Cothera Bioscience Announces First Patient Dosed in Global Phase II Trial of PC-002 for Relapsed/Refractory High-Grade B-Cell Lymphoma and Burkitt Lymphoma

Cothera Bioscience, the parent company of ZhiKangBoYao, announced that PC-002, its first-in-class drug targeting the Myc protein, has completed the first dose administration in the inaugural patient. This trial is a global, multicenter, single-arm, monotherapy, confirmatory Phase II clinical study targeting patients with high-grade B-cell lymphoma and Burkitt lymphoma who are refractory or have relapsed.

Myc proteins are overexpressed in more than 50% of tumors, making them one of the most important “undruggable” oncology targets. PC-002 targets the degradation of Myc family proteins through a unique mechanism of action (MOA). By inhibiting deubiquitinating enzyme (DUB) activity, it increases the level of ubiquitination on the surface of intracellular Myc family proteins, thereby promoting protein degradation, shortening protein half-life, and selectively inducing apoptosis in Myc-dependent tumor cells. Consequently, PC-002 holds promise as a blockbuster therapeutic for various cancers. Additionally, an article by Kesarui Biotech elucidating the mechanism of action of PC-002 has been published in the European Journal of Pharmaceutical Sciences.¹。

Dr. Wu Yue, Co-founder and CEO of Coser Bio, commented, “We are delighted to have administered the first dose in this pivotal proof-of-concept trial. Deubiquitinases represent a novel class of drug targets with significant potential in the development of new therapies for cancer and inflammatory diseases. PC-002 is currently the most advanced deubiquitinase inhibitor in clinical development worldwide. It works by accelerating the degradation of the Myc protein, thereby inducing apoptosis in tumor cells. High-grade lymphomas, including Burkitt lymphoma, are highly dependent on the Myc protein. These are aggressive, life-threatening malignancies that currently lack effective treatment options. We look forward to validating the efficacy of PC-002 in treating these lymphomas through this clinical trial, providing new strategies to improve patient outcomes, and achieving breakthroughs in the development of therapeutics targeting Myc-driven tumors.”

Kaiserui Biologics is a clinical-stage biotechnology company developing therapies for oncology targets with high unmet medical needs that were previously considered undruggable. The company’s competitive advantage lies in its clinically validated translational medicine platform, which leverages synthetic lethality and protein degradation pathways to treat cancer.

In terms of the R&D pipeline, PC-002 is a first-in-class small-molecule drug targeting Myc-mutant tumors. Global multicenter Phase 2 clinical trials for high-grade B-cell lymphoma (including Burkitt lymphoma) are currently underway in China, the United States, and South Korea. Additionally, the U.S. FDA has approved the initiation of global multicenter Phase 2 clinical trials for neuroendocrine prostate cancer (NEPC). The second compound is zotiraciclib (ZTR/TG02). ZTR is a highly potent oral CDK9 inhibitor capable of crossing the blood-brain barrier and degrading proteins encoded by short-half-life, anti-apoptotic oncogenes such as Mcl-1 and Myc. This compound is being developed for the treatment of high-grade glioma (HGG) and diffuse intrinsic pontine glioma (DIPG). ZTR has successfully completed a Phase 1b clinical trial sponsored and conducted by the U.S. National Cancer Institute (NCI) and is poised to launch an international multicenter Phase 2 clinical trial.

Kaiserui Bio's competitive advantage lies in its independently developed i-CR^®By leveraging a technological platform that integrates conditional reprogramming for primary tumor cell culture with high-content drug screening systems, we can efficiently and unbiasedly expand patient-derived primary tumor cells in vitro while preserving tumor heterogeneity. Furthermore, by utilizing these patient-derived primary tumor cells for high-efficiency in vitro drug screening via the high-content screening system, this approach is better suited for personalized medicine and new drug development for clinical patients. Through collaborations with leading oncology medical centers, the company has successfully conducted prospective clinical trials, achieving i-CR^®This system can effectively predict the actual clinical efficacy of drugs, thereby holding promise for substantially improving the efficiency and clinical success rate of novel anti-tumor drug development. The experimental results have been published in an international journal (Transl Oncol. 2021 Jan;14(1):100935).

For more information about Kesarui Biotech, please visit the official website:www.cotherabio.com

1. Li et al. YM155 Inhibits Neuroblastoma Growth through Degradation of MYCN: A New Role as a USP7 Inhibitor, European Journal of Pharmaceutical Sciences (2022) doi:https://doi.org/10.1016/j.ejps.2022.106343