2. Academic Validation
  3. EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity

EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity

  • ACS Med Chem Lett. 2015 Mar 4;6(5):491-5. doi: 10.1021/acsmedchemlett.5b00037.
John E Campbell 1,  Kevin W Kuntz 1,  Sarah K Knutson 1,  Natalie M Warholic 1,  Heike Keilhack 1,  Tim J Wigle 1,  Alejandra Raimondi 1,  Christine R Klaus 1,  Nathalie Rioux 1,  Akira Yokoi 2,  Satoshi Kawano 2,  Yukinori Minoshima 2,  Hyeong-Wook Choi 3,  Margaret Porter Scott 1,  Nigel J Waters 1,  Jesse J Smith 1,  Richard Chesworth 1,  Mikel P Moyer 1,  Robert A Copeland 1
Affiliations

Affiliations

  • 1 Epizyme, Inc. , 400 Technology Square, Fourth Floor, Cambridge, Massachusetts 02139, United States.
  • 2 Eisai Co., Ltd. , Tokodai 5-1-3, Tsukuba, Ibarakai 300-2635, Japan.
  • 3 Eisai, Inc. , 4 Corporate Drive, Andover, Massachusetts 01810, United States.
PMID: 26005520 DOI: 10.1021/acsmedchemlett.5b00037
Abstract

Inhibitors of the protein methyltransferase Enhancer of Zeste Homolog 2 (EZH2) may have significant therapeutic potential for the treatment of B cell lymphomas and other Cancer indications. The ability of the scientific community to explore fully the spectrum of EZH2-associated pathobiology has been hampered by the lack of in vivo-active tool compounds for this Enzyme. Here we report the discovery and characterization of EPZ011989, a potent, selective, orally bioavailable inhibitor of EZH2 with useful pharmacokinetic properties. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma. Hence, this compound represents a powerful tool for the expanded exploration of EZH2 activity in biology.

Keywords

B cell lymphoma; EZH2; KARPAS-422; Methyltransferase; PRC2; in vivo chemical probe; xenograft.

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