What is the mechanism of action of tamoxifen?

Tamoxifen (TAM) is known to have a dual mechanism of action: (1) to compete with 17β-estradiol (E2) at the receptor site and to block the promotional role of E2 in breast cancer; and (2) to bind DNA after metabolic activation and to initiate carcinogenesis.

What is tamoxifen wiki?

Tamoxifen, sold under the brand name Nolvadex among others, is a selective estrogen receptor modulator used to prevent breast cancer in women and treat breast cancer in women and men. It is also being studied for other types of cancer. It has been used for Albright syndrome.

Is tamoxifen an estrogen antagonist?

Tamoxifen is both an antagonist and an agonist of the estrogen receptor. However, a molecular explanation exists for this apparent paradox. The dual action is a function of the estrogen receptor complex present in a particular cell or tissue.

When was tamoxifen first used?

In 1978, following a series of successful clinical trials in humans, the U.S. Food and Drug Administration (FDA) approved tamoxifen for the treatment of metastatic estrogen receptor-positive breast cancer.

How is tamoxifen absorbed?

Tamoxifen is well absorbed after oral administration, and appears to be more than 99% bound to plasma proteins (mostly to albumin) (Lien et al., 1989).

What is the chemical formula for tamoxifen?

Tamoxifen | C26H29NO – PubChem.

What is the structure of tamoxifen?

Why is tamoxifen a SERM?

Selective estrogen receptor modulators (SERMs) are synthetic molecules which bind to estrogen receptors (ER) and can modulate its transcriptional capabilities in different ways in diverse estrogen target tissues. Tamoxifen, the prototypical SERM, is extensively used for targeted therapy of ER positive breast cancers.

Is tamoxifen an immunosuppressant?

Whilst its role in breast cancer treatment may be diminishing, a growing body of evidence has defined a novel role for tamoxifen as an immune modulator.

Does tamoxifen bind to estrogen receptor?

Tamoxifen binds to the estrogen receptor but does not activate it fully, halting estrogen-induced growth. Of course, estrogen has many effects throughout the body. It is dangerous to block its action indiscriminately.

How is tamoxifen excreted?

Tamoxifen is extensively metabolized after oral administration. Studies in women receiving 20 mg of 14C tamoxifen have shown that approximately 65% of the administered dose is excreted from the body over a period of 2 weeks with fecal excretion the primary route of elimination.

What functional groups are in tamoxifen?

Analogs were generated by modification of the hydrophilic functional group of Tamoxifen by hydroxyl, amide, carboxyl, and sulfhydryl functional groups, in an attempt to improve their activity and selectivity.