| Literature DB >> 19874311 |
Susan E Bates1, Zhirong Zhan, Kenneth Steadman, Tomasz Obrzut, Victoria Luchenko, Robin Frye, Robert W Robey, Maria Turner, Erin R Gardner, William D Figg, Seth M Steinberg, Alex Ling, Tito Fojo, Kin Wah To, Richard L Piekarz.
Abstract
Romidepsin has shown promise in the treatment of T-cell lymphomas, and so we evaluated molecular endpoints gathered from 61 patients enrolled on a phase II trial of romidepsin in cutaneous and peripheral T-cell lymphoma at the National Institutes of Health. The endpoints included histone H3 acetylation and ABCB1 gene expression in peripheral blood mononuclear cells (PBMCs); ABCB1 gene expression in tumour biopsy samples; and blood fetal haemoglobin levels (HbF), all of which were increased following romidepsin treatment. The fold increase in histone acetylation in PBMCs at 24 h was weakly to moderately well correlated with the pharmacokinetic parameters C(max) and area under the curve (AUC)(last) (rho = 0.37, P = 0.03 and rho = 0.36, P = 0.03 respectively) and inversely associated with clearance (rho = -0.44; P = 0.03). Histone acetylation in PBMCs at 24 h was associated with response (P = 0.026) as was the increase in fetal haemoglobin (P = 0.014); this latter association may be due to the longer on-study duration for patients with disease response. Together, these results suggest that pharmacokinetics may be an important determinant of response to histone deacetylase inhibitors (HDIs) - the association with histone acetylation in PBMCs at 24 h is consistent with a hypothesis that potent HDIs are needed for a critical threshold of drug exposure and durable activity.Entities:
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Year: 2009 PMID: 19874311 PMCID: PMC2838427 DOI: 10.1111/j.1365-2141.2009.07954.x
Source DB: PubMed Journal: Br J Haematol ISSN: 0007-1048 Impact factor: 6.998