Purpose: Efsitora is an insulin receptor agonist designed for once-weekly administration. Injection region preference varies among people with diabetes. This study compared the pharmacokinetic profile of efsitora when administered subcutaneously (SC) into the abdomen, upper arm, or thigh. An intravenous (IV) bolus administration was included to determine the absolute bioavailability.
Method: This was a single-center, 2-part, randomized study conducted in healthy participants. Part A was a parallel design to assess the relative bioavailability of efsitora following a single 100U dose administered SC into the upper arm or thigh, compared to the abdominal wall (N=153). Part B was a 2 period, crossover design to determine the absolute bioavailability of efsitora following a single 100U dose administered SC into the abdominal wall compared to a 44U IV administration (N=10). Blood was sampled for pharmacokinetics for 65 days (~9 weeks) post-dose.
Results: All 90% CIs for the ratios of total efsitora exposure or maximum efsitora concentration of the thigh or upper arm, vs abdomen were contained within 0.80 and 1.25. The absolute bioavailability was 86% into the abdominal wall. Efsitora was well tolerated after single SC injections and IV bolus administration.
Conclusion: Efsitora can be injected SC into the abdomen, upper arm, or thigh, without a change in exposure.
J. Leohr: None. S. Suriyapperuma: Employee; Eli Lilly and Company. A. Ghosh: None. D.G. Waters: Employee; Eli Lilly and Company. T. Fukuda: Employee; Eli Lilly and Company.
