On December 18, 2019 Zentalis Pharmaceuticals (the "Company" or "Zentalis"), a clinical-stage biopharmaceutical company focused on developing clinically differentiated, novel small molecule therapeutics that target fundamental pathways in cancer, reported that the U.S. Food and Drug Administration (FDA) has previously cleared its Investigational New Drug (IND) application for its third oncology drug candidate, ZN-c3, and that it has dosed the first patient in a Phase 1/2 clinical trial evaluating ZN-c3 in patients with advanced solid tumors (Press release, Zentalis Pharmaceuticals, DEC 18, 2019, View Source [SID1234552480]).
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The Company is developing ZN-c3, an oral small molecule DNA Damage Response (DDR) drug candidate targeting WEE1 in cancer settings. WEE1 is a protein tyrosine kinase that regulates the cell cycle by serving as a checkpoint preventing DNA replication in the presence of DNA damage. The inhibition of WEE1 aims to generate sufficient DNA damage in cancer cells to cause them to undergo a programmed cell death called apoptosis, thereby preventing tumor growth. The Company has applied its medicinal chemistry expertise to design and synthesize its oral, small molecule compound, ZN-c3, with a potentially best-in-class product profile, including good solubility, selectivity and pharmacokinetic properties. We believe these characteristics will provide for a differentiated drug product to help fight cancer, if ZN-c3 is approved.
There is currently no FDA-approved WEE1 inhibitor. The Company is evaluating the potential of ZN-c3 in a Phase 1/2 clinical trial as monotherapy and in combination with an FDA-approved PARP inhibitor. As of December 16, 2019, the Company has enrolled two patients in this clinical trial. The Company expects to report preliminary data from this clinical trial in 2021.
"We are excited about targeting WEE1 because of its potential for potent anti-tumor activity across multiple cancer types," said Dr. Kevin Bunker, Chief Operating Officer at Zentalis Pharmaceuticals. "ZN-c3 is an internally developed drug candidate that was designed to be a best-in-class molecule with optimized selectivity, great oral bioavailability, and tolerability. We believe these characteristics will provide significant clinical benefit for cancer patients."