Exelixis Announces Initiation of First-In-Human Phase 1 Trial Evaluating XL114 Monotherapy in Patients with Non-Hodgkin’s Lymphoma

– XL114 is a CARD11-BCL10-MALT1 pathway inhibitor with demonstrated activity in lymphoma models that are resistant to Bruton's tyrosine kinase inhibitors –

ALAMEDA, CA, USA I April 14, 2022 I 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.

More information about this trial is available at ClinicalTrials.gov.

About NHL

According to the American Cancer Society, more than 80,000 people will be diagnosed with NHL in 2022, making it the seventh most common cancer in the U.S.1 Age is one of the strongest risk factors for NHL, meaning cases are expected to rise as the American population ages.1,2 NHL comprises more than 60 subtypes, with DLBCL as the most common.3 About 85% of NHL cases in the U.S. affect B cells, and the remainder affect T cells or Nature Killer (NK) cells.3,4 NHL can also be classified by how quickly the cancer grows; about 40% of cases, including chronic lymphocytic leukemia, are “indolent,” or slow-growing, whereas 60%, including DLBCL, are “aggressive,” or rapidly progressing.3,5 Although standard of care first-line therapy can be curative, up to 50% of patients with DLBCL may be refractory to treatment or relapse.6 The overall five-year survival rate for NHL is 73%.7

About XL114

XL114 is a novel anti-cancer compound that inhibits the CARD11-BCL10-MALT1 complex, a key component of signaling downstream of B- and T-cell receptors, which promotes B- and T-cell lymphoma survival and proliferation. In preclinical studies, the compound was shown to have activity in lymphoma models that are resistant to Bruton's tyrosine kinase inhibitor therapy, and in subsets of B-cell lymphomas in which Bruton's tyrosine kinase inhibitors are not active. XL114 is currently being developed for NHL.

About Exelixis

Founded in 1994, Exelixis, Inc. (Nasdaq: EXEL) is a commercially successful, oncology-focused biotechnology company that strives to accelerate the discovery, development and commercialization of new medicines for difficult-to-treat cancers. Following early work in model system genetics, we established a broad drug discovery and development platform that has served as the foundation for our continued efforts to bring new cancer therapies to patients in need. Our discovery efforts have resulted in four commercially available products, CABOMETYX® (cabozantinib), COMETRIQ® (cabozantinib), COTELLIC® (cobimetinib) and MINNEBRO® (esaxerenone), and we have entered into partnerships with leading pharmaceutical companies to bring these important medicines to patients worldwide. Supported by revenues from our marketed products and collaborations, we are committed to prudently reinvesting in our business to maximize the potential of our pipeline. We are supplementing our existing therapeutic assets with targeted business development activities and internal drug discovery – all to deliver the next generation of Exelixis medicines and help patients recover stronger and live longer. Exelixis is a member of the Standard & Poor’s (S&P) MidCap 400 index, which measures the performance of profitable mid-sized companies. For more information about Exelixis, please visit www.exelixis.com, follow @ExelixisInc on Twitter or like Exelixis, Inc.on Facebook.

SOURCE: Exelixis

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