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芳香化酶抑制剂在乳腺癌中的进化历程与未来发展方向

The Evolutionary Tale and Future Directions of Aromatase Inhibitors in Breast Carcinoma.

作者信息

Bhattacharjee Dipanjan, Kumari K Meena, Avin S, Babu V Amberkar Mohan

机构信息

Department of Pharmacology, Kasturba Medical College, Manipal Campus, Manipal University, Manipal, Karnataka, 576104, India.

出版信息

Anticancer Agents Med Chem. 2017 Nov 24;17(11):1487-1499. doi: 10.2174/1871520617666170327114831.

DOI:10.2174/1871520617666170327114831
PMID:28356008
Abstract

Aromatase inhibitors have often been likened to that of 'medical scalpels' for the treatment of breast carcinoma. By inhibiting the singular step of aromatisation, they have proven to be extremely effective allies in the treatment of breast cancer among postmenopausal women. However, their relevance soon may not be limited to the post-menopausal age group alone. Recent studies have hinted at their utility amongst the premenopausal women; combined with ovarian ablation techniques, aromatase inhibitors may prove to be equally effective and more, as compared to tamoxifen in this age-group. Additionally, explorations aimed at ascertaining their potential utility as an effective preventive strategy against breast carcinoma have yielded encouraging results. However, for aromatase inhibitors to be able to attain their full potential, further strategic fine-tuning aimed at maximising their efficacy and minimising their potentially far-reaching adverse effects, is the need of the hour. Despite the recent diversification, the issue of resistance to aromatase inhibitors in breast cancer threatens to derail the advances so gained till date. Fortunately, a few novel ploys have come to the fore, for instance combining aromatase inhibitors with HER-2 antibodies that could potentially help circumvent the menace of resistance in the near future. Till date, the utility of aromatase inhibitors can at best be described as onedimensional. However, with the unearthing of potential new avenues for its application, this assortment of molecules today stands on the precipice of ushering in a new revolution in the treatment of breast carcinoma.

摘要

芳香化酶抑制剂常被比作治疗乳腺癌的“手术刀”。通过抑制芳香化这一单一过程,它们已被证明是绝经后女性乳腺癌治疗中极为有效的辅助手段。然而,其应用范围可能很快不再局限于绝经后年龄组。最近的研究暗示了它们在绝经前女性中的效用;与卵巢去势技术相结合,芳香化酶抑制剂在这个年龄组中可能被证明与他莫昔芬同样有效甚至更有效。此外,旨在确定其作为预防乳腺癌有效策略的潜在效用的探索也取得了令人鼓舞的结果。然而,为了使芳香化酶抑制剂能够充分发挥其潜力,当下需要进一步进行战略微调,以最大限度地提高其疗效并尽量减少其潜在的深远副作用。尽管最近有了多样化发展,但乳腺癌对芳香化酶抑制剂产生耐药性的问题有可能使迄今取得的进展付诸东流。幸运的是,一些新策略已崭露头角,例如将芳香化酶抑制剂与HER-2抗体联合使用,这可能在不久的将来有助于规避耐药性的威胁。到目前为止,芳香化酶抑制剂的效用充其量只能说是单一的。然而,随着其潜在新应用途径的发现,这类分子如今正处于引发乳腺癌治疗新革命的边缘。

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