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| Clinical data | |
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| Drug class | Nonsteroidal estrogen;Nuclear factor κB inhibitor |
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| Formula | C34H31F3N2O2 |
| Molar mass | 556.629 g·mol−1 |
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WAY-204688, also known asSIM-688, is asyntheticnonsteroidal estrogen andnuclear factor κB (NF-κB) inhibitor which was originated by ArQule andWyeth and was under development by Wyeth for the treatment ofrheumatoid arthritis, non-specificinflammation, andsepsis but was never marketed.[1][2][3] It is a "pathway-selective"estrogen receptor (ER)ligand which inhibits NF-κB with anIC50Tooltip half-maximal inhibitory concentration of 122 nM and withmaximal inhibition relative toestradiol of 94%.[3][4] Inhibition of NF-κB by WAY-204688 appears to be dependent onagonism of theERα, as it is reversed by theERα antagonistfulvestrant, but is not dependent on theERβ.[3][4] In contrast to the case of NF-κB inhibition, WAY-204688 produces only slight elevation ofcreatine kinasein vitro, a measure of classical estradiol effects.[3][4] It reachedphase Iclinical trials prior to the discontinuation of its development.[1]
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