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Phase 1 and preclinical profiling of ESM‐HDAC391, a myeloid‐targeted histone deacetylase inhibitor, shows enhanced pharmacology and monocytopaenia

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To improve the tolerability and therapeutic application of histone deacetylase inhibitors (HDACi), by application of an esterase‐sensitive motif (ESM), to target pharmacological activity directly to mononuclear myeloid cells expressing the… Click to show full abstract

To improve the tolerability and therapeutic application of histone deacetylase inhibitors (HDACi), by application of an esterase‐sensitive motif (ESM), to target pharmacological activity directly to mononuclear myeloid cells expressing the processing enzyme carboxylesterase‐1 (CES1).

Keywords: pharmacology; phase preclinical; myeloid; esm; histone deacetylase

Journal Title: British Journal of Clinical Pharmacology
Year Published: 2022

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