title: Relative Bioavailability of a Single Dose of Belimumab Administered Subcutaneously by Prefilled Syringe or Autoinjector in Healthy Subjects.
abstract: Intravenous belimumab is approved for the treatment of systemic lupus erythematosus; subcutaneous self-administration would enable greater patient access. This study assessed relative bioavailability, tolerability, and safety of 1 subcutaneous dose of self-administered belimumab by healthy subjects using a single-use autoinjector or prefilled syringe. Subjects (randomized 1:1:1:1) self-administered belimumab 200 mg subcutaneously (abdomen or thigh) by prefilled syringe or autoinjector. Pharmacokinetics, adverse events (AEs), injection-site pain, and administration errors were recorded. Of 81 subjects, 5 experienced administration errors and were excluded from pharmacokinetic analyses. Mean serum belimumab concentration profiles were similar for both devices, with a weak trend toward higher concentrations for thigh injection compared with abdominal injections. Maximum observed serum concentration was slightly higher with the autoinjector (27.0 vs 25.3 µg/mL) and area under the concentration-time curve slightly lower (701 vs 735 day · μg/mL), compared with the prefilled syringe. Incidence of AEs was 51% (41 of 81 subjects; headache was most common), with no serious or severe AEs. Median injection-site pain scores were low (0 after 1 hour). Device handling was reported as acceptable by ≥95% of autoinjector users and ≥90% of prefilled syringe users for each characteristic assessed. These results support the use of either device for belimumab subcutaneous administration.
authors.affiliation: PAREXEL, Research Triangle Park, NC, USA.
authors.forename: Herbert
authors.initials: H
authors.lastname: Struemper
authors.affiliation: Quintiles, Overland Park, KS, USA.
authors.forename: Thomas
authors.initials: T
authors.lastname: Murtaugh
authors.affiliation: GlaxoSmithKline, Hertfordshire, UK.
authors.forename: Jane
authors.initials: J
authors.lastname: Gilbert
authors.affiliation: GlaxoSmithKline, King of Prussia, PA, USA.
authors.forename: Matthew E
authors.initials: ME
authors.lastname: Barton
authors.affiliation: GlaxoSmithKline, Potomac, MD, USA.
authors.forename: Joseph
authors.initials: J
authors.lastname: Fire
authors.affiliation: GlaxoSmithKline, King of Prussia, PA, USA.
authors.forename: James
authors.initials: J
authors.lastname: Groark
authors.affiliation: GlaxoSmithKline, Potomac, MD, USA.
authors.forename: Norma Lynn
authors.initials: NL
authors.lastname: Fox
authors.affiliation: GlaxoSmithKline, King of Prussia, PA, USA.
authors.forename: David
authors.initials: D
authors.lastname: Roth
authors.affiliation: GlaxoSmithKline, King of Prussia, PA, USA.
authors.forename: David
authors.initials: D
authors.lastname: Gordon
mesh_terms: D000328:Adult; D061067:Antibodies, Monoclonal, Humanized / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D019540:Area Under Curve; D001682:Biological Availability; D005260:Female; D006801:Humans; D007166:Immunosuppressive Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D007279:Injections, Subcutaneous; D008297:Male; D010146:Pain / Q000453:epidemiology / Q000209:etiology*; D012646:Self Administration; D013594:Syringes; D055815:Young Adult
chemical_list: D061067:Antibodies, Monoclonal, Humanized; D007166:Immunosuppressive Agents; C511911:belimumab
keywords: autoinjector; belimumab; bioavailability; pharmacokinetics; subcutaneous