创新链/学科链/研发链/产业链

新药研发前沿动态 / 医药领域趋势进展

芳香化酶抑制剂与选择性雌激素受体调节剂的眼部不良反应及其机制的研究进展

Advances in Research on Ocular Adverse Effects and Mechanisms of Aromatase Inhibitors and Selective Estrogen Receptor Modulators

  • 摘要: 芳香化酶抑制剂和选择性雌激素受体调节剂是治疗雌激素受体阳性乳腺癌的关键药物。芳香化酶抑制剂通过抑制雌激素的生成,而选择性雌激素受体调节剂则通过拮抗雌激素受体,降低细胞周期蛋白D1基因、细胞周期蛋白依赖性激酶4/6基因等原癌基因的表达,从而抑制乳腺癌细胞的增殖。雌激素受体主要分布于乳腺、子宫、骨骼和眼部等组织。在眼部,雌激素受体存在于泪腺、晶状体和视网膜等部位。雌激素在维持泪液分泌、保持晶状体透明度以及视网膜稳定中发挥重要作用。因此,这两类药物会影响眼部生理功能,导致患者出现干眼症、白内障和视网膜病变等眼部不良反应。综述了芳香化酶抑制剂和选择性雌激素受体调节剂引发的眼部不良反应及发生机制,旨在为这两类药物治疗方案的改进和新型抗乳腺癌药物的开发提供参考。

     

    Abstract: Aromatase inhibitors (AIs) and selective estrogen receptor modulators (SERMs) are key medications for treating estrogen receptor (ER)-positive breast cancer. AIs suppress estrogen production, while SERMs antagonize estrogen receptors, thereby downregulating the expression of proto-oncogenes such as Cyclin D1 and Cyclin-dependent kinase 4/6 (CDK4/6), ultimately inhibiting the proliferation of breast cancer cells. ERs are primarily distributed in tissues including the breast, uterus, bones, and eyes. In the eyes, ERs are present in ocular tissues such as the lacrimal glands, lens, and retina. Estrogen plays crucial roles in maintaining tear secretion, preserving lens transparency, and stabilizing the retina. Consequently, AIs and SERMs can cause ocular adverse effects, including dry eye syndrome, cataracts, and retinopathy. This review summarizes the ocular adverse effects induced by AIs and SERMs and explores their underlying mechanisms, aiming to provide references for optimizing therapeutic regimens of these drugs and developing novel anti-breast cancer drugs.

     

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