Drug intelligence / Profile preview

rucaparib + lucitanib

Development stage
Unknown
Lead developer
Clovis Oncology
Modality
Small Molecules
Administration
Oral
01

Overview

Rucaparib + lucitanib is an oral investigational combination therapy for advanced solid tumors. **Rucaparib** is a small molecule inhibitor of poly(ADP-ribose) polymerase (PARP) 1, 2, and 3, which impairs DNA repair in cancer cells, leading to cell death, particularly in tumors with homologous recombination repair (HRR) deficiencies. **Lucitanib** is a small molecule tyrosine kinase inhibitor that selectively targets vascular endothelial growth factor receptors (VEGFR1–3), platelet-derived growth factor receptors (PDGFRα/β), and fibroblast growth factor receptors (FGFR1–3), exerting antiangiogenic and antiproliferative effects. Preclinical data suggest lucitanib may enhance antitumor activity of rucaparib through increased tumor hypoxia and sensitivity to PARP inhibition. The combination is being studied for tolerability, safety, and preliminary efficacy, with early results showing manageable toxicity and early evidence of disease stability in heavily pretreated patients with advanced solid tumors, including those with BRCA1/2, ATM, PALB2, RAD51B, and CDK12 mutations[1][3][9].

02

Targets

PARP3 (Poly(adp-ribose) polymerase 3)PDGFRA (Platelet-derived growth factor receptor alpha)VEGFR2 (Vascular endothelial growth factor receptor 2)PDGFRB (Platelet-derived growth factor receptor beta)FGFR3 (Fibroblast growth factor receptor 3)CSF1R (Macrophage colony-stimulating factor receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)FGFR2 (Keratinocyte growth factor receptor)TNKS2 (Tankyrase 2)FGFR1 (Fibroblast growth factor receptor 1)PARP2 (Poly (adp-ribose) polymerase 2)

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