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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 as SIM-688, is a synthetic nonsteroidal estrogen and nuclear factor κB (NF-κB) inhibitor which was originated by ArQule and Wyeth and was under development by Wyeth for the treatment of rheumatoid arthritis, non-specific inflammation, and sepsis but was never marketed.[1][2][3] It is a "pathway-selective" estrogen receptor (ER) ligand which inhibits NF-κB with an IC50Tooltip half-maximal inhibitory concentration of 122 nM and with maximal inhibition relative to estradiol of 94%.[3][4] Inhibition of NF-κB by WAY-204688 appears to be dependent on agonism of the ERα, as it is reversed by the ERα antagonist fulvestrant, but is not dependent on the ERβ.[3][4] In contrast to the case of NF-κB inhibition, WAY-204688 produces only slight elevation of creatine kinase in vitro, a measure of classical estradiol effects.[3][4] It reached phase I clinical trials prior to the discontinuation of its development.[1]
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