A Phase I and Pharmacokinetic Study of the Oral Histone Deacetylase Inhibitor, MS-275, in Patients with Refractory Solid Tumors and Lymphomas
Open accessAbstract
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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The most common toxicities observed included fatigue and hematologic, gastrointestinal, and metabolic adverse events, similar to previous studies incorporating entinostat.
“The most common toxicities observed included fatigue and hematologic, gastrointestinal, and metabolic AEs, similar to previous studies incorporating entinostat.11,14,15”
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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)
- Venue
- Clinical Cancer Research
- Published
- 2008-07-15
- Volume
- 14
- Issue
- 14
- Pages
- 4517-4525
- ISSN
- 1078-0432 (ISSN-L)
- 1557-3265
- 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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