Drug intelligence / Profile preview

sunitinib + rapamycin

Development stage
Unknown
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].

Brand names
Rapamune
Other names
sirolimus
02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)FKBP1AKIT (c-KIT proto-oncogene receptor tyrosine kinase)CSF1R (Macrophage colony-stimulating factor receptor)Mechanistic target of rapamycin complex 1PDGFRB (Platelet-derived growth factor receptor beta)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)

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