Somatostatin Receptor 2-Targeting Compounds
Somatostatin Receptor 2-Targeting Compounds
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DOI：
10.2967/jnumed.117.191015
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发表时间：
2017-09-01
影响因子：
9.3
通讯作者：
Bodei, Lisa
中科院分区：
文献类型：
--
作者：
Duijzentkunst, Daan A. Smit;Kwekkeboom, Dik J.;Bodei, Lisa
放射性标记的生长抑素类似物的神经内分泌肿瘤（NETs）的分子成像和治疗是治疗诊断化合物发展的里程碑。In-111-pentetreotide全身动脉造影术彻底改变了NETs的诊断和分期以及治疗结果的评价。目前，正电子放射性核素的诊断准确率大于90%。肽受体放射性核素治疗（PRRT）已成为分化良好的不可手术或转移性NETs和一线治疗后疾病进展的患者的公认治疗方法。据报道，疾病控制率（既往疾病进展患者的完全或部分缓解或疾病稳定）高达95%，长期血液学和肾毒性发生率低。在最近发表的一项随机试验中，与使用长效和可重复的奥曲肽强化治疗中肠NET相比，PRRT将疾病进展和死亡的风险降低了79%。PRRT的未来发展包括使用生长抑素受体拮抗剂和α-放射性核素，这可能会进一步提高治疗效果。
The molecular imaging and treatment of neuroendocrine tumors (NETs) with radiolabeled somatostatin analogs represent a milestone in the development of theranostic compounds. Whole-body scintigraphy with In-111-pentetreotide has revolutionized the diagnosis and staging of NETs and the evaluation of treatment outcomes. At present, diagnostic accuracy with positron-emitting radionuclides is greater than 90%. Peptide receptor radionuclide therapy (PRRT) has become a well-accepted treatment for patients with well-differentiated inoperable or metastatic NETs and disease progression after first-line treatment. Disease control rates (complete or partial remission or stable disease in patients with formerly progressive disease) of up to 95%, with a low incidence of long-term hematologic and renal toxicity, have been reported. In a recently published randomized trial, compared with intensified treatment of midgut NETs with long-acting and repeatable octreotide, PRRT reduced the hazard of disease progression and death by 79%. Upcoming developments in PRRT include the use of somatostatin receptor antagonists and a-emitting radionuclides, which may further enhance treatment outcomes.