Safety, Tolerability, Pharmacokinetics, and Concentration-QTc Analysis of Tetrodotoxin: A Randomized, Dose Escalation Study in Healthy Adults.

ABSTRACT: Tetrodotoxin (TTX) is a highly specific voltage-gated sodium channel (VGSC) blocker in clinical evaluation as a peripheral-acting analgesic for chronic pain. This study presents the first published results of the safety including cardiac liability of TTX at therapeutic-relevant concentrations in twenty-five healthy adults. Randomized, double-blind, placebo-, and positive- (moxifloxacin) controlled study evaluated single ascending doses of 15 µg, 30 µg, and 45 µg TTX over 3 periods with a 7-day washout between each period. Subcutaneous injections of TTX were readily absorbed, reaching maximum plasma concentration (C_max) within 1.5 h. Both extent of exposure (AUC) and C_max increased in proportion to dose. No QT prolongation was identified by concentration-QTc analysis a

SUBMITTER: Kavoosi M 

PROVIDER: S-EPMC7472037 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature