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Expert Review of Endocrinology & Metabolism Volume 7, 2012 - Issue 5
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Drug Profile

Pasireotide (SOM230): a novel pituitary-targeted medical therapy for the treatment of patients with Cushing’s disease

Kelley J Moloney Seattle Pituitary Center, Swedish Neuroscience Institute, Seattle, WA, USA; Seattle Pituitary Center, Swedish Neuroscience Institute, Seattle, WA, USA. [email protected]
,
Jennifer U Mercado Seattle Pituitary Center, Swedish Neuroscience Institute, Seattle, WA, USA; Seattle Pituitary Center, Swedish Neuroscience Institute, Seattle, WA, USA
,
William H Ludlam Novartis Pharmaceuticals Corporation, East Hanover, NJ, USA; Novartis Pharmaceuticals Corporation, East Hanover, NJ, USA
&
Marc R Mayberg Seattle Pituitary Center, Swedish Neuroscience Institute, Seattle, WA, USA; Seattle Pituitary Center, Swedish Neuroscience Institute, Seattle, WA, USA
Pages 491-502 | Published online: 10 Jan 2014

References

  • Newell-Price J, Bertagna X, Grossman AB, Nieman LK. Cushing’s syndrome. Lancet 367(9522), 1605–1617 (2006).
  • Bolland MJ, Holdaway IM, Berkeley JE et al. Mortality and morbidity in Cushing’s syndrome in New Zealand. Clin. Endocrinol. (Oxf.) 75(4), 436–442 (2011).
  • Etxabe J, Vazquez JA. Morbidity and mortality in Cushing’s disease: an epidemiological approach. Clin. Endocrinol. (Oxf.) 40(4), 479–484 (1994).
  • Lindholm J, Juul S, Jørgensen JO et al. Incidence and late prognosis of Cushing’s syndrome: a population-based study. J. Clin. Endocrinol. Metab. 86(1), 117–123 (2001).
  • Dekkers OM, Biermasz NR, Pereira AM et al. Mortality in patients treated for Cushing’s disease is increased, compared with patients treated for nonfunctioning pituitary macroadenoma. J. Clin. Endocrinol. Metab. 92(3), 976–981 (2007).
  • Ambrosi B, Faglia G; Multicenter Pituitary Tumor Study Group LR. Epidemiology of pituitary tumors. In: Pituitary Adenomas: New Trends In Basic And Clinical Research. Faglia G, Beck-Peccoz P, Ambrosi B, Travaglini P, Spada A, (Eds). Excerpta Medica, Amsterdam, The Netherlands 159–168 (1991).
  • Arnardóttir S, Sigurjonsdóttir HA. The incidence and prevalence of Cushing’s disease may be higher than previously thought: results from a retrospective study in Iceland 1955 through 2009. Clin. Endocrinol. (Oxf.) 74(6), 792–793 (2011).
  • Anderson GH Jr, Blakeman N, Streeten DH. The effect of age on prevalence of secondary forms of hypertension in 4429 consecutively referred patients. J. Hypertens. 12(5), 609–615 (1994).
  • Catargi B, Rigalleau V, Poussin A et al. Occult Cushing’s syndrome in Type-2 diabetes. J. Clin. Endocrinol. Metab. 88(12), 5808–5813 (2003).
  • Chiodini I, Torlontano M, Scillitani A et al. Association of subclinical hypercortisolism with Type 2 diabetes mellitus: a case–control study in hospitalized patients. Eur. J. Endocrinol. 153(6), 837–844 (2005).
  • Chiodini I, Mascia ML, Muscarella S et al. Subclinical hypercortisolism among outpatients referred for osteoporosis. Ann. Intern. Med. 147(8), 541–548 (2007).
  • Nieman LK, Biller BM, Findling JW et al. The diagnosis of Cushing’s syndrome: an Endocrine Society Clinical Practice Guideline. J. Clin. Endocrinol. Metab. 93(5), 1526–1540 (2008).
  • Boscaro M, Barzon L, Fallo F, Sonino N. Cushing’s syndrome. Lancet 357(9258), 783–791 (2001).
  • Biller BM, Grossman AB, Stewart PM et al. Treatment of adrenocorticotropin-dependent Cushing’s syndrome: a consensus statement. J. Clin. Endocrinol. Metab. 93(7), 2454–2462 (2008).
  • Atkinson AB, Kennedy A, Wiggam MI, McCance DR, Sheridan B. Long-term remission rates after pituitary surgery for Cushing’s disease: the need for long-term surveillance. Clin. Endocrinol. (Oxf.) 63(5), 549–559 (2005).
  • Fleseriu M, Loriaux DL, Ludlam WH. Second-line treatment for Cushing’s disease when initial pituitary surgery is unsuccessful. Curr. Opin. Endocrinol. Diabetes. Obes. 14(4), 323–328 (2007).
  • Rizk A, Honegger J, Milian M, Psaras T. Treatment options in Cushing’s disease. Clin. Med. Insights. Oncol. 6, 75–84 (2012).
  • Lamberts SW, Bons EG, Bruining HA, de Jong FH. Differential effects of the imidazole derivatives etomidate, ketoconazole and miconazole and of metyrapone on the secretion of cortisol and its precursors by human adrenocortical cells. J. Pharmacol. Exp. Ther. 240(1), 259–264 (1987).
  • Castinetti F, Morange I, Jaquet P, Conte-Devolx B, Brue T. Ketoconazole revisited: a preoperative or postoperative treatment in Cushing’s disease. Eur. J. Endocrinol. 158(1), 91–99 (2008).
  • Fleseriu M, Biller BM, Findling JW, Molitch ME, Schteingart DE, Gross C; on behalf of the SEISMIC Study Investigators; The SEISMIC Study Investigators include. Mifepristone, a glucocorticoid receptor antagonist, produces clinical and metabolic benefits in patients with Cushing’s syndrome. J. Clin. Endocrinol. Metab. 97(6), 2039–2049 (2012).
  • Castinetti F, Conte-Devolx B, Brue T. Medical treatment of Cushing’s syndrome: glucocorticoid receptor antagonists and mifepristone. Neuroendocrinology 92(Suppl. 1), 125–130 (2010).
  • Castinetti F, Fassnacht M, Johanssen S et al. Merits and pitfalls of mifepristone in Cushing’s syndrome. Eur. J. Endocrinol. 160(6), 1003–1010 (2009).
  • Heaney AP, Fernando M, Yong WH, Melmed S. Functional PPAR-γ receptor is a novel therapeutic target for ACTH-secreting pituitary adenomas. Nat. Med. 8(11), 1281–1287 (2002).
  • Ambrosi B, Dall’Asta C, Cannavo S et al. Effects of chronic administration of PPAR-γ ligand rosiglitazone in Cushing’s disease. Eur. J. Endocrinol. 151(2), 173–178 (2004).
  • Morcos M, Fohr B, Tafel J et al. Long-term treatment of central Cushing’s syndrome with rosiglitazone. Exp. Clin. Endocrinol. Diabetes 115(5), 292–297 (2007).
  • Catrina SB, Virtanen K, Hällsten K, Lönnqvist F, Nuutila P, Brismar K. Effect of rosiglitazone on early-morning plasma cortisol levels. Neuro. Endocrinol. Lett. 26(6), 763–4; author reply 765 (2005).
  • Kreutzer J, Jeske I, Hofmann B et al. No effect of the PPAR-γ agonist rosiglitazone on ACTH or cortisol secretion in Nelson’s syndrome and Cushing’s disease in vitro and in vivo. Clin. Neuropathol. 28(6), 430–439 (2009).
  • Cannavò S, Ambrosi B, Chiodini I et al. Baseline and CRH-stimulated ACTH and cortisol levels after administration of the peroxisome proliferator-activated receptor-γ ligand, rosiglitazone, in Cushing’s disease. J. Endocrinol. Invest. 27(5), RC8–R11 (2004).
  • Suri D, Weiss RE. Effect of pioglitazone on adrenocorticotropic hormone and cortisol secretion in Cushing’s disease. J. Clin. Endocrinol. Metab. 90(3), 1340–1346 (2005).
  • Miller JW, Crapo L. The medical treatment of Cushing’s syndrome. Endocr. Rev. 14(4), 443–458 (1993).
  • Pivonello R, Ferone D, de Herder WW et al. Dopamine receptor expression and function in corticotroph pituitary tumors. J. Clin. Endocrinol. Metab. 89(5), 2452–2462 (2004).
  • Pivonello R, De Martino MC, Cappabianca P et al. The medical treatment of Cushing’s disease: effectiveness of chronic treatment with the dopamine agonist cabergoline in patients unsuccessfully treated by surgery. J. Clin. Endocrinol. Metab. 94(1), 223–230 (2009).
  • Vilar L, Naves LA, Azevedo MF et al. Effectiveness of cabergoline in monotherapy and combined with ketoconazole in the management of Cushing’s disease. Pituitary 13(2), 123–129 (2010).
  • Godbout A, Manavela M, Danilowicz K, Beauregard H, Bruno OD, Lacroix A. Cabergoline monotherapy in the long-term treatment of Cushing’s disease. Eur. J. Endocrinol. 163(5), 709–716 (2010).
  • Lila AR, Gopal RA, Acharya SV et al. Efficacy of cabergoline in uncured (persistent or recurrent) Cushing disease after pituitary surgical treatment with or without radiotherapy. Endocr. Pract. 16(6), 968–976 (2010).
  • Manavela MP, Danilowicz K, Bruno OD. Macrocorticotropinoma shrinkage and control of hypercortisolism under long-term cabergoline therapy: case report. Pituitary doi:10.1007/s11102-011-0309-0 (2011) (Epub ahead of print).
  • 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. 91(11), 4482–4488 (2006).
  • Hofland LJ, van der Hoek J, Feelders R et al. The multiligand somatostatin analogue SOM230 inhibits ACTH secretion by cultured human corticotroph adenomas via somatostatin receptor type 5. Eur. J. Endocrinol. 152(4), 645–654 (2005).
  • Fehm HL, Voigt KH, Lang R, Beinert KE, Raptis S, Pfeiffer EF. Somatostatin: a potent inhibitor of ACTH hypersecretion in adrenal insufficiency. Klin. Wochenschr. 54(4), 173–175 (1976).
  • Lamberts SW, Uitterlinden P, Klijn JM. The effect of the long-acting somatostatin analogue SMS 201-995 on ACTH secretion in Nelson’s syndrome and Cushing’s disease. Acta Endocrinol. 120(6), 760–766 (1989).
  • Tyrrell JB, Lorenzi M, Gerich JE, Forsham PH. Inhibition by somatostatin of ACTH secretion in Nelson’s syndrome. J. Clin. Endocrinol. Metab. 40(6), 1125–1127 (1975).
  • Ambrosi B, Bochicchio D, Fadin C, Colombo P, Faglia G. Failure of somatostatin and octreotide to acutely affect the hypothalamic-pituitary-adrenal function in patients with corticotropin hypersecretion. J. Endocrinol. Invest. 13(3), 257–261 (1990).
  • Petersenn S, Rasch AC, Presch S, Beil FU, Schulte HM. Genomic structure and transcriptional regulation of the human somatostatin receptor type 2. Mol. Cell. Endocrinol. 157(1-2), 75–85 (1999).
  • 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 tumor cells. Am. J. Physiol. Endocrinol. Metab. 289(2), E278–E287 (2005).
  • 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 143(10), 4123–4130 (2002).
  • Schmid HA. Pasireotide (SOM230): development, mechanism of action and potential applications. Mol. Cell. Endocrinol. 286(1-2), 69–74 (2008).
  • Hofland LJ. Somatostatin and somatostatin receptors in Cushing’s disease. Mol. Cell. Endocrinol. 286(1-2), 199–205 (2008).
  • Ma P, Wang Y, van der Hoek J et al. Pharmacokinetic-pharmacodynamic comparison of a novel multiligand somatostatin analog, SOM230, with octreotide in patients with acromegaly. Clin. Pharmacol. Ther. 78(1), 69–80 (2005).
  • Petersenn S, Unger N, Hu K et al. Pasireotide (SOM230), a novel multireceptor-targeted somatostatin analogue, is well tolerated when administered as a continuous 7-day subcutaneous infusion in healthy male volunteers. J. Clin. Pharmacol. 52(7), 1017–1027 (2012).
  • Boscaro M, Ludlam WH, Atkinson B et al. Treatment of pituitary-dependent Cushing’s disease with the multireceptor ligand somatostatin analog pasireotide (SOM230): a multicenter, Phase II trial. J. Clin. Endocrinol. Metab. 94(1), 115–122 (2009).
  • Boscaro M, Zhang Y, Sen K et al. Long-term treatment of Cushing’s disease with pasireotide (SOM230): results from a Phase II extension study. Endocr. Rev. 31 (3 Suppl. 1), S333 (Abstract P1–274) (2010).
  • Colao A, Petersenn S, Newell-Price J et al. Pasireotide B2305 Study Group. A 12-month Phase 3 study of pasireotide in Cushing’s disease. N. Engl. J. Med. 366(10), 914–924 (2012).
  • Feelders RA, de Bruin C, Pereira AM et al. Pasireotide alone or with cabergoline and ketoconazole in Cushing’s disease. N. Engl. J. Med. 362(19), 1846–1848 (2010).
  • Ben-Shlomo A, Melmed S. Somatostatin agonists for treatment of acromegaly. Mol. Cell. Endocrinol. 286(1-2), 192–198 (2008).
  • Mazziotti G, Floriani I, Bonadonna S, Torri V, Chanson P, Giustina A. Effects of somatostatin analogs on glucose homeostasis: a meta-analysis of acromegaly studies. J. Clin. Endocrinol. Metab. 94(5), 1500–1508 (2009).
  • Patil CG, Prevedello DM, Lad SP et al. Late recurrences of Cushing’s disease after initial successful trans-sphenoidal surgery. J. Clin. Endocrinol. Metab. 93(2), 358–362 (2008).

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