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tinodasertib + dasatinib
- Development stage
- Discontinued
- Lead developer
- Experimental Drug Development Centre
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Tinodasertib + dasatinib is an experimental combination therapy consisting of the MNK1/2 inhibitor tinodasertib (also known as ETC-1907206 or ETC-206) and the multi-kinase inhibitor dasatinib. Developed by the Experimental Drug Development Centre (EDDC) at A*STAR, this combination was designed to target advanced hematologic malignancies, specifically Philadelphia chromosome-positive (Ph+) and Philadelphia chromosome-negative (Ph-) acute lymphoblastic leukemia (ALL), as well as chronic myeloid leukemia (CML) in accelerated or blast phases. Tinodasertib selectively inhibits mitogen-activated protein kinase-interacting kinases 1 and 2 (MNK1/2), thereby blocking the phosphorylation of eukaryotic translation initiation factor 4E (eIF4E) and suppressing the translation of oncogenic mRNAs. Dasatinib targets BCR-ABL and SRC family kinases. Preclinical data suggested synergistic effects in blast crisis CML models, but a Phase 1 clinical trial (NCT03414450) evaluating the combination was withdrawn due to recruitment challenges.
- Brand names
- TinodasertibSprycel
- Other names
- Tinodasertibdasatinib
02
Targets
ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)SFK (SRC family kinases)
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