PASIREOTIDE, A MULTI-SOMATOSTATIN RECEPTOR LIGAND WITH POTENTIAL EFFICACY FOR TREATMENT OF PITUITARY AND NEUROENDOCRINE TUMORS

被引：25

作者：

Feelders, R. A. ^{[1
]}

de Herder, W. W. ^{[1
]}

Neggers, S. J. ^{[1
]}

van der Lely, A-J. ^{[1
]}

Hofland, L. J. ^{[1
]}

机构：

[1] Erasmus MC, Endocrinol Sect, Dept Internal Med, Rotterdam, Netherlands

来源：

DRUGS OF TODAY | 2013年 / 49卷 / 02期

关键词：

Pasireotide; Cushing's disease; SOM-230; Growth hormone release inhibitors; ANALOG SOM230; GROWTH-HORMONE; CELL-PROLIFERATION; MEDICAL-TREATMENT; CUSHINGS-DISEASE; CATECHOLAMINE LEVELS; OCTREOTIDE; SUBTYPES; EVEROLIMUS; EXPRESSION;

D O I：

10.1358/dot.2013.49.2.1915142

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Somatostatin receptors are an important target for medical treatment of pituitary and neuroendocrine tumors. To date, five somatostatin receptor (sst) subtypes have been identified. The currently available somatostatin analogues octreotide and lanreotide have predominantly affinity for sst(2). Pasireotide is a sst multireceptor ligand with affinity for sst(1), sst(2), sst(3) and sst(5) and this broader binding profile may translate into a higher efficacy with respect to suppression of hormone production and cell growth in certain tumors. Experimental animal studies and in vitro studies with cultured tumor cells have shown that pasireotide strongly suppresses growth hormone and adrenocorticotropin production. In addition, pasireotide can influence tumor cell growth via effects on apoptosis and angiogenesis. In this review, the role of somatostatin receptors in pituitary and neuroendocrine tumors is briefly discussed followed by an overview of possible applications of pasireotide based on recent trials in patients with acromegaly, Cushing's disease and neuroendocrine tumors.

引用

页码：89 / 103

页数：15

共 85 条

[1] The effects of SOM230 on cell proliferation and adrenocorticotropin secretion in human corticotroph pituitary adenomas [J].

Batista, Dalia L. ;

Zhang, Xun ;

Gejman, Roger ;

Ansell, Peter J. ;

Zhou, Yunli ;

Johnson, Sarah A. ;

Swearingen, Brooke ;

Hedley-Whyte, E. Tessa ;

Stratakis, Constantine A. ;

Klibanski, Anne .

JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM, 2006, 91 (11) :4482-4488

[2] TSH-secreting adenomas [J].

Beck-Peccoz, Paolo ;

Persani, Luca ;

Mannavola, Deborah ;

Campi, Irene .

BEST PRACTICE & RESEARCH CLINICAL ENDOCRINOLOGY & METABOLISM, 2009, 23 (05) :597-606

[3] Constitutive Somatostatin Receptor Activity Determines Tonic Pituitary Cell Response [J].

Ben-Shlomo, Anat ;

Zhou, Cuiqi ;

Pichurin, Oxana ;

Chesnokova, Vera ;

Liu, Ning-Ai ;

Culler, Michael D. ;

Melmed, Shlomo .

MOLECULAR ENDOCRINOLOGY, 2009, 23 (03) :337-348

[4] Treatment of adrenocorticotropin-dependent Cushing's syndrome: A consensus statement [J].

Biller, B. M. K. ;

Grossman, A. B. ;

Stewart, P. M. ;

Melmed, S. ;

Bertagna, X. ;

Bertherat, J. ;

Buchfelder, M. ;

Colao, A. ;

Hermus, A. R. ;

Hofland, L. J. ;

Klibanski, A. ;

Lacroix, A. ;

Lindsay, J. R. ;

Newell-Price, J. ;

Nieman, L. K. ;

Petersenn, S. ;

Sonino, N. ;

Stalla, G. K. ;

Swearingen, B. ;

Vance, M. L. ;

Wass, J. A. H. ;

Boscaro, M. .

JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM, 2008, 93 (07) :2454-2462

[5] Treatment of Pituitary-Dependent Cushing's Disease with the Multireceptor Ligand Somatostatin Analog Pasireotide (SOM230): A Multicenter, Phase II Trial [J].

Boscaro, M. ;

Ludlam, W. H. ;

Atkinson, B. ;

Glusman, J. E. ;

Petersenn, S. ;

Reincke, M. ;

Snyder, P. ;

Tabarin, A. ;

Biller, B. M. K. ;

Findling, J. ;

Melmed, S. ;

Darby, C. H. ;

Hu, K. ;

Wang, Y. ;

Freda, P. U. ;

Grossman, A. B. ;

Frohman, L. A. ;

Bertherat, J. .

JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM, 2009, 94 (01) :115-122

[6] HYPOTHALAMIC POLYPEPTIDE THAT INHIBITS SECRETION OF IMMUNOREACTIVE PITUITARY GROWTH-HORMONE [J].

BRAZEAU, P ;

VALE, W ;

BURGUS, R ;

LING, N ;

BUTCHER, M ;

RIVIER, J ;

GUILLEMIN, R .

SCIENCE, 1973, 179 (4068) :77-79

[7] SOM230: a novel somatostatin peptidomimetic with broad somatotropin release inhibiting factor (SRIF) receptor binding and a unique antisecretory profile [J].

Bruns, C ;

Lewis, I ;

Briner, U ;

Meno-Tetang, G ;

Weckbecker, G .

EUROPEAN JOURNAL OF ENDOCRINOLOGY, 2002, 146 (05) :707-716

[8] Phase I study of pasireotide (SOM 230) and everolimus (RAD001) in advanced neuroendocrine tumors [J].

Chan, Jennifer A. ;

Ryan, David P. ;

Zhu, Andrew X. ;

Abrams, Thomas A. ;

Wolpin, Brian M. ;

Malinowski, Paige ;

Regan, Eileen M. ;

Fuchs, Charles S. ;

Kulke, Matthew H. .

[9] A 12-Month Phase 3 Study of Pasireotide in Cushing's Disease [J].

Colao, Annamaria ;

Petersenn, Stephan ;

Newell-Price, John ;

Findling, James W. ;

Gu, Feng ;

Maldonado, Mario ;

Schoenherr, Ulrike ;

Mills, David ;

Salgado, Luiz Roberto ;

Biller, Beverly M. K. .

NEW ENGLAND JOURNAL OF MEDICINE, 2012, 366 (10) :914-924

[10] Medical therapy for clinically non-functioning pituitary adenomas [J].

Colao, Annamaria ;

Di Somma, Carolina ;

Pivonello, Rosario ;

Faggiano, Antongiulio ;

Lombardi, Gaetano ;

Savastano, Silvia .

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