Development of a novel powder formulation for treatment of idiopathic pulmonary fibrosis

Wayne Morley¹, Irene Parisini¹, Martina Larini¹, Arnaud Fillius¹, Paola Zarantonello¹ Lise Gravelle² & Anders Pedersen²

¹Aptuit S.r.l, Via Alexander Fleming 4, Verona, 37135, Italy

²Galecto Biotech AB, Cobis Science Park, Ole Maaloes Vej 3, Copenhagen, DK-2200, Denmark

Summary

Idiopathic Pulmonary Fibrosis is a fatal disease that leads to a reduction in lung capacity. A novel inhalation formulation of TD139, a small molecule Galectin-3 inhibitor, was developed and a fast approach from formulation development to Phase I Clinical Supply was established under cGMP (current Good Manufacturing Practice) environment.  Four dose strengths were developed including two containing only API (Active Pharmaceutical Ingredient) without excipients (100% API) and two formulations containing 3% API, blended with Lactose using a high shear blender. Over a 3 month period the formulations demonstrated a stable FPD (Fine Particle Dose, as a percentage of label claim) at standard and stressed conditions (25°C/60%RH and 40°C/75%RH, respectively), indicating good stability and robustness of the formulations. The project showed market potential for the TD139 product, and an effective approach to manufacturing, with the first patient dosed within six months of starting the project.