The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.

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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
DrugTargetPropertyMeasurementpHTemperature (°C)
CelecoxibProstaglandin G/H synthase 2IC 50 (nM)1000N/AN/ADetails
DiclofenacProstaglandin G/H synthase 1IC 50 (nM)150N/AN/ADetails
DiclofenacProstaglandin G/H synthase 2IC 50 (nM)50N/AN/ADetails
IndomethacinProstaglandin G/H synthase 1IC 50 (nM)20N/AN/ADetails
IndomethacinProstaglandin G/H synthase 1IC 50 (nM)200N/AN/ADetails
IndomethacinProstaglandin G/H synthase 2IC 50 (nM)500N/AN/ADetails
IndomethacinProstaglandin G/H synthase 2IC 50 (nM)30N/AN/ADetails
MeloxicamProstaglandin G/H synthase 1IC 50 (nM)1400N/AN/ADetails
MeloxicamProstaglandin G/H synthase 2IC 50 (nM)700N/AN/ADetails
RofecoxibProstaglandin G/H synthase 1IC 50 (nM)19000N/AN/ADetails
RofecoxibProstaglandin G/H synthase 1IC 50 (nM)>15000N/AN/ADetails
RofecoxibProstaglandin G/H synthase 2IC 50 (nM)20N/AN/ADetails
RofecoxibProstaglandin G/H synthase 2IC 50 (nM)500N/AN/ADetails