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Tamoxifen citrate

Tamoxifen citrate structure

CAS No:
54965-24-1
Formula:
C26H29NO.C6H8O7
Chemical Name:
Tamoxifen citrate
Synonyms:
Ethanamine,2-[4-[(1Z)-1,2-diphenyl-1-buten-1-yl]phenoxy]-N,N-dimethyl-,2-hydroxy-1,2,3-propanetricarboxylate (1:1);Ethanamine,2-[4-(1,2-diphenyl-1-butenyl)phenoxy]-N,N-dimethyl-,(Z)-,2-hydroxy-1,2,3-propanetricarboxylate (1:1);Ethanamine,2-[4-[(1Z)-1,2-diphenyl-1-butenyl]phenoxy]-N,N-dimethyl-,2-hydroxy-1,2,3-propanetricarboxylate (1:1);Tamoxifen citrate;Nolvadex;ICI 46474;Tamoplex;Z-Tamoxifen citrate;Tamox-Puren;Zemide;Kessar;Tamofen;TMX;Tomaxasta;Noltam;Nourytam;I.C.I.46474 citrate;Istubal;Valodex;Soltamox;Genox;7244-97-5
Categories:
Active Pharmaceutical Ingredients > Antineoplastic Agents

Description

Tamoxifen, sold under the brand name Nolvadex among others, is a medication that is used to prevent breast cancer in women and treat breast cancer in women and men. The introduction of the anti-oestrogen tamoxifen in the early 1970s represented a landmark in the treatment of breast cancer. Over 40 years later, tamoxifen has been shown to be effective not only for early and advanced breast cancer, but also for ductal carcinoma in situ (DCIS) and the chemoprevention of breast cancer in high-risk

Tamoxifen Citrate is the citrate salt of an antineoplastic nonsteroidal selective estrogen receptor modulator (SERM). Tamoxifen competitively inhibits the binding of estradiol to estrogen receptors, thereby preventing the receptor from binding to the estrogen-response element on DNA. The result is a reduction in DNA synthesis and cellular response to estrogen. In addition, tamoxifen up-regulates the production of transforming growth factor B (TGFb), a factor that inhibits tumor cell growth, and down-regulates insulin-like growth factor 1 (IGF-1), a factor that stimulates breast cancer cell growth. Tamoxifen also down-regulates protein kinase C (PKC) expression in a dose-dependant manner, inhibiting signal transduction and producing an antiproliferative effect in tumors such as malignant glioma and other cancers that overexpress PKC.|One of the SELECTIVE ESTROGEN RECEPTOR MODULATORS with tissue-specific activities. Tamoxifen acts as an anti-estrogen (inhibiting agent) in the mammary tissue, but as an estrogen (stimulating agent) in cholesterol metabolism, bone density, and cell proliferation in the ENDOMETRIUM.

Tamoxifen citrate Basic Attributes

Molecular Weight：

563.64

Exact Mass：

563.252

EC Number：

259-415-2

UNII：

7FRV7310N6

NSC Number：

757345|180973

DSSTox ID：

DTXSID8021301

NCI Thesaurus Code：

C855

HScode：

29225090

Characteristics

PSA：

145

XLogP3：

4.74760

Appearance：

White to off-white Powder

Melting Point：

140-142 °C

Boiling Point：

665.9ºC at 760 mmHg

Flash Point：

356.5ºC

Water Solubility：

H2O: slightly soluble ;methanol: soluble 50mg/mL, clear, colorless

Storage Conditions：

2-8°C

Toxicity：

LD50 in mice, rats (mg/kg): 200, 600 i.p.; 62.5, 62.5 i.v.; 3000-6000, 1200-2500 orally (Furr, Jordan)

Collision Cross Section：

197.2 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Hazard category：

IRRITANT

Transport codes：

UN 3077 9 / PGIII

wgk germany：

hazard class code：

45-60-61-22-64-36/37/38

safety instructions：

53-36/37/39-45-36-26

RTECS Number：

KH2387000

Marks：

T,Xi

Stability/Shelf Life：

Stable under normal temperatures and pressures.

Precautionary statement(s)：

P201, P202, P260, P263, P264, P270, P273, P281, P301+P312, P308+P313, P330, P391, P405, P501

Hazard Statements：

H302

GHS Classification：

|Danger|H302 (97.44%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P260, P263, P264, P270, P273, P281, P301+P312, P308+P313, P314, P330, P391, P405, and P501|Aggregated GHS information provided by 78 companies from 14 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

Drug: Tamoxifencitrate

MeSH：

Antineoplastic agents that are used to treat hormone-sensitive tumors. Hormone-sensitive tumors may be hormone-dependent, hormone-responsive, or both. A hormone-dependent tumor regresses on removal of the hormonal stimulus, by surgery or pharmacological block. Hormone-responsive tumors may regress when pharmacologic amounts of hormones are administered regardless of whether previous signs of hormone sensitivity were observed. The major hormone-responsive cancers include carcinomas of the breast, prostate, and endometrium; lymphomas; and certain leukemias. (From AMA Drug Evaluations Annual 1994, p2079) (See all compounds classified as Antineoplastic Agents, Hormonal.)|Agents that inhibit BONE RESORPTION and/or favor BONE MINERALIZATION and BONE REGENERATION. They are used to heal BONE FRACTURES and to treat METABOLIC BONE DISEASES such as OSTEOPOROSIS. (See all compounds classified as Bone Density Conservation Agents.)|Compounds which inhibit or antagonize the action or biosynthesis of estrogenic compounds. (See all compounds classified as Estrogen Antagonists.)|A structurally diverse group of compounds distinguished from ESTROGENS by their ability to bind and activate ESTROGEN RECEPTORS but act as either an agonist or antagonist depending on the tissue type and hormonal milieu. They are classified as either first generation because they demonstrate estrogen agonist properties in the ENDOMETRIUM or second generation based on their patterns of tissue specificity. (Horm Res 1997;48:155-63) (See all compounds classified as Selective Estrogen Receptor Modulators.)

MeSH Entry Terms：

Citrate, Tamoxifen

Tamoxifen citrate Use and Manufacturing

Uses

An antiestrogen with potent anti-cancer and PKC inhibitory activities

Use Classification：

Human drugs -> Rare disease (orphan)|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Drug Function and Efficacy

Tamoxifen is a non-steroidal anti-estrogen drug. Its Z isomer competes with estrogen receptors for binding, preventing the effect of estrogen and thus inhibiting the proliferation of breast cancer cells.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Tamoxifen Citrate Tablets
Ingredients	The main ingredient of this product is tamoxifen citrate. Its chemical name is (Z)-N,N-dimethyl-2-[4-(1,2-diphenyl-1-butenyl)phenoxy]-ethylamine citrate. Molecular formula: C26H29NOC6H8O7. Molecular weight: 563.65
Indication	Estrogen can affect the therapeutic effect of this product; antacids, cimetidine, ranitidine, etc. change the pH value in the stomach, causing the enteric coating of this product to decompose prematurely, which has a stimulating effect on the stomach.
Specifications	10 mg (as tamoxifen)
Manufacturer	Liaoning Yuhuang Pharmaceutical Co., Ltd.

Tamoxifen citrate
Manufacturer	Bei Jing Scrianen Pharmaceutical Co., Ltd.

Tamoxifen Citrate Tablets
Ingredients	Tamoxifen citrate.
Indication	Estrogen may affect the therapeutic effect of this product.
Specifications	10 mg (as tamoxifen)

See More Related Drugs

Registered Holders

APITORIA PHARMA PRIVATE LTD

United States
Active
EXCELLA GMBH AND CO KG

United States
Active
Excella GmbH & Co. KG

Germany
Active

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