Aim. To study the tolerability, safety, pharmacokinetics (PK) and pharmacodynamics of single intravenous infusions of Angipur in healthy male volunteers.Material and methods. The Phase I trial included 20 healthy male volunteers (mean age, 30,8±7,7 years; mean body weight, 77,4±12,1 kg). Angipur (0,02% concentrate for solution for infusion) was administered to every subject in single doses 0,015, 0,05, 0,09 mg/kg for 3 consecutive days. Volunteers were divided in 6 groups (1, 1, 3, 5, 5, 5); every following group was recruited only after the previous one finished the study. The following were assessed: rate and severity of adverse events (AEs), key PK parameters of Angipur and its antiplatelet activity by impedance aggregometry.Results. No moderate or severe AEs, as well as no serious AEs were reported according to obtained data of clinical and laboratory monitoring of healthy subjects. Totally 6 mild AEs were registered in 4 subjects. Four AEs (mild hematological deviations and episode of nose bleed) were classified as possibly related to study drug and 1 AE (positive fecal occult blood test) — probably related. Key PK parameters of Angipur in single intravenous doses 0,015, 0,05 и 0,09 mg/kg were determined as follows: Cmax — 12,44±4,689, 46,10±14,295, 92,48±33,896 ng/ml; Vd — 304,01±55,300, 299,67±64,244, 252,96±47,790 l; T1/2 — 6,72±1,290, 6,84±2,341, 6,06±2,287 h; Cl — 32,19±6,919, 32,29±8,357, 31,55±10,113 l/h, respectively. Dose proportionality (linear PK) for parameters Cmax, AUC0-t and AUC0-∞ was established. Dose-dependent reduction of ADP-induced platelet aggregation degree and area under curve was revealed at period of 15 min to 2-4 h after Angipur infusion in doses 0,05 and 0,09 mg/kg.Conclusion. Results of phase I clinical trial demonstrated good tolerability of single intravenous infusions of Angipur (0,015, 0,05 и 0,09 mg/kg) in healthy subjects. We determined key PK parameters and indicated dose-dependent antiplatelet activity of Angipur.