Chemistry:WAY-204688
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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 IC50 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]
References
- ↑ 1.0 1.1 "SIM 688 - AdisInsight". https://adisinsight.springer.com/drugs/800022078.
- ↑ "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. January 2011. doi:10.2174/138955711793564079. PMID 21034406.
- ↑ 3.0 3.1 3.2 3.3 "Chapter 10 Novel Selective Estrogen Receptor Modulators (SERMs)". Annual Reports in Medicinal Chemistry Volume 42. Annual Reports in Medicinal Chemistry. 42. 2007. pp. 147–160. doi:10.1016/S0065-7743(07)42010-3. ISBN 9780123739124.
- ↑ 4.0 4.1 4.2 "The activity of pathway-selective estrogen receptor ligands in experimental septic shock". Shock 24 (6): 535–540. December 2005. doi:10.1097/01.shk.0000183388.90895.cb. PMID 16317384.
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