Scientific Data on PI3K/mTOR Inhibitor VS-5584 Published in Molecular Cancer Therapeutics

CAMBRIDGE, Mass.--(BUSINESS WIRE)--

Verastem, Inc., (VSTM), a clinical-stage biopharmaceutical company focused on discovering and developing drugs to treat cancer by the targeted killing of cancer stem cells, announced the publication of data for VS-5584 in Molecular Cancer Therapeutics.

VS-5584 is a potent and selective inhibitor of the PI3K/mTOR pathway. Previous research has described a central role of this pathway in cancer stem cells. The current study details the biochemical properties and preclinical effects of this compound in multiple human tumor models.

The PI3K/mTOR signaling pathway appears critical for the survival and self-renewal of cancer stem cells, said Jonathan Pachter, Ph.D., Verastem Vice President and Head of Research. We have established a broad platform to assess cancer stem cell inhibition in multiple types of human cancer. VS-5584 has been one of the most impressive cancer stem cell inhibitors we have seen to date across these assays.

VS-5584 demonstrated potent and highly selective activity against class 1 PI3K enzymes and dual-inhibitory actions against mTORC1 and mTORC2. The compound was profiled across >400 kinases covering all major families of the human kinome. In addition to the biochemical effects, VS-5584 exhibited broad anti-tumor efficacy, including tumor regression, across multiple human tumor models in the published study.

PI3K and mTOR inhibitors continue to show promise for the treatment of cancer, said Dr. Jose Baselga, member of the Verastem Scientific Advisory Board. We have gained clinical experience with PI3K and mTOR inhibitors in recent years, and it appears that the dual blockade of PI3K and mTOR may be synergistic for maximum clinical benefit.

VS-5584 is an orally available compound with favorable pharmacokinetics that induces long-lasting and dose-dependent inhibition of PI3K/mTOR signaling in tumor tissue.

We are currently evaluating VS-5584 in IND-enabling toxicity studies prior to entry into a Phase 1 trial, said Dr. Joanna Horobin, Verastem Chief Medical Officer. We anticipate initiating clinical testing of VS-5584 during the second half of 2013 in patients with advanced cancers. In addition to safety, the study will evaluate initial signs of clinical activity and cancer stem cell inhibition.

The publication is titled VS-5584, a Novel and Highly Selective PI3K/mTOR Kinase Inhibitor for the Treatment of Cancer and can be accessed at: http://bit.ly/WBkOwN.

About Verastem, Inc.

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Scientific Data on PI3K/mTOR Inhibitor VS-5584 Published in Molecular Cancer Therapeutics