Crisdesalazine

Last updated

Crisdesalazine
Crisdesalazine.svg
Clinical data
Trade names GedaCure
Other namesAAD-2004; AAD2004
Drug class Microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor; Free radical scavenger
Identifiers
  • 2-hydroxy-5-[2-[4-(trifluoromethyl)phenyl]ethylamino]benzoic acid
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
Chemical and physical data
Formula C16H14F3NO3
Molar mass 325.287 g·mol−1
3D model (JSmol)
  • C1=CC(=CC=C1CCNC2=CC(=C(C=C2)O)C(=O)O)C(F)(F)F
  • InChI=1S/C16H14F3NO3/c17-16(18,19)11-3-1-10(2-4-11)7-8-20-12-5-6-14(21)13(9-12)15(22)23/h1-6,9,20-21H,7-8H2,(H,22,23)
  • Key:UTMVACIBQLDZLP-UHFFFAOYSA-N

Crisdesalazine (INN Tooltip International Nonproprietary Name; 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]

Contents

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

References

  1. 1 2 3 "Crisdesalazine". AdisInsight. 21 February 2023. Retrieved 19 October 2024.
  2. 1 2 3 4 5 Nango H, Tsuruta K, Miyagishi H, Aono Y, Saigusa T, Kosuge Y (June 2023). "Update on the pathological roles of prostaglandin E2 in neurodegeneration in amyotrophic lateral sclerosis". Translational Neurodegeneration. 12 (1) 32. doi: 10.1186/s40035-023-00366-w . PMC   10278279 . PMID   37337289.
  3. 1 2 3 Dunkel P, Chai CL, Sperlágh B, Huleatt PB, Mátyus P (September 2012). "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. doi:10.1517/13543784.2012.703178. PMID   22741814.
  4. ↑ "GNT Pharma's GedaCure® Approved for the Treatment of Dogs With Cognitive Dysfunction Syndrome". BioSpace. 10 February 2021. Retrieved 19 October 2024.
  5. 1 2 Pereira-Leite C, Nunes C, Jamal SK, Cuccovia IM, Reis S (July 2017). "Nonsteroidal Anti-Inflammatory Therapy: A Journey Toward Safety". Medicinal Research Reviews. 37 (4): 802–859. doi:10.1002/med.21424. PMID   28005273.
  6. ↑ Lima IV, Bastos LF, Limborço-Filho M, Fiebich BL, de Oliveira AC (2012). "Role of prostaglandins in neuroinflammatory and neurodegenerative diseases". Mediators of Inflammation. 2012 946813. doi: 10.1155/2012/946813 . PMC   3385693 . PMID   22778499.
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