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imatinib mesylate + cyclophosphamide
- Development stage
- Unknown
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
This combination therapy consists of imatinib mesylate, a small molecule tyrosine kinase inhibitor, and metronomic (low-dose, continuous) cyclophosphamide, an alkylating chemotherapy agent. Investigated by the Centre Oscar Lambret, the regimen aims to leverage the synergistic antiangiogenic effects of both drugs. Imatinib targets KIT, BCR-ABL, platelet-derived growth factor receptors (PDGFR), and colony-stimulating factor 1 receptor (CSF1R), while metronomic cyclophosphamide provides continuous suppression of tumor angiogenesis and potentially modulates the immune environment. The combination has been studied in Phase I trials for rare, inoperable, or metastatic tumors, including imatinib-refractory gastrointestinal stromal tumors (GIST), chordoma, and mucosal melanoma.
- Brand names
- GleevecGlivecCytoxan
- Other names
- imatinib + metronomic cyclophosphamide
02
Targets
ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)CSF1R (Macrophage colony-stimulating factor receptor)DNAPDGFRA (Platelet-derived growth factor receptor alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)
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