Melen-Mucha Gabriela, Lawnicka Hanna, Kierszniewska-Stepien Dorota, Komorowski Jan, Stepien Henryk
Department of Immunoendocrinology, Medical University of Lodz, 91-425 Lodz, Dr Sterling 3 Street, Lodz, Poland.
Recent Pat Anticancer Drug Discov. 2006 Jun;1(2):237-54. doi: 10.2174/157489206777442197.
Somatostatin (SS) was originally discovered as a hypothalamic neurohormone which inhibits growth hormone secretion. The synthesis of the first two metabolically stabilized and more potent SS analogs, octreotide and lanreotide leads to the establishment of applications for them and to introduction into routine therapies. The effectiveness of octreotide or lanreotide in controlling symptoms and GH/IGF-I hypersecretion in acromegalic patients, both preoperatively and postoperatively is well proven. Similarly, these drugs are also very effective in the treatment of TSH-secreting adenomas. The introduction of these drugs into therapy of the functional neuroendocrine tumors of the gastrointestinal tract was a crucial step in the treatment. Octreotide and lanreotide are the drugs of choice in the treatment of patients with: VIPoma, glucagonoma and carcinoid syndrome. Somatostatin receptor scintigraphy with OctreoScan has been recommended as the best imaging technique in these tumors in the localization and staging procedure. SS analogs, coupled to radioisotope or cytotoxic drugs, create another class of SS molecules, very promising in the therapy of the endocrine glands tumors and in other tumors. Another class of SS analogs comprises hybrid molecules, which are chimera of sst2 agonist and D2 agonist, possessing more potent activity than these agonists, applied together.
生长抑素(SS)最初是作为一种抑制生长激素分泌的下丘脑神经激素被发现的。首批两种代谢稳定且活性更强的SS类似物奥曲肽和兰瑞肽的合成,促使它们得以应用并被引入常规治疗。奥曲肽或兰瑞肽在控制肢端肥大症患者术前和术后症状以及生长激素/胰岛素样生长因子-I分泌过多方面的有效性已得到充分证实。同样,这些药物在治疗促甲状腺激素分泌型腺瘤方面也非常有效。将这些药物引入胃肠道功能性神经内分泌肿瘤的治疗是治疗过程中的关键一步。奥曲肽和兰瑞肽是治疗患有以下疾病患者的首选药物:血管活性肠肽瘤、胰高血糖素瘤和类癌综合征。用奥曲肽扫描进行生长抑素受体闪烁显像已被推荐为这些肿瘤定位和分期过程中的最佳成像技术。与放射性同位素或细胞毒性药物偶联的SS类似物,构成了另一类SS分子,在治疗内分泌腺肿瘤和其他肿瘤方面非常有前景。另一类SS类似物包括杂合分子,它们是生长抑素受体2激动剂和多巴胺D2激动剂的嵌合体,比单独应用这些激动剂具有更强的活性。