Pharmacokinetics of a new Autogel formulation of the somatostatin analogue lanreotide after a single subcutaneous dose in healthy volunteers

Abstract

Abstract The pharmacokinetics/tolerability of lanreotide Autogel have been evaluated. Healthy volunteers (n = 24) first received immediate-release lanreotide as a single subcutaneous (s.c.) injection. After two days, 40 or 60 mg lanreotide Autogel was injected subcutaneously. Blood was sampled at various intervals for 56 days. Systemic/local adverse events and changes in biological profile/vital signs were recorded. Lanreotide Autogel produced a prolonged-release pharmacokinetic profile: mean area under the serum concentration-time curve from time 0 to infinity (AUC) was 53.73 + 8.99 and 79.48 + 13.06 ng mL−1 day for 40 and 60 mg, respectively, mean peak serum concentration (Cmax) was 4.38 + 2.91 and 5.71 + 3.52 ng mL−1, respectively, median time to reach Cmax (minimum-maximum) was 0.50 (0.083–18.0) and 0.38 (0.083–9.01) days, respectively, mean apparent elimination half-life was 21.63 + 9.42 and 22.01 + 9.87 days, respectively, and relative bioavailability was 0.93 + 0.12 and 0.82 + 0.15, respectively. Thus, lanreotide Autogel exhibited linear pharmacokinetics for the doses studied. Pharmacokinetic profiles were similar in both genders, apart from statistically significant differences in Cmax and Cmax/AUC. The Autogel formulation of lanreotide was well tolerated, with systemic adverse events being mild/moderate. Erythema and a painless subcutaneous induration were the most common local adverse events. Lanreotide Autogel provided a prolonged dosing interval and good tolerability for treating acromegaly and carcinoid syndrome.