Zentalis Pharmaceuticals: FDA Lifts Partial Hold on Azenosertib Studies

Zentalis Pharmaceuticals Announces FDA Clears Hold on Azenosertib Clinical Trials

San Diego, Sept. 16, 2024 – Zentalis Pharmaceuticals, Inc., a clinical-stage biopharmaceutical company focused on developing small molecule therapeutics targeting cancer, has announced that the U.S. Food and Drug Administration (FDA) has lifted the partial clinical hold on studies of azenosertib. Azenosertib is a novel, selective, and orally administered inhibitor of WEE1. This clearance allows Zentalis to resume patient enrollment in all ongoing clinical trials for azenosertib without any modifications to the current clinical development plan.

According to Kimberly Blackwell, M.D., Chief Executive Officer of Zentalis, the company is thankful for the FDA's collaborative approach and thorough review of their comprehensive safety data related to the azenosertib program. The lifting of the hold has reinforced the company's confidence in the therapeutic potential of azenosertib, especially in addressing unmet needs in treating gynecologic malignancies.

Zentalis has announced plans to present data from azenosertib monotherapy trials and provide further updates on its clinical development later in the year. The company is on schedule to meet all previously disclosed data timelines for the remainder of 2024.

Azenosertib, currently being tested in ovarian cancer and other tumor types, is a pioneering inhibitor of WEE1. WEE1 is a key regulator of cell cycle checkpoints, preventing the replication of cells with damaged DNA. By inhibiting WEE1, azenosertib facilitates cell cycle progression despite high DNA damage levels, leading to mitotic catastrophe and the subsequent death of cancer cells.

Zentalis Pharmaceuticals is dedicated to creating and developing unique small molecule treatments that target fundamental biological pathways in cancer. The company's lead product candidate, azenosertib (ZN-c3), is considered a potential first-in-class and best-in-class WEE1 inhibitor for advanced solid tumors. Azenosertib is being tested both as a standalone treatment and in combination with other chemotherapy agents across multiple clinical trials. It has shown to be well tolerated and effective against various tumor types.

The company's research in the azenosertib program also includes exploring enrichment strategies for high genomic instability tumors, such as Cyclin E1 positive tumors, homologous recombination deficient tumors, and those with oncogenic driver mutations. Zentalis leverages its expertise in cancer biology and medicinal chemistry to advance research on protein degraders further. The company operates out of San Diego.

Zentalis Pharmaceuticals remains committed to developing innovative therapies that can significantly impact cancer treatment, leveraging their deep scientific expertise and robust clinical data to push the boundaries of cancer therapeutics.