Inhaled Oxytocin (GR121619) Safety, Tolerability, and PK Profile to be Assessed in Healthy Females

Postpartum hemorrhage (PPH) remains a leading cause of maternal mortality, particularly in resource-poor settings. The current gold standard, intramuscular (IM) oxytocin, faces significant challenges due to its requirement for refrigeration and administration by trained healthcare professionals (HCPs). These limitations compromise its stability and effectiveness where cold chain infrastructure is lacking. Exploring alternative, more stable, and easily administrable routes for oxytocin is critical to improve PPH prophylaxis globally, making the inhaled route a promising area of investigation.

This single-blind, ascending dose-escalation study is designed to evaluate the safety, tolerability, and pharmacokinetic (PK) profile of inhaled oxytocin. Fifteen healthy premenopausal female volunteers will be enrolled and assigned to one of two treatment sequences. Participants will receive up to four fixed escalating doses of inhaled oxytocin (GR121619): 50 mcg, 200 mcg, 400 mcg, and 600 mcg. Systemic exposure from these inhaled doses will be compared against a single 10 international units (IU) dose of IM oxytocin. The study will also assess the safety and tolerability of five non-pharmacologically active components used in the placebo formulation.

The abstract outlines the design of a first-in-human study for inhaled oxytocin, not its results. Researchers designed this single-blind, ascending dose-escalation study to evaluate the safety and tolerability of inhaled oxytocin and its placebo components. The primary objective is to establish the PK characteristics of up to four fixed escalating doses: 50 mcg, 200 mcg, 400 mcg, and 600 mcg. Systemic exposure from these inhaled doses will be compared against a single 10 IU intramuscular (IM) oxytocin dose. The study aims to determine if inhaled administration can achieve comparable systemic exposure to the established IM route, which is crucial for its potential as a prophylactic therapy for postpartum hemorrhage (PPH). The study will enroll a total of 15 subjects.

This study is specifically designed to be the first investigation of oxytocin in humans via the inhaled route, aiming to evaluate its safety, tolerability, and pharmacokinetics across escalating doses.