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enzastaurin + sunitinib
- Development stage
- Discontinued
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Enzastaurin + sunitinib is an experimental combination of two oral small-molecule kinase inhibitors evaluated primarily for the treatment of metastatic renal cell carcinoma (RCC). **Enzastaurin** is a selective inhibitor of protein kinase C beta (PKC-β), with additional activity against phosphatidylinositol 3-kinase/AKT and GSK3-beta signaling pathways, and is believed to induce antiproliferative, pro-apoptotic, and antiangiogenic effects in tumor cells. **Sunitinib** is a multi-targeted receptor tyrosine kinase (RTK) inhibitor with activity against vascular endothelial growth factor receptors (VEGFRs), platelet-derived growth factor receptors (PDGFRs), and other kinases, exerting antitumor and antiangiogenic effects. The combination was hypothesized to produce synergistic antiangiogenic and antitumor effects in RCC. Clinical studies indicated a synergistic reduction of tumor cell viability in preclinical models, but clinical development was discontinued due to tolerability concerns and lack of further sponsor support for enzastaurin in solid tumors[1][2][3].
- Brand names
- Sutent (for sunitinib)none for the combination
- Other names
- none for the combination
02
Targets
PRKCB (Protein kinase C beta)VEGFR4 (Vascular endothelial growth factor Receptor-3)PRKCG (Protein kinase C gamma)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PRKCA (Protein kinase C alpha)VEGFR-1 (Vascular endothelial growth factor receptor 1)FLT3 (Fms related receptor tyrosine kinase 3)VEGFR2 (Vascular endothelial growth factor receptor 2)PDGFRA (Platelet-derived growth factor receptor alpha)CSF1R (Macrophage colony-stimulating factor receptor)GSK3 (Glycogen synthase kinase 3 beta)PRKCE (Protein Kinase C epsilon)FGFR1 (Fibroblast growth factor receptor 1)PDGFRB (Platelet-derived growth factor receptor beta)
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