The current landscape of aromatase inhibitors for the treatment of estrogen receptor-positive breast carcinoma

Abstract

Estrogen receptor-positive (ER+) breast carcinoma represents a significant portion of breast cancer cases and is characterized by the presence of estrogen receptors that promote tumor growth upon estrogen binding. ER + breast cancer progression involves hormonal influences, interactions within the tumor microenvironment, and genetic mutations that may lead to treatment resistance. Successful therapeutic options include hormonal therapies, particularly aromatase inhibitors (AIs), which aim to block the effects of estrogen or reduce its synthesis. With higher efficacy than tamoxifen, AIs such as anastrozole, letrozole, and exemestane have become widely employed in adjuvant and first-line treatments for advanced breast cancer. AIs function by inhibiting the enzyme aromatase, which converts androgens into estrogens in the peripheral tissues. Because too much estrogen might promote tumor growth, this decrease in estrogen levels is essential for treating ER+ malignancies. To provide a comprehensive overview of AIs in the treatment of ER+ breast cancer, this study examined the pharmacokinetics, clinical uses, mechanisms of action, and problems with treatment resistance. To maximize therapeutic approaches and enhance patient outcomes in the treatment of ER breast cancer, it is imperative to understand these characteristics.