Safety, tolerability, and serum/tear pharmacokinetics of human
recombinant epidermal growth factor eyedrops in healthy subjects
Abstract
Aims: The aim of this study was to evaluate the safety/tolerability, and
pharmacokinetics (PKs) of rhEGF eyedrops after administration of a
single and multiple doses in healthy subjects. Methods: A phase 1,
randomized, double-blind, placebo-controlled, and single ascending dose
(SAD) and multiple ascending dose (MAD) study were conducted in 3 dose
groups (10, 50, and 100 μg/mL). The subjects randomly received rhEGF
eyedrops or their placebo in a 3:1 ratio. Serial blood and tear samples
for PK analysis were collected up to 36 h and 180 h post-dose in SAD and
MAD study, respectively. In addition, the serum and tear EGF
concentrations were measured. Immunogenicity evaluations were conducted
using serum anti-EGF antibody level. Results: A total of 50 subjects
were enrolled and 48 subjects completed the study. Adverse drug
reactions were mild and transient. There were no serious adverse events
in this study. The tear EGF concentrations rapidly increased and
returned to baseline after 4 hours without serum EGF level change after
the administration of rhEGF eyedrops. Conclusion: rhEGF eyedrops were
safe and well-tolerated in healthy subjects in a dose range of 10-100
μg/mL, which indicated it was suitable for further studies for corneal
injury patients.