Relevance of Aromatase Inhibitors in Breast Cancer Treatment

Abstract

: Efficacious treatment for breast cancer is still a challenge despite the presence of various treatment options. Aromatase enzyme present in the breast tissue is responsible for estrogen formation from androgens. Aromatase inhibitors manifest remarkably ameliorated therapeutic efficacy as compared to the current therapeutic options available and exhibit a better safety profile as compared to the other drugs. Clinical resistance to aromatase inhibitors is perceived as a lack of growth inhibition by aromatase inhibitors treatment and cancer therapy becomes ineffective in causing a decrease in the size of the tumor. Naturally extracted aromatase inhibitors have a huge positive impact on vitality and living standards. This review article highlights the particulars about the currently approved steroidal and non-steroidal aromatase inhibitors for clinical use, adverse effects associated with their use and approach to tackling the problem, various strategies to overcome aromatase inhibitors resistance, information on the synthesis of various peculiar aromatase inhibitors which can prove as highly efficient and potent drugs in the near future and the drugs of natural and semi-synthetic origin which can demonstrate to be more efficient, potent and less-toxic than conventional therapy.

Identification of somatic mutation-driven enhancers and their clinical utility in breast cancer

“… 42 Aminoglutethimide was the first inhibitor evaluated in clinical studies for treatment of hormone-dependent breast cancer. 43 These small molecular drugs could be potential candidates for enhancer-based cancer therapy.…”

One of the 5-aminosalicylates drug, mesalamine as a drug repurposing lead against breast cancer

“…The overexpression of EGFR results in the large size of the tumor, poor differentiation as well as clinical outcomes; Aromatase is responsible for regulating hyperplasia when circulating estrogen is not present; ALOX5 is known to play a critical role in inflammation tied to cancer such as breast and colorectal. mTOR gives a great advantage to the growth of tumors, activates protein synthesis, and suppresses autophagy (Harris et al 2020;Sood et al 2021;Hare and Harvey 2017;Sigismund et al 2018). mTOR plays a central role on PI3K/Akt/mTOR pathway which is one of the critical pathway affecting cell survival and metabolism in normal and pathophysiological situations, especially in cancer (Mossmann et al 2018).…”

A comprehensive overview of the relationship between RET gene and tumor occurrence

“…Multiple kinase inhibitors easily generate toxicity because of the off-target effects. Most of them were not authorized by the FDA ( 76 – 80 ). Immune checkpoint inhibitors as the post-line treatment option were sensible for driver gene mutation patients ( 38 , 63 , 81 , 82 ).…”