British journal of clinical pharmacology
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Br J Clin Pharmacol · Jul 2005
Randomized Controlled Trial Clinical TrialClinical pharmacology of DP-b99 in healthy volunteers: first administration to humans.
To investigate the safety, tolerability and pharmacokinetics of DP-b99 in healthy volunteers. DP-b99 is a newly developed lipophilic, cell permeable derivative of BAPTA (1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid), which selectively modulates the distribution of metal ions in hydrophobic milieu, and is in clinical development as a neuroprotectant for cerebral ischaemic stroke. To our knowledge no BAPTA derivative has ever been administered to man. Here we report the first human administration of DP-b99 in a phase I, two-part, double-blind, randomized placebo controlled study, with single IV doses of 0.003-1.0 mg kg(-1) day(-1) DP-b99 (part 1) or multiple ascending doses of 0.03-1.0 mg kg(-1) day(-1) DP-b99 over 4 days (part 2). ⋯ This study suggests that DP-b99 is well tolerated in healthy young and elderly volunteers within the dose range evaluated. Studies to investigate further the efficacy of the compound are in progress.