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
Georg GolorMario Maldonado

Abstract

Pasireotide (SOM230) is a multireceptor-targeted somatostatin analog with high binding affinity for four of the five somatostatin receptor subtypes (sst(1,2,3) and sst(5)), and potential clinical activity in several neuroendocrine and oncologic conditions, including acromegaly, Cushing's disease, and neuroendocrine tumors (NET). This manuscript reports the first-in-man dose-escalation study of pasireotide, evaluating its safety, tolerability, and pharmacokinetics (PK) in healthy male volunteers. A single dose of pasireotide 1-1200 μg was administered subcutaneously in four to eight subjects per dose level, with two additional subjects per cohort administered placebo. PK and safety evaluations were carried out over 7 days post-dose. Growth hormone (GH) suppression was evaluated using a GH-releasing hormone stimulation test on Day -1 and Day 1 at 3-5 hours post-injection. Seventy-two subjects completed the study. Pasireotide was well tolerated with no serious adverse events observed at any dose. Transient elevations in blood glucose levels were observed 2-6 hours after administration of pasireotide at doses between 200 μg and 1200 μg, but this resolved without intervention by 23 hours post-dosing. The maximum tolerable dose was n...Continue Reading

References

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Jun 28, 2006·Annals of Oncology : Official Journal of the European Society for Medical Oncology·C Susini, L Buscail
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Citations

Jan 26, 2016·Expert Opinion on Pharmacotherapy·Luiz Eduardo Wildemberg, Mônica R Gadelha
Jan 10, 2014·Expert Opinion on Emerging Drugs·Sylvère Störmann, Jochen Schopohl
May 3, 2014·Journal of Clinical Pharmacology·Ruediger KornbergerKe Hu
May 7, 2015·Journal of Veterinary Internal Medicine·C J ScudderS J M Niessen
Apr 18, 2018·Stress : the International Journal on the Biology of Stress·Antônio Ribeiro-OliveiraKevin C J Yuen
Aug 25, 2017·The Journal of Endocrinology·Alejandro Ibáñez-Costa, Márta Korbonits
Sep 3, 2016·The Journal of Endocrinology·Alejandro Ibáñez-CostaJusto P Castaño
May 29, 2015·Drugs·Kate McKeage
Dec 29, 2020·Frontiers in Endocrinology·Rosario PivonelloAnnamaria Colao

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