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Safety, tolerability, and pharmacokinetics of repeated oral doses of 2-hydroxybenzylamine acetate in healthy volunteers: a double-blind, randomized, placebo-controlled clinical trial.

ABSTRACT: BACKGROUND:2-Hydroxybenzylamine (2-HOBA) is a selective dicarbonyl electrophile scavenger being developed as a nutritional supplement to help protect against the development of conditions associated with dicarbonyl electrophile formation, such as the cognitive decline observed with Mild Cognitive Impairment or Alzheimer's disease. METHODS:This study evaluated the safety, tolerability, and pharmacokinetics of repeated oral doses of 2-HOBA acetate (500 or 750?mg) administered to healthy volunteers every eight hours for two weeks. The effects of 2-HOBA on cyclooxygenase function and cerebrospinal fluid penetrance of 2-HOBA were also investigated. RESULTS:Repeated oral administration of 2-HOBA was found to be safe and well-tolerated up to 750?mg TID for 15?days. 2-HOBA was absorbed within 2?h of administration, had a half-life of 2.10-3.27?h, and an accumulation ratio of 1.38-1.52. 2-HOBA did not interfere with cyclooxygenase function and was found to be present in cerebrospinal fluid 90?min after dosing. CONCLUSIONS:Repeated oral administration of 2-HOBA was found to be safe and well-tolerated. These results support continued development of 2-HOBA as a nutritional supplement. TRIAL REGISTRATION:Studies are registered at ClinicalTrials.gov (NCT03555682 Registered 13 June 2018, NCT03554096 Registered 12 June 18).

SUBMITTER: Pitchford LM

PROVIDER: S-EPMC6945443 | biostudies-literature | 2020 Jan

REPOSITORIES: biostudies-literature

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Safety, tolerability, and pharmacokinetics of repeated oral doses of 2-hydroxybenzylamine acetate in healthy volunteers: a double-blind, randomized, placebo-controlled clinical trial.

Pitchford Lisa M LM Driver Patricia M PM Fuller John C JC Akers Wendell S WS Abumrad Naji N NN Amarnath Venkataraman V Milne Ginger L GL Chen Sheau-Chiann SC Ye Fei F Roberts L Jackson LJ Shoemaker M Benjamin MB Oates John A JA Rathmacher John A JA Boutaud Olivier O

BMC pharmacology & toxicology 20200106 1

<h4>Background</h4>2-Hydroxybenzylamine (2-HOBA) is a selective dicarbonyl electrophile scavenger being developed as a nutritional supplement to help protect against the development of conditions associated with dicarbonyl electrophile formation, such as the cognitive decline observed with Mild Cognitive Impairment or Alzheimer's disease.<h4>Methods</h4>This study evaluated the safety, tolerability, and pharmacokinetics of repeated oral doses of 2-HOBA acetate (500 or 750 mg) administered to hea ...[more]

PMID: 31907026

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Dataset Information

Safety, tolerability, and pharmacokinetics of repeated oral doses of 2-hydroxybenzylamine acetate in healthy volunteers: a double-blind, randomized, placebo-controlled clinical trial.

Publications

Safety, tolerability, and pharmacokinetics of repeated oral doses of 2-hydroxybenzylamine acetate in healthy volunteers: a double-blind, randomized, placebo-controlled clinical trial.

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