Endocrine therapy of breast cancer, endocrine therapy for breast cancer has more than 100 years of history. 1886 Beaon first reported oophorectomy can reduce breast cancer; 20th century, 40 years, Higgins applied testosterone or estrogen removal of the success of the treatment of prostate cancer, endocrine therapy for cancer foundation. The occurrence and development of breast cancer by endocrine regulation, currently in the anti-estrogen, aromatase inhibitors, and pituitary RH-LH analogue treatment on three levels.
About the efficacy of endocrine therapy is the most important factor receptor status and age of the patient involvement organs. In general, the soft tissue response to invasion by those who should be better than the liver.
1. Anti-Estrogens
D tamoxifen (tamoxifen, TAM) is the most common non-simplified anti-estrogen drugs, the main mechanism is competitive and estrogen receptors in cancer cells of estrogen CER. There are two control ER protein function CTAF, TAM can inhibit the function of activated TAF2 TAF1, is the ER protein partial agonist. TAM to DES and blood in the competitive ER protein in vitro to anti-ER-positive breast cancer cells, and other physiological functions.
Indications TAM ER-positive patients are mainly pre-menopausal patients efficiency of 30% – 40%, 35% of postmenopausal patients – 60%, respectively. TAM treatment of patients with advanced breast cancer treatment and surgical menopause are similar. TAM as early as mid-term ER-positive postmenopausal breast cancer patients adjuvant application, can improve the cure rate of 15%. General usage for each TAM 10mg, 2 times a day or every p 20mg, day 1. TAM resistance was mainly due to variation of ER, TAM metabolism, TAM reduce the level of cells and so on.
(2) toremifen chemical structure, therapeutic and TAM close to the same dosage and usage and TAM, TAM, but weaker than estrogen, similar to the clinical efficacy and TAM.
(3) Qu network Raloxifene (droloxifene, DRL) affinity, rapid onset, short half-life. Whether clinical or pre-menopausal and postmenopausal patients are similar to TAM.
Endocrine therapy of breast cancer, 2. Aromatase inhibitors
(1) aminoglutethimide (aminoglutethi Aguilar de, AG) were the most commonly used aromatase inhibitors. General daily dose 250-50Omg, two weeks gradually increase the amount to the daily 500-1000mg, while taking daily prednisolone 40mg. AG adverse reactions are drowsiness, the dose to 19 when there is a serious skin mill. As AG adverse reactions are more common as the TAM second-line drugs after treatment failure, but the AG has good effect when the bone can be used as first choice. And progesterone combined, effects can be more than TAM.
(2) Formestane Simplified hormone synthesis 4 – two from the base Androstene pay, under physiological conditions in the competitive inhibition of aromatase to estrogen reduced the organization to play a therapeutic role. Slowly absorbed after intramuscular injection, the maximum plasma concentration on day 4, half-life of between 5-10 days, effective in 23% -33%, main side effects were facial flushing, skin itching, burning sensation, a few may have to digest channel response, edema. This product is mainly used for postmenopausal patients. General deep intramuscular injection every 2 weeks 1 times, each time 250mg. Premenopausal patients disabled.
(3) to curved buildings (letrozole, trade name: femara) synthetic aromatase inhibitors can effectively inhibit tumor aromatase. Pregnant trouble and more effective than AG, the TAM resistant advanced patients also have a certain effect, remission duration and better tolerated than AG, is currently a drug widely valued. General daily 2mg, comparable long-term use. Similar adverse reactions and AG, but relatively light.
(4) ansatrozole (arimidex) as non-simplified class of AG derivatives, the role of a long time. Tablets, usually taken 1 per day, each 1mg.
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