Ruige Pharmaceutical's new generation of CDK2/4/6 small molecule inhibitors received clinical approval in the U.S.

Recently, Regal Pharmaceuticals announced that it has obtained the approval of the U.
S.
Food and Drug Administration (FDA) to conduct clinical studies of a new generation of CDK2/4/6 small molecule inhibitor RGT-419B
.
RGT-419B is a new generation of CDK2/4/6 small molecule inhibitor with optimized kinase activity profile
.
It is expected to improve the safety of currently approved CDK4/6 inhibitors and overcome resistance to these inhibitors.
These inhibitors are used in combination with endocrine therapy to treat premenopausal/postmenopausal hormone receptor positive (HR+ ), human epidermal growth factor receptor 2 negative (HER2-) advanced or metastatic breast cancer patients
.
In cell model experiments, RGT-419B showed single-drug activity, and compared with abemaciclib and palbociclib, it had a greater inhibitory effect on the growth of ER+ tumor cells
.
In ER+ breast cancer cells resistant to currently approved CDK4/6 inhibitors, RGT-419B showed complete inhibition of cancer cell proliferation
.
In these experiments, when RGT-419B is used in combination with a selective estrogen receptor degrader or PI3K signaling pathway inhibitor, its inhibitory effect on tumor cells is further enhanced
.
As a single agent and in combination with other approved therapies, RGT-419B will initially be developed to treat HER2-, ER+ breast cancer patients who have primary or acquired resistance to currently approved CDK4/6 inhibitors
.
With the widespread adoption of CDK4/6 inhibitors in clinical practice, refractory and relapsed patients who were previously treated with CDK4/6 inhibitors are becoming a larger and clinically significant unmet medical need
.
The clinical development project of RGT-419B will solve this resistance to CDK4/6 and other hormone receptor modulating therapies, and provide new opportunities for improving the survival and quality of life of patients with advanced breast cancer
.
RGT-419B is the first of many innovative oncology drugs being developed by Regal Pharmaceuticals
.
Founder and CEO Dr.
Qiu Xiayang said: "This milestone marks the successful entry of Regal Pharmaceuticals into the field of tumor treatment
.
We have found the best choice for multiple CDKs through our self-developed AI-assisted new drug development CARD platform.
, Successfully promoted innovative drugs to enter the clinical development stage in the United States
.
At the same time, we are very excited that this opportunity can bring new and differentiated treatment options to many breast cancer patients around the world
.
"