Cited by 175Histone Deacetylase Inhibitors ResearchEpigenetics and DNA MethylationProtein Degradation and Inhibitors

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A Phase I and Pharmacokinetic Study of the Oral Histone Deacetylase Inhibitor, MS-275, in Patients with Refractory Solid Tumors and Lymphomas

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Gore, Lia, Rothenberg, Mace L., O'Bryant, Cindy L., Schultz, Mary Kay, Sandler, Alan B., Coffin, Denise, McCoy, Candice, Schott, Astrid, Scholz, Catherine, Eckhardt, S. Gail·2008·Clinical Cancer Research

DOI 10.1158/1078-0432.ccr-07-1461PMC PMC2813676

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Abstract

Purpose: To evaluate the toxicity profile, pharmacologic, and biological properties of 3-pyridylmethyl N-{4-[(2-aminophenyl)carbamoyl]benzyl}carbamate (MS-275), a histone deacetylase inhibitor, when administered orally on three different dosing schedules. Experimental Design: Patients with advanced solid malignancies and lymphomas were treated on three dose schedules: once every other week, twice weekly for 3 weeks every 28 days, and once weekly for 3 weeks every 28 days. First-cycle plasma pharmacokinetics and peripheral blood mononuclear cell histone acetylation were determined. Results: Twenty-seven patients received ≥149 courses of treatment. Hypophosphatemia and asthenia were dose limiting on the weekly and twice-weekly dosing schedules; there was no dose-limiting toxicity on the every other week schedule. Pharmacokinetic variables revealed dose-dependent and dose-proportional increases. Two of 27 patients showed partial remissions, including one patient with metastatic melanoma who had a partial response and has remained on study for >5 years. Six patients showed prolonged disease stabilization. Levels of histone H3 and H4 acetylation in peripheral blood mononuclear cells increased qualitatively but with a high degree of interpatient variation. Conclusions: MS-275 is well tolerated at doses up to 6 mg/m2 every other week or 4 mg/m2 weekly for 3 weeks followed by 1 week of rest and results in biologically relevant plasma concentrations and antitumor activity. Twice-weekly dosing was not tolerable due to asthenia, and further evaluation of this schedule was halted. The recommended dose for further disease-focused studies is 4 mg/m2 given weekly for 3 weeks every 28 days or 2 to 6 mg/m2 given once every other week.

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Research works printed but not linked: 2

Wei Y, Qian, DZ, Ren M, et al. In vivo real-time imaging of transcriptional activation of the RARβ gene promoter by the histone deacetylase inhibitor MS-275 in a prostate cancer model. In: Proceedings of the AACR; 2004; Orlando, FL.
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Authors: Gore, L., Rothenberg, M. L., O'Bryant, C. L., Schultz, M. K., Sandler, A. B., Coffin, D., McCoy, C., Schott, A., Scholz, C., & Eckhardt, S. G.
Affiliations: University of Colorado Cancer Center (US)
Vanderbilt-Ingram Cancer Center (US)
1University of Colorado Cancer Center, Aurora, Colorado;
3Bayer Healthcare, Seattle, Washington; and
Bayer (Germany) (DE)
ORCID: Gore, Lia
Sandler, Alan B.
McCoy, Candice
Eckhardt, S. Gail
Venue: Clinical Cancer Research
Publisher: American Association for Cancer Research (AACR)
Published: 2008-07-15
Volume: 14
Issue: 14
Pages: 4517-4525
ISSN: 1078-0432 (ISSN-L)
1557-3265
DOI: 10.1158/1078-0432.ccr-07-1461
PMC: PMC2813676
OpenAlex: W2170925020
Cited by: 171
References: 21
Citations by year: 2026: 7 · 2025: 4 · 2024: 9 · 2023: 5 · 2022: 3 · 2021: 11 · 2020: 7 · 2019: 8 · 2018: 6 · 2017: 9 · 2016: 9 · 2015: 8 · 2014: 10 · 2013: 15 · 2012: 13
FWCI: 6.44
Type: journal article
Language: en
Open access: bronze
doi.org
Locations: Clinical Cancer Research (publishedVersion)
PubMed (publishedVersion)
PubMed Central (acceptedVersion)
Funders: National Institutes of Health (NIH K12)
Cancer Center, University of Colorado
National Cancer Institute (CA-86913, K24CA106349, K12CA086913)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Histone Deacetylase Inhibitors Research
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Epigenetics and DNA Methylation
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
Keywords: entinostat, histone deacetylase inhibitors, oral administration, dosing regimen, pharmacokinetics, refractory solid tumors, lymphoma, hypophosphatemia, asthenia, histone H3 and H4 acetylation, peripheral blood mononuclear cells, metastatic melanoma, anticancer activity, toxicity
MeSH terms: Administration, Oral, Adult, Aged, Antineoplastic Agents, Benzamides, Enzyme Inhibitors, Female, Humans, Lymphoma, Male, Middle Aged, Neoplasms, Pyridines, Area Under Curve, Maximum Tolerated Dose, Histone Deacetylase Inhibitors

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A Phase I and Pharmacokinetic Study of the Oral Histone Deacetylase Inhibitor, MS-275, in Patients with Refractory Solid Tumors and Lymphomas

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