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Exemestane
drug data and news
Exemestane drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Exemestane | ||
| Brand Names/Synonyms | Aromasin; EXEMESTANE; Exemestance; Exemestane; Exemestane [Inn]; Exemestane [Usan:Inn:Ban]; Exemestano [Inn-Spanish]; Exemestanum [Inn-Latin] | ||
| Indication | For the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy. | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | aromatase is an enzyme that converts hormones to estrogen in the body's adrenal glands. The aromatase inhibitors (AIs) are drugs that reduce estrogen levels by blocking the action of aromatase in the adrenal glands. The selective AIs (SAIs) selectively reduce levels of estrogen without interfering with levels of other steroid hormones that are produced by the adrenal gland. Drugs in this class include anastrozole (ArimidexÆ), letrozole (FemaraÆ) and exemestane (AromasinÆ). | ||
| Mechanism Of Action | 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 adrenal biosynthesis of corticosteroids or aldosterone. 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. | ||
| Exemestane News (When available) |
Aromasin® Improves Breast Cancer Outcomes Without Compromising ... Feb 28, 2006 Optimising Herceptin-based Therapy in HER2-positive Metastatic ... Feb 22, 2006 Generalists Equal Specialists in Follow-Up Care for Early Breast ... Feb 20, 2006 Buddies For Life: Medication May Prevent Some Forms Of Breast ... Feb 8, 2006 Buddies For Life: Medication May Prevent Some Forms Of Breast ... Feb 8, 2006 Warning of risk of from vaginal oestrogen Jan 26, 2006 Vaginal Dryness Meds May Counteract Breast Cancer Drugs Jan 26, 2006 Women With Breast Cancer Beware Jan 25, 2006 The drug that may improve the outcome for high-risk women Jan 20, 2006 (PRN) US Oncology Research Network Presenting Numerous Studies at ... 11 Dec 2005 ARIMIDEX(R) (anastrozole) Featured in Studies Evaluating Impact of ... Dec 9, 2005 Femara gets approval for early adjuvant use in UK Dec 8, 2005 Fresh hope for Scots as cancer drug approved Nov 16, 2005 Few takers for preventive drug Nov 15, 2005 Scots will be first to receive new breast cancer drug Nov 15, 2005 Scots get cancer drug first Nov 16, 2005 Aromasin® Approved for Early Breast Cancer Oct 10, 2005 Local study testing drug to prevent breast cancer Oct 9, 2005 FDA Approves Pfizer's Aromasin (Exemestane Tablets) for Adjuvant ... Oct 5, 2005 FDA Approves Pfizer's Aromasin Treament Oct 6, 2005 International Approvals: Aromasin, IPM Wound Gel, Risperdal Consta Sep 19, 2005 Breast Cancer Weight Gain Oct 7, 2005 Pfizer Receives European Approval to Market Aromasin(R) for ... Sep 13, 2005 Confusion over drug funds hit cancer sufferers Sep 12, 2005 Pfizer breast-cancer drug wins EU green light Sep 13, 2005 British confusion seen with cancer drugs Sep 13, 2005 COMUNICADO: New International Treatment Guidelines Verify Crucial ... Sep 7, 2005 Benefit With Aromatase Inhibitors in the Adjuvant Setting for ... Aug 25, 2005 Talking about a revolution in breast cancer treatment Sep 5, 2005 Breast Cancer Adjuvant Therapy May Trigger Joint Pain Sep 2, 2005 Some Loss of Hip Bone Density Among Postmenopausal Women Treated ... Aug 11, 2005 Breast cancer treatment options multiply Aug 29, 2005 Carle Breast Cancer Study Aug 24, 2005 Breast cancer, switch to Anastrozole after two years of Tamoxifen ... Aug 14, 2005 Carle joins in major drug trial Aug 3, 2005 AstraZeneca breast cancer drug can improve survival: study Aug 5, 2005 New Weapon In Breast Cancer Fight? Jul 25, 2005 National Breast Cancer Study Jul 20, 2005 Cancer therapy: clinical trials to trigger antihormonals market ... Jul 8, 2005 | ||
| Dosage Forms | tablets | ||
| Drug_Category | Antineoplastic Agents; ATC:L02BG06 | ||
| Absorption | 42% | ||
| Interactions |
-->Interactions for Exemestane: Exemestane is extensively metabolized by CYP 3A4, but coadministration of ketoconazole, a potent inhibitor of CYP 3A4, has no significant effect on exemestane pharmacokinetics. Significant pharmacokinetic interactions mediated by inhibition of CYP isoenzymes therefore appear unlikely. Co-medications that induce CYP 3A4 (e.g., rifampicin, phenytoin, carbamazepine, phenobarbital, or St. Johnís wort) may significantly decrease exposure to exemestane. Dose modification is recommended for patients who are also receiving a potent CYP 3A4 inducer (see DOSAGE AND ADMINISTRATION and CLINICAL PHARMACOLOGY). Drug/Laboratory Tests Interactions No clinically relevant changes in the results of clinical laboratory tests have been observed. | ||
| Toxicity | Convulsions | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 10,13-dimethyl-6-methylidene-7,8,9,10,11,12,13,14,15,16-decahydrocyclopenta[a]phenanthrene-3,17-dione | ||
| Chemical Formula | C20H24O2 | ||
| Molecular Weight | 296.403 g/mol | ||
| Smiles String | CC12CCC3C(C1CCC2=O)CC(=C)C4=CC(=O)C=CC34C | ||
| Melting Point | 155.13°C | ||
| Water Solubility | non-soluble | ||
| State | Solid | ||
| LogP/Hphobicity | 4.222 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic | ||
| Half Life | 24 hours | ||
| Protein Binding [%] | 90% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Exemestane.html http://www.rxlist.com/cgi/generic3/exemest.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00144 | ||
| CAS Registry Number | 107868-30-4 | ||
| KEGG Compound ID | C08162 | ||
| PubChem ID | SID:196561 | ||
| PharmGKB ID | Not Available | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2242705 |
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