Pasireotide in Acromegaly: An Overview of Current Mechanistic and Clinical Data

Neuroendocrinology
Susan L Samson

Abstract

Acromegaly is an insidious neuroendocrine disorder caused by hypersecretion of growth hormone (GH) by a somatotroph adenoma. Somatostatin receptor ligands (SRLs) are recommended as first-line medical therapy in patients for whom surgery has failed or is contraindicated. There are 5 known somatostatin receptor subtypes (SSTRs), 2 of which, i.e. SSTR2 and SSTR5, are expressed by a majority of somatotroph adenomas. The currently available SRLs, i.e. octreotide and lanreotide, primarily bind to SSTR2. Pasireotide (SOM230) is a new multireceptor-targeted SRL which has a broader binding profile and an increased affinity for SSTR1, 2, 3, and 5. PubMed searches were performed to identify all of the available published English language data on pasireotide with regard to the mechanism of action, in vitro effects, and clinical data. Preclinical studies have demonstrated that pasireotide has a broader range of functional activity than octreotide. Recently, the efficacy of pasireotide in attenuating GH and insulin-like growth factor 1 (IGF-1) levels in patients with acromegaly has been evaluated in phase III clinical trials. Pasireotide demonstrated superiority over octreotide in achieving biochemical control (i.e. GH ≤2.5 µg/l and age- and...Continue Reading

Citations

Mar 8, 2016·Trends in Endocrinology and Metabolism : TEM·Nicoleta Cristina Olarescu, Jens Bollerslev
Sep 3, 2016·The Journal of Endocrinology·Alejandro Ibáñez-CostaJusto P Castaño
Mar 29, 2018·The Journal of Clinical Endocrinology and Metabolism·Alessia CozzolinoAndrea M Isidori
Aug 21, 2018·Expert Review of Pharmacoeconomics & Outcomes Research·Ewa OrlewskaKatarzyna Orlewska
Jan 1, 2019·Expert Review of Endocrinology & Metabolism·Coralys AbreuMoisés Mercado
Jun 2, 2017·Endocrinology, Diabetes & Metabolism Case Reports·Murray B Gordon, Kellie L Spiller

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