10. Perspectives in the Development of Novel Treatment Approaches

Bjornsti M.A. , Houghton P.J. : The TOR pathway: A target for cancer therapy. Nat Rev Cancer, 4: 335–348, 2004.

Wullschleger S. , Loewith R. , Hall M.N. : mTOR signaling in growth and metabolism. Cell, 124: 471–484, 2006.

Pouysségur J. , Dayan F. , Mazure N.M. : Hypoxia signalling in cancer and approaches to enforce tumour regression. Nature, 441: 437–443, 2006.

Shaw R.J. , Cantley L.C. : Ras, PI(3)K and mTOR signalling controls tumour cell growth. Nature, 441: 424–430, 2006.

Faivre S. , Kroemer G. , Raymond E. : Current development of mTOR inhibitors as anticancer agents. Nat Rev Drug Discovm, 5: 671–688, 2006.

Fingar D.C. , Richardson C.J. , Tee A.R. , Cheatham L. , Tsou C. , Blenis J. : mTOR controls cell cycle progression through its cell growth effectors S6K1 and 4E-BP1/eukaryotic translation initiation factor 4E. Mol Cell Biol, 24: 200–216, 2004.

Jensen R.T. , Berna M.J. , Bingham D.B. , Norton J.A. : Inherited pancreatic endocrine tumor syndromes: Advances in molecular pathogenesis, diagnosis, management, and controversies. Cancer, 113: 1807–1843, 2008.

Plank T.L. , Logginidou H. , Klein-Szanto A. , Henske E.P. : The expression of hamartin, the product of the TSC1 gene, in normal human tissues and in TSC1- and TSC2-linked angiomyolipomas. Mod Pathol, 12: 539–545, 1999.

Verhoef S. , van Diemen-Steenvoorde R. , Akkersdijk W.L. , Bax N.M. , Ariyurek Y. , Hermans C.J. , van Nieuwenhuizen O. , Nikkels P.G. , Lindhout D. , Halley D.J. , Lips K. , van den Ouweland A.M. : Malignant pancreatic tumour within the spectrum of tuberous sclerosis complex in childhood. Eur J Pediatr, 158: 284–287, 1999.

Eledrisi M.S. , Stuart C.A. , Alshanti M. : Insulinoma in a patient with tuberous sclerosis: Is there an association? Endocr Pract, 8: 109–112, 2002.

Johannessen C.M. , Reczek E.E. , James M.F. : The NF1 tumor suppressor critically regulates TSC2 and mTOR. Proc Natl Acad Sci USA 102: 8573–8578, 2000.

Tan C.C. , Hall R.I. , Semeraro D. , Irons R.P. , Freeman J.G. : Ampullary somatostatinoma associated with von Recklinghausen's neurofibromatosis presenting as obstructive jaundice. Eur J Surg Oncol, 22: 298–301, 1996.

van Basten J.P. , van Hoek B. , de Bruïne A. , Arends J.W. , Stockbrügger R.W. : Ampullary carcinoid and neurofibromatosis: Case report and review of the literature. Neth J Med, 44: 202–206, 1994.

Yoshida A. , Hatanaka S. , Ohi Y. , Umekita Y. , Yoshida H. : Von Recklinghausen's disease associated with somatostatinrich duodenal carcinoid (somatostatinoma), medullary thyroid carcinoma and diffuse adrenal medullary hyperplasia. Acta Pathol Jpn, 41: 847–856, 1991.

Hammel P.R. , Vilgrain V. , Terris B. , Penfornis A. , Sauvanet A. , Correas J.M. , Chauveau D. , Balian A. , Beigelman C. , O'Toole D. , Bernades P. , Ruszniewski P. , Richard S. : Pancreatic involvement in von Hippel-Lindau disease. The Groupe Francophone d'Etude de la Maladie de von Hippel-Lindau. Gastroenterology, 119: 1087–1095, 2000.

Zhao J. , Moch H. , Scheidweiler A.F. , Baer A. , Schäffer A.A. , Speel E.J. , Roth J. , Heitz P.U. , Komminoth P. : Genomic imbalances in the progression of endocrine pancreatic tumors. Genes Chromosomes Cancer, 32: 364–372, 2001.

Papouchado B. , Erickson L.A. , Rohlinger A.L. , Hobday T.J. , Erlichman C. , Ames M.M. , Lloyd R.V. : Epidermal growth factor receptor and activated epidermal growth factor receptor expression in gastrointestinal carcinoids and pancreatic endocrine carcinomas. Mod Pathos, 18: 1329–1335, 2005.

vonWichert G. , Jehle P.M. , Hoeflich A. , Koschnick S. , Dralle H. , Wolf E. , Wiedenmann B. , Boehm B.O. , Adler G. , Seufferlein T. : Insulin-like growth factor-I is an autocrine regulator of chromogranin A secretion and growth in human neuroendocrine tumor cells. Cancer Res, 60: 4573–4581, 2000.

Van Gompel J.J. , Chen H. : Insulin-like growth factor 1 signaling in human gastrointestinal carcinoid tumor cells. Surgery, 136: 1297–1302, 2004.

McDaniel M.L. , Marshall C.A. , Pappan K.L. , Kwon G. : Metabolic and autocrine regulation of the mammalian target of rapamycin by pancreatic beta-cells. Diabetes, 51: 2877–2885, 2002.

Missiaglia E. , Dalai S. , Barbi S. , Beghelli S. , Falconi M. , della Peruta M. , Piemonti L. , Capurso G. , Di Florio A. , delle Fave G. , Pederzoli P. , Croce C.M. , Scarpa A. : Pancreatic endocrine tumors: expression profiling evidences a role for AKT-mTOR pathway. J Clin Oncol, 28: 245–255, 2009.

Yao J.C. , Phan A.T. , Chang D.Z. , Wolff R.A. , Hess K. , Gupta S. , Jacobs C. , Mares J.E. , Landgraf A.N. , Rashid A. , Meric-Bernstam F. : Efficacy of RAD001 (everolimus) and octreotide LAR in advanced low- to intermediate-grade neuroendocrine tumors: Results of a phase II trial. J Clin Oncol, 26: 4311–4318, 2008.

Yao J.C. , Lombard-Bohas C. , Baudin E. , Kvols L.K. , Rougier P. , Ruszniewski P. , Hoosen S. , St. Peter J. , Haas T. , Lebwohl D. , Van Cutsem E. , Kulke M.H. , Hobday T.J. , O'Dorisio T.M. , Shah M.H. , Cadiot G. , Luppi G. , Posey J.A. , Wiedenmann B. : Daily oral everolimus activity in patients with metastatic pancreatic neuroendocrine tumors after failure of cytotoxic chemotherapy: a phase II trial. J Clin Oncol, 28: 69–76, 2010.

Kulke M.H. , Bergsland M.D. , Yao J.C. : Glycemic control in patients with insulinoma treated with everolimus. N Engl J Med, 360: 195–197, 2009.

Aspinwall C.A. , Lakey J.R. , Kennedy R.T. : Insulin-stimulated insulin secretion in single pancreatic beta cells. J Biol Chem, 274: 6360–6365, 1999.

Leibiger I.B. , Leibiger B. , Moede T. , Berggren P.O. : Exocytosis of insulin promotes insulin gene transcription via the insulin receptor/PI-3 kinase/p70 s6 kinase and CaM kinase pathways. Mol Cell, 1: 933–938, 1998.

Fuhrer D.K. , Kobayashi M. , Jiang H. : Insulin release and suppression by tacrolimus, rapamycin and cyclosporin A are through regulation of the ATP-sensitive potassium channel. Diabetes Obes Metab, 3: 393–402, 2001.

Di Paolo S. , Teutonico A. , Leogrande D. , Capobianco C. , Schena P.F. : Chronic inhibition of mammalian target of rapamycin signaling downregulates insulin receptor substrates 1 and 2 and AKT activation: a crossroad between cancer and diabetes? J Am Soc Nephrol, 17: 2236–2244, 2006.

Zatterstrom U.K. , Felbor U. , Fukai N. , Olsen B.R. : Collagen XVIII/endostatin structure and functional role in angiogenesis. Cell Struct Funct, 25: 97–101, 2000.

O'Reilly M.S. , Boehm T. , Shing Y. , Fukai N. , Vasios G. , Lane W.S. , Flynn E. , Birkhead J.R. , Olsen B.R. , Folkman J. : Endostatin: An endogenous inhibitor of angiogenesis and tumor growth. Cell, 88: 277–285, 1997.

Perletti G. , Concari P. , Giardini R. , Marras E. , Piccinini F. , Folkman J. , Chen L. : Antitumor activity of endostatin against carcinogeninduced rat primary mammary tumors. Cancer Res, 60: 1793–1796, 2000.

Bergers G. , Javaherian K. , Lo K.M. , Folkman J. , Hanahan D. : Effects of angiogenesis inhibitors on multistage carcinogenesis in mice. Science, 284: 808–812, 1999.

Boehm T. , Folkman J. , Browder T. , O'Reilly M.S. : Antiangiogenic therapy of experimental cancer does not induce acquired drug resistance. Nature, 390: 404–407, 1997.

Herbst R.S. , Hess K.R. , Tran H.T. , Tseng J.E. , Mullani N.A. , Charnsangavej C. , Madden T. , Davis D.W. , McConkey D.J. , O'Reilly M.S. , Ellis L.M. , Pluda J. , Hong W.K. , Abbruzzese J.L. : Phase I study of recombinant human endostatin in patients with advanced solid tumors. J Clin Oncol, 20: 3792–3803, 2002.

Eder J.P. Jr. , Supko J.G. , Clark J.W. , Puchalski T.A. , Garcia-Carbonero R. , Ryan D.P. , Shulman L.N. , Proper J. , Kirvan M. , Rattner B. , Connors S. , Keogan M.T. , Janicek M.J. , Fogler W.E. , Schnipper L. , Kinchla N. , Sidor C. , Phillips E. , Folkman J. , Kufe D.W. : Phase I clinical trial of recombinant human endostatin administered as a short intravenous infusion repeated daily. J Clin Oncol, 20: 3772–3784, 2002.

Thomas J.P. , Arzoomanian R.Z. , Alberti D. , Marnocha R. , Lee F. , Friedl A. , Tutsch K. , Dresen A. , Geiger P. , Pluda J. , Fogler W. , Schiller J.H. , Wilding G. : Phase I pharmacokinetic and pharmacodynamic study of recombinant human endostatin in patients with advanced solid tumors. J Clin Oncol, 21: 223–231, 2003.

Hansma A.H. , Broxterman H.J. , van der Horst I. , Yuana Y. , Boven E. , Giaccone G. , Pinedo H.M. , Hoekman K. : Recombinant human endostatin administered as a 28-day continuous intravenous infusion, followed by daily subcutaneous injections: A phase I and pharmacokinetic study in patients with advanced cancer. Ann Oncol, 16: 1695–1701, 2005.

Kulke M.H. , Bergsland E.K. , Ryan D.P. , Enzinger P.C. , Lynch T.J. , Zhu A.X. , Meyerhardt J.A. , Heymach J.V. , Fogler W.E. , Sidor C. , Michelini A. , Kinsella K. , Venook A.P. , Fuchs C.S. : Phase II study of recombinant human endostatin in patients with advanced neuroendocrine tumors. J Clin Oncol, 24: 3555–3561, 2006.

Atkins M.B. , Hidalgo M. , Stadler W.M. , Logan T.F. , Dutcher J.P. , Hudes G.R. , Park Y. , Liou S.H. , Marshall B. , Boni J.P. , Dukart G. , Sherman M.L. : Randomized phase II study of multiple dose levels of CCI-779, a novel mammalian target of rapamycin kinase inhibitor, in patients with advanced refractory renal cell carcinoma. J Clin Oncol, 22: 909–918, 2004.

Baselga J. , Fumoleau P. , Gil M. , Colomer R. , Roche H. , Cortes-Funes H. , Burstein H. , Kaufman P. , Kong S. , Moore L. : Phase, II, 3-arm study of CCI-779 in combination with letrozole in postmenopausal women with locally advanced or metastatic breast cancer: preliminary results. Proc Am Soc Clin Oncol, 23: 13, 2004.

Chan S. , Scheulen M.E. , Johnston S. , Mross K. , Cardoso F. , Dittrich C. , Eiermann W. , Hess D. , Morant R. , Semiglazov V. , Borner M. , Salzberg M. , Ostapenko V. , Illiger H.J. , Behringer D. , Bardy-Bouxin N. , Boni J. , Kong S. , Cincotta M. , Moore L. : Phase II study of temsirolimus (CCI-779), a novel inhibitor of mTOR, in heavily pretreated patients with locally advanced or metastatic breast cancer. J Clin Oncol, 23: 5314–5322, 2005.

Raymond E. , Alexandre J. , Faivre S. , Vera K. , Materman E. , Boni J. , Leister C. , Korth-Bradley J. , Hanauske A. , Armand J.P. : Safety and pharmacokinetics of escalated doses of weekly intravenous infusion of CCI-779, a novel mTOR inhibitor, in patients with cancer. J Clin Oncol, 22: 2336–2347, 2004.

Duran I. , Kortmansky J. , Singh D. , Hirte H. , Kocha W. , Goss G. , Le L. , Oza A. , Nicklee T. , Ho J. , Birle D. , Pond G.R. , Arboine D. , Dancey J. , Aviel-Ronen S. , Tsao M-S , Hedley D. , Siu L.L. : A phase II clinical and pharmacodynamic study of temsirolimus in advanced neuroendocrine carcinomas. Br J Cancer, 95: 1148–1154, 2006.

Druker B.J. , Talpaz M. , Resta D.J. , Peng B. , Buchdunger E. , Ford J.M. , Lydon N.B. , Kantarjian H. , Capdeville R. , Ohno-Jones S. , Sawyers C.L. : Efficacy and safety of a specific inhibitor of the BCR-ABLt yrosine kinase in chronic myeloid leukemia. N Engl J Med, 344: 1031–1037, 2001.

Demetri G.D. , von Mehren M. , Blanke C.D. , Van den Abbeele A.D. , Eisenberg B. , Roberts P.J. , Heinrich M.C. , Tuveson D.A. , Singer S. , Janicek M. , Fletcher J.A. , Silverman S.G. , Silberman S.L. , Capdeville R. , Kiese B. , Peng B. , Dimitrijevic S. , Druker B.J. , Corless C. , Fletcher C.D. , Joensuu H. : Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors. N Engl J Med, 347: 472–480, 2002.

Yao J.C. , Zhang J.X. , Rashid A. , Yeung S-C J. , Szklaruk J. , Hess K. , Xie K. , Ellis L. , Abbruzzese J.L. , Ajani J.A. : Clinical and in vitro studies of imatinib in advanced carcinoid tumors. Clin Cancer Res, 13: 234–240, 2007.

Terris B. , Scoazec J.Y. , Rubbia L. , Bregeaud L. , Pepper M.S. , Ruszniewski P. , Belghiti J. , Fléjou J. , Degott C. : Expression of vascular endothelial growth factor in digestive neuroendocrine tumours. Histopathology, 32: 133–138, 1998.

Ambs S. , Bennett W.P. , Merriam W.G. , Ogunfusika M.O. , Oser S.M. , Khan M.A. , Jones R.T. , Harris C.C. : Vascular endothelial growth factor and nitric oxide synthase expression in human lung cancer and the relation to p53. Br J Cancer, 78: 233–239, 1998.

Phan A.T. , Wang L. , Xie K. : Association of VEGF expression with poor prognosis among patients with low-grade neuroendocrine carcinoma. J Clin Oncol 24: 18s, (abs 4091), 2006.

Yao J.C. , Phan A. , Hoff P.M. , Chen H.X. , Charnsangavej C. , Yeung S-C J. , Hess K. , Ng C. , Abbruzzese J.L. , Ajani J.A. : Targeting Vascular Endothelial Growth Factor in Advanced Carcinoid Tumor: A Random Assignment Phase II Study of Depot Octreotide With Bevacizumab and Pegylated Interferon Alfa-2b. J Clin Oncol, 26: 1316–1323, 2008.

Mendel D.B. , Laird A.D. , Xin X. , Louie S.G. , Christensen J.G. , Li G. , Schreck R.E. , Abrams T.J. , Ngai T.J. , Lee L.B. , Murray L.J. , Carver J. , Chan E. , Moss K.G. , Haznedar J.O. , Sukbuntherng J. , Blake R.A. , Sun L. , Tang C. , Miller T. , Shirazian S. , McMahon G. , Cherrington J.M. : In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: Determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res, 9: 327–337, 2003.

Abrams T.J. , Lee L.B. , Murray L.J. , Pryer N.K. , Cherrington J.M. : SU11248 inhibits KIT and platelet-derived growth factor receptor beta in preclinical models of human small cell lung cancer. Mol Cancer Ther, 2: 471–478, 2003.

Murray L.J. , Abrams T.J. , Long K.R. , Ngai T.J. , Olson L.M. , Hong W. , Keast P.K. , Brassard J.A. , O'Farrell A.M. , Cherrington J.M. , Pryer N.K. : SU11248 inhibits tumor growth and CSF-1R-dependent osteolysis in an experimental breast cancer bone metastasis model. Clin Exp Metastasis, 20: 757–766, 2003.

O'Farrell A.M. , Abrams T.J. , Yuen H.A. , Ngai T.J. , Louie S.G. , Yee K.W. , Wong L.M. , Hong W. , Lee L.B. , Town A. , Smolich B.D. , Manning W.C. , Murray L.J. , Heinrich M.C. , Cherrington J.M. : SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood, 101: 3597–3605, 2003.

Demetri G.D. , van Oosterom A.T. , Garrett C.R. , Blackstein M.E. , Shah M.H. , Verweij J. , McArthur G. , Judson I.R. , Heinrich M.C. , Morgan J.A. , Desai J. , Fletcher C.D. , George S. , Bello C.L. , Huang X. , Baum C.M. , Casali P.G. : Efficacy and safety of sunitinib in patients with advanced gastrointestinal stromal tumour after failure of imatinib: A randomised controlled trial. Lancet, 368: 1329–1338, 2006.

Motzer R.J. , Michaelson M.D. , Redman B.G. , Hudes G.R. , Wilding G. , Figlin R.A. , Ginsberg M.S. , Kim S.T. , Baum C.M. , DePrimo S.E. , Li J.Z. , Bello C.L. , Theuer C.P. , George D.J. , Rini B.I. : Activity of SU11248, a multitargeted inhibitor of vascular endothelial growth factor receptor and plateletderived growth factor receptor, in patients with metastatic renal cell carcinoma. J Clin Oncol, 24: 16–24, 2006.

Motzer R.J. , Rini B.I. , Bukowski R.M. , Curti B.D. , George D.J. , Hudes G.R. , Redman B.G. , Margolin K.A. , Merchan J.R. , Wilding G. , Ginsberg M.S. , Bacik J. , Kim S.T. , Baum C.M. , Michaelson M.D. : Sunitinib in patients with metastatic renal cell carcinoma. JAMA, 295: 2516–2524, 2006.

Motzer R.J. , Hutson T.E. , Tomczak P. , Michaelson M.D. , Bukowski R.M. , Rixe O. , Oudard S. , Negrier S. , Szczylik C. , Kim S.T. , Chen I. , Bycott P.W. , Baum C.M. , Figlin R.A. : Sunitinib versus interferon alfa in metastatic renal cell carcinoma. N Engl J Med, 356: 115–124, 2007.

Kulle M.H. , Lenz H-J , Meropol N.J. , Posey J. , Ryan D.P. , Picus J. , Bergsland E. , Stuart K. , Tye L. , Huang X. , Li J.Z. , Baum C.M. , Fuchs C.S. : Activity of sunitinib in patients with advanced neuroendocrine tumors. J Clin Oncol, 26: 3403–3410, 2008.

Raymond E. , Niccoli-Sire P. , Bang Y. , Borbath I. , Lombard-Bohas C. , Valle J.W. , Patyna S. , Lu D. , Chao R.C. , Raoul J. : Updated results of the phase III trial of sunitinib (SU) versus placebo (PBO) for treatment of advanced pancreatic neuroendocrine tumors (NET). Proc ASCO GI 2010 (abs 127), 2010.

Hofland L.J. , Lamberts S.W.J. : The pathophysiological consequences of somatostatin receptor internalization and resistance. Endocr Rev, 24: 28–47, 2003.

Ferone D. , Pivonello R. , Resmini E. , Boschetti M. , Rebora A. , Alberelli M. , Albanese V , Colao A. , Culler M.D. , Minuto F. : Pre-clinical and clinical experiences with the role of dopamine receptors in the treatment of pituitary adenomas. Eu J Endocrinol, 156; S37–S43, 2007.

Panetta R. , Patel Y.C. : Expression of mRNA for all five human somatostatin receptors (hSSTR1–5) in pituitary tumors. Life Sciences, 56: 333–342, 1995.

Stefaneanu L. , Kovacs K. , Horvath E. , Buchfelder M. , Fahlbusch R. , Lancranjan L. : Dopamine D2 receptor gene expression in human adenohypophysial adenomas. Endocrine, 14: 329–336, 2001.

Zatelli M.C. , Piccin D. , Tagliati F. , Bottoni A. , Ambrosio M.R. , Margutti A. , Scanarini M. , Bondanelli M. , Culler M.D. , degli Uberti E.C. : Dopamine receptor subtype 2 and somatostatin receptor subtype 5 expression influences somatostatin analogs effects on human somatotroph pituitary adenomas in vitro. J Mol Endocrinol, 35: 333–341, 2005.

Taboada G.F. , Luque R.M. , Bastos W. , Guimaraes R.F. , Marcondes J.B. , Chimelli L.M. , Fontes R. , Mata P.J. , Filho P.N. , Carvalho D.P. , Kineman R.D. , Gadelha M.R. : Quantitative analysis of somatostatin receptor subtype (SSTR1-5) gene expression levels in somatotropinomas and non-functioning pituitary adenomas. Eur J Endocrinol, 156: 65–74, 2007.

Ferone D. , de Herder W.W. , Pivonello R. , Kros J.M. , van Koetsveld P.M. , de Jong T. , Minuto F. , Colao A. , Lamberts S.W.J. , & Hofland L.J. : Correlation of in vitro and in vivo somatotropic adenoma responsiveness to somatostatin analogs and dopamine agonists with immunohistochemical evaluation of somatostatin and dopamine receptors and electron microscopy. J Clin Endocrinol Metab, 93: 1412–1417, 2008.

Saveanu A. , Jaquet P. : Somatostatin-dopamine ligands in the treatment of pituitary adenomas. Rev Endocr Metab Disord, 10(2), 83–90, 2009. (2008, Epub ahead of print).

Miller G.M. , Alexander J.M. , Bikkal H.A. , Katznelson L. , Zervas N.T. , Klibanski A. : Somatostatin receptor subtype gene expression in pituitary adenomas. J Clin Endocrinol Metab, 80: 1386–1392, 1995.

Fusco A. , Gunz G. , Jaquet P. , Dufour H. , Germanetti A.L. , Culler M.D. , Barlier A. , Saveanu A. : Somatostatinergic ligands in dopaminesensitive or -resistant prolactinomas. Eur J Endocrinol, 158: 595–603, 2007.

Renner U. , Arzberger T. , Pagotto U. , Leimgruber S. , Uhl E. , Muller A. , Lange M. , Weindl A. , Stalla G.K. : Heterogeneous dopamine D2 receptor subtype messenger ribonucleic acid expression in clinically nonfunctioning pituitary adenomas. J Clin Endocrinol Metab, 83: 1368–1375, 1998.

Pivonello R. , Matrone C. , Filippella M. , Cavallo L.M. , Di Somma C. , Cappabianca P. , Colao A. , Annunziato L. , Lombardi G. : Dopamine receptor expression and function in clinically non-functioning pituitary tumors: comparison with the effectiveness of cabergoline treatment. J Clin Endocrinol Metab, 89: 1674–1683, 2004.

Batista D.L. , Zhang X. , Gejman R. , Ansell P.J. , Zhou Y. , Johnson S.A. , Swearingen B. , Hedley-Whyte E.T. , Stratakis C.A. , Klibanski A. : The effects of SOM230 on cell proliferation and adrenocorticotropin secretion in human corticotroph pituitary adenomas. J Clin Endocrinol Metab, 91: 4482–4488, 2006.

de Bruin C. , Feelders R.A. , Lamberts S.W.J. , Hofland L.J. : Somatostatin and dopamine receptors as targets for medical treatment of Cushing's Syndrome. Rev Endocr Metab Disord, 42: 47–56, 2009.

O'Toole D. , Saveanu A. , Couvelard A. , Gunz G. , Enjalbert A. , Jaquet P. , Ruszniewski P. , Barlier A. : The analysis if quantitative expression of somatostatin and dopamine receptors in gastro-entero-pancreatic tumors opens new therapeutic strategies. Eur J Endocrinol, 155: 849–57, 2006.

Pivonello R. , Ferone D. , de Herder W.W. , Faggiano A. , Bodei L. , de Krijger R.R. , Lombardi G. , Colao A. , Lamberts S.W.J. , Hofland L.J. : Dopamine receptor expression and function in corticotroph ectopic tumors. J Clin Endocrinol Metab, 92: 65–69, 2007.

Pivonello R. , Ferone D. , Lamberts S.W.J. , Colao A. : Cabergoline plus lanreotide for ectopic Cushing's syndrome. N Engl J Med, 352(23): 2457–2458, 2005.

Rocheville M. , Lange D.C. , Kumar U. , Patel S.C. , Patel R.C. , Patel Y.C. : Receptors for dopamine and somatostatin: formation of hetero-oligodimers with enhanced functional activity. Science, 288: 154–157, 2000.

Lesage C. , Seymour C. , Urbanavicius V. , Beckers A. , Kazanavicius G. , Colao A. : Clinical pharmacology and pharmacokinetics of the novel chimeric compound BIM 23A760: results of a multicenter, open-label, phase 2, single-dose study in acromegaly. J Clin Endocrinol Metab, 2010, in press.

de Herder W.W. , Hofland L.J. , van der Lely A.J. , Lamberts S.W. : Somatostatin receptors in gastroentero-pancreatic neuroendocrine tumours. Endocr Relat Cancer, 10: 451–458, 2003.

Kaltsas G.A. , Mukherjee J.J. , Grossman A.B. : The value of radiolabelled MIBG and octreotide in the diagnosis and management of neuroendocrine tumours. Ann Oncol, 12: 47–50, 2001.

de Herder W.W. , Hofland L.J. , van der Lely A.J. , Lamberts S.W. : Peptide receptors in gut endocrine tumours. Bailliere's Clin Gastroenterol, 10: 571–587, 1996.

Hofland L.J. , van Koetsveld P.M. , Waaijers M. , Lamberts S.W. : Internalisation of isotope-coupled somatostatin analogues. Digestion, 57: 2–6, 1996.

De Jong M. , Bernard B.F. , De Bruin E. , Van Gameren A. , Bakker W.H. , Visser T.J. , Macke H.R. , Krenning E.P. : Internalization of radiolabelled [DTPA0]octreotide and [DOTA0,Tyr3]octreotide: peptides for somatostatin receptor-targeted scintigraphy and radionuclide therapy. Nucl Med Commun, 19: 283–288, 1998.

Andersson P. , Forssell-Aronsson E. , Johanson V. , Wangberg B. , Nilsson O. , Fjalling M. , Ahlman H. : Internalization of indium-111 into human neuroendocrine tumor cells after incubation with indium-111-DTPA-D-Phe1-octreotide. J Nucl Med, 37: 2002–2006, 1996.

Duncan J.R. , Stephenson M.T. , Wu H.P. , Anderson C.J. : Indium-111-diethylenetriaminepentaacetic acid-octreotide is delivered in vivo to pancreatic, tumor cell, renal, and hepatocyte lysosomes. Cancer Res, 57: 659–671, 1997.

Krenning E.P. , Kooij P.P. , Bakker W.H. , Breeman W.A. , Postema P.T. , Kwekkeboom D.J. , Oei H.Y. , de Jong M. , Visser T.J. , Reijs A.E. , Lamberts S.W.J. : Radiotherapy with a radiolabeled somatostatin analogue, [111In-DTPA-D- Phe1]-octreotide. A case history. Ann NY Acad Sci, 733: 496–506, 1994.

Bakker W.H. , Krenning E.P. , Breeman W.A. , Kooij P.P. , Reubi J.C. , Koper J.W. , de Jong M. , Lameris J.S. , Visser T.J. , Lamberts S.W. : In vivo useofa radioiodinated somatostatin analogue: dynamics, metabolism, and binding to somatostatin receptor-positive tumors in man. J Nucl Med, 32: 1184–1189, 1991.

Bakker W.H. , Krenning E.P. , Reubi J.C. , Breeman W.A. , Setyono-Han B. , de Jong M. , Kooij P.P. , Bruns C. , van Hagen P.M. , Marbach P. , Visser T.J. , Lamberts S.W.J. : In vivo application of [111In-DTPA-D-Phe1]-octreotide for detection of somatostatin receptor-positive tumors in rats. Life Sci, 49: 1593–1601, 1991.

Kwekkeboom D.J. , Krenning E.P. : Somatostatin receptor imaging. Semin Nucl Med, 32: 84–91, 2002.

Gibril F. , Jensen R.T. : Diagnostic uses of radiolabelled somatostatin receptor analogues in gastroenteropancreatic endocrine tumours. Dig Liver Dis, 36: 106–120, 2004.

Oberg K. , Eriksson B. : Nuclear medicine in the detection, staging and treatment of gastrointestinal carcinoid tumours. Best Pract Res Clin Endocrinol Metab, 19: 265–276, 2005.

Gabriel M. , Decristoforo C. , Maina T. , Nock B. , vonGuggenberg E. , Cordopatis P. , Moncayo R. : 99mTc-N4-[Tyr3]Octreotate Versus 99mTc-EDDA/HYNIC-[Tyr3]Octreotide: an intrapatient comparison of two novel Technetium-99m labeled tracers for somatostatin receptor scintigraphy. Cancer Biother Radiopharm, 19: 73–79, 2004.

Decristoforo C. , Maina T. , Nock B. , Gabriel M. , Cordopatis P. , Moncayo R. : ⁹⁹mTc-Demotate 1: first data in tumour patients-results of a pilot/phase I study. Eur J Nucl Med Mol Imaging, 30: 1211–1219, 2003.

Virgolini I. , Britton K. , Buscombe J. , Moncayo R. , Paganelli G. , Riva P. : In- and Y-DOTA-lanreotide: results and implications of the MAURITIUS trial. Semin Nucl Med, 32: 148–155, 2002.

Virgolini I. , Traub T. , Novotny C. , Leimer M. , Fuger B. , Li S.R. , Patri P. , Pangerl T. , Angelberger P. , Raderer M. , Burggasser G. , Andreae F. , Kurtaran A. , Dudczak R. : Experience with indium-111 and yttrium-90-labeled somatostatin analogs. Current Pharmacy Design, 8: 1781–1807, 2002.

Krenning E.P. , de Jong M. , Kooij P.P. , Breeman WA , Bakker WH , de Herder W.W. , van Eijck C.H. , Kwekkeboom D.J. , Jamar F. , Pauwels S. , Valkema R. : Radiolabelled somatostatin analogue(s) for peptide receptor scintigraphy and radionuclide therapy. Ann Oncol, 10: 23–29, 1999.

Valkema R. , De Jong M. , Bakker W.H. , Breeman W.A. , Kooij P.P. , Lugtenburg P.J. , De Jong F.H. , Christiansen A. , Kam B.L. , De Herder W.W. , Stridsberg M. , Lindemans J. , Ensing G. , Krenning E.P. : Phase I study of peptide receptor radionuclide therapy with [In-DTPA]-octreotide: the Rotterdam experience. Semin Nucl Med, 32: 110–122, 2002.

De Jong M. , Bakker W.H. , Breeman W.A. , Bernard B.F. , Hofland L.J. , Visser T.J. , Srinivasan A. , Schmidt M. , Béhé M. , Mäcke H.R. , Krenning E.P. : Pre-clinical comparison of [DTPA0, Tyr3]octreotide and [DOTA⁰, D-Phe¹, Tyr³] octreotide as carriers for somatostatin receptor-targeted scintigraphy and radionuclide therapy. Int J Cancer, 75: 406–411, 1998.

Reubi J.C. , Schar J.C. , Waser B. , Wenger S. , Heppeler A. , Schmitt J.S. , Macke H.R. : Affinity profiles for human somatostatin receptor subtypes SST1-SST5 of somatostatin radiotracers selected for scintigraphic and radiotherapeutic use. Eur J Nucl Med, 27: 273–282, 2000.

Cremonesi M. , Ferrari M. , Zoboli S. , Chinol M. , Stabin M.G. , Orsi F. , Maecke H.R. , Jermann E. , Robertson C. , Fiorenza Tosi G. , Paganelli G. : Biokinetics and dosimetry in patients administered with ¹¹¹In-DOTA-Tyr³-octreotide: implications internal radiotherapy with ⁹⁰Y-DOTATOC. Eur J Nucl Med, 26: 877–886, 1999.

Teunissen J.J. , Kwekkeboom D.J. , Krenning E.P. : Quality of life in patients with gastroenteropancreatic tumors treated with [¹⁷⁷Lu-DOTA0,Tyr³]octreotate. J Clin Oncol, 22: 2724–2729, 2004.

Krenning E.P. , Kwekkeboom D.J. , Valkema R. , Pauwels S. , Kvols L.K. , & de Jong M. : Peptide receptor radionuclide therapy. Ann NY Acad Sci, 1014: 234–245, 2004.

Kwekkeboom D.J. , Mueller-Brand J. , Paganelli G. , Anthony L.B. , Pauwels S. , Kvols L.K. , O'Dorisio T.M. , Valkema R. , Bodei L. , Chinol M. , Maecke H.R. , & Krenning E.P. : Overview of results of peptide receptor radionuclide therapy with 3 radiolabeled somatostatin analogs. J Nucl Med, 46: 62–66, 2005.

Pauwels S. , Barone R. , Walrand S. , Borson-Chazot F. , Valkema R. , Kvols L.K. , Krenning E.P. , & Jamar F. : Practical dosimetry of peptide receptor radionuclide therapy with ⁽⁹⁰⁾Y-labeled somatostatin analogs. J Nucl Med, 46: 92–98, 2005.

Reubi J.C. , Macke H.R. , & Krenning E.P. : Candidates for peptide receptor radiotherapy today and in the future. J Nucl Med, 46: 67–75, 2005.

Cremonesi M. , Bodei L. , Ferrari M. , Tosi G. , Paganelli G. : Dosimetry in peptide radionuclide receptor therapy: a review. J Nucl Med, 47: 1467–1475, 2006.

Cremonesi M. , Botta F. , Di Dia A. , Ferrari M. , Bodei L. , De Cicco C. , Rossi A. , Bartolomei M. , Mei R. , Severi S. , Salvatori M. , Pedroli G. , Paganelli G. : Dosimetry for treatment with radiolabelled somatostatin analogues. A review. Q J Nucl Med Mol Imaging, 54: 37–51, 2010.

Bodei L. , Cremonesi M. , Grana C. , Rocca P. , Bartolomei M. , Chinol M. , Paganelli G. : Receptor radionuclide therapy with ⁹⁰Y-[DOTA]0-Tyr³-octreotide (⁹⁰Y-DOTATOC) in neuroendocrine tumours. Eur J Nucl Med Mol Imaging, 31: 1038–1046, 2004.

Otte A. , Herrmann R. , Heppeler A. , Behe M. , Jermann E. , Powell P. , Maecke H.R. , Muller J. : Yttrium-90 DOTATOC: first clinical results. Eur J Nucl Med, 26: 1439–1447, 1999.

Waldherr C. , Pless M. , Maecke H.R. , Schumacher T. , Crazzolara A. , Nitzsche E.U. , Haldemann A. , Mueller-Brand J. : Tumor response and clinical benefit in neuroendocrine tumors after 7.4 GBq ⁹⁰Y-DOTATOC. J Nucl Med, 43: 610–616, 2002.

Paganelli G. , Zoboli S. , Cremonesi M. , Bodei L. , Ferrari M. , Grana C. , Bartolomei M. , Orsi F. , De Cicco C. , Mäcke H.R. , Chinol M. , de Braud F. : Receptor-mediated radiotherapy with ⁹⁰Y-DOTA-D-Phe1-Tyr³-octreotide. Eur J Nucl Med, 28: 426–434, 2001.

Bodei L. , Cremonesi M. , Zoboli S. , Grana C. , Bartolomei M. , Rocca P. , Caracciolo M. , Mäcke H.R. , Chinol M. , Paganelli G. : Receptor-mediated radionuclide therapy with ⁹⁰Y-DOTA-TOC in association with amino acid infusion: a phase I study. Eur J Nucl Med, 30: 207–216, 2003.

Kwekkeboom D.J. , Bakker W.H. , Kam B.L. , Teunissen J.J. , Kooij P.P. , de Herder W.W. , Feelders R.A. , van Eijck C.H. , de Jong M. , Srinivasan A. , Erion J.L. , Krenning E.P. : Treatment of patients with gastro-entero-pancreatic (GEP) tumours with the novel radiolabelled somatostatin analogue [¹⁷⁷Lu-DOTA(0),Tyr³]octreotate. Eur J Nucl Med Mol Imaging, 30: 417–422, 2003.

Kwekkeboom D.J. , de Herder W.W. , Kam B.L. , van Eijck C.H. , van Essen M. , Kooij P.P. , Feelders R.A. , van Aken M.O. , Krenning E.P. : Treatment With the Radiolabeled Somatostatin Analog [¹⁷⁷Lu-DOTA0,Tyr³]Octreotate: Toxicity, Efficacy, and Survival. J Clin Oncol, 26: 2124–2130, 2008.