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Patent AT-E399539-T1: [Translated] TWO-PHASE RELEASE FORMULATION CONTAINING HISTONE DEACETYLASE INHIBITOR

Published by National Center for Biotechnology Information (NCBI) | U.S. Department of Health & Human Services | Metadata Last Checked: September 07, 2025 | Last Modified: 2025-09-06
The present invention relates to an orally available galenics formulation of Valproic Acid or derivatives thereof exhibiting a specific bi-phasic pharmacokinetic profile optimized for maximum inhibition of histone deacetylases in a therapeutic setting. This specific galenics formulation is designed for the treatment of malignant diseases and diseases associated with hypoacetylation of histones or in which induction of hyperacetylation has a beneficial effect, e.g., by induction of differentiation and/or apoptosis. Due to the bi-phasic release pattern the resulting pharmacokinetic profile is able to inhibit HDAC target enzymes most efficiently and to subsequently induce histone hyperacetylation in a rapid as well as a long-lasting fashion. This profile secures the efficient modulation of a desired target gene expression profile which contributes to the therapeutic benefit.

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