Background: 2-Hydroxybenzylamine (2-HOBA) is a selective scavenger of dicarbonyl electrophiles that protects\nproteins and lipids from being modified by these electrophiles. It is currently being developed for use as a\nnutritional supplement to help maintain good health and protect against the development of conditions associated\nwith dicarbonyl electrophile formation, such as the cognitive decline associated with Mild Cognitive Impairment\nand Alzheimerâ??s disease.\nMethods: In this first-in-human study, the safety, tolerability, and pharmacokinetics of six ascending single oral\ndoses of 2-HOBA acetate were tested in eighteen healthy human volunteers.\nResults: Reported adverse events were mild and considered unlikely to be related to 2-HOBA. There were no\nclinically significant changes in vital signs, ECG recordings, or clinical laboratory parameters. 2-HOBA was fairly\nrapidly absorbed, with a tmax of 1â??2 h, and eliminated, with a t1/2 of approximately 2 h. Both tmax and t1/2 were\nindependent of dose level, while Cmax and AUC increased proportionally with dose level.\nConclusions: 2-HOBA acetate was safe and well-tolerated at doses up to 825 mg in healthy human volunteers,\npositioning it as a good candidate for continued development as a nutritional supplement.\nTrial registration: This study is registered at ClinicalTrials.gov (NCT03176940).
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