Premium
Effect of injection site on relative bioavailability of exenatide (synthetic exendin‐4)
Author(s) -
Calara F.,
Taylor K.,
Han J.,
Aisporna M.,
Zabala E.,
Carr E.,
Fineman M.
Publication year - 2004
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1016/j.clpt.2003.11.221
Subject(s) - exenatide , cmax , medicine , abdomen , pharmacokinetics , bioavailability , geometric mean , crossover study , type 2 diabetes , urology , pharmacology , gastroenterology , diabetes mellitus , endocrinology , surgery , mathematics , geometry , alternative medicine , pathology , placebo
Exenatide is an incretin mimetic with glucoregulatory activity in patients with type 2 diabetes. Here we report the results of a randomized, open‐label, crossover study to assess the relative bioavailability of subcutaneous exenatide injected into arm or thigh vs abdomen. The study enrolled 28 subjects with type 2 diabetes: age 56.2±8.ly; BMI 33.0±5.1 kg/m 2 ; HbA 1c , 8.0±1.7% (±SD). Subjects had a single 10 μg injection of exenatide followed by 10 h of plasma sampling. Geometric LS mean exenatide AUC 0‐infin values were 63935±6608 pg*min/mL (abdomen; ±SEM), 59573±6157 pg*min/mL (arm), 62148±6424 pg*min/mL (thigh). The AUC geometric LS mean ratio for arm vs abdomen was 0.93 with geometric 90% CI ratios of 0.82 to 1.05; and for thigh vs abdomen was 0.97, geometric 90% CI ratios 0.86 to 1.1. Geometric LS mean exenatide C max values were 220±24 pg/mL (abdomen), 218±23 pg/mL (arm), and 193±21 pg/mL (thigh). The C max geometric LS mean ratio for arm vs abdomen was 0.99 with geometric 90% CI ratios of 0.85 to 1.15, and for thigh vs abdomen was 0.88, geometric 90% CI ratios 0.75 to 1.02. The most common treatment‐emergent adverse events were mild‐to‐moderate nausea, vomiting, and headache. In summary, all injection sites yielded equivalent pharmacokinetic profiles. Clinical Pharmacology & Therapeutics (2004) 75 , P58–P58; doi: 10.1016/j.clpt.2003.11.221