Drug intelligence / Profile preview

tamoxifen

Development stage
Approved
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

Tamoxifen is a selective estrogen receptor modulator (SERM) and non-steroidal antiestrogen used primarily to treat and prevent estrogen receptor-positive breast cancer in both women and men. It works by competitively inhibiting the binding of estrogen to its receptor, thereby blocking the growth-promoting effects of estrogen on breast tissue. Tamoxifen exhibits tissue-selective activity—acting as an antagonist in breast tissue but as an agonist in other tissues such as bone and uterus. It is also used to reduce the risk of invasive breast cancer following surgery or radiation for ductal carcinoma in situ (DCIS), and to lower the risk of developing breast cancer in high-risk populations. The drug was first synthesized by Dora Richardson in 1962, approved for medical use since 1977, and remains on the World Health Organization's List of Essential Medicines.

Brand names
NolvadexSoltamox
Other names
tamoxifentamoxifen hydrochloride
02

Targets

ESR1 (ERα)ESR2 (ERβ)

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