Quick detail

Prodcut Name: Tamoxifen Citrate

Other name: Nolvadex

Model NO.: CZG-ST50

Customized: Customized

Suitable for: Adult

Purity: >99%

CAS: 54965-24-1

Melting Point: 140-144 Degree Centigrade

MOQ: 10gram

Mf: C26h29no

Brand Name: Pharmlab

Transport Package: Alumiuim Foil or as Customer′s Requirement

Origin: China

Powder: Yes

Certification: GMP, ISO 9001, USP, BP

State: Solid

Grade: USP

Pack: Drum, Plastic Container

MW: 371.51

Export Markets: Global

Trademark: Pharmlab

Specification: USP

Grade: Pharmaceutical grade

What is Tamoxifen Citrate?

Tamoxifen Citrate (Nolvadex) Is an estrogen competitive antagonist and a nonsteroidal antiestrogen drug. It can compete with estrogen (estradiol) to bind to estrogen receptors in breast cancer cells, inhibit the effect of estrogen on cancer cells, inhibit tumor cell growth and development, and show anticancer effects. In clinical practice, tamoxifen citrate is commonly used to treat various types of breast cancer, particularly in women with postmenopausal breast cancer with estrogen receptor and progesterone receptor positive and with low prostate specific antigen levels.

Mechanism of action

TCT has a cis-trans isomer, its cis-isomer has a weak estrogenic effect, whereas the trans isomer has an antiestrogen effect. When the early application of tamoxifen or the presence of low concentrations, it binds to the estrogen receptor (ER) in the cytoplasm, exhibiting a weaker estrogenic effect. TCT into the nucleus, can inhibit the nuclear ER transcription and synthesis, resulting in lasting anti-estrogen effect.

It has been found that many of the new features of TCT are associated with mechanisms of action beyond their competitive estrogen receptor-membrane regulatory mechanisms. TCT as a membrane modifier, can reduce cell cycle. On this basis, TCT can also act as an antioxidant to protect the cell membrane and human LDL from oxidative damage.

Pharmacodynamics of Tamoxifen Citrate

TCT oral absorption is slow, plasma concentration in 3 ~ 6 hours to reach the peak. After absorption of the liver, tamoxifen citrate metabolism to N-desmethyl tamoxifen, its activity and tamoxifen citrate similar. The half-life of tamoxifen citrate is 5 to 7 days and its metabolite N-desmethyl tamoxifen is 7 to 14 days.

Animal experiments show that tamoxifen citric acid and N-desmethyl tamoxifen are circulating in a wide range of enteric liver. For a single oral dose of 20 mg TCT, the plasma concentration peak was about 40 ng / ml (range 67-183 ng / ml) and 336 ng ml (range: 148 to 654 ng / ml). The steady-state plasma concentration of tamoxifen citrate, which requires three to four weeks of continuous administration, generally requires the continuous administration of N-methyltamethoxamine for 3 to 8 weeks. Tamoxifen citrate and most other metabolites are mainly excreted in the feces, and a small fraction of the metabolites excreted in the urine.

Clinical application of Tamoxifen Citrate

1. Breast cancer treatment

2. Prevention of breast cancer.

Anti-tumor and anti-multidrug resistance.

Methomorphine citrate reduces the concentration and activity of cancer transfer promoters and various activating enzymes, thereby inhibiting or hindering the growth and metastasis of cancer cells, by reducing membrane permeability and enhancing the rigidity of the intercellular binding sites.

In addition, it promotes the secretion of negative growth factor-TGF-G, which inhibits the proliferation of cancer cells by inhibiting the proliferation of cancer cells, and inhibits the oxidative damage of DNA bases caused by hydrogen production from human neutrophils. In addition to breast cancer, there are other malignant tumor treatment and prevention, for the treatment of brain tumors, liver cancer, prostate cancer. In addition, tamoxifen citrate can reduce the membrane release of membrane P170 glycoprotein membrane, improve the intracellular effective concentration of cytotoxic drugs and reduce drug resistance.Heart protection

The use Tamoxifen Citrate

For the treatment of advanced and recurrent breast cancer and ovarian cancer. Anti-estrogen with potent anti-cancer and PKC inhibitory activity

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