6.1.1 A Brief History of Endocrine Therapy for Bre...
In 1896，Dr Beatson，in the United Kingdom，first reported in the Lancet journal that a case of advanced breast cancer had a life span of up to four years after the removal of the double-sided ovary，opening the way for ovarian degeneration to treat breast cancer.In 1967，Jensen discovered the presence of ER in breast cancer cells，which led to the rapid development of breast cancer endocrine therapy drugs，but also opened up the true sense of breast cancer drug endocrine therapy.In the 1960s，the academic community developed the contraceptive drug Tamoxifen（Tamoxifen，TAM）.In 1971，he was first used in clinical anti-tumor therapy，and in 1978 was approved by the U.S.FDA for the study of assisted endocrine therapy for early breast cancer.The first generation of aromatase inhibitors representing the drug amlumite was first used in the clinic as an anticonvulsant in 1955.In the 1960s，experimental lymforth was used for hormone-sensitive advanced breast cancer.(https://www.daowen.com)
In 1973，research data reported that the use of AI to treat metastatic breast can cer has achieved some results，but inhibited aromatase at the same time，affecting the metabolism of adrenal corticosteroids in the body.It was approved for use in breast cancer in 1981.The first and second generation aromatase inhibitors are gradually rejected clinically due to the large side effects and unclear efficacy.In the 1990s，internationally renowned pharmaceutical companies introduced the third generation of aromatic enzyme inhibitors，including：nonsteroidal reversible aromaticase inhibitors，representing the drug Anastrozole（Anaquzole），which was launched in the UK in 1995；Available in the UK in 1996，the steroid aromatase inactivator，which represented by the drug Exemestane（Esimetan），entered clinical practice in 1997.Fluorovis group is a new class of steroid-like estrogen receptor antagonists found in recent years，without the agonist effect.By binding to estrogen receptors，the receptor's main functional group inactivates，while causing estrogen receptor degradation and signaling pathway blocking，causing a sharp reduction in the expression of estrogen，progesterone receptors at the cellular level，and preventing or delaying resistance to endocrine therapy.In 2011，fluorovis group（250mg）was approved for listing in China for pre-esotalgenic advanced or metastatic breast cancer，which recurs after or during anti-estrogen-assisted treatment，or is advanced in anti-estrogen therapy.