The highly active estrogen metabolism and receptor protein expression are to blame for the elevated breast cancer (BC) rate in post-menopausal women. Letrozole is a powerful endocrine medication that targets and inhibits the aromatase, often known as an aromatase inhibitor (AI). It aids in the adjuvant, neoadjuvant, and metastatic treatment of HR+ breast cancer because it can boost FSH production for ovulation induction. It has recently been used in infertile pre-menopausal women. The main advantages of utilizing letrozole to enhance follicle development may be wasted in current infertility treatments. We went into great length in this review about the pharmacokinetics, pharmacodynamics, and distinct adverse effects of the drug on the heart, kidney, liver, embryo, bone, and ovary. It also causes apoptosis, necrosis, and fibrosis, which all result in the demise of cancer cells. Its central and peripheral effects on follicle formation, estrogen production in the ovaries, and their clinical implications are explored in detail in this work.
Keywords: Aromatase inhibitors; Clinical data; Letrozole; Menopausal; Toxicity; Treatment.
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