Drug evaluation: apratastat, a novel TACE/MMP inhibitor for rheumatoid arthritis.
Wyeth Research was developing apratastat (TMI-005), one in a series of dual TNFalpha-converting enzyme and matrix metalloprotease-13 inhibitors, for the potential treatment of inflammation, especially rheumatoid arthritis. By January 2005, apratastat had entered a phase II clinical trial; however, in October 2006, Wyeth reported that it had terminated development of the drug because of lack of efficacy in this trial.
Thabet
Mohamed M
MM
Leiden University Medical Center, Department of Rheumatology, Albinusdreef 2, 2300 RC Leiden, The Netherlands. M.Thabet@lumc.nl
Huizinga
Tom W J
TW
D051722:ADAM Proteins / Q000037:antagonists & inhibitors*; D000072198:ADAM17 Protein; D000818:Animals; D019540:Area Under Curve; D001172:Arthritis, Rheumatoid / Q000188:drug therapy*; D017321:Clinical Trials, Phase I as Topic; D017322:Clinical Trials, Phase II as Topic; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006207:Half-Life; D006801:Humans; D061965:Matrix Metalloproteinase Inhibitors; D051379:Mice; D008807:Mice, Inbred BALB C; D015394:Molecular Structure; D009025:Morpholines / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D010330:Patents as Topic; D051381:Rats; D011917:Rats, Inbred Lew; D016896:Treatment Outcome
D061965:Matrix Metalloproteinase Inhibitors; D009025:Morpholines; C484302:apratastat; D051722:ADAM Proteins; D000072198:ADAM17 Protein; C000606462:ADAM17 protein, human; C000606463:Adam17 protein, mouse; C000606464:Adam17 protein, rat