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Niraparib + cabozantinib
- Development stage
- Phase 2
- Lead developer
- Exelixis
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Niraparib + cabozantinib is an investigational combination therapy being studied primarily in advanced and metastatic cancers such as urothelial carcinoma (UC) and renal cell carcinoma (RCC)[2][4]. Niraparib is a selective oral poly(ADP-ribose) polymerase (PARP) inhibitor that impairs DNA repair in cancer cells by inhibiting PARP-1 and PARP-2 enzymes[5]. Cabozantinib is a small molecule tyrosine kinase inhibitor that targets multiple receptor tyrosine kinases including MET, VEGFRs (vascular endothelial growth factor receptors), AXL, RET, KIT, FLT3, TIE-2 and others[3][6][8]. The rationale for combining these agents lies in their complementary mechanisms—niraparib induces DNA damage while cabozantinib inhibits pathways involved in tumor angiogenesis and metastasis. This combination has shown promising preliminary safety and efficacy signals in early-phase clinical trials for patients with previously treated metastatic UC or RCC[2][4].
02
Targets
AXL (AXL receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)PARP1 (Poly (adp-ribose) polymerase 1)PARP2 (Poly (adp-ribose) polymerase 2)RET (Rearranged during transfection receptor tyrosine kinase)NTRK2 (Tropomyosin-related kinase receptor type B)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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