Synonyms: GS 4875 | GS-4875
Compound class:
Synthetic organic
Comment: Tilpisertib (GS-4875) is an inhibitor of the serine/ threonine kinase Cot (a.k.a. MAP3K8/TPL2). It was developed by Gilead Sciences as a potential anti-inflammatory drug to treat auto-inflammatory diseases. 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. Gilead's development pipeline now contains a TPL2 inhibitor, GS-5290, that is in phase 1 for inflammatory bowel disease. GS-5290 may be follow-up lead compound tilpisertib fosmecarbil.
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References |
1. Canales EY, Desai MC, Gorman E, Li J, Saioto RD, Taylor JG, Wright NE. (2020)
Cot modulators and methods of use thereof. Patent number: WO2020252151A1. Assignee: Gilead Sciences, Inc.. Priority date: 14/06/2019. Publication date: 17/12/2020. |