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masitinib (Masican)
Indications:
- prevention of severe asthma exacerbation in patients with eosinophil count of >= 150/uL
- pending FDA approval for amyotrophic lateral sclerosis (ALS)
- may slow cognitive deterioration & improve function in Alzheimer's disease [3]
Dosage:
- start: 4.5 mg/kg/day PO
- maximum: 6 mg/kg/day PO (no benefit of 6 vs 4.5 mg/kg/day for AD) [3]
Adverse effects:
- gastrointestinal disorders
- edema
- rash [4]
Mechanism of action:
- macrophage colony stimulating factor 1 receptor (CSF1R) inhibitor
- targets mast cells & macrophages including neurotoxic aberrant glial cells (resident macrophages in the brain) via CSF1R inhibition
- provides a neuroprotective effect & attenuates neurodegeneration Clinical trials
- in phase 3 trial [1]
- phase 2 Alzheimer's disease: 24 weeks, patients already taking cholinesterase inhibitor &/or memantine for at least 6 months
- measures: ADAS-Cog score & ADCS-ADL scale
Notes:
- Cost: $288 for 200 mg.
- at a dose of 4.5 mg/kg/day, cost for a 70 kg person would be $450/day
General
small inhibitory antineoplastic agent (ib drug)
Database Correlations
PUBCHEM correlations
References
- Frellick M
Oral Masitinib Phase 3 Results Promising for Severe Asthma
Medscape - Sep 11, 2020
https://www.medscape.com/viewarticle/937229
- Masitinib (Pending FDA Approval)
Medscape
https://reference.medscape.com/drug/masican-masitinib-1000208
- Brooks M
Repurposed Cancer Drug Shows Promise in Alzheimer's.
Medscape. August 5, 2021
https://www.medscape.com/viewarticle/956038
- Alzheimer's Association International Conference (AAIC) 2021:
Session 4-HO-04. Presented July 29, 2021.
- Alzforum: Masitinib
https://www.alzforum.org/therapeutics/masitinib
- Piette F, Belmin J, Vincent H, Schmidt N et al
Masitinib as an adjunct therapy for mild-to-moderate Alzheimer's disease:
a randomised, placebo-controlled phase 2 trial.
Alzheimers Res Ther. 2011 Apr 19;3(2):16
PMID: 21504563 PMCID: PMC3226277 Free PMC article