XL765 (SAR245409)

XL765 is an orally available inhibitor of phosphoinositide-3-kinase (PI3K) and the mammalian target of rapamycin (mTOR). 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. Given its role as a central regulator of multiple malignant processes, the PI3K pathway has substantial potential as a target for cancer therapy. mTOR is frequently activated in human tumors and plays a central role in tumor cell proliferation.

Exelixis is developing XL765 in collaboration with sanofi-aventis. Based on clinical data available to date, Exelixis and sanofi are pursuing a broad clinical development program for XL765, evaluating the compound as a single agent and in multiple combination regimens in a variety of cancer indications. Ongoing clinical trials include phase 1b/2 trials in combination with temozolomide in patients with glioblastoma, and in combination with erlotinib in patients with non-small cell lung cancer, and a phase 1 trial in patients with solid tumors or lymphoma.

Related Clinical Trials