Alzheimer's disease is one of the leading neurological disorders across the world. Therelevanceof treating Alzheimer's disease with masitinib was confirmed by the studies conducted by Francois Piette et al. The study was sponsored by AB Sciences, Paris, a pharmaceutical company specializing in the research, development and commercialization of protein kinase inhibitors (PKIs).
An important point in the pathogenesis of Alzheimer's disease is neuroinflammation. Mast cells are involved in the inflammation processes and influence the permeability of blood brain barrier. Masitinib is a selective inhibitor of tyrosine kinase and effectively inhibits the survival and activity of mast cells.
AdvertisementA placebo- controlled randomized phase 2 study was carried out in patients with mild to moderate Alzheimer's disease. In these patients, masitinib was administered as an adjunct to cholinesterase inhibitor and/ or memantine. The study included assigning masitinib with starting dose of 3 or 6 mg/kg/day or placebo randomly. The regime was given twice daily for 24 weeks. Alteration from the baseline in the Alzheimer's disease Assessment Scale-cognitive subscale (ADAS-Cog) was taken as the primary endpoint. After 12 and 24 weeks the rate of clinical cognitive lowering as per ADAS-Cog response was found to be lower with adjunctive treatment with masitinib in contrast to placebo (6% versus 50% for both time points). Significant improvements were noted with mastinib treatment on ADAS-Cog, ADCS-ADL (Alzheimer's Disease Cooperative Study - Activities of Daily Living), and Mini-Mental State Examination (MMSE), whereas the placebo treatment resulted in relative deterioration of the same.
The side- effects seen were mild to moderate in intensity and transient, more pronounced with masitinib treatment (65% versus 38% of patients). Strong adverse effects were observed almost at same occurrence rate with masitinib and placebo administration (15% versus 13% of patients, respectively). Gastrointestinal disorders, edema and rashes were the commonly seen mastinib- related side effects.
The studies concluded that masitinib add- on administration for 24 weeks resulted in improvement of Alzheimer's disease. The use of masitinib provided a pioneering opportunity for curing Alzheimer Disease.
1. Piette F et al. Masitinib as an Adjunct Therapy for Alzheimer's Disease published in Alzheimer's Research & Therapy 2011, 3: 16.