NEW ORLEANS--(BUSINESS WIRE)--Epizyme, Inc. (NASDAQ: EPZM), a clinical stage biopharmaceutical company creating novel epigenetic therapeutics for cancer patients, today presented data from clinical studies that investigated the effect of food intake on the pharmacokinetics of tazemetostat, the company’s lead investigational medicine, and the effect of tazemetostat on drugs that are metabolized by the enzyme CYP3A4/5. Epizyme reports that tazemetostat can be dosed with or without food and that the product candidate is a weak inducer of CYP3A-mediated metabolism, suggesting any potential interactions with other treatments metabolized through this pathway will be mild. The data were presented at the 2016 American Association for Cancer Research (AACR) Annual Meeting.
Tazemetostat is a first-in-class oral EZH2 inhibitor in phase 2 development for patients with non-Hodgkin lymphoma (NHL) and patients with certain genetically defined solid tumors.
“The favorable findings from these studies further support the development of tazemetostat both as a monotherapy and in combination with other agents,” said Peter Ho, M.D., Ph.D., Chief Medical Officer, Epizyme. “People living with cancer are often treated with a number of concomitant therapies, so the reduced potential for drug-drug interactions is an important consideration in treatment decision making. Additionally, the ability to take tazemetostat with or without food greatly enhances dosing convenience for patients we are treating.”
Epizyme presented results from a 13-patient study on the effect of food on the pharmacokinetics of tazemetostat in subjects with advanced solid tumors or B-cell lymphomas (abstract CT031, poster #12). Pharmacokinetic studies serve to provide information about the absorption and metabolism of medicinal compounds. The area under the plasma concentration-time curve (AUC) and maximum plasma concentration (Cmax) are pharmacokinetic parameters of the overall exposure to a drug following administration. Study findings showed that:
- AUC decreased by 7 percent and Cmax decreased by 28 percent when patients consumed a high-fat meal prior to drug administration.
- There was no observed clinically relevant effect of food intake on tazemetostat’s overall exposure.
Epizyme also presented results of a single-sequence, open-label crossover study of tazemetostat administered in conjunction with midazolam, a well-understood sedative that is a preferred probe drug in pharmacokinetic studies to predict drug-drug interactions with CYP3A (abstract CT029, poster #10). In summary, data show:
- Tazemetostat resulted in net induction of CYP3A-mediated midazolam metabolism
- Midazolam AUC and Cmax decreased approximately 40 percent and 22 percent, respectively
- Tazemetostat is shown to be a weak inducer of CYP3A-mediated metabolism
About EZH2 in Cancer
EZH2 is a histone methyltransferase (HMT) that is increasingly understood to play a potentially oncogenic role in a number of cancers. These include non-Hodgkin lymphoma, INI1-negative cancers such as malignant rhabdoid tumors and epithelioid sarcomas, certain SMARCA4-negative solid tumors, synovial sarcoma, and a range of other solid tumors.
About Tazemetostat
Epizyme is developing tazemetostat for the treatment of patients with non-Hodgkin lymphoma and for patients with certain genetically defined solid tumors. Tazemetostat is a first-in-class small molecule inhibitor of EZH2 created by Epizyme using its proprietary product platform. In some human cancers, aberrant EZH2 enzyme activity results in dysregulation of genes that control cell proliferation resulting in the rapid and unconstrained growth of tumor cells. Tazemetostat is the WHO International Non- Proprietary Name (INN) for compound EPZ-6438.
Additional information about tazemetostat, including clinical trial information, can be found here.
About Epizyme, Inc.
Epizyme, Inc. is a clinical-stage biopharmaceutical company creating novel epigenetic therapeutics for cancer patients. Epizyme has built a proprietary product platform that the Company uses to create small molecule inhibitors of chromatin modifying proteins (CMPs), such as histone methyltransferases or HMTs. CMPs are part of the system of gene regulation, referred to as epigenetics, that controls gene expression. Genetic alterations can result in changes to the activity of CMPs, making them oncogenic (cancer-causing). By focusing on the genetic drivers of cancers, Epizyme's targeted science seeks to match the right medicines with the right patients.
For more information, visit www.epizyme.com and connect with us on Twitter at @EpizymeRx.
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Any statements in this press release about future expectations, plans and prospects for Epizyme, Inc. and other statements containing the words "anticipate," "believe," "estimate," "expect," "intend," "may," "plan," "predict," "project," "target," "potential," "will," "would," "could," "should," "continue," and similar expressions, constitute forward-looking statements within the meaning of The Private Securities Litigation Reform Act of 1995. Actual results may differ materially from those indicated by such forward-looking statements as a result of various important factors, including: uncertainties inherent in the initiation of future clinical studies or expansion of ongoing clinical studies, availability and timing of data from ongoing clinical studies, whether interim results from a clinical trial will be predictive of the final results of the trial or the results of future trials, expectations for regulatory approvals to conduct trials or to market products, development progress of the Company's companion diagnostics, availability of funding sufficient for the Company's foreseeable and unforeseeable operating expenses and capital expenditure requirements, other matters that could affect the availability or commercial potential of the Company's therapeutic candidates or companion diagnostics and other factors discussed in the "Risk Factors" section of the Company's Form 10-K filed with the SEC on March 9, 2016 and in the Company's other filings from time to time with the SEC. In addition, the forward-looking statements included in this press release represent the Company's views as of the date hereof and should not be relied upon as representing the Company's views as of any date subsequent to the date hereof. The Company anticipates that subsequent events and developments will cause the Company's views to change. However, while the Company may elect to update these forward-looking statements at some point in the future, the Company specifically disclaims any obligation to do so.