Toremifene
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| Toremifene
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| Systematic (IUPAC) name | |
| 2-[4-(4-chloro-1, 2-diphenyl-but-1-enyl)phenoxy]- N,N-dimethyl-ethanamine | |
| Identifiers | |
| CAS number | |
| ATC code | L02 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C26H28ClNO |
| Mol. mass | 405.959 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Protein binding | more than 99.5% |
| Metabolism | ? |
| Half life | 5 days |
| Excretion | ? |
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| Pregnancy cat. |
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| Routes | ? |
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Toremifene citrate is an oral selective estrogen receptor modulator (SERM) which helps oppose the actions of estrogen in the body. Licensed in the United States under the brand name Fareston, toremifene citrate is FDA approved for use in advanced (metastatic) breast cancer. It is also being evaluated for prevention of prostate cancer under the brand name Acapodene.[1]
GTx Inc. is currently conducting two different phase 3 clinical trials; First, a pivotal Phase clinical trial for the treatment of serious side effects of androgen deprivation therapy (especially vertebral/spine fractures and hot flashes, lipid profile, and gynecomastia) for advanced prostate cancer, and second, a pivotal Phase III clinical trial for the prevention of prostate cancer in high risk men with high grade prostatic intraepithelial neoplasia, or PIN. Results of these trials are expected by first quarter of 2008[2]
References
- ↑ Price N, Sartor O, Hutson T, Mariani S. Role of 5a-reductase inhibitors and selective estrogen receptor modulators as potential chemopreventive agents for prostate cancer. Clin Prostate Cancer 2005;3:211-4. PMID 15882476
- ↑ GTx Inc. (2007-07-12). GTx's Phase III Clinical Development of ACAPODENE on Course Following Planned Safety Review. Press release. Retrieved on 2006-07-14.
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