Crisdesalazine

Crisdesalazine
Clinical data
Trade namesGedaCure
Other namesAAD-2004; AAD2004
Drug classMicrosomal 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
FormulaC16H14F3NO3
Molar mass325.287 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 (INNTooltip 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]

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. ^ a b c "Crisdesalazine". AdisInsight. 21 February 2023. Retrieved 19 October 2024.
  2. ^ a b c d e 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. ^ a b c 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. ^ a b 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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