XL-114

Exelixis, Inc. (Nasdaq: EXEL) today announced initiation of the dose-escalation stage of the first-in-human phase 1 trial of XL114, a novel anti-cancer compound that inhibits the CARD11-BCL10-MALT1 complex, as a monotherapy in patients with non-Hodgkin’s lymphoma (NHL) who have received prior standard therapies. The objectives of the study are to determine the recommended dose and/or the maximum tolerated dose of XL114 and to evaluate the safety and preliminary efficacy of XL114 in patients with NHL. “The initiation of the dose-escalation stage of our first-in-human phase 1 trial of XL114 marks an important milestone in our early efforts to identify treatments for people with blood cancers, such as non-Hodgkin’s lymphoma, who have exhausted known life-prolonging treatment options and are thus facing poor prognoses,” said Vicki L. Goodman, M.D., Executive Vice President, Product Development and Medical Affairs, and Chief Medical Officer, Exelixis. “Based on preclinical data demonstrating activity in lymphoma cell lines that are resistant to therapies that inhibit Bruton's tyrosine kinase, we are encouraged by the potential XL114 holds and look forward to advancing to the expansion stage once the appropriate dose is identified.” The dose-escalation stage will determine the recommended dose of XL114 in patients with advanced B- and T-cell NHL. In the cohort-expansion stage, the safety and preliminary efficacy of XL114 will be further evaluated in B-cell NHL-specific expansion cohorts, including patients with activated B-cell-like diffuse large B-cell lymphoma (DLBCL), mantle cell lymphoma and chronic lymphocytic leukemia/small lymphocytic lymphoma. The primary endpoint of the expansion stage will be objective response rate based on lymphoma-specific response criteria as assessed by the investigator. As announced last year, Exelixis in-licensed XL114 from Aurigene Discovery Technologies Limited under the companies’ July 2019 collaboration, option and license agreement. Exelixis assumed responsibility for the future clinical development, commercialization and global manufacturing of XL114.