The company has reported results from its ARIA-1 study in healthy volunteers with the drug candidate AQ280, a selective proprietary JAK1 inhibitor, being developed as a treatment for eosinophilic esophagitis (EoE) within the Regulus program.
Healthy subjects were administered single or multiple doses in a sequential escalating dosing schedule until the maximum planned dose of AQ280 was reached, describes the company in a press release. Data describing the pharmacokinetic profile, safety and pharmacodynamic biomarkers of the drug candidate have now been unblinded and evaluated.
“These results represent the first clinical data with our drug candidate AQ280 and it is a valuable milestone both in the Regulus program and for Aqilion. We are very pleased with the results, and taken together these data encourages us to progress our preparations for Phase 2 in patients with eosinophilic esophagitis,” says Sarah Fredriksson, CEO Aqilion.
Key findings according to the company
Dose: The achieved exposures in the Single Ascending Dose (SAD)- and the Multiple Ascending Dose (MAD) cohorts are in line with estimates of a therapeutically effective range based on preclinical models and will inform the dose selection for the upcoming phase 2 trial.
Safety: There were no serious adverse events and the dose escalations in SAD and MAD were not restricted by adverse events.
Pharmacokinetics: The exposure and half-life for AQ280 were well aligned with the preclinical predictions and supports once daily dosing. Food intake did not influence the pharmacokinetics in any significant way.
Pharmacodynamics: AQ280 inhibited CXCL10 in a dose-dependent manner. CXCL10 is a well-recognized biomarker for JAK inhibition.
Selectivity: The JAK1 on-target effects were evident, and dose related, and there was only minimal effects on reticulocyte values, a marker of JAK2 inhibition.
Photo of Sarah Fredriksson: Aqilion