Results of a Phase I Open-Label Clinical Trial of Direkord in Healthy Volunteers

Abstract

Direkord is an original drug containing the active substance of dicholine succinate, which enhances neuronal insulin sensitivity. In this work, we study the tolerability, safety, and pharmacokinetic parameters of dicholine succinate when administered intramuscularly in a phase I clinical trial in healthy volunteers. In total, 18 healthy volunteers –11 men and 7 women – with a mean age of 30.4±7.8 years, were recruited into a randomized study. At stage I, 6 volunteers (group 1) received dicholine succinate intramuscularly every other day with a dose escalation from 0.16 mg/kg/day to 600 mg/day. At stage II, 12 volunteers (group 2) received dicholine succinate intramuscularly at a single dose of 200 mg, and then, at stage III, the same 12 volunteers received dicholinesuccinate at a dose of 600 mg/day (3 x 200 mg at an interval of 8 hours) for seven days. The safety population in this study included all randomized volunteers. Data from 12 volunteers (group 2) were included in the calculation of the pharmacokinetic parameters. All volunteers completed all procedures of the three research stages in accordance with the protocol. According to clinical and laboratory monitoring data, no adverse events were registered during the study. The drug was well tolerated, with no signs of hyperemia, edema, and bruising being observed at the injection site. The volunteers did not complain of pain, itching, and burning. After a single injection of dicholine succinate, the concentration of choline in the bloodstream reached its maximum value after an average of 0.375±0.365 hours with the half-life of 1.271±1.071 hours. After repeated administration at a dose of 600 mg per day, no cumulation of the active substance was observed. The data obtained have confirmed a good safety profile of Direkord; therefore, the drug can be recommended for further investigation in a study involving patients.