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  Pasireotide

Description of pasireotide: Pasireotide is a synthetic long-acting cyclic peptide with somatostatin-like activity. Pasireotide activates a broad spectrum of somatostatin receptors, exhibiting a much higher binding affinity for somatostatin receptors 1, 3, and 5 than octreotide in vitro, as well as a comparable binding affinity for somatostatin receptor 2. This agent is more potent than somatostatin in inhibiting the release of human growth hormone (HGH), glucagon, and insulin. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:    Novartis

Pasireotide (SOM230) is an orphan drug currently in phase III studies for the treatment of Cushing's disease. It was developed by Novartis. Pasireotide is a somatostatin analog which has a 40-fold increased affinity to somatostatin receptor 5 than other somatostatin analogs. The drug showed therapeutical potential in a recent study (PASPORT-CUSHINGS B2305) where 162 patients were treated with either 2x 600 µg or 2x 900 µg pasireotide s.c. daily. The effectiveness of the treatment was checked by the UFC-value (urinary free cortisol) after six months of treatment. The mean reduction of UFC after six months was 47.9%, which also lead to amelioration of clinical symptoms such as blood pressure, cholesterol value, and weight loss. (source: http://en.wikipedia.org/wiki/Pasireotide).

1: Petersenn S, Unger N, Hu K, Weisshaar B, Zhang Y, Bouillaud E, Hermosillo Reséndiz K, Wang Y, Mann K. Pasireotide (SOM230), a Novel Multi-Receptor-Targeted Somatostatin Analogue, Is Well Tolerated When Administered as a Continuous 7-Day Subcutaneous Infusion in Healthy Male Volunteers. J Clin Pharmacol. 2011 Jun 14. [Epub ahead of print] PubMed PMID: 21673137.

2: Castillo V, Theodoropoulou M, Stalla J, Gallelli MF, Cabrera-Blatter MF, Haedo MR, Labeur M, Schmid HA, Stalla GK, Arzt E. Effect of SOM230 (pasireotide) on corticotropic cells: action in dogs with Cushing's disease. Neuroendocrinology. 2011;94(2):124-36. Epub 2011 Apr 28. PubMed PMID: 21525729.

3: Imhof AK, Glück L, Gajda M, Lupp A, Bräuer R, Schaible HG, Schulz S. Differential antiinflammatory and antinociceptive effects of the somatostatin analogs octreotide and pasireotide in a mouse model of immune-mediated arthritis. Arthritis Rheum. 2011 Aug;63(8):2352-62. doi: 10.1002/art.30410. PubMed PMID: 21506098.

4: Preumont V, Mermejo LM, Damoiseaux P, Lacroix A, Maiter D. Transient efficacy of octreotide and pasireotide (SOM230) treatment in GIP-dependent Cushing's syndrome. Horm Metab Res. 2011 Apr;43(4):287-91. Epub 2011 Jan 24. PubMed PMID: 21264796.

5: Kleinberg DL, Ameri P, Singh B. Pasireotide, an IGF-I action inhibitor, prevents growth hormone and estradiol-induced mammary hyperplasia. Pituitary. 2011 Mar;14(1):44-52. PubMed PMID: 20890664.

6: Pedroncelli AM. Medical treatment of Cushing's disease: somatostatin analogues and pasireotide. Neuroendocrinology. 2010;92 Suppl 1:120-4. Epub 2010 Sep 10. Review. PubMed PMID: 20829632.

7: Wilson C. Pharmacotherapy: Pasireotide shows promise for the treatment of acromegaly. Nat Rev Endocrinol. 2010 Aug;6(8):417. PubMed PMID: 20681073.

8: Arnaldi G, Boscaro M. Pasireotide for the treatment of Cushing's disease. Expert Opin Investig Drugs. 2010 Jul;19(7):889-98. Review. PubMed PMID: 20533892.

9: Bode H, Seiz M, Lammert A, Brockmann MA, Back W, Hammes HP, Thomé C. SOM230 (pasireotide) and temozolomide achieve sustained control of tumour progression and ACTH secretion in pituitary carcinoma with widespread metastases. Exp Clin Endocrinol Diabetes. 2010 Nov;118(10):760-3. Epub 2010 May 21. PubMed PMID: 20496311.

10: Feelders RA, de Bruin C, Pereira AM, Romijn JA, Netea-Maier RT, Hermus AR, Zelissen PM, van Heerebeek R, de Jong FH, van der Lely AJ, de Herder WW, Hofland LJ, Lamberts SW. Pasireotide alone or with cabergoline and ketoconazole in Cushing's disease. N Engl J Med. 2010 May 13;362(19):1846-8. PubMed PMID: 20463350.

11: Petersenn S, Schopohl J, Barkan A, Mohideen P, Colao A, Abs R, Buchelt A, Ho YY, Hu K, Farrall AJ, Melmed S, Biller BM; Pasireotide Acromegaly Study Group. Pasireotide (SOM230) demonstrates efficacy and safety in patients with acromegaly: a randomized, multicenter, phase II trial. J Clin Endocrinol Metab. 2010 Jun;95(6):2781-9. Epub 2010 Apr 21. PubMed PMID: 20410233.

12: Pöll F, Lehmann D, Illing S, Ginj M, Jacobs S, Lupp A, Stumm R, Schulz S. Pasireotide and octreotide stimulate distinct patterns of sst2A somatostatin receptor phosphorylation. Mol Endocrinol. 2010 Feb;24(2):436-46. Epub 2010 Jan 5. PubMed PMID: 20051480.

13: Fu Q, Berbée M, Boerma M, Wang J, Schmid HA, Hauer-Jensen M. The somatostatin analog SOM230 (pasireotide) ameliorates injury of the intestinal mucosa and increases survival after total-body irradiation by inhibiting exocrine pancreatic secretion. Radiat Res. 2009 Jun;171(6):698-707. PubMed PMID: 19580476; PubMed Central PMCID: PMC2742953.

14: 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 Aug;71(2):305-7. Epub 2008 Dec 3. PubMed PMID: 19067723.

15: Lesche S, Lehmann 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 Feb;94(2):654-61. Epub 2008 Nov 11. PubMed PMID: 19001514.

16: Boscaro M, Ludlam WH, Atkinson B, Glusman JE, Petersenn S, Reincke M, Snyder P, Tabarin A, Biller BM, Findling J, Melmed S, Darby CH, Hu K, Wang Y, Freda PU, Grossman AB, Frohman LA, Bertherat J. Treatment of pituitary-dependent Cushing's disease with the multireceptor ligand somatostatin analog pasireotide (SOM230): a multicenter, phase II trial. J Clin Endocrinol Metab. 2009 Jan;94(1):115-22. Epub 2008 Oct 28. PubMed PMID: 18957506.

17: Schmid HA. Preclinical evidences suggest new treatment options for endocrine disorders: Pasireotide (SOM230) and Everolimus (RAD001). Ann Endocrinol (Paris). 2008 Apr;69(2):162-3. Epub 2008 Apr 15. PubMed PMID: 18417094.

18: Ben-Shlomo A, Melmed S. Pasireotide--a somatostatin analog for the potential treatment of acromegaly, neuroendocrine tumors and Cushing's disease. IDrugs. 2007 Dec;10(12):885-95. PubMed PMID: 18041687.

19: Schmid HA. Pasireotide (SOM230): development, mechanism of action and potential applications. Mol Cell Endocrinol. 2008 May 14;286(1-2):69-74. Epub 2007 Sep 19. Review. PubMed PMID: 17977644.

20: Zatelli MC, Piccin D, Vignali C, Tagliati F, Ambrosio MR, Bondanelli M, Cimino V, Bianchi A, Schmid HA, Scanarini M, Pontecorvi A, De Marinis L, Maira G, degli Uberti EC. Pasireotide, a multiple somatostatin receptor subtypes ligand, reduces cell viability in non-functioning pituitary adenomas by inhibiting vascular endothelial growth factor secretion. Endocr Relat Cancer. 2007 Mar;14(1):91-102. PubMed PMID: 17395978.

21: Nolan LA, Schmid HA, Levy A. Octreotide and the novel multireceptor ligand somatostatin receptor agonist pasireotide (SOM230) block the adrenalectomy-induced increase in mitotic activity in male rat anterior pituitary. Endocrinology. 2007 Jun;148(6):2821-7. Epub 2007 Mar 8. PubMed PMID: 17347306.

22: Lattuada D, Casnici C, Crotta K, Mastrotto C, Franco P, Schmid HA, Marelli O. Inhibitory effect of pasireotide and octreotide on lymphocyte activation. J Neuroimmunol. 2007 Jan;182(1-2):153-9. Epub 2006 Nov 20. PubMed PMID: 17113654.