Safety, pharmacokinetics, and pharmacodynamics of TV-1380, a novel mutated butyrylcholinesterase treatment for cocaine addiction, after single and multiple intramuscular injections in healthy subjects.
Bottom Line: Two randomized, blinded phase I studies were conducted to evaluate the safety, pharmacokinetics, and pharmacodynamics of TV-1380, following single and multiple administration in healthy subjects.TV-1380 was found to be safe and well tolerated with a long half-life (43-77 hours) and showed a dose-proportional increase in systemic exposure.There was no evidence that TV-1380 affected heart rate, the uncorrected QT interval, or the heart-rate-corrected QTcF interval.
Affiliation: Teva Pharmaceuticals, Inc., Netanya, Israel.Show MeSH
Related in: MedlinePlus
Mentions: Mean plasma concentration time profiles following single dose administration are presented in Figure 2a and PK parameters in Table3. TV-1380 serum concentrations were below the lower limit of quantification (BLQ) for all or most samples treated with 0.5, 1.5, 5, and 15 mg. Median tmax ranged between 12 and 18 hours postdose and t1/2 ranged between 43 and 63 hours. Cmax and AUC increased in a dose-proportional manner (using the power model) over the 50–300 mg dose range. AUC0–t and AUC0–inf were calculated for all subjects at doses 50, 150, and 300 mg with AUC0–t being >80 in all cases, thus only AUC0–inf is reported in Table3.