Tamoxifen (True Twenty) 30.4mg/ml , 60ML

Tamoxifen (True Twenty) 30.4mg/ml , 60ML

Brand: Full Catalog
Product Code: TX60
Availability:
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Price: $60.00
Description

Tamoxifen Catalog Description (30.4mg/ml, 60ml)

Tamoxifen (trade name Nolvadex) is a selective estrogen receptor modulator (SERM) that acts as an estrogen receptor (ER) antagonist in breast tissue; uses of tamoxifen include treatment of breast cancer in women after menopause and treatment of female infertility caused by ovulatory dysfunction[1][2]. Tamoxifen is sometimes used off-label by clinicians for treatment of drug-induced gynecomastia, as an androgen substitute, and for male infertility[3][4][6][5][7][8]. Other documented effects of SERMs such as tamoxifen include increased bone mass and reduced cholesterol, without the negative side-effects of excessive estrogens[9].

The primary mechanism of action for the main functions of tamoxifen is estrogen receptor (ER) antagonism, wherein tamoxifen or its metabolites bind to the ER with no effect, and displace or prevent binding of estrogen[2][3]. The actual effects of tamoxifen administration occur locally (as in breast cancer or gynecomastia) as well as downstream (as in hypothalamic-pituitaric mediated effects such as androgen substitute and male infertility)[5][7][9]. Tamoxifen can raise testosterone in men by lowering bound estradiol and triggering a negative hypothalamic feedback loop; high estrogen levels cause the body to inhibit production of the male hormone testosterone, while tamoxifen reverses this cascade without actually lowering circulating estrogen[7].

A lesser-known mechanism of action of tamoxifen is ER agonism or partial activation;  this mechanism is responsible for the observed increased bone mass, reduced total and low-density lipoprotein (LDL) cholesterol numbers, and vaginal/uterine effects[9][10][11]. The partial agonism in some cell types is the reason tamoxifen belongs to the SERM class of compounds.
 
Citations: 
[1] The BIG 1-98 Collaborative Group.  Letrozole Therapy Alone or in Sequence with Tamoxifen in Women with Breast Cancer. N Engl J Med, 361:766 Aug. 20, 2009.
[2] Steiner AZ, Terplan M, Paulson RJ. Comparison of tamoxifen and clomiphene citrate for ovulation induction: a meta-analysis. Hum. Reprod. 20 (6): 1511–5. 2005.
[3] "Evaluation and management of gynecomastia" (French).Rev Med Suisse. 2009 Apr 8;5(198):783-7.
[4] Eckman A, Dobs A.  Drug-induced gynecomastia.  Expert Opin Drug Saf. 2008 Nov;7(6):691-702.
[5] Adamopoulos DA, Pappa A, Billa E, Nicopoulou S, Koukkou E, Michopoulos J.  Effectiveness of combined tamoxifen citrate and testosterone undecanoate treatment in men with idiopathic oligozoospermia.  Fertil Steril. 2003 Oct;80(4):914-20.
[6] Turek PJ, Williams RH, Gilbaugh JH 3rd, Lipshultz LI. The reversibility of anabolic steroid-induced azoospermia. J Urol. 1995 May;153(5):1628-30.
[7] Tsourdi E, Kourtis A, Farmakiotis D, Katsikis I, Salmas M, Panidis D.  The effect of selective estrogen receptor modulator administration on the hypothalamic-pituitary-testicular axis in men with idiopathic oligozoospermia. Fertil Steril. 2009 Apr;91(4 Suppl):1427-30.
[8]Adamopoulos DA, Nicopoulou S, Koukkou E, Pappa A, Billa Responsiveness to tamoxifen citrate and testosterone undecanoate is independent of the severity of idiopathic oligozoospermia. J Androl. 2005 Sep-Oct;26(5):565-6; author reply 566-7.
[9]Fitts JM, Klein RM, Powers CA.  Comparison of tamoxifen and testosterone propionate in male rats: differential prevention of orchidectomy effects on sex organs, bone mass, growth, and the growth hormone-IGF-I axis.  J Androl. 2004 Jul-Aug;25(4):523-34.
[10]Miodrag A, Ekelund P, Burton R, Castleden CM. Tamoxifen and partial oestrogen agonism in postmenopausal women. Age Ageing. 1991 Jan;20(1):52-4. 
[11]Webb P, Lopez GN, Uht RM, Kushner PJ. Tamoxifen activation of the estrogen receptor/AP-1 pathway: potential origin for the cell-specific estrogen-like effects of antiestrogens. Mol Endocrinol. 1995 Apr;9(4):443-56. 

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