Montelukast VersaFilm® is a unique drug opportunity for the treatment of neurodegenerative diseases of the brain, such as mild cognitive impairment, Alzheimer’s disease and dementia.

IntelGenx is working to repurpose Montelukast as a therapeutic to treat neurodegenerative diseases by re-formulating the drug using VersaFilm®, IntelGenx’ proprietary thin film technology.

Currently, Montelukast is marketed as Singulair® (Merck & Co.), a once daily tablet for the chronic treatment of asthma and seasonal allergic rhinitis. The drug was first approved by the U.S. Food and Drug Administration in 1997 and has a very good safety profile. Montelukast is a leukotriene receptor antagonist used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. Montelukast is a CysLT1antagonist; it blocks the action of leukotriene D4 (and secondary ligands LTC4 and LTE4) on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it. This reduces the bronchoconstriction otherwise caused by the leukotriene and results in less inflammation. 

IntelGenx' proprietary VersaFilm® technology offers several potential advantages over the tablet form of Montelukast, including the avoidance and minimization of first-pass-effects, improved API bioavailability, lower dosing and toxicity, easier swallowing and better patience compliance.

In a recent Phase I study, IntelGenx demonstrated that an oral film formulation of Montelukast is safe and tolerable in healthy subjects, reduces the first-pass-effect and has a 52% higher bioavailability compared to the regular Montelukast tablet, demonstrating a clear advantage of delivering Montelukast via film. IntelGenx' Montelukast VersaFilm® also crossed the blood-brain barrier, an essential feature for treating degenerative brain diseases.

IntelGenx is currently preparing for a Phase 2a proof of concept study to assess the safety, feasibility, tolerability, and efficacy of Montelukast VersaFilm® in patients with mild to moderate Alzheimer's Disease.

More Information

IntelGenx Montelukast Poster – Alzheimer’s Association International Conference 2018

2018 Alzheimer’s disease facts and figures

Researchers are discovering the first approach to healing Alzheimer's

Montekulast and Rejuvenation of the Aged Brain

Singulair® is a registered trademark of Merck & Co., Inc.