Drug intelligence / Profile preview

hydralazine + valproate + nilotinib

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

**Hydralazine + valproate + nilotinib** is an experimental combination therapy leveraging epigenetic modulation and targeted kinase inhibition for cancer treatment, particularly in contexts like chronic myeloid leukemia (CML) resistant to prior therapies. Hydralazine acts as a DNA methyltransferase inhibitor, valproate (valproic acid) inhibits histone deacetylases (HDACs), and nilotinib is a BCR-ABL tyrosine kinase inhibitor. While hydralazine + valproate has been studied in phase I trials for advanced solid tumors showing tolerability and some stable disease, and hydralazine + valproate specifically reverses imatinib resistance in CML via epigenetic mechanisms, no published clinical data exists for the exact three-drug combination, suggesting potential synergy for overcoming resistance in hematologic and solid malignancies.

02

Targets

DNMT (DNA methyltransferase)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)HDAC (HDAC family)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFR (PDGFR family)

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