Zentalis Pharmaceuticals, Inc. (NASDAQ:ZNTL), a clinical-stage biopharmaceutical company focused on discovering and developing small molecule therapeutics targeting fundamental biological pathways of cancers, today announced the publication of the discovery of ZN-c3, the Company’s highly potent and selective WEE1 inhibitor candidate, in the Journal of Medicinal Chemistry.
The inhibition of WEE1, a key regulator of the cell cycle, is a clinically validated approach for cancer treatment. The paper reviews Zentalis’ objectives in designing ZN-c3 as a potentially safer and more selective WEE1 inhibitor, overcoming limitations seen with other WEE1 inhibitors. ZN-c3 is currently being evaluated in numerous trials as both a monotherapy and in combination, and the Company recently announced positive clinical results in June. In addition, Zentalis has identified potential accelerated approval paths for ZN-c3 in both uterine serous carcinoma and a biomarker-driven setting.
“For the past decade, WEE1 has been a target of interest in the oncology treatment landscape. While the WEE1 inhibitor class has demonstrated promising clinical benefits, poor kinase selectivity and tolerability issues have potentially limited the existing candidates’ effectiveness in patients,” commented Dr. Anthony Sun, Chairman and Chief Executive Officer of Zentalis. “The Zentalis team recognized the promise of inhibiting this DNA damage response protein and set out to create a differentiated candidate with a clean selectivity profile, improving tolerability and enabling a continuous dosing regimen for better efficacy. We believe our pioneering research and clinical results reported to date provide strong evidence that ZN-c3’s profile is best-in-class, and we look forward to exploring this candidate’s therapeutic potential across a broad range of solid tumors in ongoing and planned trials.”
To view the publication, please visit the “Supporting Publications” page on Zentalis’ website at www.zentalis.com.