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Review

Emerging drugs for acromegaly

Pages 273-293 | Published online: 08 Jun 2008

Bibliography

  • Smith RG, Van der Ploeg LH, Howard AD, et al. Peptidomimetic regulation of growth hormone secretion. Endocr Rev 1997;18:621-45
  • Giustina A, Veldhuis JD. Pathophysiology of the neuroregulation of growth hormone secretion in experimental animals and the human. Endocr Rev 1998;19:717-97
  • Kelly PA, Djiane J, Postel-Vinay MC, Edery M. The prolactin/growth hormone receptor family. Endocr Rev 1991;12:235-51
  • Argetsinger LS, Campbell GS, Yang X, et al. Identification of JAK2 as a growth hormone receptor-associated tyrosine kinase. Cell 1993;74:237-44
  • Le Roith D, Bondy C, Yakar S, et al. The somatomedin hypothesis: 2001. Endocr Rev 2001;22:53-74
  • Hwa V, Oh Y, Rosenfeld RG. The insulin-like growth factor-binding protein (IGFBP) superfamily. Endocr Rev 1999;20:761-87
  • Clemmons DR. Value of insulin-like growth factor system markers in the assessment of growth hormone status. Endocrinol Metab Clin North Am 2007;36:109-29
  • Melmed S. Medical progress: acromegaly. N Engl J Med 2006;355:2558-73
  • Holdaway IM, Rajasoorya C. Epidemiology of acromegaly. Pituitary 1999;2:29-41
  • Daly AF, Rixhon M, Adam C, et al. High prevalence of pituitary adenomas: a cross-sectional study in the province of Liege, Belgium. J Clin Endocrinol Metab 2006;91:4769-75
  • Nabarro JD. Acromegaly. Clin Endocrinol (Oxf) 1987;26:481-512
  • Ezzat S, Forster MJ, Berchtold P, et al. Acromegaly. Clinical and biochemical features in 500 patients. Medicine (Baltimore) 1994;73:233-40
  • Melmed S. Acromegaly. In: Melmed S, editor, The pituitary. 2nd edition. Malden, MA: Blackwell Science, Inc.; 2002. p. 419-54
  • Colao A, Ferone D, Marzullo P, Lombardi G. Systemic complications of acromegaly: epidemiology, pathogenesis, and management. Endocr Rev 2004;25:102-52
  • Swearingen B, Barker FGN, Katznelson L, et al. Long-term mortality after transsphenoidal surgery and adjunctive therapy for acromegaly. J Clin Endocrinol Metab 1998;83:3419-26
  • Abosch A, Tyrrell JB, Lamborn KR, et al. Transsphenoidal microsurgery for growth hormone-secreting pituitary adenomas: initial outcome and long-term results. J Clin Endocrinol Metab 1998;83:3411-8
  • Bates AS, Van't Hoff W, Jones JM, Clayton RN. An audit of outcome of treatment in acromegaly. Q J Med 1993;86:293-9
  • Rajasoorya C, Holdaway IM, Wrightson P, et al. Determinants of clinical outcome and survival in acromegaly. Clin Endocrinol (Oxf) 1994;41:95-102
  • Orme SM, McNally RJ, Cartwright RA, Belchetz PE. Mortality and cancer incidence in acromegaly: a retrospective cohort study. United Kingdom Acromegaly Study Group. J Clin Endocrinol Metab 1998;83:2730-4
  • Holdaway IM, Rajasoorya RC, Gamble GD. Factors influencing mortality in acromegaly. J Clin Endocrinol Metab 2004;89:667-74
  • Ayuk J, Clayton RN, Holder G, et al. Growth hormone and pituitary radiotherapy, but not serum insulin-like growth factor-I concentrations, predict excess mortality in patients with acromegaly. J Clin Endocrinol Metab 2004;89:1613-7
  • Biermasz NR, Dekker FW, Pereira AM, et al. Determinants of survival in treated acromegaly in a single center: predictive value of serial insulin-like growth factor I measurements. J Clin Endocrinol Metab 2004;89:2789-96
  • Kauppinen-Makelin R, Sane T, Reunanen A, et al. A nationwide survey of mortality in acromegaly. J Clin Endocrinol Metab 2005;90:4081-6
  • Beauregard C, Truong U, Hardy J, Serri O. Long-term outcome and mortality after transsphenoidal adenomectomy for acromegaly. Clin Endocrinol (Oxf) 2003;58:86-91
  • Dekkers OM, Biermasz NR, Pereira AM, et al. Mortality in acromegaly: a meta-analysis. J Clin Endocrinol Metab 2008;93:61-7
  • Biermasz NR, van Thiel SW, Pereira AM, et al. Decreased quality of life in patients with acromegaly despite long-term cure of growth hormone excess. J Clin Endocrinol Metab 2004;89:5369-76
  • Melmed S, Casanueva FF, Cavagnini F, et al. Guidelines for acromegaly management. J Clin Endocrinol Metab 2002;87:4054-8
  • Giustina A, Barkan A, Casanueva FF, et al. Criteria for cure of acromegaly: a consensus statement. J Clin Endocrinol Metab 2000;85:526-9
  • Fahlbusch R, Buchfelder M, Nomikos P. Pituitary surgery. In: Melmed S, editor, The pituitary. 2nd edition. Malden, MA: Blackwell Science, Inc.; 2002. p. 405-18
  • Biermasz NR, van Dulken H, Roelfsema F. Ten-year follow-up results of transsphenoidal microsurgery in acromegaly. J Clin Endocrinol Metab 2000;85:4596-602
  • Barkan AL, Halasz I, Dornfeld KJ, et al. Pituitary irradiation is ineffective in normalizing plasma insulin-like growth factor I in patients with acromegaly. J Clin Endocrinol Metab 1997;82:3187-91
  • Barrande G, Pittino-Lungo M, Coste J, et al. Hormonal and metabolic effects of radiotherapy in acromegaly: long-term results in 128 patients followed in a single center. J Clin Endocrinol Metab 2000;85:3779-85
  • Biermasz NR, van Dulken H, Roelfsema F. Long-term follow-up results of postoperative radiotherapy in 36 patients with acromegaly. J Clin Endocrinol Metab 2000;85:2476-82
  • Brada M, Burchell L, Ashley S, Traish D. The incidence of cerebrovascular accidents in patients with pituitary adenoma. Int J Radiat Oncol Biol Phys 1999;45:693-8
  • Attanasio R, Epaminonda P, Motti E, et al. Gamma-knife radiosurgery in acromegaly: a 4-year follow-up study. J Clin Endocrinol Metab 2003;88:3105-12
  • Mahmoud-Ahmed AS, Suh JH, Mayberg MR. Gamma knife radiosurgery in the management of patients with acromegaly: a review. Pituitary 2001;4:223-30
  • Sheehan JP, Niranjan A, Sheehan JM, et al. Stereotactic radiosurgery for pituitary adenomas: an intermediate review of its safety, efficacy, and role in the neurosurgical treatment armamentarium. J Neurosurg 2005;102:678-91
  • Castinetti F, Taieb D, Kuhn JM, et al. Outcome of gamma knife radiosurgery in 82 patients with acromegaly: correlation with initial hypersecretion. J Clin Endocrinol Metab 2005;90:4483-8
  • Bauer W, Briner U, Doepfner W, et al. SMS 201-995: a very potent and selective octapeptide analogue of somatostatin with prolonged action. Life Sci 1982;31:1133-40
  • Chanson P, Timsit J, Harris AG. Clinical pharmacokinetics of octreotide. Therapeutic applications in patients with pituitary tumours. Clin Pharmacokinet 1993;25:375-91
  • Lamberts SW, van der Lely AJ, de Herder WW, Hofland LJ. Octreotide. N Engl J Med 1996;334:246-54
  • McKeage K, Cheer S, Wagstaff AJ. Octreotide long-acting release (LAR): a review of its use in the management of acromegaly. Drugs 2003;63:2473-99
  • Heron I, Thomas F, Dero M, et al. Pharmacokinetics and efficacy of a long-acting formulation of the new somatostatin analog BIM 23014 in patients with acromegaly. J Clin Endocrinol Metab 1993;76:721-7
  • Morange I, De Boisvilliers F, Chanson P, et al. Slow release lanreotide treatment in acromegalic patients previously normalized by octreotide. J Clin Endocrinol Metab 1994;79:145-51
  • Giusti M, Gussoni G, Cuttica CM, Giordano G. Effectiveness and tolerability of slow release lanreotide treatment in active acromegaly: six-month report on an Italian multicenter study. Italian Multicenter Slow Release Lanreotide Study Group. J Clin Endocrinol Metab 1996;81:2089-97
  • Caron P, Morange-Ramos I, Cogne M, Jaquet P. Three-year follow-up of acromegalic patients treated with intramuscular slow-release lanreotide. J Clin Endocrinol Metab 1997;82:18-22
  • Amato G, Mazziotti G, Rotondi M, et al. Long-term effects of lanreotide SR and octreotide LAR on tumour shrinkage and GH hypersecretion in patients with previously untreated acromegaly. Clin Endocrinol (Oxf) 2002;56:65-71
  • Chanson P, Boerlin V, Ajzenberg C, et al. Comparison of octreotide acetate LAR and lanreotide SR in patients with acromegaly. Clin Endocrinol (Oxf) 2000;53:577-86
  • Giusti M, Sessarego P, Timossi G, Bocca L. Slow-release lanreotide and octreotide LAR in the medical therapy of acromegaly. Eur J Endocrinol 2000;142:697-8
  • Caron P, Beckers A, Cullen DR, et al. Efficacy of the new long-acting formulation of lanreotide (lanreotide Autogel) in the management of acromegaly. J Clin Endocrinol Metab 2002;87:99-104
  • Caron P, Bex M, Cullen DR, et al. One-year follow-up of patients with acromegaly treated with fixed or titrated doses of lanreotide Autogel. Clin Endocrinol (Oxf) 2004;60:734-40
  • Muller AF, Kopchick JJ, Flyvbjerg A, van der Lely AJ. Clinical review 166: growth hormone receptor antagonists. J Clin Endocrinol Metab 2004;89:1503-11
  • Trainer PJ, Drake WM, Katznelson L, et al. Treatment of acromegaly with the growth hormone-receptor antagonist pegvisomant. N Engl J Med 2000;342:1171-7
  • van der Lely AJ, Hutson RK, Trainer PJ, et al. Long-term treatment of acromegaly with pegvisomant, a growth hormone receptor antagonist. Lancet 2001;358:1754-9
  • Biering H, Saller B, Bauditz J, et al. Elevated transaminases during medical treatment of acromegaly: a review of the German pegvisomant surveillance experience and a report of a patient with histologically proven chronic mild active hepatitis. Eur J Endocrinol 2006;154:213-20
  • Maffei P, Martini C, Pagano C, et al. Lipohypertrophy in acromegaly induced by the new growth hormone receptor antagonist pegvisomant. Ann Intern Med 2006;145:310-2
  • Jaffe CA, Barkan AL. Treatment of acromegaly with dopamine agonists. Endocrinol Metab Clin North Am 1992;21:713-35
  • Abs R, Verhelst J, Maiter D, et al. Cabergoline in the treatment of acromegaly: a study in 64 patients. J Clin Endocrinol Metab 1998;83:374-8
  • Zanettini R, Antonini A, Gatto G, et al. Valvular heart disease and the use of dopamine agonists for Parkinson's disease. N Engl J Med 2007;356:39-46
  • Schade R, Andersohn F, Suissa S, et al. Dopamine agonists and the risk of cardiac-valve regurgitation. N Engl J Med 2007;356:29-38
  • Sherlock M, Steeds R, Toogood AA. Dopamine agonist therapy and cardiac valve dysfunction. Clin Endocrinol (Oxf) 2007;67:643-4
  • Sassolas G, Harris AG, James-Deidier A. Long term effect of incremental doses of the somatostatin analog SMS 201-995 in 58 acromegalic patients. French SMS 201-995 – Acromegaly Study Group. J Clin Endocrinol Metab 1990;71:391-7
  • Vance ML, Harris AG. Long-term treatment of 189 acromegalic patients with the somatostatin analog octreotide. Results of the International Multicenter Acromegaly Study Group. Arch Intern Med 1991;151:1573-8
  • Ezzat S, Snyder PJ, Young WF, et al. Octreotide treatment of acromegaly. A randomized, multicenter study. Ann Intern Med 1992;117:711-8
  • Newman CB, Melmed S, Snyder PJ, et al. Safety and efficacy of long-term octreotide therapy of acromegaly: results of a multicenter trial in 103 patients: a clinical research center study. J Clin Endocrinol Metab 1995;80:2768-75. Erratum in: J Clin Endocrinol Metab 1995;80:3238
  • Melmed S, Ho K, Klibanski A, et al. Clinical review 75: recent advances in pathogenesis, diagnosis, and management of acromegaly. J Clin Endocrinol Metab 1995;80:3395-402
  • Arosio M, Macchelli S, Rossi CM, et al. Effects of treatment with octreotide in acromegalic patients: a multicenter Italian study. Italian Multicenter Octreotide Study Group. Eur J Endocrinol 1995;133:430-9
  • Newman CB, Melmed S, George A, et al. Octreotide as primary therapy for acromegaly. J Clin Endocrinol Metab 1998;83:3034-40
  • Ayuk J, Stewart SE, Stewart PM, Sheppard MC. Long-term safety and efficacy of depot long-acting somatostatin analogs for the treatment of acromegaly. J Clin Endocrinol Metab 2002;87:4142-6
  • Gillis JC, Noble S, Goa KL. Octreotide long-acting release (LAR). A review of its pharmacological properties and therapeutic use in the management of acromegaly. Drugs 1997;53:681-99
  • Fløgstad AK, Halse J, Bakke S, et al. Sandostatin LAR in acromegalic patients: long-term treatment. J Clin Endocrinol Metab 1997;82:23-8
  • Lancranjan I, Bruns C, Grass P, et al. Sandostatin LAR: a promising therapeutic tool in the management of acromegalic patients. Metabolism 1996;45:67-71
  • Stewart PM, Kane KF, Stewart SE, et al. Depot long-acting somatostatin analog (Sandostatin-LAR) is an effective treatment for acromegaly. J Clin Endocrinol Metab 1995;80:3267-72
  • Cozzi R, Attanasio R, Montini M, et al. Four-year treatment with octreotide-long-acting repeatable in 110 acromegalic patients: predictive value of short-term results? J Clin Endocrinol Metab 2003;88:3090-8
  • Bevan JS, Atkin SL, Atkinson AB, et al. Primary medical therapy for acromegaly: an open, prospective, multicenter study of the effects of subcutaneous and intramuscular slow- release octreotide on growth hormone, insulin-like growth factor-I, and tumor size. J Clin Endocrinol Metab 2002;87:4554-63
  • Freda PU, Katznelson L, van der Lely AJ, et al. Long-acting somatostatin analog therapy of acromegaly: a meta-analysis. J Clin Endocrinol Metab 2005;90:4465-73
  • Alexopoulou O, Abrams P, Verhelst J, et al. Efficacy and tolerability of lanreotide Autogel therapy in acromegalic patients previously treated with octreotide LAR. Eur J Endocrinol 2004;151:317-24
  • Ashwell SG, Bevan JS, Edwards OM, et al. The efficacy and safety of lanreotide Autogel in patients with acromegaly previously treated with octreotide LAR. Eur J Endocrinol 2004;150:473-80
  • van Thiel SW, Romijn JA, Biermasz NR, et al. Octreotide long-acting repeatable and lanreotide Autogel are equally effective in controlling growth hormone secretion in acromegalic patients. Eur J Endocrinol 2004;150:489-95
  • Andries M, Glintborg D, Kvistborg A, et al. A 12-month randomized crossover study on the effects of lanreotide Autogel and octreotide long-acting repeatable on GH and IGF-l in patients with acromegaly. Clin Endocrinol (Oxf) 2008;68:473-80
  • Sheppard MC. Primary medical therapy for acromegaly. Clin Endocrinol (Oxf) 2003;58:387-99
  • Colao A, Ferone D, Marzullo P, et al. Long-term effects of depot long-acting somatostatin analog octreotide on hormone levels and tumor mass in acromegaly. J Clin Endocrinol Metab 2001;86:2779-86
  • Attanasio R, Baldelli R, Pivonello R, et al. Lanreotide 60 mg, a new long-acting formulation: effectiveness in the chronic treatment of acromegaly. J Clin Endocrinol Metab 2003;88:5258-65
  • Bevan JS. Clinical review: the antitumoral effects of somatostatin analog therapy in acromegaly. J Clin Endocrinol Metab 2005;90:1856-63
  • Melmed S, Sternberg R, Cook D, et al. A critical analysis of pituitary tumor shrinkage during primary medical therapy in acromegaly. J Clin Endocrinol Metab 2005;90:4405-10
  • Lucas T, Astorga R, Catala M. Preoperative lanreotide treatment for GH-secreting pituitary adenomas: effect on tumour volume and predictive factors of significant tumour shrinkage. Clin Endocrinol (Oxf) 2003;58:471-81
  • Abe T, Ludecke DK. Effects of preoperative octreotide treatment on different subtypes of 90 GH-secreting pituitary adenomas and outcome in one surgical centre. Eur J Endocrinol 2001;145:137-45
  • Baldelli R, Colao A, Razzore P, et al. Two-year follow-up of acromegalic patients treated with slow release lanreotide (30 mg). J Clin Endocrinol Metab 2000;85:4099-103
  • Tachibana E, Saito K, Yoshida J. Preoperative short-term administration of octreotide for facilitating transsphenoidal removal of invasive growth hormone-secreting macroadenomas. Neurol Med Chir (Tokyo) 1999;39:496-9; discussion 499-501
  • Kristof RA, Stoffet-Wagner B, Klingmüller D, Schramm J. Does Octréotide treatment improve the surgical results of macroadenomas in acromegaly ? A randomised study. Acta Neurochir (Wien) 1999;141:399-405
  • Tamura M, Yokoyama N, Abe Y, et al. Preoperative treatment of growth hormone-producing pituitary adenoma with continuous infusion of octreotide. Endocrine J 1998;83:374-8
  • Colao A, Ferone D, Cappabianca P, et al. Effect of octreotide pretreatment on surgical outcome in acromegaly. J Clin Endocrinol Metab 1997;82:3308-14
  • Stevenaert A, Beckers A. Presurgical octreotide: treatment in acromegaly. Metabolism 1996;45:72-4
  • Plockinger U, Reichel M, Fett U, et al. Preoperative octreotide treatment of growth hormone-secreting and clinically nonfunctioning pituitary macroadenomas: effect on tumor volume and lack of correlation with immunohistochemistry and somatostatin receptor scintigraphy. J Clin Endocrinol Metab 1994;79:1416-23
  • Lundin P, Eden Engstrom B, Karlsson FA, Burman P. Long-term octreotide therapy in growth hormone-secreting pituitary adenomas: evaluation with serial MR. Am J Neuroradiol 1997;18:765-72
  • Besser GM, Burman P, Daly AF. Predictors and rates of treatment-resistant tumor growth in acromegaly. Eur J Endocrinol 2005;153:187-93
  • Stevenaert A, Harris AG, Kovacs K, Beckers A. Presurgical octreotide treatment in acromegaly. Metabolism 1992;41:51-8
  • Barkan AL, Lloyd RV, Chandler WF, et al. Preoperative treatment of acromegaly with long-acting somatostatin analog SMS 201-995: shrinkage of invasive pituitary macroadenomas and improved surgical remission rate. J Clin Endocrinol Metab 1988;67:1040-8
  • Biermasz NR, van Dulken H, Roelfsema F. Direct postoperative and follow-up results of transsphenoidal surgery in 19 acromegalic patients pretreated with octreotide compared to those in untreated matched controls. J Clin Endocrinol Metab 1999;84:3551-5
  • Petrossians P, Borges-Martins L, Espinoza C, et al. Gross total resection or debulking of pituitary adenomas improves hormonal control of acromegaly by somatostatin analogs. Eur J Endocrinol 2005;152:61-6
  • Parkinson C, Drake WM, Roberts ME, et al. A comparison of the effects of pegvisomant and octreotide on glucose, insulin, gastrin, cholecystokinin, and pancreatic polypeptide responses to oral glucose and a standard mixed meal. J Clin Endocrinol Metab 2002;87:1797-804
  • Rose DR, Clemmons DR. Growth hormone receptor antagonist improves insulin resistance in acromegaly. Growth Horm IGF Res 2002;12:418-24
  • Barkan AL, Burman P, Clemmons DR, et al. Glucose homeostasis and safety in patients with acromegaly converted from long-acting octreotide to pegvisomant. J Clin Endocrinol Metab 2005;90:5684-91
  • Parkinson C, Burman P, Messig M, Trainer PJ. Gender, body weight, disease activity, and previous radiotherapy influence the response to pegvisomant. J Clin Endocrinol Metab 2007;92:190-5
  • Schreiber I, Buchfelder M, Droste M, et al. Treatment of acromegaly with the GH receptor antagonist pegvisomant in clinical practice: safety and efficacy evaluation from the German Pegvisomant Observational Study. Eur J Endocrinol 2007;156:75-82
  • van der Lely AJ, Muller A, Janssen JA, et al. Control of tumor size and disease activity during cotreatment with octreotide and the growth hormone receptor antagonist pegvisomant in an acromegalic patient. J Clin Endocrinol Metab 2001;86:478-81
  • Colao A, Pivonello R, Auriemma RS, et al. Efficacy of 12-month treatment with the GH receptor antagonist pegvisomant in patients with acromegaly resistant to long-term, high-dose somatostatin analog treatment: effect on IGF-I levels, tumor mass, hypertension and glucose tolerance. Eur J Endocrinol 2006;154:467-77
  • Paisley AN, Rowles SV, Roberts ME, et al. Treatment of acromegaly improves quality of life, measured by AcroQol. Clin Endocrinol (Oxf) 2007;67:358-62
  • Pivonello R, Galderisi M, Auriemma RS, et al. Treatment with growth hormone receptor antagonist in acromegaly: effect on cardiac structure and performance. J Clin Endocrinol Metab 2007;92:476-82
  • Paisley AN, Hayden K, Ellis A, et al. Pegvisomant interference in GH assays results in underestimation of GH levels. Eur J Endocrinol 2007;156:315-9
  • Norman P. Vapreotide (Debipharm). Drugs 2000;3:1358-72
  • Vapreotide: BMY 41606, RC 160, Sanvar. Drugs R&D 2003;4:326-30
  • Li JK, Chow CC, Yeung VT, et al. Treatment of Chinese acromegaly with a combination of bromocriptine and octreotide. Aust N Z J Med 2000;30:457-61
  • Marzullo P, Ferone D, Di Somma C, et al. Efficacy of combined treatment with lanreotide and cabergoline in selected therapy-resistant acromegalic patients. Pituitary 1999;1:115-20
  • Cozzi R, Attanasio R, Lodrini S, Lasio G. Cabergoline addition to depot somatostatin analogues in resistant acromegalic patients: efficacy and lack of predictive value of prolactin status. Clin Endocrinol (Oxf) 2004;61:209-15
  • Selvarajah D, Webster J, Ross R, Newell-Price J. Effectiveness of adding dopamine agonist therapy to long-acting somatostatin analogues in the management of acromegaly. Eur J Endocrinol 2005;152:569-74
  • Flogstad AK, Halse J, Grass P, et al. A comparison of octreotide, bromocriptine, or a combination of both drugs in acromegaly. J Clin Endocrinol Metab 1994;79:461-5
  • Jaquet P, Gunz G, Saveanu A, et al. Efficacy of chimeric molecules directed towards multiple somatostatin and dopamine receptors on inhibition of GH and prolactin secretion from GH-secreting pituitary adenomas classified as partially responsive to somatostatin analog therapy. Eur J Endocrinol 2005;153:135-41
  • Saveanu A, Lavaque E, Gunz G, et al. Demonstration of enhanced potency of a chimeric somatostatin-dopamine molecule, BIM-23A387, in suppressing growth hormone and prolactin secretion from human pituitary somatotroph adenoma cells. J Clin Endocrinol Metab 2002;87:5545-52
  • Feenstra J, de Herder WW, ten Have SM, et al. Combined therapy with somatostatin analogues and weekly pegvisomant in active acromegaly. Lancet 2005;365:1644-6
  • Neggers SJ, van Aken MO, Janssen JA, et al. Long-term efficacy and safety of combined treatment of somatostatin analogs and pegvisomant in acromegaly. J Clin Endocrinol Metab 2007;92:4598-601
  • Patel YC. Somatostatin and its receptor family. Front Neuroendocrinol 1999;20:157-98
  • Reisine T, Bell GI. Molecular biology of somatostatin receptors. Endocr Rev 1995;16:427-42
  • Rossowski WJ, Coy DH. Specific inhibition of rat pancreatic insulin or glucagon release by receptor-selective somatostatin analogs. Biochem Biophys Res Commun 1994;205:341-6
  • Zambre Y, Ling Z, Chen MC, et al. Inhibition of human pancreatic islet insulin release by receptor-selective somatostatin analogs directed to somatostatin receptor subtype 5. Biochem Pharmacol 1999;57:1159-64
  • Yang L, Guo L, Pasternak A, et al. Spiro[1H-indene-1,4′-piperidine] derivatives as potent and selective non-peptide human somatostatin receptor subtype 2 (sst2) agonists. J Med Chem 1998;41:2175-9
  • Shimon I, Yan X, Taylor JE, et al. Somatostatin receptor (SSTR) subtype-selective analogues differentially suppress in vitro growth hormone and prolactin in human pituitary adenomas. Novel potential therapy for functional pituitary tumors. J Clin Invest 1997;100:2386-92
  • Shimon I, Taylor JE, Dong JZ, et al. Somatostatin receptor subtype specificity in human fetal pituitary cultures. Differential role of SSTR2 and SSTR5 for growth hormone, thyroid-stimulating hormone, and prolactin regulation. J Clin Invest 1997;99:789-98
  • Jaquet P, Saveanu A, Gunz G, et al. Human somatostatin receptor subtypes in acromegaly: distinct patterns of messenger ribonucleic acid expression and hormone suppression identify different tumoral phenotypes. J Clin Endocrinol Metab 2000;85:781-92
  • Saveanu A, Gunz G, Dufour H, et al. Bim-23244, a somatostatin receptor subtype 2- and 5-selective analog with enhanced efficacy in suppressing growth hormone (GH) from octreotide-resistant human GH-secreting adenomas. J Clin Endocrinol Metab 2001;86:140-5
  • Reubi JC, Eisenwiener KP, Rink H, et al. A new peptidic somatostatin agonist with high affinity to all five somatostatin receptors. Eur J Pharmacol 2002;456:45-9
  • Jaquet P, Gunz G, Saveanu A, et al. BIM-23A760, a chimeric molecule directed towards somatostatin and dopamine receptors, vs universal somatostatin receptors ligands in GH-secreting pituitary adenomas partial responders to octreotide. J Endocrinol Invest 2005;28(11 Suppl International):21-7
  • Lewis I, Bauer W, Albert R, et al. A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential. J Med Chem 2003;46:2334-44
  • Bruns C, Lewis I, Briner U, et al. 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
  • 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
  • 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
  • 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
  • Dutreix C, Degen L, Schroller S, et al. The safety, tolerability and pharmacokinetics of multiple daily doses of SOM230, a novel multi-ligand somatostatin analog [abstract P240]. International Congress of Endocrinology; 2004; Lisbon, Portugal
  • 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 2005;78:69-80
  • 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
  • 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
  • Petersenn S, Glusman JE, Abs R, et al. Long-term treatment of acromegaly with pasireotide (SOM230): preliminary results from a phase II extension study [abstract P36]. 10th International Pituitary Congress; 2007; Chicago, IL
  • Lee L, Glusman JE, Gao B, et al. The pharmacokinetic-pharmacodynamic (PK-PD) relationship of pasireotide (SOM230), a novel somatostatin analogue, in patients with acromegaly. J Clin Pharmacol 2006;46:1086
  • Petersenn S, Glusman JE, Unger N, Mann K. The effects of pasireotide (SOM230) on glucose metabolism and growth hormone (GH) nadir during oral glucose tolerance test (OGTT) in 12 patients with acromegaly from a phase II study [abstract P565]. European Congress of Endocrinology; 2007; Budapest, Hungary
  • 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
  • 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
  • Zatelli MC, Piccin D, Vignali C, et al. 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;14:91-102
  • Boscaro M, Petersenn S, Atkinson A, et al. Pasireotide (SOM230), the novel multi-ligand somatostatin analogue, is a promising medical therapy for patients with Cushing's disease: preliminary safety and efficacy results of Phase II study [abstract OR9-1]. 88th Annual Endocrine Society Meeting; 2006; Boston, MA
  • Rocheville M, Lange DC, Kumar U, et al. Receptors for dopamine and somatostatin: formation of hetero-oligomers with enhanced functional activity. Science 2000;288:154-7
  • Culler MD, Dong JZ, Taylor JE, et al. The somatostatin-dopamine chimeric molecule, BIM-23A760, is highly efficacious in suppressing GH in normal, cynomolgus monkeys (Macaca fascicularis) [abstract 09-6]. 88th Annual Endocrine Society Meeting; 2006; Philadelphia, PA
  • Culler MD, Dong JZ, Taylor JE, et al. The somatostatin-dopamine chimeric molecule, BIM-23A760, does not induce the insulin/glycemic effects observed with individual somatostatin or dopamine agonists in cynomolgus monkeys (Macaca fascicularis). 12th Meeting of the European Neuroendocrine Association; 2006; Athens, Greece [abstract OC2.11]]
  • Rosengren L, Parrow V, Chmielewska J, et al. In vivo evaluation of a novel, orally bioavailable, small molecule growth hormone receptor antagonist. Growth Horm IGF Res 2007;17:47-53
  • Rosengren L, Simko H, Aryan L, et al. Antisense and sense RNA probe hybridization to immobilized crude cellular lysates: a tool to screen growth hormone antagonists. J Biomol Screen 2005;10:260-9
  • Tachas G, Lofthouse S, Wraight CJ, et al. A GH receptor antisense oligonucleotide inhibits hepatic GH receptor expression, IGF-I production and body weight gain in normal mice. J Endocrinol 2006;189:147-54
  • Melmed S, Casanueva F, Cavagnini F, et al. Consensus statement: medical management of acromegaly. Eur J Endocrinol 2005;153:737-40
  • Maison P, Chanson P. Less is more risky? Growth hormone and insulin-like growth factor 1 levels and cardiovascular risk. Nat Clin Pract Endocrinol Metab 2006;2:650-1

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