A selective histone deacetylase inhibitor for myeloma
Mené sur 38 patients atteints d'un myélome multiple réfractaire ou récidivant, cet essai multicentrique de phase Ib évalue les toxicités en fonction des doses reçues et les caractéristiques pharmacocinétiques et pharmacodynamiques du ricolinostat combiné au lénalidomide et au dexaméthasone
Histone deacetylases (HDACs) are a family of 18 enzymes, divided into four distinct classes, with actions that affect all major cellular functions. Their broad cellular activity relates to their ability to change gene transcription through modification of histones and modify activity of non-histone proteins through lysine acetylation.1,2 Development of HDAC inhibitors in cancer treatment has focused on the antiproliferative effects of modification of gene transcription in cancer cells, but their effects on regulation of the function of non-histone proteins are unclear.
The Lancet Oncology , commentaire, 2015