BC222 is an oligosaccharide grafted with anionic charges and amino acid moieties designed to speed up the absorption of insulin lispro in the BCLIS formulation. Non-clinical data indicated that BC222 is rapidly excreted unchanged by the kidney. This open label clinical trial conducted in 12 healthy volunteers [mean±SD age 31.4±9.5 years; weight 95.3±16.8 kg; BMI 28.6±4.1 kg/m²] investigated the PK properties and safety and tolerability of a single s.c. dose of BC222 (equal to the BC222 content in 1.0 U/kg BCLIS) using validated liquid chromatography mass spectrometry assays for BC222 in plasma and urine samples. BC222 was rapidly absorbed, with a median plasma Tmax of 1.2 h (Figure). BC222 was rapidly cleared from the blood with a mean terminal half-life of 2.07 (±0.52) h reaching baseline levels 10-12 h after administration. Urinary BC222 concentrations reached 95.4±4.5% of the injected dose within 12 h post-dosing and was as high as 9 % ± 5% of the total dose after 48h indicating that BC222 was completely absorbed from the s.c. tissue into the blood and quickly cleared via the urine. BC222 was well tolerated and safe with only two mild adverse events occurring in the whole study.

In conclusion, BC222 is completely absorbed after s.c. injection and rapidly excreted by the kidneys.

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Disclosure

G. Meiffren: Employee; Self; ADOCIA. Stock/Shareholder; Self; ADOCIA. L. Plum-Moerschel: None. A. Ranson: Employee; Self; ADOCIA. Stock/Shareholder; Self; ADOCIA. E. Anastassiadis: None. C. Seroussi: Employee; Self; ADOCIA. Stock/Shareholder; Self; ADOCIA. J. Correia: Employee; Self; ADOCIA. Stock/Shareholder; Self; ADOCIA. G. Andersen: None. M. Gaudier: Employee; Self; ADOCIA. Stock/Shareholder; Self; ADOCIA. O. Soula: Board Member; Self; ADOCIA. Stock/Shareholder; Self; ADOCIA. Employee; Spouse/Partner; ADOCIA. S. Glezer: Stock/Shareholder; Self; Sanofi. Stock/Shareholder; Spouse/Partner; Sanofi. Employee; Self; ADOCIA, Novo Nordisk Inc.. Employee; Spouse/Partner; Pfizer Inc., Teva Pharmaceutical Industries Ltd.. Stock/Shareholder; Spouse/Partner; Teva Pharmaceutical Industries Ltd.. B. Alluis: None.

© 2018 by the American Diabetes Association.
2018
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