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Drug Evaluation

Exemestane: a potent irreversible aromatase inactivator and a promising advance in breast cancer treatment

Pages 267-275 | Published online: 10 Jan 2014

References

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  • ••This combined analysis of two trials of postmenopausal patients with advanced breast carcinoma has clearly demonstrated that, after disease progression with tamoxifen, treatment with anastrozole 1 mg once daily results in a statistically and clinically significant advantage over a standard treatment, megestrol acetate.
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  • ••Demonstrates the clinical superiority ofthe third-generation aromatase inhibitor letrozole over megestrol acetate, with a superior safety profile.
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  • ••Compares exemestane with megestrolacetate; time to disease progression, time to treatment failure and overall survival were all significantly better for exemestane than megestrol acetate.
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  • ••Supports the use of letrozole as first-lineendocrine therapy in postmenopausal women with advanced breast cancer.
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  • ••Landmark results from the single largestadjuvant trial ever conducted in postmenopausal patients with early breast cancer.
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  • •Highlights that the ability to block estrogen biosynthesis peripherally and locally within the breast provides new options for the treatment of hormone-sensitive breast cancers in postmenopausal women.
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  • ••The first study to reveal near totalaromatase inhibition in vivo with the use of a steroidal aromatase inhibitor and to identify exemestane as a promising new drug for the treatment of hormone-sensitive breast cancer.
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  • •This study compared the effects of the two novel, potent, nonsteroidal aromatase inhibitors anastrozole and letrozole on total-body aromatization and plasma estrogen levels. Letrozole was found to be a more potent suppressor of total-body aromatization and plasma estrogen levels compared with anastrozole in postmenopausal women with metastatic breast cancer.
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  • ••Excellent editorial providing a succinct summary on the role of these potent inhibitors of estrogen synthesis.
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