Drug intelligence / Profile preview

regorafenib + capecitabine + cyclophosphamide + aspirin

Development stage
Phase 2
Lead developer
CHU de Besançon
Modality
Small Molecules
Administration
Oral
01

Overview

This multimodal metronomic chemotherapy regimen is being evaluated by the Centre Hospitalier Universitaire de Besançon in the REPROGRAM-02 Phase II/III trial for the treatment of metastatic colorectal cancer (mCRC). The regimen consists of a two-month induction phase combining the multi-kinase inhibitor regorafenib with metronomic doses of capecitabine (625 mg/m² twice daily) and cyclophosphamide (50 mg daily), supplemented with low-dose aspirin (75 mg daily). This approach utilizes continuous low-dose administration of cytotoxic agents to achieve anti-tumor effects, anti-angiogenic activity, and immune system stimulation with improved tolerance compared to standard dosing. The strategy is designed as a sequential treatment to be administered before standard second-line chemotherapy (such as FOLFIRI or FOLFOX) to improve response rates and overall survival in patients who have progressed after first-line therapy.

Other names
Regorafenib induction in combination with metronomic cyclophosphamide, capecitabine, and low-dose aspirinMetronomic chemotherapies-CHU de Besancon
02

Targets

BRAF V600EPGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)DNAFGFR1 (Fibroblast growth factor receptor 1)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))RET (Rearranged during transfection receptor tyrosine kinase)TEK (Tie2)TS (Thymidylate synthase)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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