Abstract

Somatostatin analogs are an invaluable therapeutic option in the diagnosis and treatment of somatotropinomas, thyrotropinomas, and functioning and non-functioning gastroenteropancreatic neuroendocrine tumors. They should also be considered an effective and safe therapeutic alternative to corticotropinomas, gonadotropinomas, and prolactinomas resistant to dopamine agonists. Somatostatin analogs have also shown to be useful in the treatment of other endocrine diseases (congenital hyperinsulinism, Graves’ orbitopathy, diabetic retinopathy, diabetic macular edema), non-endocrine tumors (breast, colon, prostate, lung, and hepatocellular), and digestive diseases (chronic refractory diarrhea, hepatorenal polycystosis, gastrointestinal hemorrhage, dumping syndrome, and intestinal fistula).

Highlights

  • Somastostatin (SST) is a cyclic polypeptide derived from an SST precursor protein that is processed into several peptide hormones, including SST-14, SST-28, and neuronostatin

  • Somatostatin analogs have shown to be useful in the treatment of other endocrine diseases, non-endocrine tumors, and digestive diseases

  • It is proposed that presurgical treatment with SST synthetic analogs (SSAs) is able to improve the general condition of the patient for surgery, to relieve the symptoms related to the disease, to reduce the risk of complications related to anesthesia, and to facilitate tumor resection by shrinking or softening pituitary adenomas, which would result in better surgical outcomes

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Summary

Introduction

Somastostatin (SST) is a cyclic polypeptide derived from an SST precursor protein that is processed into several peptide hormones, including SST-14, SST-28, and neuronostatin. SST-14 is the isoform that was originally characterized [1]. Native SST is not useful in clinical practice because it has an extremely short half life of 1–3 min, rapidly degradated by ubiquitously distributed peptidases in plasma and tissues [3]. After the characterization of SST, several SST synthetic analogs (SSAs) with longer half-life were developed. Three of them have been approved in clinical practice: lanreotide and octretide are considered first-generation SSAs, and pasireotide is considered a second-generation SSA. Their main clinical use has been evaluated in Phase III clinical Trials, and some other uses have been evaluated in prospective studies

Physiological Actions of Somatostatin
SSA in Clinical Practice
Pituitary Adenomas
Somatotropinomas
Thyrotropinomas
Corticotropinomas
Gonadotropinomas
Prolactinomas
Functioning Pancreatic NETs
Antiproliferative Effects in GEP-NETs
Carcinoid Syndrome
Other Diseases
Graves’ Orbitopathy
Dumping Syndrome
Digestive and Lymphatic Fistulas
Acute Bleeding from the Gastrointestinal Tract
Hepatorenal Polycystosis
Refractory Chronic Diarrhea
Non-Endocrine Tumors
Adverse Events
Findings
Conclusions
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