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dapolsertib
- Development stage
- Phase 2
- Lead developer
- Ryvu Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Dapolsertib is an orally available, investigational small molecule that acts as a dual inhibitor of the PIM family of serine/threonine protein kinases and mutant forms of FMS-related tyrosine kinase 3 (FLT3). By inhibiting these targets, dapolsertib disrupts cell cycle progression at the G1/S phase, inhibits cell proliferation, and induces apoptosis in tumor cells overexpressing PIM kinases or expressing mutant FLT3. These pathways are implicated in hematologic malignancies such as acute myeloid leukemia (AML) and B-cell lymphoma. Dapolsertib is being developed primarily by Ryvu Therapeutics and Menarini for use in cancer therapy, with ongoing Phase II clinical trials for relapsed/refractory diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia[1][2][4][5].
- Other names
- dapolsertib
02
Targets
FLT3 (Fms related receptor tyrosine kinase 3)PIM3 (Proviral integration site for Moloney murine leukemia virus kinase 3)PIM2 (Proto-oncogene serine/threonine-protein kinase Pim2)PIM1 (Proviral integration site for moloney murine leukemia virus kinase 1)
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