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lutetium Lu 177 dotatate + sunitinib malate
- Development stage
- Unknown
- Lead developer
- Novartis
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Small Molecules, Peptides
- Administration
- Intravenous, Oral
01
Overview
lutetium Lu 177 dotatate + sunitinib malate is a combination therapy being investigated for the treatment of metastatic or unresectable pancreatic neuroendocrine tumors (pNETs). The combination pairs **lutetium Lu 177 dotatate** (Lutathera), a peptide receptor radionuclide therapy (PRRT), with **sunitinib malate** (Sutent), a multi-targeted receptor tyrosine kinase inhibitor. Lutetium Lu 177 dotatate consists of a somatostatin analogue (dotatate) linked to the beta-emitting radioisotope lutetium-177, which targets and destroys cells expressing somatostatin receptor type 2 (SSTR2). Sunitinib malate complements this by inhibiting several kinases involved in tumor growth and angiogenesis, including vascular endothelial growth factor receptors (VEGFR) and platelet-derived growth factor receptors (PDGFR). This combination is currently being evaluated in a Phase I trial (NCT05687123) sponsored by the National Cancer Institute (NCI) to determine safety and potential synergistic effects in patients with somatostatin receptor-positive pNETs.
- Other names
- 177Lu-DOTATATE + sunitiniblutetium Lu 177 dotatate and 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)SSTR2 (Somatostatin receptor type 2)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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