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apatinib + silver peroxide
- Development stage
- Preclinical
- Lead developer
- Ruijin Hospital
- Modality
- Small Molecules, Nanoparticles → Drug Delivery Systems
01
Overview
Apatinib + silver peroxide (Apa&Ag2O2@POMS) is an investigational drug delivery system consisting of OPDEA-modified PLGA microspheres co-loaded with the VEGFR2 inhibitor apatinib and silver peroxide (Ag2O2) [1115eP]. Developed for the treatment of osteosarcoma, particularly metastatic and apatinib-resistant forms, this dual-targeting therapeutic strategy aims to overcome hypoxia-driven adaptive resistance and induce mitochondrial oxidative collapse [1115eP]. Silver peroxide within the system alleviates hypoxia and suppresses the HIF-1α/VEGF/PI3K-AKT axis, thereby restoring sensitivity to VEGFR2-targeted anti-angiogenic therapy [1115eP]. Concurrently, the OPDEA modification promotes mitochondrial accumulation, leading to spatially confined reactive oxygen species (ROS) overload and activation of the ROS-JNK/p38 MAPK-caspase apoptotic pathway [1115eP].
- Other names
- Apa&Ag2O2@POMSApa&Ag2O2@POMS systemapatinib and silver peroxideapatinib/silver peroxide
02
Targets
AKT (RAC-alpha serine/threonine-protein kinase)HIF1A (Hypoxia-inducible factor 1-alpha)JNK (Mitogen-activated protein kinase kinase kinase family)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)RET (Rearranged during transfection receptor tyrosine kinase)SRC (Proto-oncogene tyrosine-protein kinase Src)VEGFA (Vascular endothelial growth factor A)VEGFR2 (Vascular endothelial growth factor receptor 2)KIT (c-KIT proto-oncogene receptor tyrosine kinase)RK (Ribokinase)
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