Synonyms: Example 1 [WO2020252151A1] [1]
Compound class:
Synthetic organic
Comment: We obtained the chemical structure for tilpisertib fosmecarbil from the WHO's proposed INN list 127 (21 July 2022). In this document it was described as a serine/ threonine kinase inhibitor and anti-inflammatory agent. The chemical structure is amongst those that are claimed as Cot (a.k.a. MAP3K8/TPL2) modulators in patent WO2020252151A1 [1]. Inhibition of Cot (which is an upstream regulator in the MEK-ERK pathway) is expected to reduce production and signalling of TNFα, for application in auto-inflammatory diseases. Gilead's development pipeline contains a TPL2 inhibitor, GS-5290, that is in phase 1 for inflammatory bowel disease. Tilpisertib fosmecarbil is likely a follow-up to the parent molecule tilpisertib (formerly GS-4875) that was tested in ulcerative colitis trial NCT04130919.
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Bioactivity Comments |
We have been unable to find quantitative data for tilpisertib fosmecarbil at its proposed molecular target. |