Atrogi Doses First Patients in Phase 1 Trial of Exercise-Mimicking Drug ATR-258
核心洞察
Swedish biotech Atrogi (搜索) has dosed the first subjects in a Phase 1 trial evaluating ATR-258, an oral therapy that mimics exercise effects by driving fat loss, increasing muscle, and improving metabolism.
The 8-week study will examine biased β2-adrenergic receptor (搜索) signaling in overweight male volunteers receiving daily oral ATR-258 dosing to measure muscle physiological effects.
ATR-258 represents a first-in-class GRK2 (搜索)-biased β2-agonist designed to unlock therapeutic potential while avoiding cardiovascular side effects typically associated with this drug class.
Swedish clinical-stage biotech company Atrogi (搜索) has announced the dosing of first subjects in a Phase 1 trial evaluating ATR-258, a first-in-class oral therapy designed to mimic the effects of exercise by driving fat loss, increasing muscle mass, and improving metabolism. The study represents a significant milestone for the company's novel approach to treating metabolic and muscle-wasting conditions.
Novel Mechanism Targets β2-Adrenergic Signaling
The 8-week, investigator-initiated interventional study will examine biased β2-adrenergic receptor (搜索) (β2-AR) signaling in human skeletal muscle using overweight male volunteers. Participants will receive daily oral dosing of ATR-258, Atrogi (搜索)'s GRK-selective long-acting β2-agonist, with the study designed to measure how effectively the candidate recapitulates the muscle physiological effects of classic β2 agonists.
"This trial will allow us to rigorously interrogate targeted downstream effector signaling associated with the β2-adrenergic receptor (搜索) in human skeletal muscle using a highly selective next generation modulator," said Morten Hostrup, Associate Professor at the University of Copenhagen and Principal Investigator of the study. "By combining detailed muscle physiological measurements with advanced molecular readouts, we aim to better understand how biased β2-adrenergic signaling regulates muscle growth and function."
Breakthrough Technology Addresses Safety Concerns
ATR-258 utilizes Atrogi (搜索)'s novel GRK2 (搜索)-biased signaling pathway approach, which was validated through a landmark study published in Cell in June 2025. This breakthrough technology enables the development of next-generation, highly selective β2-agonists for chronic use while avoiding the cardiovascular side effects typically associated with this therapeutic approach.
The Cell publication also detailed first-in-human trial data from a 69-subject Phase 1 trial, demonstrating the safety and tolerability of ATR-258 in both healthy volunteers and patients with type 2 diabetes (搜索).
Broad Therapeutic Potential
The study aims to evaluate ATR-258's potential across a range of muscle atrophic conditions. According to Hostrup, the therapy could potentially be harnessed to "preserve, or even augment, muscle function in various conditions of muscle wasting (搜索), such as immobilization, aging, and weight loss."
Professor Tore Bengtsson, Chief Scientific Officer and Founder of Atrogi (搜索), emphasized the significance of having Hostrup, whom he described as "widely recognised as the leading expert in the field," leading the investigation into ATR-258's muscle signaling effects.
Clinical Development Milestone
Paul Little, CEO at Atrogi (搜索), highlighted the importance of this development milestone: "The initiation of this study, and dosing of the first subjects, marks an important milestone for Atrogi. With safety established in Phase 1 and a validated mechanism of action, the generation of key muscle physiology data from this trial will underpin ATR-258's further development across metabolic and muscle-wasting conditions."
The company expects to share results from the trial later this year. Additional information on the study can be found on clinicaltrials.gov under NCT identifier NCT07421024.