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tanzisertib
- Development stage
- Discontinued
- Lead developer
- Bristol Myers Squibb
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Tanzisertib is a potent, selective, and orally active small molecule inhibitor of c-Jun N-terminal kinases (JNK1, JNK2, and JNK3), with IC50 values of 61 nM for JNK1, 7 nM for JNK2, and 6 nM for JNK3. It was developed as an antifibrotic agent and has been investigated in clinical trials for the treatment of idiopathic pulmonary fibrosis and discoid lupus erythematosus. The drug acts by inhibiting the phosphorylation activity of the targeted kinases within the MAPK signaling pathway, thereby modulating cellular processes such as apoptosis and inflammation. Tanzisertib received orphan drug designation in both the US and EU for idiopathic pulmonary fibrosis but its development was discontinued due to an unfavorable risk/benefit profile[1][4][5][6][7].
- Other names
- Tanzisertib [USAN]TANZISERTIB
02
Targets
MAPK3 (Mitogen-activated protein kinase 1)JNK (Mitogen-activated protein kinase kinase kinase family)MAPK14 (p38 mitogen-activated protein kinase alpha)
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