Pasireotide (som230) as a potential treatment for endocrine and nonendocrine tumors

Current Drug Therapy

Volumn 5, Issue 4, 2010, Pages 301-311

  Schmid, Herbert A ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

Author keywords

Neuroendocrine tumor; Pasireotide; Solid tumor; Somatostatin; Somatostatin analogue; SST

Indexed keywords

ANGIOPEPTIN; DEXAMETHASONE; DOCETAXEL; OCTREOTIDE; PASIREOTIDE; SOMATOMEDIN; SOMATOSTATIN RECEPTOR 1; SOMATOSTATIN RECEPTOR 2; SOMATOSTATIN RECEPTOR 3; SOMATOSTATIN RECEPTOR 4; SOMATOSTATIN RECEPTOR 5; TAMOXIFEN;

ACROMEGALY; ANGIOGENESIS; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BINDING AFFINITY; BONE PAIN; BREAST CANCER; CARCINOID SYNDROME; CLINICAL TRIAL; COLORECTAL CANCER; CONTINUOUS INFUSION; CORTICOSTERONE RELEASE; CORTICOTROPIN RELEASE; CUSHING DISEASE; DOSE RESPONSE; DRUG DOSE ESCALATION; DRUG EFFECT; DRUG EFFICACY; DRUG INHIBITION; DRUG MECHANISM; DRUG MEGADOSE; DRUG OVERDOSE; GASTRINOMA; GLIOMA; GLUCAGONOMA; GONADOTROPH ADENOMA; GROWTH HORMONE RELEASE; GROWTH HORMONE SECRETING ADENOMA; HUMAN; HYPOPHYSIS ADENOMA; IC 50; IMMUNOMODULATION; INSULINOMA; MENINGIOMA; NEUROBLASTOMA; NEUROENDOCRINE TUMOR; NONHUMAN; PHEOCHROMOCYTOMA; PRIORITY JOURNAL; PROLACTIN RELEASE; PROLACTINOMA; PROSTATE CANCER; SIGNAL TRANSDUCTION; SINGLE DRUG DOSE; THYROID MEDULLARY CARCINOMA; TREATMENT INDICATION; TREATMENT RESPONSE; TUMOR GROWTH; TUMOR VOLUME;

EID: 78649254895     PISSN: 15748855     EISSN: None     Source Type: Journal    
DOI: 10.2174/157488510792927438     Document Type: Article

References (84)

1. Bruns C, Weckbecker G, Raulf F, et al. Molecular pharmacology of somatostatin-receptor subtypes. Ann N Y Acad Sci 1994; 733: 138-46.
2. Moller LN, Stidsen CE, Hartmann B, Holst JJ. Somatostatin receptors. Biochim Biophys Acta 2003; 1616: 1-84.
3. Hofland LJ, Lamberts SW. The pathophysiological consequences of somatostatin receptor internalization and resistance. Endocr Rev 2003; 24: 28-47.
4. Fjallskog ML, Ludvigsen E, Stridsberg M, Oberg K, Eriksson B, Janson ET. Expression of somatostatin receptor subtypes 1 to 5 in tumor tissue and intratumoral vessels in malignant endocrine pancreatic tumors. Med Oncol 2003; 20: 59-67.
5. Schmid HA, Schoeffter P. Functional activity of the multiligand analog SOM230 at human recombinant somatostatin receptor subtypes supports its usefulness in neuroendocrine tumors. Neuroendocrinology 2004; 80(Suppl 1): 47-50.
6. Ma P, Wang Y, Van Der Hoek J, et al. Pharmacokineticpharmacodynamic comparison of a novel multiligand somatostatin analog, SOM230, with octreotide in patients with acromegaly. Clin Pharmacol Ther 2005; 78: 69-80.
7. Bruns C, Lewis I, Briner U, Meno-Tetang G, Weckbecker G. SOM230: a novel somatostatin peptidomimetic with broad somatotropin release inhibiting factor (SRIF) receptor binding and a unique antisecretory profile. Eur J Endocrinol 2002; 146: 707-16.
8. Weckbecker G, Lewis I, Albert R, Schmid HA, Hoyer D, Bruns C. Opportunities in somatostatin research: biological, chemical and therapeutic aspects. Nat Rev Drug Discov 2003; 2: 999-1017.
9. Hofland LJ, Van Der Hoek J, van Koetsveld PM, et al. The novel somatostatin analog SOM230 is a potent inhibitor of hormone release by growth hormone-and prolactin-secreting pituitary adenomas in vitro. J Clin Endocrinol Metab 2004; 89: 1577-85.
10. Van Der Hoek J, Waaijers M, van Koetsveld PM, et al. Distinct functional properties of native somatostatin receptor subtype 5 compared with subtype 2 in the regulation of ACTH release by corticotroph tumour cells. Am J Physiol Endocrinol Metab 2005; 289: E278-E287.
11. Batista DL, Zhang X, Gejman R, et al. The effects of SOM230 on cell proliferation and adrenocorticotropin secretion in human corticotroph pituitary adenomas. J Clin Endocrinol Metab 2006; 91: 4482-8.
12. Florio T, Morini M, Villa V, et al. Somatostatin inhibits tumor angiogenesis and growth via somatostatin receptor-3-mediated regulation of endothelial nitric oxide synthase and mitogen-activated protein kinase activities. Endocrinology 2003; 144: 1574-84.
13. Teijeiro R, Rios R, Costoya JA, et al. Activation of human somatostatin receptor 2 promotes apoptosis through a mechanism that is independent from induction of p53. Cell Physiol Biochem 2002; 12: 31-8.
14. Susini C, Buscail L. Rationale for the use of somatostatin analogs as antitumor agents. Ann Oncol 2006; 17: 1733-42.
15. Ono K, Suzuki T, Miki Y, et al. Somatostatin receptor subtypes in human non-functioning neuroendocrine tumors and effects of somatostatin analogue SOM230 on cell proliferation in cell line NCI-H727. Anticancer Res 2007; 27: 2231-9.
16. Grozinsky-Glasberg S, Shimon I, Korbonits M, Grossman AB. Somatostatin analogues in the control of neuroendocrine tumours: efficacy and mechanisms. Endocr Relat Cancer 2008; 15: 701-20.
17. Adams RL, Adams IP, Lindow SW, Atkin SL. Inhibition of endothelial proliferation by the somatostatin analogue SOM230. Clin Endocrinol (Oxf) 2004; 61: 431-6.
18. Zatelli MC, Piccin D, Vignali C, et al. Pasireotide, a multiple somatostatin receptor subtypes ligand, reduces cell viability in nonfunctioning pituitary adenomas by inhibiting vascular endothelial growth factor secretion. Endocr Relat Cancer 2007; 14: 91-102.
19. Schmid HA, Jensen MR. Inhibitory effect of Pasireotide (SOM230) in a rat pancreatic tumor model (CA20948) alone and in combination with Everolimus (RAD001). Proc AACR 2009; abst 808.
20. Fedele M, De Martino I, Pivonello R, et al. SOM230, a new somatostatin analogue, is highly effective in the therapy of growth hormone/prolactin-secreting pituitary adenomas. Clin Cancer Res 2007; 13: 2738-44.
21. Borie R, Fabre A, Prost F, et al. Activation of somatostatin receptors attenuates pulmonary fibrosis. Thorax 2007; 63: 251-8.
22. Rinke A, Müller H-H, Schade-Brittinger C, et al. Placebo controlled, double-blind, prospective, randomized study of the effect of Octreotide LAR in the control of tumor growth in patients with metastatic neuroendocrine midgut tumors: A report from the PROMID study group. J Clin Oncol 2009; 27: 4656-63.
23. Oberg K. Cancer: Antitumor effects of octreotide LAR, a somatostatin analog. Nat Rev Endocrinol 2010; 6: 188-9.
24. Lindholm J, Juul S, Jorgensen JO, et al. Incidence and late prognosis of cushing's syndrome: a population-based study. J Clin Endocrinol Metab 2001; 86: 117-23.
25. Daly AF, Rixhon M, Adam C, Dempegioti A, Tichomirowa MA, Beckers A. High prevalence of pituitary adenomas: a crosssectional study in the province of Liege, Belgium. J Clin Endocrinol Metab 2006; 91: 4769-75.
26. Etxabe J, Vazquez JA. Morbidity and mortality in Cushing's disease: an epidemiological approach. Clin Endocrinol (Oxf) 1994; 40: 479-84.
27. Biller BM, Grossman AB, Stewart PM, et al. Treatment of adreno-corticotropin-dependent Cushing's syndrome: a consensus statement. J Clin Endocrinol Metab 2008; 93: 2454-62.
28. Ambrosi B, Bochicchio D, Fadin C, Colombo P, Faglia G. Failure of somatostatin and octreotide to acutely affect the hypothalamicpituitary-adrenal function in patients with corticotropin hypersecretion. J Endocrinol Invest 1990; 13: 257-61.
29. Lamberts SW, Uitterlinden P, Klijn JM. The effect of the longacting somatostatin analogue SMS 201-995 on ACTH secretion in Nelson's syndrome and Cushing's disease. Acta Endocrinol (Copenh) 1989; 120: 760-6.
30. Hofland LJ, Van Der Hoek J, Feelders R, et al. The multi-ligand somatostatin analogue SOM230 inhibits ACTH secretion by cultured human corticotroph adenomas via somatostatin receptor type 5. Eur J Endocrinol 2005; 152: 645-54.
31. Silva AP, Schoeffter P, Weckbecker G, Bruns C, Schmid HA. Regulation of CRH-induced secretion of ACTH and corticosterone by SOM230 in rats. Eur J Endocrinol 2005; 153: R7-R10.
32. Cukier K, Tewari R, Kurth F, Schmid HA, Lai C, Torpy DJ. Significant response to pasireotide (SOM230) in the treatment of a patient with persistent, refractory Cushing's disease. Clin Endocrinol (Oxf) 2009; 71: 305-7.
33. Boscaro M, Ludlam WH, Atkinson B, et al. Treatment of pituitary dependent Cushing's disease with the multi-receptor ligand somatostatin analog pasireotide (SOM230): A multicenter, phase II trial. J Clin Endocrinol Metab 2009; 94: 115-22.
34. Ben-Shlomo A, Melmed S. Acromegaly. Endocrinol Metab Clin North Am 2008; 37: 101-22, viii.
35. Melmed S. Medical progress: Acromegaly. N Engl J Med 2006; 355: 2558-73.
36. Holdaway IM, Rajasoorya C. Epidemiology of acromegaly. Pituitary 1999; 2: 29-41.
37. Schneider HJ, Sievers C, Saller B, Wittchen HU, Stalla GK. High prevalence of biochemical acromegaly in primary care patients with elevated IGF-1 levels. Clin Endocrinol (Oxf) 2008; 69: 432-5.
38. Melmed S, Colao A, Barkan A, et al. Guidelines for acromegaly management: an update. J Clin Endocrinol Metab 2009; 94: 1509-17.
39. Colao A, Martino E, Cappabianca P, Cozzi R, Scanarini M, Ghigo E. First-line therapy of acromegaly: a statement of the A.L.I.C.E. (Acromegaly primary medical treatment Learning and Improvement with Continuous Medical Education) Study Group. J Endocrinol Invest 2006; 29: 1017-20.
40. Schmid HA, Silva AP. Short-and long-term effects of octreotide and SOM230 on GH, IGF-I, ACTH, corticosterone and ghrelin in rats. J Endocrinol Invest 2005; 28(11 Suppl): 28-35.
41. Weckbecker G, Briner U, Lewis I, Bruns C. SOM230: a new somatostatin peptidomimetic with potent inhibitory effects on the growth hormone/insulin-like growth factor-I axis in rats, primates, and dogs. Endocrinology 2002; 143: 4123-30.
42. Schmid HA, Brueggen J, Guitard P. Effects of a long-acting release formulation of pasireotide (SOM230) on hormone secretion in rats. Presented at ENDO 2007; abst P3-337.
43. Schmid HA. Pasireotide (SOM230): Development, mechanism of action and potential applications. Mol Cell Endocrinol 2008; 286: 69-74.
44. Van Der Hoek J, de Herder WW, Feelders RA, et al. A single-dose comparison of the acute effects between the new somatostatin analog SOM230 and octreotide in acromegalic patients. J Clin Endocrinol Metab 2004; 89: 638-45.
45. Van Der Hoek J, van der Lelij AJ, Feelders RA, et al. The somatostatin analogue SOM230, compared with octreotide, induces differential effects in several metabolic pathways in acromegalic patients. Clin Endocrinol (Oxf) 2005; 63: 176-84.
46. Petersenn S, Schopohl J, Barkan A, et al. Pasireotide (SOM230) demonstrates efficacy and safety in patients with acromegaly: a randomized, multicenter, Phase II trial. J Clin Endocrinol Metab 2010; 95: 2781-9.
47. Farrall A, Ruffin M, Wetli-Hermosillo K, Petersenn S. Long-term treatment of acromegaly with pasireotide (SOM230): results from a Phase II extension study. Endocr Rev 2010; 31 (Suppl. 1): S856 (OR16-5).
48. Murray RD, Kim K, Ren SG, et al. The novel somatostatin ligand (SOM230) regulates human and rat anterior pituitary hormone secretion. J Clin Endocrinol Metab 2004; 89: 3027-32.
49. Shomali ME, Katznelson L. Medical therapy of gonadotropin-producing and nonfunctioning pituitary adenomas. Pituitary 2002; 5: 89-98.
50. Hubina E, Nanzer AM, Hanson MR, et al. Somatostatin analogues stimulate p27 expression and inhibit the MAP kinase pathway in pituitary tumours. Eur J Endocrinol 2006; 155: 371-9.
51. Modlin IM, Oberg K, Chung DC, et al. Gastroenteropancreatic neuroendocrine tumours. Lancet Oncol 2008; 9: 61-72.
52. Oberg K. Neuroendocrine tumors of the gastrointestinal tract: recent advances in molecular genetics, diagnosis, and treatment. Curr Opin Oncol 2005; 17: 386-91.
53. Klöppel G, Perren A, Heitz PU. The gastroenteropancreatic neuroendocrine cell system and its tumors: the WHO classification. Ann N Y Acad Sci 2004; 1014: 13-27.
54. Yao JC, Hassan M, Phan A, et al. One hundred years after 'carcinoid': epidemiology of and prognostic factors for neuroendocrine tumors in 35,825 cases in the United States. J Clin Oncol 2008; 26: 3063-72.
55. de Herder WW, Hofland LJ, van der Lely AJ, Lamberts SW. Somatostatin receptors in gastroentero-pancreatic neuroendocrine tumours. Endocr Relat Cancer 2003; 10: 451-8.
56. Hofland LJ, Van Der Hoek J, Feelders R, van der Lely AJ, De Herder W, Lamberts SW. Pre-clinical and clinical experiences with novel somatostatin ligands: advantages, disadvantages and new prospects. J Endocrinol Invest 2005; 28(11 Suppl): 36-42.
57. Ferrante E, Pellegrini C, Bondioni S, et al. Octreotide promotes apoptosis in human somatotroph tumor cells by activating somatostatin receptor type 2. Endocr Relat Cancer 2006; 13: 955-62.
58. Asnacios A, Courbon F, Rochaix P, et al. Indium-111-pentetreotide scintigraphy and somatostatin receptor subtype 2 expression: new prognostic factors for malignant well-differentiated endocrine tumors. J Clin Oncol 2008; 26: 963-70.
59. Schmid HA, Silva AP, Van Vugt HH, Gadelha M. Pasireotide (SOM230): mechanism of action in acromegaly, Cushing's disease and GEP-NETs. Proceedings of the 13th International Congress of Endocrinology 2008; 2000-4.
60. Lesche S, Lehman D, Nagel F, Schmid HA, Schulz S. Differential effects of octreotide and pasireotide on somatostatin receptor internalization and trafficking in vitro. J Clin Endocrinol Metab 2009; 94: 654-61.
61. Kvols L, Wiedenmann B, Oberg K, et al. Safety and efficacy of pasireotide (SOM230) in patients with metastatic carcinoid tumors refractory or resistant to octreotide LAR: Results of a phase II study. ASCO GI Cancers Symposium 2006; abst 171.
62. Reubi JC, Kappeler A, Waser B, Schonbrunn A, Laissue J. Immunohistochemical localization of somatostatin receptor sst2A in human pancreatic islets. J Clin Endocrinol Metab 1998; 83: 3746-9.
63. Oberg K. Somatostatin analog octreotide LAR in gastro-enteropancreatic tumors. Expert Rev Anticancer Ther 2009; 9: 557-66.
64. Song S, Shi R, Li B, Liu Y. Diagnosis and treatment of pancreatic vasoactive intestinal peptide endocrine tumors. Pancreas 2009; 38: 811-4.
65. Stephen AE, Hodin RA. Neuroendocrine tumors of the pancreas, excluding gastrinoma. Surg Oncol Clin N Am 2006; 15: 497-510.
66. Panzuto F, Di Fonzo M, Iannicelli E, et al. Long-term clinical outcome of somatostatin analogues for treatment of progressive, metastatic, well-differentiated entero-pancreatic endocrine carcinoma. Ann Oncol 2006; 17: 461-6.
67. Werner H, Bruchim I. The insulin-like growth factor-I receptor as an oncogene. Arch Physiol Biochem 2009; 115: 58-71.
68. Allen NE, Roddam AW, Allen DS, et al. A prospective study of serum insulin-like growth factor-I (IGF-I), IGF-II, IGF-binding protein-3 and breast cancer risk. Br J Cancer 2005; 92: 1283-7.
69. Stattin P, Bylund A, Rinaldi S, et al. Plasma insulin-like growth factor-I, insulin-like growth factor-binding proteins, and prostate cancer risk: a prospective study. J Natl Cancer Inst 2000; 92: 1910-7.
70. Palmqvist R, Hallmans G, Rinaldi S, et al. Plasma insulin-like growth factor 1, insulin-like growth factor binding protein 3, and risk of colorectal cancer: a prospective study in northern Sweden. Gut 2002; 50: 642-6.
71. Petridou E, Koukoulomatis P, Alexe DM, Voulgaris Z, Spanos E, Trichopoulos D. Endometrial cancer and the IGF system: a casecontrol study in Greece. Oncology 2003; 64: 341-5.
72. Zhao H, Grossman HB, Spitz MR, Lerner SP, Zhang K, Wu X. Plasma levels of insulin-like growth factor-1 and binding protein-3, and their association with bladder cancer risk. J Urol 2003; 169: 714-7.
73. Erten C, Karaca B, Kucukzeybek Y, et al. Regulation of growth factors in hormone-and drug-resistant prostate cancer cells by synergistic combination of docetaxel and octreotide. BJU Int 2009; 104: 107-14.
74. Lo Nigro C, Maffi M, Fischel JL, Formento P, Milano G, Merlano M. The combination of docetaxel and the somatostatin analogue lanreotide on androgen-independent docetaxel-resistant prostate cancer: experimental data. BJU Int 2008; 102: 622-7.
75. Lo Nigro C, Lattanzio L, Monteverde M, et al. Octreotide and SOM230: partners of docetaxel in androgen-independent prostate cancer therapy. ASCO GU Cancers Symposium 2008; abst 230.
76. Schmid HA, Lambertini C, Nuciforo P. Antitumor activity of pasireotide (SOM230) alone and in combination with everolimus (RAD001) in DU-145 human prostate cancer model. Endocr Rev 2010; 31 (Suppl. 1): S909 (P2-39).
77. Koutsilieris M, Mitsiades CS, Bogdanos J, et al. Combination of somatostatin analog, dexamethasone, and standard androgen ablation therapy in stage D3 prostate cancer patients with bone metastases. Clin Cancer Res 2004; 10: 4398-405.
78. Prevost G, Foehrle E, Thomas F, et al. Growth of human breast cancer cell lines is inhibited by the somatostatin analog BIM23014. Endocrinology 1991; 129: 323-9.
79. Pagliacci MC, Tognellini R, Grignani F, Nicoletti I. Inhibition of human breast cancer cell (MCF-7) growth in vitro by the somatostatin analog SMS 201-995: effects on cell cycle parameters and apoptotic cell death. Endocrinology 1991; 129: 2555-62.
80. Weckbecker G, Liu R, Tolcsvai L, Bruns C. Antiproliferative effects of the somatostatin analogue octreotide (SMS 201-995) on ZR-75-1 human breast cancer cells in vivo and in vitro. Cancer Res 1992; 52: 4973-8.
81. Weber C, Merriam L, Koschitzky T, et al. Inhibition of growth of human breast carcinomas in vivo by somatostatin analog SMS 201-995: treatment of nude mouse xenografts. Surgery 1989; 106: 416-22.
82. Ruan W, Fahlbusch F, Clemmons DR, et al. SOM230 inhibits IGFI action in mammary gland development by pituitary independent mechanism: mediated through somatostatin subtype receptor 3? Mol Endocrinol 2006; 20: 426-36.
83. Canobbio L, Cannata D, Miglietta L, Boccardo F. Somatuline (BIM 23014) and tamoxifen treatment of postmenopausal breast cancer patients: clinical activity and effect on insulin-like growth factor-I (IGF-I) levels. Anticancer Res 1995; 15: 2687-90.
84. Helle SI, Mietlowski W, Guastalla JP, et al. Effects of tamoxifen and octreotide LAR on the IGF-system compared with tamoxifen monotherapy. Eur J Cancer 2005; 41: 694-701.