Dataset Information

Pharmacokinetics and safety of a single dose of the novel necrosis inhibitor LC28-0126 in healthy male subjects.

ABSTRACT:

Aims

A novel necrosis inhibitor, LC28-0126, is expected to have a cellular protective effect from ischaemic reperfusion injury in acute myocardial infarction. The objective of this study was to investigate the safety, tolerability and pharmacokinetics of LC28-0126 after a single intravenous administration in healthy male subjects.

Methods

The study was a dose-block-randomized, double-blind, placebo-controlled, single ascending dose, first-in-human trial. Subjects were randomly assigned to receive 0.3, 1, 3, 10, 25, 50, 100 or 200 mg of LC28-0126. LC28-0126 was infused for 30 min and 5 min in cohorts 1 and 2, respectively. An interim analysis to assess the tolerability and pharmacokinetics was conducted in each dose group. Blood samples were taken to determine plasma LC28-0126 concentrations from predose to 48 or 144 h postdose, and urine samples were taken from predose to 48 or 72 h postdose.

Results

Overall, 89 subjects were randomly assigned to the dose groups of the two cohorts. LC28-0126 was well tolerated, and no serious adverse events were reported. LC28-0126 showed rapid disposition in the distribution phase. Overall, the fraction of unchanged LC28-0126 excreted during the 48 or 72 h after administration was below 5%. The systemic exposure of LC28-0126 tends to be increased in a dose-proportional manner in the dose range of 0.3-200 mg.

Conclusions

A single intravenous dose of LC28-0126 was safe and well tolerated up to 200 mg. Furthermore, LC28-0126 demonstrated a predictable pharmacokinetic profile after a single intravenous infusion of doses ranging from 0.3 to 200 mg.

SUBMITTER: Kim S

PROVIDER: S-EPMC5427235 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature

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Publications

Pharmacokinetics and safety of a single dose of the novel necrosis inhibitor LC28-0126 in healthy male subjects.

Kim Seokuee S Chung Hyewon H Lee SeungHwan S Cho Sang-Heon SH Cho Hyun-Jai HJ Kim Soon Ha SH Jang In-Jin IJ Yu Kyung-Sang KS

British journal of clinical pharmacology 20170125 6

<h4>Aims</h4>A novel necrosis inhibitor, LC28-0126, is expected to have a cellular protective effect from ischaemic reperfusion injury in acute myocardial infarction. The objective of this study was to investigate the safety, tolerability and pharmacokinetics of LC28-0126 after a single intravenous administration in healthy male subjects.<h4>Methods</h4>The study was a dose-block-randomized, double-blind, placebo-controlled, single ascending dose, first-in-human trial. Subjects were randomly ass ...[more]

PMID: 28002882

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Dataset Information

Pharmacokinetics and safety of a single dose of the novel necrosis inhibitor LC28-0126 in healthy male subjects.

Aims

Methods

Results

Conclusions

Publications

Pharmacokinetics and safety of a single dose of the novel necrosis inhibitor LC28-0126 in healthy male subjects.

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