Abexinostat (PCI-24781)

Mechanism of action

From the NCI Drug Dictionary: A novel, broad-spectrum hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. Abexinostat inhibits several isoforms of HDAC, resulting in an accumulation of highly acetylated histones, followed by the induction of chromatin remodeling; the selective transcription of tumor suppressor genes; and the tumor suppressor protein-mediated inhibition of tumor cell division and induction of tumor cell apoptosis.

Preliminary data

Follicular lymphoma; Mantle cell lymphoma

1. Evens AM, Balasubramanian S, Vose JM, Harb W, Gordon LI, Langdon R, Sprague J, Sirisawad M, Mani C, Yue J, Luan Y, Horton S, Graef T, Bartlett NL. A Phase I/II Multicenter, Open-Label Study of the Oral Histone Deacetylase Inhibitor Abexinostat in Relapsed/Refractory Lymphoma. Clin Cancer Res. 2016 Mar 1;22(5):1059-66. Epub 2015 Oct 19. link to original article PubMed
2. Ribrag V, Kim WS, Bouabdallah R, Lim ST, Coiffier B, Illes A, Lemieux B, Dyer MJ, Offner F, Felloussi Z, Kloos I, Luan Y, Vezan R, Graef T, Morschhauser F. Safety and efficacy of abexinostat, a pan-histone deacetylase inhibitor, in non-Hodgkin lymphoma and chronic lymphocytic leukemia: Results of a phase 2 study. Haematologica. 2017 May;102(5):903-909. Epub 2017 Jan 25. link to original article PubMed

Also known as

• Code name: PCI-24781