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.