Colao A, Pivonello R, Auriemma R S, Galdiero M, Guerra E, Milone F, De Leo M, Lombardi G
Section of Endocrinology, Department of Molecular and Clinical Endocrinology and Oncology, Federico II University of Naples, Italy.
J Endocrinol Invest. 2005;28(11 Suppl International):58-66.
Currently available medical treatment of acromegaly includes dopamine agonists, slow release formulation of somatostatin analogues and pegvisomant, a GH-receptor antagonist. Dopamine agonists are well tolerated, not expensive but poorly effective. Somatostatin analogues are highly effective in 60-70% of patients based on the receptor profile of individual tumors. Pegvisomant is reported to normalize IGF-I levels in nearly the totality of the patients, but is devoted of tumor shrinking effect. In a preliminary study in patients with acromegaly, a new somatostatin analogue with affinity to four of the five somatostatin receptors (SOM230) was shown to be similarly effective as octreotide in some patients and more effective than octreotide in other patients. Moreover, new molecules with selective activity on the somatostatin receptor type 2, or 5, or 1 have been reported in vitro to strongly suppress GH secretion. Other new promising alternatives are the chimeric compounds with both somatostatin receptor and dopamine receptor binding. These drugs have been also shown to possess strong GH-inhibitory activity in primary cultures from GH-secreting adenomas. These drugs are the future perspectives in the treatment of patients with GH-secreting or GH/PRL-secreting tumors.
目前可用于治疗肢端肥大症的医学方法包括多巴胺激动剂、长效生长抑素类似物和培维索孟（一种生长激素受体拮抗剂）。多巴胺激动剂耐受性良好，价格不贵但效果不佳。基于个体肿瘤的受体特征，生长抑素类似物在60% - 70%的患者中具有高效性。据报道，培维索孟能使几乎所有患者的胰岛素样生长因子- I（IGF - I）水平恢复正常，但它没有肿瘤缩小作用。在一项针对肢端肥大症患者的初步研究中，一种对五种生长抑素受体中的四种具有亲和力的新型生长抑素类似物（SOM230），在一些患者中显示出与奥曲肽相似的疗效，而在其他患者中比奥曲肽更有效。此外，据体外研究报道，对生长抑素2型、5型或1型受体具有选择性活性的新分子能强烈抑制生长激素分泌。其他有前景的新选择是兼具生长抑素受体和多巴胺受体结合能力的嵌合化合物。这些药物在来自分泌生长激素腺瘤的原代培养物中也显示出具有强大的生长激素抑制活性。这些药物是治疗分泌生长激素或分泌生长激素/催乳素肿瘤患者的未来希望。
