Drug intelligence / Profile preview

inecalcitol + imatinib

Development stage
Phase 2
Lead developer
Hybrigenics
Modality
Small Molecules
Administration
Oral
01

Overview

**Inecalcitol + imatinib** is a combination treatment investigated for potential *synergistic antineoplastic activity* in cancers, particularly chronic myeloid leukemia (CML). Inecalcitol is a vitamin D₃ analog with anti-proliferative, pro-apoptotic, and anti-angiogenic effects, while imatinib is a small-molecule BCR-ABL tyrosine kinase inhibitor that disrupts key oncogenic pathways in CML. Studies in cell lines demonstrate that this combination can lead to enhanced cell killing compared to each agent alone in certain CML cell models, suggesting a synergistic mode of action. This regimen is under investigation and not an approved standard of care[1][3][5].

02

Targets

BCR-ABL1 (Breakpoint cluster region-Abelson tyrosine-protein kinase 1)CSF1R (Macrophage colony-stimulating factor receptor)DDR1 (Discoidin domain receptor 1)DDR2 (Discoidin domain receptor tyrosine kinase 2)KIT (c-KIT proto-oncogene receptor tyrosine kinase)NQO2 (Ribosyldihydronicotinamide dehydrogenase [quinone])PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)VDR (Vitamin D receptor)BCR (Immunoglobulin G B Cell Receptor)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)

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