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Polmacoxib Trade names Acelex Other names CG100649 ATC code
4-(3-(3-Fluorophenyl)-5,5-dimethyl-4-oxo-4,5-dihydrofuran-2-yl)-benzenesulfonamide
CAS Number PubChem CID ChemSpider UNII KEGG ChEMBL Formula C 18 H 16 F N O 4 S Molar mass 361.39 g·mol−1 3D model (JSmol )
CC1(C(=O)C(=C(O1)C2=CC=C(C=C2)S(=O)(=O)N)C3=CC(=CC=C3)F)C
InChI=1S/C18H16FNO4S/c1-18(2)17(21)15(12-4-3-5-13(19)10-12)16(24-18)11-6-8-14(9-7-11)25(20,22)23/h3-10H,1-2H3,(H2,20,22,23)
Key:IJWPAFMIFNSIGD-UHFFFAOYSA-N
Polmacoxib (trade name Acelex ) is a nonsteroidal anti-inflammatory drug (NSAID) used to treat osteoarthritis . It was developed as CG100649 and approved for use in South Korea in February 2015.[1] It inhibits the enzymes carbonic anhydrase and COX-2 .
A study in healthy volunteers showed drug effects on urinary prostaglandin metabolites for both polmacoxib and celecoxib that suggest a similar cardiovascular risk profile.[2] Further work by this group developed dose-exposure relationships of polmacoxib to guide clinical development strategies.[3]
References [ ]
^ "CrystalGenomics Receives MFDS Approval for Acelex (Polmacoxib)" . PR Newswire.
^ Skarke C, Alamuddin N, Lawson JA, Cen L, Propert KJ, Fitzgerald GA (June 2012). "Comparative impact on prostanoid biosynthesis of celecoxib and the novel nonsteroidal anti-inflammatory drug CG100649" . Clinical Pharmacology and Therapeutics . 91 (6): 986–93. doi :10.1038/clpt.2012.3 . PMC 3740579 . PMID 22278334 .
^ Hirankarn S, Barrett JS, Alamuddin N, FitzGerald GA, Skarke C (October 2013). "GCG100649, A Novel Cyclooxygenase-2 Inhibitor, Exhibits a Drug Disposition Profile in Healthy Volunteers Compatible With High Affinity to Carbonic Anhydrase-I/II: Preliminary Dose-Exposure Relationships to Define Clinical Development Strategies". Clinical Pharmacology in Drug Development . 2 (4): 379–86. doi :10.1002/cpdd.47 . PMID 27121942 . S2CID 35992507 .
Non-steroidal anti-inflammatory drugs (NSAIDs) (primarily M01A and M02A , also N02BA )
pyrazolones /pyrazolidines salicylates acetic acid derivatives and related substancesoxicams propionic acid derivatives (profens)n -arylanthranilic acids (fenamates )COX-2 inhibitors (coxibs)other NSAID combinations Key: underline indicates initially developed first-in-class compound of specific group; # WHO-Essential Medicines ; † withdrawn drugs ; ‡ veterinary use .
Analgesics (N02A , N02B )
Opioids
Opiates /opium
Codeine #
Morphine # (+naltrexone )
Opium
Laudanum
Paregoric
Semisynthetic Synthetic
Paracetamol -typeNSAIDs
Propionates Oxicams Acetates COX-2 inhibitors Fenamates Salicylates Pyrazolones Others
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Ion channel modulators
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Alcohol (ethanol)
Gabapentin
Gabapentin enacarbil
Leconotide
Mirogabalin
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Ziconotide
Sodium blockers
Carbamazepine
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Local anesthetics (e.g., cocaine , lidocaine )
Mexiletine
Nefopam
Tricyclic antidepressants (e.g., amitriptyline # )
Potassium openers
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Carisoprodol
Chlorzoxazone
Cyclobenzaprine
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# WHO-EM
‡ Withdrawn from market
Clinical trials :
† Phase III
§ Never to phase III
Receptor (ligands )
DP (D2 )
DP1
Agonists: Prostaglandin D2
Treprostinil
DP2
EP (E2 )
EP1 EP2
Agonists:
Misoprostol
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Treprostinil
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Agonists: Beraprost
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Prostaglandin D2
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Ricinoleic acid
Sulprostone
EP4
Agonists: Lubiprostone
Misoprostol
Prostaglandin E1 (alprostadil)
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Unsorted
FP (F2α ) IP (I2 )
Agonists:
Beraprost
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Prostacyclin (prostaglandin I2 , epoprostenol)
Prostaglandin E1 (alprostadil)
Selexipag
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Agonists:
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U-46619
Unsorted
Enzyme (inhibitors )
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Retinoids
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PGES
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Precursors: Linoleic acid
γ-Linolenic acid (gamolenic acid)
Dihomo-γ-linolenic acid
Diacylglycerol
Arachidonic acid
Prostaglandin G2
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See also
Receptor/signaling modulators
Leukotriene signaling modulators
Categories :
Analgesics Nonsteroidal anti-inflammatory drugs COX-2 inhibitors Sulfonamides Experimental cancer drugs Musculoskeletal system drug stubs Hidden categories:
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