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derazantinib + paclitaxel + ramucirumab
- Development stage
- Discontinued
- Lead developer
- Basilea Pharmaceutica
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Derazantinib + paclitaxel + ramucirumab is an investigational combination therapy being studied primarily for the treatment of HER2-negative gastric adenocarcinoma (gastric cancer). Derazantinib is an orally administered small-molecule inhibitor targeting fibroblast growth factor receptors 1, 2, and 3 (FGFR1–3), as well as colony-stimulating factor 1 receptor (CSF1R) and vascular endothelial growth factor receptor 2 (VEGFR2). Paclitaxel is a microtubule-stabilizing chemotherapeutic agent that inhibits cell division. Ramucirumab is a monoclonal antibody that targets VEGFR2, inhibiting angiogenesis. The rationale for this triple combination stems from potential synergistic anti-tumor effects due to complementary mechanisms—derazantinib’s multi-targeted kinase inhibition may enhance the antiangiogenic activity of ramucirumab and the cytotoxic effect of paclitaxel. This regimen is under clinical investigation in phase 1b/2 trials for patients with advanced or metastatic HER2-negative gastric cancer who have progressed after prior chemotherapy[1][3][5][8].
- Brand names
- ramucirumab: Cyramzapaclitaxel: Taxol
02
Targets
CSF1R (Macrophage colony-stimulating factor receptor)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)VEGFR2 (Vascular endothelial growth factor receptor 2)TUBB (Tubulin (alpha and beta subunits))
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