The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.
Article Details
- CitationCopy to clipboard
Prasit P, Wang Z, Brideau C, Chan CC, Charleson S, Cromlish W, Ethier D, Evans JF, Ford-Hutchinson AW, Gauthier JY, Gordon R, Guay J, Gresser M, Kargman S, Kennedy B, Leblanc Y, Leger S, Mancini J, O'Neill GP, Ouellet M, Percival MD, Perrier H, Riendeau D, Rodger I, Zamboni R, et al.
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.
Bioorg Med Chem Lett. 1999 Jul 5;9(13):1773-8.
- PubMed ID
- 10406640 [ View in PubMed]
- Abstract
The development of a COX-2 inhibitor rofecoxib (MK 966, Vioxx) is described. It is essentially equipotent to indomethacin both in vitro and in vivo but without the ulcerogenic side effect due to COX-1 inhibition.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Celecoxib Prostaglandin G/H synthase 2 IC 50 (nM) 1000 N/A N/A Details Diclofenac Prostaglandin G/H synthase 1 IC 50 (nM) 150 N/A N/A Details Diclofenac Prostaglandin G/H synthase 2 IC 50 (nM) 50 N/A N/A Details Indomethacin Prostaglandin G/H synthase 1 IC 50 (nM) 20 N/A N/A Details Indomethacin Prostaglandin G/H synthase 1 IC 50 (nM) 200 N/A N/A Details Indomethacin Prostaglandin G/H synthase 2 IC 50 (nM) 500 N/A N/A Details Indomethacin Prostaglandin G/H synthase 2 IC 50 (nM) 30 N/A N/A Details Meloxicam Prostaglandin G/H synthase 1 IC 50 (nM) 1400 N/A N/A Details Meloxicam Prostaglandin G/H synthase 2 IC 50 (nM) 700 N/A N/A Details Rofecoxib Prostaglandin G/H synthase 1 IC 50 (nM) 19000 N/A N/A Details Rofecoxib Prostaglandin G/H synthase 1 IC 50 (nM) >15000 N/A N/A Details Rofecoxib Prostaglandin G/H synthase 2 IC 50 (nM) 20 N/A N/A Details Rofecoxib Prostaglandin G/H synthase 2 IC 50 (nM) 500 N/A N/A Details