The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.
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.
Prasit
P
P
Merck Frosst Centre for Therapeutic Research, Pointe Claire-Dorval, Québec, Canada.
Wang
Z
Z
Brideau
C
C
Chan
C C
CC
Charleson
S
S
Cromlish
W
W
Ethier
D
D
Evans
J F
JF
Ford-Hutchinson
A W
AW
Gauthier
J Y
JY
Gordon
R
R
Guay
J
J
Gresser
M
M
Kargman
S
S
Kennedy
B
B
Leblanc
Y
Y
Léger
S
S
Mancini
J
J
O'Neill
G P
GP
Ouellet
M
M
Percival
M D
MD
Perrier
H
H
Riendeau
D
D
Rodger
I
I
Zamboni
R
R
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D016466:CHO Cells; D006224:Cricetinae; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D007213:Indomethacin / Q000009:adverse effects / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D007527:Isoenzymes / Q000737:chemistry*; D007783:Lactones / Q000008:administration & dosage / Q000009:adverse effects / Q000138:chemical synthesis* / Q000494:pharmacology*; D008565:Membrane Proteins; D011451:Prostaglandin-Endoperoxide Synthases / Q000737:chemistry*; D051381:Rats; D013450:Sulfones
D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D004791:Enzyme Inhibitors; D007527:Isoenzymes; D007783:Lactones; D008565:Membrane Proteins; D013450:Sulfones; C116926:rofecoxib; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; C496511:PTGS1 protein, human; C496540:PTGS2 protein, human; D011451:Prostaglandin-Endoperoxide Synthases; C496513:Ptgs1 protein, rat; D007213:Indomethacin