Drug intelligence / Profile preview

sunitinib + trastuzumab

Development stage
Unknown
Lead developer
Pfizer
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous, Subcutaneous
01

Overview

Sunitinib + trastuzumab is a combination therapy investigated for the treatment of HER2-positive advanced breast cancer. Sunitinib is an orally administered small-molecule multi-targeted receptor tyrosine kinase (RTK) inhibitor that blocks several kinases involved in tumor growth, angiogenesis, and metastatic progression, including platelet-derived growth factor receptors (PDGFRs), vascular endothelial growth factor receptors (VEGFRs), KIT (CD117), RET, CSF-1R, and FLT3. Trastuzumab is a monoclonal antibody that targets the human epidermal growth factor receptor 2 (HER2/ERBB2), inhibiting its signaling and mediating antibody-dependent cellular cytotoxicity. The combination has demonstrated antitumor activity in patients with HER2-positive advanced breast cancer, particularly those who were treatment-naïve or had only received prior adjuvant therapy. However, sunitinib is not approved for this indication as it did not meet primary endpoints in phase III trials for advanced breast cancer[1][2][8].

02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)PDGFRA (Platelet-derived growth factor receptor alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)EGFR T790M (Epidermal growth factor receptor T790M mutant)CSF1R (Macrophage colony-stimulating factor receptor)FLT3 (Fms related receptor tyrosine kinase 3)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)PDGFRB (Platelet-derived growth factor receptor beta)

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