Chemistry:Crisdesalazine
Crisdesalazine (INN; developmental code name AAD-2004) is a microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor and free radical scavenger which is under development for the treatment of Alzheimer's disease, amyotrophic lateral sclerosis (ALS), depressive disorders, Parkinson's disease, and spinal muscular atrophy.[1][2][3] It was also under development for the treatment of arthritis, diabetes, pain, and pancreatitis, but development for these indications was discontinued.[1] Crisdesalazine is also approved under the brand name GedaCure for treatment of dogs with canine cognitive dysfunction.[4]
Background
The drug was derived from salicylic acids like mesalazine (5-aminosalicylate), aspirin (acetylsalicylate), and sulfasalazine.[2] By inhibiting mPGES-1 (also known as prostaglandin E synthase (PTGES)), it blocks prostaglandin E2 production.[2][5] Crisdesalazine is described as having a dual action, additionally acting as a direct free radical scavenger.[2] Crisdesalazine is described as having anti-inflammatory, antioxidant, and neuroprotective effects.[3] It seems to have potentially superior therapeutic effects compared to nonsteroidal anti-inflammatory drugs (NSAIDs; or cyclooxygenase inhibitors) like ibuprofen, for instance having better selectivity and safety.[2][5]
As of February 2023, crisdesalazine is in phase 1 clinical trials for Alzheimer's disease, amyotrophic lateral sclerosis (ALS), depressive disorders, and Parkinson's disease and is in the preclinical stage of development for spinal muscular atrophy.[1] It was first described in the scientific literature in 2012.[6][3]
See also
- List of investigational antidepressants
- List of investigational Parkinson's disease drugs
- Selegiline § Veterinary use
References
- ↑ 1.0 1.1 1.2 "Crisdesalazine". 21 February 2023. https://adisinsight.springer.com/drugs/800032805.
- ↑ 2.0 2.1 2.2 2.3 2.4 "Update on the pathological roles of prostaglandin E2 in neurodegeneration in amyotrophic lateral sclerosis". Translational Neurodegeneration 12 (1). June 2023. doi:10.1186/s40035-023-00366-w. PMID 37337289.
- ↑ 3.0 3.1 3.2 "Clinical utility of neuroprotective agents in neurodegenerative diseases: current status of drug development for Alzheimer's, Parkinson's and Huntington's diseases, and amyotrophic lateral sclerosis". Expert Opinion on Investigational Drugs 21 (9): 1267–1308. September 2012. doi:10.1517/13543784.2012.703178. PMID 22741814. http://scholarbank.nus.edu.sg/handle/10635/106630.
- ↑ "GNT Pharma's GedaCure® Approved for the Treatment of Dogs With Cognitive Dysfunction Syndrome". 10 February 2021. https://www.biospace.com/gnt-pharma-s-gedacure-approved-for-the-treatment-of-dogs-with-cognitive-dysfunction-syndrome.
- ↑ 5.0 5.1 "Nonsteroidal Anti-Inflammatory Therapy: A Journey Toward Safety". Medicinal Research Reviews 37 (4): 802–859. July 2017. doi:10.1002/med.21424. PMID 28005273.
- ↑ "Role of prostaglandins in neuroinflammatory and neurodegenerative diseases". Mediators of Inflammation 2012. 2012. doi:10.1155/2012/946813. PMID 22778499.
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