A first-in-man study to evaluate the safety, tolerability, and pharmacokinetics of pasireotide (SOM230), a multireceptor-targeted somatostatin analog, in healthy volunteers

Drug Design, Development and Therapy

Volumn 6, Issue , 2012, Pages 71-79

  Golor, Georg ^a   Hu, Ke ^b   Ruffin, Matthieu ^b   Buchelt, Alexandra ^b   Bouillaud, Emmanuel ^b   Wang, Yanfeng ^b   Maldonado, Mario ^b  

^a PAREXEL INTERNATIONAL   (United States)

^b NOVARTIS PHARMA AG   (Switzerland)

Author keywords

Healthy volunteers; Pasireotide; Pharmacokinetics; Safety; Tolerability

Indexed keywords

GLUCOSE; GROWTH HORMONE; PASIREOTIDE; PLACEBO;

ABDOMINAL DISCOMFORT; ADULT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DIZZINESS; DOSE RESPONSE; DRUG ABSORPTION; DRUG CLEARANCE; DRUG DOSE ESCALATION; DRUG ELIMINATION; DRUG HALF LIFE; DRUG INDUCED HEADACHE; DRUG RESEARCH; DRUG SAFETY; DRUG STRUCTURE; DRUG TOLERABILITY; FEMALE; GLUCOSE BLOOD LEVEL; GROWTH HORMONE RELEASE; HORMONAL REGULATION; HORMONE INHIBITION; HUMAN; HUMAN EXPERIMENT; INFLUENZA; MALE; MAXIMUM PLASMA CONCENTRATION; NAUSEA; NORMAL HUMAN; SINGLE DRUG DOSE; TIME TO MAXIMUM PLASMA CONCENTRATION; VOMITING;

EID: 84862084544     PISSN: 11778881     EISSN: None     Source Type: Journal    
DOI: 10.2147/dddt.s29125     Document Type: Article

References (19)

1. 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(5):707-716.
2. Schmid HA. Pasireotide (SOM230): development, mechanism of action and potential applications. Mol Cell Endocrinol. 2008;286(1-2):69-74.
3. Susini C, Buscail L. Rationale for the use of somatostatin analogs as antitumor agents. Ann Oncol. 2006;17(12):1733-1742.
4. 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(12):2334-2344.
5. Schmid HA. Preclinical evidences suggest new treatment options for endocrine disorders: Pasireotide (SOM230) and Everolimus (RAD001). Ann Endocrinol (Paris). 2008;69(2):162-163.
6. 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(2):638-645.
7. Petersenn S, Schopohl J, Pasireotide Acromegaly Study Group, et al. Pasireotide (SOM230) demonstrates efficacy and safety in patients with acromegaly: a randomized, multicenter, Phase II trial. J Clin Endocrinol Metab. 2010;95(6):2781-2789.
8. Colao A, Fleck J, Pain S, et al. Pasireotide LAR versus octreotide LAR or lanreotide autogel in patients with inadequately controlled acromegaly: A Phase III, multicenter, randomized, parallel-group study. ENEA Abstracts. 2010;82-83:Abst OC-6.2.
9. Bronstein M, Gu F, Shen C-C, et al. A randomized, blinded, multicenter, Phase III study to assess the efficacy and safety of pasireotide LAR versus octreotide LAR in patients with active acromegaly. ENEA Abstracts. 2010;82:Abst OC-6.1.
10. Kvols L, Glusman JE, Pasireotide Carcinoid Study Group, et al. The effects of pasireotide (SOM230) on health-related quality of life in patients with metastatic carcinoid tumors refractory or resistant to octreotide LAR. J Clin Oncol. 2007;25(18)(Suppl.):Abst 4558. Available from: http://meeting.ascopubs.org/cgi/content/abstract/25/18_suppl/4558. Accessed February 22, 2012.
11. Kvols L, Oberg K, Pasireotide Carcinoid Study Group, et al. Efficacy, safety and pharmacokinetic results from a Phase II study of pasireotide (SOM230) in the treatment of patients with metastatic NETs refractory or resistant to octreotide LAR. Neuroendocrinology. 2010;92(1):Abst C57.
12. Colao A, Petersenn S, Newell-Price J, et al. A 12-month Phase 3 study of pasireotide in Cushing's disease. N Engl J Med. 2012; 366(10):914-924.
13. Cook D. Octreotide long-acting repeatable in acromegaly: achieving optimal control. The Endocrinologist. 2009;19(3):142-147.
14. Croxtall JD, Scott LJ. Lanreotide Autogel: a review of its use in the management of acromegaly. Drugs. 2008;68(5):711-723.
15. Oberg K. Somatostatin analog octreotide LAR in gastro-entero-pancreatic tumors. Expert Rev Anticancer Ther. 2009;9(5): 557-566.
16. Ipsen Ltd. Somatuline® depot (lanreotide) injection prescribing information. March 2011. Available from: http://www.somatulinedepot. com/hcp/pdf/SomatulineDepot_Full_Prescribing_Information.pdf. Accessed February 22, 2012.
17. Novartis Pharmaceuticals Corporation. Sandostatin® LAR Depot (octreotide acetate for injectable suspension) prescribing information. September 2011. Available from: http://www.pharma.us.novartis. com/product/pi/pdf/sandostatin_lar.pdf. Accessed February 22, 2012.
18. 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(1):115-122.
19. 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(1):69-80.