Drug intelligence / Profile preview

sunitinib + rapamycin

Development stage
Phase 1
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Sunitinib + rapamycin is a combination therapy involving two small molecule drugs with distinct mechanisms of action. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor that blocks several kinases implicated in tumor growth and angiogenesis, including vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR), KIT proto-oncogene receptor tyrosine kinase, Fms-like tyrosine kinase 3, Colony stimulating factor receptor type 1, and RET proto-oncogene. Rapamycin (also known as sirolimus) is an inhibitor of the mechanistic target of rapamycin (mTOR), a serine-threonine kinase involved in cell survival and proliferation via the PI3K/Akt/mTOR pathway[7]. The rationale for combining these agents lies in their complementary antiangiogenic and antiproliferative effects. Preclinical studies have shown that this combination can synergistically reduce tumor growth but may also promote metastasis under certain conditions[2][7]. Clinical trials have demonstrated that the combination is generally well-tolerated and warrants further investigation for advanced solid tumors[1][3].

Other names
sirolimus
02

Targets

CSF1R (Macrophage colony-stimulating factor receptor)FKBP1AFLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)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)Mechanistic target of rapamycin complex 1

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