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| Drug class | Nonsteroidal estrogen; Nuclear factor κB inhibitor |
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| Formula | C34H31F3N2O2 |
| Molar mass | 556.629 g·mol |
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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. 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%. 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. 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. It reached phase I clinical trials prior to the "discontinuation of its development."
References※
- ^ "SIM 688 - AdisInsight".
- ^ Ivanenkov YA, "Balakin KV," Lavrovsky Y (January 2011). "Small molecule inhibitors of NF-kB and JAK/STAT signal transduction pathways as promising anti-inflammatory therapeutics". Mini Reviews in Medicinal Chemistry. 11 (1): 55–78. doi:10.2174/138955711793564079. PMID 21034406.
- ^ Dodge JA, Richardson TI (2007). "Chapter 10 Novel Selective Estrogen Receptor Modulators (SERMs)". Annual Reports in Medicinal Chemistry Volume 42. Vol. 42. pp. 147–160. doi:10.1016/S0065-7743(07)42010-3. ISBN 978-0-12-373912-4. ISSN 0065-7743.
- ^ Opal SM, Palardy JE, Cristofaro P, Parejo N, Jhung JW, Keith JC, et al. (December 2005). "The activity of pathway-selective estrogen receptor ligands in experimental septic shock". Shock. 24 (6): 535–540. doi:10.1097/01.shk.0000183388.90895.cb. PMID 16317384. S2CID 12169698.
External links※
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