E4C5
n8:Polarizability
n10:271B4ABE-363D-11E5-9242-09173F13E4C5
n8:Refractivity
n10:271B4ABD-363D-11E5-9242-09173F13E4C5
n8:Rotatable-Bond-Count
n10:271B4ABF-363D-11E5-9242-09173F13E4C5
n8:absorption
42%
n8:affectedOrganism
Humans and other mammals
n8:casRegistryNumber
107868-30-4
n8:category
n8:containedIn
n12:271B4AAC-363D-11E5-9242-09173F13E4C5
n8:Bioavailability
n10:271B4AC6-363D-11E5-9242-09173F13E4C5
n8:Ghose-Filter
n10:271B4AC8-363D-11E5-9242-09173F13E4C5
n8:MDDR-Like-Rule
n10:271B4AC9-363D-11E5-9242-09173F13E4C5
n8:Melting-Point
n10:271B4ACB-363D-11E5-9242-09173F13E4C5
n8:Number-of-Rings
n10:271B4AC5-363D-11E5-9242-09173F13E4C5
n8:Physiological-Charge
n10:271B4AC4-363D-11E5-9242-09173F13E4C5
n8:Rule-of-Five
n10:271B4AC7-363D-11E5-9242-09173F13E4C5
n8:Traditional-IUPAC-Name
n10:271B4AB5-363D-11E5-9242-09173F13E4C5
n8:pKa--strongest-acidic-
n10:271B4AC2-363D-11E5-9242-09173F13E4C5
n8:pKa--strongest-basic-
n10:271B4AC3-363D-11E5-9242-09173F13E4C5