Drug intelligence / Profile preview

cabozantinib + lutetium Lu 177 dotatate

Development stage: Unknown
Lead developer: St. Joseph Health
Modality: Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration: Oral, Intravenous

Overview

cabozantinib + lutetium Lu 177 dotatate is a combination therapy being evaluated for the treatment of somatostatin receptor 2 (SSTR2) positive neuroendocrine tumors (NETs). It consists of cabozantinib, a small molecule multi-kinase inhibitor that targets MET, VEGFR2, and AXL to inhibit tumor growth and angiogenesis, and lutetium Lu 177 dotatate, a radiolabeled somatostatin analog. Lutetium Lu 177 dotatate binds to SSTR2 on tumor cells, delivering targeted beta-minus radiation that induces DNA damage and cell death. The combination is currently being studied by Providence Health & Services in a Phase Ib trial (NCT05360238) to determine the safety and maximum tolerated dose of cabozantinib when administered alongside standard peptide receptor radionuclide therapy (PRRT).

Other names: cabozantinib + Lu-177 DOTATATEcabozantinib + Lutathera

Targets

SSTR2 (Somatostatin receptor type 2)MET (Mesenchymal-epithelial transition factor receptor)VEGFR2 (Vascular endothelial growth factor receptor 2)AXL (AXL receptor tyrosine kinase)

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