Santen R J, Manni A, Harvey H
Breast Cancer Res Treat. 1986;7(3):129-45. doi: 10.1007/BF01806244.
'Superagonist' analogs of GnRH produce a paradoxical inhibition of gonadotropin secretion when given on a long-term basis, and may well produce a more complete 'medical oophorectomy' than antiestrogens in premenopausal breast cancer patients. Here we review the background and pharmacology of these agents, together with the experience of their use with prostate cancer and early trials in breast cancer. Their effectiveness without significant toxicity, together with new biodegradable implants for their easily acceptable long-term administration, suggest that a highly selective medical means of fully inhibiting ovarian estrogen production is now available for more extensive trials in breast cancer patients.
促性腺激素释放激素(GnRH)的“超级激动剂”类似物长期给药时会对促性腺激素分泌产生矛盾性抑制,对于绝经前乳腺癌患者,其产生的“药物性卵巢切除”效果可能比抗雌激素药物更彻底。本文综述了这些药物的背景和药理学,以及它们在前列腺癌治疗中的应用经验和在乳腺癌早期试验中的情况。它们疗效显著且毒性不大,加上新型可生物降解植入物便于长期给药,这表明一种能高度选择性地完全抑制卵巢雌激素生成的医学方法现已可供在乳腺癌患者中开展更广泛的试验。