Concordia has developed a novel, orally effective, targeted well-tolerated Ras inhibitor indicated for treatment of a wide range of malignancies including pancreatic, lung, colon and other cancers. Salirasib is the first-in-class “rasib” and is not a farnesyltransferase inhibitor (FTI) or Epidermal Growth Factor Receptor (EGFR) antagonist. Salirasib has a much broader ability to inhibit Ras signaling by dislodging all isoforms of Ras from galectin membrane binding sites.

Clinical studies have been and are being performed at recognized Centers of Excellence, including, M.D. Anderson (safety, pharmacokinetic and food effect studies in both solid tumor and hematologic malignancies), Johns Hopkins University (a Phase I/II study dosing salirasib + gemcitabine for the treatment of newly diagnosed pancreatic cancer patients) and Memorial Sloan-Kettering (a Phase II trial treating both treatment naïve and previously treated lung cancer patients with 600mg bid salirasib mono-therapy).

Salirasib is the first targeted molecule to demonstrate the ability to reduce total Ras protein levels (both wild-type and mutated) in primary human tumors. Data presented at the June 2008 ASCO meeting revealed that EGFR antibodies had little to no treatment value in colon cancer patients with K-Ras mutations. Similar data are emerging regarding the use of EGFR inhibitors in lung cancer patients with K-Ras mutation.

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 Salirasib Mechanism of Action