BET bromodomain 2, 3, and 4 inhibitor OTX015 has completed a Phase I study.

Swiss cancer drug developer OncoEthix negotiated a license to Mitsubishi Tanabe Pharma’s bromodomain inhibitor OTX015. The synthetic small molecule targets BET bromodomains 2, 3, and 4 and has completed a Phase I study. OncoEthix says it plans to start additional studies during 2012.

Recent research indicates that inhibiting BRD2/3/4/ downregulates MYC transcription, which leads to downregulation of MYC-dependent target genes. “The studies that we performed have confirmed that OTX015 is active across a wide range of hematological malignancies,” states Esteban Cvitkovic, M.D., CSL.

OTX015 is the third anticancer compound licensed in by OncoEthix since its foundation in 2007. Lead compound OTX008 is a synthetic small molecule galectin-1 inhibitor, which started in Phase I trials in patients with advanced solid tumors earlier this year. The firm’s discovery-stage compound OTX009 is a synthetic small molecule that is active in cancer cells with an epithelial phenotype that are sensitive to standard chemotherapy drugs and signal transduction modulators as well as cancer cells with mesenchymal phenotype that are highly resistant to such agents.

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