Drug intelligence / Profile preview

sunitinib + capecitabine

Development stage
Phase 3
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Sunitinib + capecitabine is a combination of two orally administered small molecule drugs used in oncology clinical trials for advanced solid tumors, including breast, pancreatic, thyroid, neuroendocrine, bladder, colorectal cancer, and cholangiocarcinoma[1][3]. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor that blocks several kinases involved in tumor growth and angiogenesis such as platelet-derived growth factor receptors (PDGFR), vascular endothelial growth factor receptors (VEGFR), KIT (CD117), RET, CSF-1R, and FLT3[5][6]. Capecitabine is an antimetabolite prodrug converted to 5-fluorouracil (5-FU) preferentially within tumor cells; 5-FU inhibits thymidylate synthase and disrupts DNA/RNA synthesis leading to apoptosis[8]. The combination has shown manageable safety profiles with some overlapping toxicities such as hand-foot syndrome and diarrhea. While the rationale for combining these agents includes their different mechanisms of action and potential synergistic antitumor activity[3], phase III studies have not demonstrated improved outcomes over monotherapy in certain settings such as metastatic breast cancer pretreated with anthracyclines[2][4].

Other names
sunitinib malate
02

Targets

CSF1R (Macrophage colony-stimulating factor receptor)FLT3 (Fms related receptor tyrosine kinase 3)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)TS (Thymidylate synthase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)

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