Pasireotide (SOM230), a novel multireceptor-targeted somatostatin analogue, is well tolerated when administered as a continuous 7-day subcutaneous infusion in healthy male volunteers

Journal of Clinical Pharmacology

Volumn 52, Issue 7, 2012, Pages 1017-1027

  Petersenn, Stephan ^a   Unger, Nicole ^a   Hu, Ke ^b   Weisshaar, Brigitte ^b   Zhang, Yilong ^b   Bouillaud, Emmanuel ^b   Reséndiz, Karina Hermosillo ^b   Wang, Yanfeng ^b   Mann, Klaus ^a  

^a UNIVERSITY OF DUISBURG ESSEN   (Germany)

^b NOVARTIS PHARMA AG   (Switzerland)

Author keywords

healthy volunteers; pasireotide; pharmacokinetics; safety; subcutaneous infusion; tolerability

Indexed keywords

ALANINE AMINOTRANSFERASE; AMYLASE; ASPARTATE AMINOTRANSFERASE; BILIRUBIN; CHOLESTEROL; CREATININE; GAMMA GLUTAMYLTRANSFERASE; GLUCAGON; GLUCOSE; INSULIN; PASIREOTIDE; TRIACYLGLYCEROL LIPASE;

ABDOMINAL PAIN; ADULT; ALANINE AMINOTRANSFERASE BLOOD LEVEL; AMYLASE BLOOD LEVEL; AREA UNDER THE CURVE; ARTICLE; ASPARTATE AMINOTRANSFERASE BLOOD LEVEL; BILIRUBIN BLOOD LEVEL; BLOOD SAMPLING; CHOLESTEROL BLOOD LEVEL; COHORT ANALYSIS; CONTINUOUS INFUSION; CREATININE BLOOD LEVEL; DIARRHEA; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DOSE ESCALATION; DRUG DOSE INCREASE; DRUG DOSE REDUCTION; DRUG FORMULATION; DRUG MEGADOSE; DRUG RELEASE; DRUG SAFETY; DRUG TOLERABILITY; DRUG WITHDRAWAL; FECES COLOR; FLATULENCE; GAMMA GLUTAMYL TRANSFERASE BLOOD LEVEL; GLUCAGON BLOOD LEVEL; GLUCOSE BLOOD LEVEL; GLUCOSE METABOLISM; HEADACHE; HUMAN; HUMAN EXPERIMENT; INSULIN BLOOD LEVEL; INTESTINAL DYSMOTILITY; MALE; NAUSEA; NORMAL HUMAN; OPEN STUDY; SIDE EFFECT; STEADY STATE; SYNCOPE; TREATMENT DURATION; TRIACYLGLYCEROL LIPASE BLOOD LEVEL; VERTIGO; XEROSTOMIA;

ADULT; BLOOD GLUCOSE; DELAYED-ACTION PREPARATIONS; DOSE-RESPONSE RELATIONSHIP, DRUG; GLUCAGON; HUMANS; INFUSIONS, SUBCUTANEOUS; INSULIN; MALE; SOMATOSTATIN; YOUNG ADULT;

EID: 84856088188     PISSN: 00912700     EISSN: 15524604     Source Type: Journal    
DOI: 10.1177/0091270011408727     Document Type: Article

References (14)

1. 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;94:115-122.
2. 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;95:2781-2789.
3. 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. (Pubitemid 40956933)
4. 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;89:638-645. (Pubitemid 38269871)
5. 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;146:707-716. (Pubitemid 34552506)
6. Schmid HA. Pasireotide (SOM230): development, mechanism of action and potential applications. Mol Cell Endocrinol. 2008;286:69-74. (Pubitemid 351680237)
7. Ben-Shlomo A, Schmid H, Wawrowsky K, et al. Differential ligand-mediated pituitary somatostatin receptor subtype signaling: implications for corticotroph tumor therapy. J Clin Endocrinol Metab. 2009;94:4342-4350.
8. Hofland LJ, Lamberts SW. Somatostatin receptors in pituitary function, diagnosis and therapy. Front Horm Res. 2004;32:235-252.
9. Hofland LJ, Lamberts SW. The pathophysiological consequences of somatostatin receptor internalization and resistance. Endocr Rev. 2003;24:28-47. (Pubitemid 36223278)
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. (Pubitemid 41076629)
11. Trotti A, Colevas AD, Setser A, et al. CTCAE v3.0: development of a comprehensive grading system for the adverse effects of cancer treatment. Semin Radiat oncol. 2003;13:176-181. (Pubitemid 36962641)
12. Ben-Shlomo A, Melmed S. Somatostatin agonists for treatment of acromegaly. Mol Cell Endocrinol. 2008;286:192-198.
13. Roges OA, Baron M, Philis-Tsimikas A. The incretin effect and its potentiation by glucagon-like peptide 1-based therapies: a revolution in diabetes management. Expert opin Investig Drugs. 2005;14:705-727. (Pubitemid 40895196)
14. Mazziotti G, Floriani I, Bonadonna S, Torri V, Chanson P, Giustina A. Effects of somatostatin analogs on glucose homeostasis: a metaanalysis of acromegaly studies. J Clin Endocrinol Metab. 2009;94:1500-1508.