Endocrinology, Diabetology and Andrology Unit, IRCCS Humanitas Research Hospital, Via Manzoni 56, 20089 Milan, Italy.
Division of Neurosurgery (NCH 1), Fondazione IRCCS Istituto Neurologico "Carlo Besta", 20133 Milan, Italy.
Medicina (Kaunas). 2022 Jun 13;58(6):794. doi: 10.3390/medicina58060794.
Somatostatin receptor ligands (SRLs) represent a true milestone in the medical therapy for acromegaly. The first-generation SRLs (FG-SRLs), octreotide and lanreotide, have demonstrated good efficacy in disease control and tumor shrinkage, and are still considered first-line medical therapies. The development of long-acting release (LAR) formulations has certainly improved the therapeutic tolerability of these drugs, although many patients still experience therapy-related burden. As such, new formulations have recently been developed to improve adherence and therapeutic efficacy and more solutions are on the way. In the case of FG-SRL-resistant disease, pasireotide, the only second generation SRL currently available, demonstrated superiority in disease control and tumor shrinkage compared to FG-SRLs. However, its use in clinical practice is still limited due to concern for impairment in glucose homeostasis. In this review, we discuss the news about the present and future role of SRLs in acromegaly, exploring the therapeutical frontiers of this drug class. Moreover, we provide practical guidance on the use of pasireotide, based on the data in the literature and our clinical experience.
生长抑素受体配体(SRLs)代表了肢端肥大症医学治疗的真正里程碑。第一代 SRLs(FG-SRLs),奥曲肽和兰瑞肽,已证明在疾病控制和肿瘤缩小方面具有良好的疗效,仍然被认为是一线医学治疗方法。长效释放(LAR)制剂的开发确实提高了这些药物的治疗耐受性,尽管许多患者仍面临与治疗相关的负担。因此,最近开发了新的制剂来提高患者的顺应性和治疗效果,更多的解决方案正在路上。对于 FG-SRL 耐药疾病,唯一可用的第二代 SRL 培高利特在疾病控制和肿瘤缩小方面优于 FG-SRLs。然而,由于对葡萄糖稳态的损害的担忧,其在临床实践中的应用仍然有限。在这篇综述中,我们讨论了 SRLs 在肢端肥大症中的当前和未来作用的新进展,探索了这类药物的治疗前沿。此外,我们根据文献中的数据和我们的临床经验,提供了培高利特的使用实用指南。