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imatinib + valproic acid

Development stage: Preclinical
Lead developer: Novartis
Modality: Small Molecules
Administration: Oral

Overview

A combination of the tyrosine kinase inhibitor imatinib and the anticonvulsant valproic acid. This combination has been investigated for its potential synergistic effects in treating Philadelphia chromosome-positive leukemias, particularly in imatinib-resistant chronic myeloid leukemia (CML). Valproic acid, acting as a histone deacetylase (HDAC) inhibitor, can enhance imatinib-induced growth arrest and apoptosis in both imatinib-sensitive and imatinib-resistant CML cell lines.

Targets

KIT (c-KIT proto-oncogene receptor tyrosine kinase)HDAC (HDAC family)PDGFRA (Platelet-derived growth factor receptor alpha)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)

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