Regor Therapeutics Announces FDA Clearance for Phase I Clinical Trial of Next-Generation CDK2/4/6 Inhibitor RGT-419B in HR+/HER2- Breast Cancer

Recently, Regor Therapeutics announced that it has received approval from the U.S. Food and Drug Administration (FDA) to initiate clinical research on RGT-419B, a next-generation small molecule inhibitor of CDK2/4/6.

RGT-419B is a next-generation small molecule inhibitor of CDK2/4/6 with an optimized kinase activity profile. It has the potential to improve the safety of currently approved CDK4/6 inhibitors and overcome resistance to these inhibitors, which are used in combination with endocrine therapy to treat premenopausal/postmenopausal patients with hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer.

In cellular model experiments, RGT-419B demonstrated single-agent activity, with a greater inhibitory effect on ER+ tumor cell growth compared to abemaciclib and palbociclib. In ER+ breast cancer cells resistant to currently approved CDK4/6 inhibitors, RGT-419B showed complete inhibition of cancer cell proliferation. In these experiments, the inhibitory effect of RGT-419B on tumor cells was further enhanced when combined with selective estrogen receptor degraders or PI3K signaling pathway inhibitors.

RGT-419B will initially be developed for the treatment of HER2-, ER+ breast cancer patients with primary or acquired resistance to currently approved CDK4/6 inhibitors, both as a single agent and in combination with other approved therapies. As CDK4/6 inhibitors have been widely adopted in clinical practice, refractory and relapsed patients previously treated with CDK4/6 inhibitors are becoming a larger, clinically significant unmet medical need. The clinical development program of RGT-419B will address this resistance to CDK4/6 and other hormone receptor modulating therapies, offering new opportunities to improve survival and quality of life for patients with advanced breast cancer.

RGT-419B is the first of many innovative oncology drugs being developed by Regor Therapeutics.Founder and CEO Dr. Xiaoyang Qiu said"This milestone marks Regor Therapeutics' successful entry into the field of oncology treatment. Using our self-developed AI-assisted drug discovery CARD platform, we have identified the optimal selectivity for multiple CDKs, successfully advancing an innovative drug into clinical development in the United States. We are also very excited about this opportunity to bring a new differentiated treatment option to breast cancer patients worldwide."

Editor: Liuli

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