Krassas G E
Department of Endocrinology and Metabolism, Panagia General Hospital, Thessaloniki, Greece.
J Endocrinol Invest. 2004 Mar;27(3):281-7. doi: 10.1007/BF03345278.
Somatostatin (SM), a peptide inhibiting the release of GH, is present and plays an inhibitory role in the regulation of several organ systems in men and other species. Various SM analogs (SM-As) have been developed and used in clinical practice because the short half-life of SM makes it unsuitable for routine treatment. Recently it has been shown that SM-As might be of therapeutic value in the treatment of active thyroid ophthalmopathy. So far, 61 patients have been treated with octreotide and the results have been published in the literature. It was found that in 41 patients the drug had a beneficial effect. Ten patients were given lanreotide and 8 of those had a positive response, while 23 patients were treated with long-acting release octreotide and 16 improved. The exact mechanism of action of SM-As has not yet been fully clarified. One possible mechanism could be a direct inhibition of insulin-like growth factor (IGF)-I mediated effects. A second mechanism could be an inhibition of the release of lymphokines and inflammatory mediators from T-lympocytes. Finally, SM-As may act directly on target cells through specific cell surface receptors. With the introduction from Novartis of SOM-230, a compound which binds with high affinity to SM-receptors (SM-Rs) subtypes 1, 2, 3 and 5, with lower affinity to SM-Rs 4, and which has a very favorable T1/2 of nearly 24 h, a much better therapeutic outcome is expected. Thus, SM-As may provide a well-tolerated therapeutic alternative to corticosteroids. However, prospective placebo-controlled studies with large numbers of patients are needed before their role in the treatment of Graves' opthalmopathy is definitely established.
生长抑素(SM)是一种抑制生长激素释放的肽,在人类和其他物种的多个器官系统调节中存在并发挥抑制作用。由于SM的半衰期短,不适合常规治疗,因此已开发出各种SM类似物(SM-As)并用于临床实践。最近有研究表明,SM-As在治疗活动性甲状腺眼病方面可能具有治疗价值。到目前为止,已有61例患者接受了奥曲肽治疗,结果已发表在文献中。发现41例患者使用该药物有有益效果。10例患者使用了兰瑞肽,其中8例有阳性反应,23例患者使用了长效释放奥曲肽,16例病情改善。SM-As的确切作用机制尚未完全阐明。一种可能的机制可能是直接抑制胰岛素样生长因子(IGF)-I介导的作用。第二种机制可能是抑制T淋巴细胞释放淋巴因子和炎症介质。最后,SM-As可能通过特定的细胞表面受体直接作用于靶细胞。随着诺华公司推出SOM-230,一种与SM受体(SM-Rs)亚型1、2、3和5具有高亲和力结合、与SM-Rs 4亲和力较低且T1/2近24小时非常有利的化合物,预计会有更好的治疗效果。因此,SM-As可能为皮质类固醇提供一种耐受性良好的治疗替代方案。然而,在其在格雷夫斯眼病治疗中的作用得到明确确立之前,需要进行大量患者的前瞻性安慰剂对照研究。