Relative Bioavailability of a Single Dose of Belimumab Administered Subcutaneously by Prefilled Syringe or Autoinjector in Healthy Subjects. Issue 3 (4th December 2015)

• Record Type: Journal Article
• Authors: Struemper, Herbert; Murtaugh, Thomas; Gilbert, Jane; Barton, Matthew E.; Fire, Joseph; Groark, James; Fox, Norma Lynn; Roth, David; Gordon, David
• Is Part Of: Clinical pharmacology in drug development. Volume 5:Issue 3(2016:May/Jun.)
• Page Start: 208
• Page End: 215
• Publication Date: 2015-12-04
• Subjects: autoinjector -- belimumab -- bioavailability -- pharmacokinetics -- subcutaneous; Drugs -- Testing -- Periodicals; Drug development -- Periodicals; Clinical pharmacology -- Periodicals; 615.580724
• DOI: 10.1002/cpdd.219
• Languages: English
• ISSNs: 2160-7648

Abstract

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.