| Attributes | Values |
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| rdf:type
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| http://linked.open...gbank/description
| - Formestane was the first selective, type I, steroidal aromatase inhibitor used in the treatment of estrogen-receptor positive breast cancer in post-menopausal women. Formestane suppresses estrogen production from anabolic steroids or prohormones. It also acts as a prohormone to 4-hydroxytestosterone, an active steroid which displays weak androgenic activity in addition to acting as a mild aromatase inhibitor. It is listed as a prohibited substance by the World Anti-Doping Agency for use in athletes. Formestane has poor oral bioavailability, and thus must be administered forthnightly (bi-weekly) by intramuscular injection. Some clinical data has suggested that the clinically recommended dose of 250mg was too low. With the discovery of newer, non-steroidal and steroidal, aromatase inhibitors which were orally active and less expensive than formestane, formestane lost popularity. Currently, formestane (categorized as an anti-estrogenic agent) is prohibited from use in sports in accordance to the regulations of the World Anti-Doping Agency. It is not US FDA approved, and the intramuscular injection form of formestane (Lentaron) which was approved in Europe has been withdrawn. (en)
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| http://linked.open...generalReferences
| - 1. Kohler, Maxie, et al. "Metabolism of 4-hydroxyandrostenedione and 4-hydroxytestosterone: Mass spectrometric identification of urinary metabolites." Steroids 72.3 (2007): 278-286. 2. Lønning, Per Eystein, et al. "Pharmacokinetics and metabolism of formestane in breast cancer patients." The Journal of steroid biochemistry and molecular biology 77.1 (2001): 39-47. 3. Murray, R., and P. Pitt. "Treatment of advanced breast cancer with formestane." Annals of oncology: official journal of the European Society for Medical Oncology/ESMO 5 (1994): S11. 4. Perez Carrion R, Alberola Candel V, Calabresi F, Michel RT, Santos R, Delozier T, Goss P, Mauriac L, Feuilhade F, Freue M, et al.: Comparison of the selective aromatase inhibitor formestane with tamoxifen as first-line hormonal therapy in postmenopausal women with advanced breast cancer. Ann Oncol. 1994;5 Suppl 7:S19-24. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/7873457 5. Vorobiof, D. A., et al. "A randomized, open, parallel-group trial to compare the endocrine effects of oral anastrozole (Arimidex®) with intramuscular formestane in postmenopausal women with advanced breast cancer." Annals of oncology 10.10 (1999): 1219-1225. (en)
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| http://linked.open...gy/drugbank/group
| - approved (en)
- withdrawn (en)
- investigational (en)
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| http://linked.open...drugbank/halfLife
| - Terminal plasma elimination half life of 18 minutes, when delivered intravenously. [2] (en)
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| http://linked.open...ugbank/indication
| - For the treatment of estrogen-receptor positive breast cancer in post-menopausal women. (en)
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| sameAs
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| Title
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| adms:identifier
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| http://linked.open...mechanismOfAction
| - Formestane is a second generation, irreversible, steroidal aromatase inhibitor. It inhibits the aromatase enzyme responsible for converting androgens to estrogens, thereby preventing estrogen production. Breast cancer may be estrogen sensitive or insensitive. A majority of breast cancers are estrogen sensitive. Estrogen sensitive breast cancer cells depend on estrogen for viability. Thus removal of estrogen from the body can be an effective treatment for hormone sensitive breast cancers. Formestane has been targeted specifically for the treatment of postmenopausal women. Unlike premenopausal women who produce most estrogen in the ovaries, postmenopausal women produce most estrogen in peripheral tissues with the help of the aromatase enzyme. Formestane, an aromatase inhibitor, can thus help to decrease the local production of estrogen by blocking the aromatase enzyme in peripheral tissues (ie. adispose tissue of the breast) to treat hormone sensitive breast cancer. (en)
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| http://linked.open...outeOfElimination
| - Renal elimination. >95% in urine, <5% in feces. (en)
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| http://linked.open.../drugbank/synonym
| - 4-Hydroxy-delta(4)-androstenedione (en)
- 4-OH-A (en)
- 4-OHAD (en)
- 4-hydroxy-4-androstene-3,17-dione (en)
- 4-hydroxy-Δ4-androstenedione (en)
- 4-hydroxyandrostenedione (en)
- CGP 32349 (en)
- CGP-32349 (en)
- Formestano (en)
- Formestanum (en)
- Lentaron (en)
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| http://linked.open...umeOfDistribution
| - Vd = 1.8 L/kg; widely distributed to organs and tissues when delivered intravenously. [2] (en)
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| http://linked.open...ynthesisReference
| - Kohler, Maxie, et al. "Metabolism of 4-hydroxyandrostenedione and 4-hydroxytestosterone: Mass spectrometric identification of urinary metabolites." Steroids 72.3 (2007): 278-286. (en)
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| foaf:page
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| http://linked.open...ugbank/IUPAC-Name
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| http://linked.open...gy/drugbank/InChI
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| 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...logy/drugbank/pKa
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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
| - Formestane has poor oral bioavailability, but is fully bioavailable when administered via the established intramuscular route. The AUC after an intravenous pulse dose does not vary considerably from that of an intramuscular dose. Within 24-48 h of the first dose of intramuscular formestane, a C(max) of 48.0 +/- 20.9 nmol/l was achieved in one study. [2] (en)
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| http://linked.open...casRegistryNumber
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| http://linked.open...drugbank/category
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| http://linked.open...rugbank/clearance
| - Plasma clearance is approximately 4.2 L/(h kg), when delivered intravenously. In women, following a 500mg dose of formestane, 20% was excreted as glucuronide within the first 24 hours. [1] One long term metabolite (3beta,4alpha-dihydroxy-5alpha-androstan-17-one) can be detected for 90 hours. A longer detection time is possible with more sensitive technology, which may be of utility in sports drug testing. [1] (en)
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| http://linked.open...k/Bioavailability
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| http://linked.open...bank/Ghose-Filter
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| 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
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| http://linked.open...strongest-acidic-
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| http://linked.open...-strongest-basic-
| |
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