Toremifene

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Toremifene
Systematic (IUPAC) name
2-[4-(4-chloro-1, 2-diphenyl-but-1-enyl)phenoxy]- N,N-dimethyl-ethanamine
Identifiers
CAS number	89778-26-7
ATC code	L02BA02
PubChem	3005573
DrugBank	APRD00391
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	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	?

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]

[edit] References

1. ^ 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
2. ^ 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.

v • d • e Sex hormones and related agents (primarily G03, also L02, H01C) - human endogenous in CAPS Progestogens: (receptor) PROGESTERONE,Dienogest, Desogestrel, Drospirenone, Dydrogesterone, Ethisterone, Etonogestrel, Ethynodiol diacetate, Gestodene, Gestonorone, Levonorgestrel, Lynestrenol, Medroxyprogesterone, Megestrol, Norelgestromin, Norethisterone, Norethynodrel, Norgestimate, Norgestrel, Norgestrienone, Tibolone Selective progesterone receptor modulator: Asoprisnil, CDB-4124 Antiprogestogen: Mifepristone Androgens: (receptor) TESTOSTERONE, Androstanolone, Fluoxymesterone, Mesterolone, Methyltestosterone, (see also anabolic steroids) Antiandrogens: Bicalutamide, Cyproterone, Dienogest, Flutamide, Nilutamide, Spironolactone Estrogens: (receptor) ESTRADIOL, ESTRIOL, ESTRONE, Chlorotrianisene, Dienestrol, Diethylstilbestrol, Ethinylestradiol, Fosfestrol, Mestranol, Polyestradiol phosphate Selective estrogen receptor modulator: Afimoxifene, Arzoxifene, Bazedoxifene, Clomifene, Fulvestrant, Lasofoxifene, Raloxifene, Tamoxifen, Toremifene Aromatase inhibitor: Aminogluthetimide, Anastrozole, Atamestane, Exemestane, Formestane, Letrozole, Vorozole Gonadotropins: (FSHR/LHCGR) ovulation stim.: Clomifene, Urofollitropin Antigonadotropins: Danazol, Gestrinone GnRH: (receptor) agonist: Buserelin, Goserelin, Histrelin, Leuprorelin, Nafarelin, Triptorelin antagonist: Abarelix, Cetrorelix, Ganirelix