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Among all aromatase inhibitors, Letrozole is commonly used for improving female fertility. It works by inhibiting aromatase which is an enzyme that catalyses the conversion of androstenedione and testosterone to estrogen by hydroxylation. Hence, Letrozole inhibits the synthesis of estrogen. [18]
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 ]
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 ]
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.
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.
Letrozole is an aromatase inhibitor which reduces estradiol levels and increases levels of FSH and LH which can stimulate ovarian follicle maturation and ovulation. Letrozole is the preferred treatment in those with infertility due to PCOS and is associated with a higher pregnancy rate than other treatments. [ 2 ]