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Letrozole, sold under the brand name Femara among others, is an aromatase inhibitor medication that is used in the treatment of breast cancer for post-menopausal women. [ 1 ] It was patented in 1986 and approved for medical use in 1996. [ 4 ]
In the Nordic countries, letrozole is practically the standard initial regimen used for ovulation induction, since no formulation of clomifene is registered for use there. [ 19 ] [ 20 ] India banned the usage of letrozole in 2011, citing potential risks to infants. [ 21 ]
Steroidal aromatase inhibitors are a class of drugs that are mostly used for treating breast cancer in postmenopausal women. High levels of estrogen in breast tissue increases the risk of developing breast cancer and the enzyme aromatase is considered to be a good therapeutic target when treating breast cancer due to it being involved in the final step of estrogen biosynthetic pathway and also ...
Ovarian stimulation with the aromatase inhibitor letrozole has been proposed for ovulation induction in order to treat unexplained female infertility. In a multi-center study funded by the National Institute of Child Health and Development, ovarian stimulation with letrozole resulted in a significantly lower frequency of multiple gestation (i.e., twins or triplets) but also a lower frequency ...
Letrozole has a 1,2,4 triazole ring which is important for binding with Fe 2+ in the heme moiety of the aromatase enzyme. Also, the cyano benzyl moiety is significant because it partly imitates the steroid backbone of the natural hormone androstenedione.
Ovulation induction is usually initially performed by giving an antiestrogen such as clomifene citrate or letrozole in order to decrease negative feedback on the pituitary gland, resulting in an increase in FSH with the aim of increasing folliculogenesis. It is the main initial medical treatment for anovulation.
Aromatase inhibitors are a common fertility treatment to treat women with PCOS. A meta-analysis analyzing live birth rates for women with PCOS treated with clomiphene compared to letrozole found that letrozole resulted in higher live birth rates. [11] However, ovulation induction remains an off-label indication, which affects use.
Antiestrogens, also known as estrogen antagonists or estrogen blockers, are a class of drugs which prevent estrogens like estradiol from mediating their biological effects in the body.