Context: LB03002 is a novel sustained-release GH preparation administered once weekly.

Objective: To examine the pharmacokinetics, pharmacodynamics and safety of LB03002 vs. daily GH.

Design and Setting: This open-label, cross-over study compared the pharmacokinetics and pharmacodynamics of LB03002 and daily GH

Patients and Other Participants: Six male and 3 female patients with adult GH deficiency (AGHD) participated in the single-center study.

Intervention: Subjects were on stable daily GH treatment before the study. Following a 4-week washout with no GH, 5 weekly doses of LB03002 were given.

Main Outcome Measure: GH and IGF-I concentrations were measured during the last dose of daily GH and during the first and fifth weekly doses of LB03002.

Results: Serum GH C_max was approximately doubled after LB03002 (6.1 ± 3.2 and 4.5 ± 2.2 µg/l at first and fifth doses) compared with daily GH (2.7 ± 2.2 µg/l). A sustained increase in GH concentration for more than 48 h was observed with LB03002, such that AUC/dose was not significantly different between daily GH and LB03002. Mean IGF-I C_max was 34-41% greater with LB03002 than with daily GH and AUC was 7-fold greater. However, normalized to GH dose, AUC IGF-I was comparable. Adverse events and local reactions were acceptable and there were no evident safety concerns with LB03002.

Conclusions: Multiple weekly doses of LB03002 appeared safe and well tolerated. Comparable GH bioavailability and sustained IGF-I elevations support the use of once weekly LB03002 to replace daily GH therapy.