Whereas the first aromatase inhibitors to be used therapeutically could be shown to produce drug-induced inhibition of the enzyme and therapeutic benefits in patients with breast cancer, they were not particularly potent and lacked specificity. However, second-generation drugs were developed and most recently third-generation inhibitors have evolved which possess remarkable specificity and potency. Initial results from clinical trials suggest that these agents will become the cornerstones of future endocrine therapy.
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