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imatinib + arsenic trioxide
- Development stage
- Preclinical
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Imatinib + arsenic trioxide is a combination therapy consisting of two small molecule drugs used primarily in the treatment of certain hematological malignancies. Imatinib is a selective tyrosine kinase inhibitor that targets BCR-ABL, c-KIT, and PDGF receptors, disrupting signaling pathways essential for cancer cell proliferation and survival. Arsenic trioxide induces apoptosis and promotes differentiation in malignant cells through mechanisms including degradation of PML-RARα fusion protein (notably in acute promyelocytic leukemia) and induction of oxidative stress. The combination has been explored for synergistic effects in chronic myeloid leukemia (CML), especially cases with resistance to imatinib monotherapy or with promyelocytic crisis transformation, as well as other hematologic cancers such as multiple myeloma and acute lymphoblastic leukemia[1][2][3].
- Other names
- imatinib mesylate + arsenic trioxideGleevec + Trisenox
02
Targets
PDGFR (PDGFR family)PML-RARA (PML-retinoic acid receptor alpha fusion protein)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)
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