High‐dose intranasal insulin in an adaptive dose‐escalation study in healthy human participants

Abstract Intranasal insulin is a putative neuroprotective therapy after cardiac arrest, but safety in humans at doses extrapolated from animal models is unknown. This phase I, open‐label adaptive dose‐escalation study explores the maximum tolerated dose of intranasal insulin in healthy human partici...

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Main Authors: Florian Schmitzberger, Jennifer Fowler, Cindy H. Hsu, Manjunath P. Pai, Robert W. Neumar, William J. Meurer, Robert Silbergleit
Format: Article
Language:English
Published: Wiley 2024-11-01
Series:Clinical and Translational Science
Online Access:https://doi.org/10.1111/cts.70071
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author Florian Schmitzberger
Jennifer Fowler
Cindy H. Hsu
Manjunath P. Pai
Robert W. Neumar
William J. Meurer
Robert Silbergleit
author_facet Florian Schmitzberger
Jennifer Fowler
Cindy H. Hsu
Manjunath P. Pai
Robert W. Neumar
William J. Meurer
Robert Silbergleit
author_sort Florian Schmitzberger
collection DOAJ
description Abstract Intranasal insulin is a putative neuroprotective therapy after cardiac arrest, but safety in humans at doses extrapolated from animal models is unknown. This phase I, open‐label adaptive dose‐escalation study explores the maximum tolerated dose of intranasal insulin in healthy human participants. Placebo or insulin at doses from 0 to 1000 units was given to healthy participants intranasally on repeated weekly visits. Serum glucose, insulin, and C‐peptide levels were measured serially at 0, 15, 30, 60, 120, 180, and 240 min after administration. Twenty‐four participants (12 female, median age 53, IQR 35–61) were enrolled. There was minimal change in average serum glucose after administration of intranasal insulin. Average serum insulin increased slightly in a dose‐dependent manner, reaching maximum concentrations at 15 min. C‐peptide decreased over time from administration in all groups. One participant had severe hypoglycemia (24 mg/dL at 45 min) and a different participant had mild hypoglycemia (51 mg/dL at 30 min), both after receiving 600 U intranasal insulin. Hypoglycemic episodes were associated with increases in serum insulin. Both participants continued in the study without hypoglycemia after additional doses. High‐dose intranasal insulin up to 1000 U was generally well tolerated, with minimal measurable systemic absorption and without significant aggregate changes in mean glucose. Idiosyncratic episodic systemic absorption and hypoglycemia require further study and additional caution in potential clinical application. Further study of its target engagement and efficacy as a neuroprotective therapy after cardiac arrest at these doses is warranted.
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spelling doaj-art-188d9feac7fa4c02855c8b4898ab54712024-11-26T07:10:37ZengWileyClinical and Translational Science1752-80541752-80622024-11-011711n/an/a10.1111/cts.70071High‐dose intranasal insulin in an adaptive dose‐escalation study in healthy human participantsFlorian Schmitzberger0Jennifer Fowler1Cindy H. Hsu2Manjunath P. Pai3Robert W. Neumar4William J. Meurer5Robert Silbergleit6Department of Emergency Medicine University of Michigan Ann Arbor Michigan USADepartment of Emergency Medicine University of Michigan Ann Arbor Michigan USADepartment of Emergency Medicine University of Michigan Ann Arbor Michigan USAMax Harry Weil Institute for Critical Care Research and Innovation Ann Arbor Michigan USADepartment of Emergency Medicine University of Michigan Ann Arbor Michigan USADepartment of Emergency Medicine University of Michigan Ann Arbor Michigan USADepartment of Emergency Medicine University of Michigan Ann Arbor Michigan USAAbstract Intranasal insulin is a putative neuroprotective therapy after cardiac arrest, but safety in humans at doses extrapolated from animal models is unknown. This phase I, open‐label adaptive dose‐escalation study explores the maximum tolerated dose of intranasal insulin in healthy human participants. Placebo or insulin at doses from 0 to 1000 units was given to healthy participants intranasally on repeated weekly visits. Serum glucose, insulin, and C‐peptide levels were measured serially at 0, 15, 30, 60, 120, 180, and 240 min after administration. Twenty‐four participants (12 female, median age 53, IQR 35–61) were enrolled. There was minimal change in average serum glucose after administration of intranasal insulin. Average serum insulin increased slightly in a dose‐dependent manner, reaching maximum concentrations at 15 min. C‐peptide decreased over time from administration in all groups. One participant had severe hypoglycemia (24 mg/dL at 45 min) and a different participant had mild hypoglycemia (51 mg/dL at 30 min), both after receiving 600 U intranasal insulin. Hypoglycemic episodes were associated with increases in serum insulin. Both participants continued in the study without hypoglycemia after additional doses. High‐dose intranasal insulin up to 1000 U was generally well tolerated, with minimal measurable systemic absorption and without significant aggregate changes in mean glucose. Idiosyncratic episodic systemic absorption and hypoglycemia require further study and additional caution in potential clinical application. Further study of its target engagement and efficacy as a neuroprotective therapy after cardiac arrest at these doses is warranted.https://doi.org/10.1111/cts.70071
spellingShingle Florian Schmitzberger
Jennifer Fowler
Cindy H. Hsu
Manjunath P. Pai
Robert W. Neumar
William J. Meurer
Robert Silbergleit
High‐dose intranasal insulin in an adaptive dose‐escalation study in healthy human participants
Clinical and Translational Science
title High‐dose intranasal insulin in an adaptive dose‐escalation study in healthy human participants
title_full High‐dose intranasal insulin in an adaptive dose‐escalation study in healthy human participants
title_fullStr High‐dose intranasal insulin in an adaptive dose‐escalation study in healthy human participants
title_full_unstemmed High‐dose intranasal insulin in an adaptive dose‐escalation study in healthy human participants
title_short High‐dose intranasal insulin in an adaptive dose‐escalation study in healthy human participants
title_sort high dose intranasal insulin in an adaptive dose escalation study in healthy human participants
url https://doi.org/10.1111/cts.70071
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