Ben-Shlomo Anat, Melmed Shlomo
Cedars-Sinai Medical Center, Los Angeles, CA 90048, USA.
Mol Cell Endocrinol. 2008 May 14;286(1-2):192-8. doi: 10.1016/j.mce.2007.11.024. Epub 2007 Nov 29.
The discovery of somatotropin-release inhibitory factor (SRIF) in hypothalamic extract in 1970 led to the synthesis of the first somatostatin analog octreotide, discovery of five somatostatin receptor subtypes, and development of additional somatostatin receptor ligands (SRL) as pharmacotherapy for acromegaly and other neuroendocrine tumors. Long-acting formulations of SRL (octreotide LAR Depot, lanreotide SR and lanreotide autogel) assure improved patient compliance with weekly up to monthly injections, and are commonly used as primary or adjuvant treatment of acromegaly. We review SRL currently available, emphasizing long-acting compounds and their efficacy in controlling acromegaly. Disease control is evaluated by biochemical markers, tumor shrinkage, and disease-symptom improvement balanced against drug-related side effects.
1970年在下丘脑提取物中发现生长激素释放抑制因子(SRIF),促使首个生长抑素类似物奥曲肽的合成、五种生长抑素受体亚型的发现以及其他生长抑素受体配体(SRL)作为肢端肥大症和其他神经内分泌肿瘤药物治疗的开发。SRL的长效制剂(奥曲肽长效释放微球、兰瑞肽SR和兰瑞肽凝胶)确保患者更好地依从性,从每周注射一次到每月注射一次,常用于肢端肥大症的一线或辅助治疗。我们回顾了目前可用的SRL,重点介绍长效化合物及其在控制肢端肥大症方面的疗效。通过生化指标、肿瘤缩小以及疾病症状改善与药物相关副作用的平衡来评估疾病控制情况。