title: Pharmacokinetics of a new Autogel formulation of the somatostatin analogue lanreotide after a single subcutaneous dose in healthy volunteers.
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 (C(max)) was 4.38 +/- 2.91 and 5.71 +/- 3.52 ng mL(-1), respectively, median time to reach C (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 C(max) and C(max)/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.
authors.affiliation: Centre d'Investigació de Medicaments, Institute of Research, Servei de Farmacologia Clínica, Hospital of Santa Creu and Sant Pau, Departament de Farmacologia i Terapèutica, UAB Barcelona, Spain.
authors.forename: R M
authors.initials: RM
authors.lastname: Antonijoan
authors.forename: M J
authors.initials: MJ
authors.lastname: Barbanoj
authors.forename: J A
authors.initials: JA
authors.lastname: Cordero
authors.forename: C
authors.initials: C
authors.lastname: Peraire
authors.forename: R
authors.initials: R
authors.lastname: Obach
authors.forename: J
authors.initials: J
authors.lastname: Vallès
authors.forename: R
authors.initials: R
authors.lastname: Chérif-Cheikh
authors.forename: M-L
authors.initials: ML
authors.lastname: Torres
authors.forename: F
authors.initials: F
authors.lastname: Bismuth
authors.forename: M
authors.initials: M
authors.lastname: Montes
mesh_terms: D000293:Adolescent; D000328:Adult; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D019540:Area Under Curve; D003692:Delayed-Action Preparations; D005260:Female; D006207:Half-Life; D006801:Humans; D007279:Injections, Subcutaneous; D008297:Male; D008657:Metabolic Clearance Rate; D010456:Peptides, Cyclic / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D013004:Somatostatin / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives / Q000493:pharmacokinetics*
chemical_list: D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D010456:Peptides, Cyclic; C060347:lanreotide; D013004:Somatostatin