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lenalidomide + sunitinib
- Development stage
- Discontinued
- Lead developer
- Bristol Myers Squibb
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Lenalidomide + sunitinib is a combination of two small molecule drugs developed for the treatment of advanced or metastatic renal cell carcinoma. **Lenalidomide** is an immunomodulatory drug that alters cytokine production, modulates T-cell and NK-cell function, and acts as a molecular glue to redirect substrate specificity of the CRL4^CRBN^ E3 ubiquitin ligase, resulting in the proteasomal degradation of target proteins such as IKZF1, IKZF3, and CK1α[2][4]. **Sunitinib** is a multi-targeted receptor tyrosine kinase inhibitor that blocks the activity of VEGF receptors, PDGF receptors, KIT, FLT-3, CSF-1R, and RET, leading to inhibition of angiogenesis and tumor cell proliferation[6]. The combination was investigated in a phase I/II trial for metastatic renal cell carcinoma, but unacceptable toxicity at tolerance limits precluded further clinical development[1][5][3]. Both agents are administered orally.
- Other names
- lenalidomidesunitinibsunitinib malate
02
Targets
CK1α (Casein kinase I alpha)CSF1R (Macrophage colony-stimulating factor receptor)CRBN (Cereblon)FLT3 (Fms related receptor tyrosine kinase 3)IKZF1 (Ikaros family zinc finger protein 1)IKZF3 (Zinc finger protein Aiolos)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)RET (Rearranged during transfection receptor tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)GFRA4 (GDNF family receptor alpha-4)
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