ChEBI: A 1,2,4-triazole compound having a 3,5-bis(2-cyano-2-propyl)benzyl group at the 1-position.
Indications and Usage
Anastrozole is a potent selective triazole aromatase inhibitor that inhibits the aromatase that cytochrome P-450 is dependent on to prevent the biosynthesis of estrogen. Estrogen is the main stimulating factor for breast cancer cell growth. This drug’s half maximal inhibitory concentration (IC50) value to human placental aromatase is 15nmol/L. Compared to the traditional drug tamoxifen, Anastrozole can comprehensively and effectively lower the risks of breast cancer recurrence and metastasis, thus extending patients’ disease-free survival.
Anastrozole is suitable for treating postmenopausal advanced breast cancer patients, especially postmenopausal advanced breast cancer patients who experienced recurrence following hormone assisted therapy.
A series of clinical trials compared the effects of third generation aromatase inhibitor Anastrozole with those of tamoxifen. The trial was a global multicenter trial and includes 381 centers in 21 countries. Since 1996, there have been 9366 patients who have participated, and the follow-up time is 100 months. 25.8% of patients in the Anastrozole group experienced recurrence, while 29.9% of patients in the tamoxifen group did. Thus, Anastrozole’s recurrence rate was 4.1% lower than that of tamoxifen, and its risk of distant metastasis was lower as well. Anastrozole is also safer than tamoxifen.
Potent and highly selective aromatase (CYP19) inhibitor (IC 50 = 15nM) that has no discernible effect on adrenocorticoid hormone synthesis. Reduces plasma estrogen levels and exhibits antitumor activity in vivo . Orally active.
An aromatase inhibitor. Used as an antineoplastic.