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vorinostat + dasatinib
- Development stage
- Unknown
- Lead developer
- City of Hope Medical Center
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
vorinostat + dasatinib is a combination therapy investigated by the City of Hope Medical Center for the treatment of advanced Philadelphia chromosome-positive (Ph+) leukemias, including chronic myelogenous leukemia (CML) and acute lymphoblastic leukemia (ALL). Vorinostat is a small molecule histone deacetylase (HDAC) inhibitor that alters gene expression and induces apoptosis. Dasatinib is a potent, small molecule dual BCR-ABL and Src family tyrosine kinase inhibitor (TKI). The combination is designed to overcome resistance to TKI monotherapy by synergistically depleting BCR-ABL protein levels and inhibiting downstream survival pathways such as STAT5 and AKT. Clinical development has focused on determining the safety and maximum tolerated dose in patients with accelerated or blast phase CML and Ph+ ALL.
- Other names
- vorinostat and dasatinibdasatinib and vorinostatSAHA and dasatinib
02
Targets
KIT (c-KIT proto-oncogene receptor tyrosine kinase)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)HDAC (HDAC family)SFK (SRC family kinases)EPHA2 (Ephrin type-A receptor 2)PDGFRB (Platelet-derived growth factor receptor beta)
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