Xeris Pharmaceuticals, Inc. (NASDAQ:XERS), a specialty pharmaceutical company leveraging its novel formulation technology platforms to develop and commercialize ready-to-use injectable drug formulations, today announced that the company has completed enrollment and successfully dosed all participants in a Phase 1 study of levothyroxine (XP-8121) to evaluate the pharmacokinetics, safety and tolerability, and potential for weekly dosing of the investigational, novel, subcutaneous (SC) injection for the treatment of hypothyroidism.
XP-8121 is a novel formulation that could potentially mitigate many of the challenges associated with oral formulations, such as identification of an ideal dose due to absorption variation and medication adherence for patients who have difficulty maintaining a stable, therapeutic serum level. Preclinical studies of SC XP-8121 showed a sustained plasma exposure profile and similar maximum plasma concentration (Cmax) when compared with equivalent doses of the oral formulation.
The Phase 1 clinical study of levothyroxine (XP-8121) is a single ascending dose crossover design in 30 healthy participants to compare matching doses of oral levothyroxine (Synthroid®) and subcutaneous (SC) XP-8121. The primary endpoints of the study are to characterize the absorption and elimination kinetics of XP-8121 and compare bioavailability of XP-8121 to oral levothyroxine. Secondary endpoints are safety and tolerability of XP-8121. The study is being conducted in partnership with Dr. Danielle Armas and Celerion, a leading contract research organization with extensive experience performing first-in-human studies.
“The potential for a once weekly subcutaneous injection of levothyroxine would represent a promising novel approach in treating patients with hypothyroidism. Drug non-compliance, resistant hypothyroidism, and limited GI absorption are some of the major reasons for treatment failure or suboptimal treatment with oral levothyroxine. These challenges could be mitigated by XP-8121 and translate into the long-term health benefit of achieving a euthyroid state for patients,” said Dr. Armas, Senior Principal Investigator, Celerion.
“Because our levothyroxine formulation enables a small volume SC injection, as an injectable maintenance therapy, it may facilitate less frequent dosing. This may provide clinical advantages over the established oral daily route, by providing predictable bioavailability, comparable safety, and ease of use,” said Dr. Ken Johnson, Xeris’ Senior Vice President of Global Development and Medical Affairs.