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tinodasertib
- Development stage
- Phase 2
- Lead developer
- AUM Biosciences
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Tinodasertib is a selective and potent oral small molecule inhibitor of mitogen-activated protein kinase (MAPK)-interacting kinases MNK1 and MNK2. By inhibiting these kinases, tinodasertib blocks the phosphorylation of eukaryotic initiation factor 4E (eIF4E), thereby interfering with cap-dependent mRNA translation—a process implicated in oncogenic transformation and tumor progression. Tinodasertib has demonstrated antineoplastic activity in preclinical models and is being investigated for use in various cancers, including advanced colorectal cancer. The drug was initially developed by Experimental Therapeutics Centre and has reached Phase II clinical trials as an investigational therapy[1][3][4][5][7].
- Other names
- 4-{6-[4-(morpholine-4-carbonyl)phenyl]imidazo[1,2-a]pyridin-3-yl}benzonitrile
02
Targets
ABCG2 (Breast cancer resistance protein)EIF4E (Eukaryotic translation initiation factor 4E)MKNK2 (MAP kinase-interacting serine/threonine-protein kinase 2)RIPK2 (Receptor-interacting protein serine/threonine kinase 2)MKNK1 (Mitogen‑activated protein kinase‑interacting serine/threonine-protein kinase 1)
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