Somatostatin Analogues: From Research to Clinical Practice

Provides state–of–the–art coverage of somatostatin analogue use in diagnostics and therapy

Studies have shown that somatostatin analogues may inhibit growth of many tumors in vivo in animal studies, which include pituitary tumors, endocrine pancreatic tumors and small cell lung cancers. Somatostatin is a 14–amino–acid peptide hormone that acts as a neurotransmitter in the central nervous system. Analogues here refer to compounds that have similar physical, chemical, biochemical, or pharmacological properties. The human somatostatin has a very short half–life in circulation (2–3 minutes) and is easily broken down by endogenous peptidases. Therefore, specific somatostatin analogues have been developed that block hormone release.

Featuring chapters from specialists in endocrinology, physiology, pathology, and nuclear medicine, Somatostatin Analogues: From Research to Clinical Practice provides comprehensive overview of somatostatin and its analogues, from their history to future perspectives. Divided into four sections, the book:

Presents the history of somatostatin discovery, the physiology of endogenous somatostatin family, its actions, receptors and receptors distribution in normal tissues as well as in malignancies and other pathologies Discusses diagnostic applications of radiolabeled somatostatin analogues, which includes giving detailed characteristics of available radiopharamaceuticals for both SPECT and PET, and focuses on the clinical entities in which such diagnostic modality is indicated Describes somatostatin analogues use in radioisotope therapy, such as: radiopharmaceuticals and isotopes for therapeutic purposes, dosimetry, dual–isotope therapy Covers the preclinical and research issues: novel somatostatin receptor agonists, pansomatostatins, somatostatin receptor antagonist, dopastatins and coritstatins
Compiled with a multidisciplinary approach, this monograph reflects the progressive nature of the field and expertise of authors who are renowned experts and researchers. Focused on future applications, novel compounds and areas for further research, this book is valuable for physicians, endocrinologists, nuclear medicine specialists, radiotherapists, pharmacists, as well as doctoral students and professors involved in somatostatin research.

Contributors viii

Preface xii

Acknowledgements xv

1 Somatostatin: The History of Discovery 1
Malgorzata Trofimiuk Müldner and Alicja Hubalewska Dydejczyk

2 Physiology of Endogenous Somatostatin Family: Somatostatin Receptor Subtypes, Secretion, Function and Regulation, and Organ Specific Distribution 6
Marily Theodoropoulou

3 Somatostatin Receptors in Malignancies and Other Pathologies 21
Marco Volante, Adele Cassenti, Ida Rapa, Luisella Righi, and Mauro Papotti

4 The Use of Radiolabeled Somatostatin Analogue in Medical Diagnosis: Introduction 31
Alberto Signore

4.1 Somatostatin Receptor Scintigraphy SPECT 35
Renata Miko ajczak and Alberto Signore

4.2 Molecular Imaging of Somatostatin Receptor Positive Tumors Using PET/CT 55

Richard P. Baum and Harshad R. Kulkarni
4.3 Other Radiopharmaceuticals for Imaging GEP NET 75
Klaas Pieter Koopmans, Rudi A. Dierckx, Philip H. Elsinga, Thera P. Links, Ido P. Kema, Helle–Brit Fiebrich, Annemieke M.E. Walekamp, Elisabeth G.E. de Vries, and Adrienne H. Brouwers

4.4 The Place of Somatostatin Receptor Scintigraphy in Clinical Setting: Introduction 86
Alicja Hubalewska Dydejczyk

4.4.1 Somatostatin Receptor Scintigraphy in Management of Patients with Neuroendocrine Neoplasms 90
Anna Sowa Staszczak, Agnieszka Stefa ska, Agata Jabrocka Hybel, and Alicja Hubalewska Dydejczyk

4.4.2 The Place of Somatostatin Receptor Scintigraphy and Other Functional Imaging Modalities in the Setting of Pheochromocytoma and Paraganglioma 112
Alicja Hubalewska Dydejczyk, Henri J.L.M. Timmers, and Malgorzata Trofimiuk Müldner

4.4.3 Somatostatin Receptor Scintigraphy in Medullary Thyroid Cancer 127
Anouk N.A. van der Horst Schrivers, Adrienne H. Brouwers, and Thera P. Links

4.4.4 Somatostatin Receptor Scintigraphy in Other Tumors Imaging 135
Malgorzata Trofimiuk Müldner and Alicja Hubalewska Dydejczyk

4.4.5 Somatostatin Receptor Scintigraphy in Inflammation and Infection Imaging 153
Alberto Signore, Kelly Luz Anzola Fuentes, and Marco Chianelli

5 Somatostatin Analogues in Pharmacotherapy: Introduction 164
Wouter W. de Herder

5.1 Somatostatin Analogues in Pharmacotherapy 166
Wouter W. de Herder

5.2 Pituitary Tumor Treatment with Somatostatin Analogues 169
Alicja Hubalewska–Dydejczyk, Aleksandra Gilis–Januszewska, and Malgorzata Trofimiuk–Müldner

5.3 Somatostatin Analogues in Pharmacotherapy of Gastroenteropancreatic Neuroendocrine Tumors 189
Frédérique Maire and Philippe Ruszniewski

5.4 Somatostatin Analogue Use in Other than Endocrine Tumor Indications 198
Aleksandra Gilis Januszewska, Malgorzata Trofimiuk Müldner, Agata Jabrocka Hybel,, and Dorota Pach

6 Peptide Receptor Radionuclide Therapy Using Radiolabeled Somatostatin Analogues: An Introduction 207
John Buscombe

6.1 Somatostatin Analogues and Radionuclides Used in Therapy 214
Esther I. van Vliet, Boen L.R. Kam, Jaap J.M. Teunissen, Marion de Jong, Eric P. Krenning, and Dik J. Kwekkeboom

6.2 PRRT Dosimetry 230
Mark Konijnenberg

6.3 Peptide Receptor Radionuclide Therapy (PRRT): Clinical Application 252
Lisa Bodei, and Giovanni Paganelli

6.4 Duo PRRT of Neuroendocrine Tumors Using Concurrent and Sequential Administration of Y 90 and Lu 177 Labeled Somatostatin Analogues 264
Richard P. Baum and Harshad R. Kulkarni

6.5 N onsystemic Treatment of Liver Metastases from Neuroendocrine Tumor 273
Daniel Putzer, Gerlig Widmann, Dietmar Waitz, Werner Jaschke, and Irene J. Virgolini

6.6 Peptide Receptor Radionuclide Therapy: Other Indications 282
Agnieszka Stefa ska, Alicja Hubalewska Dydejczyk, Agata Jabrocka Hybel, and Anna Sowa Staszczak

7 Somatostatin Analogs: Future Perspectives and Preclinical Studies Pansomatostatins 291
Aikaterini Tatsi Berthold A. Nock, Theodosia Maina, and Marion de Jong

8 Radiolabeled Somatostatin Receptor Antagonists 305
Melpomeni Fani and Helmut R. Maecke

9 Cortistatins and Dopastatins 321
Manuela Albertelli and Diego Ferone

Index 000

Alicja Hubalewska–Dydejczyk, PhD, MD, is Professor of Endocrinology and Nuclear Medicine, and Head of the Chair and Department of Endocrinology at the Jagiellonian University′s Medical College (Cracow, Poland).

Alberto Signore, MD, is Professor of Nuclear Medicine and Physician in the Department of Medical–Surgical Sciences and Translational Medicine of the Faculty of Medicine and Psychologu of "Sapienza" University in Rome, Italy.

Marion de Jong, PhD, is Professor of Nuclear Biology at the Departments of Nuclear Medicine and Radiology of the Erasmusc MC in Rotterdam, The Netherlands.

Rudi A. Dierckx, PhD, is Head of the Department of Nuclear Medicine and Molecular Imaging at the University Medical Center Groningen, University of Groningen, the Netherlands.

John Buscombe, MD, is a Consultant Physician in Nuclear Medicine Addenbrooke′s Hospital (Cambridge, UK) and Honorary Professor in Nuclear Medicine at the University of Pretoria, South Africa.

Christophe Van de Wiele, PhD, is Full Professor at the University of Ghent, Belgium.