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Ref Type Journal Article
PMID (22609854)
Authors Shi JQ, Lasky K, Shinde V, Stringer B, Qian MG, Liao D, Liu R, Driscoll D, Nestor MT, Amidon BS, Rao Y, Duffey MO, Manfredi MG, Vos TJ, D' Amore N, Hyer ML
Title MLN0905, a small-molecule plk1 inhibitor, induces antitumor responses in human models of diffuse large B-cell lymphoma.
Journal Molecular cancer therapeutics
Vol 11
Issue 9
Date 2012 Sep
Abstract Text Diffuse large B-cell lymphoma (DLBCL) is the most common of the non-Hodgkin lymphomas, accounting for up to 30% of all newly diagnosed lymphoma cases. Current treatment options for this disease are effective, but not always curative; therefore, experimental therapies continue to be investigated. We have discovered an experimental, potent, and selective small-molecule inhibitor of PLK1, MLN0905, which inhibits cell proliferation in a broad range of human tumor cells including DLBCL cell lines. In our report, we explored the pharmacokinetic, pharmacodynamic, and antitumor properties of MLN0905 in DLBCL xenograft models grown in mice. These studies indicate that MLN0905 modulates the pharmacodynamic biomarker phosphorylated histone H3 (pHisH3) in tumor tissue. The antitumor activity of MLN0905 was evaluated in three human subcutaneous DLBCL xenograft models, OCI LY-10, OCI LY-19, and PHTX-22L (primary lymphoma). In each model, MLN0905 yielded significant antitumor activity on both a continuous (daily) and intermittent dosing schedule, underscoring dosing flexibility. The antitumor activity of MLN0905 was also evaluated in a disseminated xenograft (OCI LY-19) model to better mimic human DLBCL disease. In the disseminated model, MLN0905 induced a highly significant survival advantage. Finally, MLN0905 was combined with a standard-of-care agent, rituximab, in the disseminated OCI LY-19 xenograft model. Combining rituximab and MLN0905 provided both a synergistic antitumor effect and a synergistic survival advantage. Our findings indicate that PLK1 inhibition leads to pharmacodynamic pHisH3 modulation and significant antitumor activity in multiple DLBCL models. These data strongly suggest evaluating PLK1 inhibitors as DLBCL anticancer agents in the clinic.


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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
MLN0905 MLN0905 1 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
MLN0905 MLN-0905|MLN 0905 PLK1 Inhibitor 16 MLN0905 is a small molecule inhibitor of PLK1, which may result in cell cycle arrest and antitumor activity (PMID: 22609854, PMID: 28184925).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown diffuse large B-cell lymphoma not applicable MLN0905 + Rituximab Preclinical Actionable In a preclinical study, MLN0905 combined with MabThera (rituximab) resulted in a synergistic effect when treating a diffuse large B-cell lymphoma xenograft model, demonstrating a decrease in tumor volume and increased survival (PMID: 22609854). 22609854
Unknown unknown diffuse large B-cell lymphoma not applicable MLN0905 Preclinical Actionable In a preclinical study, MLN0905 treatment resulted in decreased tumor volume in a diffuse large B-cell lymphoma xenograft model (PMID: 22609854). 22609854