Drug intelligence / Profile preview

tasisulam + sunitinib

Development stage
Discontinued
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Tasisulam + sunitinib is an experimental combination of two anticancer agents that was investigated in preclinical research studies. Tasisulam (LY573636) is a small molecule antitumor agent developed by Eli Lilly that inhibits mitotic progression and induces vascular normalization through a dual mechanism involving mitotic catastrophe and antiangiogenesis. Sunitinib (Sutent) is a multi-targeted receptor tyrosine kinase inhibitor developed by Pfizer that targets VEGFR and PDGFR. In preclinical studies, the combination significantly delayed the growth of Caki-1 renal cell carcinoma models, demonstrating synergy where monotherapy was inactive. While sunitinib is an FDA-approved therapy for several indications, the development of tasisulam was terminated by Eli Lilly in 2011 due to safety concerns and lack of efficacy in Phase II trials. There is no evidence that the tasisulam + sunitinib combination progressed into clinical development.

Other names
tasisulam sodium + sunitinib malateLY573636-sodium + sunitinib
02

Targets

DCAF15 (DDB1- and CUL4-associated factor 15 ubiquitin ligase complex)PDGFRA (Platelet-derived growth factor receptor alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)CSF1R (Macrophage colony-stimulating factor receptor)PDGFRB (Platelet-derived growth factor receptor beta)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)RBM39 (RNA-binding motif protein 39)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)

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