SAR245408 (XL147)

SAR245408 (XL147) is an orally available inhibitor of phosphoinositide-3-kinase (PI3K). PI3K plays an important role in cell proliferation and survival, and activation of the PI3K pathway is a frequent event in human tumors, promoting cell proliferation, survival, and resistance to chemotherapy and radiotherapy. Exelixis discovered SAR245408 internally and out-licensed the compound to Sanofi.  SAR245408 is being evaluated by Sanofi as a single agent and in multiple combination regimens in a variety of cancer indications. Ongoing clinical trials include a phase 2 trial in endometrial cancer, a Phase 1b/2 trial in hormone receptor positive breast cancer in combination with letrazole, and phase 1 trials in combination with a MEK inhibitor or an ErbB3 inhibitor.