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Crisdesalazine

Experimental anti-inflammatory drug From Wikipedia, the free encyclopedia

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]

Trade namesGedaCure
Other namesAAD-2004; AAD2004
CAS Number
Quick facts Clinical data, Trade names ...
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
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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]

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